Full-Text Search:
Home|Journal Papers|About CNKI|User Service|FAQ|Contact Us|中文
《Journal of Changsha Medical University》 2015-01
Add to Favorite Get Latest Update

Absorption mechanism of SM-1:a procaspase-3-activated anti-tumor agent

TANG Jing;LUO Li-na;ZHANG Hai-long;ZHENG Zhi-nan;ZHANG Jie;LI Su;HE Hua;DING Jin-song;  
Objective:Aim To study absorption characteristics of SM-1,a novel anti- tumor agent,to provide a research basis for the druggability evaluation of SM-1 and formulation design. Methods:Caco-2 cell monolayer model and in situ singlepass intestinal perfusion rat model were used to study the absorption characteristics of SM-1,and the absorption of SM-1 in vivo was evaluated through absolute bioavailability study in rats. Results:The results of cell monolayer model showed that cumulative absorption and efflux of SM-1 increased linearly with concentration(10~40mg·L-1). There were no significant differences in Papp with different concentrations(P 0.05). SM-1 was absorbed mainly through passive diffusion. The intestinal perfusion results showed that Ka and Peff of SM-1 had no significant differences(P0.05),when the concentrations ranged from 25 to 100 mg·L-1. SM-1 entered the systemic circulation mainly via on passive diffusion,indicating it is a compound with high permeability. The absorption of SM-1 in duodenum was superior toother intestinal segments(P0.05),there were no significant differences in the jejunum,ileum and colon(P0.05). The absolute bioavailability of SM-1 in rats was 29.3%. Conclusion:The membrane permeability of SM-1 is high and it can be absorbed by intestine well. The absorption mechanism of SM-1 is passive diffusion,and it possibly escapes from the efflux transporter protein. The absolute bioavailability of SM-1 in rats is low.
【Fund】: 国家“十二五”重大科技专项(No2012ZX09103101-051)
【CateGory Index】: R966
Download(CAJ format) Download(PDF format)
CAJViewer7.0 supports all the CNKI file formats; AdobeReader only supports the PDF format.
【Citations】
Chinese Journal Full-text Database 4 Hits
1 GUAN Su, CHEN Xiao1, HUANG Min (Institute of Clinical Pharmacology, Sun Yat-sen University, 1Dept of Pharmacy, the First Affiliated Hospital, Sun Yat-sen University, Guangzhou 510080);Caco-2 cell model——an effective tool for the research of drug absorption[J];Chinese Pharmacological Bulletin;2004-06
2 WANG Lai-you1,BI Hui-chang2,ZHOU Hong-bo3,WANG Su-jun1(1.School of Pharmacy,Guangdong Pharmaceutical University,Guangzhou 510006,China;2.Institute of Clinical Pharmacology,School of Pharmaceutical Sciences,Sun Yat-sen University,Guangzhou 510080,China;3.Experimental Center,Guangdong Pharmaceutical University,Guangzhou 510006,China);Absorption mechanism of Xanthotoxin in small intestine[J];Chinese Pharmacological Bulletin;2009-02
3 SONG Li, ZHANG Ning, XU De-sheng(Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China);Absorption mechanism of paeoniflorin across Caco-2 monolayer model[J];Chinese Traditional and Herbal Drugs;2008-01
4 NIE Shu-fang,PAN Wei-san,YANG Xing-gang,LIU Hong-fei,LIU Zhi-dong(Department of Pharmaceutics,Shenyang Pharmaceutical University,Shenyang 110016,China);Evaluation of gravimetry in the rat single-pass intestinal perfusion technique[J];Chinese New Drugs Journal;2005-10
【Co-citations】
Chinese Journal Full-text Database 10 Hits
