Scalable method for the isolation of anti-HIV agents from the tropical plant calophyllum
US6160131A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Dec 17, 1998 |
| Grant date | Dec 12, 2000 |
| Priority date | — |
| Expiry date | Dec 17, 2018 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D493/14
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.