Journal of Chinese Pharmaceutical Sciences

Struture Identification of Yunnanglysaponin A and B

Dong-Ying Gao, Ru-Yi Zhang, Bing Yao

1994, 3(1): 1-5.

Asbtract ( 1087 )

PDF (320KB) ( 444 )

References | Related Articles | Metrics

Two new saponins were isolated from Glycyrrhiza yunnanensis Cheng f.et L.K.Tai.On the basis of chemical and spectral evidence, their structures were elucidated as 3β-hydroxy-olean-11, 13-dien-29-oic acid-3-O-β-D-glucuropyranosyl(1-4)-β-D-glucuropyranoside and 3β, 21α-di-hydroxy-Olean-11, 13-dien-29-oic acid-3-O-β-D-glucuropyranosyl (1-4)-β-D-glucuropyranoside anddesignated as yunnanglysaponin A and B respectively.

QSAR Study on the Inhibitory Action of 5-Substituted-2,4-diaminopyrimidines on Escherichia coliDihydrofolateReductase

Ren-Li Li, Wen-Sheng Zhang, Wei-Zhang Zhao

1994, 3(1): 6-11.

Asbtract ( 1470 )

PDF (338KB) ( 478 )

References | Related Articles | Metrics

The methylene group between the phenyl ring and the diaminopyrimidine ring of trimethoprim (TMP) was bioisosteristically displaced by thio or imino groups in order to study the rolein the inhibitory activity of the bridge moiety in the molecule of benzyl pyrimidines. The Hansch approach was used in the study of quantitative structure-activity relationships (QSAR). On the basis of QSAR studies the role of the bridge moiety in inhibiting Escherichia coli dihydrofolate reductase was discussed.

Effect of Poloxamer and Adjuvants Admixture on Stability of Submicronized Emulsion

Jun-Min Zheng, Ping-Tian Ding, Shi-Bo Dong

1994, 3(1): 12-17.

Asbtract ( 1422 )

PDF (339KB) ( 481 )

References | Related Articles | Metrics

The addition of a number of adjuvants to Poloxamer 108 can diversely affect its cloud point. Poloxamer-modified soybean lecithin admixture (PSLA) can elevate the cloud point of the system to 125 ºC. The stabilizing effect on the diazepam submicronized emulsion (DSE) using PSLA as anemulsifying agent has been observed through particle size and zeta potential measurement. It was foundthat DSE had mean droplet size of 67.1 nm. The stability index was 1.06 and zeta potential was -27.15 mV, which was greater than that of DSE with the Poloxamer 108 as emulsifying agent only.

Morphological and Histological Studies on Chinese Crude Drug

De-An Guo, Sheng-Hua Li, Zhi-Cen Lou

1994, 3(1): 18-30.

Asbtract ( 996 )

PDF (648KB) ( 425 )

References | Related Articles | Metrics

The morphological and histological characters of the roots derived from Rhaponticum uniforum (L.) DC. and seven Echinops species are described and illustrated with line drawings. These Echinops species are Echinops grijisii Hance, E. latifolius Tausch., E. przewalskii Iljin., E.gmelinii Turcz., E. ritro L., E. talassicus Golosk. and E. integrifolius Kar. et Kir.. The macroscopicaland microscopical similarities and differences among the roots of above eight species are discussed andsummarized in the tables, and a key for the identification of the crude drugs is presented.

Modelling and Analysis of Interactions of Flecainid with Cardiac Sodium Channels

Yue-Jin Wu

1994, 3(1): 31-36.

Asbtract ( 386 )

PDF (337KB) ( 381 )

References | Related Articles | Metrics

Based on the gate-related receptor hypothesis, modelling and analysis of interactions of flecainide with cardiac sodium channels and the gate-related receptor were performed by computer simulation. Model-predicted apparent rates of onset off lecainide (1 μmol/L) blocking were 0.586, 0.128, 0.071, 0.042 and 0.030AP^-1 at stimulation frequencies of 0.1, 0.5, 1.0, 2.0 and 3.3 Hz, respectively. The estimated time constant of recovery from block by flecainide was 17.45 s. These results are in agreement with documented experimental data. The analysis of gate-related receptor showed that the binding and unbinding of flecainide is modulated by anactivation process. No shift of h∞ curve but a significant decrease of m³∞ curve was found in the presence of flecainide (1 μmol/L). These findings sugnficant that flecainide binds to the activation gate-related receptor, and may be trapped in the channel by the activation gate.

