[Objectives]To explore the effect and possible mechanism of bergenin in relieving allergic rhinitis(AR)in mice.[Methods]50 C57/BL6 mice were randomly divided into blank group(n=10),model group(n=10)and high(100 mg/kg)...[Objectives]To explore the effect and possible mechanism of bergenin in relieving allergic rhinitis(AR)in mice.[Methods]50 C57/BL6 mice were randomly divided into blank group(n=10),model group(n=10)and high(100 mg/kg),medium(50 mg/kg)and low(25 mg/kg)dose bergenin groups with 10 mice in each group.Except for the blank group,the other mice were sensitized by basic ways combined with attack to replicate the AR model.From the 15th d of modeling(from the second d after the end of the basic modeling),the drug group was given bergenin orally for 15 d,and the blank group and model group were given the same volume of normal saline once a day.24 h after the last establishment of the model,the content of interleukin 4(IL-4),IL-6,TNF-αand IL-1βin nasal lavage fluid and serum of mice in each group was detected by ELISA.The expression of TLR-4,NF-κB and p-NF-κB in nasal mucosa of mice was detected by Western blot.[Results]Compared with the blank group,the content of inflammatory factors IL-4,IL-6,TNF-αand IL-1βin nasal lavage fluid and serum of model group was significantly increased,and the protein expression of TLR-4 and p-NF-κB was significantly increased.After the intervention of bergenin,the content of IL-4,IL-6,TNF-αand IL-1βin nasal lavage fluid and serum and TLR-4 and p-NF-κB protein in tissue was significantly inhibited in bergenin group.[Conclusions]Bergenin can effectively reduce allergic inflammation in AR model mice,and its mechanism may be related to inhibition of inflammation and down-regulation of TLR-4/NF-κB signal pathway.展开更多
Bergenin, a C-glucoside of 4-O-methyl gallic acid from Bergenia purpurascens, is a naturally antitussive and expectorant agent. A rapid and sensitive liquid chromatography tandem mass spectrometry (LC-MS/MS) method ha...Bergenin, a C-glucoside of 4-O-methyl gallic acid from Bergenia purpurascens, is a naturally antitussive and expectorant agent. A rapid and sensitive liquid chromatography tandem mass spectrometry (LC-MS/MS) method has been developed and validated for the determination of the active component-bergenin, in rat plasma after oral administration of aqueous B. purpurascens extract. The plasma samples were pretreated by protein precipitation with acetonitrile and chromatographic separation was achieved on a Diamonsil s C 18 column (150 mm 4.6 mm, 5 mm) with isocratic elution using a mobile phase consisting of watermethanol (30:70, v/v) at a flow rate of 0.6 mL/min. The detection was accomplished by a triple-quadrupole tandem mass spectrometer in multiple-reaction monitoring (MRM) scanning via an electrospray ionization (ESI) source operating in the negative mode. The optimized mass transition ion-pairs (m/z) for quantitation were 327.3/192.0 for bergenin, and 431.1/311.1 for IS. The time for each analysis run was only 3.5 min between injections. The calibration curve exhibited good linearity (r2A sensitive, simple and rapid high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was developed and fully validated for the simultaneous quantification of buprenorphine (BUP) and its N-dealkylated metabolite norbuprenorphine (NBUP) in 200 mL human plasma. Human plasma samples were prepared using liquid-liquid extraction, and then separated on a Shiseido MG C18 (5 mm, 2.0 mm 50 mm) via 4.1 min gradient elution. Following electrospray ionization, the analytes were quantified on a triple-quadrupole mass spectrometer in multiple-reaction-monitoring (MRM) positive ion mode. Linearity was achieved from 25.0 to 10000 pg/mL for buprenorphine, from 20.0 to 8000 pg/mL for norbupre-norphine with r2>0.99. The method was demonstrated with acceptable accuracy, precision and specificity for the detection of buprenorphine and norbuprenorphine. Recovery was 81.8-88.8% for buprenorphine and 77.0-84.6% for norbuprenorphine, and the matrix effect was 95.6-97.4% for buprenorphine and 94.0-96.9% for norbuprenorphine; all were not concentration dependent. With validated matrix and autosampler stability data, this method was successfully applied in a bioequivalence study to support abbreviated new drug application. 0.99) over a range of 1.00-2000 ng/mL for bergenin. The lower limit of quantitation (LLOQ) was 1.00 ng/mL. The intra- and inter-day precisions were no more than 11.8%, and relative errors (RE) were within the range of 0.0-4.4%. The validated method was successfully applied to investigate the pharmacokinetics of bergenin after oral administration of B. purpurascens extract in rats.展开更多
