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1.
Chinese Pharmacological Bulletin ; (12): 204-209, 2020.
Article in Chinese | WPRIM | ID: wpr-857017

ABSTRACT

Aim To investigate the effect of Rhein derivative 4a containing amide structure on migration and invasion in ovarian cancer SKOV3 cells and its possible mechanism. Methods Ovarian cancer SK0V3 cells were used as target cells. Molecular docking and West-em blot were used to detect the regulatory effect of derivative 4a on Racl protein. CCK8, HE staining, Scratch and Transwell assay were used to detect the effects of derivative 4a on the proliferation, morphology , migration and invasion of SK0V3 cells, respectively. Western blot was employed to determine the expression of matrix metalloproteinases and EMT-related proteins. Results Derivative 4a could effectively bind to Racl protein, and the binding energy was-29. 10 kcal • mol"1, which was significantly lower than that of Rhein; it also could down-regulate the expression of Racl protein in SK0V3 cells. Derivative 4a could significantly inhibit the proliferation, invasion and migra tion of SKOV3 cells, and induce a large amount of cellular vacuolation; derivative 4a could also down-regu-\ late the expression of MMP-2 and MMP-9, up-regulate the expression of EMT epithelial marker protein E-ca-derin but down-regulate the expression of vimentin and j3-cantenin. Conclusions Derivative 4 a can inhibit the proliferation, migration and invasion of ovarian cancer SK0V3 cells. The mechanism may relate to its targeted regulation of Racl, thereby inhibiting the secretion of matrix metalloproteinases, up-regulating the expression of key molecule E-caderin and down-regula-ting the expression of Vimentin and (3-cantenin in EMT i process.•.

2.
Journal of Huazhong University of Science and Technology (Medical Sciences) ; (6): 145-148, 2010.
Article in Chinese | WPRIM | ID: wpr-341107

ABSTRACT

To investigate the effect of autoimmune regulator(AIRE)on phagocytic clearance of apoptotic cells,a recombinant expression vector containing full-length human AIRE cDNA was transfected into 16HBE cells.After incubation with transfected 16HBE cells,engulfment of apoptotic HL-60 cells induced by camptothecin was detected by myeloperoxidase(MPO)staining.The change in the expression of Rac 1 in transfected 16HBE cells was determined by RT-PCR and Western blotting.The results showed that the phagocytosis percentage of the experimental group,the mock trans-fection group and the negative control group(non-apoptotic cells)was(25.50±3.67)%,(6.25±1.58)%and(1.0±0.67)%,respectively.Moreover,the expressions of Rac 1 mRNA and protein were up-regulated in AIRE-transfected 16HBE cells,suggesting that A1RE may function as a regulator in the phagocytic clearance of apoptotic cells by promoting the expression of Rac 1.

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