Zhao Junqi, Zhang Fangling, Xiao Xiaolin, Wu Zhao, Hu Qichao, Jiang Yinxiao, Zhang Wenwen, Wei Shizhang, Ma Xiao, Zhang Xiaomei
State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China.
Hospital of Chengdu University of Traditional Chinese Medicine, School of Clinical Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, China.
Front Pharmacol. 2021 Nov 23;12:715359. doi: 10.3389/fphar.2021.715359. eCollection 2021.
(Lévl.) Hutch (THH) is believed to play an important role in health care and disease treatment according to traditional Chinese medicine. Moreover, it is also the representative of medicine with both significant efficacy and potential toxicity. This characteristic causes THH hard for embracing and fearing. In order to verify its prospect for clinic, a wide variety of studies were carried out in the most recent years. However, there has not been any review about THH yet. Therefore, this review summarized its characteristic of components, pharmacological effect, pharmacokinetics and toxicity to comprehensively shed light on the potential clinical application. More than 120 secondary metabolites including terpenoids, alkaloids, glycosides, sugars, organic acids, oleanolic acid, polysaccharides and other components were found in THH based on phytochemical research. All these components might be the pharmacological bases for immunosuppression, anti-inflammatory and anti-tumour effect. In addition, recent studies found that THH and its bioactive compounds also demonstrated remarkable effect on obesity, insulin resistance, fertility and infection of virus. The main mechanism seemed to be closely related to regulation the balance of immune, inflammation, apoptosis and so on in various disease. Furthermore, the study of pharmacokinetics revealed quick elimination of the main component triptolide. The feature of celastrol was also investigated by several models. Finally, the side effect of THH was thought to be the key for its limitation in clinical application. A series of reports indicated that multiple organs or systems including liver, kidney and genital system were involved in the toxicity. Its potential serious problem in liver was paid specific attention in recent years. In summary, considering the significant effect and potential toxicity of THH as well as its components, the combined medication to inhibit the toxicity, maintain effect might be a promising method for clinical conversion. Modern advanced technology such as structure optimization might be another way to reach the efficacy and safety. Thus, THH is still a crucial plant which remains for further investigation.
雷公藤(Lévl.)Hutch(THH)在中医药中被认为在医疗保健和疾病治疗中发挥着重要作用。此外,它也是功效显著但具有潜在毒性的药物的代表。这一特性使得雷公藤既让人难以接受又令人畏惧。为了验证其临床应用前景,近年来开展了各种各样的研究。然而,目前尚未有关于雷公藤的综述。因此,本综述总结了其成分特征、药理作用、药代动力学和毒性,以全面阐明其潜在的临床应用。基于植物化学研究,在雷公藤中发现了120多种次生代谢产物,包括萜类、生物碱、糖苷、糖类、有机酸、齐墩果酸、多糖等成分。所有这些成分可能是其免疫抑制、抗炎和抗肿瘤作用的药理基础。此外,最近的研究发现,雷公藤及其生物活性化合物对肥胖、胰岛素抵抗、生育能力和病毒感染也有显著作用。其主要机制似乎与调节各种疾病中免疫、炎症、凋亡等的平衡密切相关。此外,药代动力学研究表明,主要成分雷公藤甲素消除迅速。还通过多种模型研究了雷公藤红素的特性。最后,雷公藤的副作用被认为是其临床应用受限的关键。一系列报告表明,包括肝脏、肾脏和生殖系统在内的多个器官或系统都参与了其毒性作用。近年来,其在肝脏方面潜在的严重问题受到了特别关注。综上所述,考虑到雷公藤及其成分的显著作用和潜在毒性,可以联合用药以抑制毒性、维持疗效,这可能是临床转化的一种有前景的方法。结构优化等现代先进技术可能是实现疗效和安全性的另一种途径。因此,雷公藤仍是一种有待进一步研究的关键植物。