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A team of researchers discovered an anticancer activity of artificial sweeteners Saccharine and Thiosaccharine. According to these researchers, artificial sweeteners like Saccharine and Thiosaccharine, when conjugated with platinum, forming a platinum coordination complex (cisplatin) has anti-cancer activity.
Cisplatin is a member of platinum-containing anti-cancer drugs. Its full name is cis-diamminedichloroplatinum (II) and also called as cisplatinum or platamin etc. The presence of two chlorine atoms in cisplatin can be displaced slowly by water, which in turn displaced by a range of nitrogenous bases present in the DNA. Thus, a complex of cisplatin with nitrogenous bases (especially guanine) causes a cross-link of DNA. That means one chlorine atom can be displaced by guanine of one DNA strand while the second chlorine atom is displaced by the guanine of the second DNA strand forming DNA cross-link and halting the DNA replication.
However, the two chlorine atoms present in the cisplatin can easily be replaced by artificial sweeteners like saccharine and thiosaccharine resulting in the formation of platinum saccharine, cis-[Pt(sac)2(NH3)2], and platinum thiosaccharine complex, cis-[Pt(tsac)2(NH3)2] respectively. And these complexes can easily be involved in DNA cross-link formation.
The researchers synthesized cis-[Pt(sac)2(NH3)2] as colorless crystals by treating cisplatin with two equivalents of sodium saccharinate in boiling water and similarly they prepared cis-[Pt(tsac)2(NH3)2] using sodium thiosaccharinate.
Researchers took A549 human alveolar type-II cell lines to study the anti-cancer activity of artificial sweeteners Saccharine and Thiosaccharine. They took Methotrexate as a positive control and 3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MIT) assay to determine their dose-dependent cytotoxicity. The result revealed that the platinum thiosaccharine complex has higher activity than platinum saccharine complex this is because the Pt-S bond is stronger than the Pt-N bond. However, with respect to the control (Methotrexate) both showed significant anti-cancer activities.
Reference: Journal of Inorganic Biochemistry
Article DOI: 10.1016/j.jinorgbio.2014.07.017