Journal of Chinese Pharmaceutical Sciences

New Non-peptide Angiotensin Ⅱ Receptor Antagonists, 1. Substituted Quinoline Derivatives

Jiang Xuntan, Xu Tianlin, Hua Weiyi^*, Zhu Dongya, Yu Jing, Liang Shaomei

1999, 8(3): 123-134.

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The design, synthesis and angiotensin II(A II) antagonist activities of a series of quinoline derivatives (I~III) with ZD-8731 as lead compound are described. The biphenyl tetrazole moiety of ZD-8731 was replaced by bioisosteric N-phenylprrole carboxylic acid, N-phenylpyrroletetrazole and phenoxyphenylacetic acid to give compounds (I), (II) and (III), respectively. However,these changes proved to be detrimental to activities. In a test for amagonizing A II in vitro usingisolated rabbit aorta rings, all the compounds exeded competitive antagonism. The most potent active angiotensin II receptor antagoniSts of these series wee (Id) (pA2 = 6.8), (IIa) (pA2 = 7.7) and (IIIc) (pA2 = 7.2), respectively, which had the activity 1/40, 1/5 and 1/12 that of ZD-8731 (pA2 = 8.4), respectively. Their structure-activity relationships and conformational comparis0n are discussed.

Studies on the Interaction Between Eucalyptus Oil and Liquid Crystals of Skin Lipids

Dayo Abdullah, Ping Qineng^*, Liu Guojie

1999, 8(3): 135-141.

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The interaction of eucalyptus oil (EO) with skin lipid liquid crystals wasinvestigated by polarizing microscopy, DSC and X-ray diffraction. Two liquid crystals of model skinlipid were prepared. The liquid crystal l (matrix l) consisted of 5 fatty acids of stratum comeumwhile liquid crystal 2 (matrix 2) consisted of cholesterol together with 5 fatty acids. Lamellarstructure was formed in the matrix 1 and matrix 2 showed lamellar structure with maltese crosses.On the addition of EO to both liquid crystals, it was observed that small amount of EO partitioninginto the liquid crystaline structure caused dispersion and swelling of lamellar structure, while largeamount of EO resulted in the breakage and disappearance, but the EO did not promote the formation of any other structures. The interaction may be one of the explanations for the increasing permeationof drugs through stratum corneum in the presence of EO and similar penetration enhancers.

Kinetics of Crystal Growth of BDP and Its Solvates in Trichlorofluoromethane and Their Influence on the Performance of Metered Dose Inhalers

Mao Lei, Wang Juan, Bian Zuqing, Zhang Jun

1999, 8(3): 142-147.

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The purpose of this paper is to investigate the morphology change and crystalgrowth of fine particles of beclomethasone diopropionate (BDP), its ethyl acetate solvate (BDP-EtOAc) and trichlorofluoromethane solvate (BDP-P11) after contacting trichlorofluoromethane.Curves of crystal growth versus time were obtained and kinetic parameters of crystal growth were calcu1ated. The tendency and velocity of crystal growth were BDP>BDP-EtOAC>BDP-P11. K-values of crystal growth curves for BDP at 15℃ and BDP-EtOAc at 40 ℃ were 0.1637 μm·min^-1 and 0.0138 μm·min^-1 respectively. Final particle sizes of BDP were calculated and compared with measured values. Results of twin liquid impinger tests showed that BDP pressurized metered dose inhaler (pMDIs) prepared with BDP, BDP-EtOAc and BDP-P11 had deep lung drug deposition of 8%, 54% and 59%, dropping to 2%, 40%, and 57% after storage at 40℃, 75% RH for 2 weeks respectively.

Metabolism of Shikonin in Rats

Li Huiyi, Luo Shurong, Zhou Tonghui

1999, 8(3): 148-151.

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The metabolism of shikonin in rats was studied. Shikonin was administered (i.p.) to healthy, male Wistar rats pretreated with phenobarbital (PB, i.p., 60 mg·kg^-1, once a day, 3 d) by asingle dose of 20 mg·kg^-1, urine and bile were collected. The bile and urine samples wererespectively hydrolyzed with β-glucuronidase, extracted with ethyl acetate and the extractive concentrated in vacuum. The residues were dissolved in methanol and analyzed by a RP-HPLC/DADsystem for identification of shikonin metabolites. It has been proved that shikonin is metabolizedvery fast in the body and the metabolites are excreted mainly throngh the bile. The chromatograms and spectra showed that there were ten shikonin metabolites with similar UV spectra in the bile andurine respectively. The difference between in vivo and in vitro metabolic profiles of shikonin wasalso discussed.

