In vitro and in vivo study of cucurbitacins-type triterpene glucoside from Citrullus colocynthis growing in Saudi Arabia against hepatocellular carcinoma

Chromatographic investigation of fruits obtained from Citrullus colocynthis, growing in Saudi Arabia, led to isolation of two compounds; Cucurbitacin E glucoside (Cu E, 1), and Cucurbitacin I glucoside (Cu I, 2). The chemical structures of 1 and 2, were elucidated by spectroscopic analyses include; 1D (1H and 13C) and 2D (COSY, HMQC and HMBC) NMR and ESI-MS spectroscopy. The in vitro cytotoxic activity against Hepatoma Cell Line (HepG2) and mice-bearing tumor of Ehrlich's ascites carcinoma (EAC) of the compounds were estimated. Both compounds had potent inhibitory activity on HepG2 with IC50 3.5 and 2.8 nmol/mL, respectively. In addition to these activities, the in vivo study employing EAC, showed the capability of both compounds to prolong the survival time, life span and normalize the biochemical parameters of the infected mice with EAC.

In vitro cytotoxicity study of Cu E (1) and Cu I (2), isolated from Citrullus colocynthis, showed potent cytotoxic activity against HepG2 and EAC with IC50 3.5 and 2.8 nmol/mL, respectively. The in vivo study of both compounds, showed their capability to prolong the survival time, life span and normalize the biochemical parameters of the infected mice with EAC .Figure optionsDownload as PowerPoint slideHighlight
► Two cucurbitacins glucosides were obtained from saudi Citrullus colocynthis.
► Their effects against HepG2 and EAC was estimated.
► Both compounds had potent inhibitory activity on HepG2 with IC50 3.5 and 2.8 nmol/mL.
► The biochemical parameters of the isolated compounds were evaluated.