- 1. Cyclopia maculata and Cyclopia subternata (honeybush tea) inhibits adipogenesis in 3T3-L1 pre-adipocytes.
The stems, leaves and flowers of Cyclopia have been consumed as a herbal tea 'honeybush tea' to treat various medical ailments since the 19th century. Plant polyphenols are reported to inhibit adipogenesis in cell and animal models of obesity. The aim of this study was to assess the effect of hot water extracts of two Cyclopia species, C. maculata and C. subternata on obesity in an in vitro model. The total polyphenol content of unfermented C. subternata, unfermented C. maculata and fermented C. maculata extracts was 25.6, 22.4 and 10.8g GAE/100g, respectively. The major compounds present in the extracts were: the flavonoid, phloretin-3',5'-di-C-glucoside in C. subternata, the xanthone, mangiferin in unfermented C. maculata and the flavanone, hesperidin in fermented C. maculata. All of the plant extracts inhibited intracellular triglyceride and fat accumulation, and decreased PPARγ2 expression. The higher concentrations of unfermented C. maculata (800 and 1600μg/ml) and C. subternata (1600μg/ml) were cytotoxic in terms of decreased mitochondrial dehydrogenase activity. Both fermented and unfermented C. maculata, at concentrations greater than 100μg/ml, decreased cellular ATP content. Cyclopia maculata and C. subternata inhibit adipogenesis in vitro, suggesting their potential as anti-obesity agents....(more)
Dudhia Z, et al. Phytomedicine 2013 Mar 15;20(5):401-8.
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- 2. Functions of monocyte chemotactic protein-3 in transgenic mice fed a high-fat, high-cholesterol diet.
Monocyte chemotactic protein-3 (MCP-3), a chemokine that is in a superfamily of structurally related small chemotactic cytokines involved in leukocyte trafficking, is regarded as a key factor in atherogenesis. In this study, we examined the changes in atherogenic parameters including hepatic lipid accumulation and oxidative balance in MCP- 3-overexpressing transgenic mice (MCP-3 mice) under atherogenic conditions. To induce an extreme atherogenic condition, mice were fed a high-fat, high-cholesterol (HFHC) diet for 12 weeks. The body weight and food intake were not changed by MCP-3 overexpression in the aorta. On a HFHC diet, the MCP-3 mice had higher plasma levels of total cholesterol and a higher atherogenic index compared with wild-type mice, although there were no differences in the plasma HDL-cholesterol and triglyceride levels. Furthermore, an increase in lipid accumulation was observed in the aortas as well as the livers of the HFHC diet-fed MCP-3 mice compared with wild-type mice. The activities of antioxidant enzymes increased in the livers of the HFHC diet-fed MCP-3 mice, whereas supplementation with antioxidants, naringin and hesperidin, reversed the activities of the hepatic antioxidant enzymes in HFHC diet-fed MCP-3 mice, indicating that there might be more oxidative damage to the tissues in the HFHC diet-fed MCP-3 mice leading to progression towards atherosclerosis and hepatic steatosis. Microarray analyses of the aorta revealed atherosclerosis-, PPARs-, lipoprotein receptor, and apolipoprotein-related genes that were affected by the HFHC diet in MCP-3 mice. These findings suggest that aortic MCP-3 overexpression may contribute to the development of atherosclerosis and hepatic steatosis under atherogenic conditions....(more)
An SJ, et al. J Microbiol Biotechnol 2013 Mar;23(3):405-13.
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- 3. Protective Effects of Hesperidin Against Amyloid-β (Aβ) Induced Neurotoxicity Through the Voltage Dependent Anion Channel 1 (VDAC1)-Mediated Mitochondrial Apoptotic Pathway in PC12 Cells.
Amyloid-β (Aβ) is known to exert cytotoxic effects by inducing mitochondrial dysfunction. Additionally, the mitochondrial voltage-dependent anion channel 1 (VDAC1), which is involved in the release of apoptotic proteins with possible relevance in Alzheimer's disease (AD) neuropathology, plays an important role in maintaining mitochondrial function and integrity. However, the application of therapeutic drugs, especially natural products in (AD) therapy via VDAC1-regulated mitochondrial apoptotic pathway has not aroused extensive attention. In the present study, we investigated neuroprotective effects of hesperidin, a bioactive flavonoid compound, on Aβ25-35-induced neurotoxicity in PC12 cells and also examined the potential cellular signalling mechanism. Our results showed that treatment with hesperidin significantly inhibited Aβ25-35-induced apoptosis by reversing Aβ-induced mitochondrial dysfunction, including the mitochondrial permeability transition pore opening, intracellular free calcium increase and reactive oxygen species production. Further study indicated that hesperidin can increase the level of VDAC1 phosphorylation through enhancing the activity of the glycogen synthasekinase-3β and decrease the level of hexokinaseI in mitochondrial, resulting in mitochondrial release of cytochrome c. Furthermore, hesperidin inhibited mitochondria-dependent downstream caspase-mediated apoptotic pathway, such as that involving caspase-9 and caspase-3. These results demonstrate that hesperidin can protect Aβ-induced neurotoxicity via VDAC1-regulated mitochondrial apoptotic pathway, and they raise the possibility that hesperidin could be developed into a clinically valuable treatment for AD and other neuronal degenerative diseases associated with mitochondrial dysfunction....(more)
Wang DM, et al. Neurochem Res 2013 May;38(5):1034-44.
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- 4. Immobilized magnetic beads based multi-target affinity selection coupled with high performance liquid chromatography-mass spectrometry for screening anti-diabetic compounds from a Chinese medicine "Tang-Zhi-Qing".
We developed an approach for screening bioactive compounds from botanical drug using multiple target-immobilized magnetic beads coupled with high performance liquid chromatography-mass spectrometry. This novel approach was called magnetic beads based multi-target affinity selection-mass spectrometry (MT-ASMS). It can enrich and identify different types of ligands from mixture extracts. Multiple targets (maltase, invertase, lipase) were immobilized on the magnetic beads by covalent linkage using 1-(3-dimethyl-aminopropyl)-3-ethyl-carbodiimide (EDC) and N-hydroxysuccinimide (NHS) as reaction reagents, respectively. The properties of enzyme conjugated magnetic beads were characterized using transmission electron microscopy, X-ray diffractometer and vibration sample magnetometer. Several factors including pH, ion strength, incubation time and temperature were optimized using three known ligands (caffeic acid, ferulic acid, and hesperidin). The established MT-ASMS approach was applied to screening for ligands from a Chinese medicine "Tang-Zhi-Qing", which was used to treat type II diabetes in China. Seven bound compounds were identified via liquid chromatography-mass spectrometry (LC/MS). Five active compounds including 2,3,4,6-tetra-O-galloyl-d-glucose, 1,2,3,4-tetra-O-galloyl-d-glucose, 1,2,3,4,6-penta-O-galloyl-d-glucose, quercetin-3-O-β-d-glucuronide and quercetin-3-O-β-d-glucoside were identified and their activities were validated by conventional inhibitory assay. Our findings suggested that the proposed approach is efficient in screening compounds with multiple activities from extracts of botanical drugs....(more)
Tao Y, et al. J Pharm Biomed Anal 2013 May 5;78-79:190-201.
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- 5. Hesperidin protects brain and sciatic nerve tissues against cisplatin-induced oxidative, histological and electromyographical side effects in rats.
