Cell experiment:

The cells are treated with different concentrations (0.01, 0.1, 0.5, 1, 5 and 10 μg/mL) of belotecan for 24, 48 and 72 h. Control samples of each cell line are treated with medium only. Cell viability is measured using the MTS assay[1].

Animal experiment:

Mice: Nude mice with established U87MG glioma are treated with a dose of belotecan of 0 mg/kg (control group, injection with saline), 40 mg/kg (group A) or 60 mg/kg (group B). Thereafter, the dose is repeated once every 4 days for a total of four doses. Tumor volume is measured histologically and apoptosis is detected[1].

Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic and water-soluble camptothecin derivative.

Belotecan exerts a significant cytotoxic effect on YD-8, YD-9 and YD-38 cells in a time- and dose-dependent manner with IC50 values of 2.4, 0.18 and 0.05 μg/mL at 72 h following treatment. Belotecan induces apoptosis in these cell lines. Belotecan induces G2/M phase arrest in oral squamous cell cancer cells[1]. Belotecan shows a significant anticancer effect on glioma cells, with IC50 values of 9.07 nM for LN229, 14.57 nM for U251 MG, 29.13 nM for U343 MG, and 84.66 nM for U87 MG[2].

Belotecan has a significant effect on intracerebral glioma growth, with animals having significantly smaller tumors than those in the control group[3].

[1]. Kim YK, et al. Anticancer effects of CKD-602 (Camtobell®) via G2/M phase arrest in oral squamous cell carcinoma cell lines. Oncol Lett. 2015 Jan;9(1):136-142. [2]. Kim YY, et al. CKD-602, a camptothecin derivative, inhibits proliferation and induces apoptosis in glioma cell lines. Oncol Rep. 2009 Jun;21(6):1413-9. [3]. Kim CY, et al. Antitumor activity of CKD-602, a camptothecin derivative, in a mouse glioma model. J Clin Neurosci. 2012 Feb;19(2):301-5.