Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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Licochalcone H Induces Cell Cycle Arrest and Apoptosis in Human Skin Cancer Cells by Modulating JAK2/STAT3 Signaling

  • Park, Kyung-Ho (Department of Dental Pharmacology, School of Dentistry, Jeonbuk National University) ;
  • Joo, Sang Hoon (College of Pharmacy, Daegu Catholic University) ;
  • Seo, Ji-Hye (Department of Dental Pharmacology, School of Dentistry, Jeonbuk National University) ;
  • Kim, Jumi (Department of Dental Pharmacology, School of Dentistry, Jeonbuk National University) ;
  • Yoon, Goo (Department of Pharmacy, College of Pharmacy, Mokpo National University) ;
  • Jeon, Young-Joo (Stem Cell Convergence Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB)) ;
  • Lee, Mee-Hyun (College of Korean Medicine, Dongshin University) ;
  • Chae, Jung-Il (Department of Dental Pharmacology, School of Dentistry, Jeonbuk National University) ;
  • Kim, Woo-Keun (Biosystem Research Group, Department of Predictive Toxicology, Korea Institute of Toxicology) ;
  • Shim, Jung-Hyun (Department of Pharmacy, College of Pharmacy, Mokpo National University)
  • Received : 2021.09.22
  • Accepted : 2021.09.28
  • Published : 2022.01.01
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Abstract

Licochalcone H (LCH) is a phenolic compound synthetically derived from licochalcone C (LCC) that exerts anticancer activity. In this study, we investigated the anticancer activity of LCH in human skin cancer A375 and A431 cells. The 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) cell viability assay was used to evaluate the antiproliferative activity of LCH. Cell cycle distribution and the induction of apoptosis were analyzed by flow cytometry. Western blotting assays were performed to detect the levels of proteins involved in cell cycle progression, apoptosis, and the JAK2/STAT3 signaling pathway. LCH inhibited the growth of cells in dose- and time-dependent manners. The annexin V/propidium iodide double staining assay revealed that LCH induced apoptosis, and the LCH-induced apoptosis was accompanied by cell cycle arrest in the G1 phase. Western blot analysis showed that the phosphorylation of JAK2 and STAT3 was decreased by treatment with LCH. The inhibition of the JAK2/STAT3 signaling pathway by pharmacological inhibitors against JAK2/STAT3 (cryptotanshinone (CTS) and S3I-201) simulated the antiproliferative effect of LCH suggesting that LCH induced apoptosis by modulating JAK2/STAT3 signaling.

Keywords

Acknowledgement

We greatly appreciated using the Convergence Research Laboratory (established by the MNU Innovation Support Project in 2019) to conduct this research. This research was funded by the Basic Science Research Program of National Research Foundation Korea, grant number 2019R1A2C1005899. This work was carried out with the support of Cooperative Core Technology Development Project for Environmental Diseases Prevention and Management (2021003310003), funded by the Korea Ministry of Environment (MOE).

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