In the present study, the beneficial effect of hesperidin (HP), a citrus flavonoid, on cisplatin (CP)-induced neurotoxicity was investigated. A total of 28 rats were equally divided into four groups; the first group was kept as control. In the second and third groups, CP and HP were given at the doses of 7 and 50 mg/kg/day, respectively. In the fourth group, CP and HP were given together at the same doses. The results indicated that although CP caused significant induction of lipid peroxidations and reduction in the antioxidant defense system potency in the brain and sciatic nerve, HP prevented these effects of CP. Besides, CP led to histopathological damage, mainly apoptosis, as well as electromyographical (EMG) changes in sciatic nerve. On the other hand, HP treatment reversed histopathological and EMG effects of CP. In conclusion, CP had severe dose-limiting neurotoxic effects and these effects of CP can be prevented by HP treatment. Thus, it appears that coadministration of HP with CP may be a useful approach to attenuate the negative effects of CP on the nervous system....(more)
Kamisli S, et al. Toxicol Ind Health 2013 Apr 3.
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- 6. Enzymatic modification enhances the protective activity of citrus flavonoids against alcohol-induced liver disease.
Alcoholic liver disease (ALD) can be developed by a prolonged or large intake of alcohol in a short period of time. ALD is considered as a leading cause for a liver injury in modern dietary life. This study was aimed to investigate the effects of orally administrated citrus flavonoids (CFs) and their enzymatically modified ones (EM-CFs) to prevent ALD. Hesperidin and narirutin were extracted from peels of Citrus unshiu by ultra-sonication and purified further. These CFs were modified enzymatically through glycosylation and de-rhamnosylation by the actions of cyclodextrin glucanotransferase (CGTase) and hesperidinase, respectively. CFs and EM-CFs were fed to ICR mouse along with ethanol for 8weeks, and changes in lipid contents, lipid peroxidation, GSH, antioxidant enzymes activity and proinflammatory cytokines in hepatic tissues were observed. Administration of CFs and EM-CFs along with alcohol significantly suppressed increases in prognostic parameters of a hepatocellular injury. Especially, EM-CFs fed groups maintained malondialdehyde, GSH levels and catalase activity in hepatic tissues close to those of the normal diet fed group. Abrupt increases in proinflammatory cytokines such as IκB-α, TNF-α, IL-1β and IL-6 in hepatocytes due to a chronic alcohol uptake were significantly suppressed by co-administration of EM-CFs. These results indicate that although the administration of CFs can alleviate ALD through preventing excessive lipid formation, protecting the antioxidant system and suppressing induction of inflammation in hepatocytes, their effectiveness can be further improved by glycosylation and de-rhamnosylation....(more)
Park HY, et al. Food Chem 2013 Aug 15;139(1-4):231-40.
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- 7. Quality of life improvement in Latin American patients suffering from chronic venous disorder using a combination of Ruscus aculeatus and hesperidin methyl-chalcone and ascorbic acid (quality study).
AIM:
The present study assessed the effect of Ruscus aculeatus, hesperidin methyl-chalcone and ascorbic acid (HMC-AA), in the treatment of chronic venous disorders (CVD) in Latin American patients.
METHODS:
This study is an observational, single arm, multicentric and prospective trial. Patients suffering from CVD and belonging to C0s-C3 Clinical Etiological Anatomical and Physiopathological (CEAP) classes were included. Patient profiles, risk factors, clinical symptomatology and quality of life (QoL) assessed by SF-12 and CIVIQ questionnaires were evaluated at inclusion and after 12-week treatment.
RESULTS:
The main factors influencing the previous management of patients were age, gender, body mass index (BMI), familial history, physical activity, exposure to heat, heavy loads lifting, profession and clinical characteristics. All clinical symptoms significantly improved with treatment and, as BMI and CEAP classes increased. Ankle circumferences decreased over time, correlating with BMI and CEAP classes. The physical and psychological dimensions of the SF-12 score significantly increased over time and improved within each CEAP class. The CIVIQ score significantly improved over time, correlating with age and CEAP classes.
CONCLUSION:
A 12-week treatment with Ruscus aculeatus HMC-AA showed a significant decrease in the clinical symptoms and a significant improvement in the QoL of patients with CVD....(more)
Guex JJ, et al. Int Angiol 2010 Dec;29(6):525-32.
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- 8. Assessment of quality of life in Mexican patients suffering from chronic venous disorder - impact of oral Ruscus aculeatus-hesperidin-methyl-chalcone-ascorbic acid treatment - 'QUALITY Study'.
OBJECTIVES:
The present study assessed the effect of Ruscus aculeatus-hesperidin-methyl-chalcone-ascorbic acid (HMC-AA) on the quality of life (QoL) of patients suffering from chronic venous disorders (CVDs).
METHODS:
An observational, multicentre and prospective study was performed with 917 Mexican patients suffering from CVD. Patients were treated with R. aculeatus-HMC-AA. After 12 weeks of treatment, the physicians then assessed the patients' symptoms and QoL using Short Form (SF-12) and Chronic Venous Insufficiency (CIVIQ) auto-questionnaires.
RESULTS:
Patients were mainly women (86.7%), overweight or obese (72.7%) or C2 (39.3%)-C3 (27.6%). All symptoms and ankle circumferences significantly improved over time, with increasing clinical, aetiological, anatomical and pathophysiological (CEAP) classes and body mass index (BMI) (P < 0.001). Concerning QoL, all dimensions of the SF-12 score significantly improved over time (P < 0.001). Moreover, the CIVIQ scores significantly improved (P < 0.001) with increasing BMI (P < 0.002) and CEAP classes (P < 0.05).
CONCLUSION:
R. aculeatus-HMC-AA significantly improved the symptoms and QoL of CVD patients....(more)
Guex JJ, et al. Phlebology 2009 Aug;24(4):157-65.
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- 9. Ni speciation in tea infusions by monolithic chromatography--ICP-MS and Q-TOF-MS.
For humans, Ni is not considered to be an essential trace element. Its compounds, at levels present in foodstuffs and drinks, are generally considered to be safe for consumption, but for individuals who already suffer from contact allergy to Ni and may be subject to develop systemic reactions from its dietary ingestion, dietary exposure to Ni must be kept under control. Being the second most popular beverage, tea is a potential source of dietary Ni. Present knowledge on its speciation in tea infusions is poor. Therefore, complete speciation analysis, consisting of separation by liquid chromatography using a weak CIM DEAE-1 monolithic column, "on-line" detection by inductively coupled plasma mass spectrometry (ICP-MS) and "off-line" identification of ligands by hybrid quadrupole time-of-flight mass spectrometry (Q-TOF MS), was implemented for the first time to study Ni speciation in tea infusions. Total concentrations of Ni in dry leaves of white, green, oolong and black tea (Camellia sinensis) and flowers of herbal chamomile (Matricaria chamomilla) and hibiscus (Hibiscus sabdariffa) tea were determined after microwave digestion by ICP-MS. They lay between 1.21 and 14.4 mg kg(-1). Good agreement between the determined and the certified values of the Ni content in the standard reference material SRM 1573a tomato leaves confirmed the accuracy of the total Ni determination. During the infusion process, up to 85 % of Ni was extracted from tea leaves or flowers. Separation of Ni species was completed in 10 min by applying aqueous linear gradient elution with 0.6 mol L(-1) NH(4)NO(3). Ni was found to be present in the chromatographic fraction in which quinic acid was identified by Q-TOF in all the tea infusions analysed, which had pH values between 5.6 and 6.0. The only exception was the infusion of hibiscus tea with a pH of 2.7, where results of speciation analysis showed that Ni is present in its divalent ionic form....(more)
Š?an?ar J, et al. Anal Bioanal Chem 2013 Feb;405(6):2041-51.
