Journal of Chinese Pharmaceutical Sciences

A New Fluorenone Derivative from Dendrobium Chrysotoxum

Guo-Xiang Ma^**, Zheng-Tao Wang^***, Luo-Shan Xu, Guo-Jun Xu

1998, 7(2): 59-61.

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A new fluorenone derivative, named chrysotoxone (3) was isolated from the ethanolic extract of the stems of Dendrobium chrysotoxum (Orchidaceae), along with three known compounds. The structure of the new fluorenone was elucidated as 2,5,8-trihydroxy-1,4-dimethoxy-9-fluorenone.

Synthesis and Antibacterial Activities of 2-Substituted-6-oxo-8-fluoro-9-nitrogen-containing Heterocycle-6H-imidazo(4,5,1-ij)-quinoline-5-carboxylic Acids and Their Analogues

Wei-Cheng Zhou, Qing Liu, Zhen-Yu Xu, Ai-Zhen Yu, Xiu-Ping Zhang

1998, 7(2): 62-68.

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2-Alkyl-6-oxo-8-fluoro-9-(4-methylpiperazin-1-yl)-6H-imidazo(4,5,1-ij)-quino-line-5-carboxylic acids (2Ab~2Ae) were prepared by condensation of ethyl 6-fluoro-7-(4-meth-ylpiperazin-1-yl)-8-amino-1,4-dihydro-4-oxo-3-quinolinecarboxylate (5A) with the aliphatic acids in PPA. Other target compounds 2Af~2Ah, 2Bc, 2Cc, 2Aa~2Da, 2Bi and 2Ci were prepared by the condensation of 6-fluoro-7-nitrogen-containing heterocycle-8-amino-1,4-dihydro-4-oxo-3-quinoline-carboxylic acids (9A~9D) with the corresponding acids in PPA or with ethyl ortho-formate or by the diazotisation of 9B and 9C, respectively. Only 2Ab and 2Ac showed moderate antibacterial activity in in vitro test.

Improvement for the Synthesis of Centchroman

Xiao Shen Ji, Yi Miao, Yan Liu, Tao Jin, Peng Song

1998, 7(2): 69-71.

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The synthesis of centchroman has been improved. The hydrogenation under high pressure and configuration transformation in the reported route were omitted. The trans isomer was obtained in highly stereo selective Friedel Crafts alkylation and centchroman was obtained by five steps with the overall yield of 40%.

Ibuprofen-β-cyclodextrin Inclusion Complex: Preparation, Characterization, Physico-Chemical Properties and In vitro Dissolution Behavior

Gul Majid Khan, Jia-Bi Zhu

1998, 7(2): 72-79.

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Inclusion complexation between ibuprofen (IBF) and β cyclodextrin (β-CD) was investigated. Phase solubility studies of the complexation suggested the formation of a 1:3 complex and a 2:3 complex between IBF and β-CD at room temperature (23 ºC) and at 37 ºC respectively. Solid inclusion complexes were prepared by the homogeneous coprecipitation method. Scanning electron microscopy, differential scanning calorimetry, IR spectroscopy, and Xray diffractometry were used for the characterization and evaluation of the complexes. The solubility and dissolution rate of the complexes formed were found to have improved considerably over that of the physical mixture and the drug alone, indicating that β-cyclodextrin played an important role in the solubilization of ibuprofen.

Assessment of the Stability of Cefazolin Sodium in Solids by TGA Decomposition Kinetics

Chang-Qin Hu, Feng Zhang, Wei Liu, Shao-Hong Jin

1998, 7(2): 80-85.

