1. Chemical constituents from rhizomes of Abacopteris penangiana
Chinese Traditional and Herbal Drugs 2010;41(12):1936-1939
Objective: To investigate the chemical constituents of Abacopteris penangiana. Methods: Compounds were separated and purified by column chromatography with silica gel, RP C18, and Sephadex LH-20. The structures of the obtained compounds were elucidated on the basis of physicochemical properties and spectroscopic methods. Results: Seven compounds were purified and their structures were identified as: (7′Z)-3-O-(3, 4-dihydroxy phenylethenyl)-caffeic acid (1), cafeicin B (2), matteucinol (3), protocatechuin acid (4), p-methoxybenzoic acid (5), β-sitosterol (6), and β-daucosterol (7). Conclusion: Compound 1 is a new compound named abacopteric acid, and compounds 2-7 are isolated from the plant for the first time.
2.Relationship between paraquat tissue content and organ injury in paraquat poisoning rats.
Bo ZHAO ; Xiang-dong JIA ; Zhong-chen ZHANG
Chinese Journal of Industrial Hygiene and Occupational Diseases 2010;28(3):220-223
Animals
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Brain
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pathology
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Hydroxyproline
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metabolism
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Kidney
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pathology
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Liver
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pathology
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Lung
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metabolism
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pathology
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Male
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Paraquat
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metabolism
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poisoning
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Rats
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Rats, Wistar
3.Chinfloxacin hydrochloride inhibits HERG potassium channel at open state.
Xiang-mei ZHANG ; Zhong-hua ZHU ; Xiao-li SUN ; Jia GUO ; Zhong-zhong ZHAO ; Zhao ZHANG
Acta Pharmaceutica Sinica 2010;45(12):1491-1496
This study is designed to investigate the effects of chinfloxacin hydrochloride (CFX) on the kinetics of HERG K+ channel. Whole cell patch clamp technique was used to record HERG K+ currents from HEK293 cells transiently transfected with cgi-HERG-GFP plasmids and channel kinetics were assessed in the absence and presence of CFX and moxifloxacin hydrochloride (MOX). Results demonstrated that the open state of HERG K+ channel was inhibited by CFX in a concentration- and time-dependent manner, with an IC50 of 162.1 +/- 14.2 micromol x L(-1), two folds higher than its positive control MOX. But there were no significant effects on channel kinetics. In addition, the inhibitory effect of CFX on HERG was enhanced when cells were subjected to altered extracellular K+ concentration.
Anti-Bacterial Agents
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administration & dosage
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chemistry
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pharmacology
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Aza Compounds
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pharmacology
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Dose-Response Relationship, Drug
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Ether-A-Go-Go Potassium Channels
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antagonists & inhibitors
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physiology
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Fluoroquinolones
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administration & dosage
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chemistry
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pharmacology
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HEK293 Cells
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Humans
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Inhibitory Concentration 50
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Kinetics
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Molecular Structure
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Patch-Clamp Techniques
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Potassium
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pharmacology
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Quinolines
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pharmacology
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Time Factors
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Transfection
4.Design, synthesis and antiproliferative activities of artemisinin derivatives substituted by N-heterocycles.
Zhi-zhong ZUO ; Hang ZHONG ; Ting CAI ; Yu BAO ; Zhi-qiang LIU ; Dan LIU ; Lin-xiang ZHAO
Acta Pharmaceutica Sinica 2015;50(7):868-874
Increasing attention has been focused on the antitumor activity of artemisinin derivatives in recent years, for artemisinin had been reported to have cytotoxic effects against HL-60, P388 and MCF-7 tumor cells. We report here the synthesis and evaluation for antitumor activity of a series of artemisinin-ether derivatives bearing tetrahydropyrrole, morpholine, piperidine, substituted piperidines and azoles with various linkers. Sixteen 10-O-substituted dihydroartemisinin derivatives were designed and synthesized, all of which have never been reported in literatures and whose antiproliferative effects on human breast cancer MCF-7, MCF-7/Adr and HL-60 cells were determined by MTT assay or direct cell counting. Each of these artemisinin derivatives possessed better effects than dihydroartemisinin evidently against HL-60 and MCF-7 cells growth, while less potent than doxorubicin. All target compounds exhibited significantly improved potency compared to DHA and doxorubicin on the doxorubicin-resistant MCF-7/Adr cells, so did they in their sensitive counterparts MCF-7 cells. Among them, compounds GF02, GH04 and ZH04 showed strong activity against these three cell lines growth. Further research is undergoing.
