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Structure-activity Relationship of Sintenin and its Analogues on Six Human Tumor Cell Lines

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Chinese Chemical Letters 2005年第8期16卷 997-1000页

作者： Li Hong HU Bin zou Jing Xu GONG Hai Bo LI Lei Xiang YANG Chang Xin ZHOU Hua BAI Xiu Mei WU Wei CHENG Yu ZHAO Department of Traditional Chinese Medicine and Natural Drug Research College of Pharmaceutical Sciences Zhejiang University Hangzhou 310031 Zhejiang Hi sun Naturelite pharmaceutical R＆D-co. -Ltd.Hangzhou310007 State Key Laboratory of Tropical Crop Biotechnology Institute of Bioscience and BiotechnologyHaikou 571101

The synthesis of a cytotoxic natural ester sintenin 1 and thirty-three of its analogues 2-34 were carried out. The cytotoxicities of the synthetic co.pounds have been screened for human tumor cell Unes such as PC-3, Hela, A549, BEL7404, CNE, and KB. The results showed that phenolic derivatives exhibited strongest cytoxicity, and the unsaturated esters were more cytotoxic than their saturated analogues.

关键词： Synthesis natural products sintenin cytotoxicity SAR.

Research on Prediction of the Scale of OTC Drug Market in China Based on Quantitative Analysis

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Asian Journal of Social Pharmacy 2020年第3期15卷 145-152页

作者： Xu Yang Xu Lang Xue Aoming Hainan Bikai pharmaceutical co. LTD.Haikou 570311China Hainan Huiyuantang pharmaceutical co. LTD.Haikou 570311China School of Business Administration Shenyang Pharmaceutical UniversityShenyang 110016China

Objective To analyze the scale of domestic OTC drug market and its influencing factors,so as to predict its future market and provide a scientific basis for pharmaceutical enterprises to grasp the opportunities in the market.Methods The scale of OTC drug market from 1999 to 2018 in China and its influencing factors were analyzed by unit root test,Granger causality test and co.integration test.Results and co.clusion From the perspective of the global pharmaceutical market,OTC drug market has broad prospects and great development potential.Since the influence of GDP and the number of elderly populations on the scale of OTC drug market is positive,the predicted growth rate of OTC market in the next three years is 5.82%,5.86%and 5.90%,respectively.

关键词： quantitative analysis OTC drugs prediction of the scale of market unit root test granger causality test co.integration test

Study on the deactivation and regeneration of the ZSM-5 catalyst used in methanol to olefins

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Journal of Natural Gas Chemistry 2011年第3期20卷 266-270页

作者： Jingchang Zhang Haibin Zhang Xiuying Yang Zhong Huang Weiliang Cao Institute of Modern Catalysis State Key Laboratory of Chemical Resource Engineering Beijing University of Chemical Technology Bering 100029 China Hainan Institute of Science and Technology Haikou 571126 Hainan China Shandong New Time pharmaceutical co. Ltd. Jining 272400 Shandong China

ZSM-5 zeolite catalyst modified by a trace of metal cations shows high activity and high selectivity for the reaction of methanol to olefins （MTO）, but it inclines to deactivate during the reaction. In this paper, the mechanism of the catalyst deactivation and the regeneration method were studied by X-ray diffraction （XRD）, N2 adsorption-desorption, infrared spectra （IR）, and infrared spectra co.pled with NH3 molecular probes （IR-NH3）. These characterizations indicated that co.e formation was the main reason for the catalyst deactivation. To regenerate the deactivated catalyst, two methods, i.e., calcination and methanol leaching, were used. N2 adsorption-desorption, IR and IR-NH3 characteriza-tions showed that both methods can eliminate co.e deposited on the catalyst and make the catalyst reactivated. XRD showed that the structure of the catalyst did not change after regeneration. Interestingly, the regenerated catalyst even showed better catalytic performance of the MTO reaction than the fresh one. Besides, the calcination regeneration can eliminate co.e more co.pletely, however, the methanol leaching method can be more easily carried out in situ in the reactor.

关键词： methanol olefins ZSM-5 deactivation regeneration

Structural repurposing of SGLT2 inhibitor empagliflozin for strengthening anti-heart failure activity with lower glyco.uria

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Acta Pharmaceutica Sinica B 2023年第4期13卷 1671-1685页

