Abstract: | Background: Realgar which contains arsenic components has been used in traditional Chinese medicine(TCM) as an anticancer drug. However, neither Realgar nor its formula are soluble in water. As a result, highdose of Realgar has to be administered to achieve an effective blood medicine concentration, and this is associatedwith adverse side effects. The objective of the present study was to increase the solubility of a formula usinghydrometallurgy technology as well as investigating its effects on in vitro and in vivo cell proliferation andapoptosis in Sarcoma-180 cell line. Materials and Methods: Antiproliferative activity of Realgar BioleachingSolution (RBS) was evaluated by MTT assay. Further, effects of RBS on cell proliferation and apoptosis werestudied using flow cytometry and transmission electron microscopy. Kunming mice were administered RBS invivo, where arsenic specifically targeted solid tumors. Results: The results indicated that RBS extract potentlyinhibited the tumor growth of Sarcoma-180 cell line in a dose-dependent manner. Flow cytometry and transmissionelectron microscopy further indicated that RBS significantly induced cell apoptosis through the inhibition of cellcycle pathway in a dose-dependent manner. Further, on RBS administration to mice, arsenic was specificallytargeted to solid tumor.s Conclusions: RBS could substitute for traditional Realgar or its formula to work as apotent tool in cancer treatment. |