Panax notoginseng saponins(PNS)are a class of effective ingredients in Notoginseng Radix et Rhizoma,a well-known herbal medicine called San-Qi in Chinese.After oral administration,PNS inevitably interacts with gut mic...Panax notoginseng saponins(PNS)are a class of effective ingredients in Notoginseng Radix et Rhizoma,a well-known herbal medicine called San-Qi in Chinese.After oral administration,PNS inevitably interacts with gut microbiota,and thus affect the pharmacokinetic profiles and pharmacological effects.To date,studies concering gut microbiota-mediated metabolism of PNS have not been reviewed systematically.Herein,we outline the metabolic profiles of Panax notoginseng saponins mediated by gut microbiota,as well as its role in the pharmacokinetics and pharmacodynamics on the basis of reported data.The metabolic pathways of primary saponins are proposed,and step-by-step deglycosylation is found to be the primary degradation pathways of PNS mediated by gut microbiota.Specific microorganisms and enzymes involved in the metabolic processes were summarized.Gut microbiota is deeply involved in the metabolism of PNS,affects the pharmacokinetic profiles,and produces a series of active metabolites.These metabolites were documented to play an essential role in the efficacy of the parent compounds.Future studies should focus on strengthening the real-world evidence,defining the interaction between gut microbiota and PNS,and developing the strategy for modulating gut microbiota to enhance the bioavailability and efficacy of PNS.These information would be useful for further research and clinical application of PNS.展开更多
Objective:To investigate the relationship between triterpenoid saponin content and antioxidant,antimicrobial,and α-glucosidase inhibitory activities of 70%ethanolic,butanolic,aqueous,supernate and precipitate extract...Objective:To investigate the relationship between triterpenoid saponin content and antioxidant,antimicrobial,and α-glucosidase inhibitory activities of 70%ethanolic,butanolic,aqueous,supernate and precipitate extracts of Juglans regia leaves.Methods:Triterpenoid saponins of different Juglans regia leaf extracts were measured by the vanillin method.Antioxidant activity was evaluated against DPPH and ABTS free radicals.We also assessed α-glucosidase inhibitory and antimicrobial activities of the leaf extracts.Pearson’s correlation coefficient was evaluated to determine the correlation between the saponin content and biological activities.Results:The butanolic extract was most effective against DPPH with an IC50of 6.63μg/mL,while the aqueous extract showed the highest scavenging activity against ABTS free radical with an IC50of 42.27μg/mL.Pearson’s correlation analysis indicated a strong negative correlation (r=-0.956) between DPPH radical scavenging activity (IC50) and the saponin content in the samples examined.In addition,the aqueous extract showed the best α-glucosidase inhibitory activity compared with other extracts.All the extracts had fair antibacterial activity against Bacillus subtilis,Escherichia coli,and Klebsiella pneumoniae except for the aqueous extract.Conclusions:Juglans regia extracts show potent antioxidant,antimicrobial,and α-glucosidase inhibitory activities.There is a correlation between saponin levels in Juglans regia leaf extracts and the studied activities.However,additional research is required to establish these relationships by identifying the specific saponin molecules responsible for these activities and elucidating their mechanisms of action.展开更多
Saponins are the main triterpenoid ingredients from Panax notoginseng,a well-known Chinese medicine,and are important sources for producing drugs to prevent and treat cerebrovascular and cardiovascular diseases.Howeve...Saponins are the main triterpenoid ingredients from Panax notoginseng,a well-known Chinese medicine,and are important sources for producing drugs to prevent and treat cerebrovascular and cardiovascular diseases.However,the transcriptional regulatory network of saponin biosynthesis in P.notoginseng is largely unknown.In the present study we demonstrated that one R2R3-MYB transcription factor,designated PnMYB4,acts as a repressor of saponin accumulation.Suppression of PnMYB4 in P.notoginseng calli significantly increased the saponin content and the expression level of saponin biosynthetic genes.PnMYB4 directly bound to the promoters of key saponin biosynthetic genes,including PnSS,PnSE,and PnDS,to repress saponin accumulation.PnMYB4 and the activator PnMYB1 could inter-acted with PnbHLH,which is a positive regulator of saponin biosynthesis,to modulate the biosynthesis of saponin.PnMYB4 competed with PnMYB1 for binding to PnbHLH,repressing activation of the promoters of saponin structural genes induced by the PnMYB1-PnbHLH complex.Our study reveals that a complex regulatory module of saponin biosynthesis is associated with positive and negative MYB transcriptional regulators and provides a theoretical basis for improving the content of saponins and efficacy of P.notoginseng.展开更多
