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Transactions of tianjin University 2019年第6期25卷 611-617页

作者： Yu Wang Xiaofei Cheng Hongxia Zhao Qingzhi Gao tianjin key laboratory for modern drug delivery and high-efficiency School of Pharmaceutical Science and Technology Tianjin University

Two novel sugar-conjugated 5-fluorocytosine(5-FC)antineoplastic compounds were designed and synthesized to improve the selective drug uptake by targeting the tumor-specific glucose transporter(GLUT).The antitumor activity of these compounds was evaluated in four different human cancer cell lines:A549(human lung cancer cell line),HT29(human colorectal cancer cell line),H460(human lung cancer cell line),and PC3(human prostate cancer cell line).The sugar conjugates exhibited cytotoxicity similar to or higher than 5-FC and 1-hexylcarbamoyl-5-FC in A549,HT29,H460,and ***,GLUT-mediated transport of the glycoconjugate was investigated with GLUT inhibitor-mediated cytotoxicity analysis in a GLUT-overexpressing HT29 cell *** cell-killing potency of 5-FC glycoconjugate was found to depend significantly on the GLUT inhibitor,and the cellular uptake of molecules was regulated by GLUT-mediated *** the results demonstrate the potential advantages of glycoconjugation for Warburg effect-targeted drug design.

关键词： Warburg effect Glucose transporter overexpressed 5-Fluorocytosine glycoconjugate Tumor targeting

Synergistic Effect of Mixed Cosurfactants on Transdermal delivery of Indomethacin from O/W Microemulsion

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Chemical Research in Chinese Universities 2013年第2期29卷 338-343页

作者： LING Ying YU Meng GUO Fang LI Nan TAN Feng-ping tianjin key laboratory of modern drug delivery and high-efficiency School of Pharmaceutical Science and Technology Tianjin University Tianjin 300072 P. R. China

t Since large amounts of oils, surfactants and penetration enhancers used in microemulsion systems might lead to seriously skin irritation, the percutaneous absorption and penetration of indomethacin（IMC, model drug） from O/W microemulsion were enhanced by simply changing the composition of cosurfactants. Pseudo-ternary phase dia- grams were constructed with mixed cosurfactants at different ratios. Hairless rat skin was used as a barrier for per- meation experiments. Four formulations were prepared with fixed oil, surfactant and different cosurfactant con- tent（4%, 20% and 20%, mass fraction）, and formulation F4 with menthol added was evaluated to compare the en- hancement effect of it with those of mixed cosurfactants. The O/W microemulsion region was the largest when the mass ratio of ethanol/transcutol was 1：1. However, the region changed slightly for the system with incorporated mixed cosurfactants propylene glycol/transcutol. The flux and skin retention of IMC from O/W microemulsion with mixed cosurfactants were much higher than that with single cosurfactant（P〈0.01）, while incorporation of menthol would only enhance the drug flux through the skin. To conclude, mixed cosufactants could affect the phase behavior and improve the percutaneous absorption and penetration of IMC. Based on this, it provided a promising solution to enhance drug release from microemulsions without raising potential skin damage.

关键词： O/W microemulsion Mixed cosurfactant Transdermal drug delivery Menthol

The applications of hypervalent iodine(Ⅲ) reagents in the constructions of heterocyclic compounds through oxidative coupling reactions

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Science China Chemistry 2014年第2期57卷 189-214页

作者： ZHENG ZiSheng ZHANG-NEGRERIE Daisy DU YunFei ZHAO Kang tianjin key laboratory for modern drug delivery & high-efficiency School of Pharmaceutical Science and Technology Tianjin University Collaborative Innovation Center of Chemical Science and Engineering (tianjin)

Hypervalent iodine(Ⅲ)reagents have been vastly used in many useful organic *** this review article,we highlight the strategies that used the common hypervalent iodine(Ⅲ)reagents as oxidants to synthesize the heteroc... 详细信息

