Stigmasterol is a plant sterol with anti-apoptotic,anti-oxidative and anti-inflammatory effect through multiple mechanisms.In this study,we further assessed whether it exerts protective effect on human brain microvess...Stigmasterol is a plant sterol with anti-apoptotic,anti-oxidative and anti-inflammatory effect through multiple mechanisms.In this study,we further assessed whether it exerts protective effect on human brain microvessel endothelial cells(HBMECs)against ischemia-reperfusion injury and explored the underlying mechanisms.HBMECs were used to establish an in vitro oxygen and glucose deprivation/reperfusion(OGD/R)model,while a middle cerebral artery occlusion(MCAO)model of rats were constructed.The interaction between stigmasterol and EPHA2 was detected by surface plasmon resonance(SPR)and cellular thermal shift assay(CETSA).The results showed that 10μmol·L−1 stigmasterol significantly protected cell viability,alleviated the loss of tight junction proteins and attenuated the blood-brain barrier(BBB)damage induced by OGD/R in the in vitro model.Subsequent molecular docking showed that stigmasterol might interact with EPHA2 at multiple sites,including T692,a critical gatekeep residue of this receptor.Exogenous ephrin-A1(an EPHA2 ligand)exacerbated OGD/R-induced EPHA2 phosphorylation at S897,facilitated ZO-1/claudin-5 loss,and promoted BBB leakage in vitro,which were significantly attenuated after stigmasterol treatment.The rat MCAO model confirmed these protective effects in vivo.In summary,these findings suggest that stigmasterol protects HBMECs against ischemia-reperfusion injury by maintaining cell viability,reducing the loss of tight junction proteins,and attenuating the BBB damage.These protective effects are at least meditated by its interaction with EPHA2 and inhibitory effect on EPHA2 phosphorylation.展开更多
A new stigmasterol 3, 7, 22-trihydoxystigmast-5-ene (1) and a new eremophilen- olide 8-methoxy-6-angeloyloxyeremophil-7(11)-en-8, 12-olide-14-oic acid (2) were isolated from Ligularia dolichobotrys Diels. Their struc...A new stigmasterol 3, 7, 22-trihydoxystigmast-5-ene (1) and a new eremophilen- olide 8-methoxy-6-angeloyloxyeremophil-7(11)-en-8, 12-olide-14-oic acid (2) were isolated from Ligularia dolichobotrys Diels. Their structures were deduced on the basis of spectral data.展开更多
Objective:To investigate the effect of combination therapy of chloroquine and stigmasterol on Plasmodium berghei(thereafter referred to as P.berghei)malaria-induced organ pathologies.Methods:Thirty five mice weighing ...Objective:To investigate the effect of combination therapy of chloroquine and stigmasterol on Plasmodium berghei(thereafter referred to as P.berghei)malaria-induced organ pathologies.Methods:Thirty five mice weighing 20-30 g were placed into seven groups of five mice each and distributed as uninfected administered 100 mg/kg BW stigmasterol,uninfected administered only feed and water ad libitum,infected with P.berghei and-administered 50 mg/kg BW stigmasterol,100 mg/kg BW stigmasterol,100 mg/kg BW stigmasterol plus 5 mg/kg BW chloroquine,and 5 mg/kg BW chloroquine.The last group of mice served as P.berghei infected and not treated control.The levels of parasitemia,packed cell volume,and other biochemical parameters were measured.Results:Combination therapy of P.berghei infection with stigmasterol and chloroquine did not significantly(P>0.05)reduce parasitemia level while stigmasterol treatment alone significantly(P<0.05)reduced the parasitemia level.However,the P.berghei induced anemia was decreased significantly(P<0.05)upon treatment with a combination of chloroquine and stigmasterol as well as with stigmasterol alone.Furthermore,the