The antimalarial artemisinin (ART) possesses anticancer activity, but its underlying mechanism remains largely unclear. Using a chemical proteomics approach with artemisinin-based activity probes, we identified over 300 specific ART targets. This reveals an anticancer mechanism whereby ART promiscuously targets multiple critical biological pathways and leads to cancer cell death. The specific c...

Two widely used oxidizing dyes, 2,3,5-triphenyltetrazoliumchloride and méthylà ̈ne blue, can greatly potentiate hyperthermic cytotoxicity whenadministeredsimultaneouslywith 2-cyanocinnamicacid. The same compoundsare virtually nontoxic to L929 cells if administered alone at 42°Cor in combinationwith 2-cyanocinnamicacid at 37°C. Cytotoxicity was synergisticallyenhanced by the combinedregimensaf...

BACKGROUND The mechanism of cytotoxicity induction by flavonoids has been studied by many investigators, but their tumor specificity is not clear. To address this point, 10 licorice flavonoids were subjected to quantitative structure-activity relationship (QASR) analysis with cytotoxicity assay with four human oral carcinoma and three normal cell lines. MATERIALS AND METHODS Cytotoxicity was ...

A tyrosinase-directed therapeutic approach for treating malignant melanoma uses depigmenting phenolic prodrugs such as 4-hydroxyanisole (4-HA) for oxidation by melanoma tyrosinase to form cytotoxic o-quinones. However, in a recent clinical trial, both renal and hepatic toxicity were reported as side effects of 4-HA therapy. In the following, 4-HA (200 mg/kg i.p.) administered to mice caused a 7...

Lung cancer is the most commonly diagnosed with a high mortality rate. Cisplatin one of important chemotherapeutic agents for treatment lung patients, especially in advanced stages. Recent studies show that cisplatin may interact mitochondria to induce apoptosis, which partly account its cytotoxicity. In study, we explored effect resistin on cisplatin-induced cytotoxicity A549 cells and assesse...

PURPOSE Imexon is a 2-cyanoaziridine agent that has been shown to inhibit growth of chemotherapy-sensitive myeloma cells through apoptosis with decreased cellular stores of glutathione and increased reactive oxygen species (ROS). We examined the mechanism of imexon cytotoxicity in a diverse panel of dexamethasone and chemotherapy-sensitive and -resistant myeloma cell lines. EXPERIMENTAL DESIG...

BACKGROUND CD20 monoclonal antibodies are widely used in clinical practice. Antibody-dependent cellular cytotoxicity, complement-dependent cytotoxicity and direct cell death have been suggested to be important effector functions for CD20 antibodies. However, their specific contributions to the in vivo mechanism of action of CD20 immunotherapy have not been well defined. DESIGN AND METHODS Her...

Background: In Indonesia, this species was well known in Sumatera, Kalimantan, Java, and Sulawesi. Peronema canescens Jack (Sungkai) traditionally used as an anti-flatulent, fever, toothache. Sungkai leaves contain many secondary metabolites with potential anticancer activity. The reported research still limited to the cytotoxic activity of chloroform extract on HT-29 colon cancer cell line. Ho...

Introduction: The mechanism of putative cytotoxicity of 4-[3-(cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidone (rolipram), a specific phosphodiesterase-4 (PDE4) inhibitor, on glioblastoma multiforme (GBM) is almost unknown. This study aimed to investigate the role of protein kinase B (Akt) pathway in the cytotoxic effect of rolipram on human GBM U87 MG cell line and tumor-initiating cells (TICs) ...