Four new tetromycin derivatives, tetromycins 1 – 4 and a previously known one, tetromycin B ( 5 ) were isolated from Streptomyces axinellae Pol001 T cultivated from the Mediterranean sponge Axinella polypoides . Structures were assigned using extensive 1D and 2D NMR spectroscopy as well as HRESIMS analysis. The compounds were tested for antiparasitic activities against Leishmania major and Trypanosoma brucei , and for protease inhibition against several cysteine proteases such as falcipain, rhodesain, cathepsin L, cathepsin B, and viral proteases SARS-CoV M pro , and PL pro . The compounds showed antiparasitic activities against T. brucei and time-dependent inhibition of cathepsin L-like proteases with K i values in the low micromolar range.
【저자키워드】 marine sponge, tetromycin, anti-trypanosomal, protease inhibition, Streptomyces axinellae, 【초록키워드】 Structure, protease, antiparasitic, activity, NMR spectroscopy, cathepsin B, Analysis, cathepsin L, Leishmania major, Compound, cysteine protease, derivative, Trypanosoma, derivatives, protease inhibition, tested, assigned, SARS-CoV M, New, Axinella, Streptomyce,