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International Academic Conference Parallel Sessions1 On relationship between Mao Zedong and Chinese traditional culture Liu Nian’gui Social Science Department Abstract:Over the past two decades, the study on the topic of relationship between Mao Zedong and Chinese traditional culture has gradually turned out to be a hot and difficult spot. Only under the prerequisite of cleaning up the current research situation and the attitude of Mao Zedong toward Chinese traditional culture, can one deal with the issue how Mao Zedong transformed the traditional culture in a creative way and how was he deeply affected by it, thus enabling to point out the bi- directional interactive complicated relationship between Mao Zedong and Chinese traditional culture. Keywords:Mao Zedong, traditional culture, relations Self-Assembled lipid polymer hybrid nanoparticles: a robust drug delivery platform Xu Menglu Department of Pharmaceutics, School of Pharmacy Abstract:We report the engineering of a novel lipid polymer hybrid nanoparticle (NP) as a robust rug delivery platform, with high drug encapsulation yield, tunable and sustained drug release profile, excellent serum stability, and potential for differential targeting of cells or tissues. The NP comprises three distinct functional components: (i) a hydrophobic polymeric core where poorly water-soluble drugs can be encapsulated; (ii) a hydrophilic polymeric shell with antibiofouling properties to enhance NP stability and systemic circulation half-life; and (iii) a lipid monolayer at the interface of the core and the shell that acts as a molecular fence to promote drug retention inside the polymeric core, thereby enhancing drug encapsulation efficiency, increasing drug loading yield, and controlling drug release. The NP is prepared by self-assembly through a single-step nanoprecipitation method in a reproducible and predictable manner, making it potentially suitable for scale-up. Keywords: nanoparticle, encapsulate, stability, release Polyelectrolyte stabilized multilayered liposomes for oral delivery of paclitaxel Li Caibin Department of Pharmaceutics, School of Pharmacy Address: Rm.207 Building A , 639 LongMian avenue, University Town of JiangNing district, 211198 Tel: 15365078807 Email:[email protected] International Academic Conference Abstract:Paclitaxel (PTX) loaded layersome formulations were prepared using layer-by-layer assembly of the polyelectrolytes over liposomes. Stearylamine was utilized to provide positive charge to the liposomes, which were subsequently coated with anionic polymer polyacrylic acid (PAA) followed by coating of cationic polymer polyallylamine hydrochloride (PAH). Optimization of various process variables were carried out and optimized formulation was found to have particle size of 226±17.61 nm, PDI of 0.343±0.070, zeta potential of +39.9±3.79 mV and encapsulation efficiency of 71.91±3.16%. The developed formulation was further subjected to lyophilization using a universal stepwise freeze drying cycle. The lyophilized formulation was found to be stable in simulated gastrointestinal fluids and at accelerated stability conditions. In vitro drug release studies revealed that layer some formulation was able to sustain the drug release for 24 h; release pattern being Higuchi kinetics. Furthermore, cell culture experiments showed higher uptake of layersomes from lung adenocarcinoma (A549) cell lines as compared to free drug. This was subsequently corroborated by MTT assay, which revealed IC50 value of 29.37 mg/ml for developed layersome formulation in contrast to 35.42 mg/ml for free drug. The in vivo pharmacokinetics studies revealed about 4.07 fold increase in the overall oral bioavailability of PTX as compared to that of free drug. In vivo antitumor efficacy in DMBA induced breast tumor model showed significant reduction in the tumor growth as compared to the control and comparable to that of i.v. Taxol. In addition, the toxicity studies were carried out to confirm the safety profile of the developed formulation and it was found to be significantly higher as compared to Taxol. Therefore, the developed formulation strategy can be fruitfully exploited to improve the oral deliverability of difficult-to deliver drugs. Keywords: layersomes, paclitaxel, pharmacokinetics, antitumor efficacy, polyelectrolytes, nephrotoxicity Cypate