Biomedicine & Pharmacotherapy (Aug 2023)

Celastrol functions as an emerging manager of lipid metabolism: Mechanism and therapeutic potential

  • Jia Gu,
  • Ya-Ning Shi,
  • Neng Zhu,
  • Hong-Fang Li,
  • Chan-Juan Zhang,
  • Li Qin

Journal volume & issue
Vol. 164
p. 114981

Abstract

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Lipid metabolism disorders are pivotal in the development of various lipid-related diseases, such as obesity, atherosclerosis, non-alcoholic fatty liver disease, type 2 diabetes, and cancer. Celastrol, a bioactive compound extracted from the Chinese herb Tripterygium wilfordii Hook F, has recently demonstrated potent lipid-regulating abilities and promising therapeutic effects for lipid-related diseases. There is substantial evidence indicating that celastrol can ameliorate lipid metabolism disorders by regulating lipid profiles and related metabolic processes, including lipid synthesis, catabolism, absorption, transport, and peroxidation. Even wild-type mice show augmented lipid metabolism after treatment with celastrol. This review aims to provide an overview of recent advancements in the lipid-regulating properties of celastrol, as well as to elucidate its underlying molecular mechanisms. Besides, potential strategies for targeted drug delivery and combination therapy are proposed to enhance the lipid-regulating effects of celastrol and avoid the limitations of its clinical application.

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