- 1. Assessment of plant lectin antifungal potential against yeasts of major importance in medical mycology.
The search for new compounds with antifungal activity is accelerating due to rising yeast and fungal resistance to commonly prescribed drugs. Among the molecules being investigated, plant lectins can be highlighted. The present work shows the potential of six plant lectins which were tested in vitro against yeasts of medical importance, Candida albicans, Candida tropicalis, Candida parapsilosis, Cryptococcus gattii, Cryptococcus neoformans, Malassezia pachydermatis, Rhodotorula sp. and Trichosporon sp. Broth microdilution susceptibility testing was performed in accordance with standard protocols to evaluate antifungal activity. Minimum inhibitory concentration (MIC) was determined at 80% yeast growth inhibition, whereas the minimum fungicidal concentration (MFC) was evaluated after making the subcultures of each dilution. Only C. parapsilosis growth was inhibited by the lectins tested. Abelmoschus esculentus lectin showed the highest MIC (0.97 μg ml(-1)). Lectins from Canavalia brasiliensis, Mucuna pruriens and Clitoria fairchildiana presented the highest MFC at (3.90 μg ml(-1)). These results encourage further studies with wider yeast strain selections, and open new perspectives for the development of pharmacological molecules....(more)
Klafke GB, et al. Mycopathologia 2013 Feb;175(1-2):147-51.
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- 2. Effect of Mucuna pruriens (Linn.) on mitochondrial dysfunction and DNA damage in epididymal sperm of streptozotocin induced diabetic rat.
ETHNOPHARMACOLOGICAL RELEVANCE:
Mucuna pruriens Linn. (M. pruriens) is a leguminous plant that has been recognized as an herbal medicine for improving fertility and related disorders in the Indian traditional system of medicine, however without proper scientific validations.
AIM OF THE STUDY:
To study the effect of ethanolic seed extract of M. pruriens on mitochondrial dysfunction and the DNA damage in hyperglycemic rat epididymal spermatozoa.
MATERIALS AND METHODS:
Male Wistar albino rats were divided as control (Sham), diabetes induced [streptozotocin 60 mg/kg of body weight (b.w.) in 0.1M citrate buffer] (STZ), diabetic rats administered with 200mg/kg b.w. of extract (STZ+MP) and normal rats administered with 200mg/kg b.w. of extract (Sham+MP). M. pruriens was administered (gavage) once daily for a period of 60 days. On 60th day animals were sacrificed by cervical dislocation sperm were collected from epididymis and subjected various analysis like antioxidants, ROS, lipid peroxidation (LPO), DNA damage, chromosomal integrity and mitochondrial membrane potential (MMP).
RESULTS:
Significant reduction in the sperm count, motility, viability and significant increase in the number of abnormal sperm in STZ compared to sham was noticed. STZ rat sperm showed significant increase in LPO and DNA damage. Both the enzymic and non-enzymic were decreased; MMP and the mitochondrial functions were severely affected in STZ group. The diabetic rats supplemented with M. pruriens showed a remarkable recovery in antioxidant levels and reduced LPO with well preserved sperm DNA. MMP and mitochondrial function test were also preserved in STZ+MP rat sperm.
CONCLUSION:
The present study has clearly demonstrated the potency of M. pruriens to reduce the diabetic induced sperm damage induced by oxidative stress (OS). These observations are encouraging to perform similar studies in human.
Copyright © 2012 Elsevier Ireland Ltd. All rights reserved....(more)
Suresh S, et al. J Ethnopharmacol 2013 Jan 9;145(1):32-41.
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- 3. Screening for Rho-kinase 2 inhibitory potential of Indian medicinal plants used in management of erectile dysfunction.
THE AIM OF THE STUDY:
Activation of Rho-kinase 2 (ROCK-II) results in contraction of corpus cavernosum smooth muscle and ROCK-II inhibitors relax corpus cavernosum in vitro and in vivo hence, plant extracts capable of inhibiting ROCK-II enzyme may be useful in management of erectile dysfunction (ED). The aim of the study was to screen selected Indian medicinal plants, having similar ethnopharmacological use for ROCK-II inhibition.
MATERIALS AND METHODS:
Some Indian medicinal plants reported as aphrodisiacs in Ayurveda and modern scientific literature were collected, authenticated and extracted. Direct methanol and successive aqueous extracts of these plants were screened for ROCK-II inhibitory activity using HTRF(®)KinEASE™ STK S2 Kit (Cisbio Bioassays). Relaxant effect of potent extract was recorded on isolated rat corpus cavernosum.
RESULTS:
Methanolic and successive aqueous extracts of 30 plants were screened for ROCK-II inhibition and 15 herbal extracts showed inhibition ranging between 50 and 88% at 50 μg/mL. While IC(50) of Y-27632, a standard ROCK-II inhibitor, was found to be 163.8 ± 1.2 nM. The Methanolic extract of Terminalia chebula (METC) with IC(50) value of 6.09 ± 0.17 μg/mL was found to be most potent and relaxed isolated rat corpus cavernosum significantly (p<0.01). Chebulagic and chebulinic acid of METC were found to inhibit ROCK-II and might be responsible for the inhibitory potential of the extract. The traditional use of plants like Butea frondosa, Syzygium aromaticum, Butea superba, Chlorophytum borivilianum and Mucuna pruriens, as aphrodisiacs and for male sexual disorder (MSD) might be in part due to the ROCK II inhibitory potential of these plants.
CONCLUSION:
Some of the Indian medicinal plants have ROCK-II inhibitory potential and those deserve further investigation.
Copyright © 2012 Elsevier Ireland Ltd. All rights reserved....(more)
Goswami SK, et al. J Ethnopharmacol 2012 Dec 18;144(3):483-9.
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- 4. Cytoprotective activity of mulberry leaf extract against oxidative stress-induced cellular injury in rats.
