3.Advances and related issues in the use of in vitro methods to predict metabolic clearance rate of new drugs.
Acta Pharmaceutica Sinica 2007;42(10):1023-1028
The reasonable prediction of metabolic clearance rate from the humanized in vitro system is valuable in drug discovery, which is commonly used in the identification and optimization of compounds that mostly like to process appropriate pharmacokinetic characteristics in humans. A detailed development of the general theory and, models underlying the prediction of in vivo hepatic drug metabolism from in vitro data were presented. Furthermore, the accuracy when extrapolating from in vitro data considering the in vitro-in vivo correlation, method-logical issues and potential solutions were discussed as well. This review can give us a better insight into exploring methods whereby human clearance can be accurately predicted from in vitro data in the process of new drug development.
Animals
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Humans
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Metabolic Clearance Rate
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Microsomes, Liver
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metabolism
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Models, Biological
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Pharmaceutical Preparations
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metabolism
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Pharmacokinetics
5.Antiproliferative effect of soybean isoflavone on Bcap-37 cells and its relation with transforming growth factor β
Zhen-Zhou YANG ; Man-Tian MI ; Jun-Dong ZHU ; Qian-Yong ZHANG ; Ji-Guang XIONG
Journal of Third Military Medical University 2001;23(4):434-436
Objective To investigate the expression of TGF-β and TGF-β receptor in human breast cancer cell Bcap-37 inhibited by soybean isoflavones. Methods mRNA and protein of TGF-β1、TGF-βRⅠ in Bcap-37 cells were examined with reverse transcription ploymerase chain reaction(RT-PCR) and immunohistochemistry after cells were treated with daidein or genistein for 1-4 d.The expression of TGF-β1 and TGF-β2 was determined with TGF-β resistance test. Results The TGF-β1, TGF-β2 and TGF-β recepor increased in Bcap-37 cells at a concentration of 3×10-5 mol/L of genistein. No changes was found when treated with daidzein. Conclusion Genistein may inhibit the proliferation of Bcap-37 cells and accompany with increasing expression of TGF-β1, TGF-β2 and TGF-β receptor.
6.Alcohol consumption and drug use among middle school students aged 13-15 in 4 cities of China.
Lian QIAN ; Hou-guang YI ; Ben-chun TIAN ; Wei ZHANG ; Ji-bin ZHANG
Chinese Journal of Epidemiology 2006;27(6):483-487
OBJECTIVETo provide data on alcohol consumption and drug use among middle-school students aged 13-15 in 4 cities of China, and to provide evidence for developing intervention strategies on adolescents alcohol and drug use.
METHODSStandardized sample selection process of two-stage cluster-sampling was used in middle-school students in Beijing, Hangzhou, Wuhan and Urumchi. A self-administered questionnaire survey was conducted in Sept. 2003 and data was analyzed by Epi Info software.
RESULTSAmong 7344 students from grade 1 to 3, 36.5% had tasted while 14.4% had drunk alcohol in the past 30 days. 9.9% had experienced drunkness, 5.1% had been in trouble because of drinking, and 1.6% had ever used illegal drugs. Significant differences had been found in all the cities. Higher graders, older students and boys had higher rates of alcohol and addictive drug use than low graders, younger students and girls. 51.9% had been taught on take alcohol safety and another 27.6% on skills of rejecting alcohol, during the past school year.
CONCLUSIONSThe current situation of alcohol and addictive drug use among Chinese middle-school students aged 13-15 seemed to be quite critical, suggesting that it is necessary to carry out relevant health education in accordance with different characteristics in area, gender and age of the students.
Adolescent ; Alcohol Drinking ; epidemiology ; China ; epidemiology ; Female ; Humans ; Male ; Students ; Substance-Related Disorders ; epidemiology
7.Studies on the chemical constituents in root of Gentiana macrophylla from Shaanxi.
Qian-Liang CHEN ; Zhang-Yan SHI ; Guang-Zhong TU ; Wen-Ji SUN
China Journal of Chinese Materia Medica 2005;30(19):1519-1522
OBJECTIVETo in vestigate the constituents in root of Gentiana macrophylla.
METHODVarious column chromatographic techniques were used for isolation and purification of the principles. The structures were elucidated on the basis of spectral data (UV, IR, MS, 1H-, 13C-NMR etc.) and identified by comparing with standard substance.
