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chrysoeriol ameliorates hyperglycemia by regulating the carbohydrate metabolic enzymes in streptozotocin-induced diabetic rats

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Food Science and Human Wellness 2020年第4期9卷 346-354页

作者： Baskaran Krishnan Abirami Ramu Ganesan Ravindran Balasubramani Dinh Duc Nguyen Soon Woong Chang Shaoyun Wang Jianbo Xiao Balamuralikrishnan Balasubramanian Department of Biochemistry Sree Narayana Guru CollegeCoimbatore641105Tamil NaduIndia Department of Food Science and Home Economics School of Applied SciencesCollege of EngineeringScience and TechnologyFiji National UniversityFiji Islands Department of Environmental Energy and Engineering Kyonggi UniversityYoungtong-GuSuwonGyeonggi-Do16227South Korea College of Biological Science and Technology Fuzhou UniversityFuzhou 350108China International Research Center for Food Nutrition and Safety Jiangsu UniversityZhenjiang 212013China Department of Food Science and Biotechnology College of Life SciencesSejong UniversitySeoul05006South Korea

The present study aimed to evaluate the effects of chrysoeriol from Cardiospermum halicacabum in streptozotocin induced Wistar *** rats were categorized as control,diabetic control supplemented with 0,20 mg/kg chrysoeriol and 600μg/kg BW of glibenclamide for 45-day trial *** results indicated that the inclusion of chrysoeriol(20 mg/kg)showed a significant reduction in plasma glucose,hemoglobin and glycosylated hemoglobin level with a rising of plasma insulin ***,downregulated enzymes including glucose 6-phosphatase,fructose 1,6-bisphosphatase,and glycogen phosphorylase as well upregulated enzymes such as hexokinase,glucose-6-phosphate dehydrogenase,pyruvate kinase,and hepatic glycogen *** was a diminish action found in liver glycogen synthase of tested rat with a rise in gamma-glutamyl transpeptidase,towards normal levels upon treatment with *** histopathological study confirmed that renewal of the beta cells of pancreatic of chrysoeriol and glibenclamide treated *** addition,the molecular docking of chrysoeriol against glycolytic enzymes including hexokinase,glucose-6-phosphate dehydrogenase,pyruvate kinase,using Argus software shows chrysoeriol had greatest ligand binding energy as equivalent to glibenclamide,as a standard ***,chrysoeriol found to be non-toxic with potential regulation on glycemic control and upregulation of the carbohydrate metabolic enzymes.

关键词： Cardiospermum halicacabum chrysoeriol Anti-hyperglycemic Carbohydrate metabolizing enzymes

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Discovery of chrysoeriol,a PI3K-AKT-mTOR Pathway Inhibitor with Potent Antitumor Activity against Human Multiple Myeloma Cells in vitro

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Journal of Huazhong University of Science and Technology(Medical Sciences) 2010年第6期30卷 734-740页

作者：杨漾周晓曦肖敏洪振亚龚泉姜立军周剑峰 Department of Hematology Tongji HospitalTongji Medical CollegeHuazhong University of Science and Technology

This study was designed to determine the impact of chrysoeriol on proliferation and cell cycle progression in the human multiple myeloma cell lines RPMI 8226 and KM3,and its related molecular *** was identified by using the phosphorylated AKT-specific cytoblot high throughput ***-8 assay was employed to examine the growth inhibition rate and IC 50 (48 h) in peripheral blood mononuclear cells (PBMNCs),RPMI 8226 and KM3 cells treated with chrysoeriol at various *** were labeled with 5-6-carboxyfluorescein diacetate succinimidyl ester (CFSE),and the proliferation dynamics was detected by flow cytometry and analyzed with ModFit *** cell cycles of RPMI 8226 and KM3 cells were measured by flow cytometry when the IC 50 concentration of chrysoeriol was *** alterations in cell-cycle related proteins (Cyclin B1,Cyclin D1,p21) and proteins in PI3K-AKT-mTOR pathway were determined by Western blot *** results showed the proliferation of multiple myeloma cells was significantly inhibited by chrysoeriol,resulting in cell cycle arrest in G 2 /M *** could significantly reduce the expression of p-AKT (s473) and p-4eBP1 (t37/46) protein,meanwhile enhanced Cyclin B1 and p21 protein *** effects were not observed in PBMNCs from normal *** was concluded that chrysoeriol was a selective PI3K-AKT-mTOR pathway *** restrained the proliferation of human multiple myeloma cells,but didn’t affect proliferation of PBMNCs from normal *** might exhibit the cell cycle regulatory effect via the inhibition of PI3K-AKT-mTOR signal pathway.

关键词： chrysoeriol multiple myeloma proliferation inhibition G 2 /M arrest PI3K-AKT-mTOR signal pathway

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Protective effect of chrysoeriol against doxorubicin-induced cardiotoxicity in vitro

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Chinese Medical Journal 2009年第21期122卷 2652-2656页

作者： LIU Zhe SONG Xiao-dong XIN Ying WANG Xiao-jian YU Hui BAI Yong-yi LIU Jun-hao HANG Chan-na HUI Ru-tai Sino-German Laboratory for Molecular Medicine Key Laboratory for Clinical Cardiovascular Genetics of Ministry of Education Cardiovascular Institute & Fu Wai Hospital Chinese Academy of Medical Sciences Peking Union Medical College Beijing 100037 China

Background The use of doxorubicin （DOX） is limited by its dose-dependent cardiotoxicity. Reactive oxygen species （ROSs） play an important role in the pathological process of DOX-induced cardiotoxicity. The aim of this study was to evaluate the protective effect of chrysoeriol, a flavone compound, against DOX-induced apoptosis and death in H9c2 cells and to find out its preliminary mechanism. Methods We used 3-（4,5-dimethylthiazol-2-yl）-2,5-diphenyl-2H-tetrazolium bromide （MTT） assay, Hoechst33258 staining and measurement of lactate dehydrogenase （LDH） release to evaluate the protective effect of chrysoeriol against DOX-induced apoptosis and death in H9c2 cells. To find out the mechanism of this protective effect, we observed the immunofluorescence of intracellular ROS and measured the activities of malondialdehyde （MDA）, superoxide dismutase （SOD） and glutathione peroxidase （GPx）. Furthermore, we evaluated the effect of chrysoeriol on the antitumor activity of DOX in HeLa cells with MTT assay. Results The results of MTT assay, Hoechst 33258 staining and measurement of LDH release showed that chrysoeriol significantly reduced doxorubicin-induced apoptosis and cell death. chrysoeriol at a dose of 20 μg/ml notably reduced intracellular ROS, decreased the concentration of MDA in the supernatant of DOX-treated H9c2 cells and increased SOD and GPx activities to their normal levels. Further study showed that the addition of chrysoeriol did not affect the antitumor activity of DOX. Conclusion chrysoeriol could potentially serve as a novel cardioprotective agent against DOX-induced cardiotoxicity without affecting the antitumor activity of DOX.

关键词： chrysoeriol doxorubicin cardiotoxicity reactive oxygen species

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