Aim To establish a sensitive and specific liquid chromatography-massspeetrometry method for determination of scutellarin in rabbit plasma after oral administration.Methods For the quantitative analysis, rutin was used...Aim To establish a sensitive and specific liquid chromatography-massspeetrometry method for determination of scutellarin in rabbit plasma after oral administration.Methods For the quantitative analysis, rutin was used as an internal standard and solid-phaseextraction (SPE) was performed by using a Phenomenex C_8 cartridge. HPLC was carried out using aZorbax Extend-C_(18) column (150 mm x 2.1 mm ID, 5 μm) with a guard cartridge (Phenomenex) .Gradient elution was selected with the mobile phase of methanol 10 mmol·L^(-1) ammonium acetatesolution (pH adjusted to 8.0 with ammonia solution). The flow rate of mobile phase was 0.4mL·min^(-1) and the column temperature was 35 ℃ . Both scutellarin and the internal standard rutinin rabbit plasma extracts were detected by mass spectrometry using an ESI interface in the negativeion mode. Results The linear range was from 2 to 200 ng· mL^(-1), with acceptable accuracy andprecision (RSD) . Conclusion A sensitive, reliable and accurate method for the quantitation ofscutellarin in rabbit plasma has been established.展开更多
A new glycoside, gamma-pyranone-3-O-beta-D-[6'-(4'-hydroxy-3',5'-dimethyoxybenzoyl)]-glucopyranoside (erigeside D, 2), together with nine known compounds, viz., erigeside I (1), erigeside A (3), eriges...A new glycoside, gamma-pyranone-3-O-beta-D-[6'-(4'-hydroxy-3',5'-dimethyoxybenzoyl)]-glucopyranoside (erigeside D, 2), together with nine known compounds, viz., erigeside I (1), erigeside A (3), erigeside B (4), erigeside II (5), scopolin (6), icariside B-2 (7), blumenol C glucoside (8), (+)-syringaresinol O-beta-D-glucopyranoside (9) and scutellarein-7-O-beta-D-glucuronide methyl ester (10), was isolated from Erigeron breviscapus (Vant.) Hand.-Mazz. Their structures were established on the basis of spectral evidence. According to the beta-glucopyranosyl moiety in 7, the absolute configuration of 7 was determined by X-ray crystallographic analysis. Compounds 7, 8 and 9 were isolated for the first time from this genus, an compound 6 was first obtained from this plant.展开更多
Aim To establish an RP-HPLC method for the determination of scutellarin in plasma and study its pharmacokinetics in dogs. Methods Scutellarin was given to dogs by intravenous injection and determined by RP-HPLC, the m...Aim To establish an RP-HPLC method for the determination of scutellarin in plasma and study its pharmacokinetics in dogs. Methods Scutellarin was given to dogs by intravenous injection and determined by RP-HPLC, the mean plasma concentration-time curve was plotted and pharmacokinetic parameters were calculated by program 3p87. Resu;ts The concentration-time curve of scutellarin could be fitted to three-compartment model with T1/2 pi, T1/2 α and T1/2 β being 1.05 ± 0.80 min, 6.99 + 2.76 min and 51.61 + 28.78 min, respectively, Vc being 880.1 + 508.3 mL, CL being 189.6 + 53.8 mL@ min- 1, and AUC0-90 and AUC0-∞ being 574.43 + 133.95 μg@ min@ mL - 1 and 599.34 ± 132.00μg@ min@mL- 1, respectively. Conclusion The fact that the concentrations of scutellarin in plasma declined rapidly after the medication suggested that the T1/2 of scutellarin should be taken into account in drug administration and preparation development.展开更多
On the basis of extensive literature retrieval, the species, composition, pharmacology, clinical application, contraindication of Adonis L. were reviewed in this paper, to provide data for the its further development ...On the basis of extensive literature retrieval, the species, composition, pharmacology, clinical application, contraindication of Adonis L. were reviewed in this paper, to provide data for the its further development and utilization.展开更多
Five caffeoyl conjugates were isolated from the ethyl acetate soluble fraction of Erigeron breviscapus (Van.) Hand_Mazz for the first time. Along with them, nine other chemical constituents were also identified. O...Five caffeoyl conjugates were isolated from the ethyl acetate soluble fraction of Erigeron breviscapus (Van.) Hand_Mazz for the first time. Along with them, nine other chemical constituents were also identified. One new caffeoyl conjugate, erigoster A (1) with a novel basic skeleton was mainly assigned by the using a combination of two_dimensional NMR techniques.展开更多
