Journal of Chinese Pharmaceutical Sciences

Studies on the combinatorial modifications with two amino groups on the catalytic core of 10-23 DNAzyme

Pengyu Li, Zhiwen Li, Qi Wang, Junlin He

2017, 26(12): 851-857. DOI: 10.5246/jcps.2017.12.095

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As a small catalytic DNA molecule, 10-23 DNAzyme has cleavage ability against complementary RNA. Previous studies of chemical modification have shown that its catalytic core can be further optimized in order to obtain more powerful catalytic ability. The analogues of 2′-deoxyadenosine (5) and 2′-deoxyguanosine (6) could improve the cleavage ability of the DNAzyme when positioned at positions A9, G2 and G14 in the catalytic core. Moreover, their combinatorial incorporations were studied, the results implicated that the effect was position-dependent, and positive additive results could be achievedat some positions. The highly conserved G1, G2 and G14 could be optimized by single or combinatorial modification with 2′-deoxyguanosine analogues. Chemical modifications on the functional groups of the core residues would be a feasible approach for the optimization of 10-23 DNAzyme.

Synthesis, characterization and biological activities of Schiff bases derived from 2-hydroxy-3-nitrobenzaldehyde

Monisola Itohan Ikhile, Marthe Carine Djuidje Fotsing, Charmaine Arderne, Jane Catherine Ngila, Derek Tantoh Ndinteh

2017, 26(12): 858-871. DOI: 10.5246/jcps.2017.12.096

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Four novel Schiff bases were synthesized by the condensation reaction of 2-hydroxyl-3-nitrobenzaldehyde with either benzothiazoles or benzimidazolamines. The compounds 1–4 were characterized by spectroscopic and analytical methods. The crystal structures of 6-methoxy-1,3-benzothiazol-2-amine and compound 2 are reported only. The 6-methoxy-1,3-benzothiazol-2-amine was found to crystallize in the orthorhombic crystal system in the space group Pbca, having eight molecules in the unit cell, while compound 2 was found to crystallize in the monoclinic crystal system in the space group P2₁/c.The biological activities of these compounds were investigated by evaluating their antibacterial, antifungal, antimalarial, anti-HIV and anti-trypanosomiasis activities. These compounds displayed very interesting antibacterial, antifungal, antimalarial, anti-trypanosomiasis, anti-HIV and low cytotoxicity activity against HeLa cells.

Application of avidin-phospholipid vesicle complex as the stationary phase for chiral separation in open-tubular capillary electrochromatography

Ye Gao, Bailing Qiu, Qihui Liang, Di Wu, Yu Song, Nanyin Han

2017, 26(12): 872-880. DOI: 10.5246/jcps.2017.12.097

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In the present study, we developed a novel open-tubular capillary electrochromatographic method using avidin-phospholipidvesicle complex as the stationary phase for chiral separation of mexiletine hydrochloride. The avidin immobilized on the phospholipid vesicle consisting of 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE) and L-α-phosphatidyl-L-serine (PS) (80:20, mg%) was coated in the capillary. The homogeneity and separation performance of the coating were evaluated in terms of phospholipid vesicle characterization and the resolution of D,L-Tryptophan. As for mexiletine hydrochloride, four vital parameters affecting the separation efficiency of coating capillary, including buffer type, buffer pH, buffer concentration and the applied voltage, were studied in detail. Under the optimum conditions, the enantiomers could be separated well with good resolution. All the satisfactory results indicated that this method using avidin-phospholipid vesicle complex as the stationary phase was suitable and feasible, which had great potential in pharmaceutical separation of enantiomers.

Local drug interaction of metformin with carvedilol increases drug accumulation in the liver and kidney of rats

Yanrong Ma, Yanfang Wu, Yingting Duan, Xinan Wu

2017, 26(12): 881-889. DOI: 10.5246/jcps.2017.12.098

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Drug transporters determine plasma and tissue exposure of a broad variety of drugs and play a critical role in drug-drug interaction (DDI). In the present study, we aimed to investigate the effects of carvedilol on pharmacokinetics of metformin as well as the mechanism of their interaction. Results showed that plasma concentration of metformin was not significantly altered after single or 7-day co-administration of carvedilol, and the urinary excretion of metformin was also not influenced by carvedilol.However, the concentration of metformin in the liver and kidney was markedly elevated. Similarly, carvedilol did not affect the renal elimination of metformin, but increased renal concentration in isolated kidney perfusion. On the other hand, carvedilol treatment did not affect the expressions of rOCTs and rMATE1 in the liver and kidney of rats. After long-term co-administration, there were no differences in lactic acid (LCA), uric acid (URIC) and creatinine (CREA) levels between two groups. These results indicated that carvedilol increased hepatic and renal distribution of metformin, resulting in local drug interaction.

