Journal of Chinese Pharmaceutical Sciences

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2001, 10(1): 1-01.

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Desmosdumotin A, a New Compound from Desmos dumosus

Wu Jiuhong, Mao Shilong, Liao Shixuan, Yi Yanghua, Su Zhongwu

2001, 10(1): 1-2.

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A new compound, desmosdumotin A (1), was isolated from the roots of Desmos dumosus (Roxb.)Saff. Its chemical structure was established as 5-hydroxy-7-methoxy-8-formyl-3-benzoyl-2,6-dimethyl-2R,3S-dihydrochromone on the basis of spectral methods, including ¹H-¹H COSY, ¹H-¹³C COSY, and HMBC as well as singlecrystal X-ray analysis.

Syntheses and Pharmacological Activity of Some 17-[(2'-Substituted)-4'-pyrimidyl]androstene Derivatives As Inhibitors of Human 17α-Hydroxylase/C_17,20-Layse

Ru Chengjie, Lei Xiaoping, Ling Yangzhi^*, Zhang Lihe, Venkatech Hundratta, Angela Brodie

2001, 10(1): 3-8.

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A new compound, desmosdumotin A (1), was isolated from the roots of Desmos dumosus (Roxb.)Saff. Its chemical structure was established as 5-hydroxy-7-methoxy-8-formyl-3-benzoyl-2,6-dimethyl-2R,3S-dihydrochromone on the basis of spectral methods, including ¹H-¹H COSY, ¹H-¹³C COSY, and HMBC as well as singlecrystal X-ray analysis.

Parallel Synthesis ofα-Acylamino Amide Library by Ugi four-component Condensation Reaction

Xu Ping^*, Lin Wenwei, Zhang Ting, Hu Xinge, Zou Xiaomin

2001, 10(1): 9-13.

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Ugi-4CC(four-component condensation) reaction is one of isonitrile-based MCR’s (multi-component reactions), which is started with an amine, an aldehyde, a carboxylic acid and an isocyanide, after one-pot reaction to produce a compound composed of the whole four starting materials. The reaction makes full use of the specialty of isonitrile and can be used to build a series of compounds with different structural skeletons by using diverse inputs. In our work, two kinds of isonitriles were synthesized and a parallel synthesis of an α-acylamino amide library was performed to modify the Ugi reaction conditions.

The Synthesis of Some 17-(2'-Oxazolyl)-androsta-5,16-diene Derivatives as 17α-Hydroxylase/C_17,20-Lyase Inhibitors

Zhu Na, Zhao Na, Lei Xiaoping, Ling Yangzhi^*, Venkatech Hundratta, Angela Brodie

2001, 10(1): 14-19.

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Several 4'- and 5'-substituted 17-(2'-oxazolyl)-androsta-5,16-diene derivatives were designed and synthesized as inhibitors of 17α-hydroxylase/C17,20-Lyase (P45017α) for the treatment of prostatic cancer, the results of the preliminary pharmacological screening showed that compound 6c, i.e. 17-(2'-oxazoly)-androsta-5,16-diene-3-ol was a strong inhibitor, comparable with that of the reference compound VN-85. The introduction of methyl or phenyl group at the 4' or 5' position of oxazole ring decreased the activity. The in vitro activities of 3-acetate 5a~c and 8 were lower than their 3-ol counterparts 6a～c and 9 as expected. The further pharmacological study of 6c is in progress.

Study on the Degradation of Polylactide Microsphere In Vitro

He Ying, Wei Shuli

2001, 10(1): 20-23.

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This report concentrated on the rules and mechanism of the degradation of polylactide and the microspheres. The rate of degradation was assessed with five methods: observation of microsphere surface morphology by SEM, determination of the weight loss of the microspheres, determination of the molecular mass of the polymers by GPC, determination of pH and determination of the contents of lactic acid by UV spectrophotometry. The degradation of polylactide microspheres showed two-phase characteristics. At the early stage of the degradation, the high molecular mass polymers were cleaved into lower molecular mass fractions and at the late stage, there was a period of erosion and weight loss of the microspheres. The degradation was much slower for polymers with a higher molecular mass. The polylactide degradation showed good regularity.

Ciprofloxacin Loaded Bovine Serum Albumin Microspheres: Preparation and Drug Release Characterization In Vitro

Li Fengqian^*, Hu Jinhong, Lu Bin, Zhu Quangang, Sun Huajun

2001, 10(1): 24-28.

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Ciprofloxacin loaded microspheres were prepared by spray drying technique, with bovine serum albumin as the natural biodegradable wall materials. The obtained microspheres, using aqueous system, were organic solvent-free. The diameters of the spherical microspheres were in the range of 1~5 μm. The drug entrapment of microspheres, formulated with different ciprofloxacin/albumin ratios as 1:1, 1:2 and 1:4, were 46.93%, 32.96% and 20.56% (n = 3). And the encapsulation efficiencies for ciprofloxacin during spray drying were higher than 90%. Thermal denaturation programs at different temperatures (100~120 °C) for different time intervals (3~6~12 h) were further processed to stabilize the spray-dried microspheres. The higher the extent for thermal denaturation, the slower the rate of ciprofloxacin released from microspheres in vitro. So the release rate of ciprofloxacin from microspheres can be controlled by modifing the conditions of thermal denaturation.

Improving Bioavailability of Naftopidil in Dogs by Using Bioadhesion

Ding Jinsong, Jiang Xuehua

2001, 10(1): 29-33.

