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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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 IC50 values 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. |
|
体内研究
(In Vivo) |
VS 8 inhibits angiogenesis in the chick chorioallantoic membrane without oral toxicity[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| 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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