2. Academic Validation
  3. Novel Resveratrol-Based Aspirin Prodrugs: Synthesis, Metabolism, and Anticancer Activity

Novel Resveratrol-Based Aspirin Prodrugs: Synthesis, Metabolism, and Anticancer Activity

  • J Med Chem. 2015 Aug 27;58(16):6494-506. doi: 10.1021/acs.jmedchem.5b00536.
Yingdong Zhu 1,  Junsheng Fu 1 2,  Kelly L Shurlknight 1,  Dominique N Soroka 1,  Yuhui Hu 3,  Xiaoxin Chen 3,  Shengmin Sang 1
Affiliations

Affiliations

  • 1 Center for Excellence in Post-Harvest Technologies, North Carolina Agricultural and Technical State University , North Carolina Research Campus, 500 Laureate Way, Kannapolis, North Carolina 28081, United States.
  • 2 College of Life Sciences, Fujian Agriculture and Forestry University , No. 15 Shangxiadian Road, Cangshan District, Fuzhou, Fujian Province 350002, P. R. China.
  • 3 Cancer Research Program, Julius L. Chambers Biomedical/Biotechnology Research Institute, North Carolina Central University , 700 George Street, Durham, North Carolina 27707, United States.
PMID: 26204233 DOI: 10.1021/acs.jmedchem.5b00536
Abstract

Regular aspirin use has been convincingly shown to reduce the risk of colorectal Cancer. However, long-term use of aspirin leads to gastrotoxicity. Herein, we designed and synthesized a novel class of resveratrol-based aspirin prodrugs to simultaneously release aspirin and resveratrol to attenuate the side effects caused by aspirin. Prodrug RAH exerted enhanced Anticancer activities which are better than a physical mixture of aspirin and resveratrol as well as each individually. Metabolism of RAH in mice showed that the majority of RAH is decomposed to release resveratrol and aspirin or salicylic acid either in the intestine or after absorption. Mechanistic studies demonstrate RAH inhibits cell cycle arrest through downregulation of cyclins and induces Apoptosis by activation of Caspase-3 in Cancer cells. These findings highlighted the improved Anticancer properties of resveratrol-based aspirin prodrugs. RAH may represent novel and safe alternatives of aspirin for the purpose of daily use in the future.

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