2-Deoxy glycosides are widely presented in natural products and clinical reagents.The presence of 2-deoxy glycosides is essential for bioactivities of these compounds.This report provides an overview of the recent adv...2-Deoxy glycosides are widely presented in natural products and clinical reagents.The presence of 2-deoxy glycosides is essential for bioactivities of these compounds.This report provides an overview of the recent advances in the stereoselective synthesis of 2-deoxy glycosides.Particularly,the contents of this review covered the work published since the earlier reviews on this topic by Marzabadi(2000),Lowary(2009),Ding(2012) and Nagorny(2012).展开更多
Objective To evaluate the in vitro anti-hypertrophic effect of total Glycosides of Ranunculus Japonius (TGRJ). Methods Neonatal rat cardiomyocytes were cultured and hypertrophy was induced by adminis- trating isopr...Objective To evaluate the in vitro anti-hypertrophic effect of total Glycosides of Ranunculus Japonius (TGRJ). Methods Neonatal rat cardiomyocytes were cultured and hypertrophy was induced by adminis- trating isoproterenol (ISO, 10 gmol/L) or angiotensin Ⅱ (AngⅡ, 1 gmol/L) for 48 hours. In the treatment groups, cells were pretreated with TGRJ (0.3 g/L) for 30 minutes prior to hypertrophic stimuli. The anti-hypertrophic effects of TGRJ were examined by measuring cell size, total protein content, and protein synthesis. Intracellular free Ca2+ concentration ([Ca2+]i) was evaluated using fluorescence dye Fura-2/AM. Sacroplasmic/endoplasmic reticulum Ca2+ ATPase 2a (SERCA2a), atrial natriuretic peptide (ANP), B-type natriuretic peptide (BNP), and beta-myosin heavy chain (β-MHC) protein expression levels were measured by Western blotting. SERCA2a activity was assayed by p-nitrophenal phosphate disodium salt hexahydrate method. Results Increased cell size, total protein content, and protein synthesis following ISO or Ang II stimulation were significantly inhibited by pretreatment with TGRJ (all P〈0.05). This anti-hypertrophic effect of TGRJ was confirmed by its suppressing effect on elevated expression of the three hypertrophic related genetic markers, ANP, BNP, and ^-MHC. In addition, TGRJ inhibited ISO or Ang Ⅱ induced up-regulation of [Ca2+] under chronic but not acute conditions. And ISO or Ang Ⅱ induced down-regulation of SERCA2a expression and activity was also effectively rectified byTGRJ pretreatment. Conclusions The results of present study suggested that TGRJ could prevent ISO or Ang Ⅱ induced cardiac hypertrophy through improving chronic [Ca2+]i disorder, might via normalizing SERCA2a expression and activity.展开更多
Two new dammarane glycosides named notoginsenoside T-1 and T-2 were isolated from the mild acid hydrolysis products of the root saponins of Panax notoginseng. On the basis of spectroscopic evidences, their structures ...Two new dammarane glycosides named notoginsenoside T-1 and T-2 were isolated from the mild acid hydrolysis products of the root saponins of Panax notoginseng. On the basis of spectroscopic evidences, their structures were elucidated to be 6-O-beta -D-glucopyranosyl-24(25)-epoxy-3 beta ,6 alpha ,12 beta ,23 xi -tetrahydroxydammar-20(22)(E)-ene 1 and 6-O-beta -D-glucopyranosyl-24(25)-epoxy-23 xi -methoxyl-3 beta ,6 alpha ,12 beta -trihydroxydamm-ar-20(22)(E)-ene 2, respectively.展开更多
