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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. Anti-Tumor Study of Novel Alkoxylamine analog RGD-Su-AP- PD0325901 Conjugates
	HOU Jianjun,HE Hongyan,LI Xiaoxiao,CHEN Zili,WU Yun
	Pharmacy 16 July 2015
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	Abstract:Peptide-drug conjugation is one of the most promising strategies for the targeting delivery of anti-cancer drug to specific group of cells to minimize the undesirable side effects and achieve the therapeutic effects with a low dose. The ideal peptide carriers induce receptor-mediated internalization by binding to special receptors which are only or more present on the tumor cell surfaces. In our study, we found that RGD peptide conjugated PD0325901 (MEK1/2 inhibitor) had good anti-tumor growth activity on both U87 and MCF-7 cell lines. Especially on U87 cells which are the αvβ3 integrin-positive tumor cells, the dimer RGD conjugate W10 (RGD2-Su-AP-PD) and PEGylated conjugate W11 (RGD-PEG4-Su-AP-PD) showed better inhibition effect than PD0325901. Comparing with the RGD targeting moiety, W10 (with dimer RGD peptide) exhibited significantly higher activity than W4(RGD-Su-AP-PD), and W4 much higher than non-RGD-conjugated W3. And this ability to inhibit the active ERK pathway by conjugates W4 or W10 was blocked by monoclonal antibody of integrin αvβ3 on U87 cells. Comparing with the monomer RGD conjugate W4, Dimer analog W10 showed more target-specific and higher anti-tumor activity. In peptide-drug conjugates, the linker between targeting cargo and pharmacophore is important for the conjugates to bind with cell membrane receptor and allosteric pocket of MEK kinase. Modifications with PEG have been used to enhance the bioavailability and the pharmacokinetic properties of RGD-MEKI conjugate. With the PEG4 linker, the conjugate W11 showed the highest anti-proliferation activity in conjugates. W11 inhibited the DNA replication as same as parent drug/PD0325901.
	TO cite this article:HOU Jianjun,HE Hongyan,LI Xiaoxiao, et al. Anti-Tumor Study of Novel Alkoxylamine analog RGD-Su-AP- PD0325901 Conjugates[OL].[16 July 2015] http://en.paper.edu.cn/en_releasepaper/content/4650332

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	3. 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


	4. Aldehyde Mediated Nitrosation of Amino Acid
	YANG Yue,LIU Zhiying,ZHANG Fang,TANG Erqing,DUAN Jianli
	Pharmacy 09 June 2015
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	Abstract:Everyday humans consume significant quantities of amino acids and sugars. Sugars are the major source of dietary aldehydes. Imines could be produced from the reaction between the amino acid and the sugars under gastric conditions and a possible N-nitroso Amadori comound product could be formed in the endogenous nitrosation process of imines. In this study, nitrosation of the imine salt 19 has been demostrated under the simulated gastric conditions. The resulting N-nitroso Amadori compound 11 was isloated by column chromatography and the 1H NMR and 13C NMR are identical with the standard compound.
	TO cite this article:YANG Yue,LIU Zhiying,ZHANG Fang, et al. Aldehyde Mediated Nitrosation of Amino Acid[OL].[ 9 June 2015] http://en.paper.edu.cn/en_releasepaper/content/4646252


	5. Studies Towards The Synthesis of N-nitrosolactones
	LIU Miao,LI Shanshan,CHENG Shuang,DUAN Jianli
	Pharmacy 07 May 2015
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	Abstract:TBS protected 3-β-azido-lactone is a very useful synthetic intermediate for the total synthesis of C-arylglycosides and other related compounds.Actually ,The 3-β-azido-lactone can be synthetized by a very route and highly stereoselective way in high yields.?????
	TO cite this article:LIU Miao,LI Shanshan,CHENG Shuang, et al. Studies Towards The Synthesis of N-nitrosolactones[OL].[ 7 May 2015] http://en.paper.edu.cn/en_releasepaper/content/4641141


	6. Prepatation, hydrolysis and antitumor activities of pachyman and their derivatives
	YANG Ming,YU Haiyan,CEN Yihong,RAO Zhigang,ZHOU Yi,ZHANG Fang,XIAO Yuling
	Pharmacy 05 May 2015
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	Abstract:Water-soluble pachyman (WSP) was prepared by enzymatic hydrolysis of water-insoluble pachyman extracted from the fresh sclerotium of Poria cocos. Carboxymethylated, sulfated, methylated and hydroxyethylated derivatives of WSP were synthesized, respectively. Their chemical structure were confirmed by infrared spectra and molecular mass were determined by gel permeation chromatography. The antitumor activities against Hela tumor cell and Sarcoma 180 tumor cell (S180) of WSP and all the derivatives were tested in vitro. It is showed that effective chemical components with lower molecular weight of pachyman contribute to the enhancement of antitumor activity.
	TO cite this article:YANG Ming,YU Haiyan,CEN Yihong, et al. Prepatation, hydrolysis and antitumor activities of pachyman and their derivatives[OL].[ 5 May 2015] http://en.paper.edu.cn/en_releasepaper/content/4640939


