Evaluation of the constituent compounds, antioxidant, anticancer, and antimicrobial potential of Prangos ferulacea plant extract and its effect on Listeria monocytogenes virulence gene expression.

Article

作者: Hojjati, Mohammad ; Alizadeh Behbahani, Behrooz ; Noshad, Mohammad ; Vasiee, Alireza ; Jalil Sarghaleh, Shahab

Prangos ferulacea plant is very popular in Iran due to its unique properties in treating diseases and its special flavor. To check the characteristics of this plant, first, its extract was extracted using the maceration method. Its chemical composition was investigated using high-performance liquid chromatography (HPLC) that p-coumaric was identified as its main compound, and Fourier-transform infrared spectroscopy (FTIR) showed the presence of functional groups related to phenolic, flavonoid, tannins, and carboxylic acids such as caffeic acid and coumaric acid composition. Total phenol content (TPC), total flavonoid content (TFC), and beta-carotene were equal to 202.04 ± 5.46 mg gallic acid equivalent (GAE)/g dry weight, 1,909.46 ± 13 μg quercetin (QE)/g of dry weight, and 2.91 mg/100 g. The antioxidant property of the extract was evaluated using 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid (ABTS) free radical scavenging and ferric reducing antioxidant power assay (FRAP). According to the IC50 obtained for DDPH (274 ± 7.2 μg/mL) and ABTS (120.45 ± 9.6 μg/mL) and FRAP values [1.92 ± 0.05 μg ascorbic acid equivalent (AAE)/g of extract], this extract had high antioxidant properties. Cytotoxicity was evaluated against the survival of HT 29 cells that IC50 was 82.15 ± 0.02 μg/mL. The antimicrobial property of the extract was calculated using disk diffusion agar (DDA), well diffusion agar (WDA), minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC). Listeria monocytogenes has the highest sensitivity to this extract and inhibition zone based on DDA and WDA method and with an MIC and MBC equal to 16 and 128 mg/mL has the least resistance. The morphology change of L. monocytogenes strain was proved through scanning electron microscope (SEM) and confocal laser scanning microscopy (CLSM). The extract caused a significant reduction in the transcription of genes involved in the film formation ability of L. monocytogenes. The obtained results fully prove the very practical and pragmatic characteristics of P. ferulacea.

2016-03-01·Chemico-Biological Interactions2区 · 医学

DDPH, a novel antihypertensive agent, is a potential dual inhibitor of hepatic CYP2D and CYP3A

2区 · 医学

Article

作者: Chen, Hui ; He, Wenjuan ; Zhu, Yinsong ; Ren, Ping ; Hu, Jiong ; Gao, Xiujuan

DDPH (1-(2, 6-dimethylphenoxy)-2-(3, 4-dimethoxyphenylethylamino) propane hydrochloride) is a promising novel antihypertensive agent, with potent antihypertensive, neuroprotective and cardioprotective effects. This study aimed to investigate the effects of DDPH on the expression and activity of hepatic cytochrome P450 (CYP) isoforms and evaluate the metabolic drug-drug interactions of DDPH with propafenone. Our results showed that orally administered DDPH (12.5-50 mg/kg/d) for 7 days significantly inhibited CYP2D1 and CYP3A1 activity and mRNA and protein expression but weakly increased CYP1A2 activity and expression in rats. Enzyme kinetics studies showed that DDPH was a competitive inhibitor of CYP2D1 and mixed inhibitor of CYP3A1 in rat liver microsomes with Ki values of 3.70 ± 0.42 μM and 4.79 ± 1.10 μM respectively. With human liver microsomes, DDPH was a noncompetitive inhibitor of CYP2D6 (Ki = 0.85 ± 0.06 μM) and mixed inhibitor of CYP3A (Ki = 2.15 ± 0.41 μM). Further in vivo study showed that oral administration of DDPH (12.5-50 mg/kg/d) for 7 days in rats significantly increased the area under the plasma concentration-time curve (AUC) of propafenone by 25.4%-63.9%, with a concomitant decrease in the plasma clearance. In conclusion, the results indicated that DDPH inhibited CYP2D and CYP3A activities and down-regulated their protein expression and mRNA transcription. DDPH might cause metabolic drug-drug interactions through modulation of the activity and expression of CYP2D and CYP3A. This information could be important in the prediction of possible drug-drug interactions as well as for the effective therapy and the limitation of toxicity of DDPH in clinical practice.

2015-12-01·Nan fang yi ke da xue xue bao = Journal of Southern Medical University

[Comparison of cisplatin-resistant testicular cancer cell lines established by two methods].

Article

作者: Li, Beibei ; Tong, Xuhui ; Fan, Zongbing ; Dong, Shuying ; Wu, Xiaoxiang ; Wu, Jianfeng

OBJECTIVETo compare the biological behaviors of two drug-resistant testicular cancer cell lines established by different methods.METHODSDrug-resistance was induced in testicular cancer cell lines exposure of the cells to increasing concentrations of or a high dose of cisplatin (I-10/DDPi and I-10/DDPh cell lines, respectively). The morphological characteristics of the two cell lines were observed microscopically. The resistance index of the cells was determined with MTT assay, and the cell growth curves were drawn. The cellular expression of resistance-associated proteins MDR1 and P-gp was detected by Western blotting. The cell invasion ability was assessed with Transwell assay.RESULTSNormal testicular cancer cell line I-10 and the two resistant cell lines all showed an adherent growth pattern. Compared with I-10 cells, I-10/DDP cells exhibited slightly heterogenous cell sizes, irregular shapes, the presence of microvilli tentacles on the cell surface, and a scattered arrangement. The cisplatin resistance index of I-10/DDPi and I-10/DDPh cells were 3.924 and 3.099, respectively. Compared with I-10, the drug-resistant cell lines showed extended doubling time with increased expressions of MDR1 and P-gp and increased cell invasiveness, which was especially obvious in I-10/DDPi cells.CONCLUSIONBoth increasing dose exposure and high-dose exposure to cisplatin can induce cisplatin resistance in testicular cancer cells, and the resistant cells established by the latter method better mimics clinical drug-resistant tumor cells.

100 项与盐酸非洛普相关的药物交易

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