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Chinese Chemical Letters 2024年第6期35卷 279-282页

作者： Ke Zhang Sheng Zuo Pengyuan You Tong Ru Fen-Er Chen key laboratory of natural Medicines of the changbai mountain Ministry of EducationCollege of PharmacyYanbian UniversityYanji 133002China College of Chemistry and Chemical Engineering Jiangxi Normal UniversityNanchang 330022China Engineering Center of Catalysis and Synthesis for Chiral molecules Fudan UniversityShanghai 200433China Shanghai Engineering Center of Industrial Catalysis for Chiral Drugs Shanghai 200433China

A novel asymmetric[4+2]cycloaddition of 2-methylidenetrimethylene carbonate with pyrrolidonederived enones has been achieved to produce the functionalized tetrahydropyran-fused spirocyclic scaffolds via *** array of enantioenriched spiro-pyrrolidine-2,3-diones bearing adjacent quaternary and tertiary stereocenters are obtained in high yields with excellent enantioselectivities(up to 96% yield and 99% ee).The further transformation of the product has been accomplished for the construction of medical interesting β^(2,2)-amino acids and β-*** mechanistic research was well conducted.

关键词： Pyrrolidine-2,3-diones 2-Methylidenetrimethylene carbonate Asymmetric annulation Spiroheterocycles Allylic 1,3-strain

Synthesis and anticonvulsant activity of 1-substituted benzyl- N-substituted-1, 2, 3-triazole-4-formamides

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Progress in natural Science:Materials International 2006年第9期16卷 925-929页

作者： WANG Junmin, JUN Changsoo, CHAI Kyuyun, KWAK Kyungchell, QUAN Zheshan ( key laboratory of natural resources of the changbai mountain and functional molecules, Yanbian University, Yanji 133002, China Henan University of Traditional Chinese Medicine Pharmacy College, Zhengzhou 450003, China Department of Chemistry, Wonkwang University, Iksan 570-749, Korea) key laboratory of natural resources of the changbai mountain and functional molecules Yanbian University Yanji 133002 China

Substituted benzyl azids were synthesized through the reaction of substituted benzyl chloride and sodium azid, which subsequently underwent cyclization with ethyl propiolate and amidation to give thirteen 1-substituted benzyl-N-substituted-1, 2, 3-triazole-4-formamide derivatives (3a-3m) . The structure of the synthesized compounds was confirmed by IR, 1H-NMR, MS and elemental analysis. Their ant icon vulsant activity against maximal electrolshock (MES) induced seizure was tested and the result showed that all these compounds possess anticonvulsant activity in different degrees. Among those, the compounds containing chloro atoms on the phenyl ring were less potent in anticonvulsant activity, while introducing one or two fluorin atoms on benzyl system increased its activity. Furthermore, their activity decreased when there was substituent on the nitrogen atom of carboxamide, and the larger the substituent, the lower the activity.

关键词： 1-substituted benzyl-N-substituted-1 2 3-triazole-4-formamide anticonvulsant synthesis.

Two new conjugated ketonic fatty acids from the stem bark of Juglans mandshurica

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Chinese Journal of natural Medicines 2015年第4期13卷 299-302页

作者： YAO Da-Lei ZHANG Chang-Hao LI Ren LUO Jie JIN Mei PIAO Jin-Hua ZHENG Ming-Shan CUI Jiong-Mo SON Jong Keun LI Gao key laboratory of natural resources of changbai mountain and functional molecules Ministry of Education Yanbian University College of Pharmacy Department of Pharmacy Yanbian University Hospital College of Pharmacy Yeungnam University

The present study was designed to isolate and characterize novel chemical constituents of the stem bark of Juglans mandshurica Maxim.(Juglandaceae).The chemical constituents were isolated and purified by various chromatographic techniques. The structures of the compounds were elucidated on the basis of spectral data(1D and 2D NMR, HR-ESI-MS, CD, UV, and IR) and by the comparisons of spectroscopic data with the reported values in the literatures. Two long chain polyunsaturated fatty acids(1 and 2) were obtained and identified as(S)-(8E,10E)-12-hydroxy-7-oxo-8,10-octadecadienoic acid(1) and(S)-(8E, 10E)-12-hydroxy-7-oxo-8,10-octadecadienoic acid methyl ester(2). To the best of our knowledge, this is the first report on the isolation and structural elucidation of the two new conjugated ketonic fatty acids from this genus.

