Synthesis of Isocryptolepine, an Alkaloid from Cryptolepis sanguinolenta. -The title alkaloid (V) is synthesized by selective N5-methylation of known indoloquinoline (II) which can be easily prepared from aniline ( I) in four steps.
Antimalarial Activity of Cryptolepine and Isocryptolepine, Alkaloids Isolated from Cryptolepis sanguinolenta
✍ Scribed by Phillippe Grellier; Lobo Ramiaramanana; Valérie Millerioux; Eric Deharo; Joseph Schrével; François Frappier; François Trigalo; Bernard Bodo; Jean-Louis Pousset
- Publisher
- John Wiley and Sons
- Year
- 1996
- Tongue
- English
- Weight
- 493 KB
- Volume
- 10
- Category
- Article
- ISSN
- 0951-418X
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✦ Synopsis
Cryptolepis sanguinolenta extracts are currently used by African herbalists to cure malaria but the compounds involved in its antimalarial activity have not been identified. Two alkaloids, cryptolepine and isocryptolepine, have been isolated from the roots of C. sunguinolenta and their antimalarial activity evaluated. Both alkaloids possess intrinsic inhibitory activity against the human malaria parasite, Plasmodium fakiparum in vitro, whatever the chloroquine-resistance status of the strains used. Cryptolepine was slightly more efficient for parasite killing with an ICs in the range of 0.2 to 0.6 p~ compared with an ICso of about 0.8 PM for isocryptolepine. The antimalarial activity of cryptolepine was confirmed in vivo on the rodent malarial parasites Plasmodium vinckei petleri and Plasmodium berghei ANKA.
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