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	1. Synthesis and Biological Evaluation of Novel β-Carboline Derivatives as Antiproliferative Agents
	Jing Chen,Wenting Du,Xuefen Tao,Jiawei Huang,Yuliang Song
	Pharmacy 07 July 2013
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	Abstract:A series of novel β-carboline derivatives were synthesized and evaluated for their cytotoxic activities in vitro against two human tumor cell lines. Many of the compounds showed moderate to potent cytotoxic activities against the tested cell lines, in which compound 12l exhibited the most potent antiproliferative activities against KB cell line (IC50 = 4.58 μM). Preliminary mechanism research on compound 12l indicated it could inhibit DNA intercalation and tubulin polymerization.
	TO cite this article:Jing Chen,Wenting Du,Xuefen Tao, et al. Synthesis and Biological Evaluation of Novel β-Carboline Derivatives as Antiproliferative Agents[OL].[ 7 July 2013] http://en.paper.edu.cn/en_releasepaper/content/4545993


	2. Synthesis and Cytotoxicity of Novel 20-O-linked (±)-Homocamptothecin Ester Derivatives
	LI Dizao,Pan Xiandao
	Pharmacy 05 June 2013
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	Abstract:(±)-Homocamptothecin (hCPT) is a semisynthetic analogue of camptothecin (CPT) with a seven-membered β-hydroxylactone resulting from the insertion of a methylene (-CH2-) spacer between the alcohol moiety and the carboxyl group of the classical six-membered α-hydroxylactone ring of CPT. This E-ring modification provides a less reactive lactone with enhanced stability and decreased protein binding in human plasma and rather appears to improve instead of impairing its activity against topoisomerase I (Topo I) compared to CPT. In an attempt to improve the antitumor activity of homocamptothecins, a series of novel 20-O-linked hCPT ester derivatives were first designed and synthesized based on a synthetic route which acylates semi-synthesized (±)-homocamptothecin with different substituted phenoxyacetic acid ester derivatives. Most of the synthesized hCPT ester derivatives were assayed for in vitro cytotoxicity against six human cancer cell lines KB, KB/VCR, A549, HCT-8, Bel7402 and A2780 and most of the assayed compounds exhibited good antiproliferative activity on these tumor cell lines especially on KB. Here the synthesis and the in vitro antitumor evaluation of 20-O-linked substituted phenoxyacetic acid ester derivatives of (±)-hCPTs are reported.
	TO cite this article:LI Dizao,Pan Xiandao. Synthesis and Cytotoxicity of Novel 20-O-linked (±)-Homocamptothecin Ester Derivatives[OL].[ 5 June 2013] http://en.paper.edu.cn/en_releasepaper/content/4545343

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	3. Comparative studies of paeoniflorin and albiflorin from Chinese Paeony on Anti-inflammatory activities
	GAO Teng,WANG Qiangsong,CUI Yuanlu
	Pharmacy 20 May 2013
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	Abstract:Purpose: Chinese Paeony has been used for more than 1000 years in traditional Chinese medicine for the treatment of gynecological problems, cramp, pain, giddiness, and congestion. Paeoniflorin and albiflorin, monoterpene glycosides isolated from Chinese Paeony, possess a variety of pharmacological activities. The present study was investigated the anti-inflammatory activities of paeoniflorin and albiflorin using models of Lipopolysaccharides (LPS) induced RAW 264.7 cells. Methods: Production of nitric oxide (NO) was measured by the Griess colorimetric method and (ELISA). In addition, interleukin 6 (IL-6) and tumor necrosis factor alpha (TNF-α) synthesis were analyzed using enzyme-linked immunosorbent assay (ELISA). The protein expression of cyclooxygenase-2 (COX-2) was detected by cell-based ELISA. The gene expression levels of inducible nitric oxide synthase (iNOS), COX-2, TNF-α, IL-6 were detected by quantitative real-time reverse-transcription polymerase chain reaction (real-time RT-PCR). Results: The results showed that paeoniflorin and albiflorin could inhibit LPS-induced NO, TNF-α, IL-6 production and protein expression of COX-2. Furthermore, they could inhibit the mRNA expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), TNF-α, IL-6. Conclusion: These results show that albiflorin has the similar pharmacological effects to paeoniflorin on anti-inflammatory activities, which will provide a new evidence to pay albiflorin more attention to main quality control indicators of Paeoniae Radix and edit the new Chinese Pharmacopoeia.
	TO cite this article:GAO Teng,WANG Qiangsong,CUI Yuanlu. Comparative studies of paeoniflorin and albiflorin from Chinese Paeony on Anti-inflammatory activities[OL].[20 May 2013] http://en.paper.edu.cn/en_releasepaper/content/4544036


