Table of Content

15 June 2002, Volume 11 Issue 2

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Journal of Chinese Pharmaceutical Sciences

2002, 11(2):  1-01. 

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Full Papers

A New Triterpene from the Fruits of Liquidambar formosana Hance-Lulutong

Li Chun, Sun Youfu, Sun Yuru

2002, 11(2):  1-4. 

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A new triterpene named 3α-acetoxyl-25-hydroxyolean-12-en-28-oic acid (4) was isolated from the ethanolic extract of Lulutong together with seven known compounds. Among them, compound 3 named 3-oxo-12α-hydroxy-oleanan- 28,13β-olide was for the first time isolated as a natural product. The structures of compounds 3 and 4 were elucidated by spectral analysis and by X-ray diffraction.

Synthesis and Antifungal Activity of 1-(1H-1,2,4-Triazole)-2-(2,4-diflurophenyl)-3-(N-methyl-N-substituted benzylamino)-2-propanols

Sheng Chunquan, Zhang Wannian^*, Ji Haitao, Zhou Youjun, Song Yunlong, Zhu Ju, Lu Jiaguo, Yang Song

2002, 11(2):  5-10. 

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Eleven 1-(1H-1,2,4-triazole)-2-(2,4-diflurophenyl)-3-(N-methyl-N-substituted benzylamino)-2-propanols were designed and synthesized, on the basis of the crystal structure of P450 cytochrome 14α-sterol demethylase(CYP51) and the docking results of inhibitors to the active site of the enzyme. All title compounds were first by reported. Results of preliminary biological tests showed that most of title compounds exhibited activity against the seven common pathogenic fungi. Compound 11 showed best antifungal activity with broad antifungal spectrum and proved to be more active against Cryptococcus neoformans, Candida albicans, Microsporum lanosum and Trichophyton rubrum than ketoconazole. Compounds 3, 10 and 4 also had high activities.

Structure-activity Relationship of Phenothiazines for Inhibition of Protein Kinase C and Reversal of Multidrug Resistance

Peng Hui, Yang Chunzheng^*, Qi Jing, Liang Wei, Huang Niu, Guo Zongru

2002, 11(2):  11-18. 

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Studies on structure-activity relationship of phenothiazines (PTZs) for inhibition of protein kinase C (PKC)and reversal of multidrug resistance (MDR) has been made in vitro. The results showedthat the order of potency of reversaleffect of PTZs on MDR is as follows: 2-COC3H7>2-CF3>2-COCH3>H. The type of piperazinyl substitution also signifi-cantly affected potency against MDR. The results show the order: CH3>COOC2H5>C3H4OH. In addition, PKC plays amarked role in diverse cellular process including MDR. Some derivatives of PTZ was tested for inhibition of PKC, of whichPTZ11 showed the highest inhibitory effect of MDR and PKC, implying a potential reversal agent of MDR for tumor therapy inthe future. We also tried to explore the possible binding model of PTZs to PKC. Our molecular-modeling study preliminarilysuggests how these PTZs bind to PKC and provides a structural basis for the design of high affinity PKC-modulator. The infor-mation may be used in the rational design of more effective drugs.

Synthesis and Antibacterial Effect of New Alkylenedibiguanides

Wang Yi, You Qidong, Zhou Weicheng

2002, 11(2):  19-21. 

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Seven new alkylenedibiguanides were synthesized and comfirmed by ¹H NMR, MS and elemental analyses. The preliminary test in vitro showed that some of them had potential antibacterial activities.

Determination of Barbaloin in Aloe vera L. var. chinensis (Haw.) Berger and Aloe barbadensis Miller by HPLC

Gao Jun, Dai Ronghua, Wang Xi, Sui Hong, Li Kang, Bi Kaishun^* 

2002, 11(2):  22-25. 

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A reserved-phase HPLC method was developed for the determination of barbaloin in Aloe vera L. var. chinen-sis (Haw.) Berger and Aloe barbadensis Miller, and whether there was a close relationship between the contents of barbaloinand their environments in which they were growing was decided. A Hypersil ODS column (4.6 mm×200 mm, 5 μm)was usedwith a mobile phase of methanol-water (40:60, containing 0.1% acetic acid), the flow rate being 1.0 mL·min^-1, detection wavelength at 359 nm, and the column temperature being 30°C. The linear range of barbaloin was between 0.0726 and 0.726μg with a correlation coefficient of 0.9998 and the regression equation being Y=1.9202×10⁶X-1801.9. Barbaloin was sta-ble in methanol in 48 h and the instrument precision was 1.2% while the method precision was 4.9%. The contents of barba-loin of 12 samples ranged from 6.160 to 319.1 μg·g^-1. The method developed was fast and simple with good reproducibility.There was high correlation between the contents of barbaloin and their growing environments.

High Performance Liquid Chromatography-Electrospray Ionization-Mass Spectrometric Analysis of Bilobalide and Ginkgolides in Ginkgo biloba L. Leaves

Lu Dingqiang^*, Wei Ping, Ouyang Pingkai, Chen Jun

2002, 11(2):  26-30. 

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The ginkgo terpenoids including bilobalide and ginkgolides are the main pharmaceutical components in theleaves or extracts of Ginkgo biloba L. In this paper, the analysis of bilobalide and ginkgolides in leaves of Girkgo biloba L. byhigh performance liquid chromatography (HPLC)-electrospray ionization (ESI)-mass spectrometry (MS) was carried out. Theseparation was performed on Inertsil ODS3 column with methanol-water (36:64) as mobile phase, with 1 mL·min^-1 of flowrate at 35°C. Then the mass spectrum analysis was conducted by ZMD micromass electrospray ionization (ESI)-mass spectrom-eter (MS). The HPLC total ion chromatogram and selected ion chromatogram (with 325,407,423,439 of m/z) of the sampleand ESI-/MS mass spectra of the peaks in the chromatograms were obtained. So bilobalide, ginkgolide A, B, C and J in Gink-go biloba L. leaves were identified. The method is easy and rapid, with a good accuracy.