1 MU Yongping,WU Gang,QIAO Xiuwen,ZHOU Lishe,HE Yanling(Department of Biochemistry and Molecular Biology,Research Center of Biology and Medicine,Research Institute of Trace Element in Organism,Baotou Medical College,Baotou 014010,China);The Transport and Absorption of Chiral Metal Domplexes d,l-[Ni(phen)_3]~(2+) across the Model of Caco-2 Cell Monolayers[J];Journal of Baotou Medical College;2006-04
2 ZHAO Xiao-xu1,LI Jiang-ying2,CUI Yan-tang1,SUN Zhe1,ZHANG Ya-jun1(1College of Life Sciences,Northwest University,Xi'an 710069,China;2Xi'an Hospital of Traditional Chinese Medicine,Xi'an 710001,China);Assessment of tanshinone Ⅱ_A self-microemulsifying preparation with drug release in vitro and intestinal absorption in situ[J];China Journal of Traditional Chinese Medicine and Pharmacy;2012-08
3 ZHANG Jing,XUE Liang;Intestinal absorption of Candesartan cilexetil in rats[J];Academic Journal of Second Military Medical University;2008-08
4 CHAI Yi-feng*,ZHU Zhen-yu and CHEN Xiao-fei(Department of Pharmaceutical Analysis,School of Pharmacy,Second Military Medical University,Shanghai 200433),Fenxi Shiyanshi,2010,29(9):78~122;Pharmaceutical analysis(I)[J];Chinese Journal of Analysis Laboratory;2010-09
5 MO Li-li,WANG Su-jun(School of Pharmacy,Guangdong Pharmaceutical College,Guangzhou,Guangdong 510006,China);The research progresses of oral drug absorption models[J];Journal of Guangdong Pharmaceutical College;2011-01
6 GUAN Su~1, BI Hui-chang~1, CHEN Xiao~2, HUANG Min~1 (1. Institute of Clinical Pharmacology, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510080, China; 2. Department of Pharmacy, The First Affiliated Hospital, Sun Yat-sen University, Guangzhou 510080, China);Transport mechanism of cryptotanshinone across Caco-2 monolayer model[J];The Chinese Journal of Clinical Pharmacology;2005-04
7 Zhang Xiaohua1,Chen Lixue2,Jia Yimin1△(1.Department of Pharmacy,Chongqing Institute of Tumor Research,Chongqing 400030,China;2.Laboratory Research Center,the First Affiliated Hospital of Chongqing Medical University,Chongqing 400016,China);A study of rat in situ intestinal absorption of propranolol hydrochloride through single pass perfusion method[J];Chongqing Medicine;2012-36
8 WEI Peng,LIU Wei-xia,JIA Feng-lan,RUAN Ming,ZHANG Bao-xu(Department of Toxicology,School of Public Health,Peking University Health Science Center,Key Laboratory of State Administration of Traditional Chinese Medicine of Compatibility Attenuated,Beijing 100191,China);Protective effect of 8-methoxypsoralen against cocaine-induced acute hepatic injury in mice[J];China Journal of Traditional Chinese Medicine and Pharmacy;2013-03
9 LIAO Xiaohuan,WANG Junjun,HAN Fengmei,DU Peng,CHEN Yong(Hubei Province Key Laboratory of Biotechnology of Chinese Traditional Medicine,Hubei University,Wuhan 430062,China);Transport characteristics of hydrochlorothiazide in the human intestinal cell line Caco-2[J];Journal of Hubei University(Natural Science);2010-02
10 Han,Tianjiaoa,c Song,Fengruia Liu,Zhongyingb Pi,Zifeng,a Liu,Zhiqiang,a Liu,Shuyinga(a Changchun Institute of Applied Chemistry,Chinese Academy of Sciences,Changchun 130022)(b School of Pharmacy,Jilin University,Changchun 130021)(c Graduate School of the Chinese Academy of Sciences,Beijing 100039);Studies of the Intestinal Transport of the Diterpenoid Alkaloids in the Aconitum carmichaeli Combined with Different Medicinal Herbs in a Caco-2 Cell Culture System with UPLC/MS[J];Acta Chimica Sinica;2011-15