	4. CYP3A4 and CYP3A5 Polymorphism Effects on Tacrolimus Pharmacokinetics in Chinese Adult Renal Transplant Recipients: A Population Pharmacokinetic Analysis
	ZUO Xiaocong,Chee M. Ng,Jeffrey S.Barrett,LUO Aijing,ZHANG Bikui,DENG Chenhui,XI Lanyan,CHENG Ke,MING Yingzi,YANG Guoping,PEI Qi,ZHU Lijun,YUAN Hong,LIAO Haiqiang,DING Junjie,WU Di,ZHOU Yanan,JING Ningning,HUANG Zhijun
	Pharmacy 25 April 2013
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	Abstract:Objective Tacrolimus is used clinically for long-term treatment of antirejection of transplanted organs in liver and kidney transplant recipients though dose optimization is poorly managed. The goal of this study was to investigate the association between tacrolimus pharmacokinetic variability and CYP3A4 and CYP3A5 genotype by a population pharmacokinetic analysis based on routine drug monitoring data in adult renal transplantation recipients. Methods Trough tacrolimus concentrations were obtained from 161 adult kidney transplant recipients post-transplantation. The population pharmacokinetic analysis was performed using the nonlinear mixed-effect modeling software NONMEM version 7.2. The CYP3A41G and CYP3A53 genetic polymorphisms from studied patients were determined by direct sequencing using a validated automated genetic analyzer. Results A one-compartment model with first-order absorption and elimination adequately described the pharmacokinetics of tacrolimus. Covariates including CYP3A53 and CYP3A41G alleles and hematocrit were retained in the final model. The apparent clearance of tacrolimus was about 2-fold higher in kidney transplant patients with CYP3A53 and CYP3A41G higher enzymatic activity (with the CYP3A5 1/1 or 1/3 and CYP3A41/1G or CYP3A41G/1G) compared to those with lower enzymatic activity (CYP3A5 3/3 and CYP3A41/1). Conclusion This is the first study to extensively investigate the effect of CYP3A41G and CYP3A53 genetic polymorphisms and hematocrit value on tacrolimus pharmacokinetics in renal transplantation recipients. The findings suggest that CYP3A53 and CYP3A41G polymorphisms and hematocrit are determinant factor in the apparent clearance of tacrolimus. The initial dose design is mainly based on CYP3A5 and CYP3A4 genotypes as well as hematocrit.This results may also be good for the maintenance tacrolimus dose optimization and help to avoid fluctuating tacrolimus levels and improve the efficacy and tolerability of tacrolimus in kidney transplant recipients.
	TO cite this article:ZUO Xiaocong,Chee M. Ng,Jeffrey S.Barrett, et al. CYP3A4 and CYP3A5 Polymorphism Effects on Tacrolimus Pharmacokinetics in Chinese Adult Renal Transplant Recipients: A Population Pharmacokinetic Analysis[OL].[25 April 2013] http://en.paper.edu.cn/en_releasepaper/content/4530503


	5. Scaffold Evaluation of Liguzinediol Analogs as Novel Cardiotonic Agents
	LIU Zheng,LI Wei,QIN Kai,WEN Kan,ZHU Chenjian,LI Nianguang,BIAN Huimin,WEN Hongmei,CHEN Long
	Pharmacy 18 April 2013
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	Abstract:Liguzinediol (LZDO) could mediate the positive inotropic effects through sarcoplasmic reticulum Ca2+ ATPase-dependent mechanism without the risk of arrhythmia. However, the pharmacophore of LZDO contributed to the activities was not clear. The aim of this work is to explore the relationship between positive inotropic effect and scaffold of LZDO as well as to check whether the pharmacophore of LZDO on anti-heart failure activity was located at the pyrazine ring. A series of LZDO analogs (3a-b, 4a-b, 9-19) were designed and synthesised, and their activities were evaluated on isolated heart contractility by Langendorff perfusion. The results showed that the efficacy of LZDO was reduced when the hydroxyl, carboxyl or ester moieties at the side chain position of LZDO were induced, and the para-dihydroxy in LZDO was necessary for its activity. Thus, the pharmacophore of positive inotropic effect might be located at the whole scaffold of LZDO, but not at the pyrazine ring. The finding may provide important clue of pharmacophore for the development of novel cardiotonic agents.
	TO cite this article:LIU Zheng,LI Wei,QIN Kai, et al. Scaffold Evaluation of Liguzinediol Analogs as Novel Cardiotonic Agents[OL].[18 April 2013] http://en.paper.edu.cn/en_releasepaper/content/4538513


	6. Synthesis,Biological Evaluation,and Pharmacokinetic Study of Novel Liguzinediol Prodrugs
	LIU Zheng,LI Wei,WEN Hongmei,BIAN Huimin,CHEN Long,ZHANG Jing,CHEN Lei,YANG Kundi,FANG Qiuyue,CHEN Jing,FEI Yao
	Pharmacy 18 April 2013
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	Abstract: Liguzinediol (LZDO) ester prodrugs (3, 4, 5) were synthesized and evaluated in vitro and in vivo for its potential use, with the aim of prolonging the half-life of the parent drug LZDO (1a) in vivo. Prodrug 3, 4, 5 were found to be a potent positive inotropic effect on the myocardium without the risk of arrhythmia. Prodrug 3, 4, 5 rapidly underwent enzymatic hydrolysis to release the parent compound LZDO in 1-3 h in rat liver microsomes and rat plasma. The half-life of the parent compound was prolonged after intragastric administering prodrug 3. Prodrug 3 was found to be a superior prodrug candidate for increasing myocardial contractility.
	TO cite this article:LIU Zheng,LI Wei,WEN Hongmei, et al. Synthesis,Biological Evaluation,and Pharmacokinetic Study of Novel Liguzinediol Prodrugs[J].


