- 1. [Phytotherapy with a mixture of dry extracts with hepato-protective effects containing artichoke leaves in the management of functional dyspepsia symptoms].
AIM:
The aim of the study was to explore the potential of phytotherapy with artichoke leaf extract in the management of functional dyspepsia symptoms, a disorder notoriously recalcitrant to pharmacotherapy.
METHODS:
A cohort of outpatients with a clinical diagnosis of functional dyspepsia and deemed suitable candidates for non-pharmacologic treatment was prospectively observed for 60 days by 33 physicians. Treatment consisted of Cinarepa, a commercial mixture of dry extracts of artichoke leaf (Cynara scolymus) 15% of chlorogenic acid (150 mg per capsule), dandelion radix (Taraxacum officinalis) 2% of inulin, turmeric rhizome (Curcuma longa) 95% of curcumin and rosemary bud essential oil microencapsulated (Rosmarinum officinalis). The severity of 8 dyspepsia symptoms was self-evaluated on a 10-point scale. Blood chemistry testing of lipid profile and liver function was discretionary.
RESULTS:
Of the 311 patients in the cohort, the data from 305 (98%) were included in the analysis of dyspepsia symptoms and the data from 50-73 (16-23%) were entered into the analysis of blood chemistry results. A statistically significant gradual reduction in symptom severity was noted at day 30 and further improvement was observed at day 60. Global clinical response, defined as a 50% reduction in the total scores of all symptoms, was recorded in 38% of patients at 30 days and in 79% at 60 days. At 60 days, total cholesterol, LDL and triglyceride levels had decreased by 6-8% over baseline values (P < or = 0.001); transaminase (AST, ALT), and gamma GT concentrations had diminished by 13-20 U/L (P<0.01) in patients with relatively elevated baseline values.
CONCLUSION:
Phytotherapy with Cinarepa holds promise as an alternative option in the relief of functional dyspepsia symptoms and merits further investigation in controlled studies....(more)
Sannia A. Minerva Gastroenterol Dietol 2010 Jun;56(2):93-9. Italian.
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- 2. Asiaticoside induces type I collagen synthesis and osteogenic differentiation in human periodontal ligament cells.
Asiaticoside, an active ingredient extracted from Centella asiatica, has been widely used to promote wound healing. In this study, the effects of asiaticoside on proliferation, protein synthesis, and osteogenic differentiation in human periodontal ligament cells (HPDLs) were investigated. HPDLs were treated with asiaticoside at concentrations of 25, 50, and 100 µg/mL. Cell number was determined by MTT assay. The mRNA expression was analyzed by reverse transcription-polymerase chain reaction. Western blot analysis and immunocytochemistry were used to confirm protein synthesis. Osteogenic differentiation was determined by alkaline phosphatase activity, osteoblast marker gene expression, and in vitro mineralization. The results showed that asiaticoside treatment, ranging from 25 to 100 mg/mL, had no effect on cytotoxicity or cell proliferation. When HPDLs were treated with asiaticoside in serum-free medium, dose-dependent increases in the levels of fibronectin and collagen type I mRNA and protein were observed at 72 h. Moreover, asiaticoside attenuated matrix metalloproteinase-1 but enhanced tissue inhibitor of metalloproteinase-1 mRNA expression. The addition of asiaticoside to osteogenic medium resulted in an increase in alkaline phosphatase enzymatic activity, up-regulation of osteoblast marker gene mRNA expression, and enhancement of mineralization by HPDLs. These results suggest the potential application of asiaticoside for enhancing periodontal tissue healing. Copyright © 2012 John Wiley & Sons, Ltd....(more)
Nowwarote N, et al. Phytother Res 2013 Mar;27(3):457-62.
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- 3. Production of Polyclonal Antibody Against Madecassoside and Development of Immunoassay Methods for Analysis of Triterpene Glycosides in Centella asiatica.
INTRODUCTION:
Centella asiatica (L.) Urban consists of two major triterpene glycosides, asiaticoside (AS) and madecassoside (MA), as active components used for wound healing and enhancing memory.
OBJECTIVE:
To produce a polyclonal antibody against madecassoside (MA-PAb) and develop enzyme-linked immunosorbent assay (ELISA) and Eastern blotting methods for quantitative analysis of triterpene glycosides in Centella asiatica.
METHODS:
An ELISA method was developed using polyclonal antibody against MA. An Eastern blotting method on the PES membrane was established for determination of MA and AS. The immunoassays were validated for sensitivity, precision, specificity and accuracy.
RESULTS:
The prepared MA-PAb shows specificity to MA and AS. The measuring range of triterpene glycosides was 0.39-50 µg/mL using the ELISA method. An Eastern blotting method was developed for determining individual MA and AS, which could be detected in the range of 62.5-500 ng. The limit of detection for MA and AS was 31.25 ng. The two methods developed showed good specificity, precision, and accuracy, and also correlated with high-performance liquid chromatography.
CONCLUSION:
These immunoassays have several advantages that include high sensitivity as well as being rapid and facile for determination of the triterpene glycosides in C. asiatica. Copyright © 2012 John Wiley & Sons, Ltd.
Copyright © 2012 John Wiley & Sons, Ltd....(more)
Tassanawat P, et al. Phytochem Anal 2013 May;24(3):256-62.
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- 4. Beneficial effects of asiaticoside on cognitive deficits in senescence-accelerated mice.
The effect of asiaticoside isolated from Hydrocotyle sibthorpioides (AHS) on the promotion of cognition in senescence-accelerated mice (SAMP) was evaluated. Six-month old male SAMP8 mice were orally administered 20, 40 or 80mg/kg AHS daily for three months. SAMR1 mice were used as a "normal aging" control. The results showed that treatment with AHS significantly improved learning and memory abilities in behavioral tests. AHS-treated mice showed higher antioxidant enzyme activity and lower lipid oxidation in serum compared with untreated SAMP8 mice. Mechanistically, studies showed that AHS markedly reduced the content and deposition of β-amyloid peptide (Aβ) by inhibiting the expression of mRNA for amyloid protein precursor, β-site amyloid cleaving enzyme-1 and cathepsin B and promoting the expression of mRNA for neprilysin and insulin degrading enzyme. In addition, AHS significantly increased the expression of plasticity-related proteins including postsynaptic density-95, phosphor-N-methyl-d-aspartate receptor 1, phospho-calcium-calmodulin dependent kinase II, phospho-protein kinase A Catalyticβ subunit, protein kinase Cγ subunit, phospho-CREB and brain derived neurotrophic factor. Furthermore, AHS increased the levels of acetylcholine (Ach), but decreased cholinesterase (AchE) activity. These results demonstrated that AHS administration may prevent spatial learning and memory decline by scavenging free radicals, up-regulating the activity of antioxidant enzymes, decreasing the level of Aβ, ameliorating dysfunction in synaptic plasticity, and reversing abnormal changes in Ach level and AchE activity. Thus, AHS should be developed as a new drug to prevent age-related cognitive deficits....(more)
Lin X, et al. Fitoterapia 2013 Apr 2;87C:69-77.