Bergenin, isolated from the herb of Saxifrage stolonifera Curt.(Hu-Er-Cao) has hepatoprotective, anti-inflammatory, antitussive, and neuroprotective activities. The aim of the present study was to establish a simple, ...Bergenin, isolated from the herb of Saxifrage stolonifera Curt.(Hu-Er-Cao) has hepatoprotective, anti-inflammatory, antitussive, and neuroprotective activities. The aim of the present study was to establish a simple, rapid, and sensitive RP-HPLC method for determination of bergenin in rat plasma and compare its oral pharmacokinetic behaviors in normal and CCl_4-induced hepatic injury rats. With norisoboldine as an internal standard, chromatographic separation was performed on a C_(18) analytical column with acetonitrile and water(11 : 89, V/V) containing 0.1% formic acid as the mobile phase. A good linearity was obtained over the range of 100^(–1)0 000 ng·m L^(–1). The lower limit of quantification was 50 ng·m L~(^(–1)). The developed method was successfully applied to a study of the pharmacokinetic difference of bergenin(100 mg·kg^(–1)) between normal and hepatic injury rats after oral administration. Marked alterations of pharmacokinetic parameters in hepatic injury rats were observed. Compared to normal rats, the AUC_((0–∞)) of bergenin in hepatic injury rats was elevated to 2.11-fold and C_(max) was increased by 130%, whereas CL value was only 55% of the normal rats, suggesting that the systemic exposure of bergenin was significantly increased under hepatic injury status.展开更多
To synthesize a series of 3-, 4-, and/or 11-trihydroxy modified bergenin derivatives and evaluated their cytotoxic activity in vitro. The phenolic hydroxyl groups of bergenin were protected by benzyl groups with benzy...To synthesize a series of 3-, 4-, and/or 11-trihydroxy modified bergenin derivatives and evaluated their cytotoxic activity in vitro. The phenolic hydroxyl groups of bergenin were protected by benzyl groups with benzyl bromide. Treatment of dibenzyl bergenin with the corresponding acid in the presence of EDC·HCl and DMAP in CH2Cl2, followed by hydrogenation over Pd/C catalysts, afforded derivatives of bergenin esters. All of the target compounds were identified by IR, MS, and 1H NMR. Twenty-six novel and three known derivatives of bergenin esters were synthesized. Their cytotoxicity values were evaluated by the MTT assay on the inhibition of DU-145 and BGC-823 cells in vitro. Several triply-substituted(3a, 4a, 5a, 6a, 7a) and doublysubstituted(8b, 9b) bergenin derivatives exhibited higher cytotoxic activity than bergenin. The result showed that the size of substituents and the lipophilicity of the bergenin esters displayed an important role on their cytotoxic activity.展开更多
The com pound bergenin w asisolated from theaerialpartsofBergenia pur- purascens. Allprotonsand carbons ofthe com pound w ereassigned and its structure w as char- acterized as 4-m ethoxy-2-[tetrahydro-3,4,5-trihydroxy...The com pound bergenin w asisolated from theaerialpartsofBergenia pur- purascens. Allprotonsand carbons ofthe com pound w ereassigned and its structure w as char- acterized as 4-m ethoxy-2-[tetrahydro-3,4,5-trihydroxy-6-(hydroxym ethyl)pyran-2-yl]-α-re- sorcylic acid δ-lactone by using 1H-1H DQF-COSY, 1H-13CHMQCand HMBC. This w ork will be helpfulto the chem icalstructure studies ofthe sim ilar new ArylC-glycoside com pounds by m eans ofNMRspectroscopy.展开更多
