Table of Content

15 September 2002, Volume 11 Issue 3

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Journal of Chinese Pharmaceutical Sciences

2002, 11(3):  1-01. 

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Full Papers

Isolation and Identification of Steroidal Sapogenins from Total Sapogenin of Dioscorea Nipponica Makino

Du Shuhu^*, Liu Wenying, Fu Tiejun , Li Bogang, Xia Chongdao

2002, 11(3):  59-63. 

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Aim To investigate the water-soluble steroidal sapogenins from total sapogenins of Dioscorea nipponica Makino and to look for new active compounds. Methods The compounds were isolated with silica gel, PTLC and HPLC,and their structures were elucidated by acid hydrolysis, physical and chemical data and spectroscopic analyses (IR, NMR,MS, HMQC, HMBC) as well as chemical correlations. Results The two steroidal sapogenins (water-insoluble sapogenin and water-soluble sapogenin) were isolated from the total sapogenins of Dioscorea nipponica Makino. The structures were elucidated as diosgenin 3-O-{α-L-rhamnopyranosyl (1→2)-[β-D-glucopyranosyl (1→3)]}-β-D-glucopyranoside (I), diosgenin 3-O-[α-L-rhamnopyranosyl(1→3)-α-L-rhamnopyranosyl (1→4)-α-L-rhamnopyranosyl (1→4) ]-β-D-glucopyranoside (II). Conchusion Compound II is a new steroidal sapogenin and has been found in Dioscorea nipponica Makino for the first time . It was named dioscin Dc.

Screening of Common Traditional Chinese Drugs for Reversing Multidrug Resistance of KBV200 In Vitro

Zhang Qinglin, Zhao Jinghua, Cao Jurong, Song Jing, Bi Jianjin, Wang Xiaona, Gong Ping, Wu Zuze

2002, 11(3):  64-67. 

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The ethanolic extracts of 100 common traditional Chinese drugs, which are widely used in many prescriptions in treatment of cancer in China, were screened for MDR of KBV200 cell line in vitro with MTT method. The result showed 9 extracts having MDR reversal activity. They were the extracts of Fructus Lagenariae Sicerariae, Radix Glycyrrhizae, Poria, Herba Andrographitis, Radix Sophorae Tonkinensis, Caulis Mahoniae, Folium Artemisiae Argyi, Rhizoma Curcumae, Fructus Cnidii. Other 5 extracts showed cytotoxic on KBV200 cell line.

Synthesis of RGD-aPEG-Lactoside, A Potential Anti-metastasis Glycoconjugate

Niu Limin, Li Qing, Su Bin, Li Hui, Cai Mengshen, Li Zhongjun^*

2002, 11(3):  68-72. 

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The adhesive interaction between tumor cells and host cells or the extra cellular matrix plays a crucial role in metastasis. Due to the anti-metastasis effects of RGD (Arginyl-Glycyl-Aspartic acid) conjugated with PEG, hybrids of PEG armed RGD and oligosaccharides would have potential regulating effects during the metastasis process. In order to investigate this effect, GD-aPEG-Lactosid, RGD-aPEG-Lactoside glycopeptides armed by PEG were designed and successfully prepared by DCC-HOBt coupling method from aPEG-Lactoside, Boc-Gly-Asp(OBn)-OH.

Synthesis and Anticancer Activity of (E)-4-Acyloxypropenoic Acid Derivatives

Liu Yingxiang, Ji Zhizhong, Mu Xiaoshuo, Zhang Baofeng

2002, 11(3):  73-77. 

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Eighteen compounds of (E)-3-substituted-4-acyloxyphenylpropenoic acid were designed and synthesized, of which seventeen final target compounds had never been reported. Their chemical structures were determined by elementary analyses and IR as well as ¹H NMR, etc. Preliminary results of anticancer tests in vitro showed that compounds 3e, 3f, 3g,3h,3k,4h and 4j had significant anticancer activities on Ehrlich ascites carcinoma cells at 0.3 mmol·L^-1 concentration.

Preparation of Cyclosporine A Immunogen

Wu Qiongying, Dai Xiaoyan, Huang Wencai, Liu Yichao, Fan Xinjian, Chen Mina, Feng Ping

2002, 11(3):  78-82. 

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Cyclosporin A reacted with 4-benzoylbenzoic acid under ultraviolet radiation to give the conjugate of CsABBa. Then, the conjugate was linked to poly-L-lysine with the action of l-ethyl-3-(3-dimethylamino propyl)-carbodiimide hydrochloride to generate CsA immunogen. There were 13.1-17.4 molecules of CsA on each molecule of PL whose average molecular weight was 40 000. The coupling efficiency was fairly high and the constitution of CsA was maintained well.