combination of chloroquine and stigmasterol significantly(P<0.05)decreased the activities of serum alanine aminotransferase,aspartate aminotransferase,urea and spleen total proteins levels in P.berghei mice in comparison with the untreated group.Treatment of P.berghei infected mice with stigmasterol alone and in combination with chloroquine significantly(P<0.05)increased the level of serum creatinine while serum and spleen malondialdehyde levels were significantly(P<0.05)decreased.Levels of glutathione in spleen and kidney were insignificantly(P>0.05)altered upon treatment with both doses of stigmasterol as well as the combination therapy.Conclusions:This study concluded that the combination of stigmasterol and chloroquine could combat anemia and some organ pathologies associated with P.berghei infection.展开更多
Objective:To investigate the effect of combination therapy of chloroquine and stigmasterol on Plasmodium(P.)berghei malaria-induced organ pathologies.Methods:Totally 35 mice weighing 20-30g were placed into 7 groups o...Objective:To investigate the effect of combination therapy of chloroquine and stigmasterol on Plasmodium(P.)berghei malaria-induced organ pathologies.Methods:Totally 35 mice weighing 20-30g were placed into 7 groups of 5 mice each and distributed as uninfected administered 100 mg/kg BW stigmasterol,uninfected administered only feed and water ad libitum,infected with P.berghei and administered 50 mg/Kg BW stigmasterol,100 mg/kg BW stigmasterol,100 mg/kg BW stigmasterol plus 5 mg/kg BW chloroquine,and 5 mg/kg BW chloroquine.The last group of mice served as P.berghei infected and not treated control.The levels of parasitemia,packed cell volume,and other biochemical parameters were measured.Results:Combination therapy of P.berghei infection with stigmasterol and chloroquine did not significantly(P>0.05)reduce parasitemia level while stigmasterol treatment alone significantly(P<0.05)reduced the parasitemia level.However,the P.berghei induced anemia was decreased significantly(P<0.05)upon treatment with a combination of chloroquine and stigmasterol as well as with stigmasterol alone.Furthermore,the combination of chloroquine and stigmasterol significantly(P<0.05)decreased the activities of serum alanine aminotransferase,aspartate aminotransferase,urea and level of spleen total proteins in P.berghei infected mice in comparison with the untreated group.Treatment of P.berghei infected mice with stigmasterol alone and in combination with chloroquine significantly(P<0.05)increased the level of serum creatinine while serum and spleen malondialdehyde levels were significantly(P<0.05)decreased.Levels of glutathione in spleen and kidney were insignificantly(P>0.05)altered upon treatment with both doses of stigmasterol as well as the combination therapy.Conclusions:This study concluded that the combination of stigmasterol and chloroquine could combat anemia and some organ pathologies associated with P.berghei infection.展开更多
Objective To study the chemical constituents of Aeschynomene indica.Methods The constituents were isolated and purified by means of silica gel column chromatography and recrytallization,and the structures were elucida...Objective To study the chemical constituents of Aeschynomene indica.Methods The constituents were isolated and purified by means of silica gel column chromatography and recrytallization,and the structures were elucidated by physicochemical properties and spectral analyses.Results Twelve compounds were obtained and elucidated as stigmasterol tritriacontanate(1),monotetracontane(2),taraxerol(3),stigmasterol(4),stearic acid(5),heptatria- contanoic acid(6),arachidic acid(7),ursolic acid acetate(8),quercetin(9),myricetin(10),myricetin-3-O-rhamnoside(11),and rutoside(12).Conclusion All the compounds are isolated from this plant for the first time and compound 1 is a new one.展开更多