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- 5. Metabolomic Analysis of Methyl Jasmonate-Induced Triterpenoid Production in the Medicinal Herb Centella asiatica (L.) Urban.
Centella asiatica is an important source of biologically active pentacyclic triterpenoids. The enhancement of the biosynthesis of the centellosides by manipulation of associated metabolic pathways is receiving much attention. Jasmonates play critical roles in plant metabolism by up-regulating the expression of genes related to secondary metabolites. Here, we investigated the effect of methyl jasmonate (MeJa) in C. asiatica through targeted metabolomic profiling of asiaticoside and madecassoside as well as their aglycones, asiatic acid and madecassic acid. Cell suspensions were treated with 0.2 mM MeJa for 2, 4 and 6 days. Liquid chromatography coupled to mass spectrometry (LC-MS) was used to explore induced changes in metabolite profiles, both qualitatively and quantitatively. Principal component analysis (PCA)-derived scores plots revealed clusters of sample replicates for control and treated samples at 2, 4 and 6 days while loading plots aided in identifying signatory biomarkers (asiatic acid and madecassic acid, as well as asiaticoside and madecassoside) that clearly demonstrate the variability between samples. In addition to increased biosynthesis of the targeted centelloids, other differential changes in the intracellular metabolite profiles reflected the response of the C. asiatica cells to the MeJa-treatment as a reprogramming of the metabolome....(more)
James JT, et al. Molecules 2013 Apr 11;18(4):4267-81.
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- 6. [Near-infrared spectroscopy technology for online monitoring of the column separation and purification process of active components of Centella asiatica L. Urban].
The present paper is to study and develop a method for online monitoring of the column separation and purification process of active components that are madecassoside and asiaticoside of Centella asiatica L. Urban using near-infrared (NIR) spectroscopy technology. After collecting 50%-ethanol eluant, we detected their NIR spectra and developed the high performance liquid chromatography (HPLC) assay method of active components. Then, partial least square (PLS) was used to develop linear correlation between their NIR spectra and contents. During modeling, correlation coefficient (R2) and root mean square errors of cross-validation (RMSECV) were regarded as the indexes to select optimal wavenumbers and preprocessing methods. The optimal wavenumbers of madecassoside and asiaticoside were in the range of 12 000.8-7 499.8 cm(-1) and 12 000.8-9 750.3 cm(-1), respectively; R2 were 96.44 and 96.07, respectively, and RMSECV were 0.084 80 and 0.000 99, respectively. The above developed model was used for online monitoring of the contents of madecassoside and asiaticoside during the column separation and purification process of Centella asiatica L. Urban. The predicted results were satisfactory. This method was proved to be fast, convenient and precise. It can be used in online monitoring and quality control of the manufacturing of madecassoside and asiaticoside....(more)
Liu H, et al. Guang Pu Xue Yu Guang Pu Fen Xi 2013 Jan;33(1):98-101. Chinese.
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- 7. Discrimination of three Pegaga (Centella) varieties and determination of growth-lighting effects on metabolites content based on the chemometry of 1H nuclear magnetic resonance spectroscopy.
The metabolites of three species of Apiaceae, also known as Pegaga, were analyzed utilizing (1)H NMR spectroscopy and multivariate data analysis. Principal component analysis (PCA) and hierarchical cluster analysis (HCA) resolved the species, Centella asiatica, Hydrocotyle bonariensis, and Hydrocotyle sibthorpioides, into three clusters. The saponins, asiaticoside and madecassoside, along with chlorogenic acids were the metabolites that contributed most to the separation. Furthermore, the effects of growth-lighting condition to metabolite contents were also investigated. The extracts of C. asiatica grown in full-day light exposure exhibited a stronger radical scavenging activity and contained more triterpenes (asiaticoside and madecassoside), flavonoids, and chlorogenic acids as compared to plants grown in 50% shade. This study established the potential of using a combination of (1)H NMR spectroscopy and multivariate data analyses in differentiating three closely related species and the effects of growth lighting, based on their metabolite contents and identification of the markers contributing to their differences....(more)
H M, et al. J Agric Food Chem 2012 Jan 11;60(1):410-7.
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- 8. Asiaticoside induces tumour-necrosis-factor-α-mediated nitric oxide production to cure experimental visceral leishmaniasis caused by antimony-susceptible and -resistant Leishmania donovani strains.
OBJECTIVES:
The aim of this study was to investigate and characterize the efficacy of asiaticoside in an experimental model of visceral leishmaniasis caused by antimony-susceptible (AG83) and -resistant (GE1F8R and K39) Leishmania donovani.
METHODS:
The effect of asiaticoside was evaluated by microscopic counting of intracellular amastigotes in cultured macrophages stained with Giemsa. The antileishmanial effect of the compounds was assessed in infected BALB/c mice by estimation of splenic and liver parasite burdens in Leishman Donovan units. Cytokines were measured by real-time PCR and ELISA. Intracellular tumour necrosis factor-α (TNF-α) was measured by fluorescence-activated cell sorting. Nitric oxide was measured by the Griess reaction.
RESULTS:
Besides effectively inhibiting in vitro replication of the parasite within macrophages, asiaticoside treatment resulted in almost complete clearance of the liver and splenic parasite burden when administered at a dose of 5 mg/kg × 10 starting on day +30 of challenge with antimony-susceptible (AG83) and -resistant (GE1F8R and K39) L. donovani. Asiaticoside treatment was associated with a switch in the host from a Th2- to a Th1-type immune response accompanied by the induction of TNF-α-mediated nitric oxide production, all of which are important elements for macrophage function in antileishmanial defence mechanisms.
CONCLUSIONS:
These results suggest that oral therapy with asiaticoside shows promising antileishmanial efficacy in animals infected by antimony-susceptible (AG83) and -resistant (GE1F8R and K39) L. donovani....(more)
Bhaumik SK, et al. J Antimicrob Chemother 2012 Apr;67(4):910-20.