The clinical effect and safety evaluation of Shugan Quzhi capsule in the treatment of adult simple obesity

Zhiyan Lin, Huaiping Tian, Fang Li, Liping Qin, Xin Zhang, Xiaotong Lu

2017, 26(12): 890-894. DOI: 10.5246/jcps.2017.12.099

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Shugan Quzhi capsule is a hospital preparation of Xinhua Hospital affiliated to School of Medicine, Shanghai Jiaotong University. It has been used to treat adult patients with fatty liver caused by obesity, high cholesterol and other factors. In the present study, we investigated the clinical efficacy and safety of Shugan Quzhi capsule in adult simple obesity. The patients were randomly divided into the treatment group and control group. The whole treatment lasted 2 months under the same nutritional condition and diet intervention. Body weight, body mass index, total cholesterol, triglyceride, high-density lipoprotein cholesterol, low-density lipoprotein cholesterol, alanine aminotransferase, aspartate aminotransferase, blood urea nitrogen, creatinine, urine and blood routine examination were recorded before and after treatment. Our data showed that the total effective rate of treatment group was 66.67%, and body weight and body mass index after treatment the body were significantly decreased (P<0.01). The levels of total cholesterol, triglyceride, high-density lipoprotein and low-density lipoprotein after treatment were lower than before treatment, but there was no statistical difference (P>0.05). The total effective rate of control group was 39.13%, and the body weight and body mass index after treatment were also significantly lower than before (P<0.01). There was no significant difference between the treatment group and control group (P>0.05). There were no significant changes in liver function, renal function, urine routine and blood routine examination data after treatment. The results suggested that Shugan Quzhi capsule had certain therapeutic efficacy and safety in adult simple obesity.

Alpha-1-acid glycoprotein as potential predictive biomarker of docetaxel adverse effects in breast cancer patients

Weina Yu, Youyi Xiong, Zhuo Chen, Fang Wang

2017, 26(12): 895-899. DOI: 10.5246/jcps.2017.12.100

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In the present study, we aimed at identifying the potential relationship between baseline alpha-1-acid glycoprotein (AAG) and the adverse effects of docetaxel in breast cancer patients. A total of 87 breast cancer patients receiving docetaxel at a dose 75 mg/m² once every 3 weeks as a single agent in adjuvant and neoadjuvant chemotherapy were enrolled in this study. Baseline AAG was determined at the day before usage of decetaxel in the first cycle. Febrile neutropenia, grade 3–4 stomatitis, grade 3–4 diarrhea and severe asthenia was determined as safety end points. Common Terminology Criteria of AdverseEffects (CTCAE) V4.0 was used to evaluated the adverse effects during the first cycle of chemotherapy. The mean age of patients was47.7±8.89 years. Mean baseline AAG was 0.99±0.24 g/L. Primary adverse effects during the chemotherapy was febrile neutropenia (30%), grade 3–4 stomatitis (17%), grade 3–4 diarrhea(23%), and severe asthenia (20%). Among those adverse effects, febrile neutropenia, grade 3–4 stomatitis and grade 3–4 diarrhea had shown significant association with mean difference of baseline AAG (P<0.01). Patients who developed febrile neutropenia (n = 26) had lower baseline AAG level of 0.838±0.192 g/L compared with 1.051±0.236 g/L in patients who did not experience such effect (n = 61). Also, the level of baseline AAG in patients who had grade 3–4 stomatitis (0.760±0.176 g/L) and grade 3–4 diarrhea 0.800±0.172 g/L) is lower than those who did not had these events. Baseline AAG is appears to be used as a predictive biomarker of adverse effects in breast cancer patients treated with docetaxel.

Prof. Demin Zhou was awarded “Wuxi AppTec Life Science and Chemistry Awards 2017”

Lin Zhou

2017, 26(12): 900-900.

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2017年12月9日, 中国生命科学研究领域权威奖项, 第十一届“药明康德生命化学研究奖”在北京公布评选结果, 我院天然药物及仿生药物国家重点实验室周德敏教授获“杰出成就奖”。

The largest, most complex polysaccharide synthesized by Xinshan Ye and coworkers was voted as “Molecules of The Year” in Chemical & Engineering News

Shuxiang Song

2017, 26(12): 901-901.

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近日, 美国化学会旗下全球化学化工领域最有影响力的新闻杂志《化学与工程新闻》(Chemical & Engineering News, C&EN) 对本年度全世界化学化工领域的研究工作进行年终盘点, 发布了2017“年度分子”(Molecules of the Year), 我院叶新山教授课题组全合成的最大最复杂的多糖分子Arabinogalactan (Nat. Commun., 2017, 8, 14851)入选。