for NIR photothermal triggered doxorubicin release from thermosensitive liposomes Han Zhihao Biochemistry, School of Life Science and Technology Abstract: Liposomes are promising drug delivery agents due to their biodegradability, large volume and biocompatibility towards both hydrophilic and hydrophobic drugs, resulting in decreased toxicity and prolonged circulation time. However, many obstacles hinder achieving a broad utility in drug delivery, such as their low ability to control the release of therapeutic drugs. A primary focus of this thesis involves the incorporation of cypate, a hydrophobic fluorescent endowed with photothermal conversion ability, into the thermosensitive liposomes bilayer to photothermally control the release of the hydrophilic drug, doxorubicin, loaded into the aqueous central area under NIR laser irradiation. Thermosensitive liposomes (TSL) were prepared by film hydration method. For the formulation study, Dynamic Light Scattering (DLS), Differential Scanning Calorimetry (DSC) and release studies were conducted in order to characterize the liposomes。 Address: Rm.207 Building A , 639 LongMian avenue, University Town of JiangNing district, 211198 Tel: 15365078807 Email:[email protected] International Academic Conference To photothermally control the release, cypate (CYP) was incorporated into the TSL. The characterization studies confirmed that cypate loaded into liposomes didn’t affect the thermosensitivity and not only it could by its photothermal conversion ability release the drug upon NIR laser irradiation, but it also increased the drug loading without destabilizing the liposome membrane at physiological temperature. The chosen formulation labeled the name DOX-PTSL (doxorubicin loaded photothermosensitive liposomes) was further studied in vitro and in vivo. DOX-PTSL had low cytotoxicity, well uptaken by the cells and only released its content inside the cells upon NIR laser irradiation. When injected into the tumor free mice, there was no sign of toxicity, the mice stayed active and their weight remained constant, in contrast to the free doxorubicin group that lost weight in three days after administration. In tumor bearing tumor models, DOX-PTSL accumulated in the tumors by EPR effect. They had major hepato-intestinal metabolism. DOX-PTSL treated group also exhibited a clear tumor growth suppression compared to others groups. Overall, DOX-PTSL could, after undergoing deeper studies, be proposed as potential drug nanocarrier for combined chemotherapy, thermotherapy and in vivo imaging. Keywords: liposomes, cypate, thermosensitive liposomes, dynamic light scattering. Transitional mental catalyze cross-dehydrogenation coupling Wang Chunmeng Department of Pharmaceutics, School of Pharmacy Abstract: Transition-metal-catalyzed coupling reactions have emerged as a powerful tool for the selective construction of C-C bonds as well as an integral part of organic synthesis. The new C-C bond is selectively formed at positions which are determined by the leaving groups on both substrates. Substantial research has introduced highly efficient catalyst systems which even allow the activation of challenging leaving groups. However, the use of any kind of leaving group inevitably results in the co-production of unwanted stoichiometric amounts of chemical waste. The double functionalization of C–H and heteroatom–H bonds, respectively, can be facilitated by employing an oxidant, which ultimately takes up both hydrogen atoms and constitutes a thermodynamic driving force. Such reactions are generally termed oxidative coupling or cross dehydrogenative coupling (CDC). CDC can helps to reduce the number of steps, costs and the amount of waste that fulfil some of the criteria of green chemistry. Keywords: transitional mental, C-H functionalization, cross dehydrogenative coupling. Address: Rm.207 Building A , 639 LongMian avenue, University Town of JiangNing district, 211198 Tel: 15365078807 Email:[email protected] International Academic Conference Parallel Sessions2 Emerging new therapies for the treatment of type 2 diabetes mellitus: glucagon-like peptide-1 receptor agonists Lin Huisheng Department of Pharmacology, School of Pharmacy Abstract: Purpose: The goal of this article was to review the safety, efficacy, and potential for utilization of the newly approved once-weekly glucagon-like peptide-1 (GLP-1) receptor agonists