Isolation and biological evaluation of N-(4-aminocyclooctyl)-3, 5-dinitrobenzamide, a new semisynthetic derivative from the Mangrove-associated actinomycete Pseudonocardia endophytica VUK-10.

Abstract:

: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.

journal_name

3 Biotech

journal_title

3 Biotech

authors

Mangamuri UK,Vijayalakshmi M,Poda S,Manavathi B,Chitturi B,Yenamandra V

doi

10.1007/s13205-016-0472-0

subject

Has Abstract

pub_date

2016-12-01 00:00:00

pages

158

issue

2

eissn

2190-572X

issn

2190-5738

pii

10.1007/s13205-016-0472-0

journal_volume

6

pub_type

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