Improvement on Preparation of Vinylmagnesium Chloride and Its Application

Li Anliang

2002, 11(3):  83-85. 

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An improvement on the preparation of vinylmagnesium chloride is described. The new approach prevents vinyl chloride from escaping and simplifies the operation. The important advantage is that it would get rid of -45°C deep cooling. The Grignard reagent was used to test its application and qualification for the synthesis of vimyl-β-ionol or 6-methoxy-1-vinyl-1-tetralol. The former is an intermediate of isotretinoin and the latter is an intermediate of mifepristone norgestrel or norgetriene.

Pharmacokinetics and Local Tissue Disposition of Piroxicam Following Topical and Oral Application in Rats

Li Yingjian^*, Pan Yan, Xu Hui, Wei Gang, Hao Jingsong, Zheng Junmin

2002, 11(3):  86-90. 

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Objective To investigate the drug delivery and mechanism of topical administration of piroxicam in rats. Methods Four milligrams of piroxicam were administered to Wistar rats by either oral or topical routes. The drug concentrations in plasma, local tissues were determined by HPLC. Results After oral application, the Tjoint/Plasma and Tmulcle/Plasma ratios kept unchanged. During most of the experimental time(0-24 h), the values varied between 0.06 and 0.2. In contrast,the Tjoing/Plasma and Tmuscle/Plasma ratios after local application varied from 0.2 to 1.26 and from 1.89 to 5.4 respectively and were much higher than the ones by oral application. Conclusion The results showed that most piroxicam reaching the local deep tissues was attributed to the direct penetration and topical delivery is superior to oral application when the drug's target is local tissues under skin.

Enhancing the Antitumor Effect of Adriamycin Nanoparticles by Pretreating Liver Cancer with Diethyldithiocarbamate

Wu Daocheng^*, Wan Mingxi, Mo Jian

2002, 11(3):  91-96. 

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Objective To examine the possibility of enhancing adriamycin nanoparticles antitumor effect by pretreating the tumor cells with diethyldithiocarbamate(DDC). Methods The cytotoxicity of adriamycin in cells was evaluated using MTT assay. Walk-256 carcinoma was transplanted to the livers of SD rats. Seven days later, the rats were divided into five groups, which were treated, respectively, by delivering saline(control), adriamycin, adriamycin nanoparticle lipiodol, a suspension containing DDC and adriamycin nanoparticle-lipiodol emulsion, a suspension containing DDC and adriamycin liposome lipiodol emulsion to the livers bearing carcinoma by injection through gastroduodenal artery. The distribution of adriamycin in rat tissues after administration was measured by HPLC. Results The value of the IC50 (μg·mL^-1) of ADM was reduced from 18-4 to 0-74 for the resistant cells SGC7901/CVR, and from 4.0 to 0.32 for the sensitive cells SGC7901/WT by pretreating the tumor cells with DDC. The volume of every tumor in the rats treated with both DDC and adriamycin nanoparticle- lipiodol or DDC and adriamycin liposome-lipiodol emulsion decreased after the treatment. The volume of every tumor in the rats treated only with ADM or adriamycin nanoparticle lipiodol still increased. The mean values of tumor growth rate(G%) in rats decreased greatly in groups pretreated by DDC than in adriamycin nanoparticle-lipiodol or adriamycin liposome-lipiodol emulsion groups. The life prolongation rate (LPR%) in the rats treated with both DDC and adriamycin nanoparticle-lipiodol or DDC and adriamycin liposome-lipiodol emulsion increased significantly than in the rats treated only with adriamycin or adriamycin nanoparticle-lipiodol. Conclusion The antitumor effect of adriamycin can be enhanced by inhibiting the SOD in tumor cells with DDC.

Formulation of Insulin-loaded Chitosan Nanoparticles: Influence of Factors on Entrapment Efficiency

Pan Yan^*, Li Yingjian, Zhao Huiying, Hao Jinsong, Zheng Junmin

2002, 11(3):  97-100. 

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A new approach for the preparation of hydrophilic chitosan nanoparticles (CS-NPs), based on an ionic gelation process, was established which was extremely mild and involved the mixture of two aqueous phases at room temperature.One phase contained polysaccharide chitosan (CS) and polyethylene oxide (PEO), and the other polyanion sodium tripolyphosphate (TPP). Size and zeta potential of the NPs could be modulated by varying the conditions for the preparation. The new NPs prepared in our experiment showed great entrapment efficiency of insulin up to 90% and various factors had an influence on it.This hydrophilic system might be a very promising carrier for administration of therapeutic proteins and other macromolecules that were susceptible to interact with CS.

A Stability-indicating HPLC Method for the Determination of Nateglinide in a New Tablet Formulation

Qi Meiling, Wang Peng, Wang Jun, Gu Junling, Fu Ruonong

2002, 11(3):  101-104. 

