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橙皮苷VO(IV)络合物的抗氧化作用及其在癌症化学预防中的作用。

Antioxidant effects of the VO(IV) hesperidin complex and its role in cancer chemoprevention.

作者信息

Etcheverry Susana Beatriz, Ferrer Evelina Gloria, Naso Luciana, Rivadeneira Josefina, Salinas Victoria, Williams Patricia Ana María

机构信息

Centro de Química Inorgánica (CEQUINOR/CONICET,UNLP), Facultad de Ciencias Exactas, Universidad Nacional de La Plata, C. Correo 962, 1900 La Plata, Argentina.

出版信息

J Biol Inorg Chem. 2008 Mar;13(3):435-47. doi: 10.1007/s00775-007-0332-9. Epub 2007 Dec 21.

DOI:10.1007/s00775-007-0332-9
PMID:18097692
Abstract

Vanadium compounds are known for a variety of pharmacological properties. Many of them display antitumoral and osteogenic effects in several cell lines. Free radicals induce the development of tumoral processes. Natural polyphenols such as flavonoids have antioxidant properties since they scavenge different free radicals. For these reasons it is interesting to investigate the effects of a new complex generated between the vanadyl(IV) cation and the flavonoid hesperidin. The complex has been synthesized and characterized by physicochemical methods. Spectroscopic analysis revealed a 1:1 stoichiometry of ligand:VO and coordination by deprotonated cis-hydroxyl groups to the disaccharide moiety of the ligand. The complex improves the superoxide dismutase (SOD)-like activity of the ligand, but the scavenging of other radicals tested does not change upon complexation. When tested on two tumoral cell lines in culture (one of them derived from a rat osteosarcoma UMR106 and the other from human colon adenocarcinoma Caco-2), the complex enhanced the antiproliferative effects of the free ligand, and this effect correlated with the morphological alterations toward apoptosis. Also, on the osteoblastic cell line the complex stimulated cell proliferation and collagen type I production at low concentrations. At higher doses the complex behaved as a cytotoxic compound for the osteoblasts.

摘要

钒化合物因其多种药理特性而闻名。其中许多在多种细胞系中表现出抗肿瘤和成骨作用。自由基会诱导肿瘤进程的发展。天然多酚如黄酮类化合物具有抗氧化特性,因为它们能清除不同的自由基。出于这些原因,研究钒(IV)阳离子与类黄酮橙皮苷形成的新络合物的作用很有意思。该络合物已通过物理化学方法合成并表征。光谱分析表明配体与VO的化学计量比为1:1,且去质子化的顺式羟基与配体的二糖部分配位。该络合物提高了配体的超氧化物歧化酶(SOD)样活性,但络合后对其他测试自由基的清除能力没有变化。在两种培养的肿瘤细胞系(一种源自大鼠骨肉瘤UMR106,另一种源自人结肠腺癌Caco-2)上进行测试时,该络合物增强了游离配体的抗增殖作用,且这种作用与细胞凋亡的形态学改变相关。此外,在成骨细胞系上,该络合物在低浓度时刺激细胞增殖和I型胶原蛋白的产生。在较高剂量时,该络合物对成骨细胞表现出细胞毒性。

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