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Artificial Bear Bile:A Novel Approach to Balancing Medical Requirements and Animal Welfare

Engineering 2024年第7期38卷 100-112页

作者： Yong Li Yuhong Huang Nan Feng Heping Zhang Jing Qu Shuanggang Ma Yunbao Liu Jiang Li Shaofeng Xu Ling Wang Mi Zhang Jie Cai Weiping Wang Ru Feng Hang Yu Bo Yu Dailiang Liang Heping Qin Suxiang Luo Yanfen Li Meifeng Li Ruihua Wang Chen Ma Yan Wang Xiaobo Cen Xiaoxian Xu Boli Zhang Xiaoliang Wang Shishan Yu State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China The Seco.d Affiliated Hospital of Tianjin University of Traditional Chinese Medicine Tianjin 300250China zhongshan Belling Biotechnology co. Ltd.Zhongshan 528437China zhongshan Anshi Biopharmaceutical co. Ltd.Zhongshan 528437China WestChina-Frontier Pharma Tech co. Ltd.Chengdu 610041China Tianjin University of Traditional Chinese Medicine Tianjin 301617China

Bear bile has been a valuable and effective medicinal material in traditional Chinese medicine(TCM)for over 13 ***,the current practice of obtaining it through bear farming is under scrutiny for its adverse impact on bear ***,we present a new approach for creating artificial bear bile(ABB)as a high-quality and sustainable alternative to natural bear *** study addresses the scientific challenges of creating bear bile alternatives through interdisciplinary co.laborations across various fields,including resources,chemistry,biology,medicine,pharmaco.ogy,and TCM.A co.prehensive efficacy assessment system that bridges the gap between TCM and modern medical terminology has been established,allowing for the systematic screening of therapeutic *** the utilization of chemical synthesis and enzyme engineering technologies,our research has achieved the environmentally friendly,large-scale production of bear bile therapeutic co.pounds,as well as the optimization and reco.position of ABB *** resulting ABB not only closely resembles natural bear bile in its co.position but also offers advantages such as co.sistent product quality,availability of raw materials,and independence from threatened or wild *** preclinical efficacy evaluations have demonstrated the equivalence of the therapeutic effects from ABB and those from co.mercially available drained bear bile(DBB).Furthermore,preclinical toxico.ogical assessment and phase I clinical trials show that the safety of ABB is on par with that of the currently used *** innovative strategy can serve as a new research paradigm for developing alternatives for other endangered TCMs,thereby strengthening the integrity and sustainability of TCM.

关键词： Artificial bear bile chemical profile Formula optimization Pharmaco.ynamic co.sistency Preclinical toxico.ogical assessment

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ACQ到CIE转化:水合作用诱导的姜黄素晶体发光及可调热致变色用于体内药物追踪（英文）

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Science China Materials 2024年第11期67卷 3561-3569页

作者：申欢石鹏刘二刚方月飞许史杰龚俊波黄永焯 zhongshan Institute for Drug Disco.ery Shanghai Institute of Materia MedicaChinese Academy of Sciences Shanghai Institute of Materia Medica Chinese Academy of Sciences School of chemical Engineering and Technology Tianjin University SINOPEC Research Institute of Petroleum Processing co. Ltd. co.lege of chemical Engineering and Materials Science Tianjin University of Science and Technology NMPA Key Laboratory for Quality Research and Evaluation of Pharmaceutical Excipients

目前固态材料在受刺激时能够切换发光性质仍然是一个挑战,特别是对于有机材料而言.晶体中的水分子极大地影响有机晶体的吸收光谱,但是否可以系统地通过水分子调控有机发光材料的发射光谱尚不清楚.在本研究中,我们成功地制备了姜黄素一... 详细信息

目前固态材料在受刺激时能够切换发光性质仍然是一个挑战,特别是对于有机材料而言.晶体中的水分子极大地影响有机晶体的吸收光谱,但是否可以系统地通过水分子调控有机发光材料的发射光谱尚不清楚.在本研究中,我们成功地制备了姜黄素一水合物(X型),它是一种结晶诱导发光(CIE)的通道型水合物,在608 nm处发出橙色荧光,与传统的聚集诱导荧光猝灭(ACQ)形式有所不同.经过热处理后,姜黄素水合物释放出水分子,形成了新的无水合物(Ⅳ型),其发出黄绿色荧光,且最佳发射波长为575 nm.该方法可用于追踪皮下或肌肉注射后姜黄素晶体的吸收.水合物介导的单晶到单晶转变(SCSC)及其相关的发光转变是可逆的,并且对温度敏感,可为合成和设计基于聚集诱导发射(AIE)的智能发光装置提供一种环保的途径,也可用于检测空气湿度或示踪药物吸收.

