Arctigenin has a variety of pharmacological effects,such as anti-inflammatory,anti-tumor,antiviral and hypoglycemic.In this paper,the pharmacological effects and mechanisms of arctigenin were reviewed,in order to prov...Arctigenin has a variety of pharmacological effects,such as anti-inflammatory,anti-tumor,antiviral and hypoglycemic.In this paper,the pharmacological effects and mechanisms of arctigenin were reviewed,in order to provide a theoretical basis for further research and development of arctigenin.展开更多
Cutaneous melanoma is one of the most aggressive forms of skin cancer. Arctigenin, one of the major bioactive compo-nents of Arctii Fructus, has been reported to exhibit antioxidant, antitumor and anti-inflammatory ac...Cutaneous melanoma is one of the most aggressive forms of skin cancer. Arctigenin, one of the major bioactive compo-nents of Arctii Fructus, has been reported to exhibit antioxidant, antitumor and anti-inflammatory activities. In the pre-sent study, we investigated the effect of arctigenin on induction of apoptosis in highly metastatic SK-MEL-28 human melanoma cells. Arctigenin inhibited growth of SK-MEL-28 cells in a dose-dependent manner. Treatment of SK-MEL-28cells with arctigenin caused cleavage of caspases 3, 7 and 9, and poly (ADP-ribose) polymerase in a dose-dependent manner. Furthermore, acetylation of histone H3 and H4 in the SK-MEL-28 cells was dramatically increased by arctigenin treatment. Collectively, these findings indicate that arctigenin-induces apoptosis of SK-MEL-28 melanoma cells via activation of caspases and histone acetylation.展开更多
BACKGROUND:Paraquat(PQ)-induced acute lung injury(ALI)and pulmonary fi brosis are common diseases with high mortality but without eff ective antidotes in emergency medicine.Our previous study has proved that arctigeni...BACKGROUND:Paraquat(PQ)-induced acute lung injury(ALI)and pulmonary fi brosis are common diseases with high mortality but without eff ective antidotes in emergency medicine.Our previous study has proved that arctigenin suppressed pulmonary fibrosis induced by PQ.We wondered whether arctigenin could also have a protective eff ect on PQ-induced ALI.METHODS:A PQ-induced A549 cell injury model was used,and the effect of arctigenin was determined by a cell counting kit-8(CCK-8)cell viability assay.In addition,terminal deoxynucleotidyl transferase(TdT)-mediated dUTP nick-end labelling(TUNEL)staining assays and mitochondrial membrane potential assays were performed to evaluate the level of cell apoptosis.The generation of reactive oxygen species(ROS)was refl ected by dihydroethidium(DHE)staining and a 2’,7’-dichlorodihy drofluorescein diacetate(DCFH-DA)assay.Moreover,immunoblotting studies were used to assess the expression of mitogen-activated protein kinases(MAPKs)and p38 MAPK.RESULTS:Arctigenin attenuated PQ-induced inhibition of A549 cell viability in a dose-dependent manner.Arctigenin also significantly reduced PQ-induced A549 cell apoptosis,as refl ected by the TUNEL assay and mitochondrial membrane potential assay,which may result from suppressed ROS/p38 MAPK signaling because we found that arctigenin dramatically suppressed ROS generation and p38 MAPK phosphorylation.CONCLUSION:Arctigenin could attenuate PQ-induced lung epithelial A549 cell injury in vitro by suppressing ROS/p38 MAPK-mediated cell apoptosis,and arctigenin might be considered a potential candidate drug for PQ-induced ALI.展开更多
[Objectives]This study was conducted to investigate the pharmacokinetic characteristics of arctigenin from water extract of Fructus Arctii in piglets,understand its absorption,distribution,transformation and excretion...[Objectives]This study was conducted to investigate the pharmacokinetic characteristics of arctigenin from water extract of Fructus Arctii in piglets,understand its absorption,distribution,transformation and excretion in piglets,and provide theoretical reference for the development and clinical use of new veterinary drugs.[Methods]Six healthy piglets,weighing(30.0±5.0)kg,were selected and administered by gavage with a Fructus Arctii water extract at 1.0 g/kg·bw.Blood was collected from the anterior vena cava at different time points.The concentration of arctigenin in pig plasma was determined by HPLC.The main pharmacokinetic parameters were:absorption half-life(t1/2 ka)(0.098±0.006)h,distribution half-life(t1/2α)(0.208±0.009)h,elimination half-life(t1/2β)(23.816±2.151)h,apparent volume of distribution(Vd)(32.212±4.033)L/kg,apparent volume of distribution(Vd)(32.212±4.033)L/kg,clearance(CLb)(2.384±1.589)L/(h·kg),peak time(tmax)(0.251±0.011)h,peak concentration(Cmax)(0.560±0.063)μg/ml,and the area under the curve(AUC)at the time of drug administration(9.620±0.752)μg·h/ml.[Results]After oral administration of the water extract powder of Fructus Arctii,arctigenin showed a two-compartment model with absorption in piglets,with the characteristics of fast absorption,wide distribution and slow elimination.Arctigenin might have a hepatoenteral circulation in piglets,and the drug effect could last for a long time.[Conclusions]This study provides a theoretical basis and reference for the development and clinical use of new veterinary drugs.展开更多
