Danihelová Martina, Veverka Miroslav, Sturdík Ernest, Jantová Soňa
Institute of Biochemistry, Nutrition and Health Protection, Faculty of Chemical and Food Technology, Slovak University of Technology, Bratislava, Slovakia.
Eurofins Bel/Novamann s.r.o., Nové Zámky, Slovakia.
Interdiscip Toxicol. 2013 Dec;6(4):209-16. doi: 10.2478/intox-2013-0031.
Quercetin is a natural polyphenol with proven health beneficial activities. In this study 15 new quercetin derivatives were prepared with the aim to enhance their bioavailability. Modification of their physicochemical properties could herewith improve the action in cells. The prepared compounds were tested for their antioxidant and cytotoxic activity. The ability to scavenge free radicals as well as ferric reducing antioxidant power of the new derivatives was not better than that of unmodified quercetin. But for acetylated esters a better cytotoxic activity was found on human cervical cancer cells HeLa than for the initial molecule. The best effect revealed chloronaphtoquinone quercetin (IC50=13.2 µM). For this compound comparable cytotoxic action on non-cancer murine fibroblast cells was detected (IC50=16.5 µM). The obtained results indicate that appropriate lipophilization of the quercetin molecule could improve its cytotoxic action in cells, probably due to its enhanced bioavailability.
槲皮素是一种具有已证实的有益健康活性的天然多酚。在本研究中，制备了15种新的槲皮素衍生物，旨在提高它们的生物利用度。其物理化学性质的改变有望改善在细胞中的作用。对所制备的化合物进行了抗氧化和细胞毒性活性测试。新衍生物清除自由基的能力以及铁还原抗氧化能力并不比未修饰的槲皮素更好。但对于乙酰化酯，发现其对人宫颈癌细胞HeLa的细胞毒性活性比初始分子更好。最佳效果显示氯萘醌槲皮素（IC50 = 13.2 μM）。对于该化合物，在非癌性小鼠成纤维细胞中检测到了相当的细胞毒性作用（IC50 = 16.5 μM）。所得结果表明，槲皮素分子的适当亲脂化可能会改善其在细胞中的细胞毒性作用，这可能是由于其生物利用度提高所致。
