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
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.
