jm9704816_si_001.pdf (464.45 kB)
Ethnobotanical-Directed Discovery of the Antihyperglycemic Properties of Cryptolepine: Its Isolation from Cryptolepis sanguinolenta, Synthesis, and in Vitro and in Vivo Activities†
journal contribution
posted on 1998-02-24, 00:00 authored by Donald E. Bierer, Diana M. Fort, Christopher D. Mendez, 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. KingUsing 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.