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Article in Chinese | WPRIM | ID: wpr-299317


<p><b>OBJECTIVE</b>To observe the effects of deguelin on the proliferation of breast cancer MCF-7 cells and lung cancer H1299 cells in vitro and the expression of minichromosome maintenance protein 3 (MCM3) and CDC45 in the cells.</p><p><b>METHODS</b>MTT assay was used to evaluate the proliferation of MCF-7 and H1299 cells exposed to different concentrations of deguelin for 48, 72 or 96 h. The growth of the cells was observed microscopically and the changes of MCM3 and CDC45 expressions in MCF-7 and H1299 cells following deguelin treatment were detected with fluorescence quantitative PCR.</p><p><b>RESULTS</b>The proliferation of MCF-7 cells was significantly inhibited by exposure to 0.25, 0.5, 1, 5, 10, 30, and 50 µmol/L deguelin for 48, 72, and 96 h in a concentration- and time-dependent manner. In MCF-7 cells, the ICof deguelin at 48, 72, and 96 h was 9, 3, and 2 µmol/L, respectively. Deguelin treatments of H1299 cells at 0.5, 1, 5, 10, 30, 50, and 100 µmol/L also resulted in a concentration- and time-dependent inhibition of the cell growth with an ICat 96 h of 2 µmol/L. Optical microscopy of the cells revealed a decreased number of viable cells with obvious cell shrinkage following deguelin treatments. The expression of MCM3 and CDC45 were significantly reduced in the cells after deguelin treatments.</p><p><b>CONCLUSION</b>Deguelin can inhibit the proliferation of MCF-7 and H1299 cells in vitro and down-regulate the expression of MCM3 and CDC45 in the cells.</p>

Article in Chinese | WPRIM | ID: wpr-273799


<p><b>OBJECTIVE</b>To investigate performance of a biotinylated imaging probe 3a for targeted imaging of breast cancer cells.</p><p><b>METHODS</b>Ultraviolet absorption spectrum and fluorescence spectrum were employed to analyze the spectral characteristics of 3a. The fluorescence spectrums of 3a treated with different concentrations of glutathione (GSH) were obtained to determine the sensibility of 3a to GSH. Flow cytometry was used to determine the cellular uptake of 3a by MCF-7 cells, MDA-MB-231 cells and Hs 578Bst cells in the presence or absence of biotin, and the imaging performance of 3a in the 3 cell lines was assessed under an inverted fluorescent microscope. The toxicity of 3a to the cells was evaluated using MTT method.</p><p><b>RESULTS</b>3a showed the strongest absorption peak at 510 nm, and its fluorescence emission signal was the strongest at 544 nm. As the concentration of GSH increased (0-6 mmol/L), 3a exhibited an increasing fluorescence signal at 544 nm. The cellular uptake of 3a was markedly higher in MDA-MB-231 cells and MCF-7 cells than in Hs 578Bst cells. The imaging studies showed that 3a had a good breast cancer cell-targeting property and produced clear images under fluorescent microscope. MTT assay demonstrated no obvious toxicity of 3a in Hs 578Bst cells even at the concentration of 20 µmol/L, but MCF-7 cells and MDA-MB-231 cells exposed to 2-20 µmol/L 3a showed a lowered cell viability.</p><p><b>CONCLUSION</b>3a is capable of targeted imaging of breast cancer cells mediated by biotin. 3a at the concentration of 2-20 µmol/L has minimal cytotoxicity to normal breast cells but can lower the viability of breast cancer cells.</p>

Acta Pharmaceutica Sinica ; (12): 1452-1456, 2012.
Article in Chinese | WPRIM | ID: wpr-274639


The effect and mechanism of mulberry leaves extracts (MLE) on glucose uptake of insulin-resistant HepG2 cells in vitro was explored. The insulin resistant models of HepG2 were induced by high concentration of insulin for 24 h. The models were incubated in a buffer containing mulberry leaves extracts. The glucose consumption was detected by glucose assay kits and the AMP-activated protein kinase (AMPK), Akt activation was examined by Western blotting. Mulberry leaves polysaccharides, mulberry leaves flavonoids and mulberry leaves extracts advanced glucose uptake of insulin-resistant HepG2 cells; Mulberry leaves extracts enhance phosphorylation of AMPK. Mulberry leaves extracts do not change the phosphorylation status of Akt. The glucose consumptions of insulin resistant model of HepG2 were promoted by mulberry leaves extracts. MLE stimulates HepG2 cell AMPK activity acutely without changing the Akt activity.

AMP-Activated Protein Kinases , Metabolism , Cell Proliferation , Drugs, Chinese Herbal , Pharmacology , Flavonoids , Pharmacology , Glucose , Metabolism , Hep G2 Cells , Humans , Hypoglycemic Agents , Pharmacology , Insulin Resistance , Morus , Chemistry , Phosphorylation , Plant Extracts , Pharmacology , Plant Leaves , Chemistry , Plants, Medicinal , Chemistry , Polysaccharides , Pharmacology , Proto-Oncogene Proteins c-akt , Metabolism
Acta Pharmaceutica Sinica ; (12): 933-938, 2006.
Article in Chinese | WPRIM | ID: wpr-294910


<p><b>AIM</b>To study a new way to prepare high-dosage paclitaxel entrapped magnetic targeted nanoparticles and evaluate its quality.</p><p><b>METHODS</b>Fe3O4 nanoparticles are prepared by co-depositing, at the same time ultrasonic is used to decrease soft agglomerate of nanoparticles and increase disperse level of it. The property of nanoparticles surface is improved to make the integrating of liposome and nanoparticle to be tighter. At last, paclitaxel entrapped magnetic solid liposome nanoparticles have been prepared by microemulsion-curing under low-temperature. The loading efficiency and encapsulating rate were determined by reverse-phase high-perfomance chromatography.</p><p><b>RESULTS</b>The nanoparticles have spherical shape. Diameter of nanoparticle ranged from 150 nm to 170 nm. 98.29% of the drug is entrapped in the particle.</p><p><b>CONCLUSION</b>Magnetic susceptibility of nanoparticles is high, and the nanoparticles meet with the demand of targeted delivery system.</p>

Antineoplastic Agents, Phytogenic , Chemistry , Drug Compounding , Methods , Drug Delivery Systems , Emulsions , Ferrosoferric Oxide , Chemistry , Hydrogen-Ion Concentration , Liposomes , Nanoparticles , Chemistry , Paclitaxel , Chemistry , Particle Size , Temperature , Ultrasonics