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- 9. The influence of certain taxonomic and environmental parameters on biomass production and triterpenoid content in the leaves of Centella asiatica (L.) Urb. from Madagascar.
Centella asiatica (Apiaceae family; Talapetraka in Malagasy) is a tropical and subtropical plant with leaves containing glycotriterpenoids (asiaticosides) used in traditional and modern medicine. C. asiatica is collected exclusively in natural stands. It is Madagascar's second most important indigenous plant export. The objective in this study is to provide data which will make it possible to optimize the harvest and thus effectively develop this resource. Two foliar morphotypes were identified: morphotype A with small reniform leaves (leaf area ca. 4.5 cm(2) ), found in the east of Madagascar, and morphotype B with large round leaves (up to 7.5 cm(2) ) found in the west, with sympatric zones in the central part of the island. Morphotype A produces a higher biomass, and is twice as rich in asiaticosides as morphotype B. Significant variations in biomass yield and asiaticoside content are observed depending on the date of collection: higher during the rainy season (December to April) and lower during the dry season (June to August). Inter-annual variations are also observed. Populations located at around 800-1400 m altitude on the eastern side of Madagascar, in a sub-humid climate, appeared to be more productive. These results provide more precise information to the economic sector, which confirms the empirical choices made by collectors. They represent the first elements towards sustainable management of the resource, and maybe even domestication....(more)
Rahajanirina V, et al. Chem Biodivers 2012 Feb;9(2):298-308.
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- 10. Improved in vitro and in vivo collagen biosynthesis by asiaticoside-loaded ultradeformable vesicles.
The potentiality of ultradeformable vesicles as a possible topical delivery system for asiaticoside, a natural compound obtained from Centella asiatica was evaluated, because this compound exhibits collagen biosynthesis promoting activity. Ultradeformable vesicles were prepared by the extrusion technique; these vesicles were composed of Phospholipon 100 and different molar fractions of sodium cholate as the edge activator. The physicochemical properties of the ultradeformable vesicles were investigated through differential scanning calorimetry and light scattering techniques. The potential cyctotoxicity and biological activity of asiaticoside-loaded ultradeformable vesicles were evaluated on primary human dermal fibroblast cells by determining the extracellular lactic dehydrogenase activity, the cellular viability and the biosynthetic production of collagen. In vitro permeation experiments through human stratum corneum and epidermis membranes were also carried out. Ultradeformable vesicles having sodium cholate molar fraction of 0.2 proved to be the most suitable topical carriers for asiaticoside. A sodium cholate content of >0.2 was observed to be cytotoxic probably due to its co-existence with other lipid aggregates, an example being mixed micelles. Asiaticoside-loaded ultradeformable vesicles with a sodium cholate molar fraction of 0.2 elicited the greatest degree of collagen biosynthesis in human fibroblasts. Ultradeformable vesicles provided the greatest in vitro skin permeation of asiaticoside showing a 10-fold increase with respect to the free drug solution and favoured an increase in in vivo collagen biosynthesis. Ultradeformable vesicles are therefore suitable carriers for the pharmaceutical and cosmetic application of the natural agent asiaticoside....(more)
Paolino D, et al. J Control Release 2012 Aug 20;162(1):143-51.
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- 11. Effect of Agrobacterium rhizogenes and elicitation on the asiaticoside production in cell cultures of Centella asiatica.
BACKGROUND:
Centella asiatica (L.) Urb. (Apiaceae) is an important medicinal plant, and it has been using to prepare herbal medicines. The compounds responsible for the biological activity of C. asiatica are triterpenoids such as asiaticoside. Asiaticoside is also important as a marker for standardization of C. asiatica. Due to the low content, there is a need to enhance the production of asiaticoside of C. asiatica. The biotechnological approach is one of the methods that can be used to enhance its production.
OBJECTIVES:
This study was designed to enhance the production of asiaticoside from C. asiatica using A. rhizogenes and elicitation experiments.
MATERIALS AND METHODS:
Callus cultures were initiated using Murashige and Skoog (MS) medium supplemented with 1.0 mg/L indole-3-acetic acid (IAA) and 1.0 mg/L 6-benzylaminopurin (BAP). All media were supplemented with 4% (w/w) sucrose and solidified with 0.9% agar. Elicitations were done using pectin, methyl jasmonate, and Cu(2+) ions. Transformed hairy root cultures were performed using A. rhizogenes.
RESULTS:
Callus culture of C. asiatica was successfully initiated. Enhancement of the production of asiaticoside in the callus culture by elicitors pectin was up to 31%; methyl jasmonate (50 μM) in cell suspension cultures at day 14 was up to 171% compared to explant and 494% compared to control callus; copper ion (25 μM) at day 21 was up to 144% compared to explant, and 676% compared to control cell suspension cultures. While enhancement by genetic transformation using A. rhizogenes was 166-172% compare to untransformed roots
CONCLUSION:
Elicitation and genetically transformed hairy root cultures of C. asiatica produced asiaticoside up to 172% higher than untreated callus....(more)
Ruslan K, et al. Pharmacogn Mag 2012 Apr;8(30):111-5.
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- 12. Assessment of in vitro digestibility and fermentation parameters of alfalfa hay-based diet following direct incorporation of fenugreek seed (Trigonella foenum) and asparagus root (Asparagus officinalis).
This study was completed to evaluate the effect of fenugreek seed (Trigonella foenum; FS) and asparagus root (Asparagus officinalis; AR) on in vitro nutrient digestibility and fermentation patterns. Different levels [0%, 5%, 10%, 15% and 20% of dry matter (DM)] of the medicinal plants were included using alfalfa hay (AH) as a basal substrate at different incubation times (12, 18, 24 and 48 h). Total phenolic components of AH, FS and AR were 5.9, 10 and 8.3 g/kg DM, whereas total tannins were 0.4, 3.8 and 1.5 g/kg DM, respectively. Corresponding values for saponins were 10.4, 27.3 and 40.3 g/kg DM. Fenugreek seed increased (p < 0.05) in vitro organic matter (OM) digestibility at different incubation times and decreased (p < 0.05) crude protein (CP) digestibility at 18 and 24 h of incubation. Asparagus root also increased (p < 0.05) in vitro OM digestibility and decreased (p < 0.05) CP digestibility at different incubation times. Neutral detergent fibre digestibility was increased (p < 0.05) by the addition of AR or FS at low levels, but decreased (p < 0.05) noticeably by increasing level of two plants in the basal substrate. Ammonia-N concentration was markedly reduced (p < 0.05) by the addition of AR at different incubation times, and this reduction was accompanied by the decrease in CP digestibility. True DM degradability and partitioning factor (ratio of substrate DM truly degraded to gas volume produced at different times of incubation) were increased, and total volatile fatty acid concentration and total gas production were decreased (p < 0.05) with the addition of FS (at 10% and 15% DM levels) or AR (at 5%, 10% and 15% DM levels) at different incubation times. Results suggest that FS and AR may have potential as feed additives to increase the efficiency of nutrients' utilization, particularly of nitrogen in ruminant diets.
