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	1. The treatment effect of igf-1 rice capsule in mice with T1DM and T2DM and the relationship with its dosage
	ZHOU Yi,XIAO Yuling
	Pharmacy 29 February 2016
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	Abstract:In the previous study,some high expression transgenic igf-1 rice was got and its treatment on diabetic mice had been tested. In order to improve the bioavailability of igf-1 and protect from being decomposed by the digestive enzyme, the rice power had been grinded into power and made into enteric capsule. The best recipe had been tested. Through the enzyme-linked immunosorbent assay (ELISA), the igf-1 content of the rice and the capsule were determined as well as the release rate of the capsule. Type 1 diabetes model and Type 2 diabetes model had been made to inspect the effects that igf-1 capsule has on diabetic mice. The main test contained the weight effect, water intake effect and the glucose effect of igf-1 in different dosage(1mg/g,0.5mg/g and 0.25mg/g). In this study, igf-1 had showed a better effect on mice with T2DM than T1DM,and the treatment effect was closely related with the doasge.
	TO cite this article:ZHOU Yi,XIAO Yuling. The treatment effect of igf-1 rice capsule in mice with T1DM and T2DM and the relationship with its dosage[OL].[29 February 2016] http://en.paper.edu.cn/en_releasepaper/content/4679229


	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


	3. The antinociceptive effects of endomorphin-2 analogs with N-methylated modifications at C-terminus
	WANG Changlin,DIAO Yuxiang
	Pharmacy 14 January 2014
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	Abstract:In endomorphins (EMs), the C-terminal amide is an important element that can interact with opioid receptor directly. Presently, the antinociceptive effects of endomorphin-2 (EM-2) and its analogs with N-methylated modifications at C-terminus were determined using tail-flick test. The results indicated that both analogs 1 and 2 produced potent antinociceptive effects by a central opioid mechanism. At the dose of 20 nmol/kg, the maximal %MPE values of analogs 1 and 2 were 65.4 ± 4.0 and 57.8 ± 3.1, respectively, similar to that of EM-2 (60.1 ± 5.8). It was noteworthy that analog 1 showed a higher antinociceptive effect compared to EM-2, which would be helpful in the development of suitable μ-opioid therapeutics. Overall, the present results indicated that the N-methylated modifications of EM-2 C-terminus produced significant central antinociception, and N-methylation of C-terminus of EM-2 may play an important role in the regulation of antinociceptive effects.
	TO cite this article:WANG Changlin,DIAO Yuxiang. The antinociceptive effects of endomorphin-2 analogs with N-methylated modifications at C-terminus[OL].[14 January 2014] http://en.paper.edu.cn/en_releasepaper/content/4582354


	4. Pro-apoptotic effects of tectorigenin on human hepatocellular carcinoma HepG2 cells
	DING Hui,SHI Dahua,LI Erguang,WANG Yurong,JIANG Chunping,WU Junhua
	Pharmacy 16 January 2012
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	Abstract:Tectorigenin, a main isoflavone in the Iris tectorum rhizome which was used traditionally for treating liver-related diseases, was shown to inhibit the growth of human hepatoma HepG2 cells, and to induce the cell apoptosis. In the apoptotic process, the intracellular ROS and Ca2+ elevation acted as an early event followed by depolarization of mitochondrial membrane potential (MMP). And then cytochrome c was released to cytosol. Moreover, the tectorigenin treatment co-enhanced the caspase-3, -8 and -9 proteolytic activities. In conclusion, tectorigenin significantly inhibited the proliferation and induced apoptosis in human hepatocellular carcinoma HepG2 cells mainly via mitochondrial-mediated pathway. And the death receptor-dependent pathway might play a certain role in the apoptotic process. These observations indicated that tectorigenin is the active principle of Iris tectorum rhizome applied in the folk medicine for alleviating liver disorders, and that the isoflavone is a promising candidate for hepatocellular carcinoma chemotherapeutic and chemopreventive agent.
	TO cite this article:DING Hui,SHI Dahua,LI Erguang, et al. Pro-apoptotic effects of tectorigenin on human hepatocellular carcinoma HepG2 cells[OL].[16 January 2012] http://en.paper.edu.cn/en_releasepaper/content/4461207

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