Background:Diethylnitrosamine,one of food additives,possessed a strong carcinogenic effect in human.Rhizoma paridis saponins,as the main active components of Paris polyphylla,have a good anti-cancer effect in our prev...Background:Diethylnitrosamine,one of food additives,possessed a strong carcinogenic effect in human.Rhizoma paridis saponins,as the main active components of Paris polyphylla,have a good anti-cancer effect in our previous research.To verify their inhibitory effect on diethylnitrosamine-induced liver cancer,we carried out this study.Methods:We established diethylnitrosamine-induced mouse hepatocarcinoma models to evaluate antitumor of Rhizoma paridis saponins.Subsequently,gas chromatography-mass spectrometry was applied to analyze the metabolites in the urine and serum samples.Results:Rhizoma paridis saponins alleviated diethylnitrosamine-induced hepatocarcinogenesis.On the one hand,Rhizoma paridis saponins down-regulated the levels of liver function markers,such as alanine aminotransferase,aspartate transaminase and alpha fetoprotein.On the other hand,Rhizoma paridis saponins reduced metabolic disorders by increasing fructose and mannose metabolism,and decreasing pentose and glucuronate interconversion,inositol phosphate metabolism,and the process of saturated fatty acids transforming to unsaturated fatty acids,which based on the regulating mRNA expression of glucose transporter type 4,lactate dehydrogenase A,fatty acid synthetas,acetyl-CoA carboxylase and apolipoprotein A-I.Conclusion:Rhizoma paridis saponins has the potential application to inhibit chemical-induced hepatocarcinogenesis in the future.展开更多
Objective:Tribulus terrestris saponin is a traditional Chinese medicine in China.This experiment was designed to investigate the effects of tribulus terrestris saponin on the proliferation and invasion ability of non-...Objective:Tribulus terrestris saponin is a traditional Chinese medicine in China.This experiment was designed to investigate the effects of tribulus terrestris saponin on the proliferation and invasion ability of non-small cell lung cancer A549 cells.Methods:A549 cells were divided into normal control and experimental groups(Tribulus terrestris saponin 250μg/mL group,Tribulus terrestris saponin 200μg/mL group,Tribulus terrestris saponin 150μg/mL group,Tribulus terrestris saponin 100μg/mL group,Tribulus terrestris saponin 50μg/mL group).The proliferation viability of the cells in each group was detected by CCK8,the invasion of tumor cells was detected by Transwell model.The mRNA expression of MMP9 and caspase-3 in each group of cells was detected by RT-PCR.Immunofluorescence staining was used to observe the fluorescence intensity of caspase-3 in each group of cells.Results:Compared with the normal control group,tribulus terrestris saponin significantly inhibited the proliferation activity and invasion ability of A549 cells,which was statistically significant(P<0.01).In the invasion assay,compared with the control group,MMP9 expression was significantly reduced and caspase-3 expression was significantly increased in the tribulus terrestris saponin group,and both were concentration-dependent,with statistically significant differences(P<0.01).By cellular immunofluorescence staining experiments,it was found that the fluorescence expression of caspase-3 was enhanced in the experimental group compared with the normal control group,in which the high concentration saponin group was significantly higher than the low concentration group.Conclusion:Tribulus terrestris saponin can inhibit the invasive ability of A549 cells by down-regulating the expression of MMP9,and induce irreversible apoptosis by up-regulating the activation of caspase-3 expression to form caspase-3.展开更多
Arbuscular mycorrhizal fungi(AMF)are important members of the plant microbiome and affect the uptake and transfer of mineral elements by forming a symbiotic relationship with plant roots.Nitrogen(N),as an important mi...Arbuscular mycorrhizal fungi(AMF)are important members of the plant microbiome and affect the uptake and transfer of mineral elements by forming a symbiotic relationship with plant roots.Nitrogen(N),as an important mineral element,can directly affect plant growth and development at different N levels.It has been confirmed that inoculation with AMF can improve the efficiency of N utilization by plants.However,there are still fewer reports on the dynamic relationship between arbuscular mycorrhizal and plant secondary metabolites at different nitrogen levels.In this experiment,the physiological indexes and genes related to saponin synthesis were determined by applying different concentration gradients of nitrogen to the medicinal plant P.polyphylla var.yunnanensis infested by AMF as the test material.It was found that nitrogen addition increased the biomass,chlorophyll content,and nutrient content of above-and below-ground plant parts and increased the content of saponin content of P.polyphylla var.yunnanensis to some extent,but AMF inoculation increased the saponin content of P.polyphylla var.yunnanensis more significantly.AMF inoculation also promoted the expression of genes related to the saponin synthesis pathway,including 3-hydroxy-3-methylglutaryl coenzyme A synthase(HMGS),squalene epoxidase 1(SE1),and cycloartenol synthase(CAS),which is in according with the accumulation of saponin in plants.It also may increase the saponin content of AMF plants by altering the expression of P450s and UGTs related to saponin synthesis.展开更多
基金supported by Guangdong Basic and Applied Basic Research Foundation(No.2022A1515012039)Guangzhou Science and Technology Plan Project(No.2024A03J0360).
