Study on Preparation and in vitro Anticancer Activity of PFV-modified Paclitaxel/artesunate Co-loaded Targeting Micelles / 中国药房

OBJECTIVE：To prepare cell penetrating peptide PFV-modified paclitaxel （PTX）/artesunate（ART）co-loaded targeting micelles ，and to investigate in vitro anti-tumor activity. METHODS ：According to optimal technology ，PFV-modified PTX/ ART co-loaded targeting micelles were prepared by membrane hydration method ，and were characterized. Using blank micelle as blank control ，sulforhodamine B （SRB）method was used to evaluate the toxicity of PTX micelles ，ART micelles ，PTX/ART micelles and PFV-modified PTX/ART co-loaded targeting micelles to human gastric cancer BGC- 823 cells. The coumarin was used as fluorescent probe replacing PTX to prepare corresponding micelles. Then ，the uptake of BGC- 823 cells to corresponding micelles and targeting effect were observed and determined by flow cytometry and fluorescence microscope. The effects of PTX micelles ， ART micelles ，PTX/ART micelles and PFV-modified PTX/ART co-loaded targeting micelles on the invasion of BGC- 823 cells were investigated by Transwell chamber method. RESULTS ：Average particle size of PFV-modified PTX/ART co-loaded targeting micelles was （51.30±3.95）nm；PDI was 0.19±0.01，and Zeta potential was （0.21±0.02）mV. The encapsulation efficiency of PTX and ART were higher than 90％. The shape of micelles were spherical. The blank micelles had no obvious toxicity to BGC-823 cells. The IC 50 value of PTX micelles ，PTX/ART micelles and PFV-modified PTX/ART co-loaded targeting micelles to BGC-823 cells were （3.09±0.22），（1.93±0.24），（1.11±0.15）μmol/L，respectively. The distribution amount of different micelles in BGC- 823 cell nucleus in the descending order were PFV-modified coumarin/ART micelles ＞coumarin/ART micelles ＞coumarin micelles＞blank control. The order of inhibitory effect was PFV-modified PTX/ART co-loaded targeting micelles ＞PTX/ART micelles＞ART micelles ＞PTX micelles ＞blank control. CONCLUSIONS： Prepared PFV-modified PTX/ART No.81874347） co-loaded targeting micelles are in line with the quality of 1915286446@qq.com Chinese Pharmacopoeia . It shows strong cytotoxicity to BGC-823 cells，can improve the drug targeting and the cell uptake，and inhibit the inv asion and metastasis of BGC- 823 cells.

Inhibition of valdecoxib on the proliferation of human gastric cancer cells / 中国药理学通报

AIM To study the effect and mechanism of valdecoxib, a selective COX 2 inhibitor, on human gastric cancer BGC 823 cells. METHODS MTT assay and flow cytometry were used to observe the effect of valdecoxib on proliferation, apoptosis and the cell cycle distribution of BGC 823 cells. Laser confocal microscopy, transmission electron microscope and DNA fragmentation assay were further used to detect the apoptosis. The content of LDH was examined using LDH kit. RESULTS Valdecoxib in 25～400 ?mol?L -1 significantly inhibited the proliferation of BGC 823 cell in a time and dose dependent fashion, the inhibition rate of proliferation was 24 0%～92 0% after 72 h, and the rate of apoptosis was increased from (2 6?0 7)% to (7 6?1 5) %～(16 5?1 5)%. 100～400 ?mol?L -1 valdecoxib also decreased the proliferation index and the proportion of cells in the S phase, increased the proportion of cells in the G 0/G 1 phase, but had no effect on the proportion of cell in the G 2/M phase. CONCLUSION Valdecoxib inhibits human gastric cancer BGC 823 cells growth by inducing apoptosis and cell cycle arrest. The growth inhibitory effect of 400 ?mol?L -1 valdecoxib is also associated with cell necrosis.