关键词： hypervalent iodine(III) reagent oxidative coupling bond formation strategy heterocycles

Advances in biosynthesis of triterpenoid saponins in medicinal plants

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Chinese Journal of Natural Medicines 2020年第6期18卷 417-424页

作者： YAO Lu LU Jun WANG Juan GAO Wen-Yuan tianjin key laboratory for modern drug delivery and high efficiency School of Pharmaceutical Science and TechnologyTianjin UniversityTianjin 300072China key laboratory of Systems Bioengineering Ministry of EducationTianjin UniversityTianjin 300072China

In recent years, biosynthesis of triterpenoid saponins in medicinal plants has been widely studied because of their active ingredients with diverse pharmacological activities. Various oxidosqualene cyclases, cytochrome P450 monooxygenases, uridine diphosphate glucuronosyltransferases, and transcription factors related to triterpenoid saponins biosynthesis have been explored and identified. In the biosynthesis of triterpenoid saponins, the progress of gene mining by omics-based sequencing, gene screening, gene function verification, catalyzing mechanism of key enzymes and gene regulation are summarized and discussed. By the progress of the biosynthesis pathway of triterpenoid saponins, the large-scale production of some triterpenoid saponins and aglycones has been achieved through plant tissue culture, transgenic plants and engineered yeast cells. However, the complex biosynthetic pathway and structural diversity limit the biosynthesis of triterpenoid saponins in different system. Special focus can further be placed on the systematic botany information of medicinal plants obtained from omics large dataset, and triterpenoid saponins produced by synthetic biology strategies, gene mutations and gene editing technology.

关键词： Medicinal plant Cytochrome P450 monooxygenases Uridine diphosphate glucuronosyltransferases Transcription factor Triterpenoid saponins

Design and mechanism of agglomeration of aspirin crystals in pure solvents

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Particuology 2023年第11期82卷 146-156页

作者： Lihong Jia Degui Wu Pingping Cui Ling Zhou Qiuxiang Yin School of Chemical Engineering and Technology State Key Laboratory of Chemical EngineeringTianjin UniversityTianjin300072China Haihe laboratory of Sustainable Chemical Transformations Tianjin300192China tianjin key laboratory of modern drug delivery and high efficiency Tianjin300072China

Agglomeration with improved flowability for platy crystals is desirable in pharmaceutical downstream processing. The formation of agglomerates in pure solvents without the aid of bridging liquids is a convenient and low-cost method compared with complex spherical crystallization. In this work, the adhesion free energies between aspirin crystals in six solvents were calculated using Lifshitz-van der Waals acid-base theory to screen suitable solvents for agglomeration. The maximum stirring rate for agglomeration was determined by adhesion forces and dispersion forces. Then the agglomerates of plate-shaped aspirin were successfully prepared in acetone, methanol, ethanol, 2-propanol, and ethylene glycol without additives by simple cooling crystallization. The interactions between solvent and crystal surfaces were also used to explain the outcomes. A feasible mechanism for the agglomeration process of platy crystals was elucidated, involving the adhesion of dominant crystal facets at the beginning. The effect of stirring rate, cooling rate, and initial supersaturation on agglomeration degree and particle size of aspirin agglomerates were studied. The obtained aspirin agglomerates under the optimal conditions exhibited a uniform particle size distribution, a high agglomeration degree, and superior flowability.

关键词： Agglomeration Platy crystal Aspirin Adhesion force

Immobilization of penicillin G acylase onto amino-modified silica hydrogel

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Frontiers of Chemical Science and Engineering 2010年第1期4卷 87-90页

作者： Weibing DONG Huining HE Junbo GONG Victor CYANG tianjin key laboratory for modern drug delivery and high efficiency School of Chemical Engineering and TechnologyTianjin UniversityTianjin 300072China

Amino-modified silica hydrogel(N-MSHG)was prepared by a simple sol-gel processing via the cocondensation of commercial silica sol with *** G acylase(PGA),a model enzyme,was covalently immobilized onto the N-MSHG and then was used for the enzymatic synthesis of *** samples were characterized by Nitrogen sorption analysis,FT-IR and thermal gravimetric analysis(TGA).The results showed that the amino-modified gel was a mesoporous material with an average pore size of 12.64±0.17 *** immobilization process was efficient and the immobilized enzyme showed high catalytic *** yield of the synthesis of amoxicillin in aqueous media was 38%for 2.5 *** sol-gel preparation is simple and shows prominent potential value in industrial processing.

