Engineering Research Center of Modern Preparation Technology of TCM of Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China.
J Ethnopharmacol. 2022 Nov 15;298:115581. doi: 10.1016/j.jep.2022.115581. Epub 2022 Aug 7.
Grayanoids are natural diterpenoids that are mostly found in the Ericaceae family, such as Rhododendron molle (Blume) G. Don (Relevant herb: nao yang hua), Rhododendron micranthum Turcz (also known as: zhao shan bai), which have traditionally been used to treat abdominal pain, cephalgia, and rheumatoid arthritis.
The review investigated advancements in notable anti-nociception, toxicity, and probable mechanisms of grayanoids. Meanwhile some binding sites of these compounds on voltage-gated sodium channels (VSGCs) were also analyzed and evaluated.
The substantial grayanoids literature published before 2022, in SCI Finder, PubMed, Science Direct, Springer, Scopus, Wiley Online Library, J-Stage, and other literature databases had been exhaustively consulted and thoroughly screened.
More than 50 compounds in grayanoids exhibited exceptionally significant anti-nociception (intraperitoneal injection, less than 1 mg/kg), and the alteration of several substituents that were closely associated to the change in activity were investigated. Multiple possible mechanisms of analgesic action and toxicity had been proposed, with VSGCs playing a key part in both. As a result, the binding locations of these compounds on VGSCs (mostly grayanotoxin I and III) had been summarized.
The considerable anti-nociception, toxicity, and probable mechanisms of grayanoids, as well as the investigation of the binding sites on VSGCs, were discussed in this review. Furthermore, the homology of toxicity and anti-nociception of these substances was considered, as well as the possibility of grayanoids being developed as analgesics.
格雷醇类是天然二萜类化合物，主要存在于杜鹃花科中，如密枝杜鹃（Rhododendron molle (Blume) G. Don（相关草药：脑阳花））、短梗杜鹃（Rhododendron micranthum Turcz（也称为：照山白）），传统上用于治疗腹痛、头痛和类风湿性关节炎。
本综述旨在探讨格雷醇类化合物在显著的抗伤害感受、毒性和可能的作用机制方面的研究进展。同时，还分析和评估了这些化合物在电压门控钠离子通道（VSGCs）上的一些结合位点。
全面检索了 2022 年前在 SCI Finder、PubMed、Science Direct、Springer、Scopus、Wiley Online Library、J-Stage 和其他文献数据库中发表的大量格雷醇类化合物文献，并进行了彻底筛选。
格雷醇类化合物中有 50 多种化合物表现出显著的抗伤害感受作用（腹腔注射，低于 1mg/kg），并研究了与活性变化密切相关的几个取代基的变化。提出了多种可能的镇痛作用和毒性机制，VSGCs 在其中都起着关键作用。因此，总结了这些化合物在 VSGCs 上的结合部位（主要是格雷醇毒素 I 和 III）。
本综述讨论了格雷醇类化合物的显著抗伤害感受作用、毒性和可能的作用机制，以及对 VSGCs 上结合部位的研究。此外，还考虑了这些物质的毒性和抗伤害感受的同源性，以及将格雷醇类化合物开发为镇痛药的可能性。
