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Lactomycins A-C, Dephosphorylated Phoslactomycin Derivatives that Inhibit Cathepsin B, from the Marine-derived Streptomyces sp. ACT232.

ABSTRACT: Three new polyketides, lactomycins A (1)-C (3), were isolated from the culture broth of a marine-derived Streptomyces sp. ACT232 as cathepsin B inhibitors. Their structures were determined by a combination of NMR and MS data analyses to be the dephosphorylated derivatives of a phoslactomycin class of metabolites. Lactomycins exhibited cathepsin B inhibitory activity (IC50 0.8 to 4.5 ?g/mL). Even though the biosynthetic gene clusters found in the genome of the current strain have high similarity to those of phoslactomycin, neither phoslactomycins nor leustroducsins were detected by LC-MS analyses of the crude extract.

SUBMITTER: Sun Y

PROVIDER: S-EPMC5852498 | biostudies-literature | 2018 Feb

REPOSITORIES: biostudies-literature

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Lactomycins A-C, Dephosphorylated Phoslactomycin Derivatives that Inhibit Cathepsin B, from the Marine-derived Streptomyces sp. ACT232.

Sun Yi Y Carandang Rogie Royce RR Harada Yuta Y Okada Shigeru S Yoshitake Kazutoshi K Asakawa Shuichi S Nogi Yuichi Y Matsunaga Shigeki S Takada Kentaro K

Marine drugs 20180221 2

Three new polyketides, lactomycins A (1)-C (3), were isolated from the culture broth of a marine-derived <i>Streptomyces</i> sp. ACT232 as cathepsin B inhibitors. Their structures were determined by a combination of NMR and MS data analyses to be the dephosphorylated derivatives of a phoslactomycin class of metabolites. Lactomycins exhibited cathepsin B inhibitory activity (IC50 0.8 to 4.5 μg/mL). Even though the biosynthetic gene clusters found in the genome of the current strain have high simi ...[more]

PMID: 29466301

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