Ethnobotanical-Directed Discovery of the Antihyperglycemic Properties of Cryptolepine: Its Isolation from Cryptolepis sanguinolenta, Synthesis, and in Vitro and in Vivo Activities

• DOI: 10.1021/jm9704816
• Publication Date: 2002-07-26T05:23:55Z
• Authors: Donald E. Bierer; Diana M. Fort; Christopher D. Me...; Jian Luo; Patricia A. Imbach; Larisa G. Dubenko; Shivanand D. Jolad; R. Eric Gerber; Joane Litvak; Qing Lu; Pingsheng Zhang; Michael J. Reed; Nancy Waldeck; Reimar C. Bruening; Ben K. Noamesi; Richard F. Hector; Thomas J. Carlson; Steven R. King
• Keywords: Blood Glucose; Male; Indoles; Plant Extracts; Body Weight; Mice, Obese; 3T3 Cells; Fructose; In Vitro Techniques; 01 natural sciences; Diabetes Mellitus, Experimental; Indole Alkaloids; Rats; 0104 chemical sciences; 3. Good health; Eating; Mice; Alkaloids; Glucose; Adipose Tissue; Quinolines; Animals; Hypoglycemic Agents

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