Morus alba Linn. (MA), mulberry leaves have been used as a beverage for prevention of various diseases including hyperlipidemia and hyperglycemia. Recently, the antioxidant activities of the MA leaf extract have been reported. The objective of this study was to investigate the effect of the MA leaf extract on free radical-induced cellular injury. In the in vitro models, the extract scavenged stable free radical (1, 1-diphenyl-2-picrylhydrazyl; DPPH) in a concentration-dependent manner with an IC(50) of 20.10 ± 0.78 μ g/ml. The extract protected the erythrocytes from free radical (2, 2'-azobis (2-amidinopropane) dihydrochloride; AAPH)-induced hemolysis with an IC(50) of 74.22 ± 9.87 μg/ml. Additionally, the extract significantly prevented the gastric mucosal injury induced by ischemia-reperfusion (I/R) in rats when given orally at doses of 0.25 and 0.50 g/kg/day for 3 consecutive days (p < 0.05; n=7). However, this effect was not found when the higher doses (1 and 2 g/kg/day) of the extract were tested. In conclusion, these results indicate that the MA leaf extract possesses the cytoprotective activity against free radical-induced cell injury. Therefore, when given at the appropriate dose range, the mulberry leaf may potentially be used as a food supplement in patients with certain diseases in which the oxidative stress-induced cellular injury is pathologically involved....(more)
Jaruchotikamol A, et al. Pak J Pharm Sci 2013 Jan;26(1):163-8.
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- 5. Mulberry Leaf Extract Inhibits the Development of Atherosclerosis in Cholesterol-Fed Rabbits and in Cultured Aortic Vascular Smooth Muscle Cells.
This study used high-cholesterol-fed New Zealand white rabbits and aortic vascular smooth muscle cells (VSMCs) to investigate the impact of mulberry leaf extract (MLE) on the development of atherosclerosis. The results show that the major components of MLE are polyphenols, flavonoids, carbohydrates, proteins, and lipids, and the major contituents of mulberry leaf polyphenol extract (MLPE) are polyphenols and flavonoids. In addition to improvement of liver function, the atheroma burden and levels of serum cholesterol, triglycerides, and low-density lipoprotein (LDL) are also significantly reduced after MLE treatment. MLE and MLPE improved endothelial function, inhibited proliferation and migration of aortic VSMCs, and reduced atheromas in the vascular wall. In conclusion, this study demonstrates that, in addition to exerting hypolipidemic effects, MLE and MLPE can effectively inhibit proliferation and migration of aortic VSMCs, improve vascular endothelial function, and reduce atheroma burden, thereby preventing atherosclerosis....(more)
Chan KC, et al. J Agric Food Chem 2013 Mar 1.
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- 6. Mulberry Leaf Extract Inhibits Invasive Potential and Downregulates Hypoxia-Inducible Factor-1α (HIF-1α) in SK-N-BE(2)C Neuroblastoma Cells.
A neuroblastoma is an extracranial solid tumor diagnosed in childhood. Since tumor metastasis is the main cause of death for most neuroblastoma patients, an understanding of the mechanisms that modulate cancer cell invasion is a key to developing more effective chemotherapeutic agents. In the current study, we examined to determine whether mulberry leaf (ML) extract effectively inhibits the invasion potential of neuroblastoma cells in vitro. ML extract was found to suppress cell invasiveness as well as the activity and expression of matrix metalloproteinase-2 (MMP-2) under both normoxia and hypoxia in neuroblastoma. ML extract downregulated the expression of hypoxia-inducible factor-1α (HIF-1α), a well-known regulator of tumor metastasis, and its downstream targets, vascular endothelial growth factor (VEGF) and glucose transporter-1 (GLUT-1). Taken together, these results suggest that ML extract has chemotherapeutic effects on neuroblastoma cells by regulating invasion potential, thereby controlling the metastasis of neuroblastomas....(more)
Park S, et al. Biosci Biotechnol Biochem 2013 Apr 23;77(4):722-8.
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- 7. Mulberry leaf extract increases adiponectin in murine 3T3-L1 adipocytes.
We have previously shown that mulberry leaf extract (MA) causes blood glucose levels to decrease in rats with streptozotocin-induced diabetes while enhancing glucose uptake by isolated fat cells. We hypothesized that the antidiabetic activity of MA is mediated via enhancement of adiponectin secretion and adipogenesis, which consequently decreases blood glucose. In the present study, we aimed to elucidate the molecular basis for the observed antidiabetic activity using murine 3T3-L1 preadipocyte cultures. We found that treatment of differentiating 3T3-L1 cells with MA at concentrations of 5, 15, and 45 μg/mL increased expression of adiponectin messenger RNA from 1.4-fold (control) to 1.5-, 1.95-, and 2.2-fold above basal values, respectively, while causing adiponectin secretion to increase from 70 ± 7.4 ng/mL to 100 ± 1.4, 138 ± 2.0, and 176 ± 21.4 ng/mL, respectively. Furthermore, we observed an increase in both lipid accumulation and messenger RNA expression of transcription factors, such as CCAAT/enhancer-binding protein α and peroxisome proliferator-activated receptor γ; and of the fatty acid-binding protein aP2 in differentiated 3T3-L1 cells pretreated with MA. Our findings indicate that the stimulatory effects of mulberry leaf extract on adipocyte proliferation and differentiation likely occur through up-regulation of adipogenic transcription factors and downstream gene expression. Such effects of mulberry leaf extract on adiponectin secretion and adipocyte activity may account for, at least in part, the antidiabetic effects of consumption of beverages containing mulberry leaves....(more)
Naowaboot J, et al. Nutr Res 2012 Jan;32(1):39-44.
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- 8. Mulberry leaf extract stimulates glucose uptake and GLUT4 translocation in rat adipocytes.
Mulberry (Morus alba L.) leaf tea is promoted for its health benefits and the control of diabetes in Asian nations. The blood glucose lowering activity of mulberry leaf extract (MA) has been proven; however, the molecular basis underlying this effect remains unclear. The aim of the present work is to elucidate its mechanism of the antihyperglycemic action, by examining the effect of MA on glucose uptake and the translocation of glucose transporter 4 protein (GLUT4) to the plasma membrane of adipocytes isolated from diabetic rats. The incubation of adipocytes with 5-45 μg/ml MA resulted in 31-54% increase of glucose uptake in a dose-dependent manner. This glucose uptake enhancing effect was inhibited by the phosphoinositol 3-kinase (PI3-K) inhibitor, wortmannin (100 nM). The GLUT4 protein on the plasma membrane fraction of adipocytes was markedly increased after treatment with 15 μg/ml MA extract. Interestingly, gallic acid, one of the phenolic compounds found in MA extract, increased glucose uptake and enhanced the translocation of GLUT4 at concentrations comparable to the amount of gallic acid in the effective concentration ranges of MA. Thus, it is likely that gallic acid contributes, at least in part, to its antihyperglycemic activity. The present results suggest that the antihyperglycemic action of MA is mediated by increasing glucose uptake via the activation of PI3-K signaling pathway and translocation of GLUT4 to the plasma membrane. These findings are the first molecular evidence supporting the mulberry tea as herbal medicine for diabetic patients....(more)
Naowaboot J, et al. Am J Chin Med 2012;40(1):163-75.
