Yaoxue Xuebao Pub Date : 2016-12-01

Yu-zhen Hu, Miao Li, Tong-tong Zhang, Yi-guang Jin

{"title":"[Preparation of liposomal artesunate dry powder inhalers and the effect on the acute lung injury of rats].","authors":"Yu-zhen Hu, Miao Li, Tong-tong Zhang, Yi-guang Jin","doi":"","DOIUrl":"","url":null,"abstract":"Artesunate is one of artemisinin derivatives with anti-malarial and anti-inflammatory activities though its water solubility and bioavailability are low. Acute lung injury (ALI) is a seriously dispersive lung disease with a high mortality. In this study, artesunate liposomes were prepared with the film dispersion method, and then lyophilized to obtain the liposomal artesunate dry powder inhalers(LADPIs). The LADPIs were pulmonary-delivered into the lung to treat ALI in rats. The artesunate liposomes had the capsulation efficiency of 71.4%, the particle size of 47.3 nm, and the zeta potential of -13.7 m V. The LADPIs had the aerodynamic particle size of 4.2 μm and the fine particle fraction (FPF) of 34.5%. ALI was established in rats by instilling lipopolysaccharide (LPS) into the lungs. The rats quickly showed a reduction in movement and acceleration in breath followed by diarrhea and so on. The LADPIs were directly administrated into the lungs of ALI rats through airways after 1 h of LPS challenge. The treatment induced a reduction in ALI syndromes. Two inflammatory factors, including TNF-α and IL-6, were significantly reduced by the artesunate powder in the LADPI group similarly to the reduction in the positive drug dexamethasone group (P < 0.05). Therefore, the anti-inflammatory effect of LADPIs contributed to the anti-ALI activity. Furthermore, the liposomal formulation improved drug bioavailability in the lung and increased therapeutic efficiency. The LADPIs are promising medicines for therapy of ALI through local drug administration.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"51 12","pages":"1906-12"},"PeriodicalIF":0.0,"publicationDate":"2016-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36241360","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

[Characterization of the size variants of a recombinant humanized monoclonal antibody (rhumAb1)]. [重组人源化单克隆抗体(rhumAb1)大小变异的表征]。

Yaoxue Xuebao Pub Date : 2016-12-01

Jian Zhao, Wu Zhen-hua, Ming Lü, Zhi-dan Wu, Xiao Liu, Hong-hong Guo, Jin Chen, Xin-qiu Yuan, Li Chen, Bei-fen Shen, Bo-yan Zhang

{"title":"[Characterization of the size variants of a recombinant humanized monoclonal antibody (rhumAb1)].","authors":"Jian Zhao, Wu Zhen-hua, Ming Lü, Zhi-dan Wu, Xiao Liu, Hong-hong Guo, Jin Chen, Xin-qiu Yuan, Li Chen, Bei-fen Shen, Bo-yan Zhang","doi":"","DOIUrl":"","url":null,"abstract":"The composition and potency of the high temperature (40 ℃) stress induced size variants of a recombinant humanized monoclonal antibody(rhumAb1) were characterized by means of SEC-HPLC, non- reduced CE-SDS, liquid chromatography coupled with mass spectrometry (LC-MS) and antibody dependent cell-mediated cytotoxicity (ADCC) assay. The molecular masses of the four size variants (SEC-1-SEC-4) separated by SEC-HPLC and seven size variants(NR-1-NR-7) detected by non-reduced CE-SDS were all characterized by LC-MS. The major low molecular weight variants were generated due to the hinge region fragmentation of heavy chain. The hinge region cleavage was found mainly in the Ser221-Cys-Asp-Lys-Thr- His-Thr-Cys228 sequence, in which C222-D223 and H226-T227 were the major cleavage sites. The size variants of rhumAb1, namely dimer and fragments, have significantly reduced ADCC activity in comparison with the intact rhumAb1 drug product. This study provided insights into the stability profiling for rhumAb1 drug product. The study protocols presented here may be applicable to the analytical characterization of other monoclonal antibody-based therapeutic products.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"51 12","pages":"1897-905"},"PeriodicalIF":0.0,"publicationDate":"2016-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36241358","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

[A new phenylacetamide from the seeds of Lepidium apetalum Willd]. [从无瓣Lepidium aptalum wild种子中提取的一种新的苯乙酰胺]。

Yaoxue Xuebao Pub Date : 2016-12-01

Li Meng, Xiao-ke Zheng, Zhi-guang Zhang, Jing-ke Zhang, Xuan Zhao, Yan-yun Yang, Xiao-lan Wang, Hai-xue Kuang, Wei-sheng Feng

