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五环三萜衍生物的合成和对α-葡萄糖苷酶的抑制活性 被引量:5

Synthesis and inhibitory activity against α-glycosidase of pentacyclic triterpenes
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摘要 对天然产物进行结构修饰和在天然产物中分离得到的齐墩果酸和熊果酸型五环三萜衍生物,经过理化性质和光谱数据确定化合物的结构,并对α-葡萄糖苷酶抑制活性进行测定。体外活性测试表明,天然存在的和从熊果酸和齐墩果酸结构衍生的三萜化合物对α-葡萄糖苷酶均有不同程度的抑制作用,其中化合物1a和1b活性较好。因此,对五环三萜化合物进行结构衍生,可以发现高活性α-葡萄糖苷酶抑制活性化合物。 The structures of ursolic acid and oleanolic acid related compound,including natural products and synthetic derivatives of ursolic acid and oleanolic acid,were identified by physical and spectral analyses,or literature data.The inhibitory activity of the triterpene compounds against α-glycosidase were evaluated.The in vitro results showed that the test pentacyclic triterpenes exhibited diverse inhibitory activity against α-glycosidase.Within this series of compounds,1a and 1b had better inhibitory activity than that of the others.It is possible that highly active compounds with α-glycosidase inhibition activity would be found through structural modification of pentacyclic triterpenes.
出处 《中国药科大学学报》 CAS CSCD 北大核心 2010年第3期222-225,共4页 Journal of China Pharmaceutical University
基金 国家自然科学基金资助项目(No.30973620) 贵州省科技计划资助项目(No.2008-7004)~~
关键词 五环三萜 衍生物 Α-葡萄糖苷酶 抑制活性 pentacyclic triterpenes derivatives α-glycosidase inhibitors
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  • 1Chen XL, Fan YX,Zheng YG,et al. Properties and production of valienamine and its related analogues [ J ]. Chem Rev,2003,103 (5) :1 955 -1 977.
  • 2Asano N ,Nash RJ, Molyneux RJ,et al. Sugar-mimic glycosidase inhibitors: natural occurrence, biological activity and prospects for therapeutic application [ J ]. Tetrahedron: Asymmetry, 2000,11 (8):1 645 -1 680.
  • 3Pili R, Chang J, Muhlhauser J,et al. Adenovirus-mediated gene transfer of fibroblast growth factor-1 : angiogenesis and tumorigenicity in nude mice[ J]. Int J Cancer, 1997,73 (2) :258 -263.
  • 4顾觉奋,陈紫娟.α-葡萄糖苷酶抑制剂的研究及应用[J].药学进展,2009,33(2):62-67. 被引量:75
  • 5赵昱(ZhaoY),陈海永(ChenHY),郑汉其(ZhengHQ),等.A环和C环多氧化取代的五环三萜及其制备方法和用途:中国,200610104147.0[P].2008-02-06[2009-12-24].
  • 6赵昱(Zhao Y),冯菊红(Feng JH),巫秀美(WuXM),等.A环多氧化取代的五环三萜类衍生物及其制备方法和用途:中国,200610104148.5[P].2008-02-06[2009-12-24].
  • 7张前军(ZhangQJ).连钱草、假木豆化学成分及其抗菌活性研究[D].贵阳:贵州大学,2006.
  • 8李林珍(Li LZ).假地蓝化学成分研究和药理活性初筛[D].合肥:合肥医学院,2007.
  • 9陶正明,丁立生,彭树林,王明奎,张安将.乌泡子根的三萜成分[J].中草药,2002,33(2):99-101. 被引量:11
  • 10闻韧(WenR).药物合成反应[M].2版.北京:化学工业出版社,2003:303.

二级参考文献45

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同被引文献58

  • 1Peng Cho Tang.Design and synthesis of DPP-4 inhibitor for the treatment of type 2 diabetes[J].Chinese Chemical Letters,2010,21(3):253-256. 被引量:3
  • 2陈军,柳军,龚彦春,张陆勇,华维一,孙宏斌.新型糖原磷酸化酶抑制剂熊果酸衍生物的合成及其生物活性[J].中国药科大学学报,2006,37(5):397-402. 被引量:19
  • 3孟艳秋,陈瑜,王趱,刘丹.熊果酸的研究进展[J].中国新药杂志,2007,16(1):25-28. 被引量:80
  • 4Muto Y,Ninomiya M, Fujiki H. Present status of research oncancer chemoprevention in Japan[J]. Jpn J Clin Oncol, 1990,20(3):219-224.
  • 5Kwon TH, Lee B,Chung SH, et al. Synthesis and NO produc-tion inhibitory activities of ursolic acid and oleanolic acidderivatives[J]. Bull Korean Chem Soc, 2009, 30(1):119-123.
  • 6Ro DK,Paradise EM, Ouellet M,et al, Production of the anti—malarial drug precursor artemisinic acid in engineered yeast[J]. Nature, 2006, 440(7086):940-943.
  • 7Shaker KH, Bemhardta M, Elgamal MHA, et al. Triterpenoidsaponins from Fagonia indicafj]. Phytochemistry, 1999,51(8):1049-1153.
  • 8Muto Y, Ninomiya M, Fujiki H. Present status of research on cancer chemoprevention in Japan [J]. Jpn J Clin Oncol, 1990, 20(3): 219-224.
  • 9Kwon T H, Lee B, Chung S H, et al. Synthesis and NO production inhibitory activities of ursolic acid and oleanolic acid derivatives [J]. Bull Korean Chem Soc, 2009, 30(1): 119-123.
  • 10Liao Q F, Yang W, Jia Y, et al. LC-MS Determination and pharmacokinetic studies of ursolic acid in rat plasma after administration of the traditional Chinese medicinal preparation Lu-Ying extract [J]. Yakugaku Zasshi, 2005, 125(6): 509-515.

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