\ Effects of breviscapine, the active ingredient isolated from Erigeron breviscapus (Vant) Handmazz, on the changes in antioxidant enzyme activity induced by cerebral ischemiareperfusion in rats were explored. It wa...\ Effects of breviscapine, the active ingredient isolated from Erigeron breviscapus (Vant) Handmazz, on the changes in antioxidant enzyme activity induced by cerebral ischemiareperfusion in rats were explored. It was found that breviscapine improved the activities of superoxide dismutase (SOD), GSHperoxidase and catalase, while decreasing the malondialdehyde (MDA) content in the brain, which was benificial in reducing the damage from cerebral ischemiareperfusion.展开更多
The mechanisms by which breviscapine (Bre) inhibits the lipid preoxidation in rat brain mitochondria were investigated. The mitochondrial lipid peroxidation of rat brain induced by oxygen free radical was measured by ...The mechanisms by which breviscapine (Bre) inhibits the lipid preoxidation in rat brain mitochondria were investigated. The mitochondrial lipid peroxidation of rat brain induced by oxygen free radical was measured by thiobarbituric acid spectrophotometry. The chelating activities of Bre for Fe 2+ were tested by differential spectrum. Superoxide anion (O 2)from xanthine xanthine oxidase (Xan XO) system and hydroxyl radical (·OH) from FeSO 4 H 2O 2 system were determined with spectrophotometry. It was found that Bre could effectively inhibit the lipid peroxidation of brain mitochondria induced by free radicals driven from Xan XO and FeSO 4 H 2O 2 system. The IC 50 of Bre were 93 01 μmol·L -1 for Xan XO system and 62 18 μmol·L -1 for FeSO 4 H 2O 2 system. Bre also scavenged O 2 and ·OH produced by Xan XO and FeSO 4 H 2O 2 systems. The IC 50 of Bre were 32 63 μmol·L -1 for O - 2 and 20 22 μmol·L -1 for ·OH. Furthermore, the chelating Fe 2+ activity of Bre was shown. It may be concluded that Bre inhibited lipid peroxidation at different stages of the reaction of oxygen free redial with the mitochondria membrane: (1) the formation of ·OH; (2) the initiation of the lipid peroxidation, by chelating Fe 2+ and scavenging O 2 as well as ·OH. The scavenging oxygen free radicals and chelating iron are the mechanisms of inhibitory effect of Bre on lipid peroxidation.展开更多
AIM:To study the effect of breviscapine (Bre) on activity of protein kinase Cα (PKCα) and nuclear factor (NF)-κB in pancreas,and the mechanism of Bre attenuating acute pancreatitis (AP). METHODS:One hundred and eig...AIM:To study the effect of breviscapine (Bre) on activity of protein kinase Cα (PKCα) and nuclear factor (NF)-κB in pancreas,and the mechanism of Bre attenuating acute pancreatitis (AP). METHODS:One hundred and eight rats were randomly divided into acute necrotizing pancreatitis (ANP) group,Bre group (ANP + Bre group) and sham operation (SO) group,36 rats in each group. ANP model was induced by a retrograde injection of 4% sodium deoxycholate into the bilio-pancreatic duct. Fifteen minutes after the ANP model was induced,the rats in Bre group were intraperitoneally injected with Bre (0.4 mg/100 g body weight or 0.1 mL/100 g body weight). Survival time and mortality of rats were calculated. Serum amylase and malondialdehyde levels were measured,volume of ascites was recorded and morphology of pancreas and lung was evaluated at 1,5 and 10 h,after the ANP model was induced,respectively. Expressions of PKCα and subunit p65 of NF-κB in pancreas were detected by immunohistochemistry and Western blotting. RESULTS:The life span of rats was longer and the mortality was lower in Bre group than in ANP group 13.51 ± 5.46 vs 25.36 ± 8.11 (P < 0.05). The amylase and MDA levels as well as the volume of ascites were lower and the pathological changes in pancreas and lung were less in Bre group than ANP group (P < 0.05),indicating that the pancreatitis is less severe in Bre group than ANP group. The activation of PKCα and NF-κB p65 in pancreas was induced rapidly and reached their peak at 1 h or 5 h after ANP,but their activity in Bre group was significantly inhibited. CONCLUSION:Bre exerts its therapeutic effect on AP by inhibiting the activation of PKCα and NF-κB p65 in pancreas.展开更多
