Journal of Chinese Pharmaceutical Sciences

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2010, 19(6): 405-408.

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Discovery and development of antiviral drugs

Zhen Zhang, Han Wang, Ling-Yan Du, Kun-Bo Chen, Su-Long Xiao, Fei Yu, Li-He Zhang, De-Min Zhou^*

2010, 19(6): 409-422. DOI: 10.5246/jcps.2010.06.056

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In this short review we summarize the different strategies for discovery and development of antiviral agents, including targeting virus entry into host, virus replication within cells, infant virus assembly and release from the infected cells. The progress on development of various classes of antivirus agents and their potential in virus therapy, mainly targeting human immunodeﬁciency virus (HIV), was also discussed.

Synthesis of acyclic analogs of Syringolin A as potential 20S proteasome
inhibitors

Yue Yuan, Xiao-Min Zou, Yan Niu, Feng-Rong Xu, Ke Mou, Bo Zhou, Chao Wang, Yong-Jian Li, Guan-Yu Yang, Ping Xu^*

2010, 19(6): 423-435. DOI: 10.5246/jcps.2010.06.057

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A series of acyclic analogs of natural product Syringolin A (SylA) were designed and synthesized during our synthetic efforts for SylA. These acyclic analogs were prepared through a seven-step linear strategy, with total yields varying from 20%-34% for one type of analogs and 12%-18% for the other. These compounds bear a common structure of peptidyl vinyl amide, which reacts irreversibly with the proteasomal active site Thr1O^γ through Michael-type 1,4-addition. Therefore, these acyclic analogs may function the same way as SylA, as potential 20S proteasome inhibitors.

A new strategy for the synthesis of 3-deazaneplanocin A

Tian-Shu Li, Shi-Fang Lu, Lei Xing, Gui-Chun Lin, Zhu Guan, Zhen-Jun Yang^*

2010, 19(6): 436-442. DOI: 10.5246/jcps.2010.06.058

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3-Deazaneplanocin A (3-DNPA, 2), an antiviral and antitumor agent, has been synthesized in an optimized procedure in 10 steps, with an increased overall yield of 11.2%. Started from 2,4-dihyroxyl-3-nitropyridine, reduction of nitro group and ring closure of imidazole were carried out in one pot, without the separation of diaminopyridine (10), to give 3-deazapurine (11). Moreover, the conversion of 6-chloro-3-deazapurine (12) to 6-amino-3-deazapurine (13) and the synthesis of N⁶,N⁶,N9-tris-Boc-3-deazadenine (16) was promoted by microwave-aid method. Compound 16 benefited the formation of N9 isomer of 3-DNPA in Mitsunobu reaction.

Adsorption and desorption of isoliquiritigenin and liquiritigenin to carbon nanotubes

Hai-Jiao Zhao, Chun-Hai Mu, Chao-Peng Li, Bo Han, Xin-Chun Wang, Wen Chen^*

2010, 19(6): 443-450. DOI: 10.5246/jcps.2010.06.059

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The adsorption and desorption of isoliquiritigenin and liquiritigenin to different types of carbon nanotubes (CNTs) were comparatively studied in this study. The pore structure, specific surface area, surface morphologies and functional groups of the CNTs were tested by N2 adsorption, scanning electron microscope (SEM) and infrared spectra (IR). The investigation of dynamic adsorption, isothermal equilibrium adsorption and desorption of isoliquiritigenin and liquiritigenin to CNTs demonstrated that the adsorption amount on oxidized multi-walled carbon nanotubes (o-MWCNTs) was greater than that on raw multi-walled carbon nanotubes (r-MWCNTs), especially the adsorption of isoliquiritigenin to o-MWCNTs. The data of equilibrium adsorption were better represented by the Freundlich isotherm model. In addition, the adsorbed amount per unit CNTs was decreased when the temperature got higher. From the results of isothermal equilibrium adsorption and desorption to CNTs, it could be inferred that o-MWCNTs had higher adsorption to isoliquiritigenin and liquiritigenin than r-MWCNTs. Additionally, o-MWCNTs had a better desorption efficiency to isoliquiritigenin and liquiritigenin (about 48.57% and 32.86%) than r-MWCNTs (about 24.56% and 17.46%).