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To improve the bioavailability of naftopidil, bioadhesive sustained-release capsules and non-bioadhesive capsules were prepared. Bioadhesive polymers such as hydroxypropyl methylcellulose (HPMC) and Carbopol 934 (CP 934) were used in the bioadhesive capsules formulations. Naftopidil capsule and two formulations of bioadhesive sustained-release capsules (I and II) were respectively given to five healthy male dogs in an open randomized cross-over test. The naftopidil concentrations in plasma were determined by a newly developed HPLC method. The pharmacokinetic parameters and the relative bioavailability were measured. The AUC0→24, Cmax and Tmax of non-bioadhesive naftopidil capsules were 3494.7±466.47 h·ng·mL^-1, 697.48±94.22 ng·mL^-1 and 1.15±0.49 h. These pharmacokinetic parameters of bioadhesive sustained-release capsules I and II were 4618.46±316.68 h·ng·mL^-1 and 4746.44±317.22 h·ng·mL^-1, 468.59±61.25 ng·mL^-1 and 512.00±72.29 ng·mL^-1, both 4.0±0.71 h respectively. Results from statistical analysis showed that there were significant differences between the two bioadhesive formulations and the non-bioadhesive one in AUC0→24, Cmax and Tmax. The relative bioavailability of the two bioadhesive sustained-release capsules were respectively 133.40±12.72% and 137.53±17.49% when compared with non-bioadhesive capsules. The bioavailability of naftopidil in dogs was improved by using bioadhesion.

Preparation and Evaluation of Immobilized SE-30 Coated Stationary Phases for CEC

Ning Baoming, Zheng Jie, Zhang Guodong, Xu Bingjiu^*

2001, 10(1): 34-38.

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A new type of stationary phase for capillary electrochromatography (CEC), immobilized SE-30 coated silica gel, was developed and the columns packed with this new phase were prepared and evaluated. It was found that this phase could be used to make frits for the micro-columns as well as to pack the bulk of the column. By sticking together the particles in the whole of the column bed, this new packing resulted in columns with stable performance, even under rigorous conditions: more than 380 consecutive separations were effected with these columns with the mobile phase pH of 11.7.

Sub-critical Column and Capillary Chromatography with Water as Mobile Phase and Flame Ionization Detection

Lu Feng, Li Ling, Sun Peng, Wu Yutian

2001, 10(1): 39-41.

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A sub-critical chromatography (SubWC) with water as mobile phase and FID detection system is employed to separate several alcohols with high or medium polarity, with pure water as the eluent. The flow rate gets up to 50 μl·min^-1 for packed column (1 mm i.d.) and 70 μl·min^-1 for capillary (50 μm i.d.). Increasing the temperature up to 140 °C, together with temperature programming, markedly improves the separation and peak shapes within short analysis time. Sub-critical state is guaranteed.

Homoerydictyl-7-O-β-D-glycoside-A Receptor Antagonist of Platelet-activating Factor (PAF)

Guan Zengwei, Wang Yinye, Yang Xiuwei, Cui Yuxin

2001, 10(1): 42-44.

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Homoeriodictyl-7-O-β-D-glycoside, a flavonoid compound isolated from the Chinese medicinal herb, viscum coloratum inhibited platelet aggregation induced by platelet-activating factor(PAF), but it had no inhibitory activity on adenosine diphosphate-induced platelet aggregation. In the present study, we intended to get an insight into the mechanism of its anti-PAF action. Using [³H]PAF receptor binding assay we found that the compound exhibited inhibitory activity. The inhibitory rate was 18.5%, 28.4%, 58.7%, 78% and 78%, respectively, at concentrations of 10^-8, 10^-7, 10^-6, 10^-5 and 10^-4mol·L^-1, There was a visible dose-effect relationship as well as a correlation between different concentrations and their inhibitory rates (γ = 0.985, P<0.05) when the dose was equal to or less than 1×10^-5 mol·L^-1, and its IC50 was 8.0×10^-7 mol·L^-1. The inhibitory rate didn't increase with increasing concentration of the compound when it went beyond 1×10^-5 mol·L^-1 indicating competitive inhibition of binding of [³H]PAF to PAF receptor reached saturation.

Characterization of the Pharmacology of Recombinant Human GABA_A Receptor Complexes Containing A2(α1 isoleucin 148 to valine) or A2(α1 asparatic acid 151 to asparagin) ……

Wang Xiukun

2001, 10(1): 45-48.

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Recombinant human GABAA receptors were investigated in vitro by coexpression of cDNAs coding for α1, β2 and γ2 subunits in the baculovirus/Sf-9 insect cell system. A single amino acid exchange α1 (asparatic acid 151 to asparagin or α1 (threonine 149 to glutamine) in the N-terminal, extracellular part of the α1 subunit induced about 10 fold decrease in an antagonist pitrazepine affinity. Other GABAA receptor ligands had little difference in their affinity. It was likely that 151 and 149 amino acid residues were essential for the binding affinity and efficacy of pitrazepine to GABAA receptor combinations containing an α1 subunit.

Synthesis of Several 3-Oxamoyl-2-phenylindole Derivatives and Their Ability to Inhibit on Cultured Rat Luteal Cell Growth

Wang Hao, Wen Ren^*, Jiang Weiqun, Dong Xiaochun, Huang Lei, Li Ning, Cao Lin

2001, 10(1): 49-51.

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Study on Immunoliposomes and Membrane Electric Properties

Zhang Yufeng, Hou Xinpu, Xie Shusheng

2001, 10(1): 52-53.

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