RESUMO
The strain VUK-A was isolated from a sediment sample of the Coringa mangrove ecosystem was identified as Streptomyces cheonanensis based on morphological, physiological, biochemical and molecular properties. Chemical investigation of the secondary metabolites of the strain Streptomyces cheonanensis VUK-A has led to the segregation of two bioactive compounds, namely 2-Methyl butyl propyl phthalate (1) and Diethyl phthalate (2) using column chromatography. The chemical structure of the active compounds was established on the basis of spectroscopic analysis, including 1H NMR and 13C NMR spectroscopies, FTIR and EIMS. The antimicrobial activity of the bioactive compounds produced by the strain was tested against a wide variety of bacteria and fungi and expressed in terms of minimum inhibitory concentration. The compounds (1&2) were active against all the bacteria tested, and the best activity of compound 1 was recorded against Proteus vulgaris (4 µg/ml). Compounds (1&2) were active against dermatophytes and fungi but compound 1 displayed high antifungal activity against Candida albicans (8 µg/ml) and Fusarium solani (16 µg/ml) compared to standard antifungal agents. The cytotoxicity of the bioactive compound 1 was tested against MDA-MB-231, OAW-42, HeLa, and MCF-7 cell lines. The highest activity of 100 µM by compound 1 was recorded against HeLa cancer cell lines. In fact, this is the first report of 2-Methyl butyl propyl phthalate from the genus Streptomyces.
RESUMO
The present study was aimed to isolate novel bioactive compounds from actinomycetes species isolated from mangrove habitats. With this connection, Pseudonocardia endophytica (VUK-10) was isolated using dilution plate technique and was examined for its secondary metabolite profiling. After successive purification and spectroscopic characterization viz., FTIR, mass, NMR, DEPT, HMQC, HMBC, and COSY spectroscopy, two compounds were identified including a semi synthetic derivative N-(4-aminocyclooctyl)-3, 5-dinitrobenzamide (1), obtained from the precursor of novel natural product cyclooctane-1,4-diamine (3), along with a known compound 3-((1H-indol-6-yl) methyl) hexahydropyrrolo [1, 2-a] pyrazine-1, 4-dione (2). Anti cancer activities of the characterized compounds against in vitro cancerous cell line models, MDA-MB-231, OAW-42, HeLa, and MCF-7 reveal that HELA cells are most susceptible (IC50-10 nM compound 1 and 2) followed by other studied cells. On the other hand, antibacterial and antifungal activities of the studied compounds against tested pathogens revealed that there is a significant antimicrobial activity with all the tested bacterial and fungal species. Moreover, compound 1 showed the lowest MIC values against Streptococcus mutans as 4 and 16 µg/ml for Candida albicans. In conclusion, the identified novel chemical compounds in the present study may have a potential application in anticancer therapy as well as to mitigate the bacterial and fungal pathogens thus to control the infectious diseases.
RESUMO
Two proline containing cyclic dipeptides (CDPs), cyclo (L-Pro-L-Tyr) (1) and cyclo (L-Pro-L-Phe) (2) were isolated from the fermentation broth of Pseudonocardia endophytica VUK-10 originating from the Nizampatnam mangrove ecosystem on the south coast of Andhra Pradesh, India. The structures of the compounds were established by 1H NMR and 13C NMR spectroscopy, FTIR and EIMS. The antimicrobial and cytotoxic activities of the compounds were tested against a variety of medicinally and agriculturally important bacteria and fungi as well as on the MDA-MB-231, OAW-42, HeLa and MCF-7 human cell lines. Xanthomonas malvacearum was most sensitive toward 1 (MIC 4 µg/ml), whereas compound 2 had good antibacterial activity against Xanthomonas campestris (MIC 8 µg/ml). Fusarium solani was highly sensitive toward 1 (MIC 16 µg/ml). The compounds were cytotoxic against the human cell lines at micro molar concentrations; the highest activity (IC50 < 10 µM) of 1 was recorded against the MDA-MB-231 cancer cell line.