Guangdong Pharmaceutical College

Guangzhou, China

Guangdong Pharmaceutical College

Guangzhou, China
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Zhao M.,Guangdong Pharmaceutical College | Chen J.,Guangdong Pharmaceutical College | Zheng Y.,Guangdong Pharmaceutical College | Yang H.,Guangdong Pharmaceutical College
Journal of China Pharmaceutical University | Year: 2014

To investigate the inhibitory effect of Genistein(Gen) on Aβ25-35-induced neurotoxicity and to elucidate the underlying mechanism in cultured rat pheochromocytoma(PC12) cells. The injured PC12 cells were treated with Gen and its antagonist, Myr. The influence on the expression of Bcl-2 and Bax mRNA levels was detected by RT-PCR. Cell viability was assessed by staining with Hoechst 33342/PI. Protein kinase C(PKC) activity was measured with the intervention of Gen and PKC inhibitor(Myr). The results showed that Gen could increase the Bcl-2 expression, decrease the Bax expression, increase the ratio of Bcl-2/Bax, and significantly increase cell viability, as well as the activity of PKC in Aβ25-35-treated PC12 cells. Myr, a PKC inhibitor, partially blocked the activation effect of Gen. Gen exerted protective effect on Aβ25-35-induced neurotoxicity via activating the PKC signaling pathway, which further regulated the Bcl-2/Bax expression.

Tang L.,University of Illinois at Urbana - Champaign | Yang X.,University of Illinois at Urbana - Champaign | Yin Q.,University of Illinois at Urbana - Champaign | Cai K.,University of Illinois at Urbana - Champaign | And 14 more authors.
Proceedings of the National Academy of Sciences of the United States of America | Year: 2014

Nanomedicines (NMs) offer new solutions for cancer diagnosis and therapy. However, extension of progression-free interval and overall survival time achieved by Food and Drug Administration-approved NMs remain modest. To develop next generation NMs to achieve superior anticancer activities, it is crucial to investigate and understand the correlation between the physicochemical properties of NMs (particle size in particular) and their interactions with biological systems to establish criteria for NM optimization. Here, we systematically evaluated the size-dependent biological profiles of three monodisperse drug-silica nanoconjugates (NCs; 20, 50, and 200 nm) through both experiments and mathematical modeling and aimed to identify the optimal size for the most effective anticancer drug delivery. Among the three NCs investigated, the 50-nm NC shows the highest tumor tissue retention integrated over time, which is the collective outcome of deep tumor tissue penetration and efficient cancer cell internalization as well as slow tumor clearance, and thus, the highest efficacy against both primary and metastatic tumors in vivo.

Fang D.Q.,Guangzhou Medical College | Wu W.J.,Guangdong Pharmaceutical College | Zhang R.,Guangdong Pharmaceutical College | Zeng G.H.,Guangdong Pharmaceutical College | Zheng K.C.,Sun Yat Sen University
Chemical Biology and Drug Design | Year: 2012

A theoretical study on the two-dimensional, three-dimensional quantitative structure-activity relationships and docking analysis of a novel series of ethynyl-3-quinolinecarbonitriles acting as Src inhibitors has been carried out. To correlate the c-Src kinase-inhibition activity of these compounds with the two-dimensional and three-dimensional structural properties for 39 known compounds, some excellent quantitative structure-activity relationships models with satisfying internal and external predictive abilities were established. A combined method of the density functional theory, molecular mechanics and statistics as well as the comparative molecular field analysis was applied to develop two-dimensional- and three-dimensional-quantitative structure-activity relationship models. The leave-one-out cross-validation q 2 values of two-dimensional-quantitative structure-activity relationship and comparative molecular field analysis models are 0.834 and 0.812, respectively. The predictive abilities of these models were further validated by the test set including 10 compounds, and the predicted IC 50 values were in a good agreement with the experimental ones. The appropriate binding orientations and conformations of these compounds interacting with c-Src kinase were also revealed by the docking study. Based on two-dimensional- and three-dimensional-quantitative structure-activity relationship results along with docking analysis, some important factors responsible for inhibitory activity of this series of compounds were discussed in detail. These factors can be summarized as follows: selecting certain large-size substituent R 2, increasing the negative charge of the first atom of substituent R 1 and the net charge of the C 15 atom on ring-C will enhance the activity. Meanwhile, the interaction information between protein and ligand was also revealed in detail. These results help to understand the action mechanism and designing novel potential Src inhibitors. Based on the established models and some designing considerations, three new compounds with rather high predicted Src-inhibitory activity have been theoretically designed and presented to experimenters for reference. © 2012 John Wiley & Sons A/S.