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According to the analysis of the residual products by thermogravimetric analysis (TGA), the thermal decomposition process of cefazolin sodium (CEZ·Na) was thought to be similar to the degradation in solid state in its storage time. This laid a foundation for estimating the relative chemical stability of the drug by determination of its decomposition kinetics using TGA. Although the observed thermal decomposition kinetics of CEZ·Na was complex, a conversion level of 1% was chosen for evaluation of the stability of CEZ·Na crystalline since the mechanism here was more likely to be that of the actual product failure. The evaluation results suggested that the α form of CEZ·Na had the best stability and the amorphous one was the least stable one among α form, dehydrated α form and amorphous form.

Passive Electrical Properties of Animal Skin and Human Epidermal Membranes In vitro

Qi-Neng Ping, Ci-Ying Zhao

1998, 7(2): 86-90.

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The suitability of three animal skin species as the model for iontophoresis study was discussed based on the current density measurement, compared with the electrical properties of the human epidermal membrane (HEM) in vitro. The hydration during 48 h period significantly and continuously decreased the animal skin resistance and had much smaller influence on the HEM. The relationship between the pulse voltage and the current across these skin models was similar to those of HEM in different hydration status, but there were some variations in the extent due to the various sensitivities. The profiles could be simulated by the equation of V = (4ARF/T)Sinh^-1(BI). The parameters A reflected the sensitivity of the skin species to the electrical field. The hairless mouse skin and hairless guinea pig skin were more sensitive than the HEM, the sensitivity of the hairless rat skin was the lowest among the skin species. The results were further proved by the tests of long period voltage regimens, but it was found that significant alteration of the skin resistance occurred in the very short time as the electrical field was set up or discontinued.

Effects of Breviscapine on the Changes in Antioxidant Enzyme Activity Induced by Cerebral Ischemia-reperfusion in Rats

Xiao-Xia Chen, Bing He

1998, 7(2): 91-93.

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Effects of breviscapine, the active ingredient isolated from Erigeron breviscapus (Vant) Hand-mazz, on the changes in antioxidant enzyme activity induced by cerebral ischemia-reperfusion in rats were explored. It was found that breviscapine improved the activities of superoxide dismutase (SOD), GSH-peroxidase and catalase, while decreasing the malondialdehyde (MDA) content in the brain, which was benificial in reducing the damage from cerebral ischemia-reperfusion.

Effects of Tetrandrine on Cytosolic Free Calcium in Cultured Bovine Aortic Smooth Muscle Cells

Xin-Tian Li, You-Lin Wang

1998, 7(2): 94-97.

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The effects of tetrandrine (Tet) on cytosolic free calcium ([Ca²⁺]i) in subcultured bovine aortic smooth muscle cells (SMC) were studied by Fura-2 and AR-CM-MIC cation measurement system. Tet (1~100 μmol·L^-1) had no effect on the resting [Ca²⁺]i, but had inhibitory effects on [Ca²⁺]i elevation induced by high K⁺, 5-HT, ATP, Ang II and NE in the presence of extracellular Ca²⁺. High concentration of Tet also inhibited Phe-induced [Ca²⁺]i elevation in absence of extracellular Ca²⁺. Tet (1~100 μmol·L^-1) inhibited KCl (60 mmol·L^-1) induced [Ca²⁺]i elevation in dose-dependent manner, the IC50 value was 9.2 (95% confidence limits: 5.7~14.9) mmol·L^-1. The results suggested that Tet had blocking effects on both VOC and ROC in bovine aortic SMC. It appears that the mechanisms of blocking effect of Tet on ROC might be primarily due to its Ca²⁺ entry blocking effects.

The Chemical Constituents from the Roots of Bupleurum chinense DC.

Hong Liang, Yan-Jing Bai, Yu-Ying Zhao, Ru-Yi Zhang

1998, 7(2): 98-99.

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Studies on the Constituents of Aerial Parts of Scutellaria planipes

Yong-Yu Zhang, Yun-Zhen Guo, Hiroyuki Ageta, Yoshihiro Harigaya, Masayuki Onda, Kadsunori Hashimoto, Yukinobu Ikeya, Minoru Okada, Masao Maruno

1998, 7(2): 100-102.

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