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Coniferyl ferulate,isolated from Radix Angelicae sinensis,reverses multidrug resistance via strong inhibition of GST and down-regulation of P-glycoprotein

中药与天然药高峰论坛暨第十二届全国中药和天然药物学术研讨会

作者： Chang Chen~1 Xinhua Lu~2 Zhiyong Yan~3 shaojing li~1 1 institute of chinese materia medica China Academy of chinese medical Sciences Beijing 100700 China 2 New Drug Research and Development Centre of North China Pharmaceutical Group Corporation Hebei 050015 China 3 College of life science and engineering Southwest Jiaotong University Chengdu 610031 China institute of chinese materia medica China Academy of Chinese Medical Sciences Beijing 100700China New Drug Research and Development Centre of North China Pharmaceutical Group Corporation Hebei 0500 College of life science and engineering Southwest Jiaotong University Chengdu 610031 China

P-glycoprotein(P-gp)and glutathione-S-transferase(GST)are key players in multidrug resistance(MDR).Inhibition of the expression of P-gp and/or GST has emerged as a promising therapeutic strategy fo

关键词： coniferyl ferulate Radix Angelicae sinensis (Umbelliferae) multidrug resistance glutathione-S-transferase

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Coniferyl ferulate,isolated from Radix Angelicae sinensis,re...

Synthesis of three new Schizandrin Analogues

中药与天然药高峰论坛暨第十二届全国中药和天然药物学术研讨会

作者： Chang Chen~1,Xinhua Lu~2,Zhiyong Yan~3,shaojing li~1 1 institute of chinese materia medica,China Academy of chinese medical Sciences,Beijing 100700, China 2 New Drug Research and Development Centre of North China Pharmaceutical Group Corporation, Hebei,050015,China 3 College of life science and engineering,Southwest Jiaotong University,Chengdu 610031,China

P-glycoprotein(P-gp)and glutathione-S-transferase(GST)are key players in multidrug resistance(MDR).Inhibition of the expression of P-gp and/or GST has emerged as a promising therapeutic strategy for the reversal of *** ferulate(CF),isolated from Radix Angelicae sinensis(RAS),strongly inhibited human placental *** 50%inhibition concentration (IC50)was 0.3μM,which is greater than an known GST p1-1 inhibitor,ethacrynic acid(EA), using the established HTS *** analysis and computational docking were used to examine the mechanism of inhibition by *** and the expression of P-gp mRNA were evaluated in the MDR positive B-MD-C1(ADR+/+)cell line to investigate the MDR reversal effect of *** results demonstrated dual inhibition of both P-gp expression and GST activity by CF in a concentration-dependent ***,RAS may be a potential source of MDR reversing agents for pharmaceutical use.

关键词： coniferyl ferulate Radix Angelicae sinensis(Umbelliferae) multidrug resistance glutathione-S-transferase

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chinese Chemical Letters 1998年第7期9卷 631-634页

作者： Lan XIE Jing Xi XIE(institute of materia medica, chinese Academy of medical Sciences 1 Xian Nong Tan Street, Beijing 100050) chinese Acad Med Sci Inst Mat Med Beijing 100050 Peoples R China

Three new Schizandrin analogues with dibenzocycloheptatriene skeletons have been synthesized. Their structures were identified by MS, UV, IR and NMR spectral data.

关键词： schizandrin analogues

Puerarin reduces increased c-fos, c-jun, and type Ⅳ collagen expression caused by high glucose in glomerular mesangial cells

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Acta Pharmacologica Sinica 2005年第8期26卷 982-986页

作者： Cai-ping MAO, Zhen-lun GU~1 Department of Pharmacology, Suzhou institute of chinese materia medica, medical College of Soochow University Suzhou 215007, China Department of Pharmacology Suzhou Institute of Chinese Materia Medica Medical College of Soochow University Suzhou China

