Journal of Chinese Pharmaceutical Sciences

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2007, 16(1): 1-04.

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Inhibition of cysteine protease papain by metal ions and polysulfide complexes,especially mercuric ion

Jun Jiang, Xiao-Da Yang^*, Kui Wang

2007, 16(1): 1-8.

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Aim Cysteine proteases are closely associated with many human and non-human pathological processes and are potential targets for metal ions especially Hg²⁺ and the related species. In the present work, on the basis of to the general study on the effects of some metal ions on the activity of papain, a well-known representative of cysteine protease family, the inhibitory effects of Hg²⁺ and polysulfide complexes were studied. Results All the metal ions tested (Hg²⁺, Cu²⁺, Ag⁺, Au³⁺, Zn²⁺, Zn²⁺, Cd²⁺, Fe³⁺, Mn²⁺, Pb²⁺, Yb³⁺) inhibit the activity of papain anda good correlation between the inhibitory potency and softness-and-hardness was observed. Among the metals, Hg²⁺ was shown to be a potent inhibitor of papain with a K_i of 2.7×10^-6mol·L^-1 among. Excessive amounts of glutathione and cysteine could reactivate the enzyme activity of papain deactivated by Hg²⁺. These evidences supported that Hg²⁺ might bind to the catalytic site of papain. Interestingly, Hg(II) polysulfide complexes were for the first time found to inhibit papain with a K_i of 7×10^-6 mol·L^-1, whose potency is close to a well known mercury compound, thimerosal (K_i= 2.7×10^-6). In addition, Hg(II) polysulfide complexes exhibit good permeability(1.9×10^-5cm/s) to caco-2 monolayer. Conclusion These results suggested that mercury polysulfide complexes might be potential bioactive species in the interaction with cysteine proteases and other- SH-content proteins, providing a new clue to understand the mechanism of the toxicological and pharmacological actions of cinnabar and other insoluble mercury compounds.

Investigation of the binding behavior of human serum albumin and phosphorothioate oligodeoxynucleotide

Guo-Zhu Ye, Liang-Ren Zhang^*, Li-He Zhang

2007, 16(1): 9-13.

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Aim To study the binding behavior between human serum albumin(HSA) and phosphorothioate oligodeoxynucleotide(PS-ODN) and the effects of bivalent cations on the interaction. Methods Surface plasma resonance, circular dichroism and fluorescence experiments were conducted. Results (1) the binding ability was decreased along with the increase of pH; (2) Zn²⁺ and Ni²⁺ enhanced the interaction between PS-ODN and HSA; (3) Upon PS-ODN binding, the conformation of HSA was changed with an increase of β-sheet. Conclusion The results provide experimental evidences to the hypothesis that PS-ODN binds with HSA in the positive potential region, and histidine residues located in the region play a crucial role in the interaction.

Effects of binuclear copper(Ⅱ)threonine complex on blood glucose, lipids and protection of the hearts and kidneys in diabetic mice

Ying Xie, Fei Wang, Fei-Fei Li, Ming-Sheng Li, Li-Li Deng^*

2007, 16(1): 14-17.

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Aim To study the effects of binuclear copper (Ⅱ) threonine complex (Cu₂(Thr)₄) as analogue of superoxide dismutase (SOD) on blood glucose, blood lipids and vessels of hearts and kidneys in diabetic mice. Methods Diabetic mouse model was established by intraperitioneal injection of alloxan. Low, middle, and high doses of Cu₂(Thr)₄ at 0.002%, 0.02% and 0.1% were given respectively to diabetic mice following lavage. The fasting blood glucose was determined after the diabetic mice were given Cu₂(Thr)₄ for 0, 30, and 45 d. The diabetic mice were killed on the 45th day. Then glycosylated hemoglobin(HbA1c) and blood lipids were assayed, and pathologic changes in hearts and kidneys stained with HE were observed. Results Compared with the control group in which the diabetic mice were given distilled water, the value of blood glucose reduced significantly in middle dose group (P< 0.01), followed by that in low dose group(P< 0.05). TC level reduced markedly and HDL level increased significantly in all three treatment groups (P< 0.05). Especially in middle dose group, cardiac muscle fibers were neatly arranged, nucleus and cytoplasm well distributed, glomeruli showing normal structure, cells well distributed and staining being normal. Conclusion Cu₂(Thr)₄ reduces blood glucose, regulates blood lipids, and play protective action on the vessels of hearts and kidneys in diabetic mice. The effects of it in middle dose were better than those of other doses.

