Journal of Chinese Pharmaceutical Sciences

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2005, 14(4): 1-01.

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Interaction between Mitomycin C and DNA at Paraffined Graphite Electrode

GUO Ming^*, TAN Fei, HU Run-huai, YU Qing-sen

2005, 14(4): 199-203.

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Aim To investigate the electrochemical behaviors of Mitomycin C (MC) and its interaction with calf thymus DNA (ctDNA). Methods The cyclic voltammetry (CV) was carried out at a paraffined graphite electrode. Results MC showed a well-defined oxidation-reduction peak. As a result of reaction with ctDNA, the peak current of MC decreased apparently. According to corresponding electrochemical equations, the diffusion coefficient of both free and MC-DNA complex have been determined, and the heterogeneous rate constants were also obtained simultaneously. Conclusion The solid paraffined graphite electrode could be used to estimate parameters of the interaction between DNA and MC, and provide the convenient and sensitive analysis.

A Convenient Synthesis of Trans and Cis-3, 4', 5-trihydroxystilbene

WANG Zhi-xin, ZHANG Xue-jing, ZHOU Yue, ZOU Yong^*

2005, 14(4): 204-208.

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Aim To synthesize trans and cis-3, 4', 5-trihydroxystilbene by a new convenient route. Methods The reaction of 3, 5-dimethoxybenzaldehyde (3) and 4-methoxy phenylacetonitrile (4) formed the stilbene skeleton. After hydrolyzation, decarboxylation, and demethylation, we obtained trans-3, 4', 5-trihydroxystilbene (resveratrol), which can be converted to its cis-isomer by photochemical isomerization. Results Starting from 3 and 4, trans and cis-3, 4', 5-trihydroxystilbene were synthesized, respectively. Conclusion A facile method for the synthesis of trans and cis-hydroxystilbenes from readily available materials was established.

Improved Synthesis of Fructose-Derived 1, 3, 4-Oxadiazole as Novel Antitumor Agents

LIU Hong, HAN Dong, MENG Xiang-bao, LI Zhong-jun^*

2005, 14(4): 209-212.

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Aim To optimize the reaction condition for preparation of 3-spiro-1, 3, 4-oxadiazole substituted fructose and hydrolysis of its isopropylidenes stepwisely. Methods Cyclohexane was added to the reaction mixture every 8 h to remove acetic acid at 90 ºC. The isopropylidenes were hydrolyzed in 80% AcOH at 60 ºC stepwisely in a reaction time- dependent manner. Results The yields of cyclization products 1b and 1c were improved from 53% and 51% to 74% and 79% respectively. The 1, 2-di-O-isopropylidene product 3 was obtained after 1 h and the total deprotected product 4 was obtained after 3 h in 80% AcOH at 60 ºC. Conclusion The yield of 1 is improved by cyclohexane-aided azeotropic removal of AcOH from the reaction mixture. Deprotection of 1 in 80% AcOH at 60 ºC gives 3 or 4 after different time periods.

Conformation and Antitumor Activity of Novel Metal Complexes of Piperazinedithioformates

HE Fei, HUANG Hui, YIN Fu-ling, LI Run-tao, LEI Xiao-ping, ZENG Hui-hui ^*

2005, 14(4): 213-216.

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The in vitro antitumour efficacy of some novel metal complexes of piperazinedithioformates (SR-M) was examined in six cancer cell lines. The activity was compared with that of piperazinedithioformates. Biological evaluations of a series of SR-M compounds suggest that the compounds 1c (SR-Cu) and 1f (SR-Sn) show a potent antitumor activity. The stable conformation structure of SR-Cu as a representative of SR-M was investigated and confirmed by computer workshop.

Safety and Tolerance of Adefovir Dipivoxil in Chinese Healthy Volunteers: A PhaseⅠRandomized and Open-Label Trial

SUN De-qing, NI Mei-yuan, WANG Ben-jie, GUO Rui-chen^*

2005, 14(4): 217-222.

