期刊
MARINE DRUGS
卷 17, 期 1, 页码 -出版社
MDPI
DOI: 10.3390/md17010058
关键词
amphidinolides; Stragulum bicolor; cytotoxic macrolides; stereochemistry
资金
- CNR
- CNPq [490247/2011-3]
- Antitumor Drugs and Vaccines from the Sea (ADViSE) [PG/2018/0494374]
Amphidinolides are cytotoxic macrolides produced by symbiotic unicellular microalgae of the genus Amphidinium. Here we describe the identification of four related molecules belonging to this macrolide family isolated from the invertebrate Stragulum bicolor. The new molecules, named amphidinolide PX1-PX3 and stragulin A (1-4), show an unprecedented carbon skeleton whose complete stereochemistry has been determined by spectroscopic and computational methods. Differences in the structures of these molecules modulate their biological activity in a panel of tumor cell lines, but the opened derivative stragulin (4) shows a very potent and specific cytotoxic activity (IC50 0.18 mu M) against the aggressive human melanoma cell A2058.
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