Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
Background & Objective: Arsenic trioxide (As2O3) is a new drug used to treat the patients with solid tumor,but the mechanism is still unclear. This study was designed to investigate the effect of mitochondrial dependent pathway in apoptosis induced by arsenic trioxide in multidrug resistant KBv200 cells and their parental sensitive KB cells.
Methods: The cytotoxic effect of As2O3 on KB and KBv200 cells was measured by MTT assay. KB and KBv200 cells were treated respectively with As2O3 for 12, 24, 48 hours. Cell apoptosis was determined by Annexin V FITC staining. Mitochondrial membrane potential was labeled by DiOC6 and examined by flow cytometry.
Results: Arsenic trioxide showed the inhibition of KB and KBv200 cells proliferation in vitro. The IC(50)s of As2O3 to KB and KBv200 cells were (0.22+/-0.02)microg/ml and (0.20+/-0.01)microg/ml, respectively. As2O3 induced cell apoptosis in time- dependent manner. The apoptosis rates were 20.2%+/-3.1% and 52.2%+/-11.0% for KB cells and 15.8%+/-1.3% and 36.4%+/-5.9% for KBv200 cells under 2.5 microg/ml As2O3 treating 24 h and 48 h, respectively. The levels of mitochondrial membrane potential were concentration-dependently decreased after treating with arsenic trioxide for 12, 24, and 48 hours.
Conclusion: The decrease of mitochondrial membrane potential maybe plays an important role in apoptosis induced by As2O3.
Download full-text PDF |
Source |
|---|
Publication Analysis
Top Keywords
Similar Publications
TRPM4 channels contribute to Adriamycin chemoresistance in breast cancer cells.
Eur J Pharmacol
July 2025
National Engineering Research Center for the Emergency Drug, Beijing Institute of Pharmacology and Toxicology, Beijing, China. Electronic address:
Chemoresistance presents a critical challenge in breast cancer treatment. Here, we report that transient receptor potential melastatin 4 (TRPM4) plays a role in modulating doxorubicin (ADR) resistance in breast cancer cells. TRPM4 expression was significantly upregulated at both the mRNA and protein levels in MCF-7/ADR cells, a human breast cancer cell line resistant to the chemotherapy drug ADR.
View Article and Find Full Text PDFIdentification of selenium-containing benzamides as potent microtubule-targeting antitumor agents.
Bioorg Chem
June 2025
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. Electronic address:
IMB5046, a microtubule inhibitor discovered by our team, served as the lead compound for designing a series of selenium-containing benzoates and benzamides. Among these, compound 2g emerged as a lead candidate, demonstrating potent antiproliferative activity. Mechanistic studies revealed that 2g bound to the colchicine site of tubulin, caused G2/M cell cycle arrest, and generated ROS.
View Article and Find Full Text PDFDual inhibition of topoisomerase II and microtubule of podophyllotoxin derivative 5p overcomes cancer multidrug resistance.
Eur J Pharmacol
November 2024
The State Key Laboratory of Basis and New Drug Development of Natural and Nuclear Drugs, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, 100193, Beijing, China. Electronic address:
Compound 5p is a 4β-N-substituted podophyllotoxin derivative, which exhibited potent activity toward drug-resistant K562/A02 cells and decreased MDR-1 mRNA expression. Here, we further investigated its detail mechanism and tested its antitumor activity. 5p exerted catalytic inhibition of topoisomerase IIα, and didn't show the inhibitor of topoisomerase I.
View Article and Find Full Text PDFBI-2865, a pan-KRAS inhibitor, reverses the P-glycoprotein induced multidrug resistance in vitro and in vivo.
Cell Commun Signal
June 2024
State Key Laboratory of Oncology in South China, Guangdong Provincial Clinical Research Center for Cancer, Sun Yat-sen University Cancer Center, Guangzhou, 510060, P. R. China.
Background: Multidrug resistance (MDR) limits successful cancer chemotherapy. P-glycoprotein (P-gp), BCRP and MRP1 are the key triggers of MDR. Unfortunately, no MDR modulator was approved by FDA to date.
View Article and Find Full Text PDFPhenylspirodrimane with Moderate Reversal Effect of Multidrug Resistance Isolated from the Deep-Sea Fungus sp. 3A00409.
Molecules
April 2024
Fujian Provincial Key Laboratory of Pharmacology of Natural Medicine, School of Pharmacy, Fujian Medical University, Fuzhou 350122, China.
Two new phenylspirodrimanes, stachybotrins K and L ( and ), together with eight known analogues (-), were isolated from deep-sea-derived sp. MCCC 3A00409. Their structures were determined by extensive NMR data and mass spectroscopic analysis.
View Article and Find Full Text PDF