Zhao H.,Guangdong Pharmaceutical College | Zha L.,Jiangxi Normal University | Cai M.,Jiangxi Normal University
Reaction Kinetics, Mechanisms and Catalysis | Year: 2010

An MCM-41-supported mercapto rhodium complex [MCM-41-SH-Rh] was conveniently synthesized from commercially available and cheap c-mercaptopropyltriethoxysilane via immobilization on MCM-41, followed by reacting with rhodium chloride. It was found that the title complex is an efficient catalyst for the hydrosilylation reaction of olefins with triethoxysilane and can be reused several times without noticeable loss of activity. © Akadémiai Kiadó, Budapest, Hungary 2010.

Zhao H.,Jiangxi Normal University | Zhao H.,Guangdong Pharmaceutical College | Zheng G.,Jiangxi Normal University | Hao W.,Jiangxi Normal University | Cai M.,Jiangxi Normal University
Applied Organometallic Chemistry | Year: 2010

The Stille cross-coupling reaction of organostannanes with aryl halides was achieved in the presence of a catalytic amount of MCM-41-supported mercapto palladium(O) complex (1 mol%) in DMF-H2O (9:1) under air atmosphere in good to high yields. This MCM-41-supported palladium catalyst can be reused at least 10 times without any decrease in activity. Copyright © 2009 John Wiley & Sons, Ltd.

Long R.T.,Southern Medical University | Zeng W.S.,Southern Medical University | Chen L.Y.,Southern Medical University | Guo J.,Guangdong Pharmaceutical College | And 3 more authors.
International Journal of Obesity | Year: 2010

Introduction:Oxyntomodulin (OXM) is a gut hormone released from intestinal L cell. Synthetic OXM and its analog reduce food intake and body weight in both rodents and human beings by being administered intravenously. However, people find intravenous administration difficult because of its side effects and inconvenience. The aim of this study is to develop a novel oral delivery system for OXM and its analog using genetically engineered Bifidobacterium as the carrier.Methods:An OXM gene expression vector pBBADs-OXM for the Bifidobacterium genus was constructed. Human OXM sequence was fused with extracellular exo-xylanase (XynF) signal peptide (Xs) from Bifidobacterium longum under the control of the pBAD promoter. B. longum NCC2705 was transformed with the recombinant plasmid pBBADs-OXM by electroporation, and the transformed B. longum was selected using MRS plates containing 60 g ml-1 ampicillin. The OXM expression in vitro was identified by western blot and enzyme-linked immunosorbent assay (ELISA) assay after L-arabinose induction. Overweight BALB/c mice were treated with B. longum transformed with OXM after 0.2% L-arabinose induction every day for 4 weeks to investigate the effects of OXM-transformed B. longum on food intake and body weight by oral administration. The B. longum transformed with the green fluorescent protein (GFP) gene was used as negative control; orlistat, a gastrointestinal lipase inhibitor, was used as positive control; Normal saline (NS, 0.9% saline) was used as blank control. The food intakes of each group were measured every day, and body weights were measured once a week. Normal BALB/c (2 months old) mice were treated with OXM-transformed B. longum after induction by intragastric administration every day for 6 days to reveal the mechanism of transformed B. longum, with OXM exerting its biological function by oral administration. Plasma OXM, plasma ghrelin and the OXM of intestinal contents were detected by the ELISA method. Plasma glucose and triglyceride levels were analyzed using the Automatic Biochemistry Analyzer.Results:Transformed B. longum with OXM was selected and identified without biological and morphological alteration. An approximately 4-5 kDa OXM peptide was detected in both the supernatant and the cell pellet of transformed B. longum after L-arabinose induction in vitro. The food intake, body weight and blood triglyceride level of overweight mice treated with OXM-transformed B. longum were all significantly reduced compared with that of the GFP negative control group and NS control group (P>0.01). Interestingly, the plasma triglyceride level of the GFP group was significantly decreased compared with that of the NS control group (P0.01). The OXM level in the intestinal contents of the OXM group was significantly increased compared with that of the GFP negative control group and the NS group (P0.05). The plasma ghrelin level of the OXM group was significantly decreased compared with that of the GFP and NS groups (P>0.01). Unexpectedly, the ghrelin level of the GFP group was significantly increased compared with that of the NS control group (P>0.01).Conclusion:A novel oral delivery system of Bifidobacterium for human OXM has been successfully established. The expression of recombinant OXM can be detected in the supernatant and cell pellet of transformed B. longum. OXM-transformed B. longum reduces food intake, body weight and plasma lipid level in overweight mice by oral administration. © 2010 Macmillan Publishers Limited All rights reserved.

