An Anti-microbial Terpenoid Fraction from Gymnema sylvestre Induces Flip-flop of Fluorescent-Phospholipid Analogs in Mod
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An Anti-microbial Terpenoid Fraction from Gymnema sylvestre Induces Flip-flop of Fluorescent-Phospholipid Analogs in Model Membrane Himadri Gourav Behuria 1
& Santosh Kumar Sahu
1
Received: 21 May 2020 / Accepted: 16 July 2020/ # Springer Science+Business Media, LLC, part of Springer Nature 2020
Abstract
Therapeutic potential of Gymnema sylvestre on diverse cell types is predominantly due to a variety of terpenoids and their derivatives. However, their bioavailability becomes limited due to poor solubility and lower lipophilic properties, provoking the search for novel membranotropic terpenoids and their mechanism of action. A terpenoid fraction purified from Gymnema sylvestre exhibited broad spectrum antimicrobial activity against both Gram positive and Gram negative bacteria with IC50 ˂ 0.1 mg/ml. Evaluation of its membranotropic effect in vitro on reconstituted model membrane revealed that the fraction induced flip-flop of fluorescent phospholipid analogs across the lipid bilayer. The terpenoid-induced lipid flipping was biphasic with a fast linear phase (rate constant (k1) = 3 to 5 S−1) and a second slow exponential phase (rate constant (k2) = (4 to 9) × 10−3 S−1). The lipid-flippase activity of the terpenoid fraction showed concentration and incubation-dependent cooperativity, indicating their lipophilic nature and membranedestabilizing activity that facilitated lipid translocation. For the first time, our study reveals the flippase activity of a terpenoid fraction of Gymnema sylvestre that could be further explored for their membrane-mediated pharmacological properties.
Keywords Gymnema sylvestre . Giant unilamellar vesicles . Phospholipid . Flippase . Terpenoids Abbreviations CETFGS CHCl3-extracted terpenoid fraction of Gymnema sylvestre DMSO Dimethyl sulfoxide Egg-PC Egg-phosphatidylcholine EA Ethyl acetate * Santosh Kumar Sahu [email protected] Himadri Gourav Behuria [email protected]
1
Department of Biotechnology, North Orissa University, Mayurbhanj, Baripada, Odisha 757003, India
Applied Biochemistry and Biotechnology
FTIR GA GUV HEPES IC50 LSS NAO NBD-PE PE PL
Fourier-transform infrared spectroscopy Gymnemic acid Giant unilamellar vesicle N-(2-hydroxyethyl)piperazine-N′-2-ethanesulfonic acid Inhibitory concentration for 50% growth reduction Low salt solution 10 N-nonyl acridine orange N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)-1,2-dihexadecanoyl-sn-glycero-3phosphoethanolamine, triethylammonium salt Phosphatidylethanolamine Phospholipid
Introduction Terpenoids are bioactive compounds having a carbon skeleton made from 1 to 8 isoprenoid units and diverse functional groups those may or may not have a cyclic structure. They are widely used as antitumor, antiviral, antidiabetic, anti-inflammatory, hepatoprotective, analgesic, antimicrobial, and immunomodulatory therapeutics [1]. Bioactivity of terpenoids is based on their interaction with cellular membranes that leads to increased membrane permeability, loss of barrier function, uncoupling of oxidative phosphorylation, and membrane lysi
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