Details

Autor(en) / Beteiligte

• Bierer, Donald E
• Fort, Diana M
• Mendez, Christopher D
• Luo, Jian
• Imbach, Patricia A
• Dubenko, Larisa G
• Jolad, Shivanand D
• Gerber, R. Eric
• Litvak, Joane
• Lu, Qing
• Zhang, Pingsheng
• Reed, Michael J
• Waldeck, Nancy
• Bruening, Reimar C
• Noamesi, Ben K
• Hector, Richard F
• Carlson, Thomas J
• King, Steven R

Titel

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

Ist Teil von

• Journal of medicinal chemistry, 1998-03, Vol.41 (6), p.894-901

Ort / Verlag

Washington, DC: American Chemical Society

Erscheinungsjahr

1998

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• 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.