关键词： Juglans mandshurica Juglandaceae Conjugated ketonic fatty acid

Synthesis and biological evaluation of dihydrotriazine derivatives as potential antibacterial agents

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Chinese Chemical Letters 2017年第8期28卷 1737-1742页

作者： Tian-Yi Zhang Chao Li Yu-Shun Tian Jia-Jun Li Liang-Peng Sun Chang-Ji Zheng Hu-Ri Piao key laboratory of natural resources of changbai mountain&functional molecules Ministry of EducationYanbian University College of PharmacyYanji133000China Department of Pharmacy Jilin Medical UniversityJilin 132013China

A series of 1,4-dihydro-1,3,5-triazine derivatives were designed and synthesized and their antibacterial and antifungal activities were evaluated. Most of the synthesized compounds showed potent inhibition of several Gram-positive bacterial strains（including multidrug-resistant clinical isolates） and Gramnegative bacterial strains, with minimum inhibitory concentrations（MICs） in the range of 2.1–181.2 mmol/L. Compounds 7a and 7c presented the most potent inhibitory activities against Grampositive bacteria（e.g., Staphylococcus aureus 4220）, Gram-negative bacteria（e.g., Escherichia coli 1924）,and the fungus Candida albicans 7535, with MICs of 2.1 or 4.1 mmol/L. Especially, compound 7a was the most potent, with an MIC of 2.1 mmol/L against four multidrug-resistant, Gram-positive bacterial *** cytotoxic activity of the compound 7a, 7c and 7f was assessed in HepG2 cells, and the results suggest that 1,4-dihydro-1,3,5-triazine derivatives bearing a 6-benzyloxynaphthalen moiety are interesting scaffolds for the development of novel antibacterial agents.

关键词： Antibacterial activitis Antifungal activities Cytotoxicity Minimal inhibitory concentration 1 4-Dihydro-1 3 5-triazine

Synthesis, in vitro and in vivo biological evaluation of novel lappaconitine derivatives as potential anti-inflammatory agents

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Acta Pharmaceutica Sinica B 2020年第4期10卷 628-645页

作者： Lei Pang Chun-Yan Liu Guo-Hua Gong Zhe-Shan Quan key laboratory of natural resources and functional molecules of the changbai mountain Affiliated Ministry of EducationCollege of PharmacyYanbian UniversityYanji 133002China Affiliated Hospital of Inner Mongolia University for Nationalities Tongliao 028000China

Lappaconitine(LA),a natural compound with a novel C18-diterpenoid alkaloid skeleton,displayed extensive biological *** research on LA is focused mainly on its anti-tumor and analgesic effects,and therefore we aimed to investigate its anti-inflammatory potential.A series of novel LA derivatives with various substituents on the 20-N position was designed and *** the initial screening of LA derivatives against NO production,all the target compounds,except compound E2,exhibited excellent inhibitory ability relative to that of ***,compound A4 exhibited the most potent inhibition with IC50 of 12.91 mmol/*** elementary structureeactivity relationships(SARs)of NO inhibitory activity indicated that replacement of the benzene ring with an electron donating group could improve the anti-inflammatory ***,compound A4 shows an anti-inflammatory mechanism by inhibiting NO,PGE2,and TNF-a generation via the suppression of NF-kB and MAPK signaling ***,compound A4 could exert a significant therapeutic effect on LPS-induced acute lung injury(ALI)in *** on the above research,we further investigated the preliminary pharmacokinetic property of A4 in ***,compound A4 could be a promising candidate for the development of anti-inflammatory agents in the future.

关键词： Lappaconitine Anti-inflammatory activity NF-kB MAPK Acute lung injury Pharmacokinetic study

Efficient synthesis of panaxadiol derivatives using continuous-flow microreactor and evaluation of anti-tumor activity

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Chinese Chemical Letters 2015年第3期26卷 334-338页

作者： Yan Wu Wei-Qi Chen Yu-Qing Zhao Hu-Ri Piao key laboratory of natural resources and functional molecules of the changbai mountain Affiliated Ministry of EducationYanbian University College of Pharmacy Department of Chemistry Fudan University School of Traditional Chinese Materia Medica Shenyang Pharmaceutical University

An efficient method has been developed for the synthesis of a series of（20R）-panaxadiol derivatives（4a–w） using a continuous-flow *** antitumor activities of the newly synthesized compounds were evaluated in vitro in two human prostate adenocarcinoma tumor cell lines（i.e.,PC-3and LNCa P cells）,and their cytotoxicities were evaluated using a standard MTT *** 4c,4h,4p,4q and 4s exhibited higher antitumor activities toward PC-3 cell line than panaxadiol,which was used as a reference standard.

