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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

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

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

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

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

Inhibition of P2X7R modulates ECM deposition in HSCs and crosstalk with macrophages in liver fibrosis

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中国药理学与毒理学杂志 2019年第10期 772-773页

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

OBJECTIVE Modulation of immune response and reduction of extracellular matrix(ECM)deposition are both essential in the therapy of liver *** P2 X7 R might be a potential therapeutic strategy to treat liver fibrosis, we investigated whether the blockade of P2 X7 R could reverse liver fibrosis and how P2 X7 R is involved in fibrogenesis during hepatic stellate cells(HSCs) and macrophages crosstalk. METHODS In vivo,liver fibrosis model was established by thioacetamide(TAA) intraperitoneal administration in male C57 BL/6 mice. In vitro, LX-2 cells were treated with TGF-β and LPS/ATP respectively. Supernatant from LPS/ATP stimulated THP-1 macrophages were supplemented to LX-2 cells to mimic cellular crosstalk between HSCs and macrophages. RESULTS Blockade of P2 X7 R with its selective antagonist A438079, not only decreased liver injury and ECM deposition but also ameliorated inflammation by inhibiting NLRP3 inflammasome, NF-κB activation and IL-1β production in TAA-induced liver fibrosis. And the recruitment of macrophages, monocytes and granulocytes were also inhibited. In TGF-β-stimulated LX-2 cells,ECM deposition was reduced by the inhibiting of P2 X7 RTLR4-NLRP3 axis. Protein synthesis and cleavage of IL-1β and its m RNA level was dramatically increased by LPS 4 h combined with ATP 30 min than those in HSC treated with LPS or ATP alone. Additionally, LX-2 cells primed with LPS/ATP greatly increased m RNA and protein expression of caspase-1, NLRP3 and P2 x7 R, as well as liver fibrosis markers, α-SMA and typeⅠ*** events were remarkably suppressed by A438079 pretreatment. si RNA against P2 x7 R reduced protein expression of NLRP3 and α-SMA, and suppressed deposition and secretion of type Ⅰ collagen induced by LPS/ATP. Ectopic overexpression of P2 X7 R reduced the threshold of ECM deposition in HSCs induced by TGF-β.Inhibiting upstream receptors of NLRP3 inflammasome,P2 X7 receptor-selective antagonist(A438079), TLR4 inhibitor(CLI-095) reduced

关键词： liver fibrosis hepatic stellate cells macrophages P2x7R IL-1β

Photo-isomerization of Aromatic α-Hydroxy Hydrazone

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Chemical Research in Chinese Universities 2012年第5期28卷 886-890页

作者： JIN Jing-yi PAN Yan LI Xiu-hua HOU Jun WU Xue SU Zhong-min key laboratory of natural resources of changbai mountain&functional molecules Ministry of EducationYanbian UniversityYanji 133002P.R.China Institute of functional Material Chemistry Faculty of ChemistryNortheast Normal UniversityChangehun 130024P.R.China

Photo-isomerization of aromatic α-hydroxy hydrazone was reported. We investigated the structures of salicylaldehyde phenylhydrozone（SP） in the ground state using density functional theory（DFT） with the B3LYP functional and the 6-311＋G（d） basis set. All nine possible isomers of SP in the ground state consist of seven phenol forms and two ketone forms. Intrisic reaction coordinate（IRC） analysis discloses the existence of a cycle driven by the two proton transfer processes in the ground and excited states of SP, which suggests that no ketonic form could exist in the ground state. Further theoretical studies of the potential energy surfaces support a trans-cis conversion followed by a relaxation to the stable form of SP in the excited states.

关键词： Photo-isomerization Aromatic hydrazone Density functional theory Intrinsic reaction coordinate Potential energy surface