Analysis of Chlorogenic Acid in Traditional Chinese Medicines with Capillary Zone Electrophoresis

Long Hong, Yang Jinjie, Liu Huwei, Wang Tiansong, Huang Aijin, Sun Yiliang^*

1999, 8(3): 152-157.

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A simple, rapid and versatile capillary zone electrophoresis method was developed for the determination of chlorogenic acid as a marker in traditional Chinese medicines. The buffer solution used was a solution consisting of 10 mmol·L^-1 phosphate and 20 mmol·L^-1 boric acid containing 5% ethanol with the apparent pH value adjusted to 7.00. The linear calibration range was 27.7~65 μg·mL^-1 (r =0.9996). The contents of chlorogenic acid in Flos Lonicerae and eight Flos Lonicerae containing Chinese medicines wee easily determined within 15 min with the sameprocedure.

Inhibitory Effect of EGb761 on Oxidation of Human Low Density Lipoproteins Induced by Cu²⁺ In Vitro

Xu Shangzhi, Liu Gengtao

1999, 8(3): 158-162.

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The effect of extract from leaves of Ginkgo biloba (EGb761) on the oxidation ofhuman serum low density lipoproteins (LDL) induced by Cu²⁺ in vitro was investigated . LDL waspretreated with EGb761 40, 80, or 160 mg·L^-1 for 1 h and then was oxidized by CuSO4 10 μmol·L^-1 for 10 h. It was found that after the oxidation of LDL induced by Cu²⁺, vitamin E (VE) in the oxidizedLDL (ox-LDL) was exhausted, while malondialdehyde (MDA) and lipofusion (LF) were markedlyincreased, the electrophoretic mobility of apolipoprotein B (apo B) was faster. EGb761 preveded thedecrease of VE and increases of MDA and LF in the ox-LDL, and slowed down the apo Belectrophoretic mobility in a dose-dependent manner. Therefore, EGb761 inhibits LDL oxidationinduced by Cu²⁺ in vitro.

Anti-allergic Effects of Low Molecular Weight Heparin

Wang Qingli, Shang Xueyuan, Zhang Shiling

1999, 8(3): 163-166.

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Low molecular weight heparin(LMWH), a newly developed biodrug, possesses multiple non-anticoagulant activities. Our results showed that LMWH at the concentrations of 16000and 8000 u·L^-1 could significantly (P<0.01, P<0.05 vs vehicle) inhibit constriction of isolated ileum smooth muscle of ovalbumin (OA)-sensitized guinea pigs induced by OA in vitro, LMWH 200, 50and 12.5 u·kg^-1 ip could markedly (P<0.01 vs vehicle) inhibit degranulation of pericranium MC in rats, LMWH 60 and 30 u·kg^-1 ip could significantly (P<0.01, P<0.05 vs vehicle) depress the licking response induced by 4-aminopridine and the increasing of capillary permeability induced by aceticacid in mice. These results indicated that LMWH in the dosages used in the present study possessed anti-allergic activity in several animal models, and the activity was related to its inhibitory effects on the degranulation of MC and to its anti-inflammatory effect.

Triptolide Induced Apoptosis of Eosinophils in Airway of Allergic Guinea Pigs

Wang Changzheng, Lai Kefang, Guo Xiaoming

1999, 8(3): 167-170.

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In this study, the effects of triptolide extract from a Chinese herb on eosinophilic apoptosis in allergic guinea pigs was explored. The .findings showed that triptolide could inhibit eosinophilic apoptosis and the expression of bc1-2 in eosinophils from allergic guinea pigs’ airway and would be of help in treatment of airway inflammation in allergic diseases such as asthma.

A Dipeptide Isolated from Aster tataricus L.f

Wang Zhengtao, Lu Yanhua, Ye Wencai, Xu Luoshan, Xu Guojun, Shu Yuezhong

1999, 8(3): 171-172.

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Studies on the Constituents from the Rhizoma of Alisma orientalis

Peng Xian, Tan Li, Yao Bing, Zhang Ruyi

1999, 8(3): 173-174.

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