© 2012 Blackwell Verlag GmbH....(more)
Naseri V, et al. J Anim Physiol Anim Nutr (Berl) 2012 Jun 28.
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- 13. Asparagus P(R) cannot compete with first-line diuretics in lowering the blood pressure in treatment-requiring antihypertensives.
A six week clinical surveillance of 163 patients receiving maximally tolerable doses of Asparagus P((R)), a proprietary mixture pulversied dried asparagus root and parsley leaf, has not indicated any clinically useful antihypertensive effect. The profile of adverse events (with 7 patients leaving the surveillance early because of renally related complaints) contraindicates its use in hypertension or to promote flushing of the efferent tract in rental inflammatory conditions or urolithiasis....(more)
Chrubasik S, et al. Phytother Res 2009 Sep;23(9):1345-6.
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- 14. Asparagus root regulates cholesterol metabolism and improves antioxidant status in hypercholesteremic rats.
Hyperlipidemia/hypercholesteremia are major risk factors for atherosclerosis and cardiovascular diseases. Root of Asparagus racemosus (AR) is widely used in Ayurvedic system of medicine in India and is known for its steroidal saponin content. This study was designed to investigate the hypocholesteremic and antioxidant potential of AR root in both normo- and hypercholesteremic animals. Normal and hypercholesteremic male albino rats were administered with root powder of AR (5 and 10 g% dose levels) along with normal and hypercholesteremic diets, respectively, for a duration of 4 weeks. Plasma and hepatic lipid profiles, fecal sterol, bile acid excretion and hepatic antioxidant activity were assessed. Inclusion of AR root powder in diet, resulted in a dose-dependant reduction in plasma and hepatic lipid profiles, increased fecal excretion of cholesterol, neutral sterol and bile acid along with increases in hepatic HMG-CoA reductase activity and bile acid content in hypercholesteremic rats. Further, AR root also improved the hepatic antioxidant status (catalase, SOD and ascorbic acid levels). No significant changes in lipid and antioxidant profiles occurred in the normocholesteremic rats administered with AR root powder. AR root appeared to be useful as a dietary supplement that offers a protection against hyperlipidemia/hypercholesteremia in hypercholesteremic animals. The results of the present study indicate that the potent therapeutic phyto-components present in AR root i.e. phytosterols, saponins, polyphenols, flavonoids and ascorbic acid, could be responsible for increased bile acid production, elimination of excess cholesterol and elevation of hepatic antioxidant status in hypercholesteremic conditions....(more)
Visavadiya NP, et al. Evid Based Complement Alternat Med 2009 Jun;6(2):219-26.
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- 15. [Clinical effect of yiqi yangyin jiedu decoction in treating patients with advanced non-small cell lung cancer].
OBJECTIVE:
To observe the clinical therapeutic effect and mechanism of Yiqi Yangyin Jiedu Decoction (YYJD, a Chinese herbal recipe for strengthening qi, nourishing yin and removing toxic substance, consisting of milkvetch root 30 g, glehnia root 30 g, asparagus root 15 g, lilyturf root 15 g, grossy privet fruit 12 g, spikemoss herb 30 g, Chinese sage herb 30 g, manyleaf paris rhizome 30 g, etc. ) in treating patients with advanced nonsmall cell lung cancer (NSCLC).
METHODS:
Sixty patients with advanced lung cancer of qi-yin deficiency syndrome were randomized into three groups: the TCM group (A) treated with YYJD, the chemotherapy group (B) treated by chemotherapy with NP or GP protocol, and the combined treated group (C) treated with YYJD and chemotherapy in combination. The efficacy was evaluated after two cycles of treatment.
RESULTS:
The total effective rate for alleviating qi-yin deficiency syndrome in group A was 80%, significantly higher than that in Group C and B (35% and 20%, P <0.01) respectively. The KPS increasing and stabilizing rate in Group A and C was 90% and 85% respectively, significantly higher than that in Group B (75%), and difference between A and B was significant (P <0.05). In Group C after treatment, CD(3)+ showed a rising trend (P = 0.05), different to that in Group A and B (P <0.05 and P <0.01); CD(4)+ significantly increased (P <0.05) and CD(4)+/CD(8)+ ratio showed increasing trend (P = 0.06), while in Group B both were decreased significantly, showed significantly difference (P < 0.05). CD(8)+ CD(28)+ significantly increased after treatment in Group A and C (P <0.01 and P <0.05), but showed decreasing trend (P = 0.06) in Group B, significant difference was shown between B and C (P <0.05).
CONCLUSION:
YYJD can ameliorate the qi-yin deficiency syndrome evidently in advance lung cancer patients; improve their quality of life, the mechanism might be by way of enhancing T-lymphocyte activity and killer T-cell function, to elevate the T-cell mediated immunity in a round way....(more)
Liu LS, et al. Zhongguo Zhong Xi Yi Jie He Za Zhi 2008 Apr;28(4):352-5. Chinese.
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- 16. Spanning high-dimensional expression space using ribosome-binding site combinatorics.
Protein levels are a dominant factor shaping natural and synthetic biological systems. Although proper functioning of metabolic pathways relies on precise control of enzyme levels, the experimental ability to balance the levels of many genes in parallel is a major outstanding challenge. Here, we introduce a rapid and modular method to span the expression space of several proteins in parallel. By combinatorially pairing genes with a compact set of ribosome-binding sites, we modulate protein abundance by several orders of magnitude. We demonstrate our strategy by using a synthetic operon containing fluorescent proteins to span a 3D color space. Using the same approach, we modulate a recombinant carotenoid biosynthesis pathway in Escherichia coli to reveal a diversity of phenotypes, each characterized by a distinct carotenoid accumulation profile. In a single combinatorial assembly, we achieve a yield of the industrially valuable compound astaxanthin 4-fold higher than previously reported. The methodology presented here provides an efficient tool for exploring a high-dimensional expression space to locate desirable phenotypes....(more)
Zelcbuch L, et al. Nucleic Acids Res 2013 May 1;41(9):e98.