Intestinal permeability of liquiritin and isoliquiritin in the Caco-2 cell monolayer model

Li-Qin Zhang, Ying-Dong Huang, Xiu-Wei Yang^*

2010, 19(6): 451-458. DOI: 10.5246/jcps.2010.06.060

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The intestinal permeability of two flavonoid compounds liquiritin (LQ) and isoliquiritin (ILQ) was investigated using the Caco-2 cell monolayer model. In order to evaluate the permeability and predict the absorption mechanism of the two compounds, the study on bidirectional permeability from the apical (AP) side to the basolateral (BL) side as well as from the BL side to the AP side was carried out. The determination was performed by HPLC-UV method. And the permeability parameters, especially the apparent permeability coefficients (Papp), were then calculated. The Papp values of LQ and ILQ are (5.40±0.16)×10^–7 and (8.69±0.15)×10^–7 cm/s, respectively. The results of time- and concentration-dependent transport experiments indicate that both LQ and ILQ are poor absorbed mainly through passive diffusion.

Quantification of eugenol and bancroftione in Caryophylli Fructus using high-performance liquid chromatography

Shu-Juan Liu, Zong-Tao Lin, Hong Wang, Shi-Zhong Chen^*

2010, 19(6): 459-463. DOI: 10.5246/jcps.2010.06.061

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For the first time, we have utilized high-performance liquid chromatography (HPLC) to simultaneously quantify the eugenol and bancroftione in Caryophylli Fructus. The optimized parameters included: Inertsil ODS-4 column (150 mm×4.6 mm, 5 µm); column temperature: 35 ºC; mobile phase: methanol-water (65:35, v/v); flow rate: 1.0 mL/min; detection wavelength: 280 nm. Eugenol and bancroftione showed good linear relationships with peak areas within the range of (0.0998-0.8982) mg/mL (r = 0.9999) and (0.1474-1.3266) mg/mL (r = 0.9999), respectively. The average recoveries were 102.52% and 100.96% for eugenol and bancroftione, respectively. Our results showed that the established method is simple, rapid, and accurate with good reproducibility to evaluate the quality of Caryophylli Fructus.

Simultaneous analysis of 12 bioactive constituents in Gegen Qinlian pill by HPLC-DAD

Li-Jun Song, Xiao-Mei Tan, Wen-Chang Zhao, Jia-Bo Luo^*

2010, 19(6): 464-470. DOI: 10.5246/jcps.2010.06.062

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In this study, a novel and simple high performance liquid chromatography with diode array detection (HPLC-DAD) method for the simultaneous qualitative and quantitative determination of 12 bioactive components in Gegen Qinlian pill was developed. The separation was performed on a Kromasil C18 column (250 mm×4.6 mm, 5.0 μm) by gradient elution with acetonitrile and 0.02 mol/L ammonium acetate (containing 0.3% triethylamine, and adjusted pH to 4.3 using 1% glacial acetic acid) as the mobile phase at a flow rate of 0.7 mL/min. Three different detection wavelengths (250, 280, 346 nm) were set at the maximum UV absorption wavelengths of these components. Twelve components (puerarin, daidzin, baicalin, wogonoside, liquiritin, berberine, palmatine, jatrorrhizine, glycyrrhizin, baicalein, wogonin and daidzein) were identified and determined using the developed method. All calibration curves showed good linear regression (r>0.9995) within tested ranges. The injection precision, intra-day precisions and analysis repeatability were evaluated with the RSD values, which were no more than 0.97%, 1.69% and 1.71%, respectively. The recoveries were ranged from 97.4% to 100.2% with RSD values less than 1.87%. This readily available, low-cost and reliable HPLC-DAD method would improve the quality control of Gegen Qinlian pill.