作者： Yixiang Xu Chao Zhang Kai Jiang Xinchun Yang Feng Chen Zhiyang Cheng Jinlong Zhao Jiaxing Cheng Xiaokang Li Xin Chen Luoyifan Zhou Hao Duan Yunyuan Huang Yaozu Xiang Jian Li State Key Laboratory of Bioreactor Engineering Shanghai Frontiers Science Center of Optogenetic Techniques for Cell MetabolismFrontiers Science Center for Materiobiology and Dynamic ChemistryShanghai Key Laboratory of New Drug DesignSchool of PharmacyEast China University of Science and TechnologyShanghai 200237China Shanghai East Hospital School of Life Sciences and TechnologyTongji UniversityShanghai 200092China East China University of Science and Technology-Tengbai pharmaceutical Innovative Drugs Joint Research Institute Zhuhai Tengbai Pharmaceutical Co.Ltd.Zhuhai 519000China Hubei Key Laboratory of Genetic Regulation and Integrative Biology School of Life SciencesCentral China Normal UniversityWuhan 430079China Yunnan Key Laboratory of Screening and Research on Anti-pathogenic Plant Resources from West Yunnan College of PharmacyDali UniversityDali 671000China Clinical Medicine Scientific and Technical Innovation Center Shanghai Tenth People's HospitalTongji University School of MedicineShanghai 200092China Key Laboratory of Tropical Biological Resources of Ministry of Education College of PharmacyHainan UniversityHaikou 570228China

Sodium-gluco.e co.ransporter 2(SGLT2)inhibitors have been reapproved for heart failure(HF)therapy in patients with and without diabetes.However,the initial gluco.e-lowering indication of SGLT2i has impeded their uses in cardiovascular clinical practice.A challenge of SGLT2i then beco.es how to separate their anti-HF activity from gluco.e-lowering side-effect.To address this issue,we co.ducted structural repurposing of EMPA,a representative SGLT2 inhibitor,to strengthen anti-HF activity and reduce the SGLT2-inhibitory activity acco.ding to structural basis of inhibition of SGLT2.co.pared to EMPA,the optimal derivative JX01,which was produced by methylation of C2—OH of the gluco.e ring,exhibited weaker SGLT2-inhibitory activity(IC_(50)>100 nmol/L),and lower glyco.uria and gluco.e-lowering side-effect,better NHE1-inhibitory activity and cardioprotective effect in HF mice.Furthermore,JX01 showed good safety profiles in respect of single-dose/repeat-dose toxicity and hERG activity,and good pharmaco.inetic properties in both mouse and rat species.co.lectively,the present study provided a paradigm of drug repurposing to disco.er novel anti-HF drugs,and indirectly demonstrated that SGLT2-independent molecular mechanisms play an important role in cardioprotective effects of SGLT2 inhibitors.

关键词： Heart failure SGLT2 inhibitor Empagliflozin Structural repurposing NHE1(sodium-hydrogen exchanger 1)

Integrated analysis reveals an association between the rhizosphere microbiome and root rot of arecanut palm

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Pedosphere 2021年第5期31卷 725-735页

作者： Hong LI Xiang MA Yanqiong TANG Chengliang YAN Xinwen HU Xi HUANG Min LIN Zhu LIU Key Laboratory of Tropical Biological Resources of Ministry of Education School of Life and Pharmaceutical SciencesHainan UniversityHaikou 570228(China) Biotechnology Research Institute Chinese Academy of Agricultural SciencesBeijing 100081(China)

The rhizosphere microbial co.munity is crucial to plant health.Many studies have explored the association between the rhizosphere microbiome and plant disease.However,few studies have focused on root rot in arecanut palm,a disease causing devastating effects and thus resulting in eco.omic losses that co.siderably affect the development of the arecanut industry.Here,rhizosphere samples were co.lected from both healthy arecanut palm plants and root-rotted arecanut palm plants,and the microbial co.munities were analyzed using high-throughput sequencing.The root-rotted samples exhibited distinct microbial co.munity richness,diversity,and co.position co.pared with the healthy samples,which was associated with p H acco.ding to the Mantel test.Identified potential plant pathogens,including Proteobacteria,Bacteroidetes,Chytridiomyco.a,and Mortierellomyco.a,were significantly enriched in the root-rotted samples.In co.trast,potentially beneficial plant microbes,such as Acidobacteria and Gemmatimonadetes,were significantly depleted in the root-rotted samples.co.occurrence networks were co.structed to further identify microbial relationships in the root-rotted samples.These findings revealed eco.ogical imbalance among beneficial bacteria in the root-rotted samples.The present study therefore provides an integrated view of the association between the microbial co.munity and root rot in arecanut palm.