Two new flavonol glycosides, tamarixetin 3-O-β-D-xylopyranosyl-(1-2)-α-L-ribopyranoside (1) and tamarixetin 3-O-α-L-ribopyranoside (2) were isolated from the leaves of Bridelia tomentosa. Their structures wer...Two new flavonol glycosides, tamarixetin 3-O-β-D-xylopyranosyl-(1-2)-α-L-ribopyranoside (1) and tamarixetin 3-O-α-L-ribopyranoside (2) were isolated from the leaves of Bridelia tomentosa. Their structures were elucidated by 1D and 2D NMR analysis, as well as MS and IR spectra.展开更多
Two new compounds 7-hydroxy-5-O-(β-D-glucopyranoside) flavan (1) and (Z)-4',6'-dihydroxy-2'-O-(β-D-glucopyranoside) chalcone (2), along with eight known compounds, were isolated from the stem bark of Dr...Two new compounds 7-hydroxy-5-O-(β-D-glucopyranoside) flavan (1) and (Z)-4',6'-dihydroxy-2'-O-(β-D-glucopyranoside) chalcone (2), along with eight known compounds, were isolated from the stem bark of Drypetes parvifolia (Euphorbiaceae). Their structures were established on the basis of spectroscopic analysis and chemical evidence.展开更多
OBJECTIVE PP2Ac demethyl⁃ation is regulated by LCMT(a specific leucine carboxyl methyltransferase catalyzing methyla⁃tion of PP2A)and PME(a specific methylester⁃ase catalyzing demethylation of PP2A.This study was to i...OBJECTIVE PP2Ac demethyl⁃ation is regulated by LCMT(a specific leucine carboxyl methyltransferase catalyzing methyla⁃tion of PP2A)and PME(a specific methylester⁃ase catalyzing demethylation of PP2A.This study was to investigate the mechanism of Cor⁃nel iridoid glycoside(CIG)on PP2A catalytic sub⁃unit C(PP2Ac).METHODS Recombined lentivi⁃rus vector was used to deliver PME-1 genetic materials into N2a cells or transfected LCMT-1 siRNA into N2a cells to block the expression of LCMT-1.Twenty-four hours later,cells were rinsed twice with cold PBS(pH 7.4)and CIG at different concentrations(50,100 and 200 g·L^(-1),respectively)were added for 24 h.Western blotting was used to PP2Ac,demethylaion/methylation PP2Ac,LCMT-1 and PME-1.The ac⁃tivity of PP2A was detected by a biochemical as⁃say.RESULTS①Lentivirus transferred PME-1 was expressed at high level in the N2a cells after transduction.Correspondingly,the demethylation of PP2Ac was increasing and PP2A activity was decreasing after transduction.Treatment with CIG for 24 h reversed the increase of PME-1 and demethylation of PP2Ac without influencing LCMT-1 expression.PP2A activity was also sig⁃nificantly enhanced in CIG treatment group,compared with the cells after PME-1 transduc⁃tion.②LCMT-1 siRNA significantly decreased LCMT-1 expression.CIG did not affect LCMT-1expression.however,demethylation of PP2Ac is increased in siRNA-transfected cells and CIG could reversed the high demethylation of PP2Ac and PP2A activity.CONLUSION CIG increases methylation of PP2A subunit C by inhibiting PME-1.展开更多
Two new phloroglucinol glycosides, 2,6-dihydroxy-3,5-dimethyl-1-isobutyrylbenzene-4-O-beta-D-glucoside and 2,6-dihydroxy-3,5-dimethyl-1-(2-methylbutyryl) benzene-4-O-beta-D-glucoside were isolated from Hypericum japon...Two new phloroglucinol glycosides, 2,6-dihydroxy-3,5-dimethyl-1-isobutyrylbenzene-4-O-beta-D-glucoside and 2,6-dihydroxy-3,5-dimethyl-1-(2-methylbutyryl) benzene-4-O-beta-D-glucoside were isolated from Hypericum japonicum. Their structures were determined by spectroscopic and chemical methods.展开更多