文摘Panax notoginseng saponins(PNS)are a class of effective ingredients in Notoginseng Radix et Rhizoma,a well-known herbal medicine called San-Qi in Chinese.After oral administration,PNS inevitably interacts with gut microbiota,and thus affect the pharmacokinetic profiles and pharmacological effects.To date,studies concering gut microbiota-mediated metabolism of PNS have not been reviewed systematically.Herein,we outline the metabolic profiles of Panax notoginseng saponins mediated by gut microbiota,as well as its role in the pharmacokinetics and pharmacodynamics on the basis of reported data.The metabolic pathways of primary saponins are proposed,and step-by-step deglycosylation is found to be the primary degradation pathways of PNS mediated by gut microbiota.Specific microorganisms and enzymes involved in the metabolic processes were summarized.Gut microbiota is deeply involved in the metabolism of PNS,affects the pharmacokinetic profiles,and produces a series of active metabolites.These metabolites were documented to play an essential role in the efficacy of the parent compounds.Future studies should focus on strengthening the real-world evidence,defining the interaction between gut microbiota and PNS,and developing the strategy for modulating gut microbiota to enhance the bioavailability and efficacy of PNS.These information would be useful for further research and clinical application of PNS.
基金supported by the Deanship of Scientific Research at Umm Al-Qura University(Grant code:22UQU4331128DSR77).
文摘Objective:To investigate the relationship between triterpenoid saponin content and antioxidant,antimicrobial,and α-glucosidase inhibitory activities of 70%ethanolic,butanolic,aqueous,supernate and precipitate extracts of Juglans regia leaves.Methods:Triterpenoid saponins of different Juglans regia leaf extracts were measured by the vanillin method.Antioxidant activity was evaluated against DPPH and ABTS free radicals.We also assessed α-glucosidase inhibitory and antimicrobial activities of the leaf extracts.Pearson’s correlation coefficient was evaluated to determine the correlation between the saponin content and biological activities.Results:The butanolic extract was most effective against DPPH with an IC50of 6.63μg/mL,while the aqueous extract showed the highest scavenging activity against ABTS free radical with an IC50of 42.27μg/mL.Pearson’s correlation analysis indicated a strong negative correlation (r=-0.956) between DPPH radical scavenging activity (IC50) and the saponin content in the samples examined.In addition,the aqueous extract showed the best α-glucosidase inhibitory activity compared with other extracts.All the extracts had fair antibacterial activity against Bacillus subtilis,Escherichia coli,and Klebsiella pneumoniae except for the aqueous extract.Conclusions:Juglans regia extracts show potent antioxidant,antimicrobial,and α-glucosidase inhibitory activities.There is a correlation between saponin levels in Juglans regia leaf extracts and the studied activities.However,additional research is required to establish these relationships by identifying the specific saponin molecules responsible for these activities and elucidating their mechanisms of action.
基金This study was supported by Beijing Science and Technology Planning Project(Z201100005420005,China).
文摘Saponins are the main triterpenoid ingredients from Panax notoginseng,a well-known Chinese medicine,and are important sources for producing drugs to prevent and treat cerebrovascular and cardiovascular diseases.However,the transcriptional regulatory network of saponin biosynthesis in P.notoginseng is largely unknown.In the present study we demonstrated that one R2R3-MYB transcription factor,designated PnMYB4,acts as a repressor of saponin accumulation.Suppression of PnMYB4 in P.notoginseng calli significantly increased the saponin content and the expression level of saponin biosynthetic genes.PnMYB4 directly bound to the promoters of key saponin biosynthetic genes,including PnSS,PnSE,and PnDS,to repress saponin accumulation.PnMYB4 and the activator PnMYB1 could inter-acted with PnbHLH,which is a positive regulator of saponin biosynthesis,to modulate the biosynthesis of saponin.PnMYB4 competed with PnMYB1 for binding to PnbHLH,repressing activation of the promoters of saponin structural genes induced by the PnMYB1-PnbHLH complex.Our study reveals that a complex regulatory module of saponin biosynthesis is associated with positive and negative MYB transcriptional regulators and provides a theoretical basis for improving the content of saponins and efficacy of P.notoginseng.