Antineoplastic Agents
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chemical synthesis
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chemistry
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Artemisinins
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chemical synthesis
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chemistry
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Breast Neoplasms
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pathology
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Cell Proliferation
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Doxorubicin
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Drug Design
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HL-60 Cells
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drug effects
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Humans
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MCF-7 Cells
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drug effects
5.Resources Survey on Rare and Endangered Medicinal Plant Swertia mussotii Franch
Jifeng ZHAO ; Xiang LIU ; Changhua WANG ; Zhiwei ZHANG ; Songyun QIN ; Guoyue ZHONG
World Science and Technology-Modernization of Traditional Chinese Medicine 2014;(4):845-850
The resource of rare and endangered medicinal plant Swertia mussotii Franch. in Tibet, Qinghai and Sichuan province were surveyed by ways of documents, interview, quadrat and market investigation. The results indi-cated that Swertia mussotii Franch. mainly distributed in Zuogong and Mangkang of Tibet, Yushu of Qinghai province, Shiqu, Daofu, Kangding, Maerkang, Jinchuan and Xiaojin of Sichuan province. According to the height above sea level, the distribution altitude was from 2 300 m (Kangding of Sichuan province) to 3 900 m (Mangkang of Tibet). There are distributions of Swertia mussotii Franch. within the scope of 2 600 m. The illumination, water, soil, temperature and altitude had significant influence on the distribution, growth and reserve of Swertia mussotii Franch. from different angles. In recent years, there was huge increase of market requirement in Swertia mussotii Franch. which were used in Tibetan medicine Zangyinc he n. Excess collection was the primary cause of rapid decreasing in resource of Swertia mussotii Franch.. It was suggested to strengthen the management of rational collection, as well as to accelerate the development of cultivation and production.
6.Implementation of Calgary-Cambridge consultation guide in family medicine practice
Linxi PEI ; Dongfeng GUO ; Junhua ZHONG ; Yunpeng ZHAO ; Shengnan ZHANG ; Yingjun XIANG ; Guangqiang LAI
Chinese Journal of General Practitioners 2013;12(12):977-979
Five general practitioners were trained for application of the enhancing CalgaryCambridge guide in consultation.The consultation time in 50 patients were recorded before and after training and the satisfaction degree of patients was investigated by questionnaire survey.Results showed that the length of consultation time after training was longer than that before training (490 s vs 277 s,P < 0.05) and also longer than that of specialists (490 s vs 268 s,P <0.05).The overall satisfaction rate of patients was increased after training (72% vs 88%,P <0.05).The results indicate that training of Calgary-Cambridge guide for doctor-patient communication can improve the communication skills of general practitioners.
8.Effect of PSMA7 on RB pathway in A549 cells
Xiang HUANG ; Yuheng ZHONG ; Jiayu TAN ; Xuewei XU ; Rui LIANG ; Shaoxia LIANG ; Jing ZHAO
Chinese Journal of Immunology 2017;33(4):516-519
Objective:To investigate the effect of upregulated and downregulated PSMA7 on the cell cycle and Cyclin D1,CDK4,P16,Rb of RB pathway in A549 cells.Methods:Transfected upregulated pcDNA3.1-PSMA7 vecter and downregulated pGPU6/Hygro-PSMA7-265 vecter into A549 cells,and then tested the effect of PSMA7 on the cell cycle of A549 cells by flow cytometry,and detected the protein level of Cyclin D1,CDK4,P16,Rb by Western blot.Results:Compared with the control group,the cell cycle of the A549 cells did not change significantly,and the expression of Cyclin D1,CDK4 decreased but P16,Rb increased when PSMA7 was upregulated.Compared with the control group,the proportion of phase G0/G1,G2/M of the A549 cells decreased and phase S increased,and the expression of Cyclin D1,CDK4 increased but P16,Rb decreased when PSMA7 was downregulated.There was statistical significance for those results.Conclusion:PSMA7 could affect the expression of Cyclin D1,CDK4,P16,Rb protein level of RB pathway in A549 and promoted the A549 cells into phase S when it′s downregulated.
