Awang N, Kamaludin N F, Ghazali A R
Environmental Health and Industrial Safety Programme, School of Diagnostic and Applied Health Sciences, Faculty of Health Sciences, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur, Malaysia.
Pak J Biol Sci. 2011 Aug 1;14(15):768-74. doi: 10.3923/pjbs.2011.768.774.
Cancer is one of the main causes of mortality and morbidity in world. New compounds are currently being synthesized to combat this disease. The organotins are gaining more attention as anti-cancer agents due to their potent cytotoxicity properties. In this study, a series of newly synthesized organotins namely dimethyltin (IV) (compound 1), dibutyltin (IV) (compound 2) and triphenyltin (IV) benzylisopropyldithiocarbamate (compound 3) were assessed for their cytotoxic activities against human Chang liver cells and hepatocarcinoma HepG2 cells. The cytotoxicity of these organotins in both cells upon 24 h treatment was assessed using 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. Compound 2 and 3 exhibited potent cytotoxic activities towards both cells where the IC50 values were less then 10 microM. The IC50 value for compound 2 was 2.5 microM in Chang liver cells and 7.0 microM in HepG2 cells whereas compound 3 exhibited an IC50 value of 1.5 microM in Chang liver cells and 2.5 microM in HepG2 cells. Therefore, compound 2 and 3 were more toxic against human Chang liver cells as compared to hepatocarcinoma HepG2 cells. Interestingly, compound 1 did not have any IC50 value in both cells and hence can be classified as non-toxic. In conclusion, organotin (IV) benzylisopropyldithiocarbamate with insertion of dibutyl and triphenyl functional group possess potent cytotoxicity properties. Structural modification of these compounds can be carried out in further studies to produce less or non toxic effects towards normal human cell.
癌症是全球主要的死亡和发病原因之一。目前正在合成新的化合物来对抗这种疾病。有机锡因其强大的细胞毒性特性，作为抗癌剂正受到越来越多的关注。在本研究中，评估了一系列新合成的有机锡，即二甲基锡（IV）（化合物1）、二丁基锡（IV）（化合物2）和三苯基锡（IV）苄基异丙基二硫代氨基甲酸盐（化合物3）对人张氏肝细胞和肝癌HepG2细胞的细胞毒性活性。使用3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四氮唑溴盐（MTT）法评估这些有机锡在两种细胞中经24小时处理后的细胞毒性。化合物2和3对两种细胞均表现出强大的细胞毒性活性，其IC50值小于10微摩尔。化合物2在张氏肝细胞中的IC50值为2.5微摩尔，在HepG2细胞中的IC50值为7.0微摩尔，而化合物3在张氏肝细胞中的IC50值为1.5微摩尔，在HepG2细胞中的IC50值为2.5微摩尔。因此，与肝癌HepG2细胞相比，化合物2和3对人张氏肝细胞的毒性更大。有趣的是，化合物1在两种细胞中均没有任何IC50值，因此可归类为无毒。总之，插入二丁基和三苯基官能团的有机锡（IV）苄基异丙基二硫代氨基甲酸盐具有强大的细胞毒性特性。在进一步的研究中可以对这些化合物进行结构修饰，以对正常人类细胞产生较小或无毒性作用。