Determination of nifedipine concentration in human plasma by LC-MS and its application in pharmacokinetic study

Jing Zhang, Hao-Jing Song, Fan-Long Bu, Chun-Min Wei, Gui-Yan Yuan, Xiao-Yan Liu, Ben-Jie Wang, Rui-Chen Guo^*

2010, 19(6): 471-476. DOI: 10.5246/jcps.2010.06.063

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A sensitive and reproducible electro-spray ionization liquid chromatography-mass spectrometry (ESI-LC-MS) method was developed and validated to determine the concentration of nifedipine in human plasma. Following a simple liquid-liquid extraction with methylene chloride, nifedipine and nitrendipine (used as internal standard) were separated on a Diamonsil ODS column (150 mm×4.6 mm, 5 μm) by isocratic elution with acetonitrile-5 mmol/L ammonium acetate (52:48, v/v) at the flow rate of 1 mL/min, and detected by mass spectrometry in the selected ion monitoring (SIM) mode. The pseudomolecular ions [M+Na]⁺(m/z 369.0 for nifedipine and 383.1 for nitrendipine) were selected as the target ions for quantification with fragment electric voltage of 110 V for nifedipine and 100 V for IS. Method validation demonstrated that the developed method had excellent specificity and sensitivity, and acceptable precision and accuracy. Good linearity was achieved over a wide range of (2-600) µg/L (r²>0.998). The plasma samples were stable after storing for more than 14 d and after two freeze-thaw cycles (-20 °C to 25 °C). The method was successfully applied to clinical pharmacokinetic studies of nifedipine.

Influence of sex on the pharmacokinetics of modafinil in healthy Chinese volunteers

Long-Shan Zhao, Shuo Gao, Tao Guo^*, Dong-Ya Xia

2010, 19(6): 477-481. DOI: 10.5246/jcps.2010.06.064

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The purpose of this study was to determine the pharmacokinetic characteristics of modafinil and its metabolite modafinil acid in healthy subjects including Chinese Mongolian, Korean and Uyghur, and assess the influence of sex on the pharmacokinetic profiles of modafinil in Chinese subjects. Fifteen healthy Chinese male subjects and fifteen female subjects received 200 mg of modafinil, and the plasma samples were collected at the designed time points. The plasma modafinil concentration was determined by HPLC-UV method. Pharmacokinetic parameters were calculated by DAS software. The pharmacokinetics of modafinil for all of the subjects were in accordance with the two-compartment open model. The mean pharmacokinetic parameters for males and females are as follows: Cmax(4.39±0.53) and (5.86±1.23) μg/mL, AUC0-∞ (65.36±13.93) and (71.74±16.48) μg·h/mL, t1/2β (15.19±3.05) and (14.48±3.95) h for modafinil; Cmax (2.68±0.52) and (3.56±0.57) μg/mL, AUC0-∞ (29.99±6.05) and (34.53±6.41) μg·h/mL, t1/2β (6.46±1.31) and (5.35±1.46) h for modafinil acid, respectively. Statistical analysis of the pharmacokinetics of modafinil and modafinil acid in male and female groups shows that sex has a significant impact on the metabolism of modafinil and modafinil acid. More attention should be paid on the dosage to male or female patients.

Secondary metabolites from marine derived fungus Penicillium terrestre

Hui Liu, Jian Chen, Zhi-Wei Deng, Hua-Rong Huang, Wen-Han Lin^*

2010, 19(6): 482-486. DOI: 10.5246/jcps.2010.06.065

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Chemical examination of an unidentified sponge associated marine fungus Penicillium terrestre resulted in the isolation of eight compounds. Their structures are identified as cyclo (glycyl-D-proline) (1), cyclo (L-prolyl-L-alanine) (2), cyclo (L-prolyl-D-alanine) (3), cyclo (L-leucyl-trans-4-hydroxy-L-proline) (4), cyclo (L-leucyl-cis-4-hydroxy-D-proline) (5), cyclo (L-trans-(4-hydroxyprolinyl)-L-phenylalanine) (6), hexylitaconic acid (7), and hexylitaconic methylate (8), based on spectroscopic analysis (1D, 2D NMR). Compounds 7, 8 were obtained from the genus Penicillium for the first time, while compounds 1-6 were isolated from the fungus Penicillium terrestre for the first time.

Executive associate editor-in-chief of Journal of Chinese Pharmaceutical Sciences attended the 14th Conference of Chinese University Science and Technology Journal Council

Journal of Chinese Pharmaceutical Sciences

2010, 19(6): 487-487.

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Peking University Pharmaceutical Forum Opened on Nov. 27, 2010

Department of Natural Medicines

2010, 19(6): 488-488.

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