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- 10. Biosorption of arsenic from aqueous solution using dye waste.
The purpose of this study is to examine on removal of arsenic from water by biosorption through potential application of herbal dye wastes. Four different flower dye residues (after extraction of natural dye) viz. Hibiscus rosasinensis, Rosa rosa, Tagetes erecta, and Canna indica were utilized successfully for the removal of arsenic from aqueous solution. Batch studies were carried out for various parameters viz. pH, sorbent dose, contact time, initial metal ion concentration, and temperature. Data were utilized for isothermal, kinetic, and thermodynamic studies. Scanning electron microscopy (SEM), energy-dispersive x-ray spectroscopy (EDAX), and Fourier transform infrared (FTIR) analyses of biomass were performed. The results showed that 1 g/100 ml for 5.0-5.5 h contact time at pH 6.0-7.5 with agitation rate 150 rpm provided 98, 96, 92, and 85 % maximum absorption of arsenic by R. rosa, H. rosasinensis, T. erecta, and C. indica, respectively, at initial concentration of 500 ppb. Data followed Langmuir isotherm showing sorption to be monolayer on heterogeneous surface of biosorbent. Negative values of ΔG° indicated spontaneous nature, whereas ΔH° indicates exothermic nature of system followed by pseudo-first-order adsorption kinetics. FTIR results showed apparent changes in functional group regions after metal chelation. SEM and EDAX analyses showed the changes in surface morphology of all test biosorbents. Herbal dye wastes, used as biosorbent, exhibited significant (85-98 %) removal of arsenic from aqueous solution. Hence, these biosorbents are cost-effective, easily available, eco-friendly, and comparatively more effective than other biosorbents already in use. These may be used to remove arsenic and other toxic metals from water....(more)
Nigam S, et al. Environ Sci Pollut Res Int 2013 Feb;20(2):1161-72.
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- 11. In vitro antibacterial activity of Hibiscus rosa-sinensis flower extract against human pathogens.
OBJECTIVE:
To access the in vitro antibacterial activity of Hibiscus rosa-sinensis (H. rosa- sinensis) flower extract against human pathogens.
METHODS:
Antibacterial activity was evaluated by using disc and agar diffusion methods. The protein was run through poly acrylmide gel electrophoresis to view their protein profile.
RESULTS:
The results showed that the cold extraction illustrates a maximum zone of inhibition against Bacillus subtillis (B. subtillis), Escherichia coli (E. coli) viz., (17.00 ± 2.91), (14.50 ± 1.71) mm, followed by hot extraction against, E. coli, Salmonella sp. as (11.66 ± 3.14), (10.60 ± 3.09) mm. In methanol extraction showed a highest zone of inhibition recorded against B. subtillis, E. coli as (18.86 ± 0.18), (18.00 ± 1.63) mm pursued by ethanol extraction showed utmost zone of inhibition recorded against Salmonella sp. at (20.40 ± 1.54) mm. The crude protein from flower showed a maximum inhibitory zone observed against Salmonella sp., E. coli viz., (16.55 ± 1.16), (14.30 ± 2.86) mm. The flower material can be taken as an alternative source of antibacterial agent against the human pathogens.
CONCLUSIONS:
The extracts of the H. rosa-sinensis are proved to have potential antibacterial activity, further studies are highly need for the drug development....(more)
Ruban P, et al. Asian Pac J Trop Biomed 2012 May;2(5):399-403.
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- 12. Evaluation of the wound-healing activity of Hibiscus rosa sinensis L (Malvaceae) in Wistar albino rats.
OBJECTIVE:
To investigate the wound-healing potency of the ethanolic extract of the flowers of Hibiscus rosa sinensis.
MATERIALS AND METHODS:
The wound-healing activity of H. rosa sinensis (5 and 10% w/w) on Wistar albino rats was studied using three different models viz., excision, incision and dead space wound. The parameters studied were breaking strength in incision model, granulation tissue dry weight, breaking strength and collagen content in dead space wound model, percentage of wound contraction and period of epithelization in excision wound model. The granulation tissue formed on days 4, 8, 12, and 16 (post-wound) was used to estimate total collagen, hexosamine, protein, DNA and uronic acid. Data were analyzed by Analysis of Variance (ANOVA) test. P<0.05 was considered statistically significant.
RESULTS:
The extract increased cellular proliferation and collagen synthesis at the wound site, as evidenced by increase in DNA, total protein and total collagen content of granulation tissues. The extract-treated wounds were found to heal much faster as indicated by improved rates of epithelialization and wound contraction. The extract of H. rosa sinensis significantly (P<0.001) increased the wound-breaking strength in the incision wound model compared to controls. The extract-treated wounds were found to epithelialize faster, and the rate of wound contraction was significantly (P<0.001) increased as compared to control wounds. Wet and dry granulation tissue weights in a dead space wound model increased significantly (P<0.001). There was a significant increase in wound closure rate, tensile strength, dry granuloma weight, wet granuloma weight and decrease in epithelization period in H. rosa sinensis-treated group as compared to control and standard drug-treated groups.
CONCLUSION:
The ethanolic extract of H. rosa sinensis had greater wound-healing activity than the nitrofurazone ointment....(more)
Bhaskar A, et al. Indian J Pharmacol 2012 Nov-Dec;44(6):694-8.
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- 13. Antidepressant-like activity of anthocyanidins from Hibiscus rosa-sinensis flowers in tail suspension test and forced swim test.
AIM:
Flowers of Hibiscus rosa-sinensis Linn (Malvaceae) popularly known as "China-rose flowers" contain flavonoids. Flavonoids have been found to have antidepressant activity. The aim of the present study is to evaluate the antidepressant activity of flavonoids in H. rosa-sinensis flowers with possible involvement of monoamines.
MATERIALS AND METHODS:
Anti-depressant activity of methanol extract containing anthocyanins (MHR) (30 and 100 mg/kg) and anthocyanidins (AHR) (30 and 100 mg/ kg) of H. rosa-sinensis flowers were evaluated in mice using behavioral tests such as tail suspension test (TST) and forced swim test (FST). The mechanism of action involved in antidepressant activity was investigated by observing the effect of extract after pre-treatment with low dose haloperidol, prazosin and para-chlorophenylalanine (p-CPA).
RESULTS:
Present study exhibited significant decrease in immobility time in TST and FST, similar to that of imipramine (10 mg/kg, i.p.) which served as a positive control. The extract significantly attenuated the duration of immobility induced by Haloperidol (50 μg/ kg, i.p., a classical D(2)-like dopamine receptor antagonist), Prazosin (62.5 μg/kg, i.p., an α(1)-adrenoceptor antagonist) and p-chlorophenylalanine (100 mg/kg, i.p., × 3 days; an inhibitor of serotonin synthesis) in both TST and FST.
CONCLUSION:
It can be concluded that MHR and AHR possess potential antidepressant activity (through dopaminergic, noradrenergic and serotonergic mechanisms) and has therapeutic potential in the treatment of CNS disorders and provides evidence at least at preclinical levels....(more)
Shewale PB, et al. Indian J Pharmacol 2012 Jul-Aug;44(4):454-7.