Aim: Increased expression of c-fos, c-jun and type Ⅳ collagen (CoⅣ) in glomerular mesangial cells (GMC) are important characteristics of diabetic nephropathy. Both c-los and c-jun regulate the gene expression of extracellular matrix components, and CoⅣ is the main component of the extracellular matrix. It has been reported that puerarin inhibits aggregation of the extracellular matrix in diabetic rats by an as yet unknown mechanism. The aim of this study is to investigate the effect of puerarin on c-fos, c-jun and CoⅣ expression in GMC cultured in medium containing 5.6 or 27.8 mmol/L glucose. Methods: The expressions of c-fos and c-jun were measured at the protein level using flow cytometry. CoⅣ content was detected using radioimmunoassay. Protein kinase C (PKC) activity was measured using liquid scintillation counting. Results: Puerarin (10-5mmol/L) significantly ameliorated the high-glucose effect on c-fos, c-jun and CoⅣ expression. This effect is accompanied by a reduced PKC activity in these cells. Coclusion: Our results suggest that reduced PKC activity and expression of c-fos and c-jun in GMC might participate in the mechanisms underlying the therapeutic effect of puerarin on diabetic nephropathy.

关键词： puerarin glomerular mesangial cells extracellular matrix diabetic nephropathy

IDENTIFICATION OF A METABOliTE OF BIPHENYLDIMETHYLDICARBOXYLE IN HUMAN URINE

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chinese Chemical Letters 1996年第4期7卷 345-346页

作者： Ya Wei li Xiu Yuan ZHU(institute of materia medica, chinese Academy of medical SciencesBeijing 100050) institute of materia medica Chinese Academy of Medical Sciences Beijing 100050

The metabolism of biphenyldimethyldicarboxylate (BDD), an antihepatitis drug, was studied in human urine by deuterium labeled compound and GC-MS. It was found that the metabolite is mono-O-demethylated BDD, which conf...

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A Pair of Dimeric Stilbene Epimers from Gnetum Montanum

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chinese Chemical Letters 1998年第11期9卷 0-0,0页

作者： Hao CHEN Mao liN (institute of materia medica, chinese Academy of medical Sciences and Peking Union medical College, 1 Xian Nong Tan Street, Beijing 100050) chinese Acad Med Sci Inst Mat Med Beijing 100050 Peoples R China Peking Union Med Coll Beijing 100050 Peoples R China

A pair of dimeric stilbenes, gnetifolin M and gnetifolin N were isolated from the lianas of Gnetum montanum. All attempts to separate them by HPLC were unsuccessful. Their str-uctures were elucidated by the spectrosco... 详细信息

关键词： Gnetum montanum, gnetacea, stilbene gnetifolins M, N.

Overcoming multidrug resistance(MDR) in cancer by nanotechnology

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Science China Chemistry 2010年第11期53卷 2226-2232页

作者： BU HuiHui,GAO Yu & li YaPing Shanghai institute of materia medica,chinese Academy of Sciences,Shanghai 201203,China 1. Shanghai institute of materia medica Chinese Academy of Sciences Shanghai 201203 China

The emerging nanotechnology-based drug delivery holds tremendous potential to deliver chemotherapeutic drugs for treatment of multidrug resistance(MDR) *** drug delivery system could improve the pharmacokinetic behavior of antitumor drugs,deliver chemotherapeutic drugs to target sites,control release of drugs,and reduce the systemic toxicity of drugs in MDR *** review addresses the use of nanotechnology to overcome MDR classified on the bases of the fundamental mechanisms of MDR and various approaches to deliver drugs for treatment of MDR cancer.

关键词： nanotechnology nanoparticles multidrug resistance chemotherapeutic drugs cancer drug delivery system

STRUCTURE　ELUCIDATION　AND　SYNTHESIS　OF　CONISEliN　FROM　CONISEliUM　VAGINATUM　THELL

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chinese Chemical Letters 1995年第1期6卷 41-44页

作者： Ping Yu DING Ruo Yun CHEN De Duan YU institute of materia medica, chinese Academy of medical Sciences, Beijing1 00050 chinese Acad Med Sci Inst Mat Med Beijing 100050 Peoples R China

Coniselin, a new natural compound, was isolated from the roots of Coniselium Vaginatum *** structure was elucidated by means of spectroscopic analysis (UV, IR, MS, NMR, DEPT) and confirmed by total synthesis.