关键词： curcumin crystallization-induced emission channel-type hydrate single-crystal-to-single-crystal transition reversible luminescence

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Strategy of preparing Smco.based films with high co.rcivity and remanence ratio achieved by temperature and chemical optimization

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Journal of Rare Earths 2024年第7期42卷 1289-1297,I0004页

作者： Yansong Gong Zhaoguo Qiu Sizhe Liang Xinrui Zheng Hongxia Meng Zhigang Zheng Deyang Chen Shengfu Yuan Weixing Xia Dechang Zeng J.P.Liu School of Materials Science and Engineering South China University of TechnologyGuangzhou510640China zhongshan R&D Center for Materials Surface and Thin Films Technology of the South China University of Technology Gent Materials Surface Technology(Guangdong)Co.Ltd.Zhongshan528437China Institute for Advanced Materials South China Academy of Advanced OptoelectronicsSouth China Normal UniversityGuangzhou510006China Yangjiang Branch Guangdong Laboratory Materials Science and Technology Yangjiang Advanced Alloys LaboratoryYangjiang529500China Laboratory of Rare-Earth Magnetic Functional Materials Ningbo Institute of Material Technology and EngineeringChinese Academy of SciencesNingbo315201China Department of Physics University of Texas at ArlingtonArlingtonTX76019USA

Smco.based films with excellent intrinsic magnetic properties have promising applications in micro-electro-mechanical system(MEMS).However,due to the co.plexity of phase co.position and unco.trollable crystallization degree of Smco.hard magnetic phase in the film,both the co.rcivity(Hc)and remanence(Mr)of films are difficult to enhance *** this paper,Smco.based films were deposited with a Cr underlayer and capping layer on single crystal Si substrates via magnetron sputtering *** effects of annealing parameters and Sm/co.atomic ratio on the phase structure and co.rcivity of films are *** adjusting the Sm/co.atomic ratio from 1:5 to 1:4,co.soft magnetic phase disappears and the single phase Smco. is obtained,leading to the increase of co.rcivity of the films from 30 to 34 *** influence of deposition temperature and Cu doping on magnetic properties of Smco.based films was *** the deposition temperature increases from room temperature to 250℃,the co.rcivity will further increase from 34 to 51 ***,a severe kink is observed in the demagnetization curves due to the poor exchanged *** analysis of transmission electron microsco.y(TEM)co.firms that the average size of non-hard magnetic amorphous phase exceeds the effective exchanged co.pling length of Smco.,which co.tributes to the deco.pling and low remanence ***,doping Cu and applying a post-annealing process can significantly improve the crystallization degree of the *** the co.rcivity and the remanence ratio of the demagnetization curves are greatly *** propose a plausible strategy to prepare the Smco.based films with high co.rcivity and remanence ratio by temperature and chemical optimization,which can be utilized in high performed MEMS devices.

关键词： Rare earths Smco.based films Phase co.position Crystallization co.ditions co.rcivity Remanence ratio

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创制人工熊胆——在医药需求和动物福利之间实现平衡的创新路径（英文）

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Engineering 2024年第7期 100-112页

作者：李勇黄宇虹冯楠张和平屈晶马双刚刘云宝李江徐少锋王玲张咪蔡杰王伟平冯茹于航于博梁待亮秦和平罗素芗李艳芬李美凤王瑞华马辰王琰岑小波徐孝先张伯礼王晓良庾石山 State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia Medica Chinese Academy of Medical Sciences & Peking Union Medical College The Seco.d Affiliated Hospital of Tianjin University of Traditional Chinese Medicine zhongshan Belling Biotechnology co. Ltd. zhongshan Anshi Biopharmaceutical co. Ltd. WestChina-Frontier Pharma Tech co. Ltd. Tianjin University of Traditional Chinese Medicine

Bear bile has been a valuable and effective medicinal material in traditional Chinese medicine (TCM) for over 13 ***,the current practice of obtaining it through bear farming is under scrutiny for its adverse impact on bear ***,we present a new approach for creating artificial bear bile (ABB)as a high-quality and sustainable alternative to natural bear *** study addresses the scientific challenges of creating bear bile alternatives through interdisciplinary co.laborations across various fields,including resources,chemistry,biology,medicine,pharmaco.ogy,and TCM.A co.prehensive efficacy assessment system that bridges the gap between TCM and modern medical terminology has been established,allowing for the systematic screening of therapeutic *** the utilization of chemical synthesis and enzyme engineering technologies,our research has achieved the environmentally friendly,large-scale production of bear bile therapeutic co.pounds,as well as the optimization and reco.position of ABB *** resulting ABB not only closely resembles natural bear bile in its co.position but also offers advantages such as co.sistent product quality,availability of raw materials,and independence from threatened or wild *** preclinical efficacy evaluations have demonstrated the equivalence of the therapeutic effects from ABB and those from co.mercially available drained bear bile (DBB).Furthermore,preclinical toxico.ogical assessment and phase I clinical trials show that the safety of ABB is on par with that of the currently used *** innovative strategy can serve as a new research paradigm for developing alternatives for other endangered TCMs,thereby strengthening the integrity and sustainability of TCM.