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Aim To assess the safety and tolerance of adefovir dipivoxil (ADV) in Chinese healthy volunteers. Methods A total of 52 healthy volunteers, 26 males and 26 females, aged from 19 to 26 were enrolled in the study. Forty-two subjects were randomized into 5, 10, 20, 40, and 60 mg dose groups (6-10 subjects in each) matched by sex and weight for single-dose trial. Ten subjects were orally given 10 mg of ADV tablets once daily for 7 d for multiple-dose trial. Physical examination, vital signs examination, electrocardiography, type-B ultrasonography, chest fluoroscopy, routine blood test, routine urine test, coagulation tests, and blood biochemical test were conducted on schedule and statistically evaluated. Results Asthenia frequently occurred in multiple-dose trial, nausea, abdominal pain, and diarrhea occurred in both single- and multiple-dose trials. ALT, bilirubin, CK, and LDH were slightly elevated. All adverse reactions and laboratory abnormalities were mild, and the frequency and severity were not related to doses. Conclusion ADV is safe and well tolerated in Chinese healthy volunteers at dose of 5-60 mg once daily or 10 mg once daily for 7 d. The recommended oral dosage regimen is 10 mg once daily. Attention should be paid to renal and liver functions, CK, AMY and LDH, if we take ADV for a long period of time.

Pharmacokinetics of Active Metabolite of Prulifloxacin in Healthy Chinese

WEI Chun-min^**, WANG Ben-jie, LI Hui-yun, GUO Rui-chen^*

2005, 14(4): 223-226.

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Aim To investigate the pharmacokinetics of NM394 (an active metabolite of prulifloxacin) and evaluate the dose relationship and accumulation characteristics after single and multiple doses of prulifloxacin. Methods Twelve healthy volunteers were given 132.1 mg, 264.2 mg, and 396.3 mg of prulifloxacin tablets in a randomized 3 ×3 crossover design test for single doses trial. With one-week washout period, 264.2 mg of prulifloxacin tablets were given for multiple doses trial. NM394 in plasma was determined by a sensitive HPLC method and its pharmacokinetic parameters were analyzed and evaluated by Drug and Statistics saftware (version 1.0). Results The Cmax, Tmax, t1/2, AUC0-24, and AUC0-∞ of NM394 after single doses of 132.1 mg, 264.2 mg, and 396.3 mg of prulifloxacin tablets were 0.64±0.25 μg·mL^-1, 1.06±0.35 μg·mL^-1, and 1.45±0.44 μg·mL^-1, respectively; Tmax 0.94±0.22 h, 1.02±0.17 h, and 0.98±0.23 h, respectively; t1/2 8.37±0.70 h, 7.70±0.82 h, and 7.78±0.77 h, respectively; AUC0-24 2.93±0.78 μg·mL^-1·h, 4.39±1.05 μg·mL^-1·h, and 5.55±1.32 μg·mL^-1·h, respectively; AUC0-∞ 3.32±0.84 μg·mL^-1·h, 4.82±1.06 μg·mL^-1·h, and 6.10±1.38 μg·mL^-1·h, respectively. And the Cmax,Tmax, t1/2, AUC0-24, and AUC0-∞ after multiple doses of 264.4 mg prulifloxacin tablets were 1.20±0.33 μg·mL^-1, 0.67±0.12 h, 7.38±1.03 h, 5.58±1.25 μg·mL^-1·h, and 6.09±1.24 μg·mL^-1·h, respectively. Conclusion The Cmax and AUC of NM394 are in high correlation with given prulifloxacin doses. There are no differences in pharmacokinetic characteristics of NM394 between single and multiple doses. No accumulation in plasma is observed after multiple doses of 264.2 mg per day for 7 d.

Determination of Liquiritigenin, Liquiritin, Isoliquiritigenin and Isoliquiritin in Extract of Traditional Chinese Medicine Sijunzi Decoction by High-Performance Liquid Chromatography

LIU Yang, YANG Jun-shan^*

2005, 14(4): 227-230.

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Aim An HPLC-UV method for the analysis of Traditional Chinese Medicine (TCM) preparation, Sijunzi decoction, has been developed. Four flavonoid marker compounds, liquiritigenin, liquiritin, isoliquiritigenin, and isoliquiritin, from Radix Glycyrrhizae were quantitatively analyzed in this preparation. Methods The separation was performed on a reversed-phase C18 column by using a gradient elution with mobile phase of (A) water-formic acid (100∶0.04, V/V) (pH 3) and (B) acetonitrile. The mobile phase gradient was set from 0-5 min at 10% of B and 45 min to 90% of B. The assay was carried out at a flow rate of 0.2 mL·min^-1 at room temperature with the UV detection wavelengths at 280 nm and 368 nm. Results The extract (25 mg·mL^-1) of Sijunzi decoction contains 1.47 μg·mL^-1 liquiritigenin, 16.40 μg·mL^-1 liquiritin, 0.66 μg·mL^-1 isoliquiritigenin, and 2.12 μg·mL^-1 isoliquiritin. The recoveries for the sample preparation of the markers were 102.2%, 97.7%, 100.3%, and 99.9%, respectively. Conclusion The method is simple and accurate. This study reports a routine quantitative method for the analysis of multiple components in Sijunzi decoction by HPLC.

