ABSTRACT
Aim To explore the concentration range of organic solvent which can both effectively increase solubility of the difficult soluble medicine monomer, and have low toxicity to cells, and to clarify the influence of different concentration of ethanol on curcumol efficacy.Methods Different DMSO and ethanol concentrations were diluted in culture medium and incubated with cells A549, NCI-H460, NCI-H1299, NCI-1650, LTEP-a2 and SPC-A1 for 12 h, 24 h, or 48 h, cell viability was tested by a colorimetric assay with 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide(MTT), and different concentrations of ethanol with/without different concentrations of curcumol were also prepared with culture medium, then incubate with A549 and NCI-H460 cells for 24 h, and cell viability was tested by MTT as well.Results Within 48 h the solution with 0.008(V/V) DMSO or less had no significant effect on the cell A549 compared with control group, for NCI-H1650 the concentration was 0.004(V/V) or less, for NCI-H460 the result turned to be 0.002(V/V) or less, and the solution with DMSO below 0.001(V/V) had significant effect on the three other cells, NCI-H1299, LTEP-a2 and SPC-A1.While within 48 h, the liquor with 0.004(V/V) ethanol or less did not exhibit significant cytotoxic effect on the cell A549, for NCI-H460 and NCI-H1650 the result of ethanol concentration became 0.002(V/V) or less, for NCI-H1299 the data was 0.001(V/V) or less, and the liquor with ethanol below 0.001(V/V) showed significant cytotoxic effect on LTEP-a2and SPC-A1.When the proportion of ethanol in solution was below 0.01, it has no cytotoxic on cell A549 and NCI-H460, and the curcumol solution prepared with this kind of ethanol solution only represented the efficacy of curcumol on the cells.Since the solution with 0.01(V/V) ethanol dissolved the curcumol better, the cell viability changed from about 100% to about 35%.Conclusions Different organic solvent expressed different toxicity to the same cell, and the sensitivity of different cells to one organic solvent is dissimilar.and DMSO could be the optimum solvent for A549 and NCI-H1650, while the optimum solvent of NCI-H1299 is ethanol, for NCI-H460 it could be both and DMSO and ethanol, and DMSO and ethanol is not suitable for LETP-a2, SPC-A1 to be solvent.
ABSTRACT
Aim To determine the effective compo-nents of Semen Ziziphi Spinosae for sedative-hypnotic and its mechanism. Methods The extraction of Se-men Ziziphi Spinosae and the rat brain homogenates were prepared. High concentrations of Diazepam com-petitively replaced the ligand compounds of Semen Ziz-iphi Spinosae combining BDZ receptor in brain tissue, and all the compounds with sedative and hypnotic effects were collected and identified by HPLC and LC-MS technique, as the compounds extracted from the brain tissue were administered with Semen Ziziphi Spi-nosae. The brain tissue was administered with Diaze-pam, and with Semen Ziziphi Spinosae and Diazepam. Results The HPLC chromatograms show that the peak time of BDZ receptor ligand compounds was 2. 71 min and 46. 87min, when compared with Diazepam. And the LC-MS chromatograms display the relative molecu-lar weight of the ligand compounds was 274. 28 m/z, 453. 34 m/z,496. 34 m/z and 608. 38 m/z respective-ly. According to the fingerprint of Semen Ziziphi Spi-nosae, these compounds may be fatty acid substances and lupine pill triterpene compounds. Conclusions On the basis of the principle of receptor ligand bind-ing, we established a way to quickly analyze and iden-tify the role of natural products in the same drug target compounds. The method not only can clearly define the effective components of natural products, but also clar-ify the mechanism of action of the compounds. The ac-tive ingredient of calm hypnosis in Semen Ziziphi Spi-nosae may be fatty acid substances Palmitic acid ( C16 H32 O2 ) and lupine pill triterpene compounds Alphitolic acid( C30 H48 O4 ) and Spinosin( C28 H32 O15 ) . They exert their sedative and hypnotic effects by combining with BDZ receptor, and the research has laid a theoretical foundation for the further study about mechanism of Se-men Ziziphi Spinosae.
ABSTRACT
Objective To report the use of self expanding metallic stents in treatment of benign tracheobronchial stenosis. Methods Nineteen patients with benign tracheobronchial stenosis were treated with implantation of self expanding stents (Ultraflex, Microvasive). Results Stents produced immediate improvement in clinical pulmonary sign and symptoms. Pulmonary function tests in 10 patients demonstrated a mean improvement in FEV1of 45%, FVC of 38%. Following up duration ranged from 10-18 months. Complications included recurrent pneumonia in 3 patients, airway obstruction due to granuloma formation in 2 patients, and stent migration in 1 patient. They were treated successfully with antibiotic therapy, laser therapy, and stent reimplantation, respectively. Conclusion Self expanding metallic stent implantation is a feasible and effective method of treating benign tracheobronchial stenosis.