Journal of Chinese Pharmaceutical Sciences

Study on 3D-QSAR of Retinoids 3D-Interaction between Retinoids and their Receptor

Min-Min Wang, Niu Huang, Guang-Zhong Yang, Zong-Ru Guo^*

1996, 5(2): 57-62.

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Fast and precise prediction of the receptor-ligand binding constant is an important aspect of structure-based drug design. Almost all de novo design methods or 3D database search methods tend to structure generation instead of structure evaluation. In this article, epididymal retinoic acid binding protein (ERABP) was used as a template to simulate the interaction between retinoids and their receptor. We deduced an equation predicting the drug-receptor binding constant. Furthermore, the conformers after docking were used in CoMFA analysis to get a pharmacophore model of this series of compounds.

Chemical Constituents of Tussilago farfara L.

Wei Shi, Gui-Qiu Han^*

1996, 5(2): 63-67.

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Two new sesquiterpenes, named tussilagonone (1) and neotussilagolactone (2), together with two known sesquiterpenes (3) and (4) and two phthalic acid derivatives (5) and (6), were isolated from the flower buds of Tussilago farfara . The structures of (1) and (2) were determined on the basis of spectroscopic analyses. Compounds (1) and (2) exhibited activities against platelet aggregation caused by platelet activating factor.

Two New Coumarins from the Roots of Aegle marmelos

Xiu Wei Yang, Masao Hattori, Tsuneo Namba

1996, 5(2): 68-73.

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Two new coumarins, named marm inal (13) and 7’-O-methylmarm in (15), along with nineteen know n compounds: (β-sitosteryl pentadecanoate (1), 4-methoxy-1-methyl-2-quino lone ( 2), aurap ten (3), 4-sito sten-3-one (4), lupeo l (5), imperato rin (6), xantho toxin (7), dictamnine (8), (+)-epoxyaurap ten (9), (β-sito-sterol (10), (γ-fagarine (11), sk imm ianine (12), scoparone (14), umbelliferone (16), scopo let in (17), decursino l (18), marmesin (19), marm in (20), and integriquinolone (21) w ere iso lated from the methano lic ext ract of the roo ts of Aegle marmelo s Corr. (family Rutaceae).

Electrophysiologic Effects of Sophoridine on a Canine Model of Ischemic Ventricular Tachyarrhythmias

Zhi-Bin Guo, Hong-Yu Cao, Zhi Xu, Qing Li

1996, 5(2): 74-80.

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A canine model of ischemic ventricular tachyarrhythmias was established in open-chest dogs subjected to programmed electrical stimulation (PES) for 5-8 days after acute myocardial infarction. The electrophysiologic effects of sophoridine (Sop) and procainamide (PA) were observed in this canine model. With routine methods of PES, ventricular tachycardia (VT) and ventricular fibrilation (VF) could be reproducibly initiated in this model. Both drugs distinctly lengthened the QTc interval ( P <0.01) and the effective refractory period (ERP) in normal and ischemic ventricular myocardium ( P <0.01), decreased the dispersion of ERP in ischemic myocardium and the dispersion of ERP in left ventricle (P <0.05), and increased the diastolic excitability threshold of normal and ischemic ventricular myocardium remarkably ( P <0.01). Both drugs effectively prevented the PES-induced VT or VF and ischemia-induced VF ( P <0.05). The results indicated that this canine model is a good and reliable one, sophoridine and procainamide may be effective in preventing the onset of reentrant ventricular tachyarrhythmias after myocardial ischemic damage.

A Study on the Multi-Compartment Linear Circulation Pharmacokinetic Model for the Targeting Drug Delivery System

Zhi-Rong Zhang, Tsuneji Nagai

1996, 5(2): 81-87.

