Albiflorin （AF） is the main active component extracted from Paeoniae Radix Alba. This study investigated the efficacy of AF in attenuating inflammatory injury by regulating the TLR4 signaling pathway and its negativ...Albiflorin （AF） is the main active component extracted from Paeoniae Radix Alba. This study investigated the efficacy of AF in attenuating inflammatory injury by regulating the TLR4 signaling pathway and its negative regulating factor Tollip in an experimental ulcerative colitis （UC） model. We administrated trinitrobenzene sulfonic acid for 21 d to induce UC in rats. The efficacy of AF in attenuating UC was assessed using various biochemical markers, such as tumor necrosis factor-α （TNF-α）, interleukin- 1 （IL- 1）, interleukin- 10 （IL- 10）, 5-hydroxytryptamine （5-HT）, and tissue myeloperoxidase （MPO）, along with histopathological studies on toll-like receptor-4 （TLR-4） signaling pathway and its negative regulating factor Tollip. The results showed that AF can significantly downregulate the levels of TNF-α, IL-1, IL-10, and 5-HT. AF decreased the activation of TLR4, MyD88, and NF-κB p65 protein expression by increasing Tollip expression. AF can relieve symptoms of UC by suppressing the activation of the TLR4 signaling pathway and upregulating its negative regulating factor Tollip. Therefore, AF may be a potential natural product for treating UC.展开更多
A simple, sensitive and specific high performance liquid chromatography-tandem mass spectrometry （HPLC-MS/MS）method combined with solid phase extraction has been developed and validated for the simultaneous quantifi...A simple, sensitive and specific high performance liquid chromatography-tandem mass spectrometry （HPLC-MS/MS）method combined with solid phase extraction has been developed and validated for the simultaneous quantification of paeoniflorinand albiflorin in rats plasma and tissue homogenate after administration of total glycosides of paeony （TGP）. Chromatographicseparation was achieved on a C15 column （150 mmx4.6 mm, 5 pro） with mobile phase consisted of acetonitrile-0.05% formicacid aqueous （20： 80, v/v） at a flow rate of 0.5 mL/min. The analytes were detected with triple-quadrupole mass spectrometer usingturbo ion spray with negative ionization in the multiple reaction-monitoring （MRM） modes. The results of method validationconformed to the requirements for the determination of biological samples. This method was successfully applied to thepharmacokinetics and tissue distribution study of TGP in rats. The results showed that paeonifiorin and albiflorin wereabsorbed and reached peak value quickly, and had the similar pharmacokinetic characteristics. Both of them underwent a rapid andwide distribution in the tissues throughout the whole body, among which stomach was the main distribution tissue. Moreover, theyhad the ability to cross the blood-brain barrier.展开更多
Paeonia lactiflora root(baishao in Chinese) is a commonly used herb in traditional Chinese medicines(TCM). Two isomers, paeoniflorin(PF) and albiflorin(AF), are isolated from P. lactiflora. The present study aimed to ...Paeonia lactiflora root(baishao in Chinese) is a commonly used herb in traditional Chinese medicines(TCM). Two isomers, paeoniflorin(PF) and albiflorin(AF), are isolated from P. lactiflora. The present study aimed to investigate the protective effects of PF and AF on myelosuppression induced by chemotherapy in mice and to explore the underlying mechanisms. The mouse myelosuppression model was established by intraperitoneal(i.p.) injection of cyclophosphamide(CP, 200 mg×kg^(–1)). The blood cell counts were performed. The thymus index and spleen index were also determined and bone morrow histological examination was performed. The levels of tumor necrosis factor-α(TNF-α) in serum and colony-stimulating factor(G-CSF) in plasma were measured by Enzyme-Linked Immunosorbent Assays(ELISA) and the serum levels of interleukin-3(IL-3), granulocyte-macrophagecolony- stimulatingfactor(GM-CSF), and interleukin-6(IL-6) were measured by radioimmunoassay(RIA). The levels of m RNA expression protein of IL-3, GM-CSF and G-CSF in spleen and bone marrow cells were determined respectively. PF and AF significantly increased the white blood cell(WBC) counts and reversed the atrophy of thymus. They also increased the serum levels of GM-CSF and IL-3 and the plasma level of G-CSF and reduced the level of TNF-α in serum.. PF enhanced the m RNA level of IL-3 and AF enhanced the m RNA levels of GM-CSF and G-CSF in the spleen. PF and AF both increased the protein levels of GM-CSF and G-CSF in bone marrow cells. In conclusion, our results demonstrated that PF and AF promoted the recovery of bone marrow hemopoietic function in the mouse myelosuppression model.展开更多