引用次数: 0

[The in vitro inhibition and induction of cytochrome P450 activities by bentysrepinine: a novel candidate of anti-hepatitis B virus drug]. [一种新的抗乙型肝炎病毒候选药物——苯替利平体外抑制和诱导细胞色素P450活性]。

Yaoxue Xuebao Pub Date : 2016-12-01

Hui-rong Fan, Xiao-yan Ci, Wei Li, Shi-qi Dong, Yong Zeng, Xiu-lin Yi, Duan-yun Si, Chang-xiao Liu

{"title":"[The in vitro inhibition and induction of cytochrome P450 activities by bentysrepinine: a novel candidate of anti-hepatitis B virus drug].","authors":"Hui-rong Fan, Xiao-yan Ci, Wei Li, Shi-qi Dong, Yong Zeng, Xiu-lin Yi, Duan-yun Si, Chang-xiao Liu","doi":"","DOIUrl":"","url":null,"abstract":"Bentysrepinine (Y101), a derivative of phenyalanine dipeptide, has a novel mechanism in the treatment of hepatitis B virus (HBV) infection with a good anti-HBV effect. In the present study, a fluorometric-based high throughput method using cytochrome P450 (CYP) screening kit was adopted to evaluate in vitro inhibition potential of Y101 on CYP isoenzymes by calculating remaining enzyme activities and inhibitory potential (IC(50) values) using the determined values of fluorescence intensity. The result showed that Y101 exhibited little activity in the inhibition of CYP1A2, CYP3A4, CYP2C9, CYP2C19 and CYP2D6 (IC(50) > 100 μmol·L(-1)). Y101 was used to treat human primary hepotocytes for 72 h, and the enzyme activities of CYP1A2, CYP2B6 and CYP3A4 were determined with a cocktail of probe substrates for the three CYP isoforms. The metabolites were simultaneously determined using a LC-MS/MS method. Y101 had no activity in the induction of CYP1A2, CYP2B6 and CYP3A4 on the basis of the following results: 1 The ratio of enzyme activities between test and control groups were all below than 1 (varied from 0.662 to 0.928); 2 The induction potential of Y101 were lower than forty percent compared with that of positive groups. The above results suggest that Y101 has little activity in the regulation of metabolic drug-drug interactions based on the CYP isoform changes following co-administration of drugs.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"51 12","pages":"1864-70"},"PeriodicalIF":0.0,"publicationDate":"2016-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36228347","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 anti-tumor activity of ciprofloxacin-histone deacetylase inhibitor conjugates]. 环丙沙星-组蛋白去乙酰化酶抑制剂偶联物的合成及抗肿瘤活性研究。

Yaoxue Xuebao Pub Date : 2016-12-01

Ting Pei, Fang Liu, Ai-ping Deng

引用次数: 0

[The drug development based on sphingosine-1-phosphate signaling pathway]. [基于鞘氨醇-1-磷酸信号通路的药物开发]。

Yaoxue Xuebao Pub Date : 2016-12-01

Jie Bai, Jin-ping Hu

引用次数: 0

[Effect and mechanism of miR-206/miR-613 on expression of OATP1B1]. [miR-206/miR-613对OATP1B1表达的影响及机制]。

Yaoxue Xuebao Pub Date : 2016-12-01

Yun Rao, Gao-feng Jin, Ming-yi Liu, Xin-hua Li, Hong Zhang, Chun-hua Xia, Yu-qing Xiong

