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Lactomycins A–C, dephosphorylated phoslactomycin derivatives that inhibit Cathepsin B, from the marine-derived streptomyces sp. ACT232

  • Yi Sun
  • , Rogie Royce Carandang
  • , Yuta Harada
  • , Shigeru Okada
  • , Kazutoshi Yoshitake
  • , Shuichi Asakawa
  • , Yuichi Nogi
  • , Shigeki Matsunaga
  • , Kentaro Takada

Research output: Contribution to journalArticlepeer-review

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 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.

Original languageEnglish (US)
Article number70
JournalMarine Drugs
Volume16
Issue number2
DOIs
StatePublished - Feb 2018
Externally publishedYes

Keywords

  • Cathepsin B
  • Enzyme inhibitory
  • Phoslactomycin
  • Streptomyces

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Pharmacology, Toxicology and Pharmaceutics (miscellaneous)

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