Abstract

Because of the special living environment, marine-derived actinomycetes, especially the genus Streptomyces, possess distinct and complex metabolic capabilities, resulting in wide diversity of their secondary metabolites in chemical structures and biological activities.1 Among them, many valuable lead compounds were obtained for discovery of new antibiotics.2, 3, 4 Bafilomycins are a family of polyene macrolides containing a 16-member lactone ring. Thirteen bafilomycin antibiotics have been isolated, including bafilomycins A1, A2, B1, B2, C1 and C2 from Streptomyces griseus sp. sulphurus (TU 1922),5 bafilomycins D and E from S. griseus TU 25996 and bafilomycins F–J from Streptomyces spp.7 Among them, bafilomycins D and E contain the ring-opened side chain different from other bafilomycins. Bafilomycins have antibacterial, antifungal, antineoplastic and immunosuppressive activities.5 Some bafilomycins are specific inhibitors of vacuolar-type H+-ATPase (V-ATPase),8, 9, 10, 11 in which bafilomycin A1 is the most used. Being a specific inhibitor of V-ATPase, bafilomycin A1 can prevent the re-acidification of synaptic vesicles once they have undergone exocytosis. In addition, bafilomycin A1 has antimalarial activity.12 Bafilomycins B1 and C1 have been mentioned as potential antiosteoporotic agents in treating bone lytic diseases.

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