Effect of Quercetin on CYP1A2, CYP2E1, CYP3A2 Activities and its Inhibitory Mechanism Studies in Rat Liver Microsomes

ZHOU Jiang-quan^*, TANG Zhi-qiang

2005, 14(4): 231-236.

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Aim To assess the potential effect of quercetin (QU), an natural plant estrogen, on CYP1A2, CYP2E1, and CYP3A2 activities in rat liver microsomes; and to identify the magnitude of inhibitory effect and the probable inhibitory mechanism of QU. Methods QU and specific substrate were concurrently incubated, with HPLC detection of the substrate metabolites for data analysis. The magnitude of inhibitory effect of QU on CYP3A2 was compared with those of ketoconazole (Ket) and erythromycin (Ery). The mechanism of its inhibitory effect on CYP3A2 and CYP2E1 was derived from Lineweaver-Burk plots. Results HPLC methods were in good linear relationship with r>0.999 1. Relative standard deviations for intra-day and inter-day were<8.4%. Recovery of each analyte in the concentrations studied was between 91.1% and 107.6 %. QU (up to 8 μmol·L-1) showed potent induction to CYP1A2 (338.1% of the negative control)while inhibited CYP2E1 (49.2% of the negative control) and CYP3A2 (60.3% of the negative control) activity. The magnitude of inhibitory effect for QU on CYP3A2 was between those for Ket and Ery (Ket>QU>Ery). QU exhibited competitive inhibition of CYP3A2 dextromethorphan N-demethylation reaction and expressed noncompetitive inhibition of CYP2E1 chlorzoxazone-6-hydroxylation reaction. Conclusion HPLC assay has been validated with precision and accuracy. QU is an effective inhibitor of several CYP isoforms. It may cause relevant drug-drug interactions with CYP3A substrates. As a plant flavonoid, QU has potential not only in molecular advantage but also in CYP450 module capability for further application in cancer chemotherapy.

A Survey of Drug Supply Organizations in Rural Areas in four Provinces of China

HU Ming^*, ZENG Yu, YANG Jun-bin, WU Peng

2005, 14(4): 237-241.

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Aim To realize the present situation of drug purchase, supply, and use in the health service organizations and drug distributors in rural areas, and to put forward some suggestions. Methods An interview survey was conducted in 20 township hospitals, 26 countryside drugstores, and 84 village dispensaries in Hainan, Anhui, Henan, and Sichuan Provinces. Results (1) The main drug supplying organizations in the countryside are township hospitals and village dispensaries. (2) The personnel in the drug supplying organizations are rather inadequately educated. (3) The drug resources in the grass-roots countryside are complex and disordered. (4) Most of the countryside retail drugstores are small, and the number of drugstores is small, but their development potential is great. Conclusion (1) A basic drug catalogue for rural areas should be made up. (2) Legitimate drug wholesale companies should be encouraged to supply drugs for vast countryside. (3) Development of drug distributionstations in townships should be promoted. (4) The administration of drugs in the countryside should be strengthened.

Phenylethanoid Glycosides from Cultivated Cistanche salsa

YANG Jian-hua, DU Nian-sheng^*, Rena Kasimu

2005, 14(4): 242-245.

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A Sensitive High-Performance Liquid Chromatography Coupled with Solid- Phase Extraction for Determination of Fexofenadine in Beagle Plasma

MA Lei, YIN Li-li, SUN Jin, HE Zhong-gui^*

2005, 14(4): 246-249.

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Cantharidin and Its Analogues:Anticancer and Ser/Thr Protein Phosphatase Inhibitory Activities

SHI Qing-hua, WANG Yu-ling, SONG Hong-rui^*, CHENG Mao-sheng

2005, 14(4): 250-256.

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This paper mainly describes the anticancer activities and Ser/Thr protein phosphatase inhibitory activities of cantharidin and its analogues.

CONTENTS OF VOLUME 14
AUTHOR INDEX

2005, 14(4): 257-264.

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