A new guaianolide from the roots of Valeriana fauriei Briq.

Zhen-Xue Zhang^*, Jin-Zong You, Xin-Sheng Yao

2007, 16(1): 18-19.

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Aim To screen sedative constituents from Valeriana fauriei Briq. Result A new guaiane-type compound named as valerianin C was isolated from the roots of Valeriana fauriei Briq. Conclusion The new compound was elucidated as 8α-acetoxyl-3α,4α,10-trihydroxyl-guaia-1(2)-ene-12, 6α-olide on the basis of its NMR data, especially 2D-NMR techniques.

Chemical constituents of the unripe fruits of Evodia rutaecarpa

Xiu-Wei Yang^*, Jie Teng

2007, 16(1): 20-23.

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Aim To investigate the chemical constituents of the unripe fruits of Evodia rutaecarpa (Juss.) Benth. and provide a scien-tific basis for its quality control. Methods The compounds were isolated by silica gel column chromatography and identified by spec-tral analysis. Results Sixteen compounds were identified as evodiamine(1), rutaecarpine(2), β-sitosterol(3), isorhamnetin(4), evodol(5), quercetin(6), limonin(7), wuzhuyurutine A(8), evodirutaenin(9), shihulimonin A(10), wuzhuyurutine B(11), wuchuyuamide I(12), daucosterol(13), trans-caffeic acid methylate(14), dehydroevodiamine(15) and sucrose(16). Conclusion Compounds 4, 6, 10 and 14 were isolated from the title plant for the first time.

Studies on the chemical constituents of the active fraction of Gui-Zhi decoction

Shuo Zhou, Hong Liang^*, Shao-Qing Cai, Yu-Ying Zhao

2007, 16(1): 24-26.

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Aim To study the chemical constituents of the active fraction of Gui-Zhi decoction. Method The constituents were isolated and purified by column chromatography, and their structures were identified on the basis of spectral analysis. Result Six compounds, formononetin(1), liquiritigenin(2), isoliquiritigenin(3), 6-gingerol (4), (3S,5S)-1-(4-hydroxy-3-methoxyphenyl)-decane-3,5-diol (5), (3R,5S)-1-(4-hydroxy-3-methoxyphenyl) -decane -3,5-diol (6) were obtained. Conclusion All those compounds were isolated from the active fraction of Gui-Zhi decoction for the first time.

Chemical comparison of Artemisia borealis and three Chinese Artemisia plants

Fang Tian, Li Liu, De-Qiang Dou^*, Ting-Guo Kang, Smith David

2007, 16(1): 27-32.

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Aim To compare the chemical constituents of Artemisia borealis with three other Artemisia plants which are generally used in traditional Chinese medicine. Method The chemical components of essential oil from the leaves of A. borealis were analyzed by GC- MS and the chemical components of water extracts of the four plants were compared by HPLC fingerprint method. Conclusion From the essential oil of A. borealis, 52 peaks were separate, 48 of them were identified by GC-MS analysis, indicative that aromadendrane-4-ol is the highest constituent, which made up 24.73% of the total essential oil. In addition the chief constituents of the leaves of A.borealis are similar to the three other plants but its pattern of HPLC fingerprint is different. The content of chlorogenic acid in aerial part of A. annus and A. scapillaries, leaves of A. borealis and A. argyi are 0.065, 0.192, 0.617and 0.178 % respectively.

Induction and expression of T4 lysozyme gene in Pichia pastoris

Wen-Jing Hao, Gang-Qiang Li, Miao-Yun Xu, Zhao-Rong Wei, Hai-Min Chen, De-Hu Liu^*, Tie-Min Ai^*^*

2007, 16(1): 33-37.

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Aim To induce and express the T4 lysozyme in Pichia pastoris and test the antibacterial activity of the protein. Methods T4 lysozyme gene was inserted into expression vector pPIC9K of Pichia pastoris with the fusion at N terminal. The recombinant plasmid was digested by Sal I and then introduced into prepared GS115 competent cells by electroporation. Positive clone and multiple inserts were screened. The secreted proteins in the supernatants were tested. In the agar holes diffusion assay, our expressed protein showed significant antibacterial circles. Results T4 lysozyme protein inhibited the growth of staphylococcus aureus and streptococcus Pneumoniae. There was no difference in the bactericidal activity and the amount of protein expression between the single and multiple copies. The antibacterial activity of expressed protein remained the same during the heat stability test. Conclusion T4 lysozyme was successfully induced and expressed in Pichia pastoris. There is no relationship between copy number and expression. T4 lysozyme protein is heat stable.

