Objectives: The purpose of the study is to characterize antimycobacterial phytoconstituent from ethyl acetate extract of dried bulbs of Allium sativum Linn. (Alliaceae) and elucidating the probable mode of action of the bioactive molecule.Methods: Serial extraction, Mycobacterium tuberculosis assay by agar well diffusion method, minimal inhibitory concentration by microplate alamar blue assay, Fourier transform infrared (FT-IR), nuclear magnetic resonance (NMR) spectroscopy, liquid chromatography (LC)-electrospray ionization (ESI)-mass spectrometry (MS)/MS, cell leakage assay, scanning electron microscopy (SEM), inhibition property of linear alkylbenzene sulfonate (LAS) in the presence of rifampicin on M. tuberculosis were performed.Results: Ethyl acetate extract displayed significant inhibition properties against M. tuberculosis H37Ra (MTCC 300). Subsequently, the bioactivity-guided fractionation was employed to purify the phytochemical. Analysis of FT-IR, LC-MS (ESI), 1H, and13C-NMR spectrum revealed that the bioactive phytochemicals are the variants of LAS, with C12-alkyl being predominant, and the minimum inhibitory concentration was found to be 5.56 μg/ml. Morphological examination by SEM and cell leakage assay indicated that these molecules change the membrane fluidity.Conclusion: The results thus suggest the possibility of using low concentrations of LAS to effect changes in membrane fluidity, thereby enhancing the efficacy of antibiotic treatment.

Jayaraman G

Department of Biotechnology

School of Bio Sciences and Technology

Vellore Campus

Muniyan R

Varatharajan S

Naz S

Nandicoori V.K

Fulltext

Vellore Institute of Technology (VIT) is a private university located in&nbsp;Tamil Nadu, India. Founded in 1984, as Vellore Engineering College, the institution offers 20 undergraduate, 34 postgraduate, four integrated and four research programs. It has campuses in Vellore, Amravati, Bhopal and Chennai.

VIT is one of the top ranked private universities in India according to NIRF, THE and QS Rankings.&nbsp;Govt. of India has recognized&nbsp;VIT, Vellore as an&nbsp;Institution of Eminence. This has allowed VIT to take independent quality initiatives and move up in world ranking.

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VIT University

Asian Journal of Pharmaceutical and Clinical Research

Context: The bulb of Allium sativum Linn (Alliaceae) has numerous medicinal values. Though the petroleum ether extract of the bulb has shown to exhibit antimycobacterial activity, the phytochemical(s) responsible for this inhibitory activity is not known. Objective: To characterize the bioactive compounds in the petroleum ether extract of Allium sativum (garlic) that inhibit the growth of Mycobacterium tuberculosis H37Ra. Materials and methods: Bioactivity-guided fractionation was employed to isolate the bioactive compounds. Antimycobacterial activity was evaluated by well-diffusion method and microplate alamar blue assay (MABA). Infrared spectroscopy, mass spectrometry and nuclear magnetic resonance spectroscopy were used to characterize the bioactive compounds. Autodock was used to obtain information on molecular recognition, and molecular dynamics simulation was performed using GROMACS. Results: The bioactive compounds that inhibited the growth of M. tuberculosis H37Ra were found to be lauric acid (LA) and myristic acid (MA). The minimal inhibitory concentration of LA and MA was found to be 22.2 and 66.7 μg/mL, respectively. In silico analysis revealed that these fatty acids could bind at the cleft between the N-terminal and C-terminal lobes of the cytosolic domain of serine/threonine protein kinase B (PknB). Discussion and conclusion: The inhibition activity was dependent on the alkyl chain length of the fatty acid, and the amino acid residues involved in binding to fatty acid was found to be conserved across the Pkn family of proteins. The study indicates the possibility of using fatty acid derivatives, involving Pkn family of proteins, to inhibit the signal transduction processes in M. tuberculosis. © 2016 Informa UK Limited, trading as Taylor &amp; Francis Group.

Pharmaceutical Biology

Lauric acid and myristic acid fromAllium sativuminhibit the growth ofMycobacterium tuberculosisH37Ra:in silicoanalysis reveals possible binding to protein kinase B

Molecules

Membrane Interactions of Phytochemicals as Their Molecular Mechanism Applicable to the Discovery of Drug Leads from Plants

Encyclopedia of Membranes

Nanotechnology Membrane

Edible Medicinal and Non Medicinal Plants

Allium sativum

European Journal of Medicinal Chemistry

Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells

ALLIUM SATIVUM LINN. CONTAINS LINEAR ALKYLBENZENE SULFONATES THAT ALTER MEMBRANE FLUIDITY FOR THE INHIBITION OF MYCOBACTERIUM TUBERCULOSIS H37RA

Journal	Asian Journal of Pharmaceutical and Clinical Research
Publisher	Innovare Academic Sciences Pvt Ltd
ISSN	0974-2441
Open Access	Yes