关键词： antitumor adenocarcinoma toward silica batch shorter spectrometer incubated equiv acetate

Dihydroquercetin ameliorates alcoholic liver steatosis through P2x7R-NLRP3 inflammasome pathway

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中国药理学与毒理学杂志 2018年第4期32卷 338-339页

作者： Yu ZHANG Xia LI Kai-li XIA Min JIANG Ben-wen CUI Yan-ling WU Ji-xing NAN Li-hua LIAN key laboratory for natural Resource of changbai mountain & functional molecules Ministry of Education College of Pharmacy Yanbian University Yanji 133002 China

OBJECTIVE Dihydroquercetin(TAX) is the most abundant dihydroflavone found in ***,milk thistle and Douglas fir *** investigated whether TAX could inhibit the lipid accumulation in alcoholic liver steatosis in vivo and in *** An in vivo model was established by *** treating mice with ethanol,and an in vitro model was created by treating HepG2 cells with *** TAX regulated Sterol Regulatory Element-binding Protein-1(SREBP1) and Acetyl CoA Carboxylase(ACC) expression via elevating Liver Kinase B1(LKB1)/AMP-activated Kinase(AMPK)***,TAX upregulated SIRT1 expression,which suppressed by ethanal *** of Purinergic 2X7 receptor(P2x7R),nucleotide-binding oligomerization domain-like *** protein 3(NLRP3) and Cysteine protease-1(caspase-1) cleavage by TAX resulted in the *** of Interleukin-1β(IL-1β) production and ***,TAX reduced lipogenesis and *** lipid oxidation via the regulation of AMPK and ACC in ethanol-treated steatotic HepG2 *** downregulated IL-1β cleavage response to Lipopolysaccharides(LPS) plus adenosine triphosphate(ATP) stimulation in HepG2 cells.P2x7R deficiency attenuated lipid accumulation with increasing AMPK activity and decreasing SREBP1 expression in ethanol-treated HepG2 *** Our data showed that TAX exhibited the inhibitory properties on lipogenesis and hepatoprotective ***,indicating that TAX has therapeutic potential for preventing alcoholic liver steatosis.

关键词：二氢黄酮酒精肝治疗方法化合物

P2X7 receptor inhibitor suppressed extracellular ATP/LPS-primed human hepatic stellate cells activation via downregulating NLRP3 inflammasome

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中国药理学与毒理学杂志 2015年第S1期29卷 67-68页

作者： ShuangJIANG QuanJIN Yan-lingWU You-liYAO Ji-xingNAN Li-huaLIAN key laboratory for natural Resource of changbai mountain &functional molecules Ministry of Education College of Pharmacy Yanbian University Yanji 133022 China

OBJECTIVE To investigate the effect of P2X7receptor(P2X7r)inhibition,using a specific inhibitor(A438079)to prevent the development of liver fibrosis on human hepatic stellate cells,*** The supernatant from lipopolysaccharide(LPS)-stimulated RAW264.7 mouse macrophages was supplemented to LX-2 cells for 24 ***-2cells were primed with LPS for 4h and subsequently stimulated for 30 min with 3mmol·L-1 of adenosine 5′-triphosphate(ATP).A438079(10μmol·L-1)was supplemented to LX-2 cells 10 min prior to *** Directly treated with LPS on LX-2 cells,mRNA expressions of IL-1β,IL-18 and IL-6 were increased,as well as P2X7 *** caspase-1,ASC and NLRP3 mRNA expressions were increased with LPS *** stimulation also increasedα-SMA and collagenⅠ mRNA *** treatment of LX-2cells with mediums from LPS-primed RAW264.7mouse macrophages exhibited greater increase of mRNA expressions of above genes than those in LX-2directly treated with *** of directly or indirectly LPS-stimulated LX-2 cells with A438079 both suppressed IL-1βmRNA *** addition treatment of LPS-primed LX-2 cells with 3mmol·L-1 ATP induced the significant increase of IL-1β,IL-6,caspase-1,pannexin-1,α-SMA and collagenⅠ mRNA expression,the increasing ofα-SMA protein expression and cleavage of IL-1β.These events were significantly suppressed by pretreatment with P2X7 rantagonist A438079.P2X7 rblockade also significantly reduced the protein expression ofα-*** Our results suggest that the involvement of the P2X7r-NLRP3 inflammasome pathway in the secretion of IL-1βfrom extracellular ATP/LPS-stimulated human hepatic stellate *** study demonstrated that repression of the P2X7 rrepresents a novel potential therapeutic approach to control liver fibrosis.

