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 language | English (US) |
|---|---|
| Article number | 70 |
| Journal | Marine Drugs |
| Volume | 16 |
| Issue number | 2 |
| DOIs | |
| State | Published - Feb 2018 |
| Externally published | Yes |
Keywords
- Cathepsin B
- Enzyme inhibitory
- Phoslactomycin
- Streptomyces
ASJC Scopus subject areas
- Pharmaceutical Science
- Drug Discovery
- Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
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