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- 9. Screening α-glucosidase inhibitors from mulberry extracts via DOSY and relaxation-edited NNR.
Inhibition of the α-glucosidase activity is a therapeutic approach for diabetes. In this study, an effective strategy for screening α-glucosidase inhibitors based on Nuclear magnetic resonance (NMR) techniques was developed to screen and identify α-glucosidase inhibitors from Mulberry leaf extract. As a result, deoxynojirimycin, as a potential α-glucosidase inhibitor, was found. The study suggested that our strategy was a powerful tool for screening and identification of α-glucosidase inhibitors in complex samples. Furthermore the interaction between α-glucosidase and its inhibitor was studied by NMR....(more)
Shang Q, et al. Talanta 2012 Aug 15;97:362-7.
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- 10. Mulberry leaf extract inhibits cancer cell stemness in neuroblastoma.
Emerging evidence proposes that most cancers originate from a rare subpopulation of cells, called cancer stem cells (CSCs), which possess characteristics including differentiation, self-renewal, and tumorigenicity. Currently, available therapeutic agents cannot effectively eliminate CSCs. Therefore, the development of a nontoxic, natural treatment that can either overcome chemoresistance or promote the elimination of CSCs is highly desirable. The current study examined whether mulberry leaf (ML) ethanolic extract can effectively eliminate neuroblastoma stem cell-like population. Our data demonstrated that 10-40 μg/ml of ML extract significantly enhanced differentiation by elongating neurites and reducing clonogenicity and sphere formation as shown by the decreased expression of stem cell markers and increased expression of differentiation markers. The knock-down of delta-like 1 homologue by siRNA enhanced the significant inhibitory effects of 40 μg/ml of ML extract on colony formation. Furthermore, phosphorylation of the extracellular signal-regulated kinase (ERK) was increased by 20 or 40 μg/ml of ML extract and the MEK/ERK inhibitors completely blocked differentiation induced by the extract. Taken together, these findings provide experimental evidence that ML may have chemopreventive effects on neuroblastoma cells by inhibiting CSCs characteristics as well as regulating CSCs pathways, which may provide a therapeutic option for controlling the growth of neuroblastoma cells....(more)
Park S, et al. Nutr Cancer 2012 Aug;64(6):889-98.
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- 11. Comparison of 1-deoxynojirimycin and aqueous mulberry leaf extract with emphasis on postprandial hypoglycemic effects: in vivo and in vitro studies.
Carbohydrate digestion by α-glucosidase and subsequent glucose uptake at the brush border are critical for postprandial blood glucose control. Any specific inhibitors are useful as hyperglycemia modulating agents. In this study, it was postulated that an array of active components in mulberry leaf extract (MLE) may provide higher potency in inhibiting intestinal glucose absorption compared to the single component 1-deoxynojirimycin (DNJ), which is recognized as a promising inhibitor of intestinal glucose absorption. Both MLE and DNJ were active in inhibiting α-glucosidase. However, in Caco-2 cells, only MLE showed significant inhibition of 2-deoxyglucose uptake, whereas DNJ was ineffective. For glucose loading, co-administration of MLE resulted in potent inhibitions of glucose responses compared to those by DNJ in Sprague Dawley (SD) rats, but this was not found for maltose loading. These novel findings add evidence that the unabsorbed phytochemicals in MLE compete with glucose for intestinal glucose transporters, but DNJ itself does not. We also evaluated the timing of MLE consumption. By administering MLE for 30 min before glucose loading, the incremental area under the curve (IAUC) was significantly lowered in the rats, as compared to a simultaneously administered group. Similarly, cellular glucose uptake was significantly reduced in Caco-2 cells following pretreatment....(more)
Kwon HJ, et al. J Agric Food Chem 2011 Apr 13;59(7):3014-9.
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- 12. Mulberry leaf extract reduces postprandial hyperglycemia with few side effects by inhibiting α-glucosidase in normal rats.
Mulberry (Morus alba L.) leaf extract (MLE) was investigated as a potent plant-derived α-glucosidase inhibitor with low α-amylase inhibitory activity. MLE was prepared by heating in an autoclave at 121 °C for 15 minutes, and its in vitro and in vivo antihyperglycemic activities were investigated. The adverse side effects of MLE were analyzed by measuring the weight and volume of the cecum, stool color, starch content in the cecum, and the integrity of intestinal transporting capacity. The in vitro inhibitory activity of MLE on intestinal α-glucosidase was potent and that on intestinal α-amylase was very weak compared with acarbose. Sugar loading tests with starch, maltose, and sucrose showed that MLE may reduce postprandial increases in blood glucose by acting as an intestinal α-glucosidase inhibitor. Feeding tests suggested that MLE may exhibit fewer adverse side effects than other α-glucosidase inhibitors, such as abdominal flatulence and meteorism, which are attributed to the impaired digestion of starch by strong inhibition of intestinal α-amylase. These results suggest that MLE could be used in the development of pharmaceutical foods to control the blood glucose levels of diabetic patients by inhibiting intestinal α-glucosidase with reduced side effects....(more)
Kim GN, et al. J Med Food 2011 Jul-Aug;14(7-8):712-7.
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- 13. Polyphenol-rich extract from mulberry leaf inhibits vascular smooth muscle cell proliferation involving upregulation of p53 and inhibition of cyclin-dependent kinase.
This study was carried out to investigate the impact of polyphenol-rich extract from mulberry leaf on the proliferation of vascular smooth muscle cell (VSMC) and verify its mechanism in vitro. VSMC proliferation is an important pathophysiological process in the development of atherosclerosis, which is the major cause of coronary artery disease (CAD). Polyphenol-rich foods, such as mulberry leaf, have been reported to reduce the risk of CAD. The effect of mulberry leaf extract (MLE) on cell growth was measured by a growth curve assay, on distribution of cells in the cell cycle by flow cytometry, and on cyclin-dependent kinase (CDK) activity and cell-cycle regulatory proteins by Western blot, immunoblotting, and immunoprecipitation analyses. The results showed that MLE induced phosphorylation of p53, promoted expression of p21 and p27, decreased CDK2/4 activity, inhibited phosphorylation of Rb, and thereby blocked the G1 to S transition in the cell cycle....(more)
Chan KC, et al. J Agric Food Chem 2010 Feb 24;58(4):2536-42.