关键词： liver fibrosis hepatic stellate cells P2X7receptor

Gentiopicroside ameliorates LKB1/AMPK-dependent alcoholic hepatosteatosis via P2x7R-NLRP3 inflammasome

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中国药理学与毒理学杂志 2018年第4期32卷 265-266页

作者： Xia LI Yu ZHANG Kai-li XIA Min JIANG Ben-wen CUI Yan-ling WU Ji-xing NAN Li-hua LIAN key laboratory for natural Resource of changbai mountain & functional molecules Ministry of Education College of Pharmacy Yanbian University Yanji 133002 China

OBJECTIVE Regulating P2x7R-NLRP3 inflammasome activation might be a potential therapeutic strategy to treat alcoholic *** investigated whether this process would be modulated by gentiopicroside(GPS),which is attributed to the bitterness of gentian root *** An in vivo model was established by intragastrically treating mice with ethanol,and an in vitro model was created by treating HepG2 cells with ethanol or treating RAW 264.7 macrophages and murine bone marrow-derived macrophages(BMDMs) with lipopolysaccharides(LPS) plus adenosine ***(ATP).RESULTS In alcoholic hepatosteatotic mice model,GPS decreased serum *** and triglyceride *** regulated sterol regulatory element-binding protein-1(Srebp1),peroxisome proliferators-actived receptors α(PPARα) and acetyl CoA carboxylase(ACC) expression via elevating liver kinase B1(LKB1)/AMP-activated Kinase(AMPK).Suppression of nucleotide-binding oligomerization domain-like receptor protein 3(NLRP3),caspase-1 and expression by GPS resulted in the inhibition of interleukin-1β(IL-1β) *** ethanol-exposed HepG2 cells,GPS reduced *** and promoted lipid oxidation via P2x7R-NLRP3 inflammasome activation.P2x7R silencing enhanced AMPK activity,and reduced Srebp1 expression in ethanol-treated *** *** P2x7R-mediated inflammatory response to extracellular ATP in LPS-primed RAW 264.7 *** and ***,P2x7R deficiency attenuated IL-1β cleavage in RAW 264.7 ***,and GPS further suppressed IL-1β *** Activation of LKB1/AMPK signaling by GPS might be mediated by P2x7R-NLRP3 inflammasome,suggesting a therapeutic utility of P2x7R blockade in alcoholic hepatosteatosis treatment.

关键词：炎症酒精肝治疗方法临床分析

Toll-like receptor 4-related regulation of Ornithogalum caudatum extract on inflammatory responses in LPS activated macrophages

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中国药理学与毒理学杂志 2018年第4期32卷 284-285页

作者： Xin HAN Jian SONG Jing ZHANG Ya-mei LI Ying FAN Dan-yang SHAO Li-shuang HOU Li-hua LIAN Ji-xing NAN Yan-ling WU key laboratory for natural Resource of changbai mountain & functional molecules Ministry of Education College of Pharmacy Yanbian University Yanji 133002 China

OBJECTIVE To investigate toll-like receptor 4(TLR4)-related the regulation of Ornithogalum caudatum extract(OCE) on inflammatory responses in lipopolysaccharide(LPS) activated *** Primary peritoneal macrophage,Raw 264.7,and THP-1 were incubated in 96-well plate for 24 h and treated with OCE of the concentration of 0-400 μg/ml for 4 *** viability of cells was measured by MTT *** concentrations of OCE were added into the medium of primary *** macrophage,Raw 264.7,and THP-1,respectively,then following with lipopolysaccharides(LPS).Cells were harvested and the total cellular protein and nuclear protein were extracted,and the protein content was determined using BCA protein assay *** expressions of TLR4,inducible nitric oxide synthase(iNOS),cyclooxygenase 2(COX-2),α-inhibitor of NF-κB(IκB-α) and nuclear factor-κB(NF-κB) were assayed by Western *** expressions of interleukin-1α(IL-1α),interleukin-1β(IL-1β),interleukin-18(IL-18),and tumor necrosis factor-α(TNF-α) were measured by *** The results of MTT showed that OCE has no cytotoxicity in Raw 264.7 cells between 1.56 μg/ml and 400 μg/*** with normal group,the expressions of TLR4,iNOS,COX-2,NF-κB and IL-1α,IL-1β,IL-18,TNF-α,the level of nitric oxide(NO) were significantly increased by LPS stimulation,while OCE *** reduced these increase induced by ***,OCE pretreatment reversed the reduction of IκB-α after LPS *** OCE might suppress TLR4 expression and block the *** process of NF-κB and iNOS,further decrease the expression of COX-2 and inhibit the release of inflammatory factors.

关键词：尾砂提取物巨噬细胞炎症临床分析治疗方法