Yaoxue Xuebao Pub Date : 2017-01-01

Le-le Ding, Zhen-hao Tian, Jie Hou, Zi-miao Weng, Jing-nan Cui, Ling Yang, Guang-bo Ge

{"title":"[Design and development of fluorescent probe substrates for carboxylesterase 1 using BODIPY as the basic fluorophore].","authors":"Le-le Ding, Zhen-hao Tian, Jie Hou, Zi-miao Weng, Jing-nan Cui, Ling Yang, Guang-bo Ge","doi":"","DOIUrl":"","url":null,"abstract":"Carboxylesterase 1 (CE1) is an important serine hydrolase in mammals, which involved in the hydrolysis of a variety of compounds (endogenous substrates like cholesterol and xenobiotic compounds like ester-contain drugs and pesticides). This study aimed to design and develop the fluorescent probe substrates for human carboxylesterase 1 (hCE1), on the basis of the structural features of hCE1 preferred substrates. Four carboxylic esters deriving from BODIPY-8-carboxylic acid were designed and synthesized. After then, reaction phenotyping assays and chemical inhibition assays were used to evaluate the selectivity of these four ester derivatives towards hCE1. Our results clearly demonstrated that the substrate specificity of these ester substrates towards hCE1 would be improved with the decrease of the alcohol group on BODIPY-8-carboxylesters, while BODIPY-8-carboxylesters with small alcohol groups including methyl (BCM) and ethyl (BCE) esters could serve as the ideal probe substrates for hCE1. Given that BCM exhibit rapid hydrolytic rate in hCE1, we further investigate the enzymatic kinetics of this fluorescent probe substrate in both human liver microsomes (HLM) and recombinant hCE1, as well as to explore its potential application in high-throughput screening of hCE1 inhibitors by using HLM as enzyme source. The results showed that the kinetic behaviors and the affinity of BCM in HLM is much closed to those in recombinant hCE1, implying that hCE1 played the key roles in BCM hydrolysis in HLM. Furthermore, the inhibition study demonstrated that BCM could be used for rapid screening and characterization of hCE1 inhibitors, by using HLM to replace recombinant hCE1 as enzyme source.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"52 1","pages":"58-65"},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36231434","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

[Research progress of human cytochrome P450 2J2 and its ligands]. [人细胞色素P450 2J2及其配体研究进展]。

Yaoxue Xuebao Pub Date : 2017-01-01

Hong-ying Ma, Jing Ning, Guang-bo Ge, Ling Yang, Da-cheng Hao

引用次数: 0

[Personalized dosing from perspective of pharmacogenomics of drug metabolizing enzymes and transporters]. [从药物代谢酶和转运体的药物基因组学角度看个体化给药]。

Yaoxue Xuebao Pub Date : 2017-01-01

Quan Zhou, Lu-shan Yu, Su Zeng

引用次数: 0

[Research in rheological properties of four types of ophthalmic preparations]. 四种眼科制剂流变学特性的研究

Yaoxue Xuebao Pub Date : 2017-01-01

Xiao-luan Wu, Jian-fang Ma, Xiao-yu Fan, Lin-bo Wang, Xing-sheng Peng

{"title":"[Research in rheological properties of four types of ophthalmic preparations].","authors":"Xiao-luan Wu, Jian-fang Ma, Xiao-yu Fan, Lin-bo Wang, Xing-sheng Peng","doi":"","DOIUrl":"","url":null,"abstract":"This study is prepared to provide the basis of rheological parameters for the additional quality standard of ophthalmic gels, the rheological properties of the ophthalmic gels and the other three types of ophthalmic preparations. The medicines were compared through the study of the rheological properties for four types of ophthalmic preparations. The cone-plate rheometer was used to determine the dynamic and steady rheological parameters of four types of ophthalmic preparations. The similarities and differences of the measured results were analyzed to summarize the rheological indexes and parameters which are applied to distinguish the ophthalmic gels and the other types of ophthalmic preparations. 1 The elastic modulus should be greater than the viscous modulus for the ophthalmic gels in the range of the linear viscoelastic region. 2 The ophthalmic gels should be shear thinning non-Newtonian fluid with a certain yield stress and thixotropy. 3 The dynamic viscosity of the ophthalmic gels should be greater than 0.5 Pa·S at the temperature of 25 ℃ with the 50 s-1 shear rate. The typical rheological indexes and parameters of the ophthalmic gels were proposed in this article. The determination methods are simple and feasible. The rheological indexes and parameters have an important significance in the prescription design, production technology and quality control of the ophthalmic gels.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"52 1","pages":"146-52"},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36231655","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

