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Epigallocatechin-3-gallate (EGCG), as one of the main components of green tea, has a variety of biological activities. Both in vitro and in vivo experiments widely demonstrate that EGCG has anticancer activities. The molecular mechanism of EGCG against cancer was much complicated, and EGCG suppressed tumor cell proliferation and/or induced cell apoptosis through multi-pathways. This paper reviewed the anticancer molecular mechanism of EGCG, including EGCG anti-oxidantion, prooxidation, retardant of tumor cell cycle, inhibition of tumor cell angiogenesis, inducement of cancer cell apoptosis, and regulation of microRNA, summarized the research progress of three strategies for improving bioavailability of EGCG: nano-packaging technology, synergistic application and molecular modification, and looked into research and development on anticancer activity of EGCG.
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Objective Cistanches Herba is a kind of tonic traditional Chinese medicine with several therapy effects including tonifying kidney-yin, anti-dementia, anti-aging and relaxing bowel. Phenylethanoid glycosides (PhGs) are the major effective components in C. tubulosa. However, there were no further studies on molecular pharmacologic mechanisms due to its complex components and mechanism diversity of action in PhGs till to now. The aim of this study was to investigate the target protein groups and related mechanisms associated with PhGs in anticerebral ischemia-reperfusion injury. Methods The middle cerebral artery occlusion (MCAO) model was established in rats, and the protective effects of PhGs on cerebral ischemia-induced injuries were determined. A kind of solid bead whose surface was cross-linked with PhGs was prepared to capture the target proteins from brain tissue lysates. The target proteins were further identified with LC-MS/MS. Results PhGs significantly inhibited cerebral ischemia-induced injuries by reducing ischemia size and rat behavioral scores and elevated the SOD levels in rat brain tissues. Eighteen target proteins were identified based on “target fishing” strategy and divided into 9 kinds according to their biological functions, including anti-oxidation, ion channel, immunoregulation, cell survival and cytoskeleton, etc. Conclusion These findings reveal the potential pharmacological mechanisms of PhGs in anti-dementia, fatigability alleviating, anti-tumor, immunoloregulation, etc, and also present a promising technology for investigating the complicated pharmacological mechanisms of traditional Chinese medicine.
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AIM To explore the therapeutic effects of polysaccharide from Anemarrhena asphodeloides Bunge (PAA) on diabetic rats and potential mechanism of action.METHODS The rat model for diabetes was established by intraperitoneal injection of STZ (60 mg/kg),and sixty rats were assigned to control-,model-,glibenclamide-(25 mg/kg) groups and three groups of PAA-(50,100,200 mg/kg).Drugs were intragastrically administrated to rats once a day for 28 days.The rat body weight,glucose tolerance,fasting blood glucose (FBG),fasting insulin (FINS),IL-6,TNF-α,CAT,SOD,MDA,insulin receptor substrate (IRS1),Phospho-IRS1 and glucose transporter protein 4 (Glut4) were tested.RESULTS PAA could increase rat body weight and FINS level,reduce FBG level,and improve the glucose tolerance.The levels of IL-6 and TNF-α in serum,and MDA content in hepatic tissue were decreased,and the activities of CAT and SOD in hepatic tissue were increased.Meanwhile,PAA could also reduce the Phospho-IRS1 expression,and increase the Glut4 expression in hepatic tissue.CONCLUSION PAA has an anti-diabetic effect,whose mechanism is involved in anti-inflammatory,antioxidation,decreasing Phospho-IRS1 expression,and increasing Glut4 expression.
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AIM To explore the therapeutic effects of polysaccharide from Anemarrhena asphodeloides Bunge (PAA) on diabetic rats and potential mechanism of action.METHODS The rat model for diabetes was established by intraperitoneal injection of STZ (60 mg/kg),and sixty rats were assigned to control-,model-,glibenclamide-(25 mg/kg) groups and three groups of PAA-(50,100,200 mg/kg).Drugs were intragastrically administrated to rats once a day for 28 days.The rat body weight,glucose tolerance,fasting blood glucose (FBG),fasting insulin (FINS),IL-6,TNF-α,CAT,SOD,MDA,insulin receptor substrate (IRS1),Phospho-IRS1 and glucose transporter protein 4 (Glut4) were tested.RESULTS PAA could increase rat body weight and FINS level,reduce FBG level,and improve the glucose tolerance.The levels of IL-6 and TNF-α in serum,and MDA content in hepatic tissue were decreased,and the activities of CAT and SOD in hepatic tissue were increased.Meanwhile,PAA could also reduce the Phospho-IRS1 expression,and increase the Glut4 expression in hepatic tissue.CONCLUSION PAA has an anti-diabetic effect,whose mechanism is involved in anti-inflammatory,antioxidation,decreasing Phospho-IRS1 expression,and increasing Glut4 expression.
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The plants of genus Solanum L. contain alkaloids, flavonoids, steroids, and other various chemical constituents which exhibit protective activity, antifungal, antiviral, antitumor, and anti-oxidant activities. This paper reviews the research survey of the chemical constituents and biological activities of the plants of Solanum L. from domestic and foreign over the last 20 years, and provides the relative reference for the further development of the plants in Solanum L.
