A Meta-Analysis on the Relationship Between Derivatization and Cytotoxicity of Chalcone Compound

Rui-qiang Su
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Abstract

Cancer is a worldwide leading cause of death. The development of an effective anti-cancer drug is with pressing need. Chalcone and its derivatives have been considered as general anti-cancer compounds. Because of its easy synthesis and good biological activity, Chalcones has attracted extensive attention. However, the potency of Chalcones to various cancer types and the ideal modification site on Chalcones has not been well documented. Herein, we systematically retrieved multiple pieces of literature from the Web-Of-Science search engine and examined chalcone derivatization literature from 2017 to 2022. Through meta-analysis, we found significant heterogeny between the cytotoxicity effects of chalcone compounds between normal cells and cancer cells (P <0.05). Chalcone derivatives indicate different potency to glioma (mean 0.46 μM), skin cancer (mean 6.63 μM), colon cancer (mean 7.87 μM), colorectal cancer (mean 8.12 μM), and brain cancer (mean 9.53 μM). Moreover, the modification site also statistically correlates to the potency of Chalcone derivatives. Among fluorine, bromine, chloride modifications, ortho chlorine substitution shows the optimal potency as indicated by the minimum overall mean IC50 values.
查尔酮衍生物化与细胞毒性关系的meta分析
癌症是世界范围内导致死亡的主要原因。迫切需要研制一种有效的抗癌药物。查尔酮及其衍生物被认为是一般的抗癌化合物。查尔酮因其易于合成和具有良好的生物活性而受到广泛关注。然而,查尔酮对各种类型癌症的效力和查尔酮的理想修饰位点尚未得到很好的证明。本文系统地检索了Web-Of-Science搜索引擎上的多篇文献,并对2017年至2022年的查尔酮衍生化文献进行了研究。通过meta分析,我们发现查尔酮类化合物在正常细胞和癌细胞之间的细胞毒性作用存在显著的异质性(P <0.05)。查尔酮衍生物对胶质瘤(平均0.46 μM)、皮肤癌(平均6.63 μM)、结肠癌(平均7.87 μM)、结直肠癌(平均8.12 μM)和脑癌(平均9.53 μM)的效价不同。此外,修饰位点也与查尔酮衍生物的效价有统计学相关性。在氟、溴、氯化物改性中,邻氯取代的效价最优,其总体平均IC50值最小。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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