Objective:To study the mechanism of insulin resistance in the cholesterol gallstone formation from insulin signal transduction pathway so as to reveal the possible mechanism and the effective role of Albiflorin Granul...Objective:To study the mechanism of insulin resistance in the cholesterol gallstone formation from insulin signal transduction pathway so as to reveal the possible mechanism and the effective role of Albiflorin Granule on preventing the cholesterol gallstones.Methods:Serum triglycerides(TG),free fatty acid(FFA),and total cholesterol(TC) from different groups were measured and liver cells Ins R,PKB,IKK-β protein expression levels were detected by western blotting.Results:Albiflorin significantly decreased the cholesterol gallstone formation rate,increased glucose infusion rate in gallstone guinea pigs and improved insulin resistance.Compared with the normal group,insulin receptor and PKB protein expression in GS group were significantly reduced.IKK-β protein in the GS group increased significantly and Albiflorin could reduce IKK-β protein expression in guinea pig liver cells.Conclusions:The model of insulin resistance in cholesterol gallstone guinea pig was successfully established,which plays an important role in the cholesterol gallstone formation.All aspects of insulin signaling pathway are involved in gallstone formation.Albiflorin can regulate various aspects of insulin signal transduction pathway to prevent the formation of gallbladder.展开更多
The depressant-like effects of albiflorin(AF) were studied on stressed chronic restraint stress(CRS) rats. Experimental rats were subjected to immobilization stress for a daily 6 h-restraining in a plastic restrainer ...The depressant-like effects of albiflorin(AF) were studied on stressed chronic restraint stress(CRS) rats. Experimental rats were subjected to immobilization stress for a daily 6 h-restraining in a plastic restrainer for continuous 21 d and were treated with 30 or 15 mg·kg-1 of AF for 21 d. Control rats were maintained in completely non stressed conditions. Behavioral tests and biochemical analysis were applied to investigating a regulatory mechanism of anti-stress of AF. Treatment with AF significantly restored the depressant-like behaviors. Besides, AF increased the levels of 5-hydroxytryptophan(5-HT), 5-hydroxyindoleacetic acid(5-HIAA),noradrenaline(NE) and dopamine(DA) in the hippocampus and increased the level of brain-derived neurotrophic factor(BDNF) in serum and protein expression in hippocampus. In addition, AF decreased the levels of hypothalamo-pituitary-adrenal(HPA) cascade,reduced the level of NO and c GMP in serum and inhibited the overexpression of 5-HT2AR m RNA and protein expression. Taken together, AF can modulate the NO-mediated network pathway in the hippocampus against stress-induced depressive-like behaviors.These physiological and behavioral changes allow rats to avoid potential deleterious effects of stress that may result from chronically elevated levels of glucocorticosteroids over days.展开更多
In order to facilitate the preparation of paeoniflorin(PF)and albiflorin(AF),two chief bioactive constituents in Paeonia lactiflora Pall(PL),induction and culture of callus from PL were studied.With a modified woody p...In order to facilitate the preparation of paeoniflorin(PF)and albiflorin(AF),two chief bioactive constituents in Paeonia lactiflora Pall(PL),induction and culture of callus from PL were studied.With a modified woody plant medium supplemented with 0.5 mg·L-16-benzylaminopurine,1.0 mg·L-1naphthylacetic acid,0.1 mg·L-1thidiazuron and 30 g·L-1sucrose,callus was induced from four kinds of explants:leaf,stems,petiole,and root.The potency to form callus varies between different explants and leaf explants exhibits the highest capacity(100%).On the other hand,root-derived callus(R-callus)produces the highest level of total amount of PF and AF,31.8 mg·g-1dry mass,which is higher than the corresponding level in the root of field cultivated PL.Furthermore,the time needed is only 40 days,remarkably shorter than the cultivation time of PL,about 4–5 years.Higher accumulation levels of PF and AF with shorter production time indicate that callus culture of PL is a promising powerful tool for production of PF and AF in the future.展开更多