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Mangiferin also called Chinonin or mango, is mainly extracted from the Anacardiaceae and Gentianaceae plants. As polyphenol compounds, Mangiferin shows a strong antioxidant activity and a variety of pharmacological effects. In recent years, laboratory study has identified a variety of pharmacological effects associated with Mangiferin including preventing diabetes and its complications, regulating lipid metabolism abnormalities, antitumor, cardiovascular protection,anti hyperuricemia, neuro-protection, anti oxidation, anti-inflammation, antipyresis and analgesia, anti-bacteria and antivirus, antiradiation, liver pro-tection, promoting skeletal growth, anti allergy and immune reg-ulation,etc. In this paper, the research progress of pharmacolog-ical effects of Mangiferin is reviewed, analyzed and summarized in order to provide reference for further research and develop-ment.
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Objective: To study the in vivo pharmacodynamics characteristics of Buyang Huanwu Decoction (BHD) in mice, and to provide reference for rational clinical drug use. Methods: The level of MDA and activity of SOD in liver tissue of mice were determined after ig treatment with BHD or its drug-containing serum. Further more, the time-effect and dose-effect relationship of BHD on MDA level and SOD activity were carried out. The parameters of pharmacodynamics were estimated based on the time-effect and dose-effect curves. Results: Compared with control group, both BHD and its drug-containing serum could reduce MDAlevel, while raise SOD activity in the liver of mice (P < 0.05). Time-effect curves both present multi-peak but most pharmacodynamics parameters showed significant differences (P < 0.05), except tp and t1/2(Ka). Conclusion: BHD has obvious antioxidant effect and pharmacodynamics characteristics can be described as one-compartment model.
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Objective: To compare the contents of three homoisoflavones and their anti-oxidative activity of Ophiopogon japonicus in Sichuan (OJS) and Zhejiang (OJZ). Methods: The determination was performed on ACQUITYTM UPLC BEH C18 column (100 mm×2.1 mm, 1.7 μm), the Ultra Performance Liquid Chromatography-Photo-Diode Array (UPLC-PDA) technology was applied, and the mobile phase consisted of acetonitrile and 0.2% formic acid aqueous solution (55:45) with gradient elution program, flow rate was 0.20 mL/min with 2 μL of sample quantity at 296 nm, and the anti-DPPH radical efficiency of water extract from Ophiopogonis Radix were evaluated by UV-photometer. Results: The average values of methylophiopogonone A, methylophiopogonanone A, and methylophiopogonanone B were (3.06±0.54), (40.10±5.63), and (29.51±5.06) μg/g in OJS, respectively; while those in OJZ were (9.22±3.52), (106.63±27.56), and (256.97±61.79) μg/g, separately. The IC50 value was 16.59 mg/mL in OJS, while that in OJZ was 14.48 mg/mL. The IC50 value of positive control VC was 7.06 μg/mL. Conclution: Compared with OJS, the contents of homoisoflavones in OJZ are higher, and the anti-radical efficiency of water extract from OJZ is stronger. It provides the basis for the quality evaluation and geo-authentic research of Ophiopogonis Radix.
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Objective: To study the protective effect of Danqi Piantan Capsule (DPC, a capsule made of Salviae Miltiorrhizae Radix, Astragali Radix, Paeoniae Rugra Radix, etc. for the poststroke recovery) on the cerebral ischemia in the rat model of cerebral ischemia-reperfusion and its mechanism. Methods: One hundred and eighty male SD rats were randomly divided into six groups: Sham operation, model, positive drug (6.58 mg/kg), the high-, mid-, and low-dose (306, 153, and 76 mg/kg) DPC groups. The rats were ig administered once daily for consecutive 3 d, and the rat models with left middle cerebral artery occlusion (MCAO) were established at 1 h after the last administration. The blood samples were collected from the fossa orbitalis vein of rats at 24 h after the surgery, used to determine the content of serum superoxide dismutases (SOD) and endothelin (ET). The brain tissue samples were collected at 72 h after the surgery for determining the cerebral infarct size and cerebral index through TTC-staining. Results: Compared with the model group, the high- and mid-dose DPC could significantly reduce (P < 0.05) the cerebral index for the cerebral ischemia-reperfusion injury of rats; The three groups of DPJ all could enhance the activity of SOD, especially the high- and mid-dose groups had the significant difference (P < 0.05); The three groups also could reduce the content of ET, but there was no significant difference. Conclusion: DPC has the protective effect on cerebral ischemia-reperfusion and its mechanism may be related with relieving cerebral edema, anti-oxidantion, and inhibiting ET.
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Objective: To study the protective effect of Danhong Injection (DI) on primary cultured neonate rat brain microvascular endothelial cells (rBMECs) injury. Methods: The primary cultured rBMEC model was established and the identification of rabbit anti rat VIII factor was carried out. The cells were divided into control, model, low-, mid-, and high-dose (25, 50, and 100 μL/mL) DI groups in hypoxic condition for 4 h after administration. The cell morphology was observed under microscope, the apoptosis rate and DNA content were determined by flow cytometry, and the lactate dehydrogenase (LDH) level in cultural supernatants and cell superoxide dismutase (SOD) activity were detected according to the kit methods. Results: DI (50 and 100 μL/mL) could alleviate the rBMEC damage induced by hypoxia remarkably, improve the cell morphology of rBMECs, decrease the apoptosis significantly, inhibit the blockage of rBMECs in G1/S phase and the leakage of LDH, and increase the SOD activity. Conclusion: DI plays a significant role in the protection on injured primary cultured rBMECs induced by hypoxia, and the mechanism may be related to the enhancement of cellular anti-oxidative capacity and the inhibition of apoptosis.