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1.
J Appl Microbiol ; 121(4): 973-87, 2016 Oct.
Article in English | MEDLINE | ID: mdl-27406903

ABSTRACT

AIMS: The aim of this study was to isolate and characterize the bioactive compound of Micromonospora auratinigra, HK-10 and its antibacterial inhibitory mechanism. METHODS AND RESULTS: An oily bioactive compound was extracted from HK-10 (GenBank accession no. JN381554) and found to have promising antibacterial activity. The compound was characterized as 2-methylheptylisonicotinate (1) by (1) H, (13) C NMR and mass spectroscopy. Minimum inhibitory concentration (MIC) of this molecule was tested by micro broth dilution method and was found to be 70, 40, 80, 60, 60 and 50 µg for Staphylococcus aureus, Bacillus subtilis, Proteus vulgaris, Echerichia coli, Pseudomonas aeruginosa and Mycobacterium abscessus respectively. The effects of compound 1 were studied on bacterial membrane structure using scanning electron microscopy. The results indicated a membrane-disrupting mechanism, resulting in the dysfunction of the cytoplasmic membrane structure and cell death of the pathogenic bacterial strains. Kinetics of growth of the test organisms was also analysed and indicated 2-methylheptylisonicotinate 1 as a bactericidal agent. Furthermore, we have studied the binding affinity of 1 towards different membrane proteins of pathogenic bacteria by in silico analysis. CONCLUSIONS: 2-methylheptylisonicotinate was isolated from M. auratinigra, a rare actinobacterial strain possessing antibacterial activity through a membrane-disrupting mechanism, and has MICs similar to standard antibiotic neomycin sulphate. It is the first report about a strain of M. auratinigra, isolated from Indo-Burma biodiversity hotspot of North-east India with new antimicrobial activities. In silico studies have also supported these results performed on various membrane targets of pathogenic bacteria. SIGNIFICANCE AND IMPACT OF THE STUDY: The antibacterial potential of M. auratinigra is reported for the first time. The results indicate the possible use of 2-methylheptylisonicotinate as a source of antibacterial agent against dreaded human pathogens.


Subject(s)
Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/pharmacology , Bacteria/drug effects , Isonicotinic Acids/isolation & purification , Isonicotinic Acids/pharmacology , Micromonospora/chemistry , Soil Microbiology , Bacteria/classification , Humans , India , Kinetics , Microbial Sensitivity Tests , Micromonospora/classification , Micromonospora/ultrastructure
2.
Arch Pharm Res ; 34(3): 377-82, 2011 Mar.
Article in English | MEDLINE | ID: mdl-21547668

ABSTRACT

Forty-one compounds including two new constituents, senecainin A (1) and 3-methoxyisonicotinic acid (2), were characterized from the methanol extracts of the whole plant of Senecio scandens. The structures of the new compounds were comprehensively established with the aid of 1D and 2D NMR spectroscopic and mass spectrometric analyses. The chemical structures of known compounds were identified by comparison of their spectroscopic and physical data with those reported in the literature. In addition, the antioxidant activity of some of the isolates was examined in the DPPH free radical scavenging assay. Among the tested compounds, (-)-monoepoxylignanolide, (-)-pinoresinol and (-)-epi-pinoresinol displayed significant antioxidant bioactivity.


Subject(s)
Antioxidants/pharmacology , Cyclohexanones/pharmacology , Drugs, Chinese Herbal/pharmacology , Isonicotinic Acids/pharmacology , Senecio/chemistry , Antioxidants/isolation & purification , Biphenyl Compounds/chemistry , Cyclohexanones/isolation & purification , Drugs, Chinese Herbal/isolation & purification , Free Radical Scavengers/isolation & purification , Free Radical Scavengers/pharmacology , Free Radicals/chemistry , Isonicotinic Acids/isolation & purification , Molecular Structure , Picrates/chemistry
3.
J Chromatogr B Biomed Sci Appl ; 754(2): 477-86, 2001 Apr 25.
Article in English | MEDLINE | ID: mdl-11339291

ABSTRACT

New methods of ion interaction reagent (IIR) RP-HPLC are presented for the determination of anti-tuberculosis drugs and their metabolites, singly or in multi-component mixtures, in biological fluids. The following analytes are considered: isoniazid, ethionamide, pyrazinamide, morphazinamide, p-aminosalicylic acid, nicotinic and isonicotinic acids. Aqueous solutions of three different ion interaction reagents are alternatively or comparatively used as the mobile phases, namely: (A) 5.00 mM octylamine at pH 3.00 for o-phosphoric acid, (B) 5.00 mM octylamine at pH 8.00 for o-phosphoric acid, and (C) 5.00 mM 1,6 diaminohexane at pH 6.00 for o-phosphoric acid. The response linearity between peak area and analyte concentration is verified for all the analytes in the concentration range within the determination limits and 2.00 mg/l. Detection limits are always lower than 82 microg/l for standard solutions; in the analysis of samples of rat serum, rat plasma and human serum, the matrix effect is negligible, the detection limits are always lower than 94 microg/l and the average recovery yield is always greater than 96%.


Subject(s)
Antitubercular Agents/blood , Chromatography, High Pressure Liquid/methods , Aminosalicylic Acid/blood , Aminosalicylic Acid/metabolism , Animals , Antitubercular Agents/metabolism , Calibration , Ethionamide/blood , Ethionamide/metabolism , Humans , Isoniazid/blood , Isoniazid/metabolism , Isonicotinic Acids/isolation & purification , Niacin/isolation & purification , Pyrazinamide/blood , Pyrazinamide/metabolism , Pyrazines/blood , Pyrazines/metabolism , Quality Control , Rats
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