文章：

利用黄酮类化合物取代状态预测人类黑色素瘤抗癌效果：一项体外研究

Using Flavonoid Substitution Status to Predict Anticancer Effects in Human Melanoma Cancers: An In Vitro Study

原文发布日期：23 January 2024

DOI: 10.3390/cancers16030487

类型: Article

开放获取: 是

英文摘要：

Skin cancers are a dominant type of cancer that impacts millions per year. Cancer is a heterogeneous disease triggered by the irreversible impairment of cellular homeostasis and function. In this study, we investigated the activity of 37 structurally diverse flavonoids to find potentially active substances using two melanoma cell lines: C32 and A375. First, the cytotoxic potential and DNA biosynthesis inhibition of flavonoids were tested to determine the most active compounds in cancer and normal cells. Second, the molecular mechanism of the anticancer activity of flavonoids was elucidated using Western blot and immunofluorescence analyses. Compounds1,6,15, and37reduced the viability of A375 and C32 cell lines via the intrinsic and extrinsic pathways of apoptosis, whereas16and17acted in a higher degree via the inhibition of DNA biosynthesis. In our experiment, we demonstrated the anticancer activity of compound15(5,6-dihydroxyflavone) for the first time. The in vitro studies pointed out the importance of the flavonoid core in hydroxyl groups in the search for potential drugs for amelanotic melanoma.

摘要翻译： 

皮肤癌是每年影响数百万人的主要癌症类型。癌症是一种异质性疾病，由细胞稳态和功能的不可逆损伤引发。本研究采用C32和A375两种黑色素瘤细胞系，对37种结构多样的黄酮类化合物进行活性筛选，以寻找潜在活性物质。首先通过细胞毒性测试和DNA生物合成抑制实验，测定黄酮类化合物在癌细胞与正常细胞中的活性差异，从而筛选出最具活性的化合物。随后采用蛋白质印迹法和免疫荧光分析技术，阐明黄酮类化合物抗癌活性的分子机制。研究发现化合物1、6、15和37通过内在与外在凋亡途径降低A375和C32细胞系的存活率，而化合物16和17主要通过抑制DNA生物合成发挥作用。本实验首次证实了化合物15（5,6-二羟基黄酮）的抗癌活性。体外研究结果表明，在寻找无色素性黑色素瘤潜在药物的过程中，黄酮母核羟基化结构具有重要研究价值。

原文链接：

Using Flavonoid Substitution Status to Predict Anticancer Effects in Human Melanoma Cancers: An In Vitro Study