Lutein and lutein esters in marigold flowers was quantitatively determined by high performance chromatography (HPLC) with ODS-C 18 column.A mixture of CH3CNCD*2CH3OHCD*2CH3COOCH2CH3 with volume ratio of 55∶1∶44 wa...Lutein and lutein esters in marigold flowers was quantitatively determined by high performance chromatography (HPLC) with ODS-C 18 column.A mixture of CH3CNCD*2CH3OHCD*2CH3COOCH2CH3 with volume ratio of 55∶1∶44 was used as mobile phase at a flow rate of 1.0 mL/min and detection was carried out at 460nm. The column temperature was about 20℃. The contents of lutein and lutein esters were determined by analytical curve of lutein since lutein and lutein esters have the same spectral characteristics. Determination results of hexane extracts and saponified samples of lutein show that the saponification transforms the esters into free lutein. The increase of the content of dipalmitate and palmitate stearate reveals that the reaction includes transesterifications.展开更多
文摘Aim To establish a sensitive and specific liquid chromatography-massspeetrometry method for determination of scutellarin in rabbit plasma after oral administration.Methods For the quantitative analysis, rutin was used as an internal standard and solid-phaseextraction (SPE) was performed by using a Phenomenex C_8 cartridge. HPLC was carried out using aZorbax Extend-C_(18) column (150 mm x 2.1 mm ID, 5 μm) with a guard cartridge (Phenomenex) .Gradient elution was selected with the mobile phase of methanol 10 mmol·L^(-1) ammonium acetatesolution (pH adjusted to 8.0 with ammonia solution). The flow rate of mobile phase was 0.4mL·min^(-1) and the column temperature was 35 ℃ . Both scutellarin and the internal standard rutinin rabbit plasma extracts were detected by mass spectrometry using an ESI interface in the negativeion mode. Results The linear range was from 2 to 200 ng· mL^(-1), with acceptable accuracy andprecision (RSD) . Conclusion A sensitive, reliable and accurate method for the quantitation ofscutellarin in rabbit plasma has been established.
文摘A new glycoside, gamma-pyranone-3-O-beta-D-[6'-(4'-hydroxy-3',5'-dimethyoxybenzoyl)]-glucopyranoside (erigeside D, 2), together with nine known compounds, viz., erigeside I (1), erigeside A (3), erigeside B (4), erigeside II (5), scopolin (6), icariside B-2 (7), blumenol C glucoside (8), (+)-syringaresinol O-beta-D-glucopyranoside (9) and scutellarein-7-O-beta-D-glucuronide methyl ester (10), was isolated from Erigeron breviscapus (Vant.) Hand.-Mazz. Their structures were established on the basis of spectral evidence. According to the beta-glucopyranosyl moiety in 7, the absolute configuration of 7 was determined by X-ray crystallographic analysis. Compounds 7, 8 and 9 were isolated for the first time from this genus, an compound 6 was first obtained from this plant.
文摘Aim To establish an RP-HPLC method for the determination of scutellarin in plasma and study its pharmacokinetics in dogs. Methods Scutellarin was given to dogs by intravenous injection and determined by RP-HPLC, the mean plasma concentration-time curve was plotted and pharmacokinetic parameters were calculated by program 3p87. Resu;ts The concentration-time curve of scutellarin could be fitted to three-compartment model with T1/2 pi, T1/2 α and T1/2 β being 1.05 ± 0.80 min, 6.99 + 2.76 min and 51.61 + 28.78 min, respectively, Vc being 880.1 + 508.3 mL, CL being 189.6 + 53.8 mL@ min- 1, and AUC0-90 and AUC0-∞ being 574.43 + 133.95 μg@ min@ mL - 1 and 599.34 ± 132.00μg@ min@mL- 1, respectively. Conclusion The fact that the concentrations of scutellarin in plasma declined rapidly after the medication suggested that the T1/2 of scutellarin should be taken into account in drug administration and preparation development.
文摘On the basis of extensive literature retrieval, the species, composition, pharmacology, clinical application, contraindication of Adonis L. were reviewed in this paper, to provide data for the its further development and utilization.
文摘Five caffeoyl conjugates were isolated from the ethyl acetate soluble fraction of Erigeron breviscapus (Van.) Hand_Mazz for the first time. Along with them, nine other chemical constituents were also identified. One new caffeoyl conjugate, erigoster A (1) with a novel basic skeleton was mainly assigned by the using a combination of two_dimensional NMR techniques.
