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

1
Laboratory of Aquatic Natural Products Chemistry, Graduate School of Agricultural and Life Sciences, The University of Tokyo, Tokyo 113-8657, Japan
2
Laboratory of Aquatic Molecular Biology and Biotechnology, Graduate School of Agricultural and LifeSciences, The University of Tokyo, Tokyo 113-8657, Japan
3
Japan Agency for Marine-Earth Science and Technology (JAMSTEC), Natsushima, Yokosuka, Kanagawa237-0061, Japan
*
Authors to whom correspondence should be addressed.
Present address: Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China
Mar. Drugs 2018, 16(2), 70; https://doi.org/10.3390/md16020070
Received: 12 December 2017 / Revised: 12 February 2018 / Accepted: 12 February 2018 / Published: 21 February 2018
(This article belongs to the Special Issue Natural Products from Marine Actinomycetes)
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 μg/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. View Full-Text
Keywords: Streptomyces; cathepsin B; enzyme inhibitory; phoslactomycin Streptomyces; cathepsin B; enzyme inhibitory; phoslactomycin
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Sun, Y.; Carandang, R.R.; Harada, Y.; Okada, S.; Yoshitake, K.; Asakawa, S.; Nogi, Y.; Matsunaga, S.; Takada, K. Lactomycins A–C, Dephosphorylated Phoslactomycin Derivatives that Inhibit Cathepsin B, from the Marine-derived Streptomyces sp. ACT232. Mar. Drugs 2018, 16, 70.

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