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用Caco_2细胞单层模型比较两种具类胰岛素效应的氧钒配合物的小肠吸收能力

科学通报 2002年第20期47卷 1550-1555页

作者：杨晓改王夔杨晓达王夔杨晓达王夔杨晓达袁兰北京大学药学院化学生物学系北京100083 北京大学药学院天然药物及仿生药物国家重点实验室北京100083 北京大学药学院预防药物研究室北京100083 北京大学医学部分析测试中心北京100083

应用Caco-2细胞单层肠吸收模型比较了两种结构相似但降糖效应显著不同的重要氧钒配合物双乙酰丙酮氧钒（VO（acac）2）和双麦芽酚氧钒（VO（ma）2）经肠道的吸收能力.实验发现,两种钒化合物都通过被动扩散的途径转运,其表观渗透系数（... 详细信息

应用Caco-2细胞单层肠吸收模型比较了两种结构相似但降糖效应显著不同的重要氧钒配合物双乙酰丙酮氧钒（VO（acac）2）和双麦芽酚氧钒（VO（ma）2）经肠道的吸收能力.实验发现,两种钒化合物都通过被动扩散的途径转运,其表观渗透系数（顶端→底端）分别为（82.0±6.7）×10-7和（14.6± 0.7）×10-7cm·s-1;表明VO（acac）2的吸收能力远远大于VO（ma）2.这可能与化合物及其配体在转运过程中的代谢有关.吸收的差异可能导致两种化合物生物利用度的巨大差别,这可能是VO（acac）2降糖效应优于VO（ma）2的主要原因.

关键词： Caco-2细胞单层模型类胰岛素效应氧钒配合物吸收能力 ADME 肠吸收降糖作用

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Vanadyl complexes work with cinnamaldehyde in promoting cell viability under the β-amyloid burden in SH-SY5Y neural cells

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Journal of Chinese Pharmaceutical Sciences 2016年第10期25卷 754-763页

作者：李雪白力丹董雅琼常青武睿章京杨晓达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化学生物学系北京100191 北京大学医学部基础医学院病理学系北京100191 国家中医药管理局中药复方解毒重点研究室北京100027

The Alzheimer＇s disease （AD） is one of the common cognitive disorders in the elderly. AD shares some similar pathological characters with diabetes mellitus （DM）, suggesting potential application of anti-diabetic agents, such as vanadyl complexes, in therapeutic treatment of AD. In the present work, we studied the effects of vanadyl acetylacetonate （VO（acac）2） and cinnamaldehyde （CA） on an AD model based on SH-SY5Y neural cells. The experimental results showed that VO（acac）2 at sub-micromolar concentrations could improve the viability of neural cells with or without increased β-amyloid （Aβ） burden; and the combination of VO（acac）2 and CA showed an additive cell protection effects. Further investigation revealed that for SH-SY5Y neural cells, VO（acac）2 could activate PPART-AMPK signal transduction and inhibit GSK 3β, one of the major kinases for Tau hyperphosphorylation. Meanwhile, CA could correct the abnormal mitochondrial morphology due to Aβ-induced excessive mitochondrial fission, thus restoring/enhancing the mitochondrial function. In addition, both VO（acac）2 and CA decreased intracellular reactive oxygen species （ROS） level and inhibited formation of toxic Aβ oligomers. Overall, VO（acac）2 might work with CA in improving the neural cell viability under the Aβ burden, suggesting application of vanadium metallodrugs in AD treatment.

关键词： Alzheimer＇s disease β-Amyloid SH-SY5Y cells Vanadium Cinnamaldehyde

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Semi-synthesis of mangiferin-7-O-β-D-glucuronide

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Journal of Chinese Pharmaceutical Sciences 2017年第8期26卷 556-565页

作者：杨博威梁丹琳魏雄孟祥豹李中军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化学生物学系北京100191 江西师范大学国家单糖化学合成工程技术研究中心江西南昌330022

Mangiferin is a natural plant polyphenol with a structure of xanthone C-glycoside and it displays a wide spectrum of pharmacological activities. Investigation of the metabolites of mangiferin is valuable in studying the mechanisms of its various pharmacological properties and developing novel drugs from the mangiferin derivatives. Among the metabolites of mangiferin, mangiferin-7-O-β-D-glucuronide has been reported as the phase Ⅱ metabolite of mangiferin. Herein we described the first semi-synthesis of mangiferin-7-O-β-D-glucuronide with the natural product mangiferin as the starting material. In this work, we adopted several regioselective protection procedures to distinguish the different hydroxyl groups in the structure of mangiferin, and we accomplished the glycosylation under the phase-transfer catalysis conditions. In this method, we efficiently synthesized the glucuronide derivative of mangiferin in 10 steps with highly regioselective protection.

关键词： Mangiferin-7-O-β-D-glucuronide Semi-synthesis Regioselective protection Glycosylation

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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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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 evaluation of 8-deaza-5,6,7,8-tetrahydromethotrexate derivatives as dihydrofolate reductase inhibitors

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Journal of Chinese Pharmaceutical Sciences 2012年第2期21卷 142-148页

作者：田超张志丽刘俊义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

A series of N5-substituted 8-deaza-5,6,7,8-tetrahydromethotrexate derivatives were synthesized and evaluated as inhibitors of dihydrofolate reductase（DHFR）.The results indicated that modification of the pteridine ri... 详细信息

关键词： 8-Deaza-5 6 7 8-tetrahydromethotrexate Synthesis Dihydrofolate reductase inhibitory activities

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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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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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