Effect of к-Selenocarrageenan on the Production of tumor Necrosis Factor (TNF)

Luo-Xin Zhang, jian-Ming Jiang, Yong-Feng Jia

1994, 3(1): 37-42.

Asbtract ( 464 )

PDF (339KB) ( 480 )

References | Related Articles | Metrics

The present study was designed to investigate the effect ofк-selenocarrageenan (Se-carra) on the production of tumor necrosis factor (TNF) from macrophages of micein vitro. It wasfound that Se-carra 0.1~10 μg/ml promoted the production of TNF from peritoneal macrophages of mice induced by LPS in vitro. It was demonstrated that 0.1~10μg/ml had no direct cytotoxic action onthe target cells. Besides, under the same condition Se-carra had no effect on the reaction of L929 cellsto r-TNF. Further experiment showed that peritoneal macrophages pretreated with Se-carra 0.1~10μg/ml for 8 h before LPS also enhanced the release of TNF.

Hyroxyl Radical Scavenging Effect of Salvianolic Acids

Yu Liu, Jun-Tian Zhang

1994, 3(1): 43-50.

Asbtract ( 1271 )

PDF (372KB) ( 439 )

References | Related Articles | Metrics

The effects of salvianolic acids (sal A) on hydroxylation of salicylic acid in EDTA- H2O2-Fe²⁺ and Vit C-H2O2-Fe²⁺ systems were studied. In the latter system, the compounds were shown to dose-dependently inhibit the hydroxylation of salicylic acid and the efficacy order was basically incorrespondence with that for anti-lipid-peroxidation. But in the former system, the effects weresomewhat complex, most of the compounds dose-dependently inhibited hydroxylation of salicylic acidexcept Sal A, which, like Vit C, promoted hydroxylation at lower concentration but inhibited it at higherconcentration. These compounds were found to chelate to or react with iron ions, but their apparentchelating constants were about 100 fold lower than that of EDTA. Salvianolic acids were thusconsidered to be hydroxyl radical scavengers.

Binding of Carboline Derivatives to Calf Thymus DNA─Determination of Binding Mode and Binding Strength

Ming Yang, Kui Wang, Chuan-Bing Zang, Bao-Huai Wang, You-MinZhang

1994, 3(1): 51-58.

Asbtract ( 1305 )

PDF (369KB) ( 556 )

References | Related Articles | Metrics

The relationship between anticancer activity of six carboline derivatives (CB1-6)and their binding mode and binding strength with DNA was studied. Binding mode was established by study of structural changes in DNA helix, which involved assessment of changes in the viscosity, ³¹P NMR and CD spectra of DNA as well as hypochromism in UV-Vis determination and ¹H NMR spectra of the aromatic protons of CB1-6 by titration with DNA. Binding strength was evaluated by spectroscopic and microcalorimetric measurements. The results indicate that the binding depends strongly on the ring automaticity and the substituent groups, which accords well with the findings in bioactivity tests.

Characterization of a Platelet-Activating Factor Receptor Antagonist, Kadsurenone:Specific Inhibition of Platelet-activating Factor in vitro and in vivo

Yi-Zheng Shen, Chang-Ling Li, Yin-Yie Wang, Xiao-Dong Guo, Gue-QiuHan

1994, 3(1): 59-65.

Asbtract ( 474 )

PDF (354KB) ( 464 )

References | Related Articles | Metrics

Kadsurenone (Kad) is a lignan isolated from the Chinese herbal plant Heifenteng (Piper futokadsura). In the present paper the effects of Kad on PAF receptor using radioligand binding assay, as well as on rabbit platelet aggregation are reported. The experimental results indicated that Ked is a potent and specific PAF antagonist. The Ki value of Kad binding PAF receptor of washed rabbit platelets was found to be 2×10^-12 mol/L. Experiment in vitro showed that the rabbit platelet aggregation induced by PM was inhibited by Kad (IC50 = 2.6 μmol/L). However, no inhibitory effecton the aggregation induced by arachidonic acid and ADP was observed. Kad (0.1 mg/kg, iv)completely inhibited PAF-induced platelet aggregation in rabbits and the effect lasted for 2 hr. The formation of platelet thrombus in rats was inhibited by iv Kad (7.1 mg/kg; 14.2 mg/kg) or po (80 mg/kg, 120 mg/kg).The inhibitory rate of Kad was 25.4%, 38.2%, 21.4% and 34.6% respectively. It issuggested that the PAF is an important factor in thrombosis and Kad is a specific PAF receptor an-tagonist .