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- 14. Pichia bruneiensis sp. nov., a biofilm-producing dimorphic yeast species isolated from flowers in Borneo.
Taxonomic analysis of five yeast strains isolated from Hibiscus flowers in Brunei (Borneo) is described. The strains represent a dimorphic, biofilm-producing, anamorphic budding yeast species for which the name Pichia bruneiensis is proposed. P. bruneiensis alternates between yeast and pseudohyphal modes of growth. The pseudohyphae form biofilms on the surface of liquid media and penetrate into solid substrates. The sequences of the D1/D2 domains of the large subunit rRNA genes, the internal transcribed spacer (ITS) regions and the 18S rRNA genes were identical in the five strains and indicated a close phylogenetic relationship with teleomorph species of the genus Pichia. In a phylogenetic analysis of these sequences, the closest relative of the new species was Pichia fermentans (6% nucleotide substitutions and indels in the D1/D2 domain). The type strain is 11-485(T) and has been deposited in the Centralbureau voor Schimmelcultures (Utrecht, the Netherlands) as CBS 12611(T), the National Collection of Agricultural and Industrial Micro-organisms (Budapest, Hungary) as NCAIM Y.02019(T) and the Culture Collection of Yeasts (Bratislava, Slovakia) as CCY 29-189-1(T). Mycobank no. MB800537....(more)
Sipiczki M. Int J Syst Evol Microbiol 2012 Dec;62(Pt 12):3099-104.
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- 15. Practical considerations for the use of pollen δ13C value as a paleoclimate indicator.
RATIONALE:
Workers have shown a correlation between temperature and the pollen δ(13)C value, and therefore suggested using pollen δ(13)C values to reconstruct paleotemperature. To evaluate the potential for pollen δ(13)C values to be used as a paleotemperature proxy, it is essential to quantify the variability in pollen δ(13)C values and to evaluate the effect of temperature on pollen δ(13)C values, in isolation, under controlled environmental conditions.
METHODS:
Pollen was isolated from 146 Hibiscus flowers from 26 plants within a single climate environment to evaluate isotopic variability in pollen δ(13)C values. The nearest leaf (n = 82) and flower phloem (n = 30) were also sampled to measure the δ(13)C variability in carbon providing the raw material for new growth. To evaluate the correlation between temperature and pollen δ(13)C values, we isolated pollen from 89 Brassica rapa plants grown in controlled growth chambers with temperatures ranging from 17 to 32°C.
RESULTS:
The range in pollen δ(13)C values collected from different flowers on the same Hibiscus plant was large (average = 1.6‰), and could be as much as 3.2‰. This amount of variability was similar to that seen between flower-adjacent leaves, and phloem extracted from styles of individual flowers. In controlled growth chamber experiments, we saw no correlation between temperature and the pollen (R(2) = 0.005) or leaf (R(2) = 0.10) δ(13)C values.
CONCLUSIONS:
We measured large variability in pollen δ(13)C values. When temperature was isolated from other environmental parameters, temperature did not correlate with the pollen δ(13)C value. These results complicate the supposed relationship between temperature and pollen δ(13)C values and caution against using nanogram isotope analytical techniques for characterizing whole-plant individuals.
Copyright © 2012 John Wiley & Sons, Ltd....(more)
King DC, et al. Rapid Commun Mass Spectrom 2012 Sep 30;26(18):2165-72.
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- 16. Long-term ingestion of Hibiscus sabdariffa calyx extract enhances myocardial capillarization in the spontaneously hypertensive rat.
The effects of Hibiscus sabdariffa (HS) in lowering blood pressure in human and animal hypertension have been documented. This study investigated the effect of the water extract of the dried calyx of HS and Hibiscus anthocyanins (HAs) on left ventricular myocardial capillary length and surface area in spontaneously hypertensive rats (SHRs). Twelve-week-old male SHRs were divided into eight groups (six rats in each group). Three groups were given three doses; 10%, 15% and 20% of the water extract of HS in lieu of drinking water for 10 consecutive weeks (HS10, HS15 and HS20) with one group kept as control (C). Another three groups were given three doses of the HAs orally at doses of 50, 100 and 200 mg/kg for five consecutive days with one group kept as a control (C). Systolic (SBP) and diastolic (DBP) blood pressures, as well as heart rate (HR), were measured weekly. After the experimental protocols, the left ventricles (LV) of all rats were obtained. Capillary surface area density and length density were determined by unbiased sterological methods on 3 μm LV tissue samples from perfusion-fixed hearts. HS ingestion significantly reduced SBP, DBP and LV mass in a dose-dependent fashion but did not affect the HR. HS significantly increased surface area and length density of myocardial capillaries by 59%, 65% and 86%, and length density by 57%, 77% and 57%, respectively. Myocyte nuclear volume was significantly decreased in HS-treated rats. There was a decrease (although insignificant) in SBP and DBP with HA ingestion compared with controls. These changes suggest that the observed beneficial effect of HS on high BP in SHRs could be mediated through a reduction in the diffusion distance between capillaries and myocytes, as well as new vessel formation. It is proposed that these effects might be beneficial in restoring myocyte normal nutritional status compromised by the hypertrophic state of hypertension....(more)
Inuwa I, et al. Exp Biol Med (Maywood) 2012 May 1;237(5):563-9.
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- 17. Genetic control of white flower color in scarlet rosemallow (Hibiscus coccineus Walter).
Scarlet rosemallow (Hibiscus coccineus Walter) is a diploid, perennial, erect, and woody shrub. The species is a desirable inclusion in home landscapes because it is a native plant with attractive flowers and unusual foliage. The objective of these experiments was to determine the number of loci, number of alleles, and gene action controlling flower color (red vs. white) in scarlet rosemallow. Three white-flowered and 1 red-flowered parental lines were used to create S(1) and F(1) populations, which were self-pollinated or backcrossed to generate S(2), F(2), and BC(1) populations. Evaluation of these generations showed that flower color in these populations was controlled by a single diallelic locus with red flower color completely dominant to white. I propose that this locus be named "white flower" with alleles W and w....(more)
Gettys LA. J Hered 2012 Jul;103(4):594-7.
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- 18. Antidepressant-like effects of methanol extract of Hibiscus tiliaceus flowers in mice.
BACKGROUND:
Hibiscus tiliaceus L. (Malvaceae) is used in postpartum disorders. Our purpose was to examine the antidepressant, anxiolytic and sedative actions of the methanol extract of H. tiliaceus flowers using animal models.
METHODS:
Adult male Swiss albino mice were treated with saline, standard drugs or methanol extract of H. tiliaceus and then subjected to behavioral tests. The forced swimming and tail suspension tests were used as predictive animal models of antidepressant activity, where the time of immobility was considered. The animals were submitted to the elevated plus-maze and ketamine-induced sleeping time to assess anxiolytic and sedative activities, respectively.
RESULTS:
Methanol extract of H. tiliaceus significantly decreased the duration of immobility in both animal models of antidepressant activity, forced swimming and tail suspension tests. This extract did not potentiate the effect of ketamine-induced hypnosis, as determined by the time to onset and duration of sleeping time.
CONCLUSION:
Our results indicate an antidepressant-like profile of action for the extract of Hibiscus tiliaceus without sedative side effect....(more)
Vanzella C, et al. BMC Complement Altern Med 2012 Apr 12;12:41.