RESULTEight compounds were identified. Four compounds isolated from the chloroform fraction are: 5-carboxyl-3,4-dihydrogen-1H-2-benzopyran-1-one (1), erythrocentauric acid (2), roburic acid (3), oleanolic acid (4). Water fraction gave four known secoiridoid glucosides. They were: gentiopicroside (5), swertiamarine (6), sweroside (7), 6'-O-beta-D-glucosylgentiopicroside (8).
CONCLUSION1 is a novel compound. It was named as erythrocentauric acid. 2 was isolated from genus Gentiana and 8 was isolated from G. macrophylla for the first time.
Gentiana ; chemistry ; Glucosides ; chemistry ; isolation & purification ; Iridoid Glucosides ; Iridoids ; chemistry ; isolation & purification ; Isocoumarins ; chemistry ; isolation & purification ; Molecular Structure ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry
8.High specific PCR identification of Bungarus multicinctus and its adulterants.
Cheng-qiang FENG ; Xiao-jing TANG ; Lu-qi HUANG ; Zhong-zhi QIAN ; Ji ZHANG ; Guang-hong CUI
China Journal of Chinese Materia Medica 2006;31(13):1050-1053
OBJECTIVETo develop a convenient and effective method for the identification of Bungarus multicinctus.
METHODBased on the sequence of Cyt b gene fragment of B. multicinctus and its adulterants, a pair of highly specific primer (HJL- and HJH-) were designed for distinguishing B. ulticinctus from other species of snake. To establish specific PCR reaction condition, the primers were employed to amplify the DNA templates extracted from B. multicinctus and 6 other species of snake, under different annealing temperature. Using this method, B. multicinctus was identified from 18 samples bought from many drugstores.
RESULTA 230 bp DNA fragment was amplified from B. multicinctus in PCR with annealed temperature at 67 degrees C, whereas no DNA fragment was amplified from other snake samples under the same reaction condition, B. multicinctus could be clearly distinguished from others by PCR reaction with the highly specific primers. In the present study, 18 sample, bought from different drugstores, were also identified by the highly specific PCR with the primers. The results indicated that 14 samples were B. multicinctus and the other 4 were adulterant, which was consistent with the conclusion of authentication based on morphological.
CONCLUSIONThe primers designed in the present study were highly specific for B. multicinctus.
Animals ; Base Sequence ; Bungarus ; classification ; genetics ; Cytochromes b ; genetics ; DNA ; genetics ; DNA Primers ; Drug Contamination ; Materia Medica ; Molecular Sequence Data ; Polymerase Chain Reaction ; methods ; Sequence Analysis, DNA ; Snakes ; classification ; genetics ; Species Specificity
9.Analysis on causes of death of childhood leukemia from 1981 to 2000 in the city of Tianjin.
Ke-Xin CHEN ; Guang-Lin WU ; Min HE ; Shu-Fen DONG ; Ji-Fang WANG ; Bi-Yuan QIAN
Chinese Journal of Pediatrics 2004;42(8):617-620
OBJECTIVELeukemia is a major cause of death of children in China, which accounts for 50 % of all cancers of children. Data from Tianjin Cancer Hospital was analyzed for mortality of leukemia in children under 20 years from 1981 to 2000 in the city of Tianjin.
METHODSAll physicians and medical staff of the hospitals and clinics in the registry area were responsible for filling out the report forms for every new case diagnosed as malignant tumors. Death certificates for malignant tumors have been registered at the local police station and the residential files were checked. All cancer cases with insufficient information were traced to his/her family and relevant persons worked in the clinic. Tianjin Cancer Registry Center periodically conducted an active re-checking program to review all patient records on cancers that was not registered in this period. Tumors diagnosed in this study were coded according to the International Classification of Diseases for Oncology (ICD-O). Mortality rates were calculated by age, sex and date of death.
RESULTSThe types of acute lymphoid leukemia, acute myeloid leukemia and chronic myeloid leukemia were the most common types of childhood leukemia in Tianjin, comprised 69.3%, 20.9 % and 8.0%, respectively. The mortality for childhood leukemia decreased slowly during the period of 1981 to 2000 in Tianjin. Mortality and morbidity ratios were 0.51.
CONCLUSIONCombined with characteristics of individual forms of childhood leukemia mortality, further epidemiological research is needed to prevent childhood leukemia.
Adolescent ; Cause of Death ; Child ; Child, Preschool ; China ; epidemiology ; Humans ; Infant ; Leukemia ; mortality ; Young Adult