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Mechanism of action of the bile acid receptor TGR5 in obesity

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Acta Pharmaceutica Sinica B 2024年第2期14卷 468-491页

作者： Weijun Lun Qihao Yan Xinghua Guo Minchuan Zhou Yan Bai Jincan He Hua Cao Qishi Che Jiao Guo Zhengquan Su Guangdong Engineering Research Center of Natural Products and New Drugs Guangdong Provincial University Engineering Technology Research Center of Natural Products and DrugsGuangdong Pharmaceutical UniversityGuangzhou 510006China Guangdong Metabolic Disease Research Center of Integrated Chinese and Western Medicine Key Laboratory of Glucolipid Metabolic DisorderMinistry of Education of ChinaGuangdong TCM Key Laboratory for Metabolic DiseasesGuangdong Pharmaceutical UniversityGuangzhou 510006China School of Public Health Guangdong Pharmaceutical UniversityGuangzhou 510310China School of Chemistry and chemical Engineering Guangdong Pharmaceutical UniversityZhongshan 528458China Guangzhou Rainhome Pharm&Tech co. Ltd.Science CityGuangzhou 510663China

G protein-co.pled receptors(GPCRs)are a large family of membrane protein receptors,and Takeda G protein-co.pled receptor 5(TGR5)is a member of this *** a membrane receptor,TGR5 is widely distributed in different parts of the human body and plays a vital role in regulating metabolism,including the processes of energy co.sumption,weight loss and blood gluco.e *** studies have shown that TGR5 plays an important role in gluco.e and lipid metabolism disorders such as fatty liver,obesity and *** the global obesity situation beco.ing more and more serious,a co.prehensive explanation of the mechanism of TGR5 and filling the gaps in knowledge co.cerning clinical ligand drugs are urgently *** this review,we mainly explain the anti-obesity mechanism of TGR5 to promote the further study of this target,and show the electron microsco.e structure of TGR5 and review recent studies on TGR5 ligands to illustrate the specific binding between TGR5 receptor binding sites and ligands,which can effectively provide new ideas for ligand research and promote drug research.

关键词： Obesity TGR5 Bile acids Ligand Appetite Metabolism GLP-1 Inflammation

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Influence of Emulsifiers on the Synthesis of Insulin-loaded Nanocapsules in Double Emulsion

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Chinese Journal of Chemistry 2006年第1期24卷 109-113页

作者：朱银燕张高勇洪昕林董金凤夏必来 Department of Chemistry Wuhan University Wuhan Hubei 430072 China China Research Institute of Daily chemical Industry Taiyuan Shangxi 030001 China zhongshan Daqiao chemical Industry co. Ltd. Zhongshan Guangzhou 528403 China

Insulin entrapped nanocapsules to use polylactide （PLA） as the encapsulating material were prepared through a modified water-in-oil-in-water （W/O/W） emulsification and solvent evaporation method, The average particle size of PLA nanocapsules obtained was decreased to （181.5 ± 8.4） nm, and capably adjusted from 180 to 370 nm by using different types and co.tent of nonionic emulsifiers. The influence of emulsifiers on property of nanocapsules was discussed in detail. The effects of spans and tweens to modify the size of the nanocapsules were different, which can be due to the distribution of the surfactants on the inner interface between the inner water and oil of the double emulsion. The encapsulation efficiency and drug release of nanocapsules were affected obviously by the co.tent and type of emulsifiers.

关键词： insulin nanocapsules double emulsion emulsifier polylactide

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Electrochemical investigation on the formations of Dy-Ni alloy films in dimethylformamide

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Rare Metals 2002年第2期21卷 85-89页

作者： HE Fengrong, WANG Yu, LIU Guankun, and SA LichangSchool of Chemistry and chemical Engineering, zhongshan University. Guangzhou 510275, China School of Chemistry and chemical Engineering Zhongshan University Guangzhou 510275

The elexctrochemical properties of Dy (III), Ni(II) + Ni(II) indimethylformamide were studied by cyclic voltammetry on Pt or Cuelectrode. Black, metallic lustered, co.pact and well adhesive Dy-Nialloy films can be co.deposited on Cu electrode bysweeping-potential-deposition method within some potentials. SEM,EDAX and XRD were used to analyze the alloy films. The Dy co.tent inthe Dy-Ni alloy film is up to 56.91/100 (mass fraction) and the Dy-Ni alloy films are amorphous.

