Journal of Chinese Pharmaceutical Sciences

Graphical contents list

2009, 18(4): 289-292.

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Interference RNA induction and drug target validation

Xin Jin^#, Ting-Ting Sun^#, Qi Wang, Huan Xu, Tie-Jun Wei, Qiu-Chen He, Li-He Zhang, De-Min Zhou^*

2009, 18(4): 293-301.

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The ability to knockdown the expression of an endogenous gene by RNAi has emerged as a powerful strategy for the rapid identification of specific gene functions. Vector-based constitutive expression of shRNA can result in stable and efficient knockdown of target genes. However, constitutive expression of shRNA imposes major limitations when analyzing the function of genes whose expression is vital for the survival of an organism. Inducible RNAi systems can circumvent this limitation by enabling the inhibition of expression of an essential gene only when the inducing agent is present, and the level of knockdown of the essential gene can be controlled and adjusted by the concentration of inducing agent. In this review, we briefly summarize the recent development of various inducible RNAi systems and their potential applications in drug target validation.

Convenient synthesis of urea-linked hydroxyl-alkylamine derivatives of aminoglycosides

Pan Pan, Gui-Hui Chen, Xiang-Bao Meng, Ying Chen , Zhong-Jun Li^*, Shu-Chun Li^*

2009, 18(4): 302-312.

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A series of urea-linked hydroxyl-alkylamine derivatives of aminoglycosides have been obtained by modification of neamine (1), kanamycin (2) and ribostamycin (3) at 1, 6' and 3'' N-sites, respectively, through selective cyclization and nucleophilic ring-opening of cyclic carbamates. All the products showed no noticeable activity in the antibiotic test in vitro. The result suggests that the urea-linked hydroxyl-alkylamine derivatives of aminoglycosides may not be suitable structures for the enhancement of antibiotic activity.

Design and synthesis of L-5'-noraristeromycin analogues as potent antitumor agents

Min-Jun Huang, Zhen-Jun Yang, Liang-Ren Zhang^*, Li-He Zhang

2009, 18(4): 313-319.

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Nucleoside analogues show a variety of biological activities. To prepare new purine nucleoside analogues that could inhibit the proliferation of tumor cells and resist enzyme hydrolysis, we designed and synthesized 15 different L-5'-noraristeromycin analogues, in which thioether, sulfoxide or sulfone function was introduced to replace the 5'-hydroxymethyl group. Their anti-tumor activities were assayed in vitro. One compound showed potent anti-tumor activity.

Synthesis of a novel class of cyclophosphamide bis-spiropiperazinium salts

Mo Liu, Ze-Mei Ge^*, Tie-Ming Cheng, Run-Tao Li^*

2009, 18(4): 320-325.

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Based on the principle of association, a novel class of cyclophosphamide bis-spiropiperazinium compounds was designed and synthesized. A new method of synthesis, separation and purification for this kind of compounds was also developed.

Simultaneous determination of four nucleosides in Carthamus tinctorius L.
and Safflower injection using high-performance liquid chromatography

Fei-Ran Zhou, Ming-Bo Zhao, Peng-Fei Tu^*

2009, 18(4): 326-330.

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We quantitatively determined four nucleosides, including cytidine, uridine, guanosine, and adenosine, in Carthamus tinctorius L. and Safflower injection. Separation was performed on a Zorbax Eclipse XDB-18 column using a gradient elution with mobile phases of 0.05% trifluoroacetic acid (TFA) aqueous solution (A) and methanol (B). The assay was carried out at a flow rate of 1 mL/min at 25 °C with detection at 260 nm. Cytidine, uridine, adenosine and guanosine showed good linearity in the ranges of 4.02-603 μg/mL (r² = 0.9998), 9.38-1407 μg/mL (r² = 0.9999), 80.6-8060 μg/mL (r² = 0.9999) and 2.10-630 μg/mL (r²= 0.9987) with average recoveries of 97.2%, 94.5%, 98.6% and 108.6%, respectively. The contents of cytidine, uridine, adenosine and guanosine in different Carthamus tinctorius L. and Safflower injection were significantly different. This is the first report on the quantitative determination of nucleosides in Carthamus tinctorius L. and Safflower injection.

