Varacin: a novel benzopentathiepin from Lissoclinum vareau that is cytotoxic toward a human colon tumor

Journal of the American Chemical Society
1991.0

Abstract

Ascidians of the genus Lissoclinum have been an exceptional source of interesting and often biologically active natural products. Lissoclinum patella has yielded cytotoxic cyclic peptides, cytotoxic and antiviral polypropionate-derived macrocycles, and a polyketide lactone. Lissoclinum vareau, a lavender-colored encrusting species collected in the Fiji Islands, is the source of the recently reported bright red heteroaromatic pigments varamine A and varamine B. We now report the benzopentathiepin varacin (1), a novel L. vareau metabolite that exhibits potent antifungal activity against Candida albicans (14-mm zone of inhibition of 2 µg of varacin/disk) and cytotoxicity toward the human colon cancer HCT 116 with an IC50 of 0.05 µg/mL, 100 times the activity of 5-fluorouracil (5-FU) in this assay. Varacin also exhibited a 1.5-fold differential toxicity toward the CHO cell line EM9 (chlorodeoxyuridine sensitive) versus BR1 (BCNU resistant), providing preliminary evidence that varacin damages DNA.

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