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	1. Cyathane Diterpenoids of Macrofungi
	YIN Xia,CAO Chenyu,GAO Jinming
	Pharmacy 31 August 2015
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	Abstract:Cyathane diterpenoids, occurring exclusively in higher mushrooms, represent an important class of secondary metabolites, possessing a characteristic 5/6/7 tricyclic carbon scaffold. These compounds show a diverse range of biological activities, such as antimicrobial, anti-MRSA, agonistic toward the kappa-opioid receptor, anti-inflammatory, anti-proliferative and NGF-like properties. This review, citing 96 references, summarises their chemistry and bioactivities of cyathane diterpenoids isolated from higher mushrooms in the last four decades, to illustrate the chemo-diversity and biological significance of these diterpenoids.
	TO cite this article:YIN Xia,CAO Chenyu,GAO Jinming. Cyathane Diterpenoids of Macrofungi[OL].[31 August 2015] http://en.paper.edu.cn/en_releasepaper/content/4653605


	2. Crystal Structure and New Polymorphic Forms of Lorcaserin Hydrochloride
	LIU Song,ZHOU Mengqing,GU Jiali,GAO Haitao,ZHANG Guoqing
	Pharmacy 08 July 2015
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	Abstract:With the recrystallization method, a new lorcaserin hydrochloride form has been prepared, and compared with the original form. The two forms had been analyzed by using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermal gravimetric analysis (TGA), and scanning electron microscopy (SEM). The new form was confirmed exist, and it is different from t the original form. This is the first report about the lorcaserin hydrochloride new form .
	TO cite this article:LIU Song,ZHOU Mengqing,GU Jiali, et al. Crystal Structure and New Polymorphic Forms of Lorcaserin Hydrochloride[OL].[ 8 July 2015] http://en.paper.edu.cn/en_releasepaper/content/4649729


	3. 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].


	4. 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


	5. Determination of 5-Hydroxyindole-3-acetic acid, dihydroxyphenylacetic acid and homovanillic acid in the brains of freely moving rats using microdialysis coupled with HPLC-ECD
	LIU Rui,DUAN Jin-ao,GUO Jianming,TANG Yuping,QIAN Dawei
	Pharmacy 12 January 2013
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	Abstract:In present paper, microdialysis (MD) combined with high performance liquid chromatography with electrochemical detection (HPLC-ECD) was applied for the determination of 5-hydroxyindole-3-acetic acid (5-HIAA), dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) in the hypothalamus of LPS-induced hyperthermia rats. The extracellular neurotransmitters of 5-HIAA, DOPAC and HVA could be detected increasing significantly in rat brain 150 min after LPS injection. The result showed that dynamic change of neurotransmitters in rat brain could be determined easily by MD coupled with HPLC-ECD. Furthermore, the advantage that fewer animals sacrifice occurred in the microdialysis experiment was confirmed.
	TO cite this article:LIU Rui,DUAN Jin-ao,GUO Jianming, et al. Determination of 5-Hydroxyindole-3-acetic acid, dihydroxyphenylacetic acid and homovanillic acid in the brains of freely moving rats using microdialysis coupled with HPLC-ECD[OL].[12 January 2013] http://en.paper.edu.cn/en_releasepaper/content/4511624


	6. Synthesis and antidiabetic activity of 5,7-dihydroxyflavonoids and analogues
	Qin Nan,Chang Liushuan,Li Chunbao,Jin Meina,Duan Hongquan
	Pharmacy 15 January 2012
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	Abstract:Aim of the study: This is a study aiming to evaluate the structural elements essential to the antidiabetic activity of flavonoids. Methods: We synthesized two series of flavonoids, 5,7-dihydroxyflavanones and 5,7-dihydroxyflavones. Results: In a screening for in vitro potential antidiabetic activity, most of the flavonoids showed a remarkable in vitro activity, and compounds 5f, 7d, and 10c were significantly more effective than the positive control, metformin. Conclusion: The biological activity was mainly affected by introducing structural modification at the ring B moiety of the flavonoid skeleton. The results suggest that 5,7-dihydroxyflavonoids can be considered promising candidates in the development of new antidiabetic lead compounds.
	TO cite this article:Qin Nan,Chang Liushuan,Li Chunbao, et al. Synthesis and antidiabetic activity of 5,7-dihydroxyflavonoids and analogues[OL].[15 January 2012] http://en.paper.edu.cn/en_releasepaper/content/4462427


	7. 3D-QSAR and docking studies of suberoylanilide hydroxamic like analogues inhibitors of Histone deacetylase
	Bai Xue ,Min Ji ,Hongtao Wei ,Aijun Lu,Jian Liu
	Pharmacy 23 June 2009
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	Abstract:Histone deacetylase (HDAC) inhibition is a recent, clinically validated therapeutic strategy for cancer treatment. 3D-QSAR studies of some suberoylanilide hydroxamic acid (SAHA) like analogues were performed by comparative molecular field analysis (CoMFA) to rationalize the structural requirements responsible for the inhibitory activity of these compounds. The docking results provided a reliable conformational alignment scheme for 3D-QSAR model. Based on the docking conformations, highly predictive comparative molecular field analysis (CoMFA) was performed with a cross-validated q2 of 0.684. The non-cross-validated analysis with 3 optimum components revealed a conventional r2 value of 0.948, F=127.023, and an estimated standard error of 0.165. Furthermore, the 3D-QSAR models were mapped back to the binding site of the HDLP, to get a better understanding of vital interactions between the hydroxamic acids and the zinc. Based on the docking and CoMFA analyses, we have identified some key features in the histone deacetylase inhibitors that are responsible for HDAC inhibitory activity. The analyses may be used to design more potent histone deacetylase inhibitors and predict their activity prior to synthesis.
	TO cite this article:Bai Xue ,Min Ji ,Hongtao Wei , et al. 3D-QSAR and docking studies of suberoylanilide hydroxamic like analogues inhibitors of Histone deacetylase[OL].[23 June 2009] http://en.paper.edu.cn/en_releasepaper/content/33361

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