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- 19. Aromatic glycosides from the flower buds of Lonicera japonica.
Six new glycosides (1-6) have been isolated from the flower buds of Lonicera japonica. Their structures including the absolute configurations were determined by spectroscopic and chemical methods as ( - )-2-hydroxy-5-methoxybenzoic acid 2-O-β-d-(6-O-benzoyl)-glucopyranoside (1), ( - )-4-hydroxy-3,5-dimethoxybenzoic acid 4-O-β-d-(6-O-benzoyl)-glucopyranoside (2), ( - )-(E)-3,5-dimethoxyphenylpropenoic acid 4-O-β-d-(6-O-benzoyl)-glucopyranoside (3), ( - )-(7S,8R)-(4-hydroxyphenylglycerol 9-O-β-d-[6-O-(E)-4-hydroxy-3,5-dimethoxyphenylpropenoyl]-glucopyranoside (4), ( - )-(7S,8R)-(4-hydroxy-3-methoxyphenylglycerol 9-O-β-d-[6-O-(E)-4-hydroxy-3,5-dimethoxyphenylpropenoyl]-glucopyranoside (5), and ( - )-4-hydroxy-3-methoxyphenol β-d-{6-O-[4-O-(7S,8R)-(4-hydroxy-3-methoxyphenylglycerol-8-yl)-3-methoxybenzoyl]}-glucopyranoside (6), respectively....(more)
Wang F, et al. J Asian Nat Prod Res 2013 Apr 24.
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- 20. Purification and partial characterization of polyphenol oxidase from the flower buds of Lonicera japonica Thunb.
The purification and partial enzymology characteristics of polyphenol oxidase from Lonicera japonica (LjPPO) were studied in this paper. The crude enzyme solution was purified in turn by ammonium sulfate, dialysis, and DEAE-cellulose ion-exchange chromatography after preliminary treatments. Purification resulted in 31-fold enrichment and its molecular weight was estimated to be ~49 kDa exhibited on sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE). The pH for optimal conditions of LjPPO was 7.5, and the temperature was 25 °C, in addition, the inhibitive effects of inhibitors were enhanced positively with increasing of the concentration. Moreover, crude enzyme solution showed diphenolase activity toward catechol, l-dopa and chlorogenic acid rather than monophenolase and triphenolase activity, and the best substrate was catechol because of the highest V(max)/K(m) value. However, the oxidation of diphenol related to browning significantly, so the data obtained in this research provided theoretical basis for the prevention of enzymatic browning of L. japonica during processing.
Copyright © 2012 Elsevier Ltd. All rights reserved....(more)
Liu NN, et al. Food Chem 2013 May 1;138(1):478-83.
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- 21. Prophylactic effects of Lonicera japonica extract on dextran sulphate sodium-induced colitis in a mouse model by the inhibition of the Th1/Th17 response.
Inflammatory bowel diseases (IBD) are chronically relapsing inflammatory disorders of the intestine. Although some therapeutic agents, including steroids, are available for the treatment of IBD, these agents have limited use. Therefore, dietary supplements have emerged as possible interventions for IBD. Japanese honeysuckle flower, the flower of Lonicera japonica, is a well-known dietary supplement and has been used to prevent or treat various inflammatory diseases. In the present study, we investigated the effects of L. japonica on experimental murine colitis. Colitis was induced by 5 % dextran sulphate sodium (DSS) in Balb/c mice. The water extract of L. japonica (LJE) at doses of 20, 100 or 500 mg/kg was orally administered to mice twice per day for 7 d. Body weight, colon length and a histological damage score were assessed to determine the effects on colitis. Cytokine profiles were assessed to examine the effects on helper T (Th) cell-related immunological responses. In addition, CD4CD25Foxp3T cells were analysed in vivo and in vitro for investigating the effects on regulatory T (Treg) cells. LJE showed dose-dependent inhibitory effects against colon shortening, weight loss and histological damage. LJE down-regulated IL-1β, TNF-α, interferon-γ, IL-6, IL-12 and IL-17. However, LJE did not show any significant effects on IL-10, IL-23, transforming growth factor-β1 and Treg cell populations. In conclusion, LJE showed protective effects against DSS-induced colitis via the Th1/Th17 pathway and not via Treg cell-related mechanisms....(more)
Park JW, et al. Br J Nutr 2013 Jan 28;109(2):283-92.
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- 22. [Study on the chemical constituents of Lonicera similes].
OBJECTIVE:
To study the chemical constituents of flower buds of Lonicera similes.
METHODS:
The chemical constituents were isolated and purified with macroporous resin, silica gel column chromatography, gel chromatography, ect. The structures were elucidated according to the references combined with the application of spectrum techniques such as 1H-NMR, 13C-NMR ect.
RESULTS:
Nine compounds were isolated and their structures were identified as 5-hydroxyl-7,4'-dimethoxyflavone (I), rutin (II), quercetin (III), amentoflavone (IV), aesculetin (V), beta-sitosterol (VI), 5-hydroxyl-7,3', 4'-trimethoxyflavone (VIII), oleanolic acid (VIII), beta-daucosterin (IX).
CONCLUSION:
Among the nine isolated compounds, compounds I, II, III, IV, V, are flavonoids. Compounds I , IV, V, VII, VIII, IX are isolated from this plant for the first time....(more)
Zheng GY, et al. Zhong Yao Cai 2012 Nov;35(11):1792-5. Chinese.
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- 23. [Clinical observation of treating 62 patients with severe aplastic anemia failing in immunosuppressive therapy by integrative medicine].
OBJECTIVE:
To explore treatment methods for patients with severe aplastic anemia (SAA) failing in immunosuppressive therapy (IST).
