来自自然界的靶向 G 蛋白偶联大麻素受体的小分子:药物发现和开发的潜在线索。

Q4 Engineering International Journal of Advanced Mechatronic Systems Pub Date : 2015-01-01 Epub Date: 2015-11-17 DOI:10.1155/2015/238482
Charu Sharma, Bassem Sadek, Sameer N Goyal, Satyesh Sinha, Mohammad Amjad Kamal, Shreesh Ojha
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引用次数: 0

摘要

大麻素分子提取自大麻植物,作用于 1 型和 2 型大麻素受体(CB1 和 CB2),这两种受体已被视为药物发现和开发的潜在治疗靶点。目前,有许多基于大麻素的合成药物被用于临床实践,如常用的纳比隆、屈大麻酚和Δ(9)-四氢大麻酚,它们通过 CB1/CB2 受体发挥作用。然而,众所周知,这些基于合成的大麻衍生化合物会对精神产生不良影响,并被用于滥用药物。这促使我们寻找一种对精神疾病不良影响最小的安全替代药物。近年来,人们从大麻以外的植物中分离出了许多植物大麻素。一些研究表明,这些植物大麻素对大麻素受体具有亲和力、效力、选择性和功效,并能抑制内源性大麻素代谢酶,从而降低内源性大麻素系统的亢奋程度。此外,与人工合成的大麻素相比,这些天然提取的分子所产生的不良影响最小。因此,以植物为基础的大麻素分子被证明是前景广阔的新兴治疗替代品。本综述概述了调节大麻素受体的配体和植物的治疗潜力,制药业可能会对这些配体和植物感兴趣,以寻找更安全的新药,开发未来的治疗方法。
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Small Molecules from Nature Targeting G-Protein Coupled Cannabinoid Receptors: Potential Leads for Drug Discovery and Development.

The cannabinoid molecules are derived from Cannabis sativa plant which acts on the cannabinoid receptors types 1 and 2 (CB1 and CB2) which have been explored as potential therapeutic targets for drug discovery and development. Currently, there are numerous cannabinoid based synthetic drugs used in clinical practice like the popular ones such as nabilone, dronabinol, and Δ(9)-tetrahydrocannabinol mediates its action through CB1/CB2 receptors. However, these synthetic based Cannabis derived compounds are known to exert adverse psychiatric effect and have also been exploited for drug abuse. This encourages us to find out an alternative and safe drug with the least psychiatric adverse effects. In recent years, many phytocannabinoids have been isolated from plants other than Cannabis. Several studies have shown that these phytocannabinoids show affinity, potency, selectivity, and efficacy towards cannabinoid receptors and inhibit endocannabinoid metabolizing enzymes, thus reducing hyperactivity of endocannabinoid systems. Also, these naturally derived molecules possess the least adverse effects opposed to the synthetically derived cannabinoids. Therefore, the plant based cannabinoid molecules proved to be promising and emerging therapeutic alternative. The present review provides an overview of therapeutic potential of ligands and plants modulating cannabinoid receptors that may be of interest to pharmaceutical industry in search of new and safer drug discovery and development for future therapeutics.

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来源期刊
International Journal of Advanced Mechatronic Systems
International Journal of Advanced Mechatronic Systems Engineering-Mechanical Engineering
CiteScore
1.20
自引率
0.00%
发文量
5
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