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- 17. Effective Inhibition of Skin Cancer, Tyrosinase, and Antioxidative Properties by Astaxanthin and Astaxanthin Esters from the Green Alga Haematococcus pluvialis.
Astaxanthin mono- (AXME) and diesters (AXDE) were characterized and examined for anticancer potency with total carotenoids (TC) and astaxanthin (AX) against UV-7,12-dimethylbenz(a)anthracene (DMBA)-induced skin cancer model in rat. At 200 μg/kg bw, AXDE and AXME reduced UV-DMBA-induced tumor incidences up to 96 and 88%, respectively, when compared to AX (66%) and TC (85%). UV-DMBA has been known to generate high levels of free radicals and tyrosinase enzyme, leading to characteristic symptoms of skin pigmentation and tumor initiation. Intriguingly, ∼7-fold increase in tyrosinase and 10-fold decrease in antioxidant levels were normalized by AXDE and AXME as opposed to only ∼1.4-2.2-fold by AX and TC, respectively. This result together with the appearance of 72 and 58 ng/mL of retinol in the serum of respective AXE-treated (AXDE + AXME) and AX-treated animals suggested that better anticancer potency of AXEs could be due to increased bioavailability....(more)
Rao AR, et al. J Agric Food Chem 2013 Apr 16.
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- 18. Tagging of biomolecules with deuterated water (D<sub>2</sub>O) in commercially important microalgae.
To understand the effect of any biomolecules in specific metabolic pathways in humans, bioavailability and for other basic understanding, stable isotopically-labelled biomolecules (preferably deuterated) is the fundamental pre-requisite. Production of deuterated biomolecules such as, astaxanthin, β-carotene, lutein, chlorophyll-a, and eicosapentaenoic acid (EPA, 20:5n-3) by metabolic tagging have been shown in commercially important microalgae, Haematococcus pluvialis and Phaeodactylum tricornutum. These microalgae were grown in appropriate optimized medium supplemented with 25 % (v/v) deuterated water. LC-MS analysis showed a maximum of 20, 25, 23, 24, and 27 % replacement of hydrogen by deuterium atoms respectively in astaxanthin, β-carotene, lutein, chlorophyll-a, and EPA. To our knowledge, this is the first report on the production of deuterated astaxanthin, chlorophyll-a and EPA by these microalgae....(more)
Saha SK, et al. Biotechnol Lett 2013 Mar 12.
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- 19. Pigment production by a new thermotolerant microalga Coelastrella sp. F50.
Microalgae are good crops to produce natural pigments because of their high growth rates. Tropical zones are better locations than temperate areas for microalgal cultivation because they have longer duration of daylight and more stable temperatures throughout the year, but the high temperatures pose a challenge to microalgal cultivation. A newly isolated thermotolerant microalga produces reddish pigments under environmental stress. Morphological and molecular evidence including meridional ribs on the cell wall, pigment production, and its 18S rDNA sequence suggests that this microalga belongs to the genus Coelastrella. Salt stress and high light intensity accelerated biosynthesis of the pigments, and significant quantities of oil accumulated as the cells experienced stress due to nutrient deficiency. This microalga could withstand temperature of 50°C for more than 8h, which is a necessary trait for outdoor cultivation in tropical areas. The pigments contain astaxanthin, lutein, canthaxanthin, and β-carotene as analysed by using HPLC....(more)
Hu CW, et al. Food Chem 2013 Jun 15;138(4):2071-8.
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- 20. Astaxanthin ameliorates lung fibrosis in vivo and in vitro by preventing transdifferentiation, inhibiting proliferation, and promoting apoptosis of activated cells.
Astaxanthin, a member of the carotenoid family, is the only known ketocarotenoid transported into the brain by transcytosis through the blood-brain barrier. However, whether astaxanthin has antifibrotic functions is unknown. In this study, we investigated the effects of astaxanthin on transforming growth factor β1-mediated and bleomycin-induced pulmonary fibrosis in vitro and in vivo. The results showed that astaxanthin significantly improved the structure of the alveoli and alleviated collagen deposition in vivo. Compared with the control group, the astaxanthin-treated groups exhibited downregulated protein expressions of α-smooth muscle actin, vimentin, hydroxyproline, and B cell lymphoma/leukemia-2 as well as upregulated protein expressions of E-cadherin and p53 in vitro and in vivo. Astaxanthin also inhibited the proliferation of activated A549 and MRC-5 cells at median inhibitory concentrations of 40 and 30μM, respectively. In conclusion, astaxanthin could relieve the symptoms and halt the progression of pulmonary fibrosis, partly by preventing transdifferentiation, inhibiting proliferation, and promoting apoptosis of activated cells....(more)
Wang M, et al. Food Chem Toxicol 2013 Jun;56:450-8.
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- 21. Origin of the Bathochromic Shift of Astaxanthin in Lobster Protein: 2D Electronic Spectroscopy Investigation of β-Crustacyanin.
We report on ultrafast spectroscopy study of β-crustacyanin, the carotenoprotein responsible for the coloration of the lobster shell. β-Crustacyanin is formed by two closely positioned astaxanthin molecules encapsulated in protein. The 2D electronic spectroscopy together with two-color pump-probe was applied to investigate the electronic structure, the excited-state dynamics, and the influence of the excitonic interaction between the two carotenoids in β-crustacyanin. By using the ∼20 fs laser pulses tuned to absorption bands of the S0-S2 and S1-Sn transitions of carotenoids, we were able to trace full excitation relaxation dynamics, starting with S2-S1 relaxation on the ∼30 fs time scale and finishing with the ground-state recovery of 3.2 ps. Superimposed on the relaxation dynamics in the 2D spectra, we observed long-lived beating signals at the characteristic frequencies of astaxanthin vibrational modes. We assign these oscillations to the ground-state vibrational wavepacket dynamics. All major features of the 2D spectra, including amplitude and phase maps of the long-lived oscillations, were reproduced by employing the exciton-vibronic model. Consistent modeling of all optical properties of β-crustacyanin (including absorption and circular dichroism spectra) points to the relatively weak coupling between the two astaxanthin molecules (∼250 cm<sup>-1</sup>). This implies that the excitonic coupling provides insignificant contribution to the bathochromic shift in β-crustacyanin. We discuss the origin of the shift and propose that it is caused by two major effects: conformational changes of astaxanthin molecules (increase in effective conjugation length) together with increased charge-transfer character of the S2 state. We put the bathochromic shift in the broad perspective of other "blue" carotenoids properties....(more)
Christensson N, et al. J Phys Chem B 2013 Apr 10.