	7. Design, synthesis and prelimnary biological activity studies of dithiocarbamate-3-epi-Jaspine B hybrids
	Zhang En,Wang,Shang,Jiao,Wei-Wei,Xu,Jin-Mei,Liu,Hong-Min
	Pharmacy 17 April 2015
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	Abstract:A series of dithiocarbamate-3-epi-Jaspine B hybrids were designed and synthesized from D-xylose. Lipophilic long alkyl dithiocarbamate was introduced to C4 position of 3-epi-jaspine B in the new molecules. Their anticancer activity against two selected tumor cell lines (MGC-803 and B16-F10) were evaluated. Most synthesized compounds exhibited moderate activity against MGC-803 and B16-F10. Among them, compound 16d showed best inhibition against MGC-803 (IC50 = 16.39 μM). Compound 16f exhibited best inhibition against B16-F10 (IC50 = 14.83 μM). This is the first report about the synthesis and in vitro cytotoxic evaluation of dithiocarbamate -3-epi-jaspine B hybrids.
	TO cite this article:Zhang En,Wang,Shang,Jiao,Wei-Wei, et al. Design, synthesis and prelimnary biological activity studies of dithiocarbamate-3-epi-Jaspine B hybrids[OL].[17 April 2015] http://en.paper.edu.cn/en_releasepaper/content/4639429


	8. The Design of Pegylated Anticancer Drugs
	WANG Jinqiang,SHEN Youqing
	Pharmacy 04 January 2015
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	Abstract:Poly (ethylene oxide) was a water soluble non-immunological compound often used for preparation of polymer-conjugated drugs. High molecular weight PEG (>20 KDa) was used to dissolve drugs in water and prolong the circulating time in vivo. Linear and dentritic PEG-drug conjugate was developed to achieve the best in vivo result. In addition, low molecular weight PEG (<20 KDa) have also been used to increase water solubility in the form of nanoparticles and to introduce non-immunological property to prolong the circulating time. As described ind published reviews, the pegylated drugs were mainly focused on high molecular PEG, and most clinic or pre-clinic PEG-drugs followed this formulation. However, due to the development of nano-technology, pegylated nano-particles have also gone into pre- or clinic research. So it is necessary to have a whole introduction of this area. We will divided this area by the structure of the compounds and the drug. In the interest of brievity, we would mainly describe the anti-cancer small molucular compound drug, and protein would not be included in the review.
	TO cite this article:WANG Jinqiang,SHEN Youqing. The Design of Pegylated Anticancer Drugs[OL].[ 4 January 2015] http://en.paper.edu.cn/en_releasepaper/content/4626589


	9. Facile synthesis and cytotoxicity of 1'(N)-acetic acid esters of 20(S)-camptothecins
	LI Dizao
	Pharmacy 09 September 2014
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	Abstract:A series of novel 1'(N)-acetic acid esters of 20(S)-camptothecins (CPTs) have been synthesized and all of the esters were assayed for in vitro cytotoxicity against five human cancer cell lines A549, Bel7402, BGC-823, HCT-8 and A2780. The results showed that most of the assayed compounds exhibited good antiproliferative activity on these tumor cell lines. Here the synthesis and the in vitro antitumor evaluation of 20-O-linked substituted 1'(N)-acetic acid ester derivatives of CPTs are reported.
	TO cite this article:LI Dizao. Facile synthesis and cytotoxicity of 1'(N)-acetic acid esters of 20(S)-camptothecins[OL].[ 9 September 2014] http://en.paper.edu.cn/en_releasepaper/content/4608374


	10. Endoplasmic Reticulum Stress-induced hepatic stellate cell apoptosis through calcium-mediated JNK/P38 MAPK and Calpain/Caspase-12 pathways
	LI Xiaohui,WANG Yarui,WANG Huan,HUANG Cheng,HUANG Yan,LI Jun
	Pharmacy 11 March 2014
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	Abstract:Recent reports considered that it was the disturbance of calcium homeostasis and the accumulation of misfolded proteins in the endoplasmic reticulum (ER) that activated hepatic stellate cells (HSCs) apoptosis and promoted fibrosis resolution. However, the signal-transducing events that are activated by ER stress after HSCs activation were incompletely understood. In this study, we induced ER stress with thapsigargin (TG), and determined the activation of calpain and the cleavage of caspase by analyzing the protein levels and the correspondingly increased intracellular calcium levels and the induction of the proapoptotic transcription factor CHOP. Moreover, the phosphorylation of JNK/p38 MAPK was followed by the activation of the executioner caspases, caspase-3. As expected, preventing an increase in intracellular calcium levels using intracellular calcium chelators, EGTA and BAPTA/AM, could substantially inhibit the phosphorylation of JNK/p38 MAPK, abolish the activation of calpains, namely caspase-12, caspase-9 and caspase-3, and provide significant protection for TG-treated activated HSCs. Interestingly, pretreatment with p38 MAPK inhibitor SB202190, JNK inhibitor SP600125, the pan-caspase inhibitor z-VAD-FMK, or calpain inhibitors calpeptin, significantly reduced the cell apoptosis and the cleavage of caspase-12 and caspase-3. However, pretreatment with z-VAD-FMK failed to reduce the activation of calpain. Additionally, pretreatment with SB202190 and SP600125 also decreased the expression of CHOP. Importantly, PDGF-induced collagen Col1α1 and α-smooth muscle actin (α-SMA), markers for the perpetuation phase of HSCs activation, were inhibited in TG-treated activated HSCs. These findings showed that the calpain/caspase activation induced by ER stress and the JNK/p38 MAPK phosphorylation induced by the increase of intracellular calcium concentration releasing from ER are the novel signaling pathway underlying the molecular mechanism of fibrosis recovery.
	TO cite this article:LI Xiaohui,WANG Yarui,WANG Huan, et al. Endoplasmic Reticulum Stress-induced hepatic stellate cell apoptosis through calcium-mediated JNK/P38 MAPK and Calpain/Caspase-12 pathways[OL].[11 March 2014] http://en.paper.edu.cn/en_releasepaper/content/4589681

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