Cytotoxic and pro-apoptotic activities of medicarpin from Canavalia maritima
(Aubl.) via the suppression of NF-κB activation in HeLa cells

Min-Juan Xu, Xin-Ping Huang, Min Li^*, Wan Sun, Jing-Rong Cui, Wen-Han Lin

2009, 18(4): 331-336.

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Three known pterocarpin derivatives, (-)-medicarpin (PD1), (-)-2-hydroxy4,9-dimethoxypterocarpan (PD2), and 4-hydroxy-3-methoxy-8,9-methylene-dioxypterocarpan (PD3) were isolated from Canavalia maritima, for the first time. The cytotoxic and pro-apoptotic activities of (-)-medicarpin in cutured human tumor HeLa cells and its effect on NF-κB activation were investigated. We found that PD1 inhibited NF-κB activation by high content screening analysis, and PD1 exhibited cytotoxicity by SRB assay. In addition, we found that PD1 induced nuclear condensation and increased membrane permeability and mitochondrial transmembrane potential in HeLa cells in a dose and time dependent manner. In conclusion, our data suggested that (-)-medicarpin was capable of inhibiting tumor cell growth in vitro and inducing apoptosis, which might be via the suppression of NF-κB activation.

Synergistic effect of ethaselen and cisplatin treatment against tumor cell lines

Jing Li, Jia-Ning Fu, Qiang Tan, Hui-Hui Zeng^*

2009, 18(4): 337-341.

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The antitumor activities of ethaselen (BBSKE) in combination with cisplatin (CDDP) in vitro have been investigated in human stomach cancer cell line BGC 823 and human lung cancer cell line PG-BE1. MTT method was used to assess the individual effects of ethaselen and cisplatin and their combined effects on cell proliferation of BGC 823 cells and PG-BE1 cells. Additionally, we used the classic median effect theory to calculate the combination index (CI) of ethaselen and cisplatin with different dose regimes in combination, and compared the effective dosages of cisplatin in individual treatment and combination treatment. When ethaselen and cisplatin were used in combination, a synergistic effect was observed. The most remarkable synergistic effect was observed when the dose ratio of cisplatin to ethaselen was 2:3 in BGC 823 cell line and 1:3 in PG-BE1 cell line. The dose of cisplatin could be decreased markedly in combination group to reach the same inhibitory effect, and this effect was gradually raised with the increase of the concentration of drugs.

In vitro and in vivo evaluation of a self-microemulsifying drug delivery system for silybin

Xin-Ru Li, Yu-Sheng Pei, Yan-Qing Huang, Yan-Xia Zhou, Yu-Chen Zhang, Yan Liu^*

2009, 18(4): 342-347.

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To enhance the oral absorption of the poorly water-soluble drug silybin, a self-microemulsifying drug delivery system (SMEDDS) composed of ethyl linoleate, Cremophor EL and PEG 400 for oral administration of silybin was formulated, and its physicochemical properties and bioavailability of silybin were evaluated. The in vitro release of silybin from microemulsion and dispersion of silybin from SMEDDS were significantly faster than those from the commercial silybin hard capsule, respectively. The area under the drug concentration-time curve (AUC) and the mean maximum plasma level (Cmax) of the SMEDDS were remarkably greater than those of the hard capsule after oral administration to rats. The absorption of silybin formulated in SMEDDS exhibited a 2.3-fold increase in bioavailability as compared with the hard capsule. These results demonstrated that SMESDDS might be a useful drug delivery system for the oral delivery of the poorly water-soluble drug silybin.

A simple capillary zone electrophoresis method for the determination of mycophenolic acid in human plasma

Zhen Xiong, Jing-Li Duan^*, Suo-Di Zhai, Lei Zhao, Peng Xu

2009, 18(4): 348-353.

