Current topics in medicinal chemistry · 2025
Traditional Design and Modification of "Celastrol" Nano-Delivery Systems for Cancer: A Review.
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Law Siu Kan, Ng Sze Wing, Wang Yanping, Wu Xiao Xiao
Аннотация
INTRODUCTION: Cancer is a prevalent public health issue and a significant global problem. Patients receive different treatments, including Western Medicine (WM) and Traditional Chinese Medicine (TCM). This review article aims to discuss a Traditional Chinese Medicine (TCM), "Celastrol," its traditional design, modification, and nano-drug delivery systems for the treatment of cancer.
METHODS: Nine electronic databases, such as WanFang Data, PubMed, ScienceDirect, Scopus, Web of Science, SpringerLink, SciFinder, and China National Knowledge Infrastructure (CNKI), were used to find relevant information from the past twenty years, with searched keywords including "celastrol," "cancer," and "nano-drug delivery system," etc., without language restrictions.
RESULTS: Celastrol is a therapeutic agent with anticancer properties against liver and breast cancers, ovarian cancer, multiple myeloma, and glioma. PI3K/Akt/mTOR, Bcl-2/Bax-caspases, EGFR, ROS/JNK, NF-κB, STAT3, JNK/Nrf2/HO-1, VEGF, AR/miR-101, HSF1-LKB1-AMPKα-YAP, Wnt/β-catenin, and CIP2A/c-MYC signaling pathways are the possible mechanisms by which celastrol acts against cancer.
CONCLUSION: A naturally occurring bioactive substance, "celastrol," is extracted from the root of Tripterygium wilfordii Hook F. Its effectiveness can be enhanced with the support of nanotechnology to overcome its limitations in cancer treatment. However, the toxicity, dosage, and safety assessments of celastrol and nanocelastrol in cancer applications must be further investigated.
METHODS: Nine electronic databases, such as WanFang Data, PubMed, ScienceDirect, Scopus, Web of Science, SpringerLink, SciFinder, and China National Knowledge Infrastructure (CNKI), were used to find relevant information from the past twenty years, with searched keywords including "celastrol," "cancer," and "nano-drug delivery system," etc., without language restrictions.
RESULTS: Celastrol is a therapeutic agent with anticancer properties against liver and breast cancers, ovarian cancer, multiple myeloma, and glioma. PI3K/Akt/mTOR, Bcl-2/Bax-caspases, EGFR, ROS/JNK, NF-κB, STAT3, JNK/Nrf2/HO-1, VEGF, AR/miR-101, HSF1-LKB1-AMPKα-YAP, Wnt/β-catenin, and CIP2A/c-MYC signaling pathways are the possible mechanisms by which celastrol acts against cancer.
CONCLUSION: A naturally occurring bioactive substance, "celastrol," is extracted from the root of Tripterygium wilfordii Hook F. Its effectiveness can be enhanced with the support of nanotechnology to overcome its limitations in cancer treatment. However, the toxicity, dosage, and safety assessments of celastrol and nanocelastrol in cancer applications must be further investigated.