Adsorption equilibria of paeoniflorin and albiflorin on a cyano-silica column(CN column) from the solution of supercritical carbon dioxide(scCO2) modified with ethanol were studied. The adsorption capacity at 308.15 K...Adsorption equilibria of paeoniflorin and albiflorin on a cyano-silica column(CN column) from the solution of supercritical carbon dioxide(scCO2) modified with ethanol were studied. The adsorption capacity at 308.15 K,313.15 K, 318.15 K and 323.15 K under pressures corresponding to carbon dioxide/ethanol densities from0.347 g·cm^-3 to 0.662 g·cm^-3 were determined using the elution by characteristic point method(ECP). The effects of temperature and pressure on the solute loading were investigated. The results showed that the lower the temperature, the higher the adsorption capacity. With the decrease of density of scCO2, the adsorption capacity strengthens. The maximum adsorption capacity of paeoniflorin(albiflorin) on the CN column was15.24 mg·ml^-1(31.14 mg·ml^-1) in the range of 0–1.84 mg·ml^-1(0–1.67 mg·ml^-1) of paeoniflorin(albiflorin)standard solution. The adsorption capacity of albiflorin was twice as much as that of paeoniflorin under the same conditions. Adsorption data of paeoniflorin and albiflorin could be well described by the Langmuir model and Freundlich model. Compared with the two model fitting results, the adsorption of paeoniflorin and albiflorin belonged to the monolayer adsorption under conditions of 308.15–323.15 K and 10–17 MPa.展开更多
Aim Paeoniflorin （PF） and albiflorin （AF） are the main components of total peony glucosides （TPG）, which has been widely used as the valuable monoterpene glycosides in Paeouia lactiflora Pall and have many biolo...Aim Paeoniflorin （PF） and albiflorin （AF） are the main components of total peony glucosides （TPG）, which has been widely used as the valuable monoterpene glycosides in Paeouia lactiflora Pall and have many biological activities such as anti-inflammatory, anti-hypertension and antioxidation effects. In this study, the pharmacokinetic interaction and possible interaction mechanism among Pie and A1e and TGP were conducted and in- vestigated. A sensitive and specific ultra high-performance liquid chromatography - tandem mass spectrometry method （UPLC-MS） was successfully developed and validated for simultaneous quantification of Pie and AF in rat plasma after intragastric administration and the comparative study of pharmacokinetics for PF and A1e in different combinations. The combinations of Pie （ 80 mg· kg^- 1 ）, Ale （ 14 mg ·kg^- 1 ）, co-administration of Pie （ 80 mg · kg^-1） and Ale （14 mg· kg^-1）, TPG （Pie 80 rag. kg^-1） and TPG （Alel4 mg.·1kg^-1） were orally administrated to rats respectively. Chromatographic separation was performed on a ZORBAX Eclipse plus Cls column using 0.2% formic acid-methanol （79：21, V/V） as mobile phase. The calibration curves were linear in ranges of 0.5 - 1000 μg · L^-1. The results indicated that the main pharmacokinetic parameters including AUC, MRT and tl/2 between the single ingredient （ Pie and Ale） and TPG had significant difference （ P 〈 0.05 or P 〈 0.01 ）. The different phar- macokinetics data implied that the multiple active components of TPG resulting some potential drug-drug interac- tions, which may promote the absorption and decease the elimination of Pie and Ale. Our results could be helpful for further investigation of the interaction mechanism of Pie and Ale.展开更多
Objective： To observe the effect of paeoniflorin （PF）, albiflorin （AF） on the hemogram, visceral index and hematopoiesis cytokine in the rats of syndrome of stagnation of liver qi and blood deficiency, and to ...Objective： To observe the effect of paeoniflorin （PF）, albiflorin （AF） on the hemogram, visceral index and hematopoiesis cytokine in the rats of syndrome of stagnation of liver qi and blood deficiency, and to discuss the material base and mechanism of effect of nourishing blood and smoothing the liver of Baishao （Radix Paeoniae Alba）. Methods： Male SD rats were randomly divided into groups according to the sucrose preference test and body weight （n = 12）. Except the normal control, the other groups were treated with the chronic stress stimulation combined with radiation respectively to establish the model of syndrome of stagnation of liver qi and blood deficiency. The body weight, visceral index and the quantity of Leucocyte, Red Blood Cells, Hemoglobin in peripheral hemogram were monitored, then plasma and serum were separated. Radioimmunoassay was used to analyze the levels of Lnterleukin-3, Granulocyte-macrophage Colony-stimulating Factor, Lnterleukin-6 and Tumor Necrosis Factor-α in plasma. Results： Compared with that of model group, 30 mg·kg^-1 PF and 30 mg·kg^-1 AF of the weight, spleen index, quantity of Leucocyte were increased significantly （P 〈 0.05, P 〈 0.01）. The results of Radioimmunoassay showed that the levels of Interleukin-3 increased （P 〈 0.05, P 〈 0.05） and the levels of Tumor Necrosis Factor-α decreased in both 30 mg·kg^-1 PF and 30 mg·kg^-1 AF groups （P 〈 0.05, P 〈 0.05）. Conclusion： The effect of PF and AF on the regulation of bone marrow hematopoietic system and immune system play a role in the blood of rats with syndrome of stagnation of liver qi and blood deficiency, which suggests that both of them are the main active ingredients of nourishing blood and smoothing the liver of Baishao.展开更多