in the treatment of type 2 diabetes. Methods: Published articles for Phase III trials were found by performing a MEDLINE search using the search terms exenatide, exenatide once weekly, DURATION, albiglutide, and HARMONY as key terms.Search results were restricted by using filters to include clinical trials in humans. A search of relevant diabetes journals (including Diabetes Care and Diabetologia) was also performed to find abstracts for studies that did not have complete published articles at the time of this review. Findings: Exenatide once weekly reduced glycosylated hemoglobin (HbA1c) by –1.0% to –2.0% when used as monotherapy and add-on therapy; it also provided significant weight loss ranging from 2 to 4 kg and maintained a relatively low risk of hypoglycemia. Albiglutide was able to reduce glycosylated hemoglobin levels between –0.5% and –0.84% when used as monotherapy and in combination with other antidiabetic medications. The newest once-weekly GLP-1 receptor agonist, dulaglutide, reduced glycosylated hemoglobin levels between –0.78% and –1.51% and demonstrated noninferiority to once-daily liraglutide. Implications: The GLP-1 receptor agonists have proven efficacy in the treatment of type 2 diabetes and may provide patients with additional nonglycemic benefits, including significant weight loss and decreased systolic blood pressure. The newer once-weekly formulations are more convenient than the BID and once-daily medications, which could improve adherence and may be more attractive to providers and patients. Keywords: albiglutide, dulaglutide, exenatide, GLP-1 receptor agonists, liraglutide, lixisenatide. Isolation and primary culture of rat hepatic cells Zhang Xiaoxia Department of Pharmacology, School of Pharmacy Abstract: Primary hepatocyte culture is a valuable tool that has been extensively used in basic research of liver function, disease, pathophysiology, pharmacology and other related subjects. The method based on two-step collagenase perfusion for isolation of intact hepatocytes was first introduced by Berry and Friend in 1969 and, since then, has undergone many modifications. The most commonly used technique was described by Seglen in 1976. Essentially, hepatocytes are dissociated from anesthetized adult rats by a non-recirculating collagenase perfusion through the portal vein. The isolated cells are then filtered through a 100 μm pore size mesh nylon filter, and cultured onto plates. After 4-hour culture, the medium is replaced with serum-containing or Address: Rm.207 Building A , 639 LongMian avenue, University Town of JiangNing district, 211198 Tel: 15365078807 Email:[email protected] International Academic Conference serum-free medium. Primary culture of hepatocytes is an in vitro model widely used to study various aspects of liver physiology and pathology. For example, primary culture is used to assess the expression and function of drug-metabolizing enzymes including cytochromes P450, drug metabolism, drug-drug interactions, and the mechanisms of cytotoxicity and genotoxicity. Keywords: hepatocytes, isolation, primary, culture Platelets: a bridge for inflammation and thrombosis Cui Shuang Department of pharmacology, School of pharmacy Abstract: Platelets represent an important linkage between inflammation and thrombosis. Inflammation is characterized by interactions among platelets, leukocytes, and ECs. These interactions trigger autocrine and paracrine activation processes that lead to leukocyte recruitment into the vascular wall. Platelet-induced chronic inflammatory processes at the vascular wall result in development of thrombosis lesions and thrombosis. This research mainly explored the molecular mechanisms and inflammatory pathways used by platelets to initiate and accelerate thrombosis. Keywords: platelets, inflammation, thrombosis Industrial applications of metal–organic frameworks Li Li Department of Pharmaceutical Analysis, School of pharmacy Abstract: New materials are prerequisite for major breakthrough applications influencing our daily life, and therefore are pivotal for the chemical industry. Metal–organic frameworks (MOFs) constitute an emerging class of materials useful in gas storage, gas purification and separation applications as well as heterogeneous catalysis. They not only offer higher surface areas and the potential for enhanced activity than currently used materials like base