Apoptosis induced in MCF-7 human breast cancer cells by 2′,4′-dihydroxy-6-methoxy-3,5-dimethylchalcone isolated from Eugenia aquea Burm f. leaves

Subarnas, Anas; Diantini, Ajeng; Abdulah, Rizky; Zuhrotun, Ade; Hadisaputri, Yuni Elsa; Puspitasari, Irma Melyani; Yamazaki, Chiho; Kuwano, Hiroyuki; Koyama, Hiroshi

doi:10.3892/ol.2015.2981

Cited by 30 publications

(26 citation statements)

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“…ChalcEA was obtained from the leaves of E. aquea. The isolation of the compound has been reported previously by Subarnas et al (10) and its structure was shown in Fig. 1.…”

Section: Methodsmentioning

confidence: 53%

“…Previously, the compound ChalcEA obtained from the leaves of E. aquea has been shown to have antiproliferation activity in MCF7 cells and to promote proapoptotic activity via PARP protein activation (10). However, the present study investigated the effects of ChalcEA on the growth of A549 lung cancer cells as lung cancer is known as a malignant lung tumor characterized by uncontrolled cell growth in tissues of the lung (14).…”

Section: Discussionmentioning

confidence: 92%

“…A number of compounds derived from medicinal plants have potential cytotoxicity against several types of cancer 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 cells in anticancer evaluation in vitro or in vivo (5)(6)(7). Plants consumed by primates are assumed to be a promising source of therapeutic agents for the management of human diseases and a series of investigations have been conducted and provided novel findings of their cytotoxicity against breast cancer cell lines (1,(8)(9)(10). Kaempferol-3-O-rhamnoside isolated from the leaves of Schima wallichii, a plant commonly consumed by primates, exhibits inhibitory activity against MCF7 breast cancer cell proliferation through the activation of the caspase cascade signaling pathway (8).…”

Section: Introductionmentioning

confidence: 99%

“…Subarnas et al (9) evaluated antiproliferative effects of 42 species of primate-consumed plants against MCF7 human breast cell lines using an MTT bioassay and revealed that some plant extracts have strong inhibitory activity against MCF7 cell proliferation. Furthermore, 2' ,4'-dihydroxy-6'-methoxy-3' ,5'-dimethylchalcone (ChalcEA), isolated from the leaves of Eugenia aquea (E. aquea), inhibits the proliferation of MCF7 cell lines and promotes apoptosis via the activation of poly(adenosine diphosphate-ribose) polymerase (PARP) protein (10). Additionally, a friedolanostane triterpenoid from Garcinia celebica leaves inhibits the growth of MCF7 cells through induction of apoptosis and downregulation of the oncogene Akt (1).…”

Section: Introductionmentioning

confidence: 99%

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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

et al. 2020

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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-carbo xylmethoxyphenyl)-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 IC 50 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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“…ChalcEA was obtained from the leaves of E. aquea. The isolation of the compound has been reported previously by Subarnas et al (10) and its structure was shown in Fig. 1.…”

Section: Methodsmentioning

confidence: 53%

Section: Discussionmentioning

confidence: 92%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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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

et al. 2020

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“…Vinblastine is one type of the alkaloid compound which has been isolated for anti-cancer drug development. [8][9][10][11] Flavonoids might also induce antiproliferative activity of C. pallida extract. Previous study showed that it might interferes with multiple mechanism, including signal transduction.…”

Section: Resultsmentioning

confidence: 99%

Anti-proliferative Activity of Crotalaria pallida Aiton on MCF-7 Breast Cancer Cells

Rumondor¹,

Moektiwardoyo²,

Barliana³

2017

PCPR

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Crotalaria pallida Aiton (C. pallida Aiton) is empirically used as dietary supplement to treat cancer by the people of North Sulawesi. However, its scientific pharmacology activity has not been explored yet. Therefore, this study was conducted to evaluate anti-proliferative activity of C. pallida Aiton on MCF-7 breast cancer cells. The extraction of leaves and seeds were performed using ethanol, ethyl acetate, n-hexane, and water. Phytochemical screening was then performed to identify secondary metabolites in this extract. Anti-proliferative activity was evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The results indicated that ethyl acetate fraction of C. pallida Aiton has the lowest IC 50 (29,67). In conclusion, ethyl acetate fraction of C. pallida Aiton is potential to be developed as anti cancer agent.

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Total Syntheses of 4′,6′‐Dimethoxy‐2'‐Hydroxy‐3′,5′‐Dimethylchalcone Derivatives

Lee

Park

2020

Bulletin Korean Chem Soc

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Chalcone derivatives afford several pharmacological activities. However, a general synthetic method for 2',4'‐dihydroxy‐6'‐methoxy‐3',5'‐dimethylchalcone (DMC) derivatives has not been reported thus far. To address this, the preparation of 4',6'‐dimethoxy‐2'‐hydroxy‐3',5'‐dimethylchalcone (MDMC) derivatives, modified compounds of DMC, in excellent overall yields is reported herein. These compounds have recently attracted growing attention due to their various pharmacological activities. Di‐O‐methyl‐dimethylphloroacetophenone, the key intermediate containing the B‐ring moiety, was fabricated by four efficient reaction steps from commercially available phloroglucinol in a 50.1% isolated yield overall. Our synthetic route, which constructs the chalcone skeleton in the final stage via a Claisen–Schmidt condensation of the key intermediate with the desired benzaldehyde derivative, can rapidly produce a vast library of DMC derivatives.

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Apoptosis induced in MCF-7 human breast cancer cells by 2′,4′-dihydroxy-6-methoxy-3,5-dimethylchalcone isolated from Eugenia aquea Burm f. leaves

Cited by 30 publications

References 12 publications

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

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

Anti-proliferative Activity of Crotalaria pallida Aiton on MCF-7 Breast Cancer Cells

Total Syntheses of 4′,6′‐Dimethoxy‐2'‐Hydroxy‐3′,5′‐Dimethylchalcone Derivatives

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