1. Borrelidins F-I, cytotoxic and cell migration inhibiting agents from mangrove-derived Streptomyces rochei SCSIO ZJ89.
- Author
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Sun J, Shao J, Sun C, Song Y, Li Q, Lu L, Hu Y, Gui C, Zhang H, and Ju J
- Subjects
- Antineoplastic Agents chemistry, Antineoplastic Agents isolation & purification, Cell Line, Cell Movement drug effects, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, Fatty Alcohols chemistry, Fatty Alcohols isolation & purification, Fatty Alcohols pharmacology, Humans, Molecular Structure, Structure-Activity Relationship, Wound Healing drug effects, Antineoplastic Agents pharmacology, Streptomyces chemistry
- Abstract
Borrelidin A (1) is produced by several species of Streptomyces and within its bioactive scaffold, the vinylic nitrile moiety is essential for activity. We report herein newly discovered members of the borrelidin family, borrelidin F (2), borrelidin G (3), borrelidin H (4) and borrelidin I (5); all were isolated from Streptomyces rochei SCSIO ZJ89 originating from a mangrove-derived sediment sample. These structurally diverse metabolites enabled a number of new structure-activity relationships (SARs) to be identified, especially with respect to the different configurations at the C11-OH and C12-C15 double bonds for which the absolute configurations were determined using spectroscopic methods. Importantly, borrelidin H (4) was found to have a therapeutic window superior to that of borrelidin A (1) in vitro and could inhibit migration of cancer cells., (Copyright © 2018 Elsevier Ltd. All rights reserved.)
- Published
- 2018
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