文摘[Objectives]To explore the effect and possible mechanism of bergenin in relieving allergic rhinitis(AR)in mice.[Methods]50 C57/BL6 mice were randomly divided into blank group(n=10),model group(n=10)and high(100 mg/kg),medium(50 mg/kg)and low(25 mg/kg)dose bergenin groups with 10 mice in each group.Except for the blank group,the other mice were sensitized by basic ways combined with attack to replicate the AR model.From the 15th d of modeling(from the second d after the end of the basic modeling),the drug group was given bergenin orally for 15 d,and the blank group and model group were given the same volume of normal saline once a day.24 h after the last establishment of the model,the content of interleukin 4(IL-4),IL-6,TNF-αand IL-1βin nasal lavage fluid and serum of mice in each group was detected by ELISA.The expression of TLR-4,NF-κB and p-NF-κB in nasal mucosa of mice was detected by Western blot.[Results]Compared with the blank group,the content of inflammatory factors IL-4,IL-6,TNF-αand IL-1βin nasal lavage fluid and serum of model group was significantly increased,and the protein expression of TLR-4 and p-NF-κB was significantly increased.After the intervention of bergenin,the content of IL-4,IL-6,TNF-αand IL-1βin nasal lavage fluid and serum and TLR-4 and p-NF-κB protein in tissue was significantly inhibited in bergenin group.[Conclusions]Bergenin can effectively reduce allergic inflammation in AR model mice,and its mechanism may be related to inhibition of inflammation and down-regulation of TLR-4/NF-κB signal pathway.
基金supported by the Natural Science Foundation of Guangdong Province (Nos. 9151008018000003)
文摘Bergenin, a C-glucoside of 4-O-methyl gallic acid from Bergenia purpurascens, is a naturally antitussive and expectorant agent. A rapid and sensitive liquid chromatography tandem mass spectrometry (LC-MS/MS) method has been developed and validated for the determination of the active component-bergenin, in rat plasma after oral administration of aqueous B. purpurascens extract. The plasma samples were pretreated by protein precipitation with acetonitrile and chromatographic separation was achieved on a Diamonsil s C 18 column (150 mm 4.6 mm, 5 mm) with isocratic elution using a mobile phase consisting of watermethanol (30:70, v/v) at a flow rate of 0.6 mL/min. The detection was accomplished by a triple-quadrupole tandem mass spectrometer in multiple-reaction monitoring (MRM) scanning via an electrospray ionization (ESI) source operating in the negative mode. The optimized mass transition ion-pairs (m/z) for quantitation were 327.3/192.0 for bergenin, and 431.1/311.1 for IS. The time for each analysis run was only 3.5 min between injections. The calibration curve exhibited good linearity (r2A sensitive, simple and rapid high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was developed and fully validated for the simultaneous quantification of buprenorphine (BUP) and its N-dealkylated metabolite norbuprenorphine (NBUP) in 200 mL human plasma. Human plasma samples were prepared using liquid-liquid extraction, and then separated on a Shiseido MG C18 (5 mm, 2.0 mm 50 mm) via 4.1 min gradient elution. Following electrospray ionization, the analytes were quantified on a triple-quadrupole mass spectrometer in multiple-reaction-monitoring (MRM) positive ion mode. Linearity was achieved from 25.0 to 10000 pg/mL for buprenorphine, from 20.0 to 8000 pg/mL for norbupre-norphine with r2>0.99. The method was demonstrated with acceptable accuracy, precision and specificity for the detection of buprenorphine and norbuprenorphine. Recovery was 81.8-88.8% for buprenorphine and 77.0-84.6% for norbuprenorphine, and the matrix effect was 95.6-97.4% for buprenorphine and 94.0-96.9% for norbuprenorphine; all were not concentration dependent. With validated matrix and autosampler stability data, this method was successfully applied in a bioequivalence study to support abbreviated new drug application. 0.99) over a range of 1.00-2000 ng/mL for bergenin. The lower limit of quantitation (LLOQ) was 1.00 ng/mL. The intra- and inter-day precisions were no more than 11.8%, and relative errors (RE) were within the range of 0.0-4.4%. The validated method was successfully applied to investigate the pharmacokinetics of bergenin after oral administration of B. purpurascens extract in rats.