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- 22. Metabolic engineering of tomato for high-yield production of astaxanthin.
Dietary carotenoids have been shown to be beneficial to health by decreasing the risk of many diseases. Attempts to enhance carotenoids in food crops have been successful although higher plants appear to resist big changes of carotenoid biosynthesis by metabolic engineering. Here we report the generation of a more nutritious tomato by modifying the intrinsic carotenes to astaxanthin, a high-value ketocarotenoid rarely found in plants. This was achieved by co-expression of the algal β-carotene ketolase from Chlamydomonas reinhardtii and β-carotene hydroxylase from Haematococcus pluvialis, a unique pair of enzymes identified to co-operate perfectly in converting β-carotene to astaxanthin by functional complementation in Escherichia coli. Expression of the two enzymes in tomato up-regulated most intrinsic carotenogenic genes, and efficiently directed carbon flux into carotenoids, leading to massive accumulations of mostly free astaxanthin in leaves (3.12mg/g) but esterified astaxanthin in fruits (16.1mg/g) and a 16-fold increase of total carotenoid capacity therein without affecting the plant normal growth and development. This study opened up the possibility of employing crop plants as green factories for economical production of astaxanthin....(more)
Huang JC, et al. Metab Eng 2013 May;17:59-67.
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- 23. Astaxanthin Attenuates the Apoptosis of Retinal Ganglion Cells in db/db Mice by Inhibition of Oxidative Stress.
Diabetic retinopathy is a common diabetic eye disease caused by changes in retinal ganglion cells (RGCs). It is an ocular manifestation of systemic disease, which affects up to 80% of all patients who have had diabetes for 10 years or more. The genetically diabetic db/db mouse, as a model of type-2 diabetes, shows diabetic retinopathy induced by apoptosis of RGCs. Astaxanthin is a carotenoid with powerful antioxidant properties that exists naturally in various plants, algae and seafood. Here, astaxanthin was shown to reduce the apoptosis of RGCs and improve the levels of oxidative stress markers, including superoxide anion, malondialdehyde (MDA, a marker of lipid peroxidation), 8-hydroxy-2-deoxyguanosine (8-OHdG, indicator of oxidative DNA damage) and MnSOD (manganese superoxide dismutase) activity in the retinal tissue of db/db mouse. In addition, astaxanthin attenuated hydrogen peroxide(H2O2)-induced apoptosis in the transformed rat retinal ganglion cell line RGC-5. Therefore, astaxanthin may be developed as an antioxidant drug to treat diabetic retinopathy....(more)
Dong LY, et al. Mar Drugs 2013 Mar 21;11(3):960-74.
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- 24. Sphingomicrobium astaxanthinifaciens sp. nov., an astaxanthin-producing glycolipid-rich bacterium isolated from surface seawater and emended description of the genus Sphingomicrobium.
A Gram-negative, rod-shaped, strictly aerobic, flagellated and non-spore-forming marine bacterium designated as strain CC-AMO-30BT was isolated from coastal surface seawater, Taiwan. Strain CC-AMO-30BT synthesized astaxanthin (40 μg g-1 dry weight) and formed reddish-orange-colored colonies on marine agar (Difco 2216). The strain showed highest pairwise 16S rRNA gene sequence similarity to Sphingomicrobium lutaoense CC-TBT-3T (96.4%) followed by other members of the family Sphingomonadaceae (< 94%) and established a discrete phyletic lineage associated with the former. Polar lipid profile constitutes remarkable number of unidentified glycolipids (GL1-8), in addition to diphosphatidylglycerol, phosphatidylglycerol, phosphatidylethanolamine, sphingoglycolipid and two unidentified lipids (L1-2). The major fatty acids (> 5% of total fatty acids) were C 18:1 ω7c/C 18:1 ω6c (summed feature 8), C 16:1 ω7c/C 16:1 ω6c (summed feature 3), C18:1 2-OH, C18:1 ω7c methyl, C18:1 ω7c and C16:0. DNA G+C content was 70.6%; major respiratory quinone was ubiquinone Q-10; predominant polyamine was triamine sym-homospermidine. Chemotaxonomic evidences including characteristic glycolipid profile, presence of significant amounts of C18:1 2-OH, absence of typical hydroxylated fatty acids such as C14:0 2-OH, C15:0 2-OH, and C16:0 2-OH in considerable amounts, accompanied by phylogenetic distinctiveness and several other phenotypic features support the classification of strain CC-AMO-30BT as a novel species within the genus Sphingomicrobium for which the name Sphingomicrobium astaxanthinifaciens sp. nov. is proposed; the type strain is Sphingomicrobium astaxanthinifaciens CC-AMO-30BT (= JCM 18551T = BCRC 80465T)....(more)
Shahina M, et al. Int J Syst Evol Microbiol 2013 Mar 22.
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- 25. Astaxanthin ameliorates heat stress-induced impairment of blastocyst development In Vitro: -astaxanthin colocalization with and action on mitochondria-
PURPOSE:
The effects of astaxanthin (Ax) on the in vitro development of bovine embryos cultured under heat stress were investigated in combination with the assessment of its cellular accumulation and action on mitochondrial membrane potential (ΔΨm).
METHODS:
Bovine ≥8-cell embryos were collected on day 3 after in vitro fertilization and exposed to single (day 4) or repeated (day 4 and 5) heat stress (10 h/day at 40.5 °C). Ax was added into culture medium under the repeated heat stress and blastocyst development was evaluated. The cellular uptake of Ax in embryos was examined using bright-field and confocal laser-scanning microscopy, and high-performance liquid chromatography. The relationship between Ax and mitochondria localization was assessed using MitoTracker dye. The effects of Ax on ΔΨm were investigated using JC-1 dye.
RESULTS:
Blastocyst development in the repeated heat stress treatment decreased significantly (P < 0.05) compared with those in single heat stress or normal thermal treatment. The addition of Ax into culture medium did lead to a significant recovery in blastocyst development in the repeated heat-treated group. Ax was detected in cytoplasm of embryos and observed to colocalize with mitochondria. Ax recovered ΔΨm in embryos that was decreased by the heat treatment.
CONCLUSIONS:
Ax ameliorated the heat stress-induced impairment of blastocyst development. Our results suggest that the direct action of Ax on mitochondrial activity via cellular uptake is a mechanism of the ameliorating effects....(more)
Kuroki T, et al. J Assist Reprod Genet 2013 Mar 29.
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- 26. Development of HPLC fingerprint for species differentiation and quality assessment of Rhizoma Smilacis Glabrae.