关键词： mesoporous materials covalent immobilization penicillin G acylase amino-modified silica gel

Fe_(3)O_(4)@SiO_(2)-Protein A-oHSV/CD63 Ab for Capturing Virus and Exosomes

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Journal of Analysis and Testing 2024年第3期8卷 335-350页

作者： Wenqing Zheng Pingyi Zheng Ran Zhao Xinyu Xu Xiao Zhang Xiaoqian Yuan Ying Xu Zichuan Liu Youxin Li tianjin key laboratory for modern drug delivery and high-efficiency Collaborative Innovation Center of Chemical Science and EngineeringSchool of Pharmaceutical Science and TechnologyFaculty of MedicineTianjin UniversityTianjin300072China

Protein A modified magnetic spheres(Fe_(3)O_(4)@SiO_(2)-Protein A)with 22.7 emu/g saturation magnetization were prepared and *** spheres had a diameter of 10 nm and was stable up to 229.2℃,and can bond 19.694 mg/g of Protein *** Fe_(3)O_(4)@SiO_(2)-Protein A was firstly combined with oHSV-BJ-2-A antibody to capture oHSV from disease venom,and the amount of binding virus was 1.92×10^(7)to 3.44×10^(7)PFU/***_(3)O_(4)@SiO_(2)-Protein A was modified with CD63 antibody,which was further fixed using dissuccinimide octylate(DSS)as a crosslinking *** prepared Fe_(3)O_(4)@SiO_(2)-Protein A-CD63 Ab was useful in isolating and enriching exosomes from cell *** with commercial kits,Fe_(3)O_(4)@SiO_(2)-Protein A-CD63 Ab demonstrated a better purification effect,which was successfully monitored using capillary *** total content of exosomes protein extracted using Fe_(3)O_(4)@SiO_(2)-Protein A-CD63 was 3.4 mg/g,which was obviously higher than that reported in some *** addition,Fe_(3)O_(4)@SiO_(2)-Protein A-CD63 Ab also showed its repeatability through bonding and elution of 5 cycles,which was effective in cost *** indicated Fe_(3)O_(4)@SiO_(2)-Protein A-CD63 Ab had the potential for large-scale purification of exosomes in practical applications.

关键词： Immunomagnetic spheres Antibody Exosome Herpes simplex virus

Mechanism and inhibition of trisodium phosphate particle caking： Effect of particle shape and solubility

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Particuology 2016年第4期14卷 115-121页

作者： Mingyang Chen Lanlan Lin Yuqi Zhang Songgu Wu Ergang Liu Kun Wang Jingkang Wang Junbo Gong School of Chemical Engineering and Technology Tianjin University Tianjin 300072 China key laboratory modern drug delivery and high efficiency in tianjin University Tianfin 300072 China The Co-Innovation Center of Chemistry and Chemical Engineering of tianjin Tianjin 300072 China

We investigated the influence of particle shape and solubility on the caking behavior of trisodium phosphate by considering the adhesion free energy and crystal bridge theory. Caking of trisodium phosphate during the drying process under static conditions is a two-step process： adhesion followed by crystal bridge formation between particles. The adhesion free energy plays an important role in adhesion. Trisodium phosphate particles cannot adhere to each other and cake when the adhesion free energy is greater than a critical value, which varies with particle shape. Compared with granular particles, cylindrical particles have larger contact area between particles, which results in more crystal bridges forming and a higher caking ratio. Thus, the critical value is about 100 mJ/m^2 for cylindrical particles, but 60 mJ/m^2 for granular particles at 25 ℃. Concerning the solubility, when particles are similar shapes and soluble in the rinsing liquid, the caking ratio has a linear relationship with adhesion free energy. However, if the particles are insoluble in the rinsing liquid, caking can be completely prevented regardless of adhesion free energy because no crystal bridges form during the growth process. Hence, caking of trisodium phosphate particles could be inhibited by screening rinsing liquids, and optimizing the particle shape and size distribution.