metal oxides, but also provide shape/size selectivity which is important both for separations and catalysis. In the next an overview of the potential applications of MOFs in the chemical industry is presented. Furthermore, the synthesis and characterization of the materials are briefly discussed. Keywords:metal–organic frameworks, gas purification, applications Cell surface lactate receptor GPR81 is crucial for cancer cell survival Li Yao Department of pharmacology, School of pharmacy Abstract: The mechanisms that allow cancer cells to adapt to the typical tumor microenvironment Address: Rm.207 Building A , 639 LongMian avenue, University Town of JiangNing district, 211198 Tel: 15365078807 Email:[email protected] International Academic Conference of low oxygen and glucose and high lactate are not well understood. GPR81 is a lactate receptor recently identified in adipose and muscle cells that has not been investigated in cancer. In the current study, we examined GPR81 expression and function in cancer cells. We found that GPR81 was present in colon, breast, lung, hepatocellular, salivary gland, cervical, and pancreatic carcinoma cell lines. Examination of tumors resected from patients with pancreatic cancer indicated that 94% (148 of 158) expressed high levels of GPR81. Functionally, we observed that the reduction of GPR81 levels using shRNA-mediated silencing had little effect on pancreatic cancer cells cultured in high glucose, but led to the rapid death of cancer cells cultured in conditions of low glucose supplemented with lactate. We also observed that lactate addition to culture media induced the expression of genes involved in lactate metabolism, including monocarboxylase transporters in control, but not in GPR81-silenced cells. In vivo, GPR81 expression levels correlated with the rate of pancreatic cancer tumor growth and metastasis. Cells in which GPR81 was silenced showed a dramatic decrease in growth and metastasis. Implantation of cancer cells in vivo was also observed to lead to greatly elevated levels of GPR81. These data support that GPR81 is important for cancer cell regulation of lactate transport mechanisms. Furthermore, lactate transport is important for the survival of cancer cells in the tumor microenvironment. Keywords: GPR81, lactate transport, cancer cell survival Address: Rm.207 Building A , 639 LongMian avenue, University Town of JiangNing district, 211198 Tel: 15365078807 Email:[email protected] International Academic Conference Parallel Sessions3 A new synthetic sulfonylurea compound, inhibits the action of TXA2 in vivo and in vitro on platelets and aorta vascular smooth muscle Qian Lifen Pharmacognosy, School of Pharmacy Abstract: Aim: To study the inhibitory effects of I4,a totally synthetic new sulfonylurea compound ,and its mechanisms of action on TXA2 and TP. Methods: Platelet aggregation studies were performed on human platelet, rat whole blood platelet and rabbit platelet, platelets aggregation was induced by TP agonist U-46619(stable analog of TXA2, CAS 56985-40-1). Plasma TXB2 and 6-keto-prostaglandin F1α (6-keto-PGF1α) were used as markers to determine the effect of I4 on thromboxane synthesis. Fluo-3-AM was used to measure the cytosolic Ca2+ concentrations ([Ca2+]i) in rabbit platelet. Aorta rings with and without endothelium were prepared and aorta contraction was induced by U-46619.A model of type 2 diabetes mellitus was established by intraperitoneal injection of low dose of streptozocin to rats fed a high-calorie diet. Both normal rats and type 2 diabetic rats were used to assay the inhibitory effect of I4 on platelet aggregation induced by U-46619.Results: I4 exhibited a higher inhibitory potency than Glimepiride on U-46619 induced platelet aggregation in vitro and in vivo. I4 increased the ratio of plasma PGI2/TXA2 and decreased [Ca2+]i release from platelet internal stores. In addition, I4 presented a vasorelaxant activity on isolated rat aorta contraction induced by U-46619.Oral administration of I4 (1~10 mg/kg) markedly and dose-dependently inhibited platelet aggregation in both normal rats and type 2 diabetic rats. Conclusion: I4 significantly inhibited platelet aggregation induced by U-46619 in vitro and in vivo, and rat aorta contraction. It probably acts by partly blocking TXA2 action, decreasing the platelet intracellular Ca2+, and increasing the PGI2/TXA2 ratio. Keywords: I4, TXA2, TP antagonist, Ca2+ Resveratrol ameliorates trigeminal neuralgia by activating SIRT1 and limiting NLRP-3 inflammasome activation Liu Haijiao Department of Pharmacology, School of Pharmacy Abstract: Trigeminal nerve damage often leads to chronic pain syndromes including trigeminal neuralgia, a severely debilitating chronic orofacial pain syndrome. Options for treatment of neuropathic pain are limited in effectiveness and new approaches based on a better understanding of the underlying pathologies are required. Partial infraorbital nerve ligation (pIONL) effectively induced mechanical allodynia in mice lasting for more than a few weeks. It has been reported that resveratrol possesses diverse biochemical and physiological properties, including antioxidant, Address: Rm.207 Building A , 639 LongMian avenue, University Town of JiangNing district, 211198 Tel: 15365078807 Email:[email protected] International Academic Conference anticancer, antiproliferative, antifungal, antibacterial effects. We found that resveratrol may ameliorate trigeminal neuralgia in mice. Keywords: neuropathic pain, resveratrol, trigeminal neuralgia A discussion about aging Zhang Peiyan Department of Pharmacology, School of Pharmacy Abstract: Aging is an inevitable law of life process. It is a cascade of degenerative changes of tissues and organ functions with growing age. The potential anti-aging medicine based on the underlying aging mechanism has become the current hot issue in the gerontology. Research programs focusing of aging and anti-aging medicine have made great progress in recent years. This review first describes the recent advances in the aging research,followed by the factors influencing aging and then summary of the signaling pathways and their corresponding mechanisms in model organisms. After that,some potential anti-aging drugs discovered in recent years were discussed and pointed out the influence of drugs on future aging research. It will provide a reference for improving health and the quality of life in elderly people. Keywords: aging, anti-aging drugs, signaling pathway, research advances The effects of galangin on a mouse model of vitiligo induced by hydroquinone Luo Fen Department of Pharmacology, School of Pharmacy Abstract: This study was conducted to explore the anti-asthma effects of synthetic salidroside on cytokines and airway inflammation of asthma induced by diisocyanate (TDI) in mice. The experiment was carried out 60 female BALB/C mice which were randomly assigned to six experimental groups: control, vehicle, model, dexamethasone (2 mg/kg), and salidroside (24 and 48 mg/kg). After the experiment, histological studies were evaluated by the hematoxylin and eosin staining, the bronchoalveolar lavage fluid (BALF) and blood were collected from the animals, and the composition of the induced inflammatory cells, and the concentrations of certain cytokines (IL-4, INF-γ) were evaluated. GATA3 and T-bet mRNAs were evaluated by QPCR. Our study demonstrated that salidroside inhibited TDI-induced increases in eosinophil count; IL-4 and INF-γ were recovered. Histological studies demonstrated that salidroside substantially inhibited TDI-induced eosinophilia in lung tissue. Salidroside can improve T-bet mRNA and reduce GATA3 mRNA in lung. These findings suggest that salidroside may effectively ameliorate the progression of asthma and could be used as a therapy for patients with allergic asthma by regulating GATA3/T-bet balance. Keywords: salidroside, diisocyanate (TDI), asthma model, cytokines Address: Rm.207 Building A , 639 LongMian avenue, University Town of JiangNing district, 211198 Tel: 15365078807 Email:[email protected] International Academic Conference Alkaloids from stemona tuberose Zhang Lin Pharmacognosy, Department of Traditional Chinese Medicines Abatract: The roots of Stemona tuberosa have been used as an antitussive and insecticide remedy for thousands of years. Two new alkaloids, neotuberostemonine and bisdehydroneotuberostemonine were isolated from the roots of Stemona tuberosa, collected in Yunnan Province. Their structures were elucidated by various spectral methods. Keywords: Stemona tuberosa, Stemonaceae, roots, tuberostemonine alkaloids, neotuberostemonine bisdehydroneotuberostemonine Address: Rm.207 Building A , 639 LongMian avenue, University Town of JiangNing district, 211198 Tel: 15365078807 Email:[email protected]