A mathematical model based on Fick＇ s first law wasestablished to describe the process of ultrasonic-assistedextraction of arctigenin from acid hydrolyzed FructusArctii.Acid hydrolization with hydrochloric acid promo...A mathematical model based on Fick＇ s first law wasestablished to describe the process of ultrasonic-assistedextraction of arctigenin from acid hydrolyzed FructusArctii.Acid hydrolization with hydrochloric acid promotes theconversion of arctiin to arctigenin in the arctiin-rich activepharmaceutical ingredient, and the hydrolyzed products werefurther examined to investigate the process setup. Byconsidering the mechanism of the extraction process andexperimental data, the effects of parameters including solventto solid ratio, particle size of hydrolyzed samples, ethanolvolume fraction, ultrasound power, extraction temperature andextraction time on concentration of arctigenin were analyzed indetail. The model was suitable for simulating the process ofultrasonic-assisted extraction of arctigenin. The simulationresults of the model agree well with experimental data with thedeviation below 13%, indicating that the mathematical modelcan provide valuable guidance for the extraction of arctigeninfrom acid hydrolyzed FructusArctii.展开更多
The present study aimed at developing a natural compound with anti-allergic effect and stability under latex glove manufacturing conditions and investigating whether its anti-allergic effect is maintained after its ad...The present study aimed at developing a natural compound with anti-allergic effect and stability under latex glove manufacturing conditions and investigating whether its anti-allergic effect is maintained after its addition into the latex. The effects of nine natural compounds on growth of the RBL-2H3 cells and mouse primary spleen lymphocytes were determined using MTT assay. The compounds included glycyrrhizin, osthole, tetrandrine, tea polyphenol, catechin, arctigenin, oleanolic acid, baicalin and oxymatrine. An ELISA assay was used for the in vitro anti-type I/IV allergy screening; in this process β-hexosaminidase, histamine, and IL-4 released from RBL-2H3 cell lines and IFN-γ and IL-2 released from mouse primary spleen lymphocytes were taken as screening indices. The physical stability of eight natural compounds and the dissolubility of arctigenin, selected based on the in vitro pharnacodynamaic screening and the stability evaluation, were detected by HPLC. The in vivo pharmacodynamic confirmation of arctigenin and final latex product was evaluated with a passive cutaneous anaphylaxis(PCA) model and an allergen-specific skin response model. Nine natural compounds showed minor growth inhibition on RBL-2H3 cells and mouse primary spleen lymphocytes. Baicalin and arctigenin had the best anti-type I and IV allergic effects among the natural compounds based on the in vitro pharmacodynamic screening. Arctigenin and catechin had the best physical stability under different manufacturing conditions. Arctigenin was the selected for further evaluation and proven to have anti-type I and IV allergic effects in vivo in a dose-dependent manner. The final product of the arctigenin-containing latex glove had anti-type I and IV allergic effects in vivo which were mainly attributed to arctigenin as proved from the dissolubility results. Arctigenin showed anti-type I and IV allergic effects in vitro and in vivo, with a good stability under latex glove manufacturing conditions, and a persistent anti-allergic effect after being added into the latex to prevent latex allergy.展开更多
基金Supported by the Talent Training Program for the Reform and Development of Local Colleges and University of the Central Government(2020GSP16)。
文摘Arctigenin has a variety of pharmacological effects,such as anti-inflammatory,anti-tumor,antiviral and hypoglycemic.In this paper,the pharmacological effects and mechanisms of arctigenin were reviewed,in order to provide a theoretical basis for further research and development of arctigenin.