OBJECTIVE Paeoniflorin(PF) and albiflorin(AF) are the major active components of total peony glucosides(TPG) from Paeonia lactiflora Pal,which have many biological activities such as anti-inflammatory,antioxidation an...OBJECTIVE Paeoniflorin(PF) and albiflorin(AF) are the major active components of total peony glucosides(TPG) from Paeonia lactiflora Pal,which have many biological activities such as anti-inflammatory,antioxidation and anti-hypertension effects.The drug-drug pharmacokinetic interaction among PF,AF and TPG,the pharmacokinetic comparisons of AF between hypoxia and normoxia,the transport of AF cross the blood-brain barrier cell model and the transport of AF/PF/TPG cross Caco-2 cell model were investigated.METHODS A highly sensitive and rapid UPLC-MS method with multiplereaction monitoring(MRM) scanning via electrospray ionization(ESI) source operating both in the positive and negative ionization mode was successfully developed and validated for simultaneous quantitation of PF and AF in rat plasma after an oral administration of PF,AF and TPG.RESULTS The validated and developed UPLC-MS/MS method was successfully applied to simultaneously determine the AF and PF concentration in rat plasma and investigate pharmacokinetic interactions after a single intragastrical ad.ministration of PF,AF,co-administration of PF with AF and TPG,respectively.The elimination of both PF co-administered with AF and PF in TPG were slower than those for PF alone and the distribution in the tissues was wider.The combination of PF with AF or TPG could significantly increase the values of the AUC,MRT and t1/2 of the drug PF,and reduce the values of CL of PF.From a comparison of the main pharmacokinetic parameters among AF alone,AF combined with PF and AF in TPG,the values of the MRT and t1/2 of AF in TPG were greater than that of AF alone,and there were statistically signifi.cant differences in these parameters(P<0.05,P<0.01).It was also noticed that AUC and Cmax of PF in hypoxia rats were significantly decreased compared with that of normaxia rats,suggesting that there was a decreased exposure of PF in rats under hypoxia.The multiple active components in TPG may lead to DDIs between some P-gp substrates.CONCLUSION The clinical performance of total peony glucosides would be better than that of single constitute.The outcomes of the study are expected to serve as a basis for development of clinical guidelines on total peony glucosides usage.展开更多
基金National Natural Science Foundation of China(Grant No.81573602)the Project of Science and Technology for Chinese Medicine of Zhejiang Province,China(Grant No.2013KYB183)+1 种基金the Chinese Medicine Research Program of Zhejiang Province,China(Grant No.2014ZQ008,2016ZA183,2015ZQ011)Zhejiang Province Association of Traditional Chinese Medcine(Grant No.2013103)
文摘Albiflorin （AF） is the main active component extracted from Paeoniae Radix Alba. This study investigated the efficacy of AF in attenuating inflammatory injury by regulating the TLR4 signaling pathway and its negative regulating factor Tollip in an experimental ulcerative colitis （UC） model. We administrated trinitrobenzene sulfonic acid for 21 d to induce UC in rats. The efficacy of AF in attenuating UC was assessed using various biochemical markers, such as tumor necrosis factor-α （TNF-α）, interleukin- 1 （IL- 1）, interleukin- 10 （IL- 10）, 5-hydroxytryptamine （5-HT）, and tissue myeloperoxidase （MPO）, along with histopathological studies on toll-like receptor-4 （TLR-4） signaling pathway and its negative regulating factor Tollip. The results showed that AF can significantly downregulate the levels of TNF-α, IL-1, IL-10, and 5-HT. AF decreased the activation of TLR4, MyD88, and NF-κB p65 protein expression by increasing Tollip expression. AF can relieve symptoms of UC by suppressing the activation of the TLR4 signaling pathway and upregulating its negative regulating factor Tollip. Therefore, AF may be a potential natural product for treating UC.