文摘Background:Diethylnitrosamine,one of food additives,possessed a strong carcinogenic effect in human.Rhizoma paridis saponins,as the main active components of Paris polyphylla,have a good anti-cancer effect in our previous research.To verify their inhibitory effect on diethylnitrosamine-induced liver cancer,we carried out this study.Methods:We established diethylnitrosamine-induced mouse hepatocarcinoma models to evaluate antitumor of Rhizoma paridis saponins.Subsequently,gas chromatography-mass spectrometry was applied to analyze the metabolites in the urine and serum samples.Results:Rhizoma paridis saponins alleviated diethylnitrosamine-induced hepatocarcinogenesis.On the one hand,Rhizoma paridis saponins down-regulated the levels of liver function markers,such as alanine aminotransferase,aspartate transaminase and alpha fetoprotein.On the other hand,Rhizoma paridis saponins reduced metabolic disorders by increasing fructose and mannose metabolism,and decreasing pentose and glucuronate interconversion,inositol phosphate metabolism,and the process of saturated fatty acids transforming to unsaturated fatty acids,which based on the regulating mRNA expression of glucose transporter type 4,lactate dehydrogenase A,fatty acid synthetas,acetyl-CoA carboxylase and apolipoprotein A-I.Conclusion:Rhizoma paridis saponins has the potential application to inhibit chemical-induced hepatocarcinogenesis in the future.
基金National Key R&D Plan(2022YFC2305004)Hainan Province Major Science and Technology Special Project(No.ZDKJ2021036)+3 种基金Key R&D projects in Hainan Province(No.ZDYF2020223)Hainan Province Key R&D Plan International Science and Technology Cooperation Project(GHYF2022011)Hainan Provincial Innovation Team Project(No.820CXTD448)National Natural Science Foundation of China(No.82260001,82160012)。
文摘Objective:Tribulus terrestris saponin is a traditional Chinese medicine in China.This experiment was designed to investigate the effects of tribulus terrestris saponin on the proliferation and invasion ability of non-small cell lung cancer A549 cells.Methods:A549 cells were divided into normal control and experimental groups(Tribulus terrestris saponin 250μg/mL group,Tribulus terrestris saponin 200μg/mL group,Tribulus terrestris saponin 150μg/mL group,Tribulus terrestris saponin 100μg/mL group,Tribulus terrestris saponin 50μg/mL group).The proliferation viability of the cells in each group was detected by CCK8,the invasion of tumor cells was detected by Transwell model.The mRNA expression of MMP9 and caspase-3 in each group of cells was detected by RT-PCR.Immunofluorescence staining was used to observe the fluorescence intensity of caspase-3 in each group of cells.Results:Compared with the normal control group,tribulus terrestris saponin significantly inhibited the proliferation activity and invasion ability of A549 cells,which was statistically significant(P<0.01).In the invasion assay,compared with the control group,MMP9 expression was significantly reduced and caspase-3 expression was significantly increased in the tribulus terrestris saponin group,and both were concentration-dependent,with statistically significant differences(P<0.01).By cellular immunofluorescence staining experiments,it was found that the fluorescence expression of caspase-3 was enhanced in the experimental group compared with the normal control group,in which the high concentration saponin group was significantly higher than the low concentration group.Conclusion:Tribulus terrestris saponin can inhibit the invasive ability of A549 cells by down-regulating the expression of MMP9,and induce irreversible apoptosis by up-regulating the activation of caspase-3 expression to form caspase-3.
基金supported by the Key R&D Program of Yunnan Province,China(Grant No.202103AC100003202101AS070228)+2 种基金the Major Special Project of the Ministry of Science and Technology(2021YFD10002022021YFD1601003)and the National Natural Science Foundation of China(Grant No.31860075),thank you.
文摘Arbuscular mycorrhizal fungi(AMF)are important members of the plant microbiome and affect the uptake and transfer of mineral elements by forming a symbiotic relationship with plant roots.Nitrogen(N),as an important mineral element,can directly affect plant growth and development at different N levels.It has been confirmed that inoculation with AMF can improve the efficiency of N utilization by plants.However,there are still fewer reports on the dynamic relationship between arbuscular mycorrhizal and plant secondary metabolites at different nitrogen levels.In this experiment,the physiological indexes and genes related to saponin synthesis were determined by applying different concentration gradients of nitrogen to the medicinal plant P.polyphylla var.yunnanensis infested by AMF as the test material.It was found that nitrogen addition increased the biomass,chlorophyll content,and nutrient content of above-and below-ground plant parts and increased the content of saponin content of P.polyphylla var.yunnanensis to some extent,but AMF inoculation increased the saponin content of P.polyphylla var.yunnanensis more significantly.AMF inoculation also promoted the expression of genes related to the saponin synthesis pathway,including 3-hydroxy-3-methylglutaryl coenzyme A synthase(HMGS),squalene epoxidase 1(SE1),and cycloartenol synthase(CAS),which is in according with the accumulation of saponin in plants.It also may increase the saponin content of AMF plants by altering the expression of P450s and UGTs related to saponin synthesis.
