Yaoxue Xuebao Pub Date : 2017-02-01

Shuai Chen, Yuan-yuan Xia, Guang-li Wei, Quan-sheng Li, Meng-jie Liu, Yong Chen, Duan-yun Si

{"title":"[Simultaneous determination of salidroside and tyrosol in Beagle dog plasma using UHPLC-MS/MS after pre-column dansyl chloride derivatization].","authors":"Shuai Chen, Yuan-yuan Xia, Guang-li Wei, Quan-sheng Li, Meng-jie Liu, Yong Chen, Duan-yun Si","doi":"","DOIUrl":"","url":null,"abstract":"A pre-column derivatization method combined with UHPLC-MS/MS was developed for the\u0000simultaneous determination of salidroside and tyrosol in Beagle dog plasma. After protein precipitation by\u0000acetonitrile, the liquid supernatant was treated with dansyl chloride under dark conditions at 60 ℃ for 30 min,\u0000and then, the sample solution was extracted using methyl tertiary butyl ether. The multiple reaction monitoring\u0000in positive ion mode was used for MS detection of the tested analytes with the specific ion transitions of\u0000m/z 534.2→372.0 for salidroside derivative, m/z 372.0→171.0 for tyrosol derivative and m/z 506.0→171.0 for\u0000arbutin derivative. The chromatograph separation was achieved on an ACQUITY UPLC® BEH C18 column\u0000(100 mm × 2.1 mm, 1.7 μm) with a gradient mobile phase consisting of acetonitrile (0.1% formic acid)-water\u0000(10% acetonitrile, 0.1% formic acid) for 9 min. The assay showed a good linearity over the range of 0.02/0.1 −\u000020/10 μmol·L−1 with a lower limit of quantitation of 0.02 and 0.1 μmol·L−1 for salidroside and tyrosol in dog\u0000plasma, respectively. The intra- and inter-day precisions were all less than 8.68%, and the accuracy was within\u0000±11.4%. The established method with a high sensitivity, good specificity and reliability was appropriate for\u0000simultaneous determination of salidroside and tyrosol in dog plasma and successfully applied to a pharmacokinetic\u0000study after intragastric administration of salidroside to Beagle dogs.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"52 2","pages":"296-301"},"PeriodicalIF":0.0,"publicationDate":"2017-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36289261","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

[Prevention of abdominal adhesions in rats by rhynchophylline through inhibition of Smad singnaling pathway]. [通过抑制Smad信号通路预防大鼠腹腔粘连]。

Yaoxue Xuebao Pub Date : 2017-02-01

Yu Song, Hui Zhang, Rui-li Liu, Guang-fan Hai, Tong Wang, Jia-xin Yue, Wei-li Zhang, Yu-ke Ren

引用次数: 0

[Change of hepatic drug metabolism enzymes in rat depression model with kidney-yang deficiency]. [肾阳虚抑郁模型大鼠肝脏药物代谢酶的变化]。

Yaoxue Xuebao Pub Date : 2017-02-01

Shu-fen He, Wen-zheng Ju, Hao-bin Hu, Li-jing Zhu, Qian Zhang, Guo-liang Dai

引用次数: 0

[Protective effect and underlying mechanism of cordycepin on non-alcoholic fatty liver in ob/ob mice]. [冬虫夏草对ob/ob小鼠非酒精性脂肪肝的保护作用及机制]。

Yaoxue Xuebao Pub Date : 2017-01-01

Li-ping Zhong, Jin Li, Feng-zhong Wang, Hai-bo Zhu, Xu-jie Hou

{"title":"[Protective effect and underlying mechanism of cordycepin on non-alcoholic fatty liver in ob/ob mice].","authors":"Li-ping Zhong, Jin Li, Feng-zhong Wang, Hai-bo Zhu, Xu-jie Hou","doi":"","DOIUrl":"","url":null,"abstract":"This study is designed to investigate the protective effect and mechanism of cordycepin on non- alcoholic fatty liver in ob/ob mice. Twelve-week-old male ob/ob mice were divided into 5 groups according to their body weight and blood glucose, and C57BL/6J mice were used in the control group. The animals were orally administered with cordycepin for 7 weeks. Body weight and food intake were measured once a week. Blood were collected from ophthalmic venous and biochemical indexes were determined at the 2nd and 4th week. Insulin tolerance test was performed at the 5th week. After 7 weeks of administration, liver tissues were collected to determine the contents of triglycerides and total cholesterol, and pro-inflammatory cytokines. Liver histology was performed by hematoxylin-eosin and oil-red O staining. Total RNA were extracted from liver tissues and the levels of lipid metabolism-related and inflammation-related genes were detected by real time PCR. Cordycepin effectively reduced the blood lipids level and improved liver function. Nevertheless, it did not improve insulin resistance in ob/ob mice. Cordycepin significantly reduced the contents of triglycerides and cholesterol, and the levels of pro-inflammatory cytokines in liver tissues. Moreover, cordycepin remarkably suppressed the expression of genes related to lipids synthesis and inflammation. These results indicate that cordycepin may improve non-alcoholic fatty liver in ob/ob mice, and the underlying mechanism may be associated with decreased expression of genes related to lipids synthesis and inflammation.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"52 1","pages":"106-12"},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36230622","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

