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Benastatin A is a polyketide synthase-derived benastatin that has been found in Streptomyces and has diverse biological activities.1,2,3 It inhibits glutathione S-transferase (GST; Ki = 5 μM for the rat liver enzyme).2 Benastatin A is active against several bacteria, including methicillin-resistant S. aureus (MRSA; MIC = 3.12 μg/ml). It induces apoptosis and cell cycle arrest at the G1/G0 phase in Colon 26 mouse colon cancer cells when used at concentrations of 20 and 16 μM, respectively.3

1.Xu, Z., Schenk, A., and Hertweck, C.Molecular analysis of the benastatin biosynthetic pathway and genetic engineering of altered fatty acid-polyketide hybridsJ. Am. Chem. Soc.129(18)6022-6030(2007) 2.Aoyagi, T., Aoyama, T., Kojima, F., et al.Benastatins A and B, new inhibitors of glutathione S-transferase, produced by Streptomyces sp. MI384-DF12. I. Taxonomy, production, isolation, physico-chemical properties and biological activitiesJ. Antibiot. (Tokyo)45(9)1385-1390(1992) 3.Kakizaki, I., Ookawa, K., Ishikawa, T., et al.Induction of apoptosis and cell cycle arrest in mouse colon 26 cells by benastatin AJpn. J. Cancer Res.91(11)1161-1168(2000)

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