Abstract
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.