[Study of cancer cell apoptosis induced by Schizonepeta tenuifolia with microfluidic chip technology]. [微流控芯片技术研究荆芥诱导癌细胞凋亡]。

Yaoxue Xuebao Pub Date : 2017-01-01

Jia-xin Fan, Shuai Wang, Xian-sheng Meng, Yong-rui Bao, Tian-jiao Li

引用次数: 0

[Regulatory mechanisms of gut microbiota on intestinal CYP3A and P-glycoprotein in rats with dextran sulfate sodium-induced colitis]. [肠道菌群对葡聚糖硫酸钠性结肠炎大鼠肠道CYP3A和p糖蛋白的调节机制]。

Yaoxue Xuebao Pub Date : 2017-01-01

Xue-jiao Gao, Ting Li, Bin Wei, Zhi-xiang Yan, Ru Yan

{"title":"[Regulatory mechanisms of gut microbiota on intestinal CYP3A and P-glycoprotein in rats with dextran sulfate sodium-induced colitis].","authors":"Xue-jiao Gao, Ting Li, Bin Wei, Zhi-xiang Yan, Ru Yan","doi":"","DOIUrl":"","url":null,"abstract":"As important constituents of the first-line of host defense barrier, intestinal cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp) play important roles in disease pathogenesis as well as drug absorption and exposure. Clinical reports and experimental data revealed diminished intestinal CYP3 A and P-gp expression accompanying with gut dysbiosis in inflammatory bowel disease. Yet whether gut dysbiosis is associated with the down-regulation of CYP3A and P-gp and the underlying mechanisms are unclear. In this study, daily administration of fresh feces from normal rats and rats with ulcerative colitis (UC) induced by dextran sulfate sodium to normal rats resulted in alterations of gut bacterial compositions. Intestinal CYP3A2 and P-gp were significantly down-regulated in rats receiving UC feces. Outer-membrane vesicles (OMVs) are nano-scale special buds of the outer membrane which are produced by Gram-negative bacteria and mediate diverse functions including interactions within bacterial communities and communications with host. Expressions of CYP3A4 and P-gp m RNA were diminished in human epithelial colorectal adenocarcinoma cells (Caco-2) treated by OMVs from all different groups with OMVs from UC rats or rats receiving UC feces showing more significant effects. Moreover, the OMVs fractions within 30 000–50 000 Daltons from both normal and UC rats elicited more effects than fractions of other molecular weights. Treatment of Caco-2 cells with toll like receptor 4 (TLR4) inhibitor resatorvid (TAK-242) or TLR4 silence RNA (siRNA) blocked CYP3A4 and P-gp down-regulation induced by bacterial OMVs. Taken together, we proved in this study that gut microbiota can down-regulate intestinal CYP3A and P-gp partially through producing OMVs to activate the TLR4 signaling pathway.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"52 1","pages":"34-43"},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36231589","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

[Construction of serum-resistant cationic polymer α-CD-PAMAM and evaluation of its performances as gene delivery vector]. [抗血清阳离子聚合物α-CD-PAMAM的构建及其基因传递载体性能评价]。