目的探讨雷公藤多苷对Ig A肾病(Ig A nephropathy,Ig AN)患者血清离子及β2糖蛋白I(β2-glycoprotein,β2-GPI)/氧化低密度脂蛋白(oxidized low density lipoprotein,ox-LDL)的影响。方法收集丽水市人民医院肾内科2014年1月~2015...目的探讨雷公藤多苷对Ig A肾病(Ig A nephropathy,Ig AN)患者血清离子及β2糖蛋白I(β2-glycoprotein,β2-GPI)/氧化低密度脂蛋白(oxidized low density lipoprotein,ox-LDL)的影响。方法收集丽水市人民医院肾内科2014年1月~2015年4月收治的原发性Ig AN患者54例,随机分为对照组和实验组,每组27例,对照组患者常规给予盐酸贝那普利片10 mg,1次/天口服;给予双嘧达莫片50 mg,3次/天口服,实验组在对照组基础上给予雷公藤多苷片20 mg,3次/天口服。2组患者均治疗6个月。治疗结束后,对所有患者的血清Ca、P、β2-GPI/ox-LDL水平及肾功能相关指标进行检测。结果与对照组治疗后比较,实验组患者血清Ca水平较高,血清P水平较低(P〈0.05);实验组患者的血清β2-GPI/ox-LDL水平较低(P〈0.05);实验组患者的血清Scr、BUN水平较低(P〈0.05)。结论雷公藤多苷能够显著降低Ig AN患者血清P、β2-GPI/ox-LDL、Scr及BUN水平,提高血清Ca水平,改善肾功能。展开更多
基金supported by the National Natural Science Foundation of China(21272082,21402055,21472054,21672077)the State Key Laboratory of Bio-organic and Natural Products Chemistry(SKLBNPC13425)+3 种基金Natural Science Funds of Hubei Province for Distinguished Young Scholars(2015CFA035)"Thousand Talents Program"Young Investigator AwardWuhan Creative Talent Development FundHuazhong University of Science and Technology(2014ZZGH015)
文摘2-Deoxy glycosides are widely presented in natural products and clinical reagents.The presence of 2-deoxy glycosides is essential for bioactivities of these compounds.This report provides an overview of the recent advances in the stereoselective synthesis of 2-deoxy glycosides.Particularly,the contents of this review covered the work published since the earlier reviews on this topic by Marzabadi(2000),Lowary(2009),Ding(2012) and Nagorny(2012).
文摘Objective To evaluate the in vitro anti-hypertrophic effect of total Glycosides of Ranunculus Japonius (TGRJ). Methods Neonatal rat cardiomyocytes were cultured and hypertrophy was induced by adminis- trating isoproterenol (ISO, 10 gmol/L) or angiotensin Ⅱ (AngⅡ, 1 gmol/L) for 48 hours. In the treatment groups, cells were pretreated with TGRJ (0.3 g/L) for 30 minutes prior to hypertrophic stimuli. The anti-hypertrophic effects of TGRJ were examined by measuring cell size, total protein content, and protein synthesis. Intracellular free Ca2+ concentration ([Ca2+]i) was evaluated using fluorescence dye Fura-2/AM. Sacroplasmic/endoplasmic reticulum Ca2+ ATPase 2a (SERCA2a), atrial natriuretic peptide (ANP), B-type natriuretic peptide (BNP), and beta-myosin heavy chain (β-MHC) protein expression levels were measured by Western blotting. SERCA2a activity was assayed by p-nitrophenal phosphate disodium salt hexahydrate method. Results Increased cell size, total protein content, and protein synthesis following ISO or Ang II stimulation were significantly inhibited by pretreatment with TGRJ (all P〈0.05). This anti-hypertrophic effect of TGRJ was confirmed by its suppressing effect on elevated expression of the three hypertrophic related genetic markers, ANP, BNP, and ^-MHC. In addition, TGRJ inhibited ISO or Ang Ⅱ induced up-regulation of [Ca2+] under chronic but not acute conditions. And ISO or Ang Ⅱ induced down-regulation of SERCA2a expression and activity was also effectively rectified byTGRJ pretreatment. Conclusions The results of present study suggested that TGRJ could prevent ISO or Ang Ⅱ induced cardiac hypertrophy through improving chronic [Ca2+]i disorder, might via normalizing SERCA2a expression and activity.
