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2,4-Dipropylphloroglucinol inhibits the growth of human lung and colorectal cancer cells through induction of apoptosis

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Abstract

Scientists are finding the most effective chemotherapeutic agents for the treatment of cancer. In the present study, we evaluated the anticancer mechanism of DPPG, a derivative of DAPG (2,4-diacetylphloroglucinol), for the first time. DPPG and DAPG inhibited 83 and 59% of human colorectal cancer HCT116 cell growth at 40.0 µg/ml, and 74 and 57% of human lung cancer A549 cell growth at 10.0 µg/ml concentrations respectively. Furthermore, DPPG and DAPG inhibited 97 and 73% colony formation of the HCT116 cells at 20.0 µg/ml concentration. DPPG and DAPG induced apoptosis in the HCT116 and A549 cells that was confirmed by Hoechst 33342 and FITC-annexin V staining. This result also revealed that ROS generated in both the HCT116 and A549 cells after treatment with DPPG. However, no ROS production was observed in HCT116 and A549 cells after treatment with DAPG. Both DAPG and DPPG significantly increased the CASP3 protein expression that was detected by staining the cells with the super-view 488-CASP3 substrate. Expression of WNT1 gene was eliminated in DPPG and DAPG treated HCT116. Expression of MAPK1 gene was entirely abolished in DPPG treated cells, whereas a significant decrease was observed for DAPG. An intense band of CASP8 gene product was observed agarose gel for DPPG treated HCT116 cells than DAPG. Molecular docking simulation showed the high binding affinities (≥ 6.5 kcal/mol) of DPPG and DAPG with target proteins WNT1, MAPK1, CASP8, and CASP3 in HCT116 cells. This manuscript demonstrated that DAPG and DPPG inhibited lung and colorectal cancer cells by inducing apoptosis.

Graphical abstract

DAPG and DPPG inhibited A549 and HCT116 cells growth by inducing apoptosis

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Data sharing not applicable to this article as no data sets were generated or analyzed during the current study.

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The authors have not disclosed any funding.

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Authors and Affiliations

  1. Department of Biochemistry and Molecular Biology, Faculty of Science, University of Rajshahi, Rajshahi, 6205, Bangladesh

    Syed Rashel Kabir

  2. Institute of Biotechnology and Genetic Engineering (IBGE), Bangabandhu Sheikh Mujibur Rahman Agricultural University, Gazipur, 1706, Bangladesh

    Tofazzal Islam

  3. Bioinformatics Lab (Dry), Department of Statistics, Faculty of Science, University of Rajshahi, Rajshahi, 6205, Bangladesh

    Md. Nurul Haque Mollah

Authors
  1. Syed Rashel Kabir
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  2. Tofazzal Islam
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  3. Md. Nurul Haque Mollah
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Contributions

TI is responsible for DAPG and DPPG isolation. MNHM is responsible for bioinformatics related works. SRK did all of the anticancer-related works, manuscript written, edited and funded to the cancer-related research works.

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Correspondence to Syed Rashel Kabir.

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Kabir, S.R., Islam, T. & Mollah, M.N.H. 2,4-Dipropylphloroglucinol inhibits the growth of human lung and colorectal cancer cells through induction of apoptosis. Med Oncol 40, 129 (2023). https://doi.org/10.1007/s12032-023-01986-y

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  • DOI: https://doi.org/10.1007/s12032-023-01986-y

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