[Synthesis and antifungal activities of N-1,3,4-thiadiazol-2-yl-4-oxo-thiochroman-2-yl-formamide derivatives]. [n- 1,3,4-噻二唑-2-酰基-4-氧-硫代铬-2-酰基甲酰胺衍生物的合成及抑菌活性]。

Yaoxue Xuebao Pub Date : 2017-01-01

Xiao-yan Han, Sheng-bin Li, Guo-chao Liang, Guan Zhou, Yi-fan Zhong, Hui Qi, Ya-li Song, Xiao-qiang Qiao

{"title":"[Synthesis and antifungal activities of N-1,3,4-thiadiazol-2-yl-4-oxo-thiochroman-2-yl-formamide derivatives].","authors":"Xiao-yan Han, Sheng-bin Li, Guo-chao Liang, Guan Zhou, Yi-fan Zhong, Hui Qi, Ya-li Song, Xiao-qiang Qiao","doi":"","DOIUrl":"","url":null,"abstract":"Thiochromanones and 1,3,4-thiadiazoles as heterocyclic compounds have broad biological activities. In order to find novel compounds with antifungal bioactivity, substituted thiophenol and maleic anhydride were used to synthesize the intermediate 4-oxothiochromane-2-carboxylic acid. It was reacted with 2-amino-1,3,4-thiadiazole to get fourteen target compounds containing 1,3,4-thiadiazole moiety. The structures of the obtained compounds were confirmed by 1H NMR, 13C NMR and HR-MS. All compounds were investigated for antifungal activity via microdilution broth method. The results showed that the target compounds 3a and 3c to Epidermophyton floccosum and Mucor racemosus exhibited better antifungal activity than the positive control fluconazole, in which the minimum inhibition concentration can reach 8 μg·mL−1 and 16 μg·mL−1. Compound 3e showed significant inhibitory activity to Helminthosporium maydis, Sclerotinia sclerotiorum and Botrytis cinerea compared with that of the positive control carbendazim. Compound 3b exhibited inhibitory activity to Helminthosporium maydis better than the positive control carbendazim.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"52 1","pages":"113-9"},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36230626","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

[Induction study of CYP3A2 in male rats by zolmitriptan]. [佐米曲坦诱导雄性大鼠CYP3A2的研究]。

Yaoxue Xuebao Pub Date : 2017-01-01

Kun Han, Si-jie Lu, Su Zeng, Lu-shan Yu

{"title":"[Induction study of CYP3A2 in male rats by zolmitriptan].","authors":"Kun Han, Si-jie Lu, Su Zeng, Lu-shan Yu","doi":"","DOIUrl":"","url":null,"abstract":"In our preliminary studies, we observed zolmitriptan (ZOL) treatment led to induction of CYP3A2 in male not female rats. To figure out the reason is of great significance for drug-drug interactions and personalized administration. Since growth hormone (GH) is known as the major mechanistic determinant of sexually-dimorphic gene expression like CYP3A2 in rat liver, the impacts of ZOL on both plasma GH levels in non monosodium glutamate (MSG)-treated rats and CYP3A2 expression in GH depleted MSG-treated rats were studied. ZOL was shown to partially suppress GH levels in both genders. Furthermore, CYP3A2 protein and mRNA level declined in male not female MSG-treated rats. In order to study the possible molecular events involved in the depression of GH and gender-selective induction on rat CYP3A2 by ZOL, the mRNA and protein level(whole protein and nuclear protein) of hepatocyte nuclear factor 4α (HNF4α) was investigated. Nuclear accumulation of HNF4α was observed in the normal male not female rat liver tissue following ZOL treatment. However, this kind of nuclear translocation did not occur in rat hepatocytes and MSG-treated rats. These findings demonstrated CYP3A2 inducibility by ZOL was gender-selective. GH and HNF4α may play an important role in CYP3A2 induction.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"52 1","pages":"44-50"},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36230946","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