基金Natural Science Foundation of Hebei Province of China(Grant No.C2011206158,08B031)Hundreds of Innovative Talents Project of Hebei Education Department of China
文摘A simple, sensitive and specific high performance liquid chromatography-tandem mass spectrometry （HPLC-MS/MS）method combined with solid phase extraction has been developed and validated for the simultaneous quantification of paeoniflorinand albiflorin in rats plasma and tissue homogenate after administration of total glycosides of paeony （TGP）. Chromatographicseparation was achieved on a C15 column （150 mmx4.6 mm, 5 pro） with mobile phase consisted of acetonitrile-0.05% formicacid aqueous （20： 80, v/v） at a flow rate of 0.5 mL/min. The analytes were detected with triple-quadrupole mass spectrometer usingturbo ion spray with negative ionization in the multiple reaction-monitoring （MRM） modes. The results of method validationconformed to the requirements for the determination of biological samples. This method was successfully applied to thepharmacokinetics and tissue distribution study of TGP in rats. The results showed that paeonifiorin and albiflorin wereabsorbed and reached peak value quickly, and had the similar pharmacokinetic characteristics. Both of them underwent a rapid andwide distribution in the tissues throughout the whole body, among which stomach was the main distribution tissue. Moreover, theyhad the ability to cross the blood-brain barrier.
基金supported by the National Nature Science Foundation of China(Nos.81473370,81173569)
文摘Paeonia lactiflora root(baishao in Chinese) is a commonly used herb in traditional Chinese medicines(TCM). Two isomers, paeoniflorin(PF) and albiflorin(AF), are isolated from P. lactiflora. The present study aimed to investigate the protective effects of PF and AF on myelosuppression induced by chemotherapy in mice and to explore the underlying mechanisms. The mouse myelosuppression model was established by intraperitoneal(i.p.) injection of cyclophosphamide(CP, 200 mg×kg^(–1)). The blood cell counts were performed. The thymus index and spleen index were also determined and bone morrow histological examination was performed. The levels of tumor necrosis factor-α(TNF-α) in serum and colony-stimulating factor(G-CSF) in plasma were measured by Enzyme-Linked Immunosorbent Assays(ELISA) and the serum levels of interleukin-3(IL-3), granulocyte-macrophagecolony- stimulatingfactor(GM-CSF), and interleukin-6(IL-6) were measured by radioimmunoassay(RIA). The levels of m RNA expression protein of IL-3, GM-CSF and G-CSF in spleen and bone marrow cells were determined respectively. PF and AF significantly increased the white blood cell(WBC) counts and reversed the atrophy of thymus. They also increased the serum levels of GM-CSF and IL-3 and the plasma level of G-CSF and reduced the level of TNF-α in serum.. PF enhanced the m RNA level of IL-3 and AF enhanced the m RNA levels of GM-CSF and G-CSF in the spleen. PF and AF both increased the protein levels of GM-CSF and G-CSF in bone marrow cells. In conclusion, our results demonstrated that PF and AF promoted the recovery of bone marrow hemopoietic function in the mouse myelosuppression model.
