State Key Laboratory for Quality Ensurance and Sustainable Use of Dao-di Herbs, Artemisinin Research Center, and Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.
College of Animal Science and Technology, Henan Agricultural University, Zhengzhou 450002, China.
Int J Biol Sci. 2024 Oct 7;20(14):5510-5530. doi: 10.7150/ijbs.99592. eCollection 2024.
Celastrol, a compound derived from traditional Chinese medicine, has therapeutic effects and has been used to treat inflammation-related diseases, cancer, cardiovascular diseases, and neurodegenerative diseases. However, current reviews lack a comprehensive and systematic summary of the anti-tumor mechanisms and molecular targets of celastrol. For this reason, this paper reviews the anticancer properties of celastrol and the molecular mechanisms underlying its anticancer effects. This paper primarily focuses on the mechanism of action of celastrol in terms of inhibition of cell proliferation and regulation of the cell cycle, regulation of apoptosis and autophagy, inhibition of cell invasion and metastasis, anti-inflammation, regulation of immunotherapy, and angiogenesis. More importantly, the target proteins of celastrol identified by chemical proteomics or other methods are highlighted, providing detailed targets with novel therapeutic potential for anti-tumor treatment. In addition, we describe the side effects and strategies to improve the bioavailability of celastrol. In summary, this paper analyzes celastrol, a natural compound with therapeutic effects and clear targets, aiming to draw more attention from the scientific and pharmacological communities and accelerating its clinical application for the benefit of cancer patients.
从传统中药中提取的化合物，具有治疗作用，已被用于治疗炎症相关疾病、癌症、心血管疾病和神经退行性疾病。然而，目前的综述缺乏对 celastrol 抗肿瘤机制和分子靶点的全面和系统总结。为此，本文综述了 celastrol 的抗癌特性及其抗癌作用的分子机制。本文主要关注 celastrol 在抑制细胞增殖和调节细胞周期、调节细胞凋亡和自噬、抑制细胞侵袭和转移、抗炎、调节免疫治疗和血管生成方面的作用机制。更重要的是，强调了通过化学蛋白质组学或其他方法鉴定的 celastrol 的靶蛋白，为抗肿瘤治疗提供了具有新颖治疗潜力的详细靶标。此外，我们还描述了 celastrol 的副作用和提高其生物利用度的策略。总之，本文分析了具有治疗作用和明确靶点的天然化合物 celastrol，旨在引起科学界和药理学界的更多关注，加速其临床应用，造福癌症患者。
