Pithayanukul Pimolpan, Ruenraroengsak Pakatip, Bavovada Rapepol, Pakmanee Narumol, Suttisri Rutt, Saen-oon Suwipa
Faculty of Pharmacy, Mahidol University, Bangkok, Thailand.
J Ethnopharmacol. 2005 Mar 21;97(3):527-33. doi: 10.1016/j.jep.2004.12.013.
Plant polyphenols from the aqueous extracts of Pentace burmanica, Pithecellobium dulce, Areca catechu and Quercus infectoria were tested for their inhibitory activities against Naja kaouthia (NK) venom by in vitro neutralization method. The first three extracts could completely inhibit the lethality of the venom at 4 LD50 concentration and the venom necrotizing activity at the minimum necrotizing dose while also inhibited up to 90% of the acetylcholinesterase activity of NK venom at much lower tannin concentrations than that of Quercus infectoria. The ED50 of plant tannins in inhibiting NK venom activities varied according to condensed tannins and their content in the extracts. Molecular docking of the complexes between alpha-cobratoxin and either hydrolysable or condensed tannins at their lowest energetic conformations were proposed. The anti-venom activities of these plant polyphenols by selectively blocking the nicotinic acetylcholine receptor and non-selectively by precipitation of the venom proteins were suggested.
采用体外中和法,对来自缅甸五桠果、甜荚相思、槟榔和没食子栎水提取物中的植物多酚进行了针对眼镜王蛇(NK)毒液抑制活性的测试。前三种提取物在4倍半数致死剂量(LD50)浓度下可完全抑制毒液的致死性,并在最低坏死剂量下抑制毒液的坏死活性,同时在比没食子栎低得多的单宁浓度下,也能抑制高达90%的眼镜王蛇毒液乙酰胆碱酯酶活性。植物单宁抑制眼镜王蛇毒液活性的半数有效剂量(ED50)因缩合单宁及其在提取物中的含量而异。提出了α - 眼镜蛇毒素与可水解或缩合单宁在其最低能量构象下形成的复合物的分子对接。这些植物多酚的抗蛇毒活性被认为是通过选择性阻断烟碱型乙酰胆碱受体以及通过沉淀毒液蛋白的非选择性方式实现的。