Bile salts containing vesicles (bilosomes) represent a portentous vesicular carrier that showed prosperous results in delivering active moieties in the gastrointestinal tract (GIT). In this study, bilosomes were exploited to deliver sulfated polysaccharide-protein complexes of Enteromorpha intestinalis (EHEM) and enhance its activity against hepatocellular carcinoma as well as resist harsh GIT conditions. Bilosomes were prepared using the sodium salt of three different bile acids (cholic, deoxycholic, taurodeoxycholic) and two different nonionic surfactants (Span 40 and 65). The effects of experimental variables were thoroughly studied to obtain an optimum formulation loading EHEM. The selected formulation (EH-Bilo-2) prepared with sodium cholate and Span 65 displayed nano-sized (181.1 ± 16.80 nm) spherical vesicles with reasonable entrapment efficiency (71.60 ± 0.25%) and controlled release properties; and thus was investigated as anti-hepatocarcinogenic candidate for in vivo studies. Treatment of hepatocellular carcinoma (HCC) bearing rats with EH-Bilo-2 experienced significant decrease in serum α-fetoprotein, endoglin, lipocalin-2, and heat shock protein 70 levels vs. the untreated counterparts. Furthermore, the photomicrographs of their liver tissue sections showed focal area of degenerated pleomorphic hepatocytes with fine fibrosis originating from the portal area. Thus, the optimized bilosomal formulation is a promising delegate for tackling hepatocellular carcinoma owing to its powerful anti-cancer and anti-angiogenic activity.
The cytotoxic activity of petroleum ether extract of the leaves of Cassia roxburghii Linn. against HCT-116 and MCF-7 cell lines resulted with IC50=34.9 and 38.04 μg/ml, respectively, while against HepG-2 showed no activity. A bioassay guided-fractionation approach was conducted to isolate and identify the active cytotoxic principles. Further chromatographic separation and purification of the petroleum ether extract resulted in the isolation of two anthraquinones identified as aloe-emodin acetate and aloe-emodin, along with stigmasterol, β-sitosterol and palmitic acid. The structure elucidation of isolated compounds was performend using 1D, 2D-NMR and HR-MS. Furthermore, the cytotoxicity of aloe-emodin acetate and aloe-emodin were evaluated and resulted with IC50=153.30 and 70.02 μg/ml against HCT-116 and with 93.20 and 53.20 μg/ml against MCF-7, respectively, while against HepG-2 showed no activity. Moreover, the antiviral activity of the two isolated anthraquinones was tested against influenza virus-A, and resulted with IC50=10.23 as well as 2.00 and with CC50=1.32 and 0.47 μg/ml, respectively.
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