Wang Y.N.,Guangdong Pharmaceutical College
Zhong yao cai = Zhongyaocai = Journal of Chinese medicinal materials | Year: 2012

To investigate the chemical constituents from the whole herbs of Anoectochilus chapaensis. The chemical constituents were isolated and purified by repeated column chromatographies with silica gel, Sephadex LH-20 and preparative TLC. Their structures were identified by their physiochemical property and spectral data. 6 compounds were isolated and elucidated as follows: (1) Friedelin, (2) Sorghumol, (3) 5alpha, 8alpha-epidioxyergost-22-en-3beta-ol, (4) Stearic acid, (5) Octadecane and (6) Epifriedelanol. Compound (1), (2) and (4) are isolated from this plant for the first time, and compound (3), (5) and (6) are isolated from genera Anoectochilus for the first time.

Yan Y.S.,Guangdong Pharmaceutical College
Zhong yao cai = Zhongyaocai = Journal of Chinese medicinal materials | Year: 2012

To study the changes of volatile oil from different compatibility of Guizhi decoction and explore their connection. The volatile oil of Cinnamomum cassia and different compatibility of Guizhi decoction extracted by steam distillation were analyzed by GC-MS. The main components of volatile oil in Cinnamomum cassia were found in different compatibility of Guizhi decoction and they accounted the most amount of total volatile oil,but the contents of the main components were decreased, there were more components existed in different compatibility of Guizhi decoction than those in Cinnamomum cassia, the new components came from Zingiber officinale mostly. GC-MS can be used to reflect the changes of volatile oil from different compatibility of Guizhi decoction, and the result will provide some evidence for the research of regular pattern of compatibility in Guizhi decoction.

Yan Y.S.,Guangdong Pharmaceutical College
Zhong yao cai = Zhongyaocai = Journal of Chinese medicinal materials | Year: 2012

To study the optimum extraction process of total flavonoids from Psoralea coryl folia by cellulose-assisted technique. Based on single-factor experiments, the effects of pH value, temperature of enzymatic hydrolysis, time of enzymatic hydrolysis and enzyme amount on the extraction yields of total flavonoids from Psoralea corylifolia were studied by response surface methodology. The optimum enzyme-assisted extraction process was: pH value 4.9, temperature 46 degrees C, time 150 min and enzyme amount 7.2 mg/g,under this condition,the relative error of the observed and predicted values was 1.16%. The optimum enzyme-assisted extraction process is simple and feasible, the extraction rate of total flavonoids increases by 28% compared with ultrasonic extraction, so it can be used to extract total flavonoids from Psoralea corylifolia.

Zhang H.W.,Guangdong Pharmaceutical College | Li K.,Guangdong Pharmaceutical College | Liang Z.X.,Guangdong Pharmaceutical College | Wang F.Y.,Guangdong Pharmaceutical College | Lu Q.W.,Guangdong Pharmaceutical College
Chinese Chemical Letters | Year: 2012

A monolithic polymer column with mixed-mode interaction was prepared by in situ polymerization in a 1000 μL pipette. Two kinds of monomers, butyl methacrylate (BMA) and 2-(dimethylamino)ethyl methacrylate (DMAM) were applied to constructing the mixed-mode interaction of monolithic polymer column. Its solid-phase extraction properties for liquiritigenin (LQG) were evaluated by high performance liquid chromatography (HPLC) with a gradient elution procedure. After the extraction procedure was optimized, the maximum binding capacity and extraction recovery following the optimal extraction procedure were investigated. Calibration curve was expressed as A = 65.9C + 4.53 (r 2 = 0.998) with a linear range of 0.151-1.80 μg/mL. The experimental results indicate that the monolithic polymer pipette presents good extraction efficiency for LQG. It can be envisaged that the developed monolithic polymer pipette possesses the potential for its application to the enrichment of other flavonoids compounds being similar to the structure of LQG. © 2012 Kang Li.

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