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Apoptosis-mediated antiproliferation of A549 lung cancer cells mediated by Eugenia aquea leaf compound 2',4'‑dihydroxy‑6'-methoxy‑3',5'‑dimethylchalcone and its molecular interaction with caspase receptor in molecular docking simulation

  • Authors:
    • Yuni Elsa Hadisaputri
    • Noni Cahyana
    • Muchtaridi Muchtaridi
    • Ronny Lesmana
    • Taofik Rusdiana
    • Anis Yohana Chaerunisa
    • Irna Sufiawati
    • Tina Rostinawati
    • Anas Subarnas
  • View Affiliations

  • Published online on: March 19, 2020     https://doi.org/10.3892/ol.2020.11466
  • Pages: 3551-3557
  • Copyright: © Hadisaputri et al. This is an open access article distributed under the terms of Creative Commons Attribution License.

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Abstract

In a previous study, 2',4'‑dihydroxy‑6'‑methoxy‑­3',5'‑dimethylchalcone (ChalcEA) isolated from the leaves of Eugenia aquea was reported to inhibit proliferation of the breast adenocarcinoma MCF7 cell line and to promote apoptosis via activation of poly(adenosine diphosphate‑ribose) polymerase protein. The present study aimed to evaluate the inhibitory effect of ChalcEA on the proliferation of A549 lung cancer cells using a 3‑(4,5‑dimethylthiazol‑2‑yl)‑5‑(3‑carboxylmethoxyphenyl)-2‑(4‑sulfophenyl)‑2H‑tetrazolium assay, and to examine the ability of ChalcEA to induce apoptosis through activation of the caspase cascade signaling pathway in a western blotting assay. The results revealed that ChalcEA inhibited proliferation of the A549 lung cancer cell lines in a time‑ and dose‑dependent manner with IC50 values of 25.36 and 19.60 µM for 24 and 48 h treatments, respectively. Western blot analysis indicated that ChalcEA exerted its anti‑proliferative effects by promoting apoptosis via the activation of caspase‑9 and caspase‑3. Based on in silico results, ChalcEA with the binding energy of ‑6.53 kcal/mol could compete better than 4‑methyl benzenesulfonamide (‑6.43 kcal/mol) as an inhibitor of caspase‑3 (PDB: 2XYG). ChalcEA has potential since it has three hydrophobic features. These results provided a basis for further study of ChalcEA as an active compound for anticancer therapeutics.

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May 2020
Volume 19 Issue 5

Print ISSN: 1792-1074
Online ISSN:1792-1082

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APA
Hadisaputri, Y., Cahyana, N., Muchtaridi, M., Lesmana, R., Rusdiana, T., Chaerunisa, A. ... Subarnas, A. (2020). Apoptosis-mediated antiproliferation of A549 lung cancer cells mediated by Eugenia aquea leaf compound 2',4'‑dihydroxy‑6'-methoxy‑3',5'‑dimethylchalcone and its molecular interaction with caspase receptor in molecular docking simulation. Oncology Letters, 19, 3551-3557. https://doi.org/10.3892/ol.2020.11466
MLA
Hadisaputri, Y., Cahyana, N., Muchtaridi, M., Lesmana, R., Rusdiana, T., Chaerunisa, A., Sufiawati, I., Rostinawati, T., Subarnas, A."Apoptosis-mediated antiproliferation of A549 lung cancer cells mediated by Eugenia aquea leaf compound 2',4'‑dihydroxy‑6'-methoxy‑3',5'‑dimethylchalcone and its molecular interaction with caspase receptor in molecular docking simulation". Oncology Letters 19.5 (2020): 3551-3557.
Chicago
Hadisaputri, Y., Cahyana, N., Muchtaridi, M., Lesmana, R., Rusdiana, T., Chaerunisa, A., Sufiawati, I., Rostinawati, T., Subarnas, A."Apoptosis-mediated antiproliferation of A549 lung cancer cells mediated by Eugenia aquea leaf compound 2',4'‑dihydroxy‑6'-methoxy‑3',5'‑dimethylchalcone and its molecular interaction with caspase receptor in molecular docking simulation". Oncology Letters 19, no. 5 (2020): 3551-3557. https://doi.org/10.3892/ol.2020.11466