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Mycophenolic acid (MPA), an immunosuppressive drug, was determined in human plasma by a simple capillary zone electrophoresis (CZE) method. A bare fused-silica capillary with an internal diameter (i.d.) of 75 µm and an effective length of 50 cm was used for the separation. A 200 μL plasma sample was deproteinized with 400 μL acetonitrile, and the supernatant was directly injected into the capillary after a water plug at a pressure of 0.5 psi for 10 s. Boric acid (H3BO3, 200 mmol/L) solution adjusted to a pH of 8.60 with 1 mol/L sodium hydroxide (NaOH) solution was selected as the background electrolyte (BGE) through a uniform design. Calibration curve established on each day was linear over the MPA concentration range of 0.625-30.0 μg/mL in human plasma with the correlation coefficient (r) larger than 0.9997. The limit of detection (LOD) was 0.200 μg/mL. Intra- and inter-day precisions at three concentrations within the calibration range were less than 4.45%. Plasma samples collected from 14 renal transplant recipients treated with the prodrug mycophenolate mofetil (MMF) were analyzed successfully by both the developed CZE technique and a validated high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) technique. The mean absolute and relative differences between the concentrations measured by the two methods were -0.17 and -0.20%, respectively. In conclusion, the CZE method described here was validated to be accurate, precise, and economical for the clinical quantification of MPA.

A study of drug therapy problems in pharmaceutical care

Da Li, Hong Shao^*

2009, 18(4): 354-357.

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We evaluated the frequency and category distribution of drug therapy problems in young and elderly patients. A retrospective study of the medical conditions, drug therapies, and drug therapy problems identified in 102 patients was performed. The patients were divided into young patient group (<65 years of age) and elderly patient group (≥65 years of age) in a hospital pharmacy setting. Inclusion criteria: patients who were referred by the treating doctors and received evaluation by the clinical pharmacists. Exclusion criteria: patients who were unable to or refused to be evaluated by the clinical pharmacists. We found that 1) Patients in young and elderly groups had a mean of 3 and 5 medical conditions per person, respectively (P = 0.001). 2) On the average, they took 4 and 7 drug therapies per person, respectively. The elderly patients took a significantly higher number of drug therapies (P = 0.001). 3) Totally 85 drug therapy problems in 7 categories were identified within 102 patients. 4) 36.8% of young patients experienced 1 to 4 drug therapy problems whereas 61.8% of elderly patient experienced 1 to 5 drug therapy problems. Drug therapy problems were significantly more prevalent in elderly patients (P = 0.017). 5) The drug therapy problem by category had similar distribution in young and elderly patients. The elderly patients in this study encountered more drug therapy problems than young patients. Accordingly, more attention should be paid to elderly patients in pharmaceutical care practice.

Simultaneous quantitative determination of eight active components in
Polygonum multiflorum Thunb by RP-HPLC

Yan-Li Xu, Qi Dong, Feng-Zu Hu^*

2009, 18(4): 358-361.

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A sensitive and specific reversed-phase high performance liquid chromatography (RP-HPLC) method was established for the simultaneous quantitative determination of eight active components, two stilbenes (resveratrol, polydatin) and six flavonoids (rutin, quercitrin, quercetin, luteotin, isoorientin, kaempferol), in Polygonum multiflorum Thunb. The chromatographic separation was performed on a Kromasil C18 column (250 mm×4.6 mm, 5 μm), and gradient elution was carried out with water-methanol as the mobile phase at a flow rate of 1 mL/min. Stilbenes and flavonoids were respectively detected at 320 nm and 350 nm with DAD. The correlation coefficients of all the calibration curves were found to be higher than 0.9995. The average recoveries were ranged from 96.8% to 102.5% with RSD less than 4.8% for these components. RP-HPLC was validated to be a robust method for the quantitative determination of active components in Polygonum multiflorum Thunb, and it could be used in the quality control of this traditional medicine.

Review of a new book——Chemical Components of Source Plants in Traditional Chinese Medicine

Wei-Liang Weng

2009, 18(4): 362-363.

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Professors and Graduate Students from Peking University School of
Pharmaceutical Sciences Attended the Chinese Medicinal Chemistry
Symposium 2009

Jing-Jing Zhang

2009, 18(4): 364-365.

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