文摘\ Effects of breviscapine, the active ingredient isolated from Erigeron breviscapus (Vant) Handmazz, on the changes in antioxidant enzyme activity induced by cerebral ischemiareperfusion in rats were explored. It was found that breviscapine improved the activities of superoxide dismutase (SOD), GSHperoxidase and catalase, while decreasing the malondialdehyde (MDA) content in the brain, which was benificial in reducing the damage from cerebral ischemiareperfusion.
文摘The mechanisms by which breviscapine (Bre) inhibits the lipid preoxidation in rat brain mitochondria were investigated. The mitochondrial lipid peroxidation of rat brain induced by oxygen free radical was measured by thiobarbituric acid spectrophotometry. The chelating activities of Bre for Fe 2+ were tested by differential spectrum. Superoxide anion (O 2)from xanthine xanthine oxidase (Xan XO) system and hydroxyl radical (·OH) from FeSO 4 H 2O 2 system were determined with spectrophotometry. It was found that Bre could effectively inhibit the lipid peroxidation of brain mitochondria induced by free radicals driven from Xan XO and FeSO 4 H 2O 2 system. The IC 50 of Bre were 93 01 μmol·L -1 for Xan XO system and 62 18 μmol·L -1 for FeSO 4 H 2O 2 system. Bre also scavenged O 2 and ·OH produced by Xan XO and FeSO 4 H 2O 2 systems. The IC 50 of Bre were 32 63 μmol·L -1 for O - 2 and 20 22 μmol·L -1 for ·OH. Furthermore, the chelating Fe 2+ activity of Bre was shown. It may be concluded that Bre inhibited lipid peroxidation at different stages of the reaction of oxygen free redial with the mitochondria membrane: (1) the formation of ·OH; (2) the initiation of the lipid peroxidation, by chelating Fe 2+ and scavenging O 2 as well as ·OH. The scavenging oxygen free radicals and chelating iron are the mechanisms of inhibitory effect of Bre on lipid peroxidation.
基金Supported by Funds of Natural Science of Shaanxi Education, No.05JK176Natural Science of Shaanxi Province, No.2010JM4023Natural Science of Xianyang City, No. 2010K14-02(6)
文摘AIM:To study the effect of breviscapine (Bre) on activity of protein kinase Cα (PKCα) and nuclear factor (NF)-κB in pancreas,and the mechanism of Bre attenuating acute pancreatitis (AP). METHODS:One hundred and eight rats were randomly divided into acute necrotizing pancreatitis (ANP) group,Bre group (ANP + Bre group) and sham operation (SO) group,36 rats in each group. ANP model was induced by a retrograde injection of 4% sodium deoxycholate into the bilio-pancreatic duct. Fifteen minutes after the ANP model was induced,the rats in Bre group were intraperitoneally injected with Bre (0.4 mg/100 g body weight or 0.1 mL/100 g body weight). Survival time and mortality of rats were calculated. Serum amylase and malondialdehyde levels were measured,volume of ascites was recorded and morphology of pancreas and lung was evaluated at 1,5 and 10 h,after the ANP model was induced,respectively. Expressions of PKCα and subunit p65 of NF-κB in pancreas were detected by immunohistochemistry and Western blotting. RESULTS:The life span of rats was longer and the mortality was lower in Bre group than in ANP group 13.51 ± 5.46 vs 25.36 ± 8.11 (P < 0.05). The amylase and MDA levels as well as the volume of ascites were lower and the pathological changes in pancreas and lung were less in Bre group than ANP group (P < 0.05),indicating that the pancreatitis is less severe in Bre group than ANP group. The activation of PKCα and NF-κB p65 in pancreas was induced rapidly and reached their peak at 1 h or 5 h after ANP,but their activity in Bre group was significantly inhibited. CONCLUSION:Bre exerts its therapeutic effect on AP by inhibiting the activation of PKCα and NF-κB p65 in pancreas.
文摘Lutein and lutein esters in marigold flowers was quantitatively determined by high performance chromatography (HPLC) with ODS-C 18 column.A mixture of CH3CNCD*2CH3OHCD*2CH3COOCH2CH3 with volume ratio of 55∶1∶44 was used as mobile phase at a flow rate of 1.0 mL/min and detection was carried out at 460nm. The column temperature was about 20℃. The contents of lutein and lutein esters were determined by analytical curve of lutein since lutein and lutein esters have the same spectral characteristics. Determination results of hexane extracts and saponified samples of lutein show that the saponification transforms the esters into free lutein. The increase of the content of dipalmitate and palmitate stearate reveals that the reaction includes transesterifications.