基金supported by the National Science Foundation of China(30672698)
文摘Objective:To study the mechanism of insulin resistance in the cholesterol gallstone formation from insulin signal transduction pathway so as to reveal the possible mechanism and the effective role of Albiflorin Granule on preventing the cholesterol gallstones.Methods:Serum triglycerides(TG),free fatty acid(FFA),and total cholesterol(TC) from different groups were measured and liver cells Ins R,PKB,IKK-β protein expression levels were detected by western blotting.Results:Albiflorin significantly decreased the cholesterol gallstone formation rate,increased glucose infusion rate in gallstone guinea pigs and improved insulin resistance.Compared with the normal group,insulin receptor and PKB protein expression in GS group were significantly reduced.IKK-β protein in the GS group increased significantly and Albiflorin could reduce IKK-β protein expression in guinea pig liver cells.Conclusions:The model of insulin resistance in cholesterol gallstone guinea pig was successfully established,which plays an important role in the cholesterol gallstone formation.All aspects of insulin signaling pathway are involved in gallstone formation.Albiflorin can regulate various aspects of insulin signal transduction pathway to prevent the formation of gallbladder.
基金supported by the National Nature Science Foundation of China (Nos. 81473370 and 81173569)。
文摘The depressant-like effects of albiflorin(AF) were studied on stressed chronic restraint stress(CRS) rats. Experimental rats were subjected to immobilization stress for a daily 6 h-restraining in a plastic restrainer for continuous 21 d and were treated with 30 or 15 mg·kg-1 of AF for 21 d. Control rats were maintained in completely non stressed conditions. Behavioral tests and biochemical analysis were applied to investigating a regulatory mechanism of anti-stress of AF. Treatment with AF significantly restored the depressant-like behaviors. Besides, AF increased the levels of 5-hydroxytryptophan(5-HT), 5-hydroxyindoleacetic acid(5-HIAA),noradrenaline(NE) and dopamine(DA) in the hippocampus and increased the level of brain-derived neurotrophic factor(BDNF) in serum and protein expression in hippocampus. In addition, AF decreased the levels of hypothalamo-pituitary-adrenal(HPA) cascade,reduced the level of NO and c GMP in serum and inhibited the overexpression of 5-HT2AR m RNA and protein expression. Taken together, AF can modulate the NO-mediated network pathway in the hippocampus against stress-induced depressive-like behaviors.These physiological and behavioral changes allow rats to avoid potential deleterious effects of stress that may result from chronically elevated levels of glucocorticosteroids over days.
基金Supported by the National Natural Science Foundation of China(21176220,31240054)Key Technology Research and Development Project of Ningbo(2011C11023)Zhejiang Provincial Natural Science Foundation of China(Z13B060008)
文摘In order to facilitate the preparation of paeoniflorin(PF)and albiflorin(AF),two chief bioactive constituents in Paeonia lactiflora Pall(PL),induction and culture of callus from PL were studied.With a modified woody plant medium supplemented with 0.5 mg·L-16-benzylaminopurine,1.0 mg·L-1naphthylacetic acid,0.1 mg·L-1thidiazuron and 30 g·L-1sucrose,callus was induced from four kinds of explants:leaf,stems,petiole,and root.The potency to form callus varies between different explants and leaf explants exhibits the highest capacity(100%).On the other hand,root-derived callus(R-callus)produces the highest level of total amount of PF and AF,31.8 mg·g-1dry mass,which is higher than the corresponding level in the root of field cultivated PL.Furthermore,the time needed is only 40 days,remarkably shorter than the cultivation time of PL,about 4–5 years.Higher accumulation levels of PF and AF with shorter production time indicate that callus culture of PL is a promising powerful tool for production of PF and AF in the future.