Rhizoma Smilacis Glabrae (RSG) is a commonly used herbal material in functional food and Traditional Chinese Medicine. A HPLC chromatographic fingerprint was developed for its quality control and species differentiation. Nine peaks were found in the chromatogram of RSG and all these peaks were identified by diode array detection and electrospray ionization-MS/MS: 5-O-caffeoylshikimic acid, taxifolin, engeletin, isoengeletin, trans-resveratrol, astilbin and its three stereoisomers. Six of these constituents were consistently found in 18 batches of samples. The standard fingerprint of RSG was generated by mean simulation of all tested samples. Using the standard fingerprint, RSG could be easily differentiated from Rhizoma Smilacis Chinae and Rhizoma Heterosmilacis, the two species that can be confused with RSG....(more)
Zhang QF, et al. J Nat Med 2013 Jan;67(1):207-11.
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- 27. Chemical constituents comparison between Rhizoma Smilacis Glabrae and Rhizoma Smilacis Chinae by HPLC-DAD-MS/MS.
Rhizoma Smilacis Glabrae (RSG) and Rhizoma Smilacis Chinae (RSC) are two herbal materials that belong to the same genera and are both listed in the Chinese Pharmacopoeia. Chemical constituents in the two species were compared by HPLC-DAD-MS/MS. Many common constituents were found in both species, including shikimic acid, 5-O-caffeoylshikimic acid, trans-resveratrol, taxifolin, astilbin and its three stereoisomers, engeletin and isoengeletin. However, syringic acid was found only in RSG, while chlorogenic acid was found only in RSC....(more)
Zhang QF, et al. Nat Prod Res 2013;27(3):277-81.
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- 28. Aqueous solubility and stability enhancement of astilbin through complexation with cyclodextrins.
The complexation of astilbin with α-, β-, and γ-cyclodextrin (CD) was studied by phase solubility test and UV-vis spectral titration. Complexation with CDs gradually decreased the absorbance of astilbin at 291 nm and obviously increased its water solubility. The formation constant (K(a)) between astilbin and the three CDs was calculated. The stability of astilbin complexes increased in the order α-CD < γ-CD < β-CD, attributed to the CDs' cavity size. Temperature studies showed that the K(a) value decreased along with the rise of temperature. The negative values of enthalpy and entropy during complexation indicated that the complexation process was enthalpy-controlled. In alkaline medium isomerization and decomposition of astilbin were found; however, the addition of CDs significantly improved its stability through complexation. The solubility of astilbin in β-CD microcapsules prepared by the freeze-drying method was enhanced by 122.1-fold, and its dissolution profile was improved....(more)
Zhang QF, et al. J Agric Food Chem 2013 Jan 9;61(1):151-6.
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- 29. Determination of isofraxidin and astilbin by HPLC in rat plasma and its application after orally administration the extract of Sarcandra glabra.
Sarcandra glaber is a common traditional Chinese medicine used to treat psoriasis and other infectious diseases, isofraxidin and astilbin are the main components of it. In order to study the pharmacokinetics of Sarcandra glabra, an HPLC method for simultaneous determination of isofraxidin and astilbin in rat plasma was established. Plasma samples were prepared using solid phase extraction method. C(18) column with a guard was used, mobile phase was consisted of A (methanol) and B (0.1% aqueous acetic acid) with gradient elution as follows: 0 - 4min, A: 35%, B: 65%; 4 - 10min, A: 35% - 45%, B: 65% - 55%; 10 - 20min, A: 45%, B: 55%. The flow rate was 1.2 mL/min from 0 to 4 min, 1.0 mL/min from 4 to 20 min. The detection wavelength was 300 nm. A linear correlation between drug amount and peak area was established for isofraxidin in the range of 20-320 ng and for astilbin in the range of 19-304 ng. The recovery was over 68% for both compounds, the accuracy was within 8%, and the inter-day and intra-day precisions were all less than 8%. The pharmacokinetics of isofraxidin and astilbin was studied after orally administration the extract of Sarcandra glabra....(more)
Zhao RZ, et al. Pak J Pharm Sci 2013 Jan;26(1):1-6.
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- 30. PVP and surfactant combined carrier as an effective absorption enhancer of poorly soluble astilbin in vitro and in vivo.
Abstract Context: Astilbin is considered to be a new and promising immunosuppressant for immune related diseases, but limited in clinical application due to its poor water solubility, difficult oral absorption and low bioavailability. Objective: The present work studied the effect of PVP and surfactant combined carrier on its capability to improve drug absorption. Materials and methods: PVP K30-Tween 80 combined carries was applied into the astilbin solid dispersions, tested both in vivo in beagle dogs and in vitro in transport experiments across Caco-2 cell monolayers. Results and discussion: In the animal studies a many fold increase in plasma AUC was observed for the solid dispersions of drug in PVP K30-Tween 80 combined carries compared to active pharmaceutical ingredient (API). The applicability of Caco-2 monolayers as a tool for predicting the in vivo transport behavior of Astilbin in combination with a solubility enhancing carries was shown. In vitro transport studies confirmed the effect of combined carries on the absorption behavior of the astilbin. MTT studies showed the cell viability gradually decreased with the increase of the drug concentration in a dose dependent manner for astilbin and that in solid dispersions. The permeability and apparent permeability coefficients (P(app)) increased with drug in the Caco-2 cell. Conclusion: In this study, it was found that PVP K30 and Tween 80 promoted the permeability of drugs best within a certain amount. For astilbin PVP K30 and surfactant combined carrier had a strong potential to improve oral bioavailability....(more)
He Y, et al. Drug Dev Ind Pharm 2013 Jan 28.
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- 31. Macrophage biospecific extraction and HPLC-ESI-MSn analysis for screening immunological active components in Smilacis Glabrae Rhizoma.
