Synthesis and anticancer activity of new flavonoid analogs and inconsistencies in assays related to proliferation and viability measurements.
Synthesis and anticancer activity of new flavonoid analogs and inconsistencies in assays related to proliferation and viability measurements.
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DOI：
10.3892/ijo.2014.2452
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发表时间：
2014-08
影响因子：
5.2
通讯作者：
Meier GP
中科院分区：
文献类型：
--
作者：
Forbes AM;Lin H;Meadows GG;Meier GP
黄酮类化合物已被深入研究，因为它们具有抗癌、抗炎、抗病毒和抗衰老的能力，并且通常作为与其抗炎活性相关的补充剂销售。以前的研究主要集中在极性天然黄酮类化合物的作用上。我们研究了新型疏水性和亲脂性黄酮醇对人DU-145和PC-3前列腺癌细胞系的活性。所有黄酮醇类似物比天然存在的黄酮醇槲皮素、山奈酚、山奈素和高良姜素更有活性。最有效的类似物对DU-145和PC-3细胞的活性是槲皮素的6.5倍，并且在生物学相关浓度范围内（低微摩尔）。我们还评估了黄酮醇类似物对正常细胞的潜在毒性作用，在研究黄酮类化合物的抗癌作用时，这一评估经常被忽视。在这些分析过程中，我们发现各种代谢和DNA染色测定是不可靠的方法来评估细胞活力的黄酮类化合物。在没有细胞的情况下，黄酮类化合物还原比色染料，如MTT和Alcohol Blue。我们发现，黄酮醇处理的前列腺癌细胞与结晶紫染色强度低于未处理的细胞在无毒浓度。选择台盼蓝排除试验作为测量细胞活力的可靠替代方法。
Flavonoids have been studied intensely for their ability to act as anti-carcinogenic, anti-inflammatory, anti-viral and anti-aging agents and are often marketed as supplements related to their anti-inflammatory activity. Previous studies have primarily focused on the effects of polar natural flavonoids. We examined the activity of novel hydrophobic and lipophilic flavonols against human DU-145 and PC-3 prostate cancer cell lines. All flavonol analogs were more active than the naturally occurring flavonols quercetin, kaempferol, kaempferide and galangin. The most potent analogs were 6.5-fold more active against DU-145 and PC-3 cells than quercetin and fell within the biologically relevant concentration range (low micromolar). We also evaluated the potential toxic effects of flavonol analogs on normal cells, an assessment that has frequently been ignored when studying the anticancer effects of flavonoids. During these analyses, we discovered that various metabolic and DNA staining assays were unreliable methods for assessing cell viability of flavonoids. Flavonoids reduce colorimetric dyes such as MTT and Alamar Blue in the absence of cells. We showed that flavonol-treated prostate cancer cells were stained less intensely with crystal violet than untreated cells at non-toxic concentrations. The trypan blue exclusion assay was selected as a reliable alternative for measuring cell viability.
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影响因子：
7.5
作者：
Hollman, PCH;Katan, MB
通讯作者：
Katan, MB
黄酮类化合物对体外人类癌细胞的结构相关细胞毒作用
影响因子：
6.7
作者：
Chang, Hui;Mi, Mantian;Yuan, Jialin
通讯作者：
Yuan, Jialin
影响因子：
5
作者：
Garcia-Mediavilla, Victoria;Crespo, Irene;Gonzalez-Gallego, Javier
通讯作者：
Gonzalez-Gallego, Javier
白藜芦醇类似物的甲氧基衍生物在转化的成纤维细胞中选择性诱导线粒体凋亡途径的激活。
影响因子：
8.8
作者：
通讯作者：
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影响因子：
56.9
作者：
BJELDANES, LF;CHANG, GW
通讯作者：
CHANG, GW