Li Mengzhen, Xie Faren, Wang Lu, Zhu Guoxue, Qi Lian-Wen, Jiang Shujun
Clinical Metabolomics Center, China Pharmaceutical University, Nanjing, China.
Nanjing Hospital of Chinese Medicine Affiliated to Nanjing University of Chinese Medicine, Nanjing, China.
Front Pharmacol. 2022 Apr 4;13:857956. doi: 10.3389/fphar.2022.857956. eCollection 2022.
The liver plays an important role in glucose and lipid homeostasis, drug metabolism, and bile synthesis. Metabolic disorder and inflammation synergistically contribute to the pathogenesis of numerous liver diseases, such as metabolic-associated fatty liver disease (MAFLD), liver injury, and liver cancer. Celastrol, a triterpene derived from Hook.f., has been extensively studied in metabolic and inflammatory diseases during the last several decades. Here we comprehensively review the pharmacological activities and the underlying mechanisms of celastrol in the prevention and treatment of liver diseases including MAFLD, liver injury, and liver cancer. In addition, we also discuss the importance of novel methodologies and perspectives for the drug development of celastrol. Although celastrol has been claimed as a promising agent against several metabolic diseases, both preclinical and clinical studies are highly required to accelerate the clinical transformation of celastrol in treating different liver illness. It is foreseeable that celastrol-derived therapeutics is evolving in the field of liver ailments.
肝脏在葡萄糖和脂质稳态、药物代谢及胆汁合成中发挥着重要作用。代谢紊乱和炎症协同作用，促成了众多肝脏疾病的发病机制，如代谢相关脂肪性肝病（MAFLD）、肝损伤和肝癌。雷公藤红素是一种从南蛇藤属植物中提取的三萜类化合物，在过去几十年中已在代谢和炎症性疾病方面得到广泛研究。在此，我们全面综述雷公藤红素在预防和治疗包括MAFLD、肝损伤和肝癌在内的肝脏疾病中的药理活性及潜在机制。此外，我们还讨论了雷公藤红素药物开发新方法和新观点的重要性。尽管雷公藤红素已被认为是一种针对多种代谢性疾病的有前景的药物，但仍迫切需要临床前和临床研究来加速雷公藤红素在治疗不同肝脏疾病方面的临床转化。可以预见，雷公藤红素衍生疗法正在肝脏疾病领域不断发展。