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Functional analysis of transcriptional regulation of herpes simplex virus type 1 tegument protein VP22

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Science China(life Sciences) 2008年第11期51卷 966-972页

作者： YU Xian1,2, li WeiZhong1, liU LongDing1, CHE YanChun1, CUN Wei1, WU WenJuan1, HE ChunYan1, SHAO CongWen1 & li QiHan1 1 Department of Viral Immunology, institute of medical Biology, chinese Academy of medical Sciences and Peking Union medical College, Kunming 650118, China 2 institute of materia medica, North Sichuan medical College, Nanchong 637007, China 1. Department of Viral Immunology Institute of Medical Biology Chinese Academy of Medical Sciences and Peking Union Medical College Kunming 650118 China 2. institute of materia medica North Sichuan Medical College Nanchong 637007 China

The herpes simplex virus type 1 (HSV-1) tegument proteins have important functions in the viral repli- cation process. In order to investigate the role of the HSV-1 tegument protein VP22 in viral replication, its transcriptional regulation of viral promoters was investigated using the chloramphenicol acetyl- transferase (CAT) assay. The results indicate that VP22 exerts a dose-dependent transcriptional in- hibitory effect on the HSV-1 α4, TK, and gC gene promoters. VP22 had the capacity to repress tran- scriptional activation of promoters via different viral transcription regulatory factors such as VP16 and ICP0, as evidenced by the specific repression of the TK and gC gene promoters by ICP0. In addition, VP22 was capable of inhibiting the promotion of ICP0 transcriptional activation in the presence of HAT PCAF, which is even more remarkable than the VP22 repression of ICP0 transcriptional activation. Fi- nally, the transcriptional inhibitory effect of VP22 on other viral promoters was demonstrated by the analysis of β-galactosidase activities in internal controls.

关键词： herpes simplex virus type 1 tegument VP22 transcriptional regulation

Injury of Mouse Brain Mitochondria Induced by Cigarette Smoke Extract and Effect of Vitamin C on It in vitro

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Biomedical and Environmental Sciences 2003年第3期16卷 256-266页

作者： YU-MEI YANG AND GENG-TAO liUDivision of Pharmacology, institute of materia medica, chinese Academy of medical Sciences, Peking Union medical College, 1 Xian Nong Tan Street, Beijing 100050, China Division of Pharmacology Institute of Materia Medica Chinese Academy of Medical Sciences Peking Union Medical College 1 Xian Nong Tan Street Beijing 100050 Chin

Objective To investigate the toxicity of cigarette smoke extract (CSE) and nicotine on mouse brain mitochondria as well as the protective effect of vitamin C in vitro. Method Mouse brain mitochondria in vitro was incubated with CSE or nicotine in the absence or presence of vitamin C for 60 minutes, and the changes of mitochondrial function and structure were measured. Results CSE inhibited mitochondrial ATPase and cytochrome C oxidase activities in a dose-dependent manner. However, no significant changes in the peroxidation indices were observed when mitochondrial respiratory enzymes activity was inhibited, and protection of mitochondria from CSE-induced injury by vitamin C was not displayed in vitro. The effect of CSE on mouse brain mitochondria swelling response to calcium stimulation was dependent on calcium concentrations. CSE inhibited swelling of mitochondria at 6.5μmol/L Ca2+, but promoted swelling response at 250μmol/L Ca2+. Nicotine, the major component of cigarette smoke, showed no significant damage in mouse brain mitochondria in vitro. The CSE treatment induced mitochondrial inner membrane damage and vacuolization of the matrix, whereas the outer mitochondrial membrane appeared to be preserved. Conclusion The toxic effect of CSE on brain mitochondria may be due to its direct action on enzymatic activity rather than through oxygen free radical injury. Nicotine is not the responsible component for the toxicity of CSE to brain mitochondria.

关键词： Cigarette smoke extract Nicotine Vitamin C Mitochondrial function Mitochondria! structure