关键词： microbial co.munity co.occurrence network eco.ogical imbalance soil physico.hemical characteristics high-throughput sequencing

Disco.ery of a highly specific ^(18)F-labeled PET ligand for phosphodiesterase 10A enabled by novel spirocyclic iodonium ylide radiofluorination

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Acta Pharmaceutica Sinica B 2022年第4期12卷 1963-1975页

作者： Zhiwei Xiao Huiyi Wei Yi Xu Ahmed Haider Junjie Wei Shiyu Yuan Jian Rong Chunyu Zhao Guoco.g Li Weibin Zhang Huangcan Chen Yuefeng Li Lingling Zhang Jiyun Sun Shaojuan Zhang Hai-Bin Luo Sen Yan Qijun Cai Lu Hou Chao Che Steven H.Liang Lu Wang Center of Cyclotron and PET Radiopharmaceuticals Department of Nuclear Medicine and PET/CT-MRI Centerthe First Affiliated Hospital of Jinan UniversityGuangzhou 510630China Division of Nuclear Medicine and Molecular Imaging Massachusetts General Hospital&Department of RadiologyHarvard Medical SchoolBostonMA 02114USA Department of Cardiology the First Affiliated Hospital of Jinan UniversityGuangzhou 510630China State Key Laboratory of Chemical Onco.enomics Key Laboratory of Chemical GenomicsPeking University Shenzhen Graduate SchoolShenzhen 518055China Guangdong Landau Biotechnology co.Ltd. Guangzhou 510555China Key Laboratory of Tropical Biological Resources of Ministry of Education School of Pharmaceutical SciencesHainan UniversityHaikou 570228China Guangdong-Hongkong-Macao Institute of CNS Regeneration Ministry of Education CNS Regeneration Collaborative Joint LaboratoryJinan UniversityGuangzhou 510632China

As a member of cyclic nucleotide phosphodiesterase(PDE)enzyme family,PDE10A is in charge of the degradation of cyclic adenosine(cAMP)and guanosine monophosphates(cGMP).While PDE10A is primarily expressed in the medium spiny neurons of the striatum,it has been implicated in a variety of neurological disorders.Indeed,inhibition of PDE10A has proven to be of potential use for the treatment of central nervous system(CNS)pathologies caused by dysfunction of the basal ganglia–of which the striatum co.stitutes the largest co.ponent.A PDE10A-targeted positron emission tomography(PET)radioligand would enable a better assessment of the pathophysiologic role of PDE10A,as well as co.firm the relationship between target occupancy and administrated dose of a given drug candidate,thus accelerating the development of effective PDE10A inhibitors.In this study,we designed and synthesized a novel ^(18)F-aryl PDE10A PET radioligand,co.enamed[^(18)F]P10A-1910([^(18)F]9),in high radiochemical yield and molar activity via spirocyclic iodonium ylide-mediated radiofluorination.[^(18)F]9 possessed good in vitro binding affinity(IC_(50)=2.1 nmol/L)and selectivity towards PDE10A.Further,[^(18)F]9 exhibited reasonable lipophilicity(logD=3.50)and brain permeability(P_(app)>10×10^(−6) cm/s in MDCK-MDR1 cells).PET imaging studies of[^(18)F]9 revealed high striatal uptake and excellent in vivo specificity with reversible tracer kinetics.Preclinical studies in rodents revealed an improved plasma and brain stability of[^(18)F]9 when co.pared to the current reference standard for PDE10A-targeted PET,[^(18)F]MNI659.Further,dose–response experiments with a series of escalating doses of PDE10A inhibitor 1 in rhesus monkey brains co.firmed the utility of[^(18)F]9 for evaluating target occupancy in vivo in higher species.In co.clusion,our results indicated that[^(18)F]9 is a promising PDE10A PET radioligand for clinical translation.

关键词： Phosphodiesterase 10A PET radioligand 18F Spirocyclic iodonium ylide Nonhuman primate Target occupancy

Chemistry and biology of Pestalotiopsis-derived natural products

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Fungal Diversity 2014年第3期66卷 37-68页

作者： Jing Xu Xiaobo Yang Qiang Lin Key Laboratory of Protection and Development Utilization of Tropical Crop Germplasm Resources Ministry of EducationCollege of Material and Chemical EngineeringHainan UniversityHaikou 570228People’s Republic of China Institute of Functional Biomolecules State Key Laboratory of Pharmaceutical BiotechnologyNanjing UniversityNanjing 210093People’s Republic of China Key laboratory of water pollution treatment&resource reuse of Hainan province Hainan Normal UniversityHaikou 571158People’s Republic of China

Species within the fungal genus Pestalotiopsis have beco.e a topic of research in many microbial-chemical and pharmaco.ogical laboratories because they co.tain structurally co.plex,biologically active metabolites.This article is a follow-up to a previous review(Xu,Ebada,and Proksch,Fungal Divers 44:15–31,2010).It focuses particularly on new findings co.cerning the chemistry and bioactivity of Pestalotiopsis sp.,co.ering a period ranging from August 2010 to August 2013.Some 160 metabolites were isolated from Pestalotiopsis species during this period and their structures are reported within a biogenetic co.text.Bioassays showed antitumor,antifungal,and antimicrobial activities to be the most notable bioactivities of seco.dary metabolites isolated from this genus.The biogenetic pathways associated with the alkaloids,sesquiterpenes,quinines,xanthones,and lactones co.ered in this review are highlighted.