9.Analysis of monitoring results of urinary iodine of children aged 8 - 10 of Zhangjiakou city in Hebei province, 2009
Zhong-xiang, WANG ; Pei-lun, HUA ; Jie, TAN ; Yu-min, ZHANG ; Yan-qing, ZHAO
Chinese Journal of Endemiology 2012;31(1):81-83
Objective To analyze the monitoring results of urinary iodine of students aged 8 - 10 in Zhangjiakou city,problems in monitoring results,and to provide basic information for working out control strategies of iodine deficiency disorders.Methods A township(town,street) in each country of each city(district) in Zhangjiakou was selected according to 5 positions of the east,the west,the south,the north and center,and 1 village elementary school was sampled in each chosen township,twenty students(half male and female) aged 8 - 10 were selected to collect their urine samples in each school.Urinary iodine concentration was determined by arseniccerium method.Results The median of urinary iodine of the 1700 children aged 8 - 10 was 291.5 μg/L,with < 50 μg/L accounted for 0.8%(13/1700),50 ~ 99 μg/L about 4.9%(83/1700),100 - 199 μg/L about 20.5% (349/1700),200 - 299 μg/L about 29.7%(504/1700),and ≥300 μg/L about 44.9%(764/1700).Conclusions Urinary iodine has reached the elimination standard of iodine deficiency disorders in Zhangjiakou city.But the situation of more than adequate amount of urinary iodine and iodine excess is relatively serious and it is necessary to lower iodine concentration.
10.Rapid analysis of antiepileptic drugs in human plasma by micellar electrokinetic capillary chromatography.
Yu ZHAO ; Jian-zhong RUI ; Jin-heng LI ; Bing-ren XIANG
Acta Pharmaceutica Sinica 2006;41(3):210-215
AIMTo develop a rapid and feasible method based on micellar electrokinetic capillary chromatography (MECC) for the simultaneous determination of antiepileptic drugs (AEDs)--phenytoin (PHT), phenobarbital (PB), carbamazepine (CBZ), primidone (PRM) and clonazepam (CZP) in human plasma.
METHODSSeveral factors that impact the separation of AEDs with MECC were investigated, such as concentration of sodium dodecyl sulfate (SDS), buffer compositions, pH, organic modifier, internal diameter and temperature, and an optimized MECC running condition was obtained the running buffer consisted of 8 mmol x L(-1) phosphate, 3 mmol x L(-1) sodium tetraborate, and 50 mmol x L(-1) sodium dodecylsulfate (SDS) (pH 8.0), containing acetonitrile (ACN) (18%) as organic modifier. Detection at 210 nm, run at 25 kV at 30 degrees C in a untreated fused silica capillary (50/45.5 cm length, 50 microm ID).
RESULTSThe reproducibility of both migration time and relative peak area with MECC analysis were appropriate for the intra- and inter-assay coefficients. The evaluated drugs concentration intervals of PRM 1.0-40.0 microg x mL(-1), PB 1.0-60.0 microg x mL(-1), PHT 1.0-40.0 microg x mL(-1), CBZ 1.0-40.0 microg x mL(-1), CZP 0.2-8.0 microg x mL(-1) were linear with correlation coefficients higher than 0.999 1, and coefficients of the variation of the points of the calibration curve lower than 10%. The recoveries of AEDs varied from 80.0% to 100.0%, depending on the drug, with coefficients of the variation lower than 10.0%.
CONCLUSIONThe MECC technique is showed to be rapid, simple, efficient and low cost when applied to monitoring therapeutic drugs in patient treated with a combination of PHT and other AEDs such as hepatic enzyme-inducing agents.
Anticonvulsants ; blood ; Buffers ; Carbamazepine ; blood ; Chromatography, Micellar Electrokinetic Capillary ; methods ; Clonazepam ; blood ; Epilepsy ; blood ; Humans ; Hydrogen-Ion Concentration ; Phenobarbital ; blood ; Phenytoin ; blood ; Primidone ; blood ; Sensitivity and Specificity ; Sodium Dodecyl Sulfate