{"title":"[Effect and mechanism of miR-206/miR-613 on expression of OATP1B1].","authors":"Yun Rao, Gao-feng Jin, Ming-yi Liu, Xin-hua Li, Hong Zhang, Chun-hua Xia, Yu-qing Xiong","doi":"","DOIUrl":"","url":null,"abstract":"This study was designed to explore the effect and mechanism of miR-206/miR-613 on the expression of OATP1B1 gene. Bioinformatic analysis was used to predict the potential miRNAs target sites in 3’-untranslated region (3’-UTR) of OATP1B1 mRNA. The expression level of miR-206/miR-613 and OATP1B1 mRNA and protein was determined with RT-qPCR and Western blot, respectively. Luciferase assay was used to explore the exact mechanism of the effect of miR-206/miR-613 on the expression of OATP1B1 mRNA and protein. The results showed that the seed sequences of miR-206/miR-613 has perfect complementary with 3’-UTR of OATP1B1 mRNA in terms of sequence specificity. The secondary structure between miR-206/ miR-613 and 3’-UTR of OATP1B1 mRNA was rather stable. The OATP1B1 protein level was down-regulated by 24.7%, 38.8% by overexpression of miR-206/miR-613. The expression was up-regulated by 25%, 38.2% by inhibition of miR-206/miR-613. However, overexpression or inhibition of miR-206/miR-613 had no effect on the expression of OATP1B1 mRNA. The luciferase activity of p MIR/OATP1B1-WT luciferase reporter gene was decreased by 35% and 30% through overexpression of miR-206/miR-613. The expression was increased by 33.1% and 32.5% through inhibition of miR-206/miR-613. When the binding sites in the 3’-UTR of OATP1B1 mRNA complementary with miR-206/miR-613 was mutated, overexpression or inhibition of miR-206/miR-613 had no effect on the luciferase activity. Collectively, miR-206/miR-613 post-transcriptionally regulates the expression of OATP1B1 protein by directly targeting the 3’-UTR of OATP1B1 mRNA.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"51 12","pages":"1858-63"},"PeriodicalIF":0.0,"publicationDate":"2016-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36228346","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

[Overexpression of NtPMT and HnH6H changed hyoscyamine-rich Atropa belladonna to scopolamine-rich varieties]. [NtPMT和HnH6H的过表达使富含莨菪碱的颠茄变成富含东莨菪碱的品种]。

Yaoxue Xuebao Pub Date : 2016-12-01

Hong Quan, Ke Xia, Jun-lan Zeng, Min Chen, Xiao-zhong Lan, Zhi-hua Liao

{"title":"[Overexpression of NtPMT and HnH6H changed hyoscyamine-rich Atropa belladonna to scopolamine-rich varieties].","authors":"Hong Quan, Ke Xia, Jun-lan Zeng, Min Chen, Xiao-zhong Lan, Zhi-hua Liao","doi":"","DOIUrl":"","url":null,"abstract":"Atropa belladonna L. is the commercial plant material for production of tropane alkaloids, including hyoscyamine and scopolamine. The wild-type Atropa belladonna is characterized by the hyoscyamine-rich chemotype, in which the hyoscyamine content is much higher than the scopolamine content. It is the common goal for the pharmaceutical industry to increase the content of scopolamine in A. belladonna. Based on the T0 progeny of transgenic A. belladonna with NtPMT and HnH6H overexpression, T1 progeny of transgenic A. belladonna were obtained through self-pollination and used in a field trial. The 461 bp fragment of NtPMT and the 1 077 bpHnH6 H were simultaneously expressed from T1 progeny of transgenic A. belladonna, but were not obtained from the wild-type A. belladonna. At the transcription level, the expression of NtPMT and HnH6H were detected in T1 progeny of transgenic A. belladonna, but were not detected in the wild-type plants. Further, the alkaloids were analyzed by HPLC. In the stems and leaves of T1 progeny of transgenic A. belladonna, hyoscyamine was not detected and scopolamine was detected at very high levels; in the stems and leaves of wild-type A. belladonna, hyoscyamine was detected at much higher levels. In the leaves of T1 progeny of transgenic A. belladonna, the content of scopolamine was 15-36 folds higher than that of wild- type leaves; in the stems of T1 progeny of transgenic A. belladonna, the scopolamine content was 37-108 folds higher than that of wild-type stems. In conclusion, overexpression of NtPMT and HnH6H greatly enhanced conversion of hyoscyamine into high-value scopolamine and improved the commercial value of A. belladonna.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"51 12","pages":"1913-9"},"PeriodicalIF":0.0,"publicationDate":"2016-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36241361","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

[Operational models of allosteric modulation of G protein-coupled receptors]. G蛋白偶联受体变构调节的操作模型。

Yaoxue Xuebao Pub Date : 2016-12-01

Hao Gong, Shuo Zhang, Richard Dequan Ye

引用次数: 0

[Determination of anaprazole in human plasma by LC-MS/MS in pharmacokinetic study]. [LC-MS/MS法测定人血浆中阿纳拉唑的药代动力学研究]。

Yaoxue Xuebao Pub Date : 2016-12-01

Dong-xia Cheng, Xiao-jian Dai, Yi-fan Zhang, Yong-qian Wu, Chong-tie Shi, Xi-feng Ma, Jin Li, Xiao-yan Chen, Da-fang Zhong

引用次数: 0

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