文摘Adsorption equilibria of paeoniflorin and albiflorin on a cyano-silica column(CN column) from the solution of supercritical carbon dioxide(scCO2) modified with ethanol were studied. The adsorption capacity at 308.15 K,313.15 K, 318.15 K and 323.15 K under pressures corresponding to carbon dioxide/ethanol densities from0.347 g·cm^-3 to 0.662 g·cm^-3 were determined using the elution by characteristic point method(ECP). The effects of temperature and pressure on the solute loading were investigated. The results showed that the lower the temperature, the higher the adsorption capacity. With the decrease of density of scCO2, the adsorption capacity strengthens. The maximum adsorption capacity of paeoniflorin(albiflorin) on the CN column was15.24 mg·ml^-1(31.14 mg·ml^-1) in the range of 0–1.84 mg·ml^-1(0–1.67 mg·ml^-1) of paeoniflorin(albiflorin)standard solution. The adsorption capacity of albiflorin was twice as much as that of paeoniflorin under the same conditions. Adsorption data of paeoniflorin and albiflorin could be well described by the Langmuir model and Freundlich model. Compared with the two model fitting results, the adsorption of paeoniflorin and albiflorin belonged to the monolayer adsorption under conditions of 308.15–323.15 K and 10–17 MPa.
文摘Aim Paeoniflorin （PF） and albiflorin （AF） are the main components of total peony glucosides （TPG）, which has been widely used as the valuable monoterpene glycosides in Paeouia lactiflora Pall and have many biological activities such as anti-inflammatory, anti-hypertension and antioxidation effects. In this study, the pharmacokinetic interaction and possible interaction mechanism among Pie and A1e and TGP were conducted and in- vestigated. A sensitive and specific ultra high-performance liquid chromatography - tandem mass spectrometry method （UPLC-MS） was successfully developed and validated for simultaneous quantification of Pie and AF in rat plasma after intragastric administration and the comparative study of pharmacokinetics for PF and A1e in different combinations. The combinations of Pie （ 80 mg· kg^- 1 ）, Ale （ 14 mg ·kg^- 1 ）, co-administration of Pie （ 80 mg · kg^-1） and Ale （14 mg· kg^-1）, TPG （Pie 80 rag. kg^-1） and TPG （Alel4 mg.·1kg^-1） were orally administrated to rats respectively. Chromatographic separation was performed on a ZORBAX Eclipse plus Cls column using 0.2% formic acid-methanol （79：21, V/V） as mobile phase. The calibration curves were linear in ranges of 0.5 - 1000 μg · L^-1. The results indicated that the main pharmacokinetic parameters including AUC, MRT and tl/2 between the single ingredient （ Pie and Ale） and TPG had significant difference （ P 〈 0.05 or P 〈 0.01 ）. The different phar- macokinetics data implied that the multiple active components of TPG resulting some potential drug-drug interac- tions, which may promote the absorption and decease the elimination of Pie and Ale. Our results could be helpful for further investigation of the interaction mechanism of Pie and Ale.
基金General Program of National Natural Science Foundation of China （No.81473370）, Guangxi Traditional Chinese medicine Zhuang Yao medicine research and development talent team construction, （No. Gui Jiao AD16380013）, Nanning Science and Technology Plan Project （Project Number： 20133158）
文摘Objective： To observe the effect of paeoniflorin （PF）, albiflorin （AF） on the hemogram, visceral index and hematopoiesis cytokine in the rats of syndrome of stagnation of liver qi and blood deficiency, and to discuss the material base and mechanism of effect of nourishing blood and smoothing the liver of Baishao （Radix Paeoniae Alba）. Methods： Male SD rats were randomly divided into groups according to the sucrose preference test and body weight （n = 12）. Except the normal control, the other groups were treated with the chronic stress stimulation combined with radiation respectively to establish the model of syndrome of stagnation of liver qi and blood deficiency. The body weight, visceral index and the quantity of Leucocyte, Red Blood Cells, Hemoglobin in peripheral hemogram were monitored, then plasma and serum were separated. Radioimmunoassay was used to analyze the levels of Lnterleukin-3, Granulocyte-macrophage Colony-stimulating Factor, Lnterleukin-6 and Tumor Necrosis Factor-α in plasma. Results： Compared with that of model group, 30 mg·kg^-1 PF and 30 mg·kg^-1 AF of the weight, spleen index, quantity of Leucocyte were increased significantly （P 〈 0.05, P 〈 0.01）. The results of Radioimmunoassay showed that the levels of Interleukin-3 increased （P 〈 0.05, P 〈 0.05） and the levels of Tumor Necrosis Factor-α decreased in both 30 mg·kg^-1 PF and 30 mg·kg^-1 AF groups （P 〈 0.05, P 〈 0.05）. Conclusion： The effect of PF and AF on the regulation of bone marrow hematopoietic system and immune system play a role in the blood of rats with syndrome of stagnation of liver qi and blood deficiency, which suggests that both of them are the main active ingredients of nourishing blood and smoothing the liver of Baishao.