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- 14. Myricetin Induces Apoptosis in Hepg2 Cells through Akt/P70s6k/Bad Signaling and Mitochondrial Apoptotic Pathway.
The present investigation was undertaken to gain insight into the molecular mechanism by which myricetin induces apoptosis in human hepatocarcinoma HepG2 cells. Myricetin caused the disruption of mitochondrial membrane potential in a dose-dependent manner. Moreover, myricetin triggered translocation of the pro-apoptotic protein Bax to the mitochondria, downregulation of anti-apoptotic Bcl-2 expression and upregulated the expression of pro-apoptotic protein Bad in the mitochondria. The present study also showed that myricetin promoted the release of cytochrome C from mitochondria into the cytosol followed by an increase in the proteolytic activation of caspase-3 and the concomitant degradation of PARP protein. Additionally, western blot analysis showed that the Akt/p70s6k1 pathway was inhibited in myricetin-treated HepG2 cells, accordingly the phosphorylation of Bad at Ser136 was downregulated. Collectively, these findings indicate that myricetin induced apoptosis in HepG2 cell through mitochondria apoptotic pathway and Akt/p70s6k1/Bad signaling. Present results provide new information on the possible mechanisms for the anti-cancer activity of myricetin....(more)
Zhang XH, et al. Anticancer Agents Med Chem 2013 Feb 7.
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- 15. Antioxidant Rich Morus alba leaf Extract Induces Apoptosis in Human Colon and Breast Cancer Cells by the Downregulation of Nitric Oxide Produced by Inducible Nitric Oxide Synthase.
Morus species had been used widely in the traditional medicines for various diseases. In this study we report the in vitro antiproliferative activity of the methanol extract of Morus alba. The extract is capable of inducing cytotoxicity in human colon cancer (HCT-15) cells (IC(50) = 13.8 μg/ml) and breast cancer (MCF-7) cells (IC(50) = 9.2 μg/ml), resulted in significant morphological changes of the cells, fragmentation of DNA, and caspase-3 activation- characteristics of apoptosis. It downregulated the amount of nitric oxide (NO) produced as a result of inducible nitric oxide (iNOS) activation. The HPLC analysis of the extract showed epicatechin (20%), myricetin (10%), quercetin hydrate (12%), luteolin (12%), and kaempferol (6%) as the major active components and ascorbic acid, gallic acid, pelargonidine, and p-coumaric acid as the minor components. To the best of our knowledge, this is the first report showing the downregulation of iNOS and induction of apoptosis by M. alba extract....(more)
Deepa M, et al. Nutr Cancer 2013 Feb;65(2):305-10.
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- 16. Effect of emulin on blood glucose in type 2 diabetics.
Emulin™ is a patented blend of chlorogenic acid, myricetin, and quercetin that has shown efficacy in reducing midday and post-oral glucose tolerance test (OGTT) area under the curve (AUC) glucose in streptozotocin-treated rats. The purpose of this study was to determine if similar effects would be evident in type 2 diabetic humans. Forty human subjects with confirmed type 2 diabetes (10 each in 4 groups: placebo/no medication, Emulin/no medication, placebo/metformin and Emulin/metformin) were evaluated. At the end of 1 week, fasting blood glucose, 2 h postprandial, actual peak glucose, and AUC (post-50 g OGTT) were determined. The placebo-only group had a large (5%-13%) increase in all parameters. The Emulin group and those on metformin performed similarly with reductions between 1% and 5%, with Emulin slightly outperforming the medication-alone group. The most significant reduction occurred in the Emulin/metformin group, with decreases in the parameters by up to 20%. These results suggest that Emulin, if consumed regularly, could not only have the acute effect of lowering the glycemic impact of foods, but chronically lower background blood glucose levels of type 2 diabetics....(more)
Ahrens MJ, et al. J Med Food 2013 Mar;16(3):211-5.
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- 17. Evaluation of alcohol-based deep eutectic solvent in extraction and determination of flavonoids with response surface methodology optimization.
Deep eutectic solvents (DESs) are emerging rapidly as a new type of green solvent instead of an ionic liquid (IL), and are typically formed by mixing choline chloride with hydrogen bond donors. Few studies have applied DESs to the extraction and determination of bioactive compounds. Therefore, in the present study, DESs were used to extract flavonoids (myricetin and amentoflavone), which are well known and widely used antioxidants, to extend their applications. A range of alcohol-based DESs with different alcohols to choline chloride (ChCl) mixing ratios were used for extraction using several extraction methods. Other factors, such as temperature, time, water addition and solid/liquid ratio, were examined systematically using a response surface methodology (RSM). A total of 0.031 and 0.518 mg g(-1) of myricetin and amentoflavone were extracted under the optimized conditions: 35 vol% of water in ChCl/1,4-butanediol (1/5) at 70.0 °C for 40.0 min and a solid/liquid ratio of 1/1 (g 10 mL(-1)). Good linearity was obtained from 0.1 × 10(-3) to 0.1 mg mL(-1) (r(2)>0.999). The excellent properties of DESs highlight their potential as promising green solvents for the extraction and determination of a range of bioactive compounds or drugs....(more)
Bi W, et al. J Chromatogr A 2013 Apr 12;1285:22-30.
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- 18. Identification of novel dietary phytochemicals inhibiting the efflux transporter breast cancer resistance protein (BCRP/ABCG2).
Breast cancer resistance protein (BCRP/ABCG2) plays an important role in determining the absorption and disposition of consumed xenobiotics including various drugs and dietary phytochemicals and is also one of the prominent efflux transporters involved in multidrug resistance (MDR). In this study, we have investigated the interactions between ABCG2 and 56 naturally-occurring phytochemicals including phenolic acids, flavonoids, triterpenes and other common dietary phytochemicals, as well as two non plant-based compounds (hippuric acid and propyl gallate) using cell- and membrane-based transport inhibition assays. Of the non-flavonoid phytochemicals tested, berberine, celastrol, ellagic acid, limonin, oleanolic acid, propyl gallate, sinapic acid and ursolic acid demonstrated significant inhibition of ABCG2-mediated transport. Chrysoeriol, laricitrin, myricetin 3',4',5'-trimethylether, pinocembrin, quercitrin, tamarixetin, tricetin and tricetin 3',4',5'-trimethylether were also identified as novel flavonoid ABCG2 inhibitors. The identified inhibitory activity of dietary phytochemicals on ABCG2 provides a framework for further investigation of ABCG2-modulated phytochemical bioavailability, MDR, and possible food-drug interactions....(more)
Tan KW, et al. Food Chem 2013 Jun 15;138(4):2267-74.