Chemical constituents from Coriolus versicolor L.

Cheng Bi, Xiao-Yu Guo, Qing-Ming Che^*

2007, 16(1): 38-40.

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Aim To study the chemical constituents from Coriolus versicolor L.. Methods Chromatographic techniques were employed for separation and purification. The structures were identified on the basis of spectroscopic analysis. Results Eight compounds were isolated and identified as ergosta-7, 22-dien-3β-yl palmitate (1), ergosta-7, 22-dien-3β-ol (2), betulic acid (3), 4-hydroxy benzoic acid (4), 3- methoxy-4-hydroxy benzoic acid (5), 3, 5-dimethoxyl-4-hydroxy benzoic acid (6), 2-furoic acid (7), and nicotinic acid (8). Conclusion Eight compounds were reported for the first time from Coriolus versicolor L..

Total synthesis of rodgersinine A and B

Qiang Miao, Xin-Gang Xie, Ji-Yong Zhang, Xue-Gong She, Xin-Fu Pan^*

2007, 16(1): 41-42.

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Aim Syntheses of benzodioxane neolignans. Method The S_N2 reaction and Corey-Fuchs reaction was used to synthesize Rodgersinine A, 4-[3-methyl-7-[(E)-1-propenyl-2, 3-dihydro-1, 4-benzodioxin-2-yl]-1, 2-benzenediol (1) and Rodgersinine B, 4-[3-methyl-7-(1-propynyl)-2, 3-dihydro-1, 4-benzodioxin-2-yl]-1, 2-benzenediol (2). Results Total synthesis of Rodgersinine A and B was first completed. Conclusion A useful method for constructing benzodioxane neolignans by the S_N2 reaction is achieved.

Concise synthesis of oxy-bridged bicyclic azasugar and thiosugar as potential glycosidase inhibitors

Xiang-Bao Meng, Yan-Ping Li, Zhong-Jun Li^*

2007, 16(1): 43-46.

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Aim To develop a concise method for the synthesis of bicyclic azasugar and thiosugar with novel scaffold. Methods The two primary hydroxyl groups of compound 1 were selectively protected with tosyl cloloride in pyridine, followed by ring-closure with sodium sulfide or primary amine to form the oxy-bridged bicyclic molecules in good yields. Results Two bicyclic azasugars and a thiosugar were produced from L-sorbose in several steps. Conclusion The described procedures provide an efficient method to synthesize bicyclic azasugar and thiosugar with novel scaffold as potential glycosidase inhibitors.

Synthesis and stability evaluation of 5-FU-acetic podophyllic ester as anti-tumor agent

Rong Xiang, Fu-Min Zhang, Jing-Man Ni^*, Xuan Tian

2007, 16(1): 47-50.

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Aim To study a new anti-cancer drug 5-FU-acetic podophyllic ester derivatized from podophyllotoxin. Methods A novel derivative of podophyllotoxin was synthesized. Its inhibitory effects against P-388, A-549, Bel-7402 and HL-60 in vitro were tested. The stability tests under different kinds of conditions were carried out. Results The novel derivative showed stronger inhibitory activities against P-388, A-549 and Bel-7402 in vitro than VP-16. The novel derivative was found to be stable at 60 ℃ and 4500 lx light in solid-state, but was less stable in humid condition. It was more stable in methanol (4 ℃) and chloroform (25 ℃) than in methanol (25 ℃), and less stable in artificial gastric juice(AGJ, 37 ℃). Its stabilities were decreased while increasing the pH of buffer solutions. Conclusion These results could provide useful information for further study of this compound.

Preparation and physicochemical characterization of solid dispersion of quercetin and polyvinylpyrrolidone

Jing Zhu, Zhao-GangYang, Xiao-Mei Chen, Jia-Bei Sun, Gulisitan Awuti, Xuan Zhang^*, Qiang Zhang

2007, 16(1): 51-56.

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Aim The objective of this study was to prepare and characterize quercetin-polyvinylpyrrolidone (Qurc-PVP) solid dispersion with the intention of improving its dissolution properties. Methods Qurc-PVP solid dispersion was prepared by solvent method. The release rate of quercetin was determined from dissolution studies and the physicochemical properties of solid dispersion were investigated by differential scanning calorimetry (DSC), infrared spectroscopy (IR), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM). Results The results showed that the dissolution rate of quercetin was significantly improved by solid dispersion compared to that of the pure drug and physical mixture. Solubility studies revealed a markedly increase in the solubility of quercetin. The results of DSC and PXRD showed that the quercetin in solid dispersion was amorphous form. From SEM analysis, there was no quercetin crystal observed in the solid dispersions. Conclusion The solubility and dissolution of quercetin were improved by solid dispersion technique.