	7. Design,synthesis and biological evaluation of novel asymmetric monocarbonyl analogues of curcumin (MACs ) as anti-inflammatory agents
	ZHANG Yali,ZOU Peng,ZHAO Chengguang,LIANG Guang,YANG Shulin
	Pharmacy 09 March 2013
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	Abstract:In the past several years, a lot of symmetric mono-carbonyl analogues of curcumin (MACs) have been designed and synthesized in our laboratory. In the recent study, Eleven asymmetric MACs were designed and synthesized. Their bioactivities were evaluated by inhibit LPS-stimulated macrophages release proinflammation cytokines TNF-α and IL-6. The compound 1d exhibit the most inhibit activity among the test compounds. These data show that asymmetric MACs might serve as potential agents for the treatment of inflammatory diseases.
	TO cite this article:ZHANG Yali,ZOU Peng,ZHAO Chengguang, et al. Design,synthesis and biological evaluation of novel asymmetric monocarbonyl analogues of curcumin (MACs ) as anti-inflammatory agents[OL].[ 9 March 2013] http://en.paper.edu.cn/en_releasepaper/content/4528456


	8. Synthesis and cytotoxicity of 3-arylacrylic ester derivatives of the simplified saframycin-ecteinascidin skeleton prepared from L-dopa
	DONG Wenfang,GUO Ju,LIU Wei,YAN Zheng,WANG Nan,LIU Zhanzhu
	Pharmacy 08 March 2013
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	Abstract:Fifteen simplified tetrahydroisoquinoline analogues were prepared from L-dopa. The in vitro antitumor activities of these analogues were evaluated against HCT-8, BEL-7402, BGC-823, A549, A2780, MCF-7 and MX-1 cell lines. The IC50 values of the cytotoxicity of most analogues were at the level of 10-7M or 10-8M. Compound 17 with 2,3,4-trimethoxycinnamate side chain at C-22 showed the most potent antitumor activity.
	TO cite this article:DONG Wenfang,GUO Ju,LIU Wei, et al. Synthesis and cytotoxicity of 3-arylacrylic ester derivatives of the simplified saframycin-ecteinascidin skeleton prepared from L-dopa[OL].[ 8 March 2013] http://en.paper.edu.cn/en_releasepaper/content/4527983


	9. A convenient way to synthesize bufadienolactam analogs with inhibitory activity against the prostate cancer cells
	Xiao-Feng Yuan,Hai-Yan Tian,Juan Li,Shu-Tai Jiang,Ken Wing-Keung Liu,David A. Middleton,Wen-Cai Ye,Ren-Wang Jiang
	Pharmacy 28 February 2013
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	Abstract:Bufadienolactam (1) and secobufalinamide (2) were synthesized by treatment of bufalin with ammonium acetate in DMF solution. Their structures were elucidated by extensive spectroscopic methods. The structure of 2 was further confirmed by single-crystal X-ray diffraction analysis. Compound 1 and 2 didn't inhibit the Na+/K+-ATPase. However, both compounds showed significant inhibitory activity against the androgen dependent prostate cell LNCaP with IC50 values of 9.0 μM for 1 and 14.0μM for 2. The fact that compounds 1 and 2 inhibited the prostate cancer cells but no inhibition on Na+/K+-ATPase indicated that they might be potential anti-prostate cancer agents without the cardiac toxicity.
	TO cite this article:Xiao-Feng Yuan,Hai-Yan Tian,Juan Li, et al. A convenient way to synthesize bufadienolactam analogs with inhibitory activity against the prostate cancer cells[OL].[28 February 2013] http://en.paper.edu.cn/en_releasepaper/content/4525029


	10. Design, synthesis, and biological evaluation of novel dual inhibitors of secretory phospholipase A2 and sphingomyelin synthase
	Gao Xing,Gong Haojun,Men Peng,Zhou Lu,Ye Deyong
	Pharmacy 06 February 2013
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	Abstract:The secretory phospholipase A2 (sPLA2) and sphingomyelin (SMS) are the key enzymes to atherosclerosis. A novel series of eight sPLA2 and SMS dual inhibitors containing indole and α-amino cyanide fragments respectively with different length carbon chain and substitution position were designed and synthesized. In vitro biological evaluation showed that all the compounds provided inhibitory effects against both SMS and sPLA2, in which, the SMS inhibitory activities were better than the positive control compound D609. The compounds 5b and 5e had moderate SMS inhibitory effects in liver homogenate and in SMS2 high expression cell homogenate respectively, as well as had ideal sPLA2 inhibitory activities.
	TO cite this article:Gao Xing,Gong Haojun,Men Peng, et al. Design, synthesis, and biological evaluation of novel dual inhibitors of secretory phospholipase A2 and sphingomyelin synthase[OL].[ 6 February 2013] http://en.paper.edu.cn/en_releasepaper/content/4519052

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