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Effects of herbal aromatics on the permeability of MDCK-MDR1 monolayers

Journal of Chinese Pharmaceutical Sciences 2011年第6期20卷 584-589页

作者：张承悦赵攀施喆杨晓达北京大学医学部天然药物及仿生药物国家重点实验室药学院化学生物学系北京100191

inducing resuscitation with herbal aromatics is important to modulate the brain intake of drugs in traditional Chinese medicine,but limited information has been available on the mechanism of *** MDCK-MDRl monolayer is an excellent in vitro cell model to use as a tool to study blood brain barrier（BBB） *** this study,we established MDCK-MDR1 cell line by stable transfection and investigated the effects of several important herbal aromatics on BBB *** characterization experiment demonstrated the MDCK-MDRl used in this study was *** a transport study,we found several herbal aromatics increased the permeability of fluorescein isothiocyanate-labeled dextran 4kDa（FD4） and inhibited efflux of Rhodaminel23（Rhol23）.These results demonstrated that herbal aromatics enhanced the BBB permeation of drugs by both inhibition of P-gp and opening of the BBB tight junction,thus providing new insights for understanding the mechanisms of aromatic compounds＇ BBB permeability.

关键词： Herbal aromatics MDCK-MDR1 Tight junction P-gp

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Effects of Salvia miltiorrhiza injectional powder on the development of liver fibrosis initiated by dimethylnitrosamine in rats

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Journal of Chinese Pharmaceutical Sciences 2015年第1期24卷 54-62页

作者：杨莹帆孙懿赵欣郑希元蒲小平北京大学医学部药学院分子与细胞药理学系?天然药物及仿生药物国家重点实验室北京100191 北京大学医学部药学院化学生物学系北京100191

Salvia miltiorrhiza （Sm） is a traditional herbal medicine with multiple effects on various diseases. Its water-soluble parts have been used to produce injectional powder. In this study, liver fibrosis rats were induced by intraperitoneal injection of dimethylnitrosarnine for 3 consecutive days per week for 4 weeks. After 2 weeks, rats in the positive drug group were subcutaneously injected with 8×10^5 IU/kg IFNα2b, while the Sm treatment groups were intraperitoneally injected with 50, 100 and 200 mg/kg solution of Sm injectional powder, respectively, for 6 days per week for 4 weeks. The results showed that either IFNα2b or the Sm injectional powder significantly increased the body weight and liver to spleen ratio, and three doses of the powder brought down the spleen index. Serum analysis showed that both IFNα2b and the Sm powder reduced levels of alanine transaminase and total bilirubin, while only 100 and 200 mg/kg of the Sm powder ameliorated aspartate transaminase and albumin levels. In the collagen examination, reduced hyaluronic acid and procollagen type III levels, less fibrous hyperplasia and collagen deposits, and improved hepatocyte states were clearly observed in rats treated with either IFNα2b or Sm injectional powder. In addition, the mechanism of action of the Sm powder was also studied. Immunohistochemical staining showed that IFNα2b and Sm injectional powder significantly down-regulated the expression of transforming growth factor-β1 （TGF-β1） and platelet derived growth factor （PDGF）. In conclusion, Sm injectional powder has protective effects on dimethylnitrosamine-initiated liver fibrosis in rats, and the mechanism may include the down-regulation of TGF-β1 and PDGF.

关键词： Salvia miltiorrhiza Liver fibrosis Dimethylnitrosamine Transforming growth factor-β1 Platelet derived growth factor

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Detection of microRNA expressions in tissues and exfoliative cells reveals the potential role of miR-203 in oral lichen planus

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Journal of Chinese Pharmaceutical Sciences 2014年第5期23卷 279-286页

作者：冯震东史闻蔡志刚华红周德敏北京大学医学部天然药物及仿生药物国家重点实验室药学院化学生物学系北京100191 北京大学口腔医学院北京100191

Oral lichen planus （OLP） is a chronic inflammatory disorder and premalignantlesion, of which the mechanisms are still obscure. In the present study, the expression levels of miR-96/182/183 cluster, miR-203, miR-375, and miR-769-5p in both tissues and exfoliative cells of OLP patients as well as healthy volunteers were detected, differentially expressed miRNAs were identified and their correlation with OLP was evaluated by a biplot method. Experimental results show that miR-203 is significantly up-regulated in patient lesion tissues in comparison to volunteer mucosa tissues. Moreover, the contra- dictory insignificant expression changes of miR-203 as well as miR-96/182/183 cluster in comparisons of exfoliative cell samples suggest that different cell compositions in OLP lesion have distinct miRNA regulation, which accords with the histological heterogeneity of OLP. Finally, biplot analyses indicate the expression of miR-203 and miR-96/182/183 cluster are positively correlated in patient lesions. These results provide miR-203 as a molecular indicator of heterogeneity of OLP, and also a potential diagnostic biomarker or therapeutic target that deserves further studies.