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- 19. Analysis of flavonoids and the flavonoid structural genes in brown fiber of upland cotton.
BACKGROUD:
As a result of changing consumer preferences, cotton (Gossypium Hirsutum L.) from varieties with naturally colored fibers is becoming increasingly sought after in the textile industry. The molecular mechanisms leading to colored fiber development are still largely unknown, although it is expected that the color is derived from flavanoids.
EXPERIMENTAL DESIGN:
Firstly, four key genes of the flavonoid biosynthetic pathway in cotton (GhC4H, GhCHS, GhF3'H, and GhF3'5'H) were cloned and studied their expression profiles during the development of brown- and white cotton fibers by QRT-PCR. And then, the concentrations of four components of the flavonoid biosynthetic pathway, naringenin, quercetin, kaempferol and myricetin in brown- and white fibers were analyzed at different developmental stages by HPLC.
RESULT:
The predicted proteins of the four flavonoid structural genes corresponding to these genes exhibit strong sequence similarity to their counterparts in various plant species. Transcript levels for all four genes were considerably higher in developing brown fibers than in white fibers from a near isogenic line (NIL). The contents of four flavonoids (naringenin, quercetin, kaempferol and myricetin) were significantly higher in brown than in white fibers and corresponding to the biosynthetic gene expression levels.
CONCLUSIONS:
Flavonoid structural gene expression and flavonoid metabolism are important in the development of pigmentation in brown cotton fibers....(more)
Feng H, et al. PLoS One 2013;8(3):e58820.
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- 20. Virtual and in vitro bioassay screening of phytochemical inhibitors from flavonoids and isoflavones against xanthine oxidase and cyclooxygenase-2 for gout treatment.
Synthetic drugs such as allopurinol and benzbromarone are commonly used to treat the complex pathogenesis of gout, a metabolic disease that results from an inflammation of the joints caused by precipitation of uric acid. We seek to discover novel phytochemicals that could treat gout, by targeting the xanthine oxidase and cyclooxygenase-2 enzymes. In this study, we report the screening of nine compounds of flavonoids from the ZINC and PubChem databases (containing 2092 flavonoids) using the IGEMDOCK software tool against the xanthine oxidase and cyclooxygenase-2 3D protein structures. Each compound was also evaluated by an in vitro bioassay testing the inhibition of xanthine oxidase and cyclooxygenase-2. Myricetin and luteolin were found to be the potential dual inhibitors of xanthine oxidase and cyclooxygenase-2 as demonstrated by IC(50): 62.7 and 3.29 μg/mL (xanthine oxidase)/70.8 and 16.38 μg/mL (cyclooxygenase-2), respectively. In addition, structure-activity relationships and other important factors of the flavonoids binding to the active site of xanthine oxidase and cyclooxygenase-2 were discussed, which is expected for further rational drug design....(more)
Li Y, et al. Chem Biol Drug Des 2013 Apr;81(4):537-44.
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- 21. New Inhibitors of ROS Generation and T-Cell Proliferation from Myrtus communis.
Phytochemical investigation on Myrtus communis Linn. afforded myrtucommuacetalone (1) with an unprecedented carbon skeleton and a new phloroglucinol-type compound, myrtucommulone M (2), along with four known constituents 3-6. Their structures were established by extensive analyses of NMR and mass spectral data as well as by single-crystal X-ray diffraction studies. These constituents were evaluated for their ability to modulate the immune response, based on their effects on various components of immune system. Compounds 1 and 5 exhibited significant inhibitory effect against nitric oxide (NO<sup>•</sup>) production. Compound 1 also exhibited significant antiproliferative activity (IC50 < 0.5 μg/mL) against T-cell proliferation. Myricetin (3) exerted a significant inhibition (IC50 = 1.6 μg/mL) on zymosan-stimulated whole blood phagocytes ROS production. Compounds 1 and 3 were active against PMA-stimulated ROS generation....(more)
Choudhary MI, et al. Org Lett 2013 Apr 19;15(8):1862-1865.
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- 22. Flavonols enhanced production of anti-inflammatory substance(s) by Bifidobacterium adolescentis: Prebiotic actions of galangin, quercetin, and fisetin.
The gut microbiota is capable of the bioconversion of flavonoids whereas influences of probiotic anaerobes on the bioactivities of flavonoids and vice versa are still unclear. Here, we investigated functional interactions with respect to the anti-inflammatory activity between flavonols and probiotic bacteria. Ten enteric (6 probiotic and 4 indigenous) bacteria were incubated with flavonols (galangin, kaempferol, quercetin, myricetin, and fisetin) under anaerobic conditions, and the supernatants were assessed for their effects on nitric oxide (NO) production in lipopolysaccaride-stimulated RAW264 cells. Although the conditioned medium from the flavonol mono-culture and almost all of the tested co-cultures failed to inhibit NO production, the medium from the Bifidobacterium adolescentis/flavonols (galangin, quercetin, and fisetin) co-culture highly suppressed NO production. This activity increased during the 1-6 H incubation in a time-dependent manner and was not observed in the co-culture using heat-inactivated B. adolescentis. Interestingly, when the B. adolescentis cell number was increased, the supernatant from the mono-culture of the bacteria showed NO suppression, suggesting that B. adolescentis may produce NO suppressant(s), and flavonols may have a promoting effect. These findings indicate that flavonols have a prebiotic-like effect on the anti-inflammatory activity of B. adolescentis. © 2013 BioFactors, 2013....(more)
Kawabata K, et al. Biofactors 2013 Mar 29.
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- 23. Antioxidant capacity, polyphenolic content and tandem HPLC-DAD-ESI/MS profiling of phenolic compounds from the South American berries Luma apiculata and L. chequén.