Several stigamasterol saponins were concisely synthesized. Name!y, four monosaccharide （glucopyranose, galactopyranose, xylopyranose, 2-acetamido-2-deoxy-a-D-glucopyranose）, lactopyranose and chacotriose were couple...Several stigamasterol saponins were concisely synthesized. Name!y, four monosaccharide （glucopyranose, galactopyranose, xylopyranose, 2-acetamido-2-deoxy-a-D-glucopyranose）, lactopyranose and chacotriose were coupled with 3-OH of stigmasterol. All the compounds were identified by NMR, IR and high resolusion MS.展开更多
Objective:To perform a simultaneous quantitative estimation of two biologically active triterpenoid compounds lupeol and a steroid compound,stigmasterol,in Abutilon indicum(A.indicum)using high-performance thin-layer ...Objective:To perform a simultaneous quantitative estimation of two biologically active triterpenoid compounds lupeol and a steroid compound,stigmasterol,in Abutilon indicum(A.indicum)using high-performance thin-layer chromatography(HPTLC).Methods:TLC aluminum plates precoated with silica-gel 60 F254(20 cmí10 cm)were used with a mobile phase of toluene-methanol-formic acid(7.0:2.7:0.3,v/v/v)and densitometric determination of these compounds was carried out at 530 nm in reflectance/absorbance mode.Results:Compact bands for lupeol and stigmasterol were obtained at R_(f)0.52±0.02 and 0.28±0.05.The limit of detection(45 and 18 ng/band),limit of quantification(135 and 54 ng/band),recovery(98.2%-99.7%and 97.2%-99.6%)and precision(≤2.18 and 1.91)were satisfactory for lupeol and stigmasterol respectively.Linearity range for lupeol and stigmasterol were 100-1000(r^(2)=0.9994)and 50-500 ng/band(r^(2)=0.9941)and the contents were estimated as(0.59±0.10)%and(0.83±0.10)%w/w respectively.The total phenolic,flavonoid,proanthocyanidin,alkaloidal and saponin contents of methanolic extract of A.indicum were also measured in this work.According to International Conference on Harmonization(ICH)guidelines,the method was validated for linearity,precision,accuracy,and recovery,limit of detection,limit of quantification,specificity,and robustness.Conclusions:The HPTLC method was found to be reproducible,accurate,and precise and could detect these two compounds at nanogram level from the A.indicum.展开更多
目的 建立灵香草Lysimachia foenum-graecum一测多评法(quantitative analysis of multi-components by single marker,QAMS)多指标成分定量控制方法,采用多元统计分析模型评价不同产地灵香草质量差异。方法 以Prep Scalar C18柱为色谱...目的 建立灵香草Lysimachia foenum-graecum一测多评法(quantitative analysis of multi-components by single marker,QAMS)多指标成分定量控制方法,采用多元统计分析模型评价不同产地灵香草质量差异。方法 以Prep Scalar C18柱为色谱柱,乙腈-0.2%磷酸为流动相(梯度洗脱),以槲皮素和熊果酸为内参物,采用QAMS法同时测定灵香草中绿原酸、杨梅素、槲皮素、山柰酚、foenumoside B、零陵香皂苷C、齐墩果酸、熊果酸、豆甾醇和β-谷甾醇含量,同时用外标法验证QAMS法的准确性。依据《中国药典》检测浸出物、总灰分和酸不溶性灰分。进一步应用主成分分析(principal component analysis,PCA)、因子分析(factor analysis,FA)和正交偏最小二乘法判别分析(orthogonal partial least squares discriminant analysis,OPLS-DA)法对15批不同产地的灵香草进行区分比较,寻找差异因子。结果 建立的相对校正因子可用于定量分析,且耐用性良好;QAMS法与外标法结果无显著差异,但各批次间差异较大。PCA结果显示15批灵香草聚为3类,FA结果显示广东和广西产地的灵香草质量较优,OPLS-DA结果显示foenumoside B、山柰酚、零陵香皂苷C、绿原酸、槲皮素和豆甾醇是影响灵香草产品质量的差异性标志物。结论 基于多指标成分定量、多元统计分析评价灵香草质量的方法,为灵香草质量标准统一和提升提供基础资料。展开更多
