RESUMEN
A new medermycin analog (1) was isolated from the marine-derived actinomycetes Streptomyces sp. ZS-A45. The structure elucidation of compound 1 was determined by the HRESIMS and extensive NMR analysis. And compound 1 exhibited significant cytotoxicity against PC3 cell lines with IC50 values of 0.81 ± 0.42 µm.
Asunto(s)
Actinobacteria/metabolismo , Antibacterianos/aislamiento & purificación , Antibacterianos/química , Antibacterianos/farmacología , Línea Celular Tumoral , Dicroismo Circular , Humanos , Espectroscopía de Resonancia Magnética , Biología Marina , Naftoquinonas/aislamiento & purificaciónRESUMEN
Four new medermycin-type naphthoquinones, strepoxepinmycins A-D (1-4), and one known compound, medermycin (5), were identified from Streptomyces sp. XMA39. Their structures were elucidated by analysis of HRESIMS, 1D and 2D NMR spectroscopic data, and ECD calculations. Among these compounds, strepoxepinmycin A (1) represents a rare 5,10-oxepindione ring system typically formed by a Baeyer-Villiger oxidation, and strepoxepinmycin B (2) is an isolation artifact derived from 1. Bioactivity evaluations of these compounds showed that compounds 3 and 4 exhibited cytotoxicity against HCT-116 and PC-3 cancer cell lines and 4 exhibited moderate inhibition of ROCK 2 protein kinase. In addition, all of the new compounds showed antibacterial activity against Escherichia coli and methicillin-resistant Staphylococcus aureus and antifungal activity against Candida albicans.
Asunto(s)
Naftoquinonas/aislamiento & purificación , Streptomyces/metabolismo , Microbiología del Agua , Antiinfecciosos/farmacología , Antineoplásicos/farmacología , Línea Celular Tumoral , Humanos , Naftoquinonas/química , Naftoquinonas/farmacologíaRESUMEN
On the basis of the one strain-many compounds strategy, five compounds including two new holomycin derivatives 2 - 3, two new cyclopropaneacetic acid derivatives 4 - 5, together with one known compound holomycin (1) were isolated from a marine-derived bacterium Streptomyces sp. DT-A37. Their structures were elucidated using NMR and HR-ESI-MS analyses. All these compounds were evaluated for their antimicrobial activity, cytotoxic activity, and inhibitory activity against BRD4 protein. Compound 1 exhibited potent cytotoxicity against H1975 cells with IC50 value of 1 µm, and its minimal inhibitory concentration values against Escherichia coli and Staphylococcus aureus were both 64 µm.