关键词: general anesthetic lead compound local anesthetic pharmacological mechanism phytochemical plant origin

Mesh : Anesthetics / chemistry therapeutic use Anesthetics, Local / classification therapeutic use Cocaine / therapeutic use Eugenol / chemistry therapeutic use Humans Phytochemicals / classification therapeutic use Syzygium / chemistry Thymol / chemistry therapeutic use Thymus Plant / chemistry

来  源:   DOI:10.3390/molecules22081369   PDF(Pubmed)

Abstract:
The majority of currently used anesthetic agents are derived from or associated with natural products, especially plants, as evidenced by cocaine that was isolated from coca (Erythroxylum coca, Erythroxylaceae) and became a prototype of modern local anesthetics and by thymol and eugenol contained in thyme (Thymus vulgaris, Lamiaceae) and clove (Syzygium aromaticum, Myrtaceae), respectively, both of which are structurally and mechanistically similar to intravenous phenolic anesthetics. This paper reviews different classes of phytochemicals with the anesthetic activity and their characteristic molecular structures that could be lead compounds for anesthetics and anesthesia-related drugs. Phytochemicals in research papers published between 1996 and 2016 were retrieved from the point of view of well-known modes of anesthetic action, that is, the mechanistic interactions with Na⁺ channels, γ-aminobutyric acid type A receptors, N-methyl-d-aspartate receptors and lipid membranes. The searched phytochemicals include terpenoids, alkaloids and flavonoids because they have been frequently reported to possess local anesthetic, general anesthetic, antinociceptive, analgesic or sedative property. Clinical applicability of phytochemicals to local and general anesthesia is discussed by referring to animal in vivo experiments and human pre-clinical trials. This review will give structural suggestions for novel anesthetic agents of plant origin.
摘要:
目前使用的大多数麻醉剂来自天然产物或与天然产物相关,尤其是植物,从古柯中分离出的可卡因(红藻,红藻科),并成为现代局部麻醉药的原型,并通过百里香中含有的百里酚和丁香酚(Thymusvulgaris,唇形科)和丁香(Syzygiumaromaticum,桃金娘科),分别,两者在结构和机制上都与静脉注射酚类麻醉药相似。本文综述了具有麻醉活性的不同类别的植物化学物质及其特征分子结构,这些分子结构可能是麻醉药和麻醉相关药物的先导化合物。1996年至2016年发表的研究论文中的植物化学物质是从众所周知的麻醉作用模式的角度进行检索的。也就是说,与Na+通道的机械相互作用,γ-氨基丁酸A型受体,N-甲基-d-天冬氨酸受体和脂质膜。搜索到的植物化学物质包括萜类化合物,生物碱和类黄酮,因为它们经常被报道具有局部麻醉剂,全身麻醉,抗伤害性,镇痛或镇静性质。通过参考动物体内实验和人体临床前试验,讨论了植物化学物质在局部和全身麻醉中的临床适用性。这篇综述将为植物来源的新型麻醉剂提供结构建议。
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