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By analyzing the observed phenomena and the data collected in the study, a multi-compartment linear circulation model for targeting drug delivery system was developed and the function formulas of the drug concentration-time in blood and target organ by computing were figured out. The drug concentration-time curve for target organ can be plotted with reference to the data of drug concentration in blood according to the model. The pharmacokinetic parameters of the drug in target organ could also be obtained. The practicability of the model was further checked by the curves of drug concentration-time in blood and target organ(liver) of liver-targeting nanoparticles in animal tests. Based on the liver drug concentration-time curves calculated by the function formula of the drug in target organ, the pharmacokinetic behavior of the drug in target organ(liver) was analyzed by statistical moment, and its pharmacokinetic parameters in liver were obtained. It is suggested that the (relative targeting index" can be used for quantitative evaluation of the targeting drug delivery systems.

The Effects of Some Penetration Enhancers on the Transdermal Iontophoretic Delivery of Insulin in Vitro

Jin-Song Hao, Da-Wei Li, Shou-Feng Li, Jun-Min Zheng

1996, 5(2): 88-92.

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The effects of some commonly used penetration enhancers such as laurocapram (AZ), oleic acid (OA), poloxamer (POL) and propylene glycol (PG) on the in vitro transdermal iontophoretic delivery of insulin through full-thickness mouse skin were investigated. The results showed that AZ had a synergistic effect on iontophoretic ability to enhance skin permeation of insulin, and PG could further increase this effect. 5% AZ / PG increased the iontophoretic steady state flux of insulin by a factor of 2.75 compared to that treated with iontophoresis alone. OA did not further enhance iontophoretic effect to increase skin permeation of insulin. The combination of iontophoresis and some enhancer provided a novel idea and possibility for transdermal delivery of insulin.

Preparation, Stability and Immunoenhancement of APS (Astragalus polysaccharide) Liposomes

Ying-Jie Deng, Feng Xu, Yi-Guang Jin, Shu-Qin Liu, Li-Mei Han, Shuo-Ning Miao, Jing-Cai Li, De-Sen Su, Yang Han, Xue-Qiu Gu

1996, 5(2): 93-99.

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Six factors and 10 levels of each factor were selected by using the (uniform design method( with the aid of the computer for preparing APS liposomes. The optimal procedure for preparing APS liposomes was established and it can suit the large scale production in a pharmaceutical factory. The shelf-life of APS liposomes at 20 ºC is 1.46 years. Diameters of the vesicles (>90% ) in APS liposomes are less than 1 μm, and the system is stable. At 40 ºC the diameters of vesicles were not changed in three months. Pharmacological experiments revealed that APS liposomes exerted a strong immunoenhancement in mice. Studies in this paper established a foundation for the production and the clinical application of APS liposomes.

Purification of Inositol. Studies on the Phase Equilibrium of the System C6H12O6-NH4Cl-C2H5OH/H2O (C2H5OH/H2O = 0.90, by wt) at 35 ºC

Dao-Dao Hu, Hong Li, Ya-Li Cui, Yu Fang, Zong-Xun Tang

1996, 5(2): 100-104.

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The solubilities and the refractive indices of the saturated solution in the system C6H12O6-NH4Cl-C2H5OH-H2O (C2H5OH/H2O = 0.90, by wt) at 35 ºC have been determined. The isotherms and refractive indices of the system at 35 ºC consist of 2 branches, corresponding to C6H12O6/H2O and NH4Cl. The composition of eutectic solution is C6H12O6: 4.40 %, NH4Cl: 13.86 %, C2H5OH: 38.88 %.

Phenylpropanoid Glycosides and Flavonoid Glycosides Isolated from Buds of Buddeja officinalis Maxim

Hu-Yi Zhang, Jing-Xian Pan

1996, 5(2): 105-108.

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Studies on the Chemical Constituents of Epimedium koreanum Nakai and Epimedium wanshanense S.Z.He et Guo

Wen-Kui Li, Pei-Gen Xiao, Ru-Yi Zhang

1996, 5(2): 109-110.

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