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百里香的抗惊厥和抗质粒共轭潜力的化学研究:体内小鼠和体外研究。

The anticonvulsant and anti-plasmid conjugation potential of Thymus vulgaris chemistry: An in vivo murine and in vitro study.

机构信息

Department of Pharmacognosy with Medicinal Plant Unit, Medical University of Lublin, Chodzki 1, PL 20-093, Lublin, Poland.

Department of Pharmacognosy with Medicinal Plant Unit, Medical University of Lublin, Chodzki 1, PL 20-093, Lublin, Poland.

出版信息

Food Chem Toxicol. 2018 Oct;120:472-478. doi: 10.1016/j.fct.2018.07.045. Epub 2018 Jul 25.

Abstract

The high-performance counter-current chromatography was used for the efficient purification of single constituents from Thymus vulgaris essential oil. Mixtures of n-heptane, ethyl acetate, methanol, and water (5:2:5:2 and 4:1:4:1 v/v), allowed purification of eugenol, 1-octen-3- ol, borneol, thymol, terpinen-4-ol, and camphor, while n-hexane, acetonitrile, and tert-butyl methyl ether (1:1:0.1 v/v) yielded carvacrol, borneol, linalyl acetate, caryophyllene oxide, p-cymene, and eucalyptol. The anticonvulsant activities were evaluated in the maximal electroshock-induced seizure test in mice model (systemic i. p. administration). The oil exerted protection against MES-induced seizures when administered 15 and 30 min before the tests (50 and 62.5%, respectively). Among the isolates, borneol, thymol, and eugenol exerted the strongest protection against seizures. Moreover, linalool had the ability to reduce the transfer of the pKM101 plasmid by 84%, what has the potential to reduce virulence and resistance spread in E. coli. No acute toxic effects towards the CNS were noticed either for the essential oil or for single compounds, in the chimney and grip-strength tests. The preclinical screening of Thymus vulgaris EO, as well as isolated terpenoids, provides evidence that the EO has partial protective activity against seizures and HPCCC technique is suitable for its large scale isolation.

摘要

高效逆流色谱法用于从普通香芹精油中高效纯化单一成分。正庚烷、乙酸乙酯、甲醇和水(5:2:5:2 和 4:1:4:1 v/v)的混合物允许纯化丁香酚、1-辛烯-3-醇、龙脑、百里酚、萜品-4-醇和樟脑,而正己烷、乙腈和叔丁基甲基醚(1:1:0.1 v/v)则产生香芹酚、龙脑、乙酸薰衣草酯、石竹烯氧化物、对伞花烃和桉油醇。在小鼠模型(全身腹腔内给药)的最大电休克诱导的惊厥试验中评估了抗惊厥活性。该油在测试前 15 和 30 分钟(分别为 50%和 62.5%)给药时对 MES 诱导的惊厥具有保护作用。在分离物中,龙脑、百里酚和丁香酚对惊厥具有最强的保护作用。此外,芳樟醇有能力将 pKM101 质粒的转移减少 84%,这有可能降低大肠杆菌的毒力和耐药性传播。在烟囱和握力试验中,无论是对精油还是单一化合物,都没有发现对中枢神经系统有急性毒性作用。普通香芹精油和分离的萜类化合物的临床前筛选提供了证据,表明精油具有部分抗惊厥活性,并且 HPCCC 技术适合其大规模分离。

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