Supercritical Fluid Extraction of Essential Oil from Dry Rhizome of Ligusticum chuanxiong Hort and Their Characterization by GC/MS

Hong Zhanying, Wang Xuezhao, Le Jian, Zhang Dongchun, Chai Yifeng, Liu Zhengliang

2002, 11(2):  31-34. 

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Supercritical fluid extraction (SFE) of essential oil from dry rhizome of Ligusticum chuanxiong Hort was de-veloped. GC/MS was used for the determination of the composition of essential oil. Forty-four compounds were identified. Theconventional extraction method was conducted in parallel for comparison. The extracts were qualitatively compared by GC/MS.The yields of SFE and steam distillation-extraction were 4.16%(v/w) and 0.8%(v/w), respectively. Application of SFE ofessential oil from dry rhizome of Ligusticum chuanxiong Hort was preferable.

Antiarrhythmic Efficacy of Neferine Assessed by Programmed Electrical Stimulation in a Canine Model of Electropharmacology

Guo Zhibin, Li Qing, Cao Hongyu, Xu Zhi

2002, 11(2):  35-42. 

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An ishemic ventricular tachyarrhythmias canine model was established in open-chest dogs subjected to programmed electrical stimulation (PES)for 5-8 days after acute myocardial infarction. The electrophysiologic effects of neferine (Nef) and procainamide (PA) were observed in this model. With routine methods of PES,ventricular tachycardia (VT)and ventricular fibrillation (VF) could be reproducibly initiated. Both drugs lengthened the QTc interval (P<0.01) and effective refractory period(ERP)of normal and ischemic ventricular myocardia (NERP and IERP) respectively (P<0.01), decreased the dispersion of ERP in ischemic myocardium and the dispersion of ERP in left ventricle (P<0.01), and increased the diastolic excitability threshold of normal and ischemic ventricular myocardia (P<0.01). The two compounds prevented the PES-induced VT or VF (Nef group P<0.01, PA group P<0.05) and ischemia-induced VF (P<0.05). The results indicated that neferine and procainamide may be effective in preventing the onset of reentrant ventricular tachyarrhythmias after myocardial ischemic damage in dogs.

Helicobacter Pylori-induced Gastritis Model in BALB/c Mice Infected With Fresh Isolates from a Human Complex Ulcer Patient

Ruan Guorui, Shi Junhua, Zhang Xueping, Chen Pingsheng, Yin Kezheng, Ge Peiling, Xu Manhua, Xu Xiangxi

2002, 11(2):  43-47. 

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A useful helicobacter pylori-induced gastritis model using BALB/c mice was established for mimicking of human gastritis induced by Helicobacter pylori (H. pylori). The H. pylori isolates were obtained freshly from a human complexulcer patient. BALB/c mice were fasted for 24 h and then 0.25 mL of 0.2 mol·L^-1 NaHCO3 was administered after by gavageto each mouse and 0.5 mL of 109 colonies formation unit per milliliter (CFU/mL) of H. pylori was administered 15 min. Onthe 3^rd day and 5^th day, the H. pylori inoculations were repeated. The inoculated mice were sacrificed in batch on the 5^th day, in the 2^nd week, 3^rd week and 4^th week. The gastric mucous membrane near pyloric portion was removed, treated and then cultured under microaerobic condition for detection of H.pylori. The remainders of the gastric membrane were fixed by 10% formaldehyde solution for pathological detection. The results showed that the H. pylori could be separated from the gastric membranes of inoculated mice. Obvious invasion of inflammatory cells in the gastric membranes of inoculated mice could be ob-served from pathologieal sections. It can be concluded that the inoculating fresh human H. pylori isolates can produce mousegastritis. This model of BALB/c mice can be used for evaluating the therapeutic agents for the treatment of gastritis induced by H. pylori.

Influences of Melatonin on the Growth of HeLa Cells

Chen Shaoya^*, Chen Chonghong

2002, 11(2):  48-51. 

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Aim To investigate the influences of melatonin (MT) on the growth of HeLa cells in vitro. Methods Theantiprolfferation activities of MT were evaluated in HeLa cells by means of trypan blue dye exclusion and MTT vital staining.The morphological changes of HeLa cells induced by MT were observed under transmission electronic microscope. Cell divisioncycle influenced by MT was assessed by a flow cytometry. Results MT produced a certain inhibition of HeLa cells at the con-centration of 2 mmol·L^-1 and prolonged the TD. The fraction of cells inhibited was 61.0%. The IC50 of HeLa cells exposed toMT for 96 h was 2.039 mmol·L^-1. The flow cytometric analyses showed that exposure to MT for 72 h reduced the number ofHeLa cells in phase S. Under electronic microscope, the HeLa cells exposed to MT for 72 h displayed morphological changesof necrosis, apoptosis, more hetero-chromosome and less somatic chromosome. Conclusion MT showed certain influences onthe growth of HeLa cells. Its mechanism may probably be attributable to reduction of the number of cells in phase S.

Communications

A New Disulfide from Garlic

Lu Maosong, Min Jimei^*

2002, 11(2):  52-53. 

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Anti-tumor Effect and Protective Effect on Chemotherapeutic Damage of Water Soluble Extracts from Hedyotis diffusa

Li Rui, Zhao Haoru^*, Lin Yining

2002, 11(2):  54-58. 

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