文摘Cutaneous melanoma is one of the most aggressive forms of skin cancer. Arctigenin, one of the major bioactive compo-nents of Arctii Fructus, has been reported to exhibit antioxidant, antitumor and anti-inflammatory activities. In the pre-sent study, we investigated the effect of arctigenin on induction of apoptosis in highly metastatic SK-MEL-28 human melanoma cells. Arctigenin inhibited growth of SK-MEL-28 cells in a dose-dependent manner. Treatment of SK-MEL-28cells with arctigenin caused cleavage of caspases 3, 7 and 9, and poly (ADP-ribose) polymerase in a dose-dependent manner. Furthermore, acetylation of histone H3 and H4 in the SK-MEL-28 cells was dramatically increased by arctigenin treatment. Collectively, these findings indicate that arctigenin-induces apoptosis of SK-MEL-28 melanoma cells via activation of caspases and histone acetylation.
基金This work was supported by the National Natural Science Foundation of China(82172182 and 82102311)Social Development Projects of Jiangsu Province(BE2017720)+2 种基金Natural Science Foundation of Jiangsu Province(BK20190247)Science Foundation of Jiangsu Health Commission(H2018039)Jiangsu Postdoctoral Research Foundation(2018K048A and 2020Z193).
文摘BACKGROUND:Paraquat(PQ)-induced acute lung injury(ALI)and pulmonary fi brosis are common diseases with high mortality but without eff ective antidotes in emergency medicine.Our previous study has proved that arctigenin suppressed pulmonary fibrosis induced by PQ.We wondered whether arctigenin could also have a protective eff ect on PQ-induced ALI.METHODS:A PQ-induced A549 cell injury model was used,and the effect of arctigenin was determined by a cell counting kit-8(CCK-8)cell viability assay.In addition,terminal deoxynucleotidyl transferase(TdT)-mediated dUTP nick-end labelling(TUNEL)staining assays and mitochondrial membrane potential assays were performed to evaluate the level of cell apoptosis.The generation of reactive oxygen species(ROS)was refl ected by dihydroethidium(DHE)staining and a 2’,7’-dichlorodihy drofluorescein diacetate(DCFH-DA)assay.Moreover,immunoblotting studies were used to assess the expression of mitogen-activated protein kinases(MAPKs)and p38 MAPK.RESULTS:Arctigenin attenuated PQ-induced inhibition of A549 cell viability in a dose-dependent manner.Arctigenin also significantly reduced PQ-induced A549 cell apoptosis,as refl ected by the TUNEL assay and mitochondrial membrane potential assay,which may result from suppressed ROS/p38 MAPK signaling because we found that arctigenin dramatically suppressed ROS generation and p38 MAPK phosphorylation.CONCLUSION:Arctigenin could attenuate PQ-induced lung epithelial A549 cell injury in vitro by suppressing ROS/p38 MAPK-mediated cell apoptosis,and arctigenin might be considered a potential candidate drug for PQ-induced ALI.
