体外研究
(In Vitro) | VS 8 (Compound VS 8) (0.01-100 μM, 24 h) shows potent anti-proliferative activity against MCF-7, MDA-MB-231, Hep G2, and HUVECs cells[1].
VS 8 induces early apoptosis in MDA-MB-231 (1413 nM, 72 h), Hep G2 (257.80 nM, 24 h), and HUVECs (1954 nM, 24 h) cells[1].
VS 8 is shown to be a pro-oxidant molecule that enhances the ROS level in Hep G2 cells[1].
VS 8 inhibits wound healing and migration of MCF-7 cancer cells[1].
VS 8 downregulates human vascular endothelial growth factor (hVEGF) and hVEGFR-2 expression in HUVECs[1].
VS 8 (257.80 nM, 48 h) arrests cell cycle at ‘G0/G1’ and ‘S’ phase in CD44+ and CD133+ CSCs, respectively[1].
VS 8 inhibits TGF-β-induced epithelial-mesenchymal transition (EMT) in hepatocellular carcinoma by the upregulation of E-cadherin and the suppression of vimentin and SNAIL[1].
Cell Proliferation Assay[1] | Cell Line: | MCF-7, MDA-MB-231, Hep G2, and HUVECs cells | | Concentration: | 0.01, 0.1, 1, 10, 50, and 100 μM | | Incubation Time: | 24 h | | Result: | Showed significantly potent anti-proliferative activity against all the selected cell lines in a dose-dependent manner, with IC50values of 953.30, 1413, 257.80, and 1954 nM against MCF-7, MDA-MB-231, Hep G2, and HUVECs cells. |
Apoptosis Analysis[1] | Cell Line: | MDA-MB-231, Hep G2, and HUVECs cells | | Concentration: | 1413, 257.80, and 1954 nM for MDA-MB-231, Hep G2, and HUVECs cells, respectively. | | Incubation Time: | 72 h for MDA-MB-231 cells; 24 h for Hep G2 and HUVECs cells | | Result: | Resulted in high population of early apoptotic MDA-MB-231 cells (68.34 ± 0.18%). A significant increase in % apoptotic index (~86.66%) was observed in Hep G2 cells. The percentage of early apoptotic cells were found to be ~37.53% in HUVECs cells. |
Cell Cycle Analysis[1] | Cell Line: | CD44+ and CD133+ CSCs isolated from Hep G2 cells | | Concentration: | 257.80 nM | | Incubation Time: | 48 h | | Result: | Arrested cell cycle at ‘G0/G1’ and ‘S’ phase in CD44+ and CD133+ CSCs, respectively. |
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体内研究
(In Vivo) | VS 8 inhibits angiogenesis in the chick chorioallantoic membrane without oral toxicity[1].
| Animal Model: | Male Wistar rats (180-220 gm)[1] | | Dosage: | 5 mg/kg | | Administration: | Oral administration (Pharmacokinetic Analysis) | | Result: | Pharmacokinetic parameters for VS 8 in rats after administration of oral dose (5 mg/ kg)[1]
| Pharmacokinetic parameters | Unit | Value | | Cmax | μg/mL | 39.7193 ± 0.36 | | Tmax | hrs | 6 ± 0 | | AUC(0-72) | mg/mL*hrs | 621.3236 ± 1.843 | | AUC(0-∞) | mg/mL*hrs | 625.2219 ± 1.864 | | AUMC(0-∞) | (mg/mL*hrs2) | 8929.284 ± 72.85 | | MRT | hrs | 14.2817 ± 0.102 | | t1/2 | hrs | 11.9277 ± 0.324 |
Data represented as mean ± SD (n = 3); t1/2, Half-Life; Cmax, Maximum Observed Concentration; Tmax, Maximum Observed Time; AUC, Area Under Curve; AUMC Area Under Movement Curve, MRT, Mean Residence Time. |
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