Ethnobotanical-directed discovery of the antihyperglycemic properties of cryptolepine:: Its isolation from Cryptolepis sanguinolenta, synthesis, and in vitro and in vivo activities

被引：130

作者：

Bierer, DE ^{[1
]}

Fort, DM ^{[1
]}

Mendez, CD ^{[1
]}

Luo, J ^{[1
]}

Imbach, PA ^{[1
]}

Dubenko, LG ^{[1
]}

Jolad, SD ^{[1
]}

Gerber, RE ^{[1
]}

Litvak, J ^{[1
]}

Lu, Q ^{[1
]}

Zhang, PS ^{[1
]}

Reed, MJ ^{[1
]}

Waldeck, N ^{[1
]}

Bruening, RC ^{[1
]}

Noamesi, BK ^{[1
]}

Hector, RF ^{[1
]}

Carlson, TJ ^{[1
]}

King, SR ^{[1
]}

机构：

[1] Shaman Pharmaceut Inc, San Francisco, CA 94080 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1998年 / 41卷 / 06期

关键词：

D O I：

10.1021/jm9704816

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Using an ethnobotanical approach in combination with in vivo-guided fractionation as a means for lead discovery, cryptolepine was isolated as an antihyperglycemic component of Cryptolepis sanguinolenta. Two syntheses of cryptolepine, including an unambiguous synthesis, are reported. The hydroiodide, hydrochloride, and hydrotrifluoromethanesulfonate (hydrotriflate) salts of cryptolepine were synthesized, and a comparison of their spectral properties and their in vitro activities in a 3T3-L1 glucose transport assay is made. Cryptolepine and its salt forms lower blood glucose in rodent models of type II diabetes. While a number of bioactivities have been reported for cryptolepine, this is the first report that cryptolepine posesses antihyperglycemic properties.

引用

页码：894 / 901

页数：8

共 60 条

[41] From plant to patient: An ethnomedical approach to the identification of new drugs for the treatment of NIDDM [J].