Synthesis and evaluation of a novel nanosized anionic linear globular dendrimer G2-ciprofloxacin conjugate against prostate cancer

Abstract

Prostate cancer is the second most common cancer in the world and the fifth cause of cancer deaths in men. Ciprofloxacin enables the inhabitation of the development of prostate cancer. In this regard, we plan to improve the anticancer effect of ciprofloxacin using the anionic G2 dendrimer in conjunction with ciprofloxacin. In the current study, we measured the size and the zeta potential as well as LC Mass to prove the fact that the conjugation was synthesized correctly. The anticancer activity among three groups including Ciprofloxacin, Ciprofloxacin –G2 dendrimer, and control was measured in vitro. In vitro studies showed that G2 anionic linear-globular polyethylene-glycol-based dendrimer, which conjugated to ciprofloxacin, was able to significantly improve the treatment efficacy over clinical ciprofloxacin alone with respect to proliferation assay. Maximal inhibitory concentration (IC50) was calculated as 200 μg/mL for ciprofloxacin alone and 30μg/mL for ciprofloxacin–G2 dendrimer. In addition, the growth of DU-145 cancerous cells was inhibited by ciprofloxacin–G2 dendrimer conjugate and the number of apoptotic and necrotic cells was increased significantly as evaluated by an annexin V-fluorescein isothiocyanate assay. Ciprofloxacin –G2 dendrimer conjugate was able to increase Bcl-2/Bax ratio in a large scale as compared with the control group and CBL alone. According to the above results, this compound could be considered as a good candidate for functional cancer treatment with low side effects.