Abstract

2′,4′-Dihydroxy-6′-methoxy-3′,5′-dimethylchalcone (DMC), a natural product derived from Syzygium nervosum A. Cunn. ex DC., was investigated for its inhibitory activities against various cancer cell lines. In this work, we investigated the effects of DMC and available anticervical cancer drugs (5-fluorouracil, cisplatin, and doxorubicin) on three human cervical cancer cell lines (C-33A, HeLa, and SiHa). DMC displayed antiproliferative cervical cancer activity in C-33A, HeLa, and SiHa cells, with IC50 values of 15.76 ± 1.49, 10.05 ± 0.22, and 18.31 ± 3.10 µM, respectively. DMC presented higher antiproliferative cancer activity in HeLa cells; therefore, we further investigated DMC-induced apoptosis in this cell line, including DNA damage, cell cycle arrest, and apoptosis assays. As a potential anticancer agent, DMC treatment increased DNA damage in cancer cells, observed through fluorescence inverted microscopy and a comet assay. The cell cycle assay showed an increased number of cells in the G0/G1 phase following DMC treatment. Furthermore, DMC treatment-induced apoptosis cell death was approximately three- to four-fold higher compared to the untreated group. Here, DMC represented a compound-induced apoptosis for cell death in the HeLa cervical cancer cell line. Our findings suggest that DMC, a phytochemical agent, is a potential candidate for antiproliferative cervical cancer drug development.

Highlights

  • The global incidence of cancer is continually increasing, with an estimated 18.1 million new patients diagnosed with cancer in 2018 [1,2]

  • DMC is a chalcone derivative isolated from the seeds of S. nervosum

  • We investigated the biological activities of DMC from S. nervosum

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Summary

Introduction

The global incidence of cancer is continually increasing, with an estimated 18.1 million new patients diagnosed with cancer in 2018 [1,2]. The seed’s methanolic extract was found to inhibit aflatoxin B1 and MeIQ (2-amino-3,4-dimethylimidazo-[4,5-f ]quinolone)-induced mutagenesis in a dose-dependent manner in a Salmonella mutation assay. This effect might occur through the inhibitory effects on carcinogen-bioactivated enzymes rather than a direct action on mutagens [10,11]. The main chemical compound isolated from the buds and seeds of S. nervosum is 2 ,4 -dihydroxy-6 -methoxy-3 ,5 -dimethylchalcone (DMC), which has been reported for biological activities, including anti-inflammatory, antiviral, antidiabetic, and anticancer [12,13,14,15,16]

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