A SCALABLE METHOD FOR THE ISOLATION OF ANTI-HIV AGENTS FROM THE TROPICAL PLANT $i(CALOPHYLLUM)

An efficient and scalable method is reported for the isolation of costatolide (2), an HIV-1-specific nonnucleoside reverse transcriptase inhibitor (NNRTI), from the latex of Calophyllum plants such as C. teysmannii var. inophylloide. An overall yield of 10.6% of costatolide, with a purity of 96%, wa...

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Hauptverfasser: XU, ZE-QI, ANDERSON, HERBERT, M, FLAVIN, MICHAEL, T, JENTA, TUAH, R, LIN, YUH-MEEI, WILLIAMS, MICHAEL, J
Format: Patent
Sprache:eng ; fre ; ger
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Zusammenfassung:An efficient and scalable method is reported for the isolation of costatolide (2), an HIV-1-specific nonnucleoside reverse transcriptase inhibitor (NNRTI), from the latex of Calophyllum plants such as C. teysmannii var. inophylloide. An overall yield of 10.6% of costatolide, with a purity of 96%, was obtained by repetitive recrystallization of the latex from a single organic solvent after the oily material was removed by treatment with hexane. A second major component of the latex, soulattrolide (3), another HIV-1 NNRTI, was also isolated. Both compounds were characterized by spectroscopic and chromatographic analyses and their in vitro anti-HIV activities were also confirmed. The results suggest that sufficient supplies of costatolide can be obtained in a relatively low-cost manner from natural sources.