基金Hubei Provincial Technical Innovation Major Project(2019AEE006)Wuhan Animal and Poultry Chinese Herbal Medicine Development Engineering Technology Research Center(2014021511020460)Hubei Provincial Central Government Guiding Local Science and Technology Development Fundation of China(2020ZYYD029)。
文摘[Objectives]This study was conducted to investigate the pharmacokinetic characteristics of arctigenin from water extract of Fructus Arctii in piglets,understand its absorption,distribution,transformation and excretion in piglets,and provide theoretical reference for the development and clinical use of new veterinary drugs.[Methods]Six healthy piglets,weighing(30.0±5.0)kg,were selected and administered by gavage with a Fructus Arctii water extract at 1.0 g/kg·bw.Blood was collected from the anterior vena cava at different time points.The concentration of arctigenin in pig plasma was determined by HPLC.The main pharmacokinetic parameters were:absorption half-life(t1/2 ka)(0.098±0.006)h,distribution half-life(t1/2α)(0.208±0.009)h,elimination half-life(t1/2β)(23.816±2.151)h,apparent volume of distribution(Vd)(32.212±4.033)L/kg,apparent volume of distribution(Vd)(32.212±4.033)L/kg,clearance(CLb)(2.384±1.589)L/(h·kg),peak time(tmax)(0.251±0.011)h,peak concentration(Cmax)(0.560±0.063)μg/ml,and the area under the curve(AUC)at the time of drug administration(9.620±0.752)μg·h/ml.[Results]After oral administration of the water extract powder of Fructus Arctii,arctigenin showed a two-compartment model with absorption in piglets,with the characteristics of fast absorption,wide distribution and slow elimination.Arctigenin might have a hepatoenteral circulation in piglets,and the drug effect could last for a long time.[Conclusions]This study provides a theoretical basis and reference for the development and clinical use of new veterinary drugs.
基金The National Natural Science Foundation of China(No.21406272,21676291)the Fundamental Research Funds for the Central Universities(No.2632017ZD01)Jiangsu Planned Projects for Postdoctoral Research Funds(No.1402060B)
文摘A mathematical model based on Fick＇ s first law wasestablished to describe the process of ultrasonic-assistedextraction of arctigenin from acid hydrolyzed FructusArctii.Acid hydrolization with hydrochloric acid promotes theconversion of arctiin to arctigenin in the arctiin-rich activepharmaceutical ingredient, and the hydrolyzed products werefurther examined to investigate the process setup. Byconsidering the mechanism of the extraction process andexperimental data, the effects of parameters including solventto solid ratio, particle size of hydrolyzed samples, ethanolvolume fraction, ultrasound power, extraction temperature andextraction time on concentration of arctigenin were analyzed indetail. The model was suitable for simulating the process ofultrasonic-assisted extraction of arctigenin. The simulationresults of the model agree well with experimental data with thedeviation below 13%, indicating that the mathematical modelcan provide valuable guidance for the extraction of arctigeninfrom acid hydrolyzed FructusArctii.
