摘要
中华帽柱木是一种具有麻醉作用的热带植物。在啮齿动物模型中研究了其粗提物、生物活性化合物和结构修饰衍生物的抗接种作用。本研究旨在总结M. speciosa的镇痛作用及其衍生物的证据,并探讨它们是否可以提供一种替代吗啡疼痛药物。结果表明,M. speciosa和它的生物碱提取物对啮齿类动物的伤害性反应有明显的抑制作用。麦草碱和7-羟基麦草碱的抗接种效果优于粗提物。结构修饰的7-羟色胺衍生物,如MGM-9、MGM-15、MGM-16,与吗啡相比,具有更好的镇痛作用。M. speciosa属植物及其衍生物主要作用于阿片受体,但各亚型之间的受体亚型特异性不同。M. speciosa及其衍生物的耐受性和不良反应与吗啡相似,MGM-9对卡伯阿片受体的亲和力可能限制药物依赖的作用。综上所述,M. speciosa衍生物可以为吗啡提供控制慢性疼痛的替代物。丝裂素和7-羟基丝裂平的结构修饰可以产生效力更高、副作用较小的化合物,但需要进行人体临床试验来验证这些化合物在临床中的应用。
关键词: 镇痛,酮,吗啡,麻醉,痛觉,阿片类,疼痛。
Current Drug Targets
Title:A Review on the Antinociceptive Effects of Mitragyna speciosa and Its Derivatives on Animal Model
Volume: 19 Issue: 12
关键词: 镇痛,酮,吗啡,麻醉,痛觉,阿片类,疼痛。
摘要: Mitragyna speciosa is a tropical plant with narcotic effects. The antinociceptive effects of its crude extracts, bioactive compounds and structurally modified derivatives have been examined in rodent models. This review aims to summarize the evidence on the antinociceptive effects of M. speciosa and its derivatives and explore whether they can offer an alternative to morphine in pain management. Methanolic and alkaloid extracts of M. speciosa were shown to attenuate the nociceptive response in rodents. Mitragynine and 7-hydroxymitragynine offered better antinociceptive effects than crude extracts. Structurally modified derivatives of 7-hydroxymitragynine, such as MGM-9, MGM- 15, MGM-16, demonstrated superior antinociceptive effects compared to morphine. M. speciosa and its derivatives mainly act on the opioid receptor, but receptor subtypes specificity differs between each compound. The tolerance and adverse side effects of M. speciosa and its derivatives are similar with morphine. The affinity of MGM-9 on kappa-opioid receptor could potentially limit the effects of drug dependence. In conclusion, M speciosa derivatives can offer alternatives to morphine in controlling chronic pain. Structural modification of mitragynine and 7-hydroxymitragynine can generate compounds with higher potency and lesser side-effects. Human clinical trials are required to validate the use of these compounds in clinical setting.
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Cite this article as:
A Review on the Antinociceptive Effects of Mitragyna speciosa and Its Derivatives on Animal Model, Current Drug Targets 2018; 19 (12) . https://dx.doi.org/10.2174/1389450118666170925154025
DOI https://dx.doi.org/10.2174/1389450118666170925154025 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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