Anticancer and antibacterial flavonoids from the callus of Ampelopsis grossedentata; a new weapon to mitigate the proliferation of cancer cells and bacteria.

A new flavonoid angelioue (1) together with five known compounds cuminatanol (2), myricetin (3), epigallocatechin (4), taxifolin (5) and dihydromyricetin (6) was isolated from the callus extract of Ampelopsis grossedentata (Hand.-Mazz.) W. T. Wang and the structures were elucidated based on their detailed spectroscopic data. Among the compounds, the new compound angelioue (1) displayed significant antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) with the MIC value of 6.68 µg mL-1 and MBC value of 53.42 µg mL-1; in contrast the other compounds showed moderate to no antibacterial activity. In addition, known dihydromyricetin (6) exhibited potent cytotoxic activities against mouse breast cancer cells (4T1), human lung adenocarcinoma (A549) and human non-small cell lung cancer (NCI-H1975) tumor cell lines with GI50 values of 17.47, 18.91 and 20.50 µM mL-1, respectively. The compounds 1-5 exhibited low micro-molar inhibitory activities. Moreover, the structure-activity relationships of the most active compounds for antibacterial and cytotoxic activities are discussed. The present findings clearly suggest that the A. grossedentata callus is a good source of bioactive compounds.

Susceptibility pattern of methicillin resistance Staphylococcus aureus (MRSA) by flow cytometry analysis and characterization of novel lead drug molecule from Streptomyces species.

BACKGROUND: Actinomycetes particularly, Streptomyces species are producing wide variety of natural products with potential bioactivities. The microbial-derived metabolites hold a strong position to combat emerging and re-emerging antimicrobial drug-resistant pathogens. OBJECTIVES: A diverse group of actinomycetes strains were isolated from unexplored regions of mangrove sediment. Further, a polyphasic approach based on 16S rRNA gene sequence analysis and to evaluate their antibacterial potential against a panel of bacterial pathogens and methicillin resistance Staphylococcus aureus (MRSA). METHODS: The mangrove sediment samples were serially diluted with sterile water and plated on inorganic starch agar medium. A total of 20 isolates were pure cultured and 16S rRNA gene sequences were deposited in the public nucleotide databases (GenBank, NCBI). All the isolates were screened for the antibacterial activity by agar overlay method. Further, the susceptibility pattern of MRSA by flow cytometry and fluorescence microscopy was analysed. RESULTS: These twenty different isolates were grouped under nine major clad and they shared 95-99% sequence identity to the 16S rRNA gene sequences of the genus Streptomyces in the public nucleotide databases. Among these strains, the isolates namely JRG-02, JRG-03, JRG-04, JRG-10 and JRG-12 exhibited a broad-spectrum antibacterial activity against Methicillin-resistant Staphylococcus aureus(MRSA) and Gram negative bacteria Klebsiella pneumoniae MTCC109. Furthermore, we have characterized the antibacterial compound production and its properties from the isolate JRG-02, a potential drug candidate. The culture conditions and various nutrient components of strain Streptomyces sp. JRG-02 were optimized for enhanced antibiotics production of the isolate. The FT-IR and LCMS spectrum analysis envisaged the chemical nature of the substance. The effect of antibacterial compound on the viability of MRSA was alone examined by flow cytometry (FACS) and fluorescence microscopy analysis. CONCLUSIONS: The present study clearly shows that the survival of diverse inhabitants of Streptomyces in the mangrove sediments. Hence, the mangrove sediment inhabiting strain Streptomyces sp. JRG-02 has potential pharmaceutical activity and genetic diversity.