Department of Histopathology, Postgraduate Institute of Medical Education and Research, Chandigarh 160 012, Punjab, India.
Department of Chemistry, Career Point University, Tikker-Kharwarian, Hamirpur 176 041, Himachal Pradesh, India.
Crit Rev Oncol Hematol. 2018 Aug;128:70-81. doi: 10.1016/j.critrevonc.2018.05.019. Epub 2018 Jun 5.
Despite the advancement in the well-equipped and sophisticated laboratories and facilities, cancer remains to be a major cause of death worldwide. Consequently, further investigation of novel strategies need to be evolved. Since the last few decades, the utilization of phytochemicals is emerging against several human cancers, including lung, breast, colon carcinoma, lymphoma, and other hematological malignancies. Terpenoids are a category of therapeutically active phytochemicals that have been utilized against cancer, cardiovascular and neurodegenerative disorders. Particularly, celastrol, a pentacyclic terpenoid, is well-studied for its variety of pharmacological properties. It is well documented that celastrol can modulate a variety of signaling pathways. Celastrol's anti-proliferative role has been found to be associated with its pro-apoptotic (via protein kinase B), anti-angiogenic (via vascular endothelial growth factor and vascular endothelial growth factor receptor), anti-metastatic (via matrix metalloproteinases), and anti-inflammatory (via cytokines and chemokines) activities. This review describes various molecular mechanisms of celastrol for understanding the biology of cancer initiation, progression as well as designing efficacious therapeutic strategies.
尽管配备了精良的实验室和设施，但癌症仍然是全球主要的死亡原因。因此，需要进一步研究新的策略。在过去的几十年中，植物化学物质的利用针对多种人类癌症，包括肺癌、乳腺癌、结肠癌、淋巴瘤和其他血液系统恶性肿瘤，已经取得了进展。三萜类化合物是一类具有治疗活性的植物化学物质，已被用于治疗癌症、心血管疾病和神经退行性疾病。特别是，具有多种药理学特性的雷公藤红素是一种五环三萜类化合物，已被广泛研究。有充分的证据表明，雷公藤红素可以调节多种信号通路。已发现雷公藤红素的抗增殖作用与其促凋亡（通过蛋白激酶 B）、抗血管生成（通过血管内皮生长因子和血管内皮生长因子受体）、抗转移（通过基质金属蛋白酶）和抗炎（通过细胞因子和趋化因子）活性有关。本综述描述了雷公藤红素的各种分子机制，以了解癌症发生、进展的生物学以及设计有效的治疗策略。