Until recently,the main pharmaceuticals used to control cholesterol and prevent cardiovascular disease(CVD)were statin-related drugs,known for their historical side effects.Therefore,there is growing interest in explo...Until recently,the main pharmaceuticals used to control cholesterol and prevent cardiovascular disease(CVD)were statin-related drugs,known for their historical side effects.Therefore,there is growing interest in exploring alternatives,such as nutritional and dietary components,that could play a central role in CVD prevention.This review aims to provide a comprehensive understanding of how natural phytosterols found in various diets combat CVDs.We begin with a description of the overall approach,then we explore in detail the different direct and indirect mechanisms that contribute to reducing cardiovascular incidents.Phytosterols,including stigmasterol,β-sitosterol,ergosterol,and fucosterol,emerge as promising molecules within nutritional systems for protection against CVDs due to their beneficial effects at different levels through direct or indirect cellular,subcellular,and molecular mechanisms.Specifically,the mentioned phytosterols exhibit the ability to diminish the generation of various radicals,including hydroperoxides and hydrogen peroxide.They also promote the activation of antioxidant enzymes such as superoxide dismutase,catalase,and glutathione,while inhibiting lipid peroxidation through the activation of Nrf2 and Nrf2/heme oxygenase-1(HO-1)signaling pathways.Additionally,they demonstrate a significant inhibitory capacity in the generation of pro-inflammatory cytokines,thus playing a crucial role in regulating the inflammatory/immune response by inhibiting the expression of proteins involved in cellular signaling pathways such as JAK3/STAT3 and NF-κB.Moreover,phytosterols play a key role in reducing cholesterol absorption and improving the lipid profile.These compounds can be used as dietary supplements or included in specific diets to aid control cholesterol levels,particularly in individuals suffering from hypercholesterolemia.展开更多
基金supported by the Key Research Project of the Science&Technology Department of Sichuan Province,China(Nos.2021YFS0131 and 2020YFS0414).
文摘Stigmasterol is a plant sterol with anti-apoptotic,anti-oxidative and anti-inflammatory effect through multiple mechanisms.In this study,we further assessed whether it exerts protective effect on human brain microvessel endothelial cells(HBMECs)against ischemia-reperfusion injury and explored the underlying mechanisms.HBMECs were used to establish an in vitro oxygen and glucose deprivation/reperfusion(OGD/R)model,while a middle cerebral artery occlusion(MCAO)model of rats were constructed.The interaction between stigmasterol and EPHA2 was detected by surface plasmon resonance(SPR)and cellular thermal shift assay(CETSA).The results showed that 10μmol·L−1 stigmasterol significantly protected cell viability,alleviated the loss of tight junction proteins and attenuated the blood-brain barrier(BBB)damage induced by OGD/R in the in vitro model.Subsequent molecular docking showed that stigmasterol might interact with EPHA2 at multiple sites,including T692,a critical gatekeep residue of this receptor.Exogenous ephrin-A1(an EPHA2 ligand)exacerbated OGD/R-induced EPHA2 phosphorylation at S897,facilitated ZO-1/claudin-5 loss,and promoted BBB leakage in vitro,which were significantly attenuated after stigmasterol treatment.The rat MCAO model confirmed these protective effects in vivo.In summary,these findings suggest that stigmasterol protects HBMECs against ischemia-reperfusion injury by maintaining cell viability,reducing the loss of tight junction proteins,and attenuating the BBB damage.These protective effects are at least meditated by its interaction with EPHA2 and inhibitory effect on EPHA2 phosphorylation.
文摘A new stigmasterol 3, 7, 22-trihydoxystigmast-5-ene (1) and a new eremophilen- olide 8-methoxy-6-angeloyloxyeremophil-7(11)-en-8, 12-olide-14-oic acid (2) were isolated from Ligularia dolichobotrys Diels. Their structures were deduced on the basis of spectral data.
