Jesridonin in combination with paclitaxel demonstrates synergistic anti-tumor activity in human esophageal carcinoma cells.

Bioorg Med Chem Lett

Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, Collaborative Innovative Center of New Drug Research and Safety Evaluation, Key Laboratory of Henan Province for Drug Quality and Evaluation, Zhengzhou University School of Pharmaceutical Sciences, 100 Kexue Avenue, Zhengzhou, Henan 450001, China. Electronic address:

Published: May 2017

The novel compound jesridonin, has extensive anti-tumor activity. In this study, we aim to investigate the cytotoxic effects of jesridonin in combination with paclitaxel. Our results showed that jesridonin in combination with paclitaxel had synergistic cytotoxic effects on human esophageal carcinoma both in vitro and in vivo. Hoechst 33258 staining and the Annexin-V FITC assay demonstrated that paclitaxel synergized with jesridonin in a stronger induction of apoptosis than treatment with paclitaxel or jesridonin alone. Western blotting results revealed that the synergistic apoptosis-induction effects of paclitaxel and jesridonin were mediated by the mitochondrial pathway. This may provide a novel strategy to overcome drug resistance for esophageal cancer therapy.

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http://dx.doi.org/10.1016/j.bmcl.2017.02.008DOI Listing

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