关键词： Caking Particle shape Solubility Adhesion free energy Crystal bridge Trisodium phosphate

Comparative chemical characters of Pseudostellaria heterophylla from geographical origins of China

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Chinese Herbal Medicines 2023年第3期15卷 439-446页

作者： Miao Sha Xiaohuan Li Yu Liu Hongyue Tian Xu Liang Xia Li Wenyuan Gao tianjin key laboratory for modern drug delivery&high-efficiency School of Pharmaceutical Science and TechnologyTianjin UniversityTianjin 300193China

Objective:Pseudostellaria heterophylla has been paid more attention in recent years,mainly as a medicine food homology *** content determination of *** is not specified in the Chinese Pharmacopoeia(version 2020).The environmental conditions in different production areas could exert an influence on the quality of *** purpose of this study is to discriminate *** collected from different geographical origins of ***:In this study,the content of polysaccharide in 28 batches of *** was determined using phenol–sulfuric *** fingerprints were established under optimised HPLC-PDA ***,the similarity analysis(SA)and the quantification of heterophyllin B were *** metabolites of *** were identified and evaluated using UHPLC-Q Exactive HF orbitrap MS *** component analysis(PCA),partial least squares discriminant analysis(PLS-DA),hierarchical cluster analysis(HCA)and orthogonal PLS-DA(OPLS-DA)were performed based on all peak ***:The polysaccharide content in Guizhou and Jiangsu was higher than that of other production areas,which varied significant from different *** the content of heterophyllin B in Anhui and Jiangsu was *** correlation coefficients of HPLC fingerprints for 28 batches samples ranged from 0.877 to 0.990,and the characteristic map can be used to identify and evaluate the quality of *** samples from Fujian,Guizhou,Jiangsu provinces can be relatively separated using multivariate statistical analysis including PCA,PLS-DA,HCA,OPLS-DA,indicating that their metabolic compositions were significantly ***,a total of 15 metabolites which were filtrated by a VIPvalue>1 and a P-value<0.05 associated with the separation of different origins were ***:HPLC fingerprint was established to evaluate the quality and authenticity of *** present work showed that the difference of g

关键词： HPLC fingerprint metabolites Pseudostellaria heterophylla(Miq.)Pax ex Pax et Hoffm polysaccharide UHPLC-Q Exactive HF orbitrap MS system

Synthesis of 3-Methylthioindoles via Intramolecular Cyclization of 2-Alkynylanilines Mediated by DMSO/DA/lSO-d_(6) and SOCI_(2)

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Chinese Journal of Chemistry 2021年第5期39卷 1211-1224页

作者： Xuemin Li Beibei Zhang Jingran Zhang Xi Wang Dongke Zhang Yunfei Du Kang Zhao tianjin key laboratory for modern drug delivery&high-efficiency School of Pharmaceutical Science and TechnologyTianjin UniversityTianjin 300072China State key laboratory of Microbial Technology Institute of Microbiol TechnologyShandong UniversityQingdaoShandong 266237China

The intramolecular cyclization of 2-alkynylanilines mediated by DMSO/SOCI_(2) was found to afford biologically interesting 3-methylthioindoles,which are rarely obtained by the exiting *** could also be replaced with its deuterated counterpart,enabling the method applicable to the construction of indole skeleton bearing a SCD_(3) moiety at its 3-position.

关键词： DMSO Electrophilic addition Cyclization 3-Methylthioindoles Synthetic methods