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A stability-indicating HPLC method is described for the determination of nateglinide in a new tablet formulation. Chromatographic separation was achieved using a mobile phase consisting of acetonitrile, methanol and phosphate buffer(70:4:20, v/v/v, pH 6.6) at a flow rate of 1.0 mL·min^-1 on a Hypersil BDS C18 column. Detection was carried out using a UV detector at 216 nm. The detector response was linear in the range of 4.94-49.4 μg·mL^-1 for nateglinide. The described method was validated with respect to selectivity, precision, accuracy and limits of detection and quantitation.

Effects of Benzyltetrahydropalmatine and Methoximine on Delayed Rectifier Potassium Channel Current in Guinea Pig Ventricular Myocytes

Li Yang^*, Fu Liying, Yao Weixing, Xia Guojin, Jiang Mingxing

2002, 11(3):  105-109. 

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Objactive To investigate the effects of benzyltetrahydropalmatine and methoximine on delayed rectifier potassium current (Ik) in guinea pig ventricular myocytes. Methods Whole-cell patch clamp technique was used to record Ik current. Results Methoximine 50 μmol·L^-1 augmented densities of Ik and Ik,tail from (12.4±1.8)pA pF^-1 and (4.2±0.5 )pA pF^-1 to (20.5±0.7)pA pF^-1 and (7.2±0.6)pA pF^-1 respectively. The effect of methoximine on the Ik and Ik,tail can be reversed by BTHP 30 μmol·L^-1, with the inhibition rates of 62.9%±4.3% and 61.1%±3.7%, respectively. When the cells were exposed only to 30 μmol·L^-1 BTHP, Ik and Ik,tail were blocked by 37.5%±6.0% and 35.9%±5.5%. Conclusion The results show that BTHP can inhibit the enhancing effect of methoximine on Ik in guinea pig ventricular myocytes.

Effects of Praeruptorin C on Vascular Hypertrophy, [Ca²⁺]_I, Collagen Content and Nitric Oxygen in Renovascular and Spontaneously Hypertensive Rats

Rao Manren^*, Liu Wanbin, Liu Peiqing, Wei Enhui

2002, 11(3):  110-114. 

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Aim To study the effects of praeruptorin C (pra-C), a pure constituent isolated from "Qianhu", the roots of Peucedanum praeruptorum Dunn (Umbelliterae), on vascular hypertrophy, collagen content, transient [Ca²⁺]i, NO and vascular response of the thoracic aorta of renovascular and spontaneously hypertensive rats (RHR, SHR). Methods RHR were given pra-C 20 mg·kg^-1·d^-1 for 9 weeks, ig. Blood pressurs of both rats were measured using tail cuff manometry. Under inverted microscopy the length and width of the smooth muscle cells were measured by using computer software MICC (Dongnan University). [Ca²⁺]i of smooth muscle cells (SMCs) was measured with Fura-2/AM. By measuring the specific amino acid hydroxyproline content, the collagen content was obtained. By using Griess reagent, the NO in the SMCs was measured. Results The intermedium of the thoracic aorta in RHR was larger than that of the normal and pra-C-treated groups. The area (length×width) of the SMCs of thoracic aorta from RHR was 73.4 μm vs normal 34.5 μm and pra-C 34μm. The collagen content of thoracic aorta was 39 ± 6.8 % dry weight in RHR, while 26.5 ± 3% in normal and 25.6 ±1.1% in pra-C treated RHR. The resting [Ca²⁺]i of SMCs was (150±8), (226±11) and (362±18) nmol·L^-1 separately in normal rats, RHR and SHR. In the presence of KCl 60 mmol·L^-1, NE 10 μmol·L^-1, ANG II 100 nmol·L^-1 and ATP 30 μmol·L^-1, the [Ca²⁺]i of SMCs were increased by 128%; 132%; 233% and 152% in RHR, respectively. Similarly, 60 mmol·L^-1 KCl and 10 μmol·L-1 NE also increased the [Ca²⁺]i of SMCs by 235% and 200% in SHR. Pretreating with pra-C could decrease the level of [Ca²⁺]i to the normal level whether in RHR or in SHR. The amount of NO of SMCs was decreased 76% in SHR compared with normal group, while pra-C could recover this change. In addition, pra-C improved the vascular responses of thoracic aorta of RHR. Conclusion These results indicate that pra-C improved the vascular hypertrophy by decreasing the area of SMCs, collagen content, SMCs [Ca²⁺]i and increasing NO production.

Communication

Study on the Terpene Compounds from Ligularia kanaitzensis

Li Yunsen, Wang Zhengtao^*, Zhang Mian, Luo Shide, Chen Jijun

2002, 11(3):  115-117. 

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