关键词： Seco.dary metabolites Bioactivity Biogenetic relationships

Gas Chromatography–Mass Spectrometry for Quantitative and Qualitative Analysis of Essential Oil from Curcuma wenyujin Rhizomes

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World Journal of Traditional Chinese Medicine 2021年第1期7卷 138-145页

作者： Xiang-Sheng Zhao Yue-Xiang Zeng Ya-Kui Zhou Rong-Tao Li Mei-Hua Yang Key Laboratory of Resources co.servation and Development of Southern Medicine of Hainan Province&Hainan Branch of the Institute of Medicinal Plant Development Chinese Academy of Medical Sciences and Peking Union Medical CollegeHaikou 570311China School of Life and pharmaceutical Sciences Hainan UniversityHaikou 570228China Institute of Medicinal Plant Development Chinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100193China

Objectives:A rapid and sensitive gas chromatography–mass spectrometry(GC–MS)method for quantitative and qualitative analysis of essential oil from Curcuma wenyujin rhizomes was established.Methods:The essential oil of C.wenyujin rhizomes was extracted by supercritical co. extraction(SFE).Six main bioactive co.pounds(eucalyptol,β-elemene,curzerene,germacrone,curdione,and curcumol)were analyzed in selected ion monitoring mode(SIM).Results:Curzerene is not originally present in C.wenyujin rhizomes,but is a product of the transformation of furanodiene at high temperature.The six target co.ponents demonstrated good linearity(R2>0.9979)over a relatively wide co.centration range.The interday and intraday variations had relative standard deviation values less than 5%and the average reco.ery ranged from 96.95%to 100.04%.The limit of quantitation ranged from 0.032 to 0.235μg/mL.The developed method was successfully used to analyze the six co.pounds in 17 samples co.lected from different origins.Significant variation was observed for the co.centrations of the six co.pounds.In addition,51 co.stituents were identified in C.wenyujin rhizome essential oil,co.sisting of 87.66%of the total essential oil,including curdione,curzerene,dehydrocurdione,germacrone,1,4-bis(2-benzimidazoyl)benzene,neocurdione,curcumenone,andβ-elemene.co.clusions:The proposed method will be useful in the quality co.trol of C.wenyujin rhizome essential oil production.

关键词： Curcuma wenyujin essential oil gas chromatography–mass spectrometry quantitative analysis supercritical co. extraction

Herb-drug interaction in the protective effect of Alpinia officinarum against gastric injury induced by indomethacin based on pharmaco.inetic, tissue distribution and excretion studies in rats

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Journal of pharmaceutical Analysis 2021年第2期11卷 200-209页

作者： Xuguang Zhang Zhenrui Xie Xun Chen Junqiang Qiu Yinfeng Tan Xiaoliang Li Hailong Li Junqing Zhang Key Laboratory of Tropical Translation Medicine of Ministry of Education Hainan Provincial Key Laboratory for Research and Development of Tropical HerbsSchool of PharmacyHainan Medical UniversityHaikou571199China

Alpinia officinarum Hance of the Chinese traditional herb for the treatment of emesis, abdominal pain and diarrhea has been used to co.nteract gastric disease induced by indomethacin in rats without obvious side effects. However, the role of herb-drug interaction between indomethacin and A. officinarum based on pharmaco.inetic, tissue distribution and excretion still remains unknown. In this study, an ultra-fast liquid-tandem mass spectrometry(UFLC-MS/MS) method was developed for simultaneous determination of indomethacin and its three metabolites, O-desmethylindomethacin(ODI), deschlorobenzoylindomethacin(NDI) and indomethacin acyl-b-D-glucuronide(IDAbG) by oral administration of indomethacin solution with and without the ethanolic extract of A. officinarum and applied to co.parative pharmaco.inetic, tissue distribution and excretion studies. Our results clarified that oral administration of A. officinarum produced significant alterations in the pharmaco.inetic parameters of indomethacin. And the pharmaco.inetic interaction between indomethacin and A. officinarum reduced the systemic exposure of indomethacin and increased its elimination. Tissue distribution results demonstrated that co.administration of A. Officinarum co.ld not reduce the accumulation of indomethacin in the target tissue of the stomach, but co.ld accelerate the excretions of indomethacin and its three metabolites including ODI, NDI and IDAb G in the bile and feces of rats in the excretion study.Therefore, A. Officinarum might have a gastrointestinal protective effect through the interaction role with indomethacin based on the pharmaco.inetics and excretion in rats.

关键词： Alpinia officinarum Hance Indomethacin Herb-drug interaction Pharmaco.inetics Tissue distribution Excretion