Cytotoxic and inhibitory effects of 4,4′-dihydroxy chalcone (RVC-588) on proliferation of human leukemic HL-60 cells

Saydam, Güray; Aydin, Hikmet Hakan; Şahin, Fahri; Kücükoglu, Özlem; Erciyas, Erçin; Terzıoğlu, Ender; Büyükkeçeci, Filiz; Omay, Serdar Bedii

doi:10.1016/s0145-2126(02)00058-9

Cited by 53 publications

(31 citation statements)

References 18 publications

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“…All the analogues were compared with the basic unsubstitutedchalcone to dertermine the cytotoxic activity.The present results demonstrate that the chalcones and their analogues inhibit the proliferation of Jurkat (human T-lymphocyte leukemia) cells by triggering apoptosis.Among them the analogues 4 and 15 exhibited most potent cytotoxicity than the parental basic chalconemolecule [26]. All the test compounds have also shown cytotoxic activity (in a concentration dependent manner) against HL-60 cells [27].The most active analogues 4 and 15 on Jurkat cells exhibited activity similar to the parental molecule against HL-60.In this case, the analogues 7 and 12 have shown the more significant activity against HL-60 cells than the parental compound, but they were not more active than the parent molecule in the case of Jurkat cells. Among the synthesized chalcones,the most active compounds were 4,15 and their IC50 values on T cell leukemia (Jurkat) cells were 1.6x10-2 mM,1.7x10-2 mM respectively.…”

Section: Biological Screening Methodology:assay Methods Of Cytotoxic Amentioning

confidence: 96%

Synthesis, in vitro Anticancer Activity Evaluation and Docking Investigations of Novel Aromatic Chalcones

Srinivasarao¹

2013

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Abstract:In a wide search program toward new anticancer agents, a series of Aromatic chalcones have been synthesized by condensing benzaldehyde derivatives with arylmethylcetone in potassium hydroxide ethanol according to the ClaisenSchmidth condensation at room temperature. The synthetic chalcones have been determined by IR spectroscopy and 1H-NMR spectroscopy. The anticancer activitiesof the compounds were evaluated against in vitro using human tumour cell lines of Jurkat and HL-60 cell lines and MTT assay. From the series, two compounds(4,15) exhibited potent growth inhibitory effects against the proliferation of human T-lymphocyte leukemia compared to the parent unsubstitutedchalcone. The result shows that the electron donating groups moiety may increase anticancer activity. Aromatic chalcones with hydroxyl group,methoxy group on A ring at positions 2 or 3 are considered as lead compounds for generation of new potential anticancer drugs in future.Similarly,the compounds(7,12) exhibited potent growth inhibitory effects against HL-60 cells. The results are very encouraging. Future studies include testing the compounds in vivo with and without radiation. Docking studies with 1NKP have shown that the compound 17 has highest IC50 against human leukemia cells (HL-60).

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Section: Biological Screening Methodology:assay Methods Of Cytotoxic Amentioning

confidence: 96%

Synthesis, in vitro Anticancer Activity Evaluation and Docking Investigations of Novel Aromatic Chalcones

Srinivasarao¹

2013

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“…In addition, a huge array of hemisynthetic or synthetic chalcone analogues has been created to identify the most efficient structure for the inhibition of proliferation (see Table 1) [9,91,95,145,148,156,179].…”

Section: Effect Of Chalcones On Tumor Progressionmentioning

confidence: 99%

Dietary chalcones with chemopreventive and chemotherapeutic potential

et al. 2011

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Chalcones are absorbed in the daily diet and appear to be promising cancer chemopreventive agents. Chalcones represent an important group of the polyphenolic family, which includes a large number of naturally occurring molecules. This family possesses an interesting spectrum of biological activities, including antioxidative, antibacterial, anti-inflammatory, anticancer, cytotoxic, and immunosuppressive potential. Compounds of this family have been shown to interfere with each step of carcinogenesis, including initiation, promotion and progression. Moreover, numerous compounds from the family of dietary chalcones appear to show activity against cancer cells, suggesting that these molecules or their derivatives may be considered as potential anticancer drugs. This review will focus primarily on prominent members of the chalcone family with an 1,3-diphenyl-2-propenon core structure. Specifically, the inhibitory effects of these compounds on the different steps of carcinogenesis that reveal interesting chemopreventive and chemotherapeutic potential will be discussed.