文摘Objective:To investigate the effect of combination therapy of chloroquine and stigmasterol on Plasmodium berghei(thereafter referred to as P.berghei)malaria-induced organ pathologies.Methods:Thirty five mice weighing 20-30 g were placed into seven groups of five mice each and distributed as uninfected administered 100 mg/kg BW stigmasterol,uninfected administered only feed and water ad libitum,infected with P.berghei and-administered 50 mg/kg BW stigmasterol,100 mg/kg BW stigmasterol,100 mg/kg BW stigmasterol plus 5 mg/kg BW chloroquine,and 5 mg/kg BW chloroquine.The last group of mice served as P.berghei infected and not treated control.The levels of parasitemia,packed cell volume,and other biochemical parameters were measured.Results:Combination therapy of P.berghei infection with stigmasterol and chloroquine did not significantly(P>0.05)reduce parasitemia level while stigmasterol treatment alone significantly(P<0.05)reduced the parasitemia level.However,the P.berghei induced anemia was decreased significantly(P<0.05)upon treatment with a combination of chloroquine and stigmasterol as well as with stigmasterol alone.Furthermore,the combination of chloroquine and stigmasterol significantly(P<0.05)decreased the activities of serum alanine aminotransferase,aspartate aminotransferase,urea and spleen total proteins levels in P.berghei mice in comparison with the untreated group.Treatment of P.berghei infected mice with stigmasterol alone and in combination with chloroquine significantly(P<0.05)increased the level of serum creatinine while serum and spleen malondialdehyde levels were significantly(P<0.05)decreased.Levels of glutathione in spleen and kidney were insignificantly(P>0.05)altered upon treatment with both doses of stigmasterol as well as the combination therapy.Conclusions:This study concluded that the combination of stigmasterol and chloroquine could combat anemia and some organ pathologies associated with P.berghei infection.
文摘Objective:To investigate the effect of combination therapy of chloroquine and stigmasterol on Plasmodium(P.)berghei malaria-induced organ pathologies.Methods:Totally 35 mice weighing 20-30g were placed into 7 groups of 5 mice each and distributed as uninfected administered 100 mg/kg BW stigmasterol,uninfected administered only feed and water ad libitum,infected with P.berghei and administered 50 mg/Kg BW stigmasterol,100 mg/kg BW stigmasterol,100 mg/kg BW stigmasterol plus 5 mg/kg BW chloroquine,and 5 mg/kg BW chloroquine.The last group of mice served as P.berghei infected and not treated control.The levels of parasitemia,packed cell volume,and other biochemical parameters were measured.Results:Combination therapy of P.berghei infection with stigmasterol and chloroquine did not significantly(P>0.05)reduce parasitemia level while stigmasterol treatment alone significantly(P<0.05)reduced the parasitemia level.However,the P.berghei induced anemia was decreased significantly(P<0.05)upon treatment with a combination of chloroquine and stigmasterol as well as with stigmasterol alone.Furthermore,the combination of chloroquine and stigmasterol significantly(P<0.05)decreased the activities of serum alanine aminotransferase,aspartate aminotransferase,urea and level of spleen total proteins in P.berghei infected mice in comparison with the untreated group.Treatment of P.berghei infected mice with stigmasterol alone and in combination with chloroquine significantly(P<0.05)increased the level of serum creatinine while serum and spleen malondialdehyde levels were significantly(P<0.05)decreased.Levels of glutathione in spleen and kidney were insignificantly(P>0.05)altered upon treatment with both doses of stigmasterol as well as the combination therapy.Conclusions:This study concluded that the combination of stigmasterol and chloroquine could combat anemia and some organ pathologies associated with P.berghei infection.
基金Guangxi Administration of Traditional Chinese Medicine Science and Technology Special,China(GZKZ09-45)
文摘Objective To study the chemical constituents of Aeschynomene indica.Methods The constituents were isolated and purified by means of silica gel column chromatography and recrytallization,and the structures were elucidated by physicochemical properties and spectral analyses.Results Twelve compounds were obtained and elucidated as stigmasterol tritriacontanate(1),monotetracontane(2),taraxerol(3),stigmasterol(4),stearic acid(5),heptatria- contanoic acid(6),arachidic acid(7),ursolic acid acetate(8),quercetin(9),myricetin(10),myricetin-3-O-rhamnoside(11),and rutoside(12).Conclusion All the compounds are isolated from this plant for the first time and compound 1 is a new one.