Preparation and bioavailability in healthy volunteers of cefaclor modified-release capsules

Lian-Dong Hu^*, Cheng-Wei Wang

2007, 16(1): 57-60.

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Aim To investigate whether modified-release cefaclor capsules could lead to a more suitable pharmacokinetic profile in the plasma. Methods Cefaclor pellets were prepared by extrusion/spheronization and coated by Eudragit L30D-55 or Eudragit NE30D, then the two sorts of pellets were filled to capsules in a 35:65 ratio to made a modified-release(MR) capsules. The bioavailability of the MR capsules was studied in 24 healthy volunteers after oral administration in a fast state using a commercially available immediate release(IR) capsule as a reference. Results The results showed that the MR formulation had a relatively good bioavailability compared with the commercial capsules, as well as a longer time keeping drug level above MIC than immediate release capsule. The relative bioavailability of the MR capsules was 97.4 ± 12.1%. Conclusion The data of the present study indicate that time of cefaclor plasma concentration above MIC can be substantially prolonged if cefaclor is administered as a modified-release product.

Pharmacokinetics of levosimendan administered as intravenous injection in Chinese healthy volunteers

Heng-Li Zhao, Xi Cui, Ben-Jie Wang, Hai-Sheng Wang, De-Qing Sun, Rui-Chen Guo^*

2007, 16(1): 61-64.

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Aim To investigate the pharmacokinetics of levosimendan administered as intravenous injection in Chinese healthy volunteers. Methods Twelve subjects were randomly divided into three groups. Each subject in the group 1 was administered at a single dose of 6 μg·kg^-1 levosimendan by intravenous bolus injection within 10 min, and then followed by intravenous infusion for 4 h at a dose per minute of 0.05 μg·kg^-1·min^-1. Similarly, each subject in the group 2(or group 3) was given by intravenous bolus injection at a dose of 12 μg·kg^-1 (or 18 μg·kg^-1) followed by an infusion at a dose of 0.10 μg·kg^-1·min^-1 (or 0.15 μg·kg^-1·min^-1) levosimendan. Blood samples were collected at 0 (prior to dosing), 0.17, 0.5, 1, 2, 3, 4, 4.25, 4.5, 4.75, 5, 5.5, 6, 7, 8 and 10 h after administrations. Levosimendan concentrations in plasma were measured by LC-MS/MS method. The pharmacokinetic parameters were calculated using a software Drug and Statistic(version 2.0). Results After administrations of levosimendan at various dose levels, the half-life(t_1/2) values were 1.50 ± 0.35, 1.64 ± 0.25 and 1.54 ± 0.39 h; the maximal concentrations after injections (C₀) were 9.54 ± 3.90, 15.95 ± 7.84 and 28.46 ± 10.74 ng·mL^-1; the areas under concentration-time(AUC_0-t (t = 7, 8)) were 33.63 ± 9.34,54.39 ± 15.34 and 78.36 ± 23.74 ng·mL^-1·h, respectively. Conclusion The C₀ and AUC_0-t values of levosimendan exhibited a dose-dependent manner, respectively. No differences in the pharmacokinetic parameters were observed between male and female Chinese subjects.

RP-HPLC determination of lycopene in microcapsules

Ding-Qiang Lu^*, Xiao-Yun Lu, Kai-Feng Lu, Ji-Jun Hu

2007, 16(1): 65-68.

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Aim A RP-HPLC method for determination of lycopene in microcapsules was established. Methods The HPLC assay was performed on an Alltima C₁₈(4.6 mm × 250 mm, 5 μm) column with a mixture of methanol-THF-water (66:30:4, V/V/V) as mobile phase at a flow rate of 1.5 mL·min^-1 and the UV detection wavelength was 472 nm. Results The linear range of lycopene was 3.6-18 μg·mL^-1, r = 0.9998, the average recovery was from 99.81% to 101.06% with RSD less than 1.83%. The RSD of intra-day and inter-day precision were less than 3.34%. Conclusion The method is simple, accurate and suitable for the determination of lycopene in microcapsules.

The Successful Opening of the First Conference of Number Three Editorial Committee of Journal of Chinese Pharmaceutical Sciences (English Version)

Journal of Chinese Pharmaceutical Sciences

2007, 16(1): 69-72.

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