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“…Several chalcones have been isolated or synthesized, and their cytotoxicity on cancer cell lines and their anticancer activity in cancer animal models have been reported. 11,12 Furthermore, the molecular mechanisms of the anticancer action of chalcones have also been investigated. The chalcones exhibited anticancer activity through multiple mechanisms including cell cycle disruption, angiogenesis inhibition, tubulin polymerization inhibition, apoptosis induction and blockade of the nuclear factorkappa B (NF-κB) signaling pathway.…”

Section: Introductionmentioning

confidence: 99%

Mechanism of cytotoxic activity of chalcone derivatives against K562 leukemia cell lines

et al. 2017

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Two chalcone derivatives i.e. (E)-1-(4-aminophenyl)-3-(2,3dimethoxyphenyl)-prop-2-en-1-one (Compound-1), and (E)-1-(4-aminophenyl)-3-phenylprop-2-en-1-one) (Compound-2), has been proven to have potential cytotoxic activity. The aim of this study was to evaluate the effect of these compounds on PI3K/Akt signalling pathway in K562 cell lines. After incubation with the tested compounds, AKT, caspase-3, STAT3 and cyclin D1 concentrations were measured using ELISA. Furthermore, cell cycle was analysed using flowcytometry. Imatinib and isotretinoin were used as positive control, whereas cell culture without treatment was used as negative control. The AKT concentration after treatment with Compound-1 and -2 was significantly lower than that control, imatinib and isotretinoin (p<0.05). The apoptotic indices after treatment with Compound-1 and -2 were significantly higher than control, however they were lower than imatinib and isotretinoin (p<0.05). The caspase-3 concentration after treatment with Compound-1 at 5 and 10 µg/mL and Compound-2 at 10 µg/mL was significantly higher than that control and imatinib, however it was lower than isotretinoin (p<0.05). The STAT3 concentration after treatment with Compound-1 and -2 was significantly lower than that control and isotretinoin at 50 µg/mL (p<0.05) and similar with imatinib (p>0.05). The cyclin D1 concentration after treatment with Compound-1 and -2 was significantly lower than that control, imatinib and isotretinoin (p<0.05). In addition, Compound-1 and -2 arrested G 0 / G 1 and G 2 /M phase in K562 cell lines, with comparable results to imatinib and isotretinoin. In conclusion, the mechanism of cytotoxic activity of Compound-1 and -2 are through the PI3K/Akt signalling pathway inhibition, apoptosis induction by upregulation of apoptotic markers, and inhibition of cell cycle progression by regulating cell cycle-related factors. ABSTRAKDua turunan kalcon yaitu (E)-1-(4-aminofenil)-3-(2,3dimetoksifenil)-prop-2-en-1-one (Senyawa-1), and (E)-1-(4-aminofenil)-3-fenilprop-2-en-1-one) (Senyawa-2), terbukti mempunyai aktivitas sitotoksik yang potensial. Tujuan penelitian ini adalah untuk mengkaji efek kedua senyawa tersebut pada jalur sinyal PI3K/Akt pada sel K562. Setelah J Med Sci, Volume 49, No. 4, 2017 October: 153-164 154 diinkubasikan dengan senyawa uji, kadar AKT, caspase-3, STAT3 dan siklin D1 diukur dengan ELISA. Selanjutnya siklus sel dianalisis dengan flowcyometry. Imatinib dan isotretinoin digunakan sebagai kontrol positif dan kultur sel tanpa perlakuan sebagai kontrol negatif. Kadar AKT setelah perlakuan dengn Senyawa-1 dan -2 lebah rendah secara nyata dibaningkan dengan kontrol, imatiib dan isotretinoin (p<0.05). Indeks apoptosis setelah perlakuan dengan Senyawa-1 dan -2 lebih tinggi secara nyata dibandingkan kontrol, tetapi lebih rendah dibandingkan imatinib dan isotretinoin (p<0.05). Kadar caspase-3 setelah perlakuan Senyawa-1 dengan kadar 5 dan 10 µg/mL dan Senyawa-2 dengan kadar 10 µg/mL lebih tinggi secara nyata dibandingkan kontrol dan imatinib, tet...

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Cytotoxic and inhibitory effects of 4,4′-dihydroxy chalcone (RVC-588) on proliferation of human leukemic HL-60 cells

Cited by 53 publications

References 18 publications

Synthesis, in vitro Anticancer Activity Evaluation and Docking Investigations of Novel Aromatic Chalcones

Synthesis, in vitro Anticancer Activity Evaluation and Docking Investigations of Novel Aromatic Chalcones

Dietary chalcones with chemopreventive and chemotherapeutic potential

Mechanism of cytotoxic activity of chalcone derivatives against K562 leukemia cell lines

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