基金Project supported by the National Natural Science Foundation of China （No. 30400564）.
文摘Several stigamasterol saponins were concisely synthesized. Name!y, four monosaccharide （glucopyranose, galactopyranose, xylopyranose, 2-acetamido-2-deoxy-a-D-glucopyranose）, lactopyranose and chacotriose were coupled with 3-OH of stigmasterol. All the compounds were identified by NMR, IR and high resolusion MS.
文摘Objective:To perform a simultaneous quantitative estimation of two biologically active triterpenoid compounds lupeol and a steroid compound,stigmasterol,in Abutilon indicum(A.indicum)using high-performance thin-layer chromatography(HPTLC).Methods:TLC aluminum plates precoated with silica-gel 60 F254(20 cmí10 cm)were used with a mobile phase of toluene-methanol-formic acid(7.0:2.7:0.3,v/v/v)and densitometric determination of these compounds was carried out at 530 nm in reflectance/absorbance mode.Results:Compact bands for lupeol and stigmasterol were obtained at R_(f)0.52±0.02 and 0.28±0.05.The limit of detection(45 and 18 ng/band),limit of quantification(135 and 54 ng/band),recovery(98.2%-99.7%and 97.2%-99.6%)and precision(≤2.18 and 1.91)were satisfactory for lupeol and stigmasterol respectively.Linearity range for lupeol and stigmasterol were 100-1000(r^(2)=0.9994)and 50-500 ng/band(r^(2)=0.9941)and the contents were estimated as(0.59±0.10)%and(0.83±0.10)%w/w respectively.The total phenolic,flavonoid,proanthocyanidin,alkaloidal and saponin contents of methanolic extract of A.indicum were also measured in this work.According to International Conference on Harmonization(ICH)guidelines,the method was validated for linearity,precision,accuracy,and recovery,limit of detection,limit of quantification,specificity,and robustness.Conclusions:The HPTLC method was found to be reproducible,accurate,and precise and could detect these two compounds at nanogram level from the A.indicum.
基金funded by the Deputyship for Research and Innovation,Ministry of Education in Saudi Arabia(Project number ISP23-81)Sunway University Research Accelerator Grant Scheme(GRTIN-RAG-SBMDC-10-2024).
文摘Until recently,the main pharmaceuticals used to control cholesterol and prevent cardiovascular disease(CVD)were statin-related drugs,known for their historical side effects.Therefore,there is growing interest in exploring alternatives,such as nutritional and dietary components,that could play a central role in CVD prevention.This review aims to provide a comprehensive understanding of how natural phytosterols found in various diets combat CVDs.We begin with a description of the overall approach,then we explore in detail the different direct and indirect mechanisms that contribute to reducing cardiovascular incidents.Phytosterols,including stigmasterol,β-sitosterol,ergosterol,and fucosterol,emerge as promising molecules within nutritional systems for protection against CVDs due to their beneficial effects at different levels through direct or indirect cellular,subcellular,and molecular mechanisms.Specifically,the mentioned phytosterols exhibit the ability to diminish the generation of various radicals,including hydroperoxides and hydrogen peroxide.They also promote the activation of antioxidant enzymes such as superoxide dismutase,catalase,and glutathione,while inhibiting lipid peroxidation through the activation of Nrf2 and Nrf2/heme oxygenase-1(HO-1)signaling pathways.Additionally,they demonstrate a significant inhibitory capacity in the generation of pro-inflammatory cytokines,thus playing a crucial role in regulating the inflammatory/immune response by inhibiting the expression of proteins involved in cellular signaling pathways such as JAK3/STAT3 and NF-κB.Moreover,phytosterols play a key role in reducing cholesterol absorption and improving the lipid profile.These compounds can be used as dietary supplements or included in specific diets to aid control cholesterol levels,particularly in individuals suffering from hypercholesterolemia.