关键词： Dy-Ni alloy film dimethylformamide (DMF) Sweeping-potential-deposition-method induced co.-deposition

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Electron microsco.y observations of surface morphologies and particle arrangement behaviors of magnetic fluids

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Science China Technological Sciences 2003年第2期46卷 168-172页

作者：沈辉徐雪青王伟 Center for Nanotechnology Research Zhongshan University Guangzhou 510275 China Guangzhou 510070 China Center for Nanotechnology Research Zhongshan University Guangzhou 510275 China Zhongshan 528411 China Guangzhou Institute of Energy co.version Guangzhou Institute of Energy ConversionHawley & Hazel Chemical Co. Ltd. Guangzhou 510070 China

The surface morphology of quasi-periodic stripe-shaped patterns of magnetite fluids was observed in applied perpendicular magnetic fields by means of scanning electron microsco.y. The nanoparticles of the magnetite fluids are arranged in oriental quasilinear chains in applied perpendicular magnetic fields as observed using transmission electron microsco.y. This arrangement results from particle-particle interactions and particle-carrier liquids interactions, which are eventually co.trolled by the magnetic fields distribution.

关键词： magnetic fluids electron microsco.y surface morphology nanoparticle arrangement behavior.

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Synthesis and crystal structure of [co.mpt)_2{P(OCH_3)_3}_2]BF_4 (Hmpt = 2-mercaptothiazoline)

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Chinese Journal of Chemistry 1999年第1期17卷 36-41,2页

作者：童叶翔康北笙苏成勇余小岚陈小明 School of Chemistry and chemical Engineering Zhongshan University Guangzhou Guangdong 510275 China

The monomeric co.alt-phosphite-thiolato co.plex [ co.(mpt)2 {P (OCH3 )3 }2 ] BF4 (Hmpt = 2-mercaptothiazoline) has been prepared and characterized by X-ray crystallography. The co.plex crystallizes in the monoclinic space group C2/c with a= 0.8078(5), b=2.6020(18), c=1.2191(7) nm, β= 99.38 (1)°, V= 2.528(3) nm3, and Z = 4. The structure co.prises discrete cations [co.mpt)2{P(OCH3)3}2.] + and anions BF4- , in which the co.alt (Ⅲ) atom is co.rdinated to two chelate mpt- and two as-oriented monodentate P(OCH3)3 ligands in a highly distorted octahedral geometry. The most distorted angles are S(2)-co.1)-S(2a) of 162.23(10)° and N(1)-co.1)-S(2) of 71. 47 (13)°, the latter is caused by the geometric co.straint of the bidentate ligand mpt- . Cyclic voltammetry has been used to study the electrochemical behavior of the title co.plex on the R electrode in MeCN solution with 0.1 mol·L-1 of Bun4NBF4 as electrolyte. The results indicate that the title co.plex is unstable in MeCN.

关键词： co.alt(III) co.plex 2-mercaptothiazoline trimethylphosphite crystal structure

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Highly selective ethylbenzene production through alkylation of dilute ethylene with gas phase-liquid phase benzene and transalkylation feed

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Journal of Natural Gas Chemistry 2009年第1期18卷 21-24页

作者： Shenglin Liu Fucun Chen Sujuan Xie Peng Zeng Xiyan Du Longya Xu State Key Laboratory of Catalysis Dalian Institute of Chemical Physics Chinese Academy of Sciences Zhongshan Road No. 457 Dalian 116023 liaoning China China petroleum Engineering co. Ltd Fushun Company Fushun 113006 liaoning China

A novel industrial process was designed for the highly selective production of ethylbenzene. It co.prised of a reactor vessel, vapor phase ethylene feed stream, benzene and transalkylation feed stream. Especially the product stream co.taining ethylbenzene was used to heat the reactor vessel, which co.sisted of an alkylation section, an upper heat exchange section, and a bottom heat exchange section. In such a novel reactor, vapor phase benzene and liquid phase benzene were co.xisted due to the heat produced by isothermal reaction between the upper heat exchange section and the bottom heat exchange section. The process was demonstrated by the thermodynamic analysis and experimental results. In fact, during the 1010 hour-life-test of gas phase ethene with gas phase-liquid phase benzene alkylation reaction, the ethene co.version was above 95%, and the ethylbenzene selectivity was above 83% （only benzene feed） and even higher than 99% （benzene plus transalkylation feed）. At the same time, the xylene co.tent in the ethylbenzene was less than 100 ppm when the reaction was carried out under the reaction co.ditions of 140-185℃ of temperature, 1.6-2.1 MPa of pressure, 3.0-5.5 of benzene/ethylene mole ratio, 4-6 v% of transalkylation feed/（benzene＋transalkylation feed）, 0.19-0.27 h^-1 of ethene space velocity, and 1000 g of 3998 catalyst loaded. Thus, co.pared with the co.ventional ethylbenzene synthesis route, the transalkylation reactor co.ld be omitted in this novel industrial process.

关键词： dilute ethylene gas phase-liquid phase benzene alkylation ethylbenzene

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