A cell-permeable membrane, as typified by Transwell insert Permeable Supports, permit accurate repeatable invasion assays, has been developed as a tool for screening immunological active components in Smilacis Glabrae Rhizoma (SGR). In this research, components in the water extract of SGR (ESGR) might conjugate with the receptors or other targets on macrophages which invaded Transwell inserts, and then the eluate which contained components biospecific binding to macrophages was identified by HPLC-ESI-MS(n) analysis. Six compounds, which could interact with macrophages, were detected and identified. Among these compounds, taxifolin (2) and astilbin (4) were identified by comparing with the chromatography of standards, while the four others including 5-O-caffeoylshikimic acid (1), neoastilbin (3), neoisoastilbin (5) and isoastilbin (6), were elucidated by their structure clearage characterizations of tandem mass spectrometry. Then compound 1 was isolated and purified from SGR, along with 2 and 4, was applied to the macrophage migration and adhesion assay in HUVEC (Human Umbilical Vein Endothelial Cells) -macrophages co-incultured Transwell system for immunological activity assessment. The results showed that compounds 1, 2 and 4 with concentration of 5μM (H), 500nM (M) and 50nM (L) could remarkably inhibit the macrophage migration and adhesion (Vs AGEs (Advanced Glycation End Produces) group, 1-L, 2-H and 4-L groups: p<0.05; other groups: p<0.01). Moreover, 1 and 4 showed satisfactory dose-effect relationship. In conclusion, the application of macrophage biospecific extraction coupled with HPLC-ESI-MS(n) analysis is a rapid, simple and reliable method for screening immunological active components from Traditional Chinese Medicine....(more)
Zheng ZG, et al. J Pharm Biomed Anal 2013 Apr 15;77:44-8.
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- 32. Preparative separation of flavonoids in plant extract of Smilacis Glabrae Roxb. by high performance counter-current chromatography.
Four flavonoids, isoastilbin, astilbin, isoengelitin, and engelitin were isolated and purified simultaneously from Smilacis Glabrae Roxb. for the first time by high performance counter-current chromatography using a system consisting of n-hexane-n-butanol-water (1:2:3, v/v/v). A total of 392.6 mg of astilbin, 71.4 mg of isoastilbin, 47.4 mg of engelitin, and 10.3 mg of isoengelitin were purified from 1.89 g of the ethyl acetate extract of Smilacis Glabrae Roxb. in six runs, each at over 94.51% purity as determined by HPLC. The structures of the four compounds were identified by their retention time, the LC-ESI-MS<sup>n</sup> in the negative ion mode, and confirmed by <sup>1</sup> H-NMR experiments. The characteristic LC-ESI-MS fragmentation patterns of the four compounds were discussed....(more)
Zhang H, et al. J Sep Sci 2013 Mar 26.
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- 33. Chemical constituents derived from Drimys brasiliensis Miers (Winteraceae).
Phytochemical investigation on Drimys brasiliensis afforded the isolation and characterisation of four drimane sesquiterpenes: polygodial (1), warburganal (2), 1-β-(p-coumaroyloxy)polygodial (3) and 1-β-(p-methoxycinnamoyl)polygodial (4), as well as four flavonoids: quercitrin (5), astilbin (6), isoastilbin (7) and neoastilbin (8). The structures were elucidated on the basis of their spectral data and compared with those reported in the literature. Compounds 2, 5-8 have been reported to occur for the first time in D. brasiliensis, while compounds 5, 7 and 8 have been reported to occur for the first time in the genus Drimys. The chemotaxonomic significance of these compounds, mainly flavonoids 5-8 in D. brasiliensis, was summarised....(more)
Mecchi MC, et al. Nat Prod Res 2013 Mar 28.
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- 34. Astilbin inhibits proliferation of rat aortic smooth muscle cells induced by angiotensin II and down-regulates expression of protooncogene.
This study examined the effect of astilbin on the proliferation of rat aortic smooth muscle cells (RASMCs) induced by angiotensin II (AngII) and explored the possible mechanisms. Cell proliferation model of RASMCs was induced by treatmente with AngII. Cells were randomly divided to 8 groups. Normally cultured VSMCs serves as blank control group; in AngII model group, cells were treated with AngII at 10(-7) mol/L; in three astilbin groups, cells were treated with 10, 15, 30 mg/L of astilbin; in three AngII+astilbin groups, cells were treated with AngII (at 10(-7) mol/L) and astilbin at 10, 15, 30 mg/L. Cell proliferation ability was detected by MTT method and the cell cycles and proliferation index were flow cytometrically determined. The expression of c-myc mRNA was assessed by using reverse transcription polymerase chain reaction (RT-PCR), and the expression of NF-κB in RASMCs was immunocytochemically observed. Our results showed that MTT metabolism in RASMCs in the basic and AngII stimulated situation was inhibited by astilbin, and the cells numbers of G(0)/G(1) phase were increased and that of G(2)/S phase were decreased markedly. Not only highly expression of c-myc gene stimulated by AngII could be inhibited by Astilbin significantly, but also the expression of NF-κB protein can be down regulated by Astilbin. We are led to conclude that astilbin astilbin can inhibit the AngII-mediated proliferation of RASMCs by blocking the transition of RASMCs from G(0)/G(1) phase to S phase and by down-regulating the expression of NF-κB, c-myc gene....(more)
Li P, et al. J Huazhong Univ Sci Technolog Med Sci 2012 Apr;32(2):181-5.
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- 35. Nuciferine stimulates insulin secretion from beta cells-an in vitro comparison with glibenclamide.
ETHNOPHARMACOLOGICAL RELEVANCE:
Several Asian plants are known for their anti-diabetic properties and produce alkaloids and flavonoids that may stimulate insulin secretion.
/>MATERIALS AND METHODS:
Using Vietnamese plants (Nelumbo nucifera, Gynostemma pentaphyllum, Smilax glabra, and Stemona tuberosa), we extracted two alkaloids (neotuberostemonine, nuciferine) and four flavonoids (astilbin, engeletin, smitilbin, and 3,5,3'-trihydroxy-7,4'-dimethoxyflavone), and studied their insulin stimulatory effects.
RESULTS:
Nuciferine, extracted from Nelumbo nucifera, stimulated both phases of insulin secretion in isolated islets, whereas the other compounds had no effect. The effect of nuciferine was totally abolished by diazoxide and nimodipine, and diminished by protein kinase A and protein kinase C inhibition. Nuciferine and potassium had additive effects on insulin secretion. Nuciferine also stimulated insulin secretion in INS-1E cells at both 3.3 and 16.7 mM glucose concentrations. Compared with glibenclamide, nuciferine had a stronger effect on insulin secretion and less beta-cell toxicity. However, nuciferine did not compete with glibenclamide for binding to the sulfonylurea receptor.
CONCLUSIONS:
Among several compounds extracted from anti-diabetic plants, nuciferine was found to stimulate insulin secretion by closing potassium-adenosine triphosphate channels, explaining anti-diabetic effects of Nelumbo nucifera.
Copyright © 2012 Elsevier Ireland Ltd. All rights reserved....(more)
Nguyen KH, et al. J Ethnopharmacol 2012 Jul 13;142(2):488-95.
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