ETHNOBOTANICAL-DIRECTED DISCOVERY OF THE ANTIHYPERGLYCEMIC PROPERTIESOF CRYPTOLEPINE - ITS ISOLATION FROM CRYPTOLEPISS-ANGUINOLENTA, SYNTHESIS, AND IN-VITRO AND IN-VIVO ACTIVITIES

Using an ethnobotanical approach in combination with in vivo-guided fr actionation as a means for lead discovery, cryptolepine was isolated a s an antihyperglycemic component of Cryptolepis sanguinolenta. Two syn theses of cryptolepine, including an unambiguous synthesis, are report ed. The hydroiodide, hydrochloride, and hydrotrifluoromethanesulfonate (hydrotriflate) salts of cryptolepine were synthesized, and a compari son of their spectral properties and their in vitro activities in a 3T 3-L1 glucose transport assay is made. Cryptolepine and its salt forms lower blood glucose in rodent models of type II diabetes. While a numb er of bioactivities have been reported for cryptolepine, this is the f irst report that cryptolepine posesses antihyperglycemic properties.