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8-烷基黄连碱同系物的合成及体外降糖作用 被引量:4

Synthesis and in vitro glucose-lowering effect of 8-alkyl-coptisine
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摘要 目的合成8-烷基黄连碱同系物并研究其在体外对细胞糖代谢的影响。方法采用与人肝细胞表型相似的HepG2细胞,检测24 h后培养液中葡萄糖消耗量,用MTT法观察细胞增殖情况。结果 8-烷基黄连碱同系物在葡萄糖浓度为10 mmol/L时可使HepG2细胞的葡萄糖消耗量有不同程度的增加,其中以8-己基黄连碱最为显著。8-烷基黄连碱同系物对HepG2细胞增殖有显著的抑制作用。结论首次合成8-烷基黄连碱同系物。8-烷基黄连碱同系物随着其烷基碳链的延长,细胞的葡萄糖消耗量先是增大,当8位烷基链碳原子数超过6时,葡萄糖消耗量逐渐减小。8-已基黄连碱是具有一定潜力的降血糖先导化合物。 Objective To investigate the effect of 8-alkyl-coptisine on glycometabolism in vitro.Methods HepG2 cells similar to human hepatic cells were used to test the glucose consumption(GC) in cultural solution in 24 h and MTT assay was used to monitor the proliferation of HepG2 cells.Results The results indicated that 8-alkyl-coptisine could increase the amounts of GC of HepG2 cells.In glucose concentration(10 mmol/L),8-hexyl-coptisine was the most significant.8-Alkyl-coptisine had notable inhibition in proliferation of HepG2 cells.Conclusion 8-Alkyl-coptisine was successfully synthesized.GC could increase as the length of the aliphatic chain increases firstly and the GC could decrease when the length of the aliphatic chain exceeds six atoms.8-Hexyl-coptisine is a potential hypoglycemic leading compound.
出处 《中草药》 CAS CSCD 北大核心 2011年第4期640-644,共5页 Chinese Traditional and Herbal Drugs
基金 重庆市科委重大专项"黄连综合开发利用"资助项目(CSTC2008AA5021) 重庆市科委攻关项目"平抑舒降糖胶囊对不同症侯糖尿病疗效及安全性研究"资助(CSTC2010AC5007) 科技部新药创制项目"黄连治疗糖尿病型高血脂并发症中药新药研究"资助(2010ZX09401-306-3-10)
关键词 8-烷基黄连碱 合成 HEPG2细胞 葡萄糖消耗 8-烷基黄连碱同系物 8-alkyl-coptisine synthesis HepG2 cell glucose consumption(GC) 8-alkyl-coptisine homolog
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  • 1Lenka G, Dosta J, Marek R. Quaternary protoberberine alkaloids [J]. Phytochemistry, 2007, 68(2): 150-175.
  • 2Jung H A, Yoon N Y, Bae H J, et al. Inhibitory activities of the alkaloids from Coptidis Rhizoma against aldose reductase [J]. Arch Pharra Res, 2008, 31(11): 1405-1412.
  • 3Yuan L J, Tu D W, Ye X L, et al. Hypoglycemic andhypocholesterolemic effects of Coptis chinensis Franchinflorescence [J]. Plant Foods Hum Nutr, 2006, 61(3): 139-144.
  • 4Rackova L, Maijekova M, Kost'alova D, et al. Antiradical and antioxidant activities of alkaloids isolated from Mahonia aquifolium structural aspects [J]. Bioorg Med Chem, 2004, 12(17)! 4709-4715.
  • 5Hirano H, Osawa E, Yamaoka Y, et al. Gastric-mucous membrane protection activity of coptisine derivatives [J]. BiolPharm Bull, 2001, 24(11): 1277-1281.
  • 6杨勇,叶小利,李学刚.4种黄连生物碱的抑菌作用[J].时珍国医国药,2007,18(12):3013-3014. 被引量:99
  • 7Iwasa K, Nishiyama Y, Ichimaru M, et al. Structureactivity relationships of quatemary protoberberine alkaloids having an antimalarial activity [J]. Eur J Med Chem, 1999, 34(12): 1077-1083.
  • 8邹晨辉,申竹芳.黄连生物碱抗糖尿病机制的研究进展[J].中草药,2004,25(11). 被引量:36
  • 9Iwasa K, Kamigauchi M, Sugiura M, et al. Antimicrobial activity of some 13-alkyl substituted protoberberinium salts [J]. Planta Med, 1997, 63(3): 196-198.
  • 10Iwasa K, Lee D U, Kang S I, et al. Antimicrobial activity of 8-alkyl- and 8-phenyl-subsfituted berbednes and their 12-bromo derivatives [J]. JNatProd, 1998, 61(9): 1150-1153.

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