基金supported by Health Innovation Personnel Training Project of Changzhou City(No.CWKJ 2010-368)Changzhou High Level Health Personnel Training Project
文摘Bergenin, isolated from the herb of Saxifrage stolonifera Curt.(Hu-Er-Cao) has hepatoprotective, anti-inflammatory, antitussive, and neuroprotective activities. The aim of the present study was to establish a simple, rapid, and sensitive RP-HPLC method for determination of bergenin in rat plasma and compare its oral pharmacokinetic behaviors in normal and CCl_4-induced hepatic injury rats. With norisoboldine as an internal standard, chromatographic separation was performed on a C_(18) analytical column with acetonitrile and water(11 : 89, V/V) containing 0.1% formic acid as the mobile phase. A good linearity was obtained over the range of 100^(–1)0 000 ng·m L^(–1). The lower limit of quantification was 50 ng·m L~(^(–1)). The developed method was successfully applied to a study of the pharmacokinetic difference of bergenin(100 mg·kg^(–1)) between normal and hepatic injury rats after oral administration. Marked alterations of pharmacokinetic parameters in hepatic injury rats were observed. Compared to normal rats, the AUC_((0–∞)) of bergenin in hepatic injury rats was elevated to 2.11-fold and C_(max) was increased by 130%, whereas CL value was only 55% of the normal rats, suggesting that the systemic exposure of bergenin was significantly increased under hepatic injury status.
基金supported by the Natural Science Foundation of China(Nos.81274064 and 81373956)the National Fund for Fostering Talents of Basic Science(NFFTBS)(No.J1030830)the Science and Technology Supporting Project of Xinjiang(No.201291160)
文摘To synthesize a series of 3-, 4-, and/or 11-trihydroxy modified bergenin derivatives and evaluated their cytotoxic activity in vitro. The phenolic hydroxyl groups of bergenin were protected by benzyl groups with benzyl bromide. Treatment of dibenzyl bergenin with the corresponding acid in the presence of EDC·HCl and DMAP in CH2Cl2, followed by hydrogenation over Pd/C catalysts, afforded derivatives of bergenin esters. All of the target compounds were identified by IR, MS, and 1H NMR. Twenty-six novel and three known derivatives of bergenin esters were synthesized. Their cytotoxicity values were evaluated by the MTT assay on the inhibition of DU-145 and BGC-823 cells in vitro. Several triply-substituted(3a, 4a, 5a, 6a, 7a) and doublysubstituted(8b, 9b) bergenin derivatives exhibited higher cytotoxic activity than bergenin. The result showed that the size of substituents and the lipophilicity of the bergenin esters displayed an important role on their cytotoxic activity.
文摘The com pound bergenin w asisolated from theaerialpartsofBergenia pur- purascens. Allprotonsand carbons ofthe com pound w ereassigned and its structure w as char- acterized as 4-m ethoxy-2-[tetrahydro-3,4,5-trihydroxy-6-(hydroxym ethyl)pyran-2-yl]-α-re- sorcylic acid δ-lactone by using 1H-1H DQF-COSY, 1H-13CHMQCand HMBC. This w ork will be helpfulto the chem icalstructure studies ofthe sim ilar new ArylC-glycoside com pounds by m eans ofNMRspectroscopy.