Yaoxue Xuebao Pub Date : 2017-01-01

Ling-hao Qin, Duan-wen Cao, Shi-rong Pan, Jian-hai Chen

{"title":"[Construction of serum-resistant cationic polymer α-CD-PAMAM and evaluation of its performances as gene delivery vector].","authors":"Ling-hao Qin, Duan-wen Cao, Shi-rong Pan, Jian-hai Chen","doi":"","DOIUrl":"","url":null,"abstract":"Polyamidoamine (PAMAM) dendrimers as synthetic gene vectors are efficient gene delivery systems. In this study, a kind of α-cyclodextrin-PAMAM conjugates polymer (Cy D-G1) was synthesized as a gene delivery vector. Based on ~1H NMR detectation, about 6.4 PAMAM-G1 molecules was grafted onto an α-CD core. Agarose gel electrophoresis revealed that Cy D-G1 could efficiently bind with DNA to condense them into nano-scale particles, which showed a similar binding capacity of PEI-25 K. Besides, it could protect DNA from DNase I degradation in a low N/P ratio. When N/P ratio in the CyD-G1/DNA polyplex was 40, the average particle size of CyD-G1/DNA polyplex was about 120 nm, and zeta potential was +21 mV. This polyplex could maintain its particle size in serum-containing solution within 360 min. In comparison with PEI-25 K carrier, CyD-G1 showed low cytotoxicity in various cell lines. Cell transfection results showed that CyD-G1 efficiently delivered DNA into cells at N/P = 80 compared with Lipofectamine 2000 and PEI-25 K. Unlike Lipofectamine 2000 and PEI-25 K, in serum-containing test condition, CyD-G1/DNA polyplex could maintain the transgene activities. The results of confocal laser scanning microscopy indicated that most DNA entered into cell nuclei within 4 h, and this phenomenon was consistent with the results calculated by flow cytometry. Taken together, CyD-G1 showed good transgene activities and the gene delivery vector could be used not only in vitro but also in vivo.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"52 1","pages":"139-45"},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36231653","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

[Recent advances in study of long β(2)-adrenoceptor agonist]. [长β(2)-肾上腺素能受体激动剂研究进展]。

Yaoxue Xuebao Pub Date : 2016-12-01

Xin-yue Ge, Yong-mei Mo, Li Pan, Mao-sheng Cheng

引用次数: 0

[Apoptosis of human hepatocellular carcinoma HepG-2 cells upon inhibition of STAT3 by 5,2’,4’-trihydroxy-6,7,5’-trimethoxy flavone nanoparticle]. [5,2 '，4 ' -三羟基-6,7,5 ' -三甲氧基黄酮纳米颗粒抑制STAT3对人肝癌HepG-2细胞凋亡的影响]。

Yaoxue Xuebao Pub Date : 2016-12-01

Bin Xiao, Xuan Zhang, Mei-lan Zhang, Xue-wu Zhang

引用次数: 0

[Determination of hepatic and small intestinal distribution of lignans of Wuzhi tablet in rats by liquid chromatography tandem mass spectrometry method]. [液相色谱串联质谱法测定五脂片木脂素在大鼠肝脏和小肠中的分布]。

Yaoxue Xuebao Pub Date : 2016-12-01

Xiao-ling Qin, Wen-hai Duan, Hai-fan Wang, Ying Wang, Xiao Chen, Min Huang, Hui-chang Bi

{"title":"[Determination of hepatic and small intestinal distribution of lignans of Wuzhi tablet in rats by liquid chromatography tandem mass spectrometry method].","authors":"Xiao-ling Qin, Wen-hai Duan, Hai-fan Wang, Ying Wang, Xiao Chen, Min Huang, Hui-chang Bi","doi":"","DOIUrl":"","url":null,"abstract":"This study was aimed to determine the hepatic and small intestinal distribution of active lignans in rats after treated with Wuzhi tablet (WZ, Schisandra sphenanthera extract) by LC-MS/MS method. Male Sprague-Dawley rats were sacrificed at 0.25, 1.5, 4, 6, 10, 24 h after an oral administration of WZ, and then hepatic and small intestinal samples were collected for analysis. The results showed that concentrations of lignans in liver and small intestine of rats were decreased with WZ pretreated time. The concentrations of all lignans in rat liver and small intestine at 0.25 h were the highest after a single oral administration. All lignans was undetectable in all tissues 24 h after oral dosing, suggesting lignans of WZ were eliminated rapidly in rats. The concentrations of schisandrin A, schisandrol B and schisantherin A in small intestine were much higher than those in the liver, suggesting the effect of WZ on the intestinal metabolism enzyme might be more potent than that on the liver. In short, the current results suggest that lignans of WZ were not accumulated in rat liver and small intestine. The concentrations of lignans of WZ in small intestine were much higher than those in liver.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"51 12","pages":"1891-6"},"PeriodicalIF":0.0,"publicationDate":"2016-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36228351","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

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