METHODS:
Totally 62 SAA patients failing in IST were treated by integrative medicine (IM). The treatment course was divided into three stages: the critical emergency stage, the improvement stage, and the recovery stage. In the critical emergency stage, patients were treated with Lingyang Yigui Decoction (LYD, consisting of 1.2 g antelope horn, 6 g coptis chinensis, 12 g stir-baked Fructus Gardeniae, 30 g rehmannia rhizoma, 50 g lalang grass rhizome, 9 g amur corktree bark, 12 g Cortex Moutan, 9 g ass-hide gelatin, 30 g red date, 6 g prepared licorice root, etc.) and Erzhi Busui Decoction (EBD, consisting of 120 g glossy privet fruit, 100 g eclipta prostrata, 24 g prepared Gold Theragran, 12 g fructus lycii, 90 g rehmannia rhizoma, 60 g astragalus, 9 g Angelica sinensis, 9 g ass-hide gelatin, 30 g honeysuckle flower, 12 g lotus plumule, and so on) alternatively, one dose daily, decocted twice, taken in two portions. Meanwhile, 50 mg Testosterone Propionate was intramuscularly injected every other day to the improvement stage. Those with fever were treated with LYD by adding 60 g gypsum, 60 g common anemarrhena, 30 g dandelion, 30 g bittersweet herb, 30 g blackend swallowwort root and rhizome, 15 g hemsley rockvine root tuber, and so on. In the improvement stage patients were treated with Jixueteng Compound (Jixueteng Zhengyang Decoction was administered to those of Shen-yang deficiency syndrome: consisting of 100 g spatholobus suberectus, 60 g astragalus, 3 g red ginseng, 12 g psoralea corylifolia, 18 g dodder seed, 12 g angelica, 18 g Herba Epimedii, 6 g common fenugreek seed, 24 g Gold Theragran, 30 g glossy privet fruit, 30 g eclipta prostrata, 6 g dried human placenta, and so on). Meanwhile, 50 mg Testosterone Propionate was intramuscularly injected every other day. Jixueteng Yijing Decoction was administered to those of Shen-yin deficiency syndrome: consisting of 100 g glossy privet fruit, 100 g eclipta prostrata, 90 g rehmannia rhizoma, 30 g spatholobus suberectus, 12 g dodder seed, 6 g psoralea corylifolia, 30 g prepared Gold Theragran, 9 g ass-hide gelatin, 9 g fructus lycii, 24 g Salvia miltiorrhiza, 30 g astragalus, 6 g angelica, and so on), one dose daily, decocted twice, taken in two portions. The treatment lasted to the recovery stage. The medication was gradually reduced to the follow-ups of drug discontinuance. Results After 6 -57 months of treatment, 12 patients (accounting for 19.4%) were basically cured, 14 (22.6%) relieved, 8 (12. 9%) markedly improved, 28 (45.2%) ineffectively, with the total effective rate of 54. 8%. Totally 23 patients had the body temperature ranging 37.6-38.5 degrees C at the first visit to our hospital. They took 2 h- 6 days to have pyretolysis ( <37.5 degrees C) after treatment. Twenty patients with body temperature higher than 38.5 degrees C took 4 h - 5 days to have pyretolysis after treatment. Totally 26 patients suffering from IST induced abnormalities of liver and renal functions (ALT, AST, BUN, and Cr) at the first visit were treated by IM for 2 months. They were restored to the normal levels in 25 cases.
CONCLUSIONS:
The treatment of SAA failing in IST had its specificity. The staging targeted treatment is in line with its pathophysiology. The key points for its treatment might be lie in the improvement and protection of hematopoietic microenvironment of bone marrows. The antisepsis and anti-inflammation of Chinese herbs hindered its aggravating tendency....(more)
Su EY, et al. Zhongguo Zhong Xi Yi Jie He Za Zhi 2012 Dec;32(12):1616-20. Chinese.
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- 24. [Different pruning to yield and quality of Lonicerea Japonicae Flos].
OBJECTIVE:
To find out the influence of differences pruning on Lonicerea Japonicae Flos on it's yield and quality, and provide reference for reasonable pruning.
METHOD: r/>Using different pruning treatments, the growth and yield and chlorogenic acid and galuteolin contents of Lonicerea Japonicae Flos were measured and compared. And the source and sink theory were used to interpret the rationality of the best way.
RESULT:
There existed significant differences in the growth and branching and yield at differences pruning methods, but not including chlorogenic acid and galuteolin contents of Lonicerea Japonicae Flos.
CONCLUSION:
The best pruning treatments is in shearing....(more)
Zhang Y, et al. Zhongguo Zhong Yao Za Zhi 2012 Nov;37(22):3371-4. Chinese.
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- 25. [Researches on the relative expression of HQT gene in different organs of Lonicera japonica].
OBJECTIVE:
To reveal the correlation between HQT gene and the biosynthesis of chlorogenic acid in Lonicera japonica.
METHODS:
RT-PCR was used to measure the relative expression of HQT gene and reference gene Actin, and agarose gel electrophoresis was used to analyse the PCR results.
RESULTS:
The brightness of Actin gene strips of different organs was properly similar to each other,but the brightness of HQT gene strips was significantly different. HQT gene strips of alabastrum were the brightest,the brightness of HQT gene strip of leaves took the second place, and the brightness of HQT gene strips of stems was very faint. This result was in accordance with the content of chlorogenic acid in different organs of Lonicera japonica.
CONCLUSION:
The expression of HQT gene with the biosynthesis of chlorogenic acid has necessary relation with Lonicera japonica....(more)
Liu Y, et al. Zhong Yao Cai 2012 Jul;35(7):1032-6. Chinese.
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- 26. Standardized butanol fraction of WIN-34B suppresses cartilage destruction via inhibited production of matrix metalloproteinase and inflammatory mediator in osteoarthritis human cartilage explants culture and chondrocytes.
BACKGROUND:
WIN-34B is a novel Oriental medicine, which represents the n-butanol fraction prepared from dried flowers of Lonicera japonica Thunb and dried roots of Anemarrhena asphodeloides BUNGE. The component herb of WIN-34B is used for arthritis treatment in East Asian countries. The aim of this study was to determine the cartilage-protective effects and mechanisms of WIN-34B and its major phenolic compounds, chlorogenic acid and mangiferin, in osteoarthritis (OA) human cartilage explants culture and chondrocytes.
METHODS:
The investigation focused on whether WIN-34B and its standard compounds protected cartilage in interleukin (IL)-1β-stimulated cartilage explants culture and chondrocytes derived from OA patients. Also, the mechanisms of WIN-34B on matrix metalloproteinases (MMPs), tissue inhibitor of matrix metalloproteinases (TIMPs), inflammatory mediators, and mitogen-activated protein kinases (MAPKs) pathways were assessed.
RESULTS:
WIN-34B was not cytotoxic to cultured cartilage explants or chondrocytes. WIN-34B dose-dependently inhibited the release of glycosaminoglycan and type II collagen, increased the mRNA expression of aggrecan and type II collagen, and recovered the intensity of proteoglycan and collagen by histological analysis in IL-1β-stimulated human cartilage explants culture. The cartilage protective effect of WIN-34B was similar to or better than that of chlorogenic acid and mangiferin. Compared to chlorogenic acid and mangiferin, WIN-34B displayed equal or greater decreases in the levels of MMP-1, MMP-3, MMP-13, ADAMTS-4, and ADAMTS-5, and markedly up-regulated TIMP-1 and TIMP-3. WIN-34B inhibited inflammatory mediators involved in cartilage destruction, such as prostaglandin E2, nitric oxide, tumor necrosis factor-alpha, and IL-1β. The phosphorylation of extracellular signal-regulated kinase, c-Jun N-terminal kinase (JNK), and p38 was significantly reduced by WIN-34B treatment, while phosphorylation of JNK was only inhibited by chlorogenic acid or mangiferin in IL-1β-stimulated chondrocytes.
CONCLUSIONS:
WIN-34B is potentially valuable as a treatment for OA by virtue of its suppression of MMPs, ADAMTSs, and inflammatory mediators, and it's up-regulation of TIMP-1 and TIMP-3 involved in the MAPK pathway....(more)
Huh JE, et al. BMC Complement Altern Med 2012 Dec 15;12:256.
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- 27. [Effect of gas-turbine green discoloring and drying processing methods on herbal quality of tetraploid Lonicerae Japonicae Flos].
OBJECTIVE:
To study the effect of gas-turbine green discoloring and drying processing method on the quality of various Lonicerae Japonicae Flos herbs.
METHOD:
DIKMA DiamonsilTM-C18 column (4.6 mm x 250 mm, 5 microm) was adopted using HPLC Waters 1525 and eluted with acetonitrile and 0.1% phosphate acid as the mobile phase. The flow rate was 1.0 mL x min(-1) , the column temperature was 25 degrees C the detection wavelength was 355 nm.
