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基于多环查耳酮的丙烯酰胺在人MCF-7和HeLa癌细胞系中的生物学评价。

Biological evaluation of polycyclic chalcone based acrylamides in human MCF-7 and HeLa cancer cell lines.

作者信息

Gunasekaran Vijayakumar, Yuvakkumar Rathinam, Ganesan Ravi, Palapetta Surya Cholayil, Gurusamy Harichandran

机构信息

Department of Polymer Science, University of Madras, Guindy Campus, Chennai, 600 025, India.

Department of Physics, Alagappa University, Karaikudi-630 003, India.

出版信息

Environ Res. 2023 Apr 1;222:115395. doi: 10.1016/j.envres.2023.115395. Epub 2023 Jan 31.

Abstract

Breast and cervical cancer account for the majority of cancer-narrated fatalities among women worldwide, necessitating the development of novel, effective therapeutic ways to combat the disease. In this study, we synthesized 6-methoxy naphthalene and anthracene-based acrylamide chalcone (NBA and ABA) and evaluated its activity for cell multiplication inhibition against two cancer cell lines from humans such as MCF-7 (Human Breast) and HeLa (Cervical) by MTT assay. Physiochemical characterization, such as FT-IR and NMR analyses, validated the synthesized NBA and ABA. Both NBA and ABA have shown antiproliferative action against two cancer cell lines, each with IC50 values of 38.46 and 48.25 μg/mL for HeLa cells and 38.02 and 36.35 μg/mL for MCF-7 cell lines. The results suggest that these acrylamide chalcones for cancer therapy at the lowest concentration. NBA and ABA could prevent cervical and breast cancer in-vitro, and their anti-cancer activity was closely related to methoxy-substituted naphthalene, anthracene ring, α, β-unsaturated carbonyl and amide group. According to docking data, the NBA and ABA have dock scores ranging from -8.7 to -11.44 kcal/mol. The highest dock score for compound ABA was -11.58 kcal/mol and compound NBA was -10.77 kcal/mol with Braf (5VAM) binding site.

摘要

乳腺癌和宫颈癌是全球女性癌症相关死亡的主要原因,因此需要开发新颖、有效的治疗方法来对抗这种疾病。在本研究中,我们合成了基于6-甲氧基萘和蒽的丙烯酰胺查尔酮(NBA和ABA),并通过MTT法评估了其对两种人类癌细胞系(如MCF-7(人乳腺癌)和HeLa(宫颈癌))细胞增殖抑制的活性。通过FT-IR和NMR分析等物理化学表征验证了合成的NBA和ABA。NBA和ABA对两种癌细胞系均显示出抗增殖作用,对HeLa细胞的IC50值分别为38.46和48.25μg/mL,对MCF-7细胞系的IC50值分别为38.02和36.35μg/mL。结果表明,这些丙烯酰胺查尔酮在最低浓度下可用于癌症治疗。NBA和ABA可在体外预防宫颈癌和乳腺癌,其抗癌活性与甲氧基取代的萘、蒽环、α,β-不饱和羰基和酰胺基团密切相关。根据对接数据,NBA和ABA的对接分数在-8.7至-11.44 kcal/mol之间。化合物ABA与Braf(5VAM)结合位点的最高对接分数为-11.58 kcal/mol,化合物NBA为-10.77 kcal/mol。

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