In vitro: |
Chem Pharm Bull (Tokyo). 1986 Jan;34(1):340-4. | Studies of platelet activating factor (PAF) antagonists from microbial products. I. Bisdethiobis(methylthio)gliotoxin and its derivatives[Reference: WebLink] | METHODS AND RESULTS: A platelet activating factor (PAF) antagonist, designated as FR-49175, was isolated from fermentation products of Penicillium terlikowskii and identified as Bisdethiobis(methylthio)gliotoxin (1). The IC50 value of this compound for PAF-induced rabbit platelet aggregation was 8.4 μM.Some derivatives of Bisdethiobis(methylthio)gliotoxin (1) were synthesized and their inhibitory activities of PAF-induced platelet aggregation were examined.
CONCLUSIONS:
Among these compounds, 5a, 6-anhydrobisdethio-3, 10a-bis(methylthio)gliotoxin (8) showed the most potent PAF inhibitory activity (IC50; 4.4 μM). | Tetrahedron Letters, 2013, 54(8):744-748. | Penicolinates A–E from endophytic Penicillium sp. BCC16054[Reference: WebLink] | METHODS AND RESULTS: Five new picolinic acid derivatives, penicolinates A–E (1–5), together with four known compounds including phenopyrrozin (6), p-hydroxyphenopyrrozin (7), gliotoxin (8), and Bisdethiobis(methylthio)gliotoxin (9) were isolated from endophytic Penicillium sp. BCC16054. The chemical structures were established from spectroscopic data-1D and 2D NMR experiments, IR, UV, and HRESIMS. CONCLUSIONS: These compounds were evaluated for antimalarial and antitubercular activities and for their activity against Bacillus cereus and Candida albicans along with cytotoxicity against both cancerous and non-cancerous cells. |
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