基金supported by National Science and Technology Infrastructure Program of China(No.2012BAI30B001)Technological Innovation Team of Jiangsu Higher Education+3 种基金National Natural Science Foundation of China(Nos.3087315630672524)New Century Excellent Talents in University(NCET-07-0851)Mega-projects of Science Research for the 12th Five-Year Plan of China(No.2011AX09401-007)
文摘The present study aimed at developing a natural compound with anti-allergic effect and stability under latex glove manufacturing conditions and investigating whether its anti-allergic effect is maintained after its addition into the latex. The effects of nine natural compounds on growth of the RBL-2H3 cells and mouse primary spleen lymphocytes were determined using MTT assay. The compounds included glycyrrhizin, osthole, tetrandrine, tea polyphenol, catechin, arctigenin, oleanolic acid, baicalin and oxymatrine. An ELISA assay was used for the in vitro anti-type I/IV allergy screening; in this process β-hexosaminidase, histamine, and IL-4 released from RBL-2H3 cell lines and IFN-γ and IL-2 released from mouse primary spleen lymphocytes were taken as screening indices. The physical stability of eight natural compounds and the dissolubility of arctigenin, selected based on the in vitro pharnacodynamaic screening and the stability evaluation, were detected by HPLC. The in vivo pharmacodynamic confirmation of arctigenin and final latex product was evaluated with a passive cutaneous anaphylaxis(PCA) model and an allergen-specific skin response model. Nine natural compounds showed minor growth inhibition on RBL-2H3 cells and mouse primary spleen lymphocytes. Baicalin and arctigenin had the best anti-type I and IV allergic effects among the natural compounds based on the in vitro pharmacodynamic screening. Arctigenin and catechin had the best physical stability under different manufacturing conditions. Arctigenin was the selected for further evaluation and proven to have anti-type I and IV allergic effects in vivo in a dose-dependent manner. The final product of the arctigenin-containing latex glove had anti-type I and IV allergic effects in vivo which were mainly attributed to arctigenin as proved from the dissolubility results. Arctigenin showed anti-type I and IV allergic effects in vitro and in vivo, with a good stability under latex glove manufacturing conditions, and a persistent anti-allergic effect after being added into the latex to prevent latex allergy.
文摘目的 探究牛蒡子苷元(ATG)对慢性心力衰竭(CHF)大鼠心室重构和炎性反应的影响,并分析其潜在机制。方法 79只SD大鼠随机选取12只为假手术组,其余大鼠采用腹主动脉缩窄术建立CHF大鼠模型,成功造模60只大鼠随机分为CHF组、ATG低剂量组(ATG-L组,10 mg/kg)、ATG高剂量组(ATG-H组,20 mg/kg)、ATG+阴性对照(ATG+NC)组[20 mg/kg ATG+100μl高迁移率族蛋白B1(HMGB1)阴性对照质粒]、ATG+HMGB1组(20 mg/kg ATG+100μl HMGB1过表达质粒),每组12只。各组给予相应干预4周后,检测大鼠心功能、B型钠尿肽、N末端B型钠尿肽前体和炎性因子白细胞介素6、TNF-α水平、心脏质量指数和左心室质量指数、心肌组织病理变化、心肌细胞横截面积和心肌胶原体积分数、左心室心肌组织HMGB1/Toll样受体4(TLR4)/核转录因子κB(NF-κB)信号通路相关蛋白表达。结果 与假手术组比较,CHF组大鼠心肌组织HMGB1(0.42±0.05 vs 0.15±0.02)、TLR4(0.70±0.09 vs 0.21±0.04)蛋白水平和磷酸化NF-κB p65(p-NF-κB p65)/NF-κB p65(0.73±0.09 vs 0.26±0.05)蛋白比值显著升高,LVEF、左心室短轴缩短率(LVFS)显著降低(P<0.05);与CHF组比较,ATG-L组和ATG-H组大鼠心肌组织HMGB1(0.33±0.04、0.24±0.04 vs 0.42±0.05)、TLR4(0.56±0.06、0.41±0.05 vs 0.70±0.09)蛋白水平和p-NF-κB p65/NF-κB p65(0.61±0.08、0.49±0.06 vs 0.73±0.09)蛋白比值依次降低,LVEF、LVFS依次升高(P<0.05);HMGB1过表达能明显减弱ATG对HMGB1/TLR4/NF-κB信号通路和CHF大鼠心室重构、炎性反应的抑制作用(P<0.05)。结论 ATG可能通过抑制HMGB1/TLR4/NF-κB信号炎性通路,抑制了CHF大鼠的心室重构。