Effect of Pentamidine Isethionate (PI) on Fertilized Ova of ICR Mice

Ying Wang, Shu-Cheng Zhang, Jing-Feng Dai, Jin-Song Qiu, Yi Qiu, Yi-Bin Sun

1994, 3(1): 66-70.

Asbtract ( 1001 )

PDF (315KB) ( 418 )

References | Related Articles | Metrics

Two kinds of fertilized ova were collected .in vivo and in vitro fertilized ova. All the ova were incubated with 0, 0.25, 0.5, 2.5 and 5.0 μg/ml Pentamidine isethionate (PI) for 15 min, respectively. After drug treatment. the fertilized ova were further cultured for 28 h to investigatethe cleavage of ova. The results showed that the cleavage of fertilized ova in the PI-treated groupswere significantly reduced in normal cleavage and increased in abnormal cleavage as compared tothose in the controls (p<0.01). It may be concluded that PI possesses an antifertility effect.

Determination of Ciprofloxacin in HumanPlasma by High-Performance Liquid Chromatography and Its Pharmaceu-tic Studies

Li Tan, Ke Li

1994, 3(1): 71-75.

Asbtract ( 1098 )

PDF (313KB) ( 398 )

References | Related Articles | Metrics

An ion-pair reversed-phase high-performance liquid chromatographic method wasdeveloped for the determination of ciprofloxacin in human plasma. A reversed phase C18 Spherisorbcolumn (25 cm×4.6 mm, 5 μm) and a mobile phase of methanol-0.008 mol/L phosphate buffer-0.5mol/L tetrabutylammonium bromide (30:75:4, v/v/v, pH 2.6) were used. The detection wavelength was276 nm and the limit of detection was 40 ng/ml at a signal-to-noise ratio of 2. Protein preciptation wasaccomplished by the addition of acetoitrile. This procedure was used to study the pharmacokinetics of two preparations of ciprofloxacin in 8 volunteers upon oral administration, randomized crossover. There was no significant difference in pharmacokinetic parameters between the two preparations. The bioavailability of the syrup was 84% of that of the tablet.

A SEP-PAK HPLC Analysis of Benzodiazepines (Nitrazepam, Clonazepam and Flunitrazepam) in Human Urine

Zhan-Pin Wu, Dong-Cai Chen

1994, 3(1): 76-80.

Asbtract ( 1765 )

PDF (320KB) ( 431 )

References | Related Articles | Metrics

An efficient method of SEP-PKA solid-phase extraction and reversed-phase, isocratic high-performance liquid chromatographic method for the simultaneous quantitation of nitrazepam, clonazepam and flunitrazepam in human urine is presented. The recoveries with SEP-PAK C18 cartridgeswere excellent for all these drugs. The drugs were separated on a reversed-phase YMC A-303 C18 co-lumn with acetonitrile-0.01 mol/L ammonium acetate (45:55, v/v) as the mobile phase. The detectionwas performed at 254 nm. Within-day and day-to-day precision were about 1~5%. The method is sensitive and reproducible and can be used in clinical and experimental toxicokinetic studies.

Induction-Differentiation Effectof β-Caroteneon Human Promyelocytic Leukemia Cells

Hui-Chen Liu, De-Zheng Wu

1994, 3(1): 81-84.

Asbtract ( 1259 )

PDF (307KB) ( 410 )

References | Related Articles | Metrics

Effects of Dismerinoneon High K+ Depolarized Slow Response Action Potentials and Intracellular cAMP Levelin Guinea Pig Papillary Muscles

Dian-Zeng Zhang, Geng-Sheng Zhao, Jie-Min Fu

1994, 3(1): 85-89.

Asbtract ( 1176 )

PDF (312KB) ( 400 )

References | Related Articles | Metrics

Constituents from Glycyrrhiza inflata and Antioxidant Activities of Phenols from the Roots of Glycyrrhiza spp.

Kun Zou, Ru-Yi Zhang

1994, 3(1): 90-90.

Asbtract ( 389 )

PDF (242KB) ( 455 )

Table of Content