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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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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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Synthesis of two multivalent lactosides with anti-adhesive activity and their fluorescein-labeled and biotin-labeled derivatives

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Journal of Chinese Pharmaceutical Sciences 2011年第4期20卷 325-334页

作者：李庆赵岳涛孟祥豹严婷婷李树春黄河清赵智辉李中军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 南京师范大学江苏省分子与药物生物技术学重点实验室生命科学院江苏南京210046

Adhesion of leukocytes to endothelium plays an important role in inflammation-associated *** previous studies showed that multivalent lactosides were able to inhibit this *** 2-azide-l,3-propandiol and glutamic acid as spacers,we synthesized divalent lactoside An-2 and tetravalent lactoside Gu-4 by means of convergent *** two compounds displayed high anti-adhesive activity and showed therapeutic effect in rats with severe burn *** addition, investigation of the anti-adhesion biological mechanism using labeled compounds YAn-2 and YGu-4 demonstrated that the target of multivalent lactosides was CD11b,theβ2 integrin subunit,on the surface of *** this paper,the synthesis of these two new multivalent lactosides as well as their fluorescein-labeled and biotin-labeled compounds is reported.

关键词： Anti-adhesion Biotin Fluorescein Multivalent-lactosides Synthesis

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钒化合物促进PPARγ表达

钒化合物促进PPARγ表达

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第十一届全国生物无机化学学术会议

作者：赵攀杨晓达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大学医学部北京100191

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Drug efficacy and pharmacological action of an organoselenium compound ethaselen,a novel antitumor drug

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Journal of Chinese Pharmaceutical Sciences 2010年第3期19卷 163-168页

作者：傅佳凝王静瑜王立辉王磊唐菀晨蔡高雄刘密曾慧慧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

Ethaselen, an organoselenium compound designed and synthesized in the School of Pharmaceutical Sciences, Peking University, has been entitled to independent intellectual property rights both at home and abroad. As one of the novel antitumor drugs, ethaselen has been extensively studied in Phase I clinical trial, and its biological target is thioredoxin reductase. In this review, we focus on the ethaselen＇s efficacy and pharmacological actions, including antitumor effects both in vitro and in vivo, and immunologic functions. These research findings not only provide the theoretical basis for the anticancer study of ethaselen, but also guide the clinical trial of ethaselen.

关键词： Ethaselen Organoselenium compounds Antitumor effect Immunologic function Thioredoxin reductase

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Synthesis and anti-tumor activities of 5-carbohydrate modified cyclophosphamide derivates

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Journal of Chinese Pharmaceutical Sciences 2010年第5期19卷 327-340页

作者：郑愉孟祥豹李树春黄河清李中军李庆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

Novel prodrugs of cyclophosphamide 1a and 1b, which comprised the galactosyl moiety, the key fraction of cyclophosphamide derivates, and the linker 4-hydroxy benzaldehyde, were synthesized. These compounds were antici... 详细信息

关键词： Cyclophosphamide Galactoside Hepatocyte targeting Anti-tumor

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Modification of the alkylating agent chlorambucil with spiropiperazinium salts

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Journal of Chinese Pharmaceutical Sciences 2010年第5期19卷 346-352页

作者：李功孙崎崔景荣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

In order to improve the antitumor activity and reduce the toxicity of the alkylating agent chlorambucil, a series of spiropiperazinium salts of chlorambucil （8） were designed and synthesized. It was found that compo... 详细信息

关键词： Chlorambucil Antitumor activity Spiropiperazinium SAR

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Study on the iodination of uracil derivatives

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Journal of Chinese Pharmaceutical Sciences 2010年第2期19卷 146-150页

作者：李立覃华张亮王孝伟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

5-Iodouracil derivatives have interesting biological activities and can serve as important substrates for the metal-catalyzed cross-coupling reactions to introduce alkyl, alkenyl, and alkynyl groups to the C-5 position of uracil derivatives. In order to find a good method to iodinate directly the C-5 of uracil derivatives, we investigated three methods, which included iodine/lead （IV） dioxide, iodine/ammonium hexanitratocerate （CAN） and iodine chloride, and examined their reactivity to different types of uracil and thiouracil derivatives.

关键词： Iodination Lead （IV） dioxide Ammonium hexanitratocerate Iodine chloride Uracil 2-Thiouracil

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