RESULT:
After being processed by the gas-turbine green discoloring and drying method, tetraploid Lonicerae Japonicae Flos showed a green color. The contents of chlorogenic acid and galuteolin were 5.31% and 0.105% , both significantly higher by 18.0% and 32.1% than those of diploid Lonicerae Japonicae Flos processed by the same method. The content of chlorogenic acid in tetraploid Lonicerae Japonicae Flos processed the gas-turbine green discoloring and drying method were also remarkably higher than that of tetraploid and diploid Lonicerae Japonicae Flos processed by traditional processing method of natural drying.
CONCLUSION:
The gas-turbine green discoloring and drying processing method is a new-type drying method suitable for tetraploid Lonicerae Japonicae Flos. Under the condition of gas-turbine green discoloring and drying processing, tetraploid Lonicerae Japonicae Flos shows much higher quality than Lonicerae Japonicae Flos, suggesting that it is a good variety worth popularizing and applying....(more)
Hu X, et al. Zhongguo Zhong Yao Za Zhi 2012 Sep;37(17):2554-7. Chinese.
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- 28. Novel antiplatelet activity of protocatechuic acid through the inhibition of high shear stress-induced platelet aggregation.
Bleeding is the most common and serious adverse effect of currently available antiplatelet drugs. Many efforts are being made to develop novel antithrombotic agents without bleeding risks. Shear stress-induced platelet aggregation (SIPA), which occurs under abnormally high shear stress, plays a crucial role in the development of arterial thrombotic diseases. Here, we demonstrate that protocatechuic acid (PCA), a bioactive phytochemical from Lonicera (honeysuckle) flowers, selectively and potently inhibits high shear (>10,000 s(-1))-induced platelet aggregation. In isolated human platelets, PCA decreased SIPA and attenuated accompanying platelet activation, including intracellular calcium mobilization, granule secretion, and adhesion receptor expression. The anti-SIPA effect of PCA was mediated through blockade of von Willebrand factor binding to activated glycoprotein Ib, a primary and initial event for the accomplishment of SIPA. Conspicuously, PCA did not inhibit platelet aggregation induced by other endogenous agonists like collagen, thrombin, or ADP that are important in both pathological thrombosis and normal hemostasis. Antithrombotic effects of PCA were confirmed in vivo in a rat arterial thrombosis model, where PCA significantly delayed the arterial occlusion induced by FeCl(3). Of particular note, PCA did not increase bleeding times in a rat tail transection model, whereas conventional antiplatelet drugs, aspirin, and clopidogrel substantially prolonged it. Collectively, these results suggest that PCA may be a novel antiplatelet agent that can prevent thrombosis without increasing bleeding risks....(more)
Kim K, et al. J Pharmacol Exp Ther 2012 Dec;343(3):704-11.
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- 29. Honokiol synergizes chemotherapy drugs in multidrug resistant breast cancer cells via enhanced apoptosis and additional programmed necrotic death.
Multidrug resistance (MDR) is a major challenge in cancer therapy. Apoptosis tolerance is one of the key mechanisms of MDR. Honokiol, a small-molecule pharmacologically active component, exhibits competent cytotoxicity in a variety of human cancer cells through apoptosis and other forms of programmed cell death (such as programmed necrosis). Although much work has been done on its antitumor effects, little attention has been paid on systemic evaluation of efficacy of honokiol combined with other chemotherapeutic agents, especially in drugresistant cell lines. Here, we systematically and quantitatively assess its combinational effect with different chemotherapeutic agents using the combination index (CI) equation. We found that honokiol synergized with chemotherapeutic agents both in sensitive and resistant, solid and non-solid (MCF-7, HL-60, MCF-7/ADR and HL-60/ADR) cell lines. Honokiol (40 µg/ml) induced necrotic cell death in MCF-7/ADR cells with characterized morphological and biochemical features. Co-incubation with honokiol and etoposide (VP-16) activated a complex death modality, which was composed of necrotic cell death and apoptosis. This dual-death pathway was shut down when pretreated with pan-caspase inhibitor (z-VAD-fmk) and cyclophilin D inhibitor (cyclosporin A). Western blot analysis results proved that honokiol also enhanced VP-16-induced apoptosis potentially via blocking nuclear factorκB (NF-κB) activation. Our data for the first time quantitatively demonstrate that honokiol synergizes frequently-used chemotherapeutic agents via enhanced apoptosis and additional programmed necrotic death. These findings indicate a promising way to circumvent MDR and apoptosis tolerance....(more)
Tian W, et al. Int J Oncol 2013 Feb;42(2):721-32.
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- 30. Honokiol protects rat hearts against myocardial ischemia reperfusion injury by reducing oxidative stress and inflammation.
Honokiol, a potent radical scavenger, has been demonstrated to ameliorate cerebral infarction following ischemia/reperfusion (I/R) injury. However, its effects on myocardial I/R injury remain unclear. The present study aimed to examine the effects of honokiol on myocardial I/R injury and to investigate its potential cardioprotective mechanisms. Sprague-Dawley rats were pretreated with honokiol and exposed to a 30-min myocardial ischemia followed by 2-h coronary reperfusion. Myocardial I/R-induced infarct size and biochemical and histological changes were compared. The expression of nuclear factor κB(NF-κB; p65) was assessed by western blotting. Pretreatment with honokiol significantly reduced infarct size, and serum creatine kinase (CK) and lactate dehydrogenase (LDH) release compared with those in the I/R group following a 2-h reperfusion. The malondialdehyde (MDA) level, myeloperoxidase (MPO) activity, concentrations of tumor necrosis factor (TNF)-α and interleukin (IL)-6 and expression level of NF-κB were all reduced by honokiol pretreatment, while honokiol inhibited the decreases in superoxide dismutase (SOD) and catalase (CAT) activities. In addition, less neutrophil infiltration and histopathological damage in the myocardium were observed in the honokiol-pretreated group. These findings indicate that honokiol pretreatment diminished myocardial I/R injury through attenuation of oxidative stress and inflammation....(more)
Wang Y, et al. Exp Ther Med 2013 Jan;5(1):315-319.
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- 31. Honokiol inhibits the inflammatory reaction during cerebral ischemia reperfusion by suppressing NF-κB activation and cytokine production of glial cells.
This study was designed to investigate the effects of honokiol, a neuroprotective agent, on cerebral edema in cerebral ischemia reperfusion (IR) mice and its mechanism of anti-inflammation. Honokiol (0.7-70μg/kg) significantly reduced brain water contents and decreased the exudation of Evans blue dye from brain capillaries in cerebral IR mice. Honokiol (0.1-10μM) significantly reduced the p65 subunit level of NF-κB in the nucleus of primary culture-microglia. It (0.01-10μM) evidently reduced nitric oxide (NO) level in the microglia culture medium and in the microglia and astrocytes coculture medium. Honokiol (0.01-10μM) significantly decreased the level of TNF-α in the microglia medium or coculture cell medium. Honokiol (10μM) decreased the level of Regulated upon Activation Normal T-cell Expressed and Secreted (RANTES/CCL5) protein in medium of microglia or astrocytes. In conclusion, Honokiol has a potent anti-inflammatory effect in cerebral ischemia-reperfusion mice and this effect might be attributed to its inhibition ability on the NF-κB activation, consequently blocking the production of inflammatory factors including: NO, tumor necrosis factor-α (TNF-α) and RANTES/CCL5 in glial cells. These results provide evidence for the anti-inflammatory effect of honokiol for the potential treatment of ischemic stroke....(more)
Zhang P, et al. Neurosci Lett 2013 Feb 8;534:123-7.
