Antitumor compounds from tunicates.

摘要: Of the six marine-derived compounds that have reached clinical trials as antitumor agents three-didemnin B, Aplidine, and ecteinascidin 743-are derived from tunicates. Di-demnin B (DB), a cyclic depsipeptide compound tunicate Trididemnum solidum, was first to enter Phases I II trials. The Phase studies, sponsored by U. S. National Cancer Institute, indicated complete or partial remissions with non-Hodgkins lymphoma, but cardiotoxicity caused didemnin be dropped further study. closely related dehydrodidemnin (DDB, Aplidine) isolated in 1988 second colonial tunicate, Aplidium albicans, spectroscopic studies assigned structural formula which pyruvyl group DDB replaced lactyl DB syntheses of been achieved. Aplidine is more active than lacks DB's cardiotoxicity. It introduced PharmaMar into January 1999. family tunicate-derived are ecteinascidins (ETs), mangrove Ecteinascidia turbinata. extracts E. turbinata were described 1969, small amount ETs prevented their isolation for over decade. structures mainly spectroscopy. ET 743 underway. Future supplies ET's should available aquaculture synthesis.