关键词： Oral lichen planus microRNA RT-qPCR Biplot method miR-203

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阿尔茨海默症病理机制中的金属代谢和金属药物

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中国科学：化学 2014年第4期44卷 541-554页

作者：张悦夏青杨晓达王夔天然和仿生药物国家重点实验室北京大学医学部药学院化学生物学系北京100191

随着人口老龄化进程的发展,阿尔茨海默症(AD)已成为威胁中国和世界人口健康和经济的重大疾病.本文综述了近年来AD病理的分子机制的新进展,分析了其中金属代谢的意义.研究发现,在AD进程中,围绕淀粉样斑块(AP)和神经缠绕斑(NFT)的形成,多... 详细信息

随着人口老龄化进程的发展,阿尔茨海默症(AD)已成为威胁中国和世界人口健康和经济的重大疾病.本文综述了近年来AD病理的分子机制的新进展,分析了其中金属代谢的意义.研究发现,在AD进程中,围绕淀粉样斑块(AP)和神经缠绕斑(NFT)的形成,多因素相互联系并发挥作用,这些主要因素包括金属内稳态、胰岛素抵抗、神经炎症、线粒体和血脑屏障改变等.与AD病理过程密切相关的主要蛋白质均参与了金属元素的生理代谢过程,而细胞金属离子的内稳态失衡加剧了AD病理的恶化.金属药物在AD诊断和治疗中可能具有以下的发展潜力:(1)AD早期诊断探针;(2)调节金属内稳态的配体和/或微量元素补充;(3)抗糖尿病金属配合物;(4)神经元和血脑屏障(BBB)保护金属药物.

关键词：阿尔茨海默症金属药物金属内稳态配体疗法神经保护

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核磁共振法研究大肠杆菌细胞内La^(3+)与钙调蛋白的相互作用

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中国稀土学报 2007年第3期25卷 344-348页

作者：杨秦刘会雪李勤杨晓达王夔北京大学医学部药学院化学生物学系北京100083 北京大学医学部药学院天然药物及仿生药物国家重点实验室北京100083

应用in-cell和cell free核磁共振(NMR)方法分别研究了柠檬酸镧与大肠杆菌细胞内15N标记的钙调蛋白(CaM)以及La3+和大肠杆菌无细胞提取液(Cell free extract,CFE)的相互作用。将所得1H-15N HSQC NMR谱与纯化过的以不同组成比结合Ca/La的... 详细信息

应用in-cell和cell free核磁共振(NMR)方法分别研究了柠檬酸镧与大肠杆菌细胞内15N标记的钙调蛋白(CaM)以及La3+和大肠杆菌无细胞提取液(Cell free extract,CFE)的相互作用。将所得1H-15N HSQC NMR谱与纯化过的以不同组成比结合Ca/La的CaM的1H-15N HSQC NMR谱比较,发现在细胞内因胞内环境拥挤,蛋白运动能力下降,使CaM的NMR信号较少且峰宽增加。而柠檬酸镧可以透过细胞膜进入细胞,并与胞内的CaM结合。无细胞提取液的NMR谱显示,加镧之前细胞内CaM主要以Ca结合态存在,而加入La3+可能形成Ca2La2CaM混合金属配合物。这和无细胞的化学体系的实验结果一致。实验结果显示,细胞水平NMR方法可用于研究稀土以至其他金属配合物与细胞的相互作用如何与细胞内钙调蛋白作用,以及有关的生物功能。

关键词：钙调蛋白 La^3+ in-cellNMR 稀土

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Fragmentation patterns of novel dispirocyclopiperazinium dibromides during electrospray ionization mass spectrometry

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Journal of Chinese Pharmaceutical Sciences 2011年第1期20卷 42-46页

作者：王欣李昂王玮李润涛北京大学医学部天然药物及仿生药物国家重点实验室药学院化学生物学系北京100191

The fragmentation patterns of a series of dispirocyclopiperazinium dibromides with strong analgesic activity during positive ion electrospray ionization mass spectrometry were analyzed. The [M-Br]^＋ 2 ions showed the characteristic isotopic peaks and were assigned as the molecular ions. The loss of a 44 Dalton unit from 2 produced ion 3 [M-Br-44]^＋ and the loss of HBr from 2 formed ion 4. Besides, the carbamates 1d-1e produced extra ions [M-2Br-33]^＋. The related fragmentation mechanisms were proposed.

关键词： Mass spectrometry Dispirocyclopiperazinium dibromides Fragmentation pathway

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Enhanced antitumor effect of TM208 in combination with 5-fluorouracil in H_(22) transplanted mice

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Journal of Chinese Pharmaceutical Sciences 2011年第6期20卷 615-626页