Native Myrtaceae fruits were gathered by South American Amerindians as a food source. At present, there is still some regional consume of the small berries from trees belonging to genus Luma that occurs in southern Chile and Argentina. The aerial parts and berries from Luma apiculata and Luma chequen were investigated for phenolic constituents and antioxidant capacity. A high performance electrospray ionisation mass spectrometry method was developed for the rapid identification of phenolics in polar extracts from both species. Thirty-one phenolic compounds were detected and 27 were identified or tentatively characterised based on photodiode array UV-vis spectra (DAD), ESI-MS-MS spectrometric data and spiking experiments with authentic standards. Twelve phenolic compounds were detected in L. apiculata fruits and 12 in the aerial parts while L. chequen yielded 10 compounds in fruits and 16 in aerial parts, respectively. From the compounds occurring in both Luma species, seven were identified as tannins or their monomers, 15 were flavonol derivatives and five were anthocyanins. The whole berry and aerial parts extracts presented high antioxidant capacity in the DPPH assay (IC50 of 10.41±0.02 and 2.44±0.03μg/mL for L. apiculata, 12.89±0.05 and 3.22±0.05 for L. chequen, respectively), which can be related to the diverse range of phenolics detected. The antioxidant capacity together with the high polyphenolic contents and compounds identified can support at least in part, their use as botanical drugs. From the compounds identified in both species, 3-O-(6″-O-galloyl)-hexose derivatives of myricetin, quercetin, laricitrin and isorhamnetin are reported for the first time for the genus Luma....(more)
Simirgiotis MJ, et al. Food Chem 2013 Aug 15;139(1-4):289-99.
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- 24. Inhibitory effect of naringenin (citrus flavonone) on N-nitrosodiethylamine induced hepatocarcinogenesis in rats.
We evaluated the effects of naringenin on N-nitrosodiethylamine (NDEA)-induced hepatocarcinogenesis in rats. Administration of NDEA induced hepatocellular carcinoma (HCC), as evidenced by changes in histopathological architecture, increased activity of cytochrome P450, decreased activity of glutathione S-transferase (GST) as well as decreased antioxidant status, enhanced lipid peroxidation and increased liver marker enzymes. Pre- and post-treatment with naringenin effectively suppressed NDEA-initiated hepatocarcinoma and the associated preneoplastic lesions by modulating xenobiotic-metabolizing enzymes (XMEs), alleviating lipid peroxidation (through both free radical scavenging and the enhanced antioxidant status), and decreased levels of liver marker enzymes. These results indicate that naringenin prevents lipid peroxidation and hepatic cell damage and also protects the antioxidant system in N-nitrosdithylamine-induced hepatocarcinogenesis....(more)
Arul D, et al. Biochem Biophys Res Commun 2013 May 3;434(2):203-9.
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- 25. Analysis of flavonoids and the flavonoid structural genes in brown fiber of upland cotton.
BACKGROUD:
As a result of changing consumer preferences, cotton (Gossypium Hirsutum L.) from varieties with naturally colored fibers is becoming increasingly sought after in the textile industry. The molecular mechanisms leading to colored fiber development are still largely unknown, although it is expected that the color is derived from flavanoids.
EXPERIMENTAL DESIGN:
Firstly, four key genes of the flavonoid biosynthetic pathway in cotton (GhC4H, GhCHS, GhF3'H, and GhF3'5'H) were cloned and studied their expression profiles during the development of brown- and white cotton fibers by QRT-PCR. And then, the concentrations of four components of the flavonoid biosynthetic pathway, naringenin, quercetin, kaempferol and myricetin in brown- and white fibers were analyzed at different developmental stages by HPLC.
RESULT:
The predicted proteins of the four flavonoid structural genes corresponding to these genes exhibit strong sequence similarity to their counterparts in various plant species. Transcript levels for all four genes were considerably higher in developing brown fibers than in white fibers from a near isogenic line (NIL). The contents of four flavonoids (naringenin, quercetin, kaempferol and myricetin) were significantly higher in brown than in white fibers and corresponding to the biosynthetic gene expression levels.
CONCLUSIONS:
Flavonoid structural gene expression and flavonoid metabolism are important in the development of pigmentation in brown cotton fibers....(more)
Feng H, et al. PLoS One 2013;8(3):e58820.
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- 26. A Genetic and Metabolic Analysis Revealed that Cotton Fiber Cell Development Was Retarded by Flavonoid Naringenin.
The cotton (Gossypium spp.) fiber is a unique elongated cell that is useful for investigating cell differentiation. Previous studies have demonstrated the importance of factors such as sugar metabolism, the cytoskeleton, and hormones, which are commonly known to be involved in plant cell development, while the secondary metabolites have been less regarded. By mining public data and comparing analyses of fiber from two cotton species (Gossypium hirsutum and Gossypium barbadense), we found that the flavonoid metabolism is active in early fiber cell development. Different flavonoids exhibited distinct effects on fiber development during ovule culture; among them, naringenin (NAR) could significantly retard fiber development. NAR is a substrate of flavanone 3-hydroxylase (F3H), and silencing the F3H gene significantly increased the NAR content of fiber cells. Fiber development was suppressed following F3H silencing, but the overexpression of F3H caused no obvious effects. Significant retardation of fiber growth was observed after the introduction of the F3H-RNA interference segment into the high-flavonoid brown fiber G. hirsutum T586 line by cross. A greater accumulation of NAR as well as much shorter fibers were also observed in the BC1 generation plants. These results suggest that NAR is negatively associated with fiber development and that the metabolism mediated by F3H is important in fiber development, thus highlighting that flavonoid metabolism represents a novel pathway with the potential for cotton fiber improvement....(more)
Tan J, et al. Plant Physiol 2013 May;162(1):86-95.
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- 27. Transgenic rice seed synthesizing diverse flavonoids at high levels: a new platform for flavonoid production with associated health benefits.
Flavonoids possess diverse health-promoting benefits but are nearly absent from rice, because most of the genes encoding enzymes for flavonoid biosynthesis are not expressed in rice seeds. In the present study, a transgenic rice plant producing several classes of flavonoids in seeds was developed by introducing multiple genes encoding enzymes involved in flavonoid synthesis, from phenylalanine to the target flavonoids, into rice. Rice accumulating naringenin was developed by introducing phenylalanine ammonia lyase (PAL) and chalcone synthase (CHS) genes. Rice producing other classes of flavonoids, kaempferol, genistein, and apigenin, was developed by introducing, together with PAL and CHS, genes encoding flavonol synthase/flavanone-3-hydroxylase, isoflavone synthase, and flavone synthases, respectively. The endosperm-specific GluB-1 promoter or embryo- and aleurone-specific 18-kDa oleosin promoters were used to express these biosynthetic genes in seed. The target flavonoids of naringenin, kaempferol, genistein, and apigenin were highly accumulated in each transgenic rice, respectively. Furthermore, tricin was accumulated by introducing hydroxylase and methyltransferase, demonstrating that modification to flavonoid backbones can be also well manipulated in rice seeds. The flavonoids accumulated as both aglycones and several types of glycosides, and flavonoids in the endosperm were deposited into PB-II-type protein bodies. Therefore, these rice seeds provide an ideal platform for the production of particular flavonoids due to efficient glycosylation, the presence of appropriate organelles for flavonoid accumulation, and the small effect of endogenous enzymes on the production of flavonoids by exogenous enzymes....(more)
Ogo Y, et al. Plant Biotechnol J 2013 Apr 3.
