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Inorg Chem:药+金属离子 = 抗癌

来源:生物谷 2016-02-19 10:21

图片来源:medicalxpress.com

2016年2月19日 讯 /生物谷BIOON/ --目前,抵御化疗耐药性的癌症对于科学家们来讲依然还是一项巨大挑战,而一种利用两组化合物配对的新型方法或许可以表现出特殊的抗癌特性,近日刊登在国际杂志Inorganic Chemistry上的一篇研究报告中,科学家们就利用疼痛药物结合金属离子进行结合,在实验室中成功地破坏了药物耐受性癌细胞,同时还保证了正常细胞不受损伤。

长期以来研究者们经常会在癌症药物中配合使用金属离子,比如顺铂就是一种基于铂的抗癌疗法,其在抵御肺癌、卵巢癌及其它癌症上已经使用了很多年了,但通常癌细胞都会产生一定的耐药性。

然而最近研究者们却利用金属离子和药物的组合来开发破坏癌细胞的新型疗法,不同于基于铂的络合物,金属络合物会表现出一定的抗癌潜能,而且很多研究都发现非甾体类的抗炎药(nonsteroidal anti-inflammatory drugs, NSAIDs)可以有效抵御特定的癌症,并且增强其它药物的作用活性。文章中研究者Paul J. Dyson就与同事决定将非甾体类的抗炎药吲哚美辛同携带钌和锇离子的双氯芬酸进行结合来观察这种组合是否具有异性的抗癌效能。

研究人员创造了多种不同的NSAID-金属离子复合物组合,随后在实验室中检测其抵御癌症的潜力,结果显示,相比顺铂而言有些组合可以更加有效地抵御卵巢癌细胞,而且相比较健康细胞而言,有些组合对顺铂耐药的癌细胞而言具有较强的毒性作用,本文研究或对于后期开发新型的药物组合来彻底抵御癌症提供了新的线索。(生物谷Bioon.com)

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Nonsteroidal Anti-inflammatory—Organometallic Anticancer Compounds

Emilia Păunescu, Sarah McArthur, Mylène Soudani, Rosario Scopelliti, and Paul J. Dyson*

Compounds that combine metal-based drugs with covalently linked targeted organic agents have been shown, in some instances, to exhibit superior anticancer properties compared to the individual counterparts. Within this framework, we prepared a series of organometallic ruthenium(II)- and osmium(II)-p-cymene complexes modified with the nonsteroidal anti-inflammatory drugs (NSAIDs) indomethacin and diclofenac. The NSAIDs are attached to the organometallic moieties via monodentate (pyridine/phosphine) or bidentate (bipyridine) ligands, affording piano-stool Ru(II) and Os(II) arene complexes of general formula [M(η6-p-cymene)Cl2(N)], where N is a pyridine-based ligand, {2-(2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetoxy)ethyl-3-(pyridin-3-yl)propanoate} or {2-(2-(2-((2,6-dichlorophenyl)amino)phenyl)acetoxy)ethyl-3-(pyridin-3-yl)propanoate}, [M(η6-p-cymene)Cl2(P)], where P is a phosphine ligand, {2-(2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetoxy)ethyl-4-(diphenylphosphanyl)benzoate} or {2-(2-(2-((2,6-dichlorophenyl)amino)phenyl)acetoxy)ethyl-4-(diphenylphosphanyl)benzoate, and [M(η6-p-cymene)Cl(N,N′)][Cl], where N,N′ is a bipyridine-based ligand, (4′-methyl-[2,2′-bipyridin]-4-yl)methyl-2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetate), (4′-methyl-[2,2′-bipyridin]-4-yl)methyl-2-(2-((2,6-dichlorophenyl)amino)phenyl)acetate), (bis(2-(2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetoxy)ethyl)[2,2′-bipyridine]-5,5′-dicarboxylate), or (bis(2-(2-(2-((2,6-dichlorophenyl)amino)phenyl)acetoxy)ethyl)[2,2′-bipyridine]-5,5′-dicarboxylate). The antiproliferative properties of the complexes were assessed in human ovarian cancer cells (A2780 and A2780cisR, the latter being resistant to cisplatin) and nontumorigenic human embryonic kidney (HEK-293) cells. Some of the complexes are considerably more cytotoxic than the original drugs and also display significant cancer cell selectivity.

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