文摘OBJECTIVE Paeoniflorin(PF) and albiflorin(AF) are the major active components of total peony glucosides(TPG) from Paeonia lactiflora Pal,which have many biological activities such as anti-inflammatory,antioxidation and anti-hypertension effects.The drug-drug pharmacokinetic interaction among PF,AF and TPG,the pharmacokinetic comparisons of AF between hypoxia and normoxia,the transport of AF cross the blood-brain barrier cell model and the transport of AF/PF/TPG cross Caco-2 cell model were investigated.METHODS A highly sensitive and rapid UPLC-MS method with multiplereaction monitoring(MRM) scanning via electrospray ionization(ESI) source operating both in the positive and negative ionization mode was successfully developed and validated for simultaneous quantitation of PF and AF in rat plasma after an oral administration of PF,AF and TPG.RESULTS The validated and developed UPLC-MS/MS method was successfully applied to simultaneously determine the AF and PF concentration in rat plasma and investigate pharmacokinetic interactions after a single intragastrical ad.ministration of PF,AF,co-administration of PF with AF and TPG,respectively.The elimination of both PF co-administered with AF and PF in TPG were slower than those for PF alone and the distribution in the tissues was wider.The combination of PF with AF or TPG could significantly increase the values of the AUC,MRT and t1/2 of the drug PF,and reduce the values of CL of PF.From a comparison of the main pharmacokinetic parameters among AF alone,AF combined with PF and AF in TPG,the values of the MRT and t1/2 of AF in TPG were greater than that of AF alone,and there were statistically signifi.cant differences in these parameters(P<0.05,P<0.01).It was also noticed that AUC and Cmax of PF in hypoxia rats were significantly decreased compared with that of normaxia rats,suggesting that there was a decreased exposure of PF in rats under hypoxia.The multiple active components in TPG may lead to DDIs between some P-gp substrates.CONCLUSION The clinical performance of total peony glucosides would be better than that of single constitute.The outcomes of the study are expected to serve as a basis for development of clinical guidelines on total peony glucosides usage.
文摘目的:探讨白芍内酯苷缓解糖尿病大鼠肾脏损伤的作用机制。方法:将10只雄性db/m小鼠(野生型对照)设为正常对照组,40只雄性C57BL/KsJ db/db小鼠(糖尿病模型)分为模型对照组,二甲双胍组,白芍内酯苷低、高剂量组,每组10只。除正常对照组和模型对照组每日灌胃生理盐水外,其余各组分别给予相应药物,持续干预12周。实验结束后,测定各组小鼠血糖、血清胰岛素、尿酸、肌酐、甘油三酯和总胆固醇水平,以及血清与肾脏组织中炎性细胞因子水平。采用蛋白印迹法检测肾组织中鞘氨醇激酶1(sphingo-sine kinase 1,SphK1)/1-磷酸鞘氨醇(sphingosine-11-phosphate,S1P)/核因子κB(nuclear factor kappa-light-chain-enhancer of activated B cells,NF-κB)信号通路的蛋白表达水平。结果:与正常对照组相比,模型对照组小鼠血糖、血脂、血清胰岛素及肾脏炎性因子水平均显著升高,肾组织中SphK1/S1P/NF-κB通路蛋白表达激活(P<0.01)。与模型对照组相比,二甲双胍组和白芍内酯苷低、高剂量组均能显著改善上述指标,其中白芍内酯苷高剂量组效果最优(P<0.01)。结论:白芍内酯苷对糖尿病大鼠肾脏损伤具有保护作用,其机制可能与调控SphK1/S1P/NF-κB信号通路有关。
