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含金属钴和一氧化碳配体的羰基钴配合物(CORMs)具有抗肿瘤和抗炎的潜力。本文在合成3个杂化型钴一氧化碳释放分子(分别含乙酰水杨酸、对氨基苯甲酸、7-羟基香豆素结构片段)的基础上,从动物毒性、抗肿瘤及抗炎活性等方面对其生物活性进行了初步评价。结果表明:配合物CO释放半衰期在43~53 min之间;小鼠经口LD50介于1 500~5 000 mg·kg-1;大鼠连续等剂量给药后,配合物1对大鼠肝细胞的生理形态和功能都有影响,对肾脏的功能和生理形态的影响都较为严重;配合物1对He La细胞和Hep G2细胞均表现出较强的生长抑制作用(IC50分别为36.20和39.25μmol·L-1),配合物2对He La细胞的增殖抑制作用低于对照组5-FU(IC50114.19μmol·L-1),但它们三者对Hep G2细胞的生长抑制作用都强于对照组5-FU(IC50 171.34μmol·L-1)。抗炎实验表明:它们均能降低细胞内亚硝酸盐水平,配合物1和2比3表现出更强的活性,通过与相应配体对照实验证实,它们的抗炎活性主要来自于CORMs释放的CO分子。
Cobalt carbonyl complexes (CORMs) containing metal cobalt and carbon monoxide ligands have antitumor and anti-inflammatory potential. Based on the synthesis of three hybrid cobalt monoxide carbon monoxide release molecules (acetylsalicylic acid, p-aminobenzoic acid and 7-hydroxycoumarin structural fragment respectively), this study aimed to study the toxicity, antitumor and anti-inflammatory activity of animal The biological activity of a preliminary evaluation. The results showed that the half life of the compound CO was between 43 and 53 min, the oral LD50 was between 1 500 and 5 000 mg · kg-1 in rats, The physiological and morphological changes of the cells affected the renal function and morphology. The complex 1 showed strong growth inhibition on HeLa cells and Hep G2 cells (IC50: 36.20 and 39.25, respectively) The inhibitory effect of complex 2 on Hela cell proliferation was lower than that of 5-FU (IC50114.19μmol·L-1), but the inhibitory effect of the three compounds on Hep G2 cells was stronger than that of 5-FU (IC50114.19μmol·L-1) Control group 5-FU (IC50 171.34μmol·L-1). Anti-inflammatory experiments showed that both of them can reduce intracellular nitrite levels, and complexes 1 and 2 to 3 showed more activity. Compared with the corresponding ligands, their anti-inflammatory activity mainly came from the release of CORMs CO molecule.