基金the members of analytic group of Laboratory of Phytochemistry, Kunming Institute of Botany, Chinese Academy of Sciences.
文摘Two new dammarane glycosides named notoginsenoside T-1 and T-2 were isolated from the mild acid hydrolysis products of the root saponins of Panax notoginseng. On the basis of spectroscopic evidences, their structures were elucidated to be 6-O-beta -D-glucopyranosyl-24(25)-epoxy-3 beta ,6 alpha ,12 beta ,23 xi -tetrahydroxydammar-20(22)(E)-ene 1 and 6-O-beta -D-glucopyranosyl-24(25)-epoxy-23 xi -methoxyl-3 beta ,6 alpha ,12 beta -trihydroxydamm-ar-20(22)(E)-ene 2, respectively.
文摘Two new flavonol glycosides, tamarixetin 3-O-β-D-xylopyranosyl-(1-2)-α-L-ribopyranoside (1) and tamarixetin 3-O-α-L-ribopyranoside (2) were isolated from the leaves of Bridelia tomentosa. Their structures were elucidated by 1D and 2D NMR analysis, as well as MS and IR spectra.
基金One of the authors(J.Wandji)is grateful for grant(No.F/2624-3F)from the International Foundation for Science(Sweden)the sponsorship of the"UniversitéParis Descartes,France"during his multiple research visits in Paris.
文摘Two new compounds 7-hydroxy-5-O-(β-D-glucopyranoside) flavan (1) and (Z)-4',6'-dihydroxy-2'-O-(β-D-glucopyranoside) chalcone (2), along with eight known compounds, were isolated from the stem bark of Drypetes parvifolia (Euphorbiaceae). Their structures were established on the basis of spectroscopic analysis and chemical evidence.
文摘OBJECTIVE PP2Ac demethyl⁃ation is regulated by LCMT(a specific leucine carboxyl methyltransferase catalyzing methyla⁃tion of PP2A)and PME(a specific methylester⁃ase catalyzing demethylation of PP2A.This study was to investigate the mechanism of Cor⁃nel iridoid glycoside(CIG)on PP2A catalytic sub⁃unit C(PP2Ac).METHODS Recombined lentivi⁃rus vector was used to deliver PME-1 genetic materials into N2a cells or transfected LCMT-1 siRNA into N2a cells to block the expression of LCMT-1.Twenty-four hours later,cells were rinsed twice with cold PBS(pH 7.4)and CIG at different concentrations(50,100 and 200 g·L^(-1),respectively)were added for 24 h.Western blotting was used to PP2Ac,demethylaion/methylation PP2Ac,LCMT-1 and PME-1.The ac⁃tivity of PP2A was detected by a biochemical as⁃say.RESULTS①Lentivirus transferred PME-1 was expressed at high level in the N2a cells after transduction.Correspondingly,the demethylation of PP2Ac was increasing and PP2A activity was decreasing after transduction.Treatment with CIG for 24 h reversed the increase of PME-1 and demethylation of PP2Ac without influencing LCMT-1 expression.PP2A activity was also sig⁃nificantly enhanced in CIG treatment group,compared with the cells after PME-1 transduc⁃tion.②LCMT-1 siRNA significantly decreased LCMT-1 expression.CIG did not affect LCMT-1expression.however,demethylation of PP2Ac is increased in siRNA-transfected cells and CIG could reversed the high demethylation of PP2Ac and PP2A activity.CONLUSION CIG increases methylation of PP2A subunit C by inhibiting PME-1.
文摘Two new phloroglucinol glycosides, 2,6-dihydroxy-3,5-dimethyl-1-isobutyrylbenzene-4-O-beta-D-glucoside and 2,6-dihydroxy-3,5-dimethyl-1-(2-methylbutyryl) benzene-4-O-beta-D-glucoside were isolated from Hypericum japonicum. Their structures were determined by spectroscopic and chemical methods.