title: Anti-mycobacterial activity of plumericin and isoplumericin against MDR Mycobacterium tuberculosis.
abstract: OBJECTIVE
  Because of the developing resistance of Mycobacterium species against currently available anti-mycobacterial drugs, there is an urgent need for new drug development. In this study, we have evaluated the in vitro anti-mycobacterial activity of Plumeria bicolor extract and its phytoconstituents - plumericin and isoplumericin against multi-drug resistance Mycobacterium tuberculosis.
  
  
  METHODS
  The in vitro anti-mycobacterial activity of chloroform extract of P. bicolor, plumericin and isoplumericin were tested against M. tuberculosis (H37Rv) and four multi-drug resistant (MDR) clinical isolates by measuring the minimum inhibitory concentration (MIC) using MTT (Tetrazolium bromide [3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide]) assay. The extract and both compounds were further evaluated by standard assay procedures to determine their minimum bactericidal concentration (MBC). Cytotoxicity of these compounds was performed against J774G8 murine macrophage cell lines. The activity was represented in the mean (±SD) of duplicate samples from three independent assays.
  
  
  RESULTS
  Plumericin showed better activity against pan sensitive as well as four MDR strains of M. tuberculosis with MIC values of 2.1 ± 0.12, 1.3 ± 0.15, 2.0 ± 0.07, 1.5 ± 0.13 & 2.0 ± 0.14 μg/mL and MBC values of 3.6 ± 0.22, 2.5 ± 0.18, 3.8 ± 0.27, 2.9 ± 0.20 & 3.7 ± 0.32 μg/mL than isoplumericin, respectively. Interestingly, both isolated active compounds showed an advantage over rifampicin (80 times) and isoniazid (8 times) by being highly active against the MDR strains. The extract and both compounds were found to be non-toxic against J774G8 macrophages up to the used concentrations.
  
  
  CONCLUSIONS
  Plumericin showed more potent activity than isoplumericin. The excellent activity of these compounds against MDR strains opens a possibility of obtaining new anti-mycobacterial drug candidate in near future.
authors: Department of Laboratory Medicine, All India Institute of Medical Sciences, New Delhi 110 029, India.
authors: Parveen
authors: P
authors: Kumar
authors: Amit
authors: A
authors: Singh
authors: Umakant
authors: U
authors: Sharma
authors: Dharmendra
authors: D
authors: Singh
authors: M P
authors: MP
authors: Dobhal
authors: Sarman
authors: S
authors: Singh
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D029062:Apocynaceae; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007192:Indenes / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D039823:Iridoids / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis; D010936:Plant Extracts; D018088:Tuberculosis, Multidrug-Resistant / Q000188:drug therapy*
chemical_list: D000995:Antitubercular Agents; D007192:Indenes; D039823:Iridoids; D010936:Plant Extracts; C516952:isoplumericin; C068511:plumericin