[Update on immune and metabolic dysregulation in major depressive disorder and the implications for drug intervention]. [重性抑郁症免疫和代谢失调的最新进展及其对药物干预的影响]。

Yaoxue Xuebao Pub Date : 2017-01-01

Xiao Zheng, Guang-ji Wang, Hai-ping Hao

引用次数: 0

[On the molecular drug design from viewpoint of precision medicine]. 精准医学视角下的分子药物设计

Yaoxue Xuebao Pub Date : 2017-01-01

Zong-ru Guo

{"title":"[On the molecular drug design from viewpoint of precision medicine].","authors":"Zong-ru Guo","doi":"","DOIUrl":"","url":null,"abstract":"Precision medicine (PM) involves the application of \"omics\" analysis and system biology to analyze the cause of disease at the molecular level for targeted treatments of individual patient. Based on the targeted treatment PM is closely related to pharmaceuticals, which, as a therapeutic means and supply front, mainly embody the two aspects: drug discovery/development, and clinical administration. Innovation of new molecular entities with safety and specific efficacy is the prerequisite and guarantee for the PM practice; on the other hand, the outcome and clues in clinical PM feedback to new drug research. PM and drug research/application are interdependent and promote each other. Aimed at precision medicine, drug discovery and development involve well-known contents: the discovery and validation of targets, the association between target functions and indications (proof of concept), lead discovery and optimization, the association between preclinical investigations and clinical trials, the lean of industrialization and pharmacoeconomics. At the molecular level the therapeutic efficacy originates from the interactive binding between specific atoms or groups of the drug molecule and the complementary atoms or groups of the macromolecular target in three-dimensional space. The strict arrangement of such critical atoms, groups, or fragments reflect specific features for a precise binding to the corresponding target. An alteration of amino acid residues in mutational targets leads to the change in conformation of the target protein, and an accurate structure of drug is necessary for binding to the mutant species and avoiding off-targeting effect. For the tailoring of clinical treatment to the individual patient design and development of various new molecular entities are critical for treatment choice according to the molecular features of biological markers of patients. This article provides some examples and methods of drug design and development in the new period.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"52 1","pages":"71-9"},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36229798","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

[Evaluation of genetic diversity and population structure of genus Tripterygium based on SSR markers]. 基于SSR标记的雷公藤属遗传多样性及群体结构评价

Yaoxue Xuebao Pub Date : 2017-01-01

Na Li, Yuan-yuan Yao, Yi-long Chen, Xu-ming Liang, Ding-ding Zheng, Xiao-mei Zhang, Da-jian Yang

{"title":"[Evaluation of genetic diversity and population structure of genus Tripterygium based on SSR markers].","authors":"Na Li, Yuan-yuan Yao, Yi-long Chen, Xu-ming Liang, Ding-ding Zheng, Xiao-mei Zhang, Da-jian Yang","doi":"","DOIUrl":"","url":null,"abstract":"The genus Tripterygium is an immune suppressor in the Chinese traditional medicines. Due to the habitat destruction and anthropogenic over-exploitation, the wild genus Tripterygium plants have decreased dramatically in recent years or even been endangered. It is critical to evaluate and protect genus Tripterygium wild resource. In this research, simple sequence repeat (SSR) molecular markers were applied to the investigation of the genetic diversity and genetic structure of 28 populations for genus Tripterygium (396 samples from 9 provinces in China). We found a high level of genetic diversity (percentage of polymorphic loci PPL = 77.29%, Shannon’s information index I = 0.639 4; Nei’s expected heterozygosity H = 0.359 9) and high genetic differentiation among the populations (gene flow N_m = 0.228 7). Based on Nei’s genetic distance, the phylogenic tree of populations was constructed and 28 populations were divided into 6 clusters according to STRUCTURE clustering analysis. T. hypoglaucumwas was mainly divided into 3 clusters, including Sichuan, Yunnan and Guizhou- Chongqing. T. regelii was separated to cluster 4, while T. wilfordii was divided into two clusters: the transition type LQ and NY were divided into cluster 5, and the others were in cluster 6. These results provide a theory basis for the conservation of wild resource, research of genetic polymorphism and molecular marker for assisted breeding of genus Tripterygium.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"52 1","pages":"153-61"},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36231640","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

[Design, synthesis, and biological evaluation of phenylpropenamides compounds as anti-platelet aggregation]. [苯丙酰胺抗血小板聚集化合物的设计、合成和生物学评价]。

Yaoxue Xuebao Pub Date : 2017-01-01

Yu Yang, Jian Zuo, Jia-ming Li, Xiao-dong Ma, Yan-chun Zhang, Wei-jun Huang

引用次数: 0

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