China Proceedings of conference Full-text Database 1 Hits
1 ZHU Meng-liang;LIANG Xin-li;MING Liang-shan;NI Bin;Wang Jie;LIAO Zheng-gen;ZHAO Guo-wei;Key Laboratory of Modern Preparation of TCM of Ministry of Education,Jiangxi University of TCM;;Transport characteristic of baicalin and the influence of Angelica dahurica extracts on absorption of baicalin in Caco-2 cell model[A];[C];2013
【Secondary Citations】
Chinese Journal Full-text Database 10 Hits
1 LIN Xiao, XU De-sheng, FENGYi (College of Chinese Materia Medico, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China);Advance in search for intestinal absorption and disposition of drugs[J];The Chinese Journal of Clinical Pharmacology;2004-01
2 ZHANG Li 1, CHEN Da wei 1, LI Fang jiu 2, SONG Ai hua 3, KUI Gang bo 1 (1 Department of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China; 2 The First Hospital Attached to China Medical University, Shenyang 110001, Chin;Studies on the absorption kinetics of famotidine in rats' intestines[J];Journal of Shenyang Pharmaceutical University;2001-03
3 ZHANG Xiang rong, PAN Wei san (School of Pharmacy , Shenyang Pharmaceutical University, Shenyang 110016, China);Studies on the absorptive kinetics of salvianoic acid A in rats′ small intestines in vivo[J];Journal of Shenyang Pharmaceutical University;2002-01
4 Wu Gang(Wu G),Sun Changhai(Sun CH),Wu Hongbin(Wu HB),et al(Department of Pharmaceutical Analysis,The Fifth School of Jiamusi University,Jiamusi 154003);Determination of phenol red in rat small intestine circulation solution by dual wavelength spectrophotometry[J];Chinese Journal of Modern Applied Pharmacy;2001-02
5 Chen Chonghong, Zhang Yuan, Chen Guangliang, Li Jun et al ( Institute of Clinical Pharmacology, Anhui Medical University, Hefei, 230032 );THE STUDIES ON PHARMACOKINETICS OF PAEONIFLORIN[J];Chinese Pharmacological Bulletin;1990-05
6 WANG Kun,ZHONG Lai Fu (Dalian Medical University, Dalian 116027);The intestinal cytochrome P450 3A and P-glycoprotein:barriers to drug absorption[J];Chinese Pharmacological Bulletin;2003-09
7 GUAN Su, CHEN Xiao1, HUANG Min (Institute of Clinical Pharmacology, Sun Yat-sen University, 1Dept of Pharmacy, the First Affiliated Hospital, Sun Yat-sen University, Guangzhou 510080);Caco-2 cell model——an effective tool for the research of drug absorption[J];Chinese Pharmacological Bulletin;2004-06
8 MU Yong-ping 1, WU Gang 1,2,3, ZHOU Li-she 2, HE Yan-ling 3 (1.Dept of Preclinical Medicine;2.the Research Center of Biology and Medicine, 3. the Research Institute of Trace Element in Organism, Baotou Medical College, Baotou 014010, China);Application of Caco-2 cell model in drug research[J];Chinese Pharmacological Bulletin;2005-05
9 Chen Jiyue(Chen JY), Xu Ziyou(Xu ZY) and Li Yiqi(Li YQ)(School of Pharmacy, Shanghai Medical University, Shanghai 200032);THE UPTAKE CHARACTERISTICS OF 5FLUOROURACIL IN THE CACO2 MODEL SYSTEM[J];ACTA PHARMACEUTICA SINICA;1998-03
10 LIU Lu,CUI Jing-Bin,FANG Hong-Zhuang(The first Clinical Hospital of Harbin Medical University, Heilongjiang Harbin 150001);The study on tinidazole absorption in rat small intestine[J];Chinese Journal of Hospital Pharmacy;2003-01
©2006 Tsinghua Tongfang Knowledge Network Technology Co., Ltd.(Beijing)(TTKN) All rights reserved