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- 32. Honokiol induces caspase-independent paraptosis via reactive oxygen species production that is accompanied by apoptosis in leukemia cells.
Our previous report has shown that honokiol (HNK), a constituent of Magnolia officinalis, induces a novel form of non-apoptotic programmed cell death in human leukemia NB4 and K562 cells. In this study, we further explored the relationship between the cell death pathway and cytoplasmic vacuolization and studied the underlying mechanism of leukemia cell death mediated by honokiol. The results showed that low concentrations of honokiol activated an novel alternative cell death fitted the criteria of paraptosis, such as cytoplasmic vacuolization derived from endoplasmic reticulum swelling, lack of caspase activation, and lack of apoptotic morphology. Results further indicated that the cell death was time- and concentration-dependent. In addition, honokiol-induced paraptosis did not involve membrane blebbing, chromatin condensation and phosphatidylserine exposure at the outer of the plasma membrane. The mechanism of the cell death may be associated, at least in part, with the increased generation of reactive oxygen species. Further analysis showed that honokiol induces cell death predominantly via paraptosis and to a certain extent via apoptosis in NB4 cells, and predominantly via apoptosis and to a certain extent via paraptosis in K562 cells. These observations suggest that cell death occurs via more than one pathway in leukemia cells and targeting paraptosis may be an alternative and promising avenue for honokiol in leukemia therapy....(more)
Wang Y, et al. Biochem Biophys Res Commun 2013 Jan 18;430(3):876-82.
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- 33. Magnolia polyphenols attenuate oxidative and inflammatory responses in neurons and microglial cells.
BACKGROUND:
The bark of magnolia has been used in Oriental medicine to treat a variety of remedies, including some neurological disorders. Magnolol (Mag) and honokiol (Hon) are isomers of polyphenolic compounds from the bark of Magnolia officinalis, and have been identified as major active components exhibiting anti-oxidative, anti-inflammatory, and neuroprotective effects. In this study, we investigate the ability of these isomers to suppress oxidative stress in neurons stimulated by the ionotropic glutamate receptor agonist N-methyl-D-aspartate (NMDA) and oxidative and inflammatory responses in microglial cells activated by interferon-γ (IFNγ) and lipopolysaccharide (LPS). We also attempt to elucidate the mechanism and signaling pathways involved in cytokine-induced production of reactive oxygen species (ROS) in microglial cells.
METHODS:
Dihydroethidium (DHE) was used to assay superoxide production in neurons, while CM-H2DCF-DA was used to test for ROS production in murine (BV-2) and rat (HAPI) immortalized microglial cells. NADPH oxidase inhibitors (for example, diphenyleneiodonium (DPI), AEBSF, and apocynin) and immunocytochemistry targeting p47phox and gp91phox were used to assess the involvement of NADPH oxidase. Western blotting was used to assess iNOS and ERK1/2 expression, and the Griess reaction protocol was employed to determine nitric oxide (NO) concentration.
RESULTS:
Exposure of Hon and Mag (1-10 μM) to neurons for 24 h did not alter neuronal viability, but both compounds (10 μM) inhibited NMDA-stimulated superoxide production, a pathway known to involve NADPH oxidase. In microglial cells, Hon and Mag inhibited IFNγ±LPS-induced iNOS expression, NO, and ROS production. Studies with inhibitors and immunocytochemical assay further demonstrated the important role of IFNγ activating the NADPH oxidase through the p-ERK-dependent pathway. Hon and, to a lesser extent, Mag inhibited IFNγ-induced p-ERK1/2 and its downstream pathway for ROS and NO production.
CONCLUSION:
This study highlights the important role of NADPH oxidase in mediating oxidative stress in neurons and microglial cells and has unveiled the role of IFNγ in stimulating the MAPK/ERK1/2 signaling pathway for activation of NADPH oxidase in microglial cells. Hon and Mag offer anti-oxidative or anti-inflammatory effects, at least in part, through suppressing IFNγ-induced p-ERK1/2 and its downstream pathway....(more)
Chuang DY, et al. J Neuroinflammation 2013 Jan 29;10:15.
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- 34. Maximizing dermal targeting and minimizing transdermal penetration by magnolol/honokiol methoxylation.
Magnolol and honokiol, predominant active compounds in the family Magnoliaceae, are known to exhibit strong anti-inflammatory activities against dermal disorders. We attempted to modify the structures of magnolol and honokiol by methoxylation to optimize the skin delivery ability. Absorption of these permeants into and through the skin was performed at both an infinite dose and saturated solubility. Superoxide anion and elastase released from human neutrophils were the biomarkers used to examine anti-inflammatory potencies of these permeants. The safety of the permeants was evaluated by keratinocyte viability and in vivo bioengineering techniques. Topical magnolol and honokiol at an infinite dose (7.5 mM) showed skin accumulations of 0.22 and 0.16 nmol/mg, respectively. Methoxylation significantly enhanced their skin absorption. Deposition amounts of dimethylmagnolol and dimethylhonokiol were respectively 15- and 7-fold greater than those of magnolol and honokiol. Contrary to the skin accumulation results, the transdermal penetration across skin decreased following methoxylation. No transdermal delivery occurred for dimethylhonokiol. Skin uptake of 4'-O-methylhonokiol was 2-fold higher than that of 2-O-methylhonokiol, although they are isomers. Methoxylated permeants demonstrated selective absorption into follicles, which showed 3-5-fold higher follicular amounts compared to magnolol and honokiol. The relative order of anti-inflammatory activities was honokiol>2-O-methylmagnolol>dimethylhonokiol>magnolol. The other compounds exhibited negligible or negative responses in activated neutrophils. Magnolol and honokiol induced slight but significant keratinocyte cytotoxicity and stratum corneum disruption. Daily administration of methoxylated permeants, especially dimethylhonokiol, produced no skin irritation for up to 7 days. Methoxylated magnolol and honokiol can be efficient and safe candidates for treating inflammatory skin disorders....(more)
Lin CF, et al. Int J Pharm 2013 Mar 10;445(1-2):153-62.
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- 35. Screening active anti-breast cancer compounds from Cortex Magnolia officinalis by 2D LC-MS.
Most of the anti-breast cancer drugs are often limited owing to drug resistance and serious adverse reactions. Therefore, development of more targeted and low toxic drugs from traditional Chinese medicines for breast cancer are needed. At the same time, establishment of fast and effective drug screening methods are urgently required. We describe here a 2D LC method of MDA-MB-231 cell membrane chromatography combined with HPLC/MS for recognition, separation, and identification of target components from traditional Chinese medicine Cortex Magnolia officinalis. The MDA-MB-231 cells membrane was used to prepare the chromatographic stationary phase in the first dimension. The active compounds had a retention characteristic on the cell membrane chromatography model (10 × 2.0 mm, 5 μm). The retention fractions were enriched using an online C(18) column (10 × 1.0 mm, 5 μm) and were analyzed by the second dimension RP chromatography. Finally, the activity of the retention fractions was tested through in vitro experiments. Results showed that the retention fractions were honokiol and magnolol and the inhibition rate on MDA-MB-231 cell growth were 23 and 64 μM, respectively. These results support the conclusion that this coupled analytical technique could be an efficient method in drug discovery....(more)
Hou X, et al. J Sep Sci 2013 Feb;36(4):706-12.
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