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- 28. Assay of phenolic compounds from four species of ber (Ziziphus mauritiana L.) fruits: Comparison of three base hydrolysis procedure for quantification of total phenolic acids.
The present study was undertaken to investigate the flavonoid profile in four species of ber (Ziziphus mauritiana Lamk.) fruit. The 12 flavonoids identified were quercetin 3-O-robinobioside, quercetin 3-O-rutinoside, quercetin 3'-O-galactoside, quercetin 3'-O-glucoside, quercetin 3'-O-rhamnoside, quercetin 3'-O-pentosylhexoside, quercetin 3-O-6'malonylglucoside, quercetin 3'-O-malonylglucoside, luteolin 7-O-6'malonylglucoside, luteolin 7-O-malonylglucoside, myricetin 3-O-galactoside, and naringenin tri glycoside. This is the first report on extraction of nine additional flavonoids from the ber fruits. In addition, we also compared the impact of three different base hydrolysis techniques namely ultrasonic assisted base hydrolysis (UABH), microwave assisted base hydrolysis (MWABH), and pressurised liquid assisted base hydrolysis (PLABH) for the quantification of total phenolic acids. Nine phenolic acids, protocatechuic acid, p-hydroxybenzoic acid, ferulic acid, chlorogenic acid, vanillic acid, caffeic acid, vanillin, ortho- and para-coumaric acids, were identified and quantified. The three major phenolic acids identified in all four ber species were p-coumaric acid, vanillin and ferulic acids. Higher amounts (p<0.05) of total phenolic acids in all cultivars were obtained with the PLABH technique as compared to other two procedures (UABH and MWABH)....(more)
Memon AA, et al. Food Chem 2013 Aug 15;139(1-4):496-502.
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- 29. Cultivar variations in antioxidant and antihyperlipidemic properties of pomelo pulp (Citrus grandis [L.] Osbeck) in Thailand.
Pomelo (Citrus grandis L. Osbeck) is a native fruit of great economic importance in Southeast Asia. To provide experimental evidence for the antioxidant and antihyperlipidemic properties of pomelo, 6 cultivars, including Kao-Yai (KY), Thong-dee (TD), Kao-Tangkwa (KT), Kao-Numpueng (KN), Ta-Koi (TK), and Tubtim Siam (TS) were evaluated. KY had the highest phenolic content, and the strongest 1,1-diphenyl-2-pireyhydrazyl radical scavenging capacity and hydroxyl radical scavenging activity. From the high-performance liquid chromatography analysis, naringin and naringenin were the major flavonoids in the KT and TK cultivars. Six pomelo cultivars had antihyperlipidemic activities including the inhibition of pancreatic lipase and cholesterol esterase, as well as cholesterol micelle formation and bile acid binding. Hierarchical clustering analysis showed that the 6 cultivars were separated into 2 classifications. In addition, the total phenolics of the pomelo cultivars were significantly correlated with ferric reducing antioxidant power and Trolox equivalent antioxidant capacity. The results suggest that pomelo provides significant health benefits and may be used for developing functional foods....(more)
Mäkynen K, et al. Food Chem 2013 Aug 15;139(1-4):735-43.
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- 30. In vitro effects of myricetin, morin, apigenin, (+)-taxifolin, (+)-catechin, (-)-epicatechin, naringenin and naringin on cytochrome b5 reduction by purified NADH-cytochrome b5 reductase.
The microsomal NADH-dependent electron transport system consisting of cytochrome b5 reductase and cytochrome b5 participates in a number of physiologically important processes including lipid metabolism as well as is involved in the metabolism of various drug and xenobiotics. In the present study, we assessed the inhibitory effects of eight dietary flavonoids representing five distinct chemical classes on cytochrome b5 reduction by purified cytochrome b5 reductase. From the flavonoids tested, myricetin was the most potent in inhibiting cytochrome b5 reduction with an IC50 value of 0.35μM. Myricetin inhibited b5 reductase noncompetitively with a Ki of 0.21μM with respect to cofactor NADH, and exhibited a non-linear relationship indicating non-Michaelis-Menten kinetic binding with respect to cytochrome b5. In contrast to the potent inhibitory activity of myricetin, (+)-taxifolin was found to be a weak inhibitor (IC50=9.8μM). The remaining flavonoids were inactive within the concentration range tested (1-50μM). Analysis of structure-activity data suggested that simultaneous presence of three OH groups in ring B is a primary structural determinant for a potent enzyme inhibition. Our results suggest that inhibition of the activity of this system by myricetin or myricetin containing diets may influence the metabolism of therapeutic drugs as well as detoxification of xenobiotics....(more)
Celik H, et al. Toxicology 2013 Apr 5;308C:34-40.
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- 31. The activation of mitochondrial BK potassium channels contributes to the protective effects of naringenin against myocardial ischemia/reperfusion injury.
Naringenin (NAR), flavonoid abundant in the genus Citrus, has been reported to interact with the large-conductance calcium-activated potassium channels (BK). Since activators of BK channels expressed in cardiac mitochondria trigger protective effects in several models of myocardial ischemia/reperfusion (I/R), this work aimed to evaluate the potential cardioprotective effects of NAR and the involvement of mitochondrial BK channels. In an in vivo model of acute infarct in rats, NAR (100mg/kg i.p.) significantly reduced the heart injury induced by I/R. This effect was antagonized by the selective BK-blocker paxilline (PAX). The cardioprotective dose of NAR did not cause significant effects on the blood pressure. In Largendorff-perfused rat hearts submitted to ischemia/reperfusion, NAR improved the post-ischemic functional parameters (left ventricle developed pressure and dP/dt) with lower extension of myocardial injury. On isolated rat cardiac mitochondria, NAR caused a concentration-dependent depolarization of mitochondrial membrane and caused a trans-membrane flow of thallium (potassium-mimetic cation). Both these effects were antagonized by selective blockers of BK channels. Furthermore, NAR half-reduced the calcium accumulation into the matrix of cardiac mitochondria exposed to high calcium concentrations. In conclusion, NAR exerts anti-ischemic effects through a "pharmacological preconditioning" that it is likely to be mediated, at least in part, by the activation of mitochondrial BK channels....(more)
Testai L, et al. Biochem Pharmacol 2013 Apr 6.