作者：贾琳徐波郭维葛泽梅李润涛崔景荣北京大学医学部天然药物及仿生药物国家重点实验室北京100191 北京大学医学部药学院化学生物学系北京100191

4-Methylpiperazine-l-carbodithioc-acid-3-cyano-3,3-diphenylpropyl ester hydrochloride（TM208）,a newly synthesized dithiocarbamate derivative,exhibits antitumor effect in vivo with low ***,the antitumor effect of TM208 in combination with drugs in clinical use for cytotoxic chemotherapy has not been *** our study,the antitumor effects and toxicities of TM208 in combination with cisplatin（DDP）,cyclophosphamide（CTX） and 5-fluorouracil（5-Fu）,respectively,were evaluated in vivo using a transplanted solid-type hepatocarcinoma H_（22） mice *** results suggested that 5-Fu（5 mg/kg/2d） potentiated the antitumor effect of TM208（100 mg/kg/d） with significantly higher tumor inhibition rates（P0.01） and a slight elevation of toxicity;however,DDP and CTX in combination with TM208 did not exhibit similar enhanced antitumor *** further investigation,we found that the TM208 and 5-Fu combination therapy led to G_2/M cell cycle arrest of tumor cells in vivo by downregulating the protein expression of cyclin Bl,cdc2,cdk7,and upregulating the expression of p21 and *** protein expression levels of cyclin Dl and cyclin E were also downregulated in tumor cells treated with TM208 and 5-Fu,while those of cdk4 and cdk2 remained *** change of mRNA expression level of cdc2 was consistent with that of its protein in each group,while the mRNA expression of cyclin B1 remained unchanged among each *** results demonstrated the dosage regimen of TM208 for combination therapy and could serve as evidence for clinical use of TM208 as an antineoplastic drug.

关键词： Combination therapy Hepatocarcinoma H_(22) Dithiocarbamate 5-Fluorouracil Cell cycle-related proteins

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Synthesis and anti-HIV-1 activity evaluation of N-1-alkyl-5-halogeno-6-alkylamino uracils as novel non-nucleoside HIV-1 reverse transcriptase inhibitors

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Journal of Chinese Pharmaceutical Sciences 2011年第2X期20卷 146-153页

作者：闫寒王孝伟郭盈张志丽刘俊义北京大学医学部药学院化学生物学系北京100191 北京大学医学部天然药物及仿生药物国家重点实验室北京100191

N-1-alkyl-5-halogeno-6-alkylamino uracils,which are novel 1-[(2-hydroxyethoxy) methyl]-6-(phenylthio) thymine (HEPT) analogues,were synthesized as the selective and potent non-nucleoside human immunodeficiency virus(HIV)-1 reverse transcriptase *** of the compounds showed potent inhibitory activity against HIV-1 reverse *** instance,compounds 1d,1m and 1n exhibited potent anti-HTV-1 activity with the IC_(50) values of 13.3,11.7 and 3.15μM,respectively, which are comparable to that of nevirapine(IC_(50) 8.38μM).

关键词： HIV-1 reverse transcriptase Non-nucleoside reverse transcriptase inhibitors HEPT analogues

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Synthesis of 2-deoxy-2-chloro-1-amino sugars and evaluation of their cytotoxicity against cancer cells

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Journal of Chinese Pharmaceutical Sciences 2013年第2期22卷 144-147页

作者：钟鸣崔希凯孟祥豹李中军韶关大学医学院药学系广东韶关512026 北京大学医学部天然药物与仿生药物国家重点实验室药学院化学生物学系北京100191

Using the potent anticancer agent 2-deoxy-2-chloro-1-amino sugar as a lead compound, its analogs were prepared in 6 steps starting from D-glucal. The key step was the synthesis of 2-chloro-1-acetamido sugars using （COCl） 2-AgNO 3-CH 3 CN system in high yields. 2-Deoxy-2-chloro-1-amino sugars were obtained by treating the corresponding acetamido sugars with HCl in MeOH. All the compounds, including the reference compound, displayed almost no cytotoxic activity to the selected cancer cell lines.

关键词： 2-Deoxy-2-chloro-1-amino sugars Cytotoxic activity Epimer

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Study on tissue distribution of a novel organoselenium antitumor compound WBSELEN

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Journal of Chinese Pharmaceutical Sciences 2011年第6期20卷 578-583页

作者：李叶桓张国州黄荣华李冬冬罗钰杨勇吴银群刘丽慧曾慧慧北京大学医学部天然药物及仿生药物国家重点实验室药学院化学生物学系北京100191 天津国际生物医药联合研究院天津300457

A novel organoselenium compound,WB（1,2-[bis（1,2-benzisoselenazolone-3（2H）-ketone）]pentane） has indicated anti-tumor *** pharmacokinetic data has never been *** using the H22 tumor bearing mouse model,the tissue distribution of WB after single and four consecutive doses（both were 120 mg/kg/d） was *** selenium content of the tissues was used as an indicator of WB absorption,distribution and *** selenium in the heart,liver, spleen,kidneys,lungs,stomach,pancreas,brain,colon,intestine,testes,plasma,and tumor were determined by generation atomic fluorescence spectrometry（AFS）.With single or multiple oral administration of WB,the selenium content significantly increased in the liver,stomach,colon,and *** selenium content in the spleen,lungs,pancreas,testes,plasma and tumor also increased compared with the controls;but no significant changes were found in the brain and *** and its metabolites distributed predominantly in the colon,liver,stomach and intestine,which resulted in a significant increase in the selenium content in both *** was no observed significant accumulation of WB in the vital organs.

关键词： Organoselenium compound Antitumor Tissue distribution Hydride generation atomic fluorescence spectrometry

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