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- 32. Regiospecific modifications of naringenin for astragalin production in Escherichia coli.
We report the production of astragalin (AST) from regiospecific modifications of naringenin (NRN) in Escherichia coli BL21(DE3). The exogenously supplied NRN was converted into dihydrokaempferol (DHK) and then kaempferol (KMF) in the presence of flavanone-3-hydroxylase (f3h) and flavonone synthase (fls1) from Arabidopsis thaliana, respectively. KMF was further modified to produce AST by 3-O-glucosylation utilizing the endogeneous UDP-glucose in presence of UGT78K1 from Glycine max. To increase the intracellular UDP-glucose concentration by channeling the carbon flux toward UDP-glucose at the branch point of glucose-6-phosphate (G6P), the chromosomal glucose phosphate isomerase (pgi) and D-glucose-6-phosphate dehydrogenase (zwf) were knocked-out in E. coli BL21(DE3). The two enzymes directly involved in the synthesis of UDP-glucose from G6P, phosphoglucomutase (nfa44530) from Nocardia farcinia and glucose-1-phosphate uridylyltransferase (galU) from E. coli K12 were overexpressed, which successfully diverted the carbon flow from glycolysis to the synthesis of UDP-glucose. Furthermore, to prevent the dissociation of UDP-glucose into UDP and glucose, the UDP-glucose hydrolase (ushA) was deleted. The E. coli ΔpgiΔzwfΔushA mutant harboring the UDP-glucose biosynthetic pathway and the aforementioned genes for the regiospecific glucosylation produced 109.3 mg/L (244 µM) of AST representing 48.8% conversion from 500 µM of NRN in 60 h without any supplementation of extracellular UDP-glucose. Biotechnol. Bioeng. 2013 9999:XX-XX. © 2013 Wiley Periodicals, Inc....(more)
Malla S, et al. Biotechnol Bioeng 2013 Apr 8.
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- 33. Quantitative Analysis of the Naringenin-inducible Proteome in Rhizobium leguminosarum by Isobaric Tagging and Mass Spectrometry.
The rhizobium-legume interaction is a critical cornerstone of crop productivity and environmental sustainability. Its potential improvement relies on elucidation of the complex molecular dialogue between its two partners. In the present study, the proteomic patterns of gnotobiotic cultures of Rhizobium leguminosarum bv. viciae 3841 grown for 6 h in presence or absence of the nod gene-inducing plant flavonoid naringenin (10 μM) were analyzed using the iTRAQ approach. A total of 1334 proteins were identified corresponding to 18.67% of the protein-coding genes annotated in the sequenced genome of bv. viciae 3841. The abundance levels of 47 proteins were increased upon naringenin treatment showing fold change ratios ranging from 1.5 to 25 in two biological replicates. Besides the nod units, naringenin enhanced the expression of a number of other genes, many of which organized in operons, including β(1-2) glucan production and secretion, succinoglycan export, the RopA outer membrane protein with homology to an oligogalacturonide specific porin motif, other enzymes for carbohydrate and amino acid metabolism, and proteins involved in the translation machinery. Data were validated at the transcriptional and phenotypic levels by reverse transcription polymerase chain reaction (RT-PCR) and an assay of secreted sugars in culture supernatants, respectively. The current approach provides not only a high-resolution analysis of the prokaryotic proteome but also unravels the rhizobium molecular dialogue with legumes by detecting the enhanced expression of several symbiosis-associated proteins, whose flavonoid-dependency had not yet been reported....(more)
Tolin S, et al. Proteomics 2013 Apr 12.
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- 34. Effects of Itraconazole, Dexamethasone and Naringin on Pharmacokinetics of Nadolol in Rats.
The aim of the present study was to clarify the involvement of P-glycoprotein (P-gp) or organic anion transporting polypeptide (Oatp) 1a5 in the pharmacokinetics of nadolol (NDL), a non-metabolized hydrophilic β-adrenoceptor blocker, in rats. Pretreatment of itraconazole (ICZ, P-gp inhibitor, 50 mg/kg) for 30 min before oral administration of NDL (10 mg/kg) significantly increased the area under the plasma concentration-time curve (AUC(0-∞)) of NDL by 1.7-fold compared with control. Intragastric administration of dexamethasone (DEX, 8 mg/kg) for 4 consecutive days increased P-gp level in the intestine and the liver. In line with this, DEX pre-treatment decreased maximum plasma concentration (C(max)) of NDL by 28% of control. To inhibit the intestinal Oatp1a5, naringin (NRG, 0.145 mg/kg) was pretreated orally for 30 min before the oral administrations of NDL or celiprolol (CEL, 10 mg/kg, Oatp1a5 substrate). Although NRG markedly reduced C(max) and AUC(0-∞) of CEL by 60% and 65% of control, respectively, little difference was observed in the plasma concentration of NDL between NRG and control. These results suggest that P-gp is greatly involved in the pharmacokinetics of NDL, while the involvement of Oatp1a5 in the pharmacokinetics of NDL may be less than that of celiprolol in rats....(more)
Miyazaki N, et al. Drug Metab Pharmacokinet 2013 Feb 19.
Related Products: Naringin
- 35. A novel porous gelatin composite containing naringin for bone repair.
As Gu-Sui-Bu (GSB) is a commonly used Chinese medical herb for therapeutic treatment of bone-related diseases, naringin is its main active component. This study elucidates how various concentrations of naringin solution affect the activities of bone cells, based on colorimetric, alkaline phosphatase activity, nodule formation, and tartrate-resistant acid phosphatase activity assays to determine the optimal concentration of naringin. GGT composite was obtained by combining genipin cross-linked gelatin and β-tricalcium phosphate. GGTN composite was prepared by mixing GGT composite with the predetermined concentration of naringin. Porous GGT and GGTN composites were then made using a salt-leaching procedure. The potential of the composites in repairing bone defects was evaluated and compared in vivo by using the biological response of rabbit calvarial bone to these composites. Consequently, the most effective concentration of naringin was 10 mg/mL, which significantly enhanced the proliferation of osteoblasts, osteoclast activity, and nodule formation without affecting the alkaline phosphatase activity of osteoblasts and mitochondrial activity of mixed-bone cells. Radiographic analysis revealed greater new bone ingrowth in the GGTN composite than in the GGT composite at the same implantation time. Therefore, the GGTN composite is highly promising for use as a bone graft material....(more)
Chen KY, et al. Evid Based Complement Alternat Med 2013;2013:283941.
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