Objective:To evaluate the antitumor activity both in vitro and in vivo of saponin–phospholipid complex of Panax notoginseng.Methods:The in vitro cytotoxic effect of saponins extract and saponin–phospholipid complex ...Objective:To evaluate the antitumor activity both in vitro and in vivo of saponin–phospholipid complex of Panax notoginseng.Methods:The in vitro cytotoxic effect of saponins extract and saponin–phospholipid complex against human lung cancer NCI-H460 and breast cancer cell lines BT474 was examined using MTS assay.For in vivo evaluation of antitumor potential,saponin and saponin–phospholipid complex were administered orally in rats induced mammary carcinogenesis by 7,12-dimethylbenz(a)anthracene,for 30 days.Results:Our data showed that saponin–phospholipid complex had stronger anticancer effect compared to saponin extract.The IC50 values of saponin–phospholipid complex and saponin extract for NCI-H460 cell lines were 28.47 mg/m L and 47.97 mg/mL,respectively and these values for BT474 cells were 53.18 mg/mL and 86.24 mg/mL,respectively.In vivo experiments,administration of saponin,saponin–phospholipid complex and paclitaxel(positive control) effectively suppressed 7,12-dimethylbenz(a) anthracene-induced breast cancer evidenced by a decrease in tumor volume,the reduction of lipid peroxidation level and increase in the body weight,and elevated the enzymatic antioxidant activities of superoxide dismutase,catalase,glutathione peroxidase in rat breast tissue.Conclusions:Our study suggests that saponin extract from Panax notoginseng and saponin–phospholipid complex have potential to prevent cancer,especially breast cancer.展开更多
Kaempferol(KA),as one of the flavonoids,has extensive pharmacological properties.However,the poor solubility of KA severely limits its clinical application.In our study,the kaempferol phospholipid complex(KA-PC)has be...Kaempferol(KA),as one of the flavonoids,has extensive pharmacological properties.However,the poor solubility of KA severely limits its clinical application.In our study,the kaempferol phospholipid complex(KA-PC)has been prepared by solvent evaporation for the enhancement of the bioavailability of KA.KA-PC was verified by scanning electron microscope characterization methods.Drug loading,solubility and long-term stability were measured.The characterization results showed that KA-PC was formed through the intermolecular interaction between KA and phospholipids.The solubility of KA-PC in water was 189 times higher than that of KA,and the solubility in n-octanol was also significantly improved.Besides,pharmacodynamic studies showed that KA-PC can significantly reduce the level of serum uric acid in mice without causing renal injury.This study expanded the clinical application of KA by preparing KA-PC.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
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
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
[Objectives]The study aims to discuss the effects of addition of arginine and glutamic acid or soybean phospholipid,vitamin E and yeast selenium in diet on the slaughter performance and meat quality of long(white)...[Objectives]The study aims to discuss the effects of addition of arginine and glutamic acid or soybean phospholipid,vitamin E and yeast selenium in diet on the slaughter performance and meat quality of long(white)×large(York)binary hybrid pigs.[Methods]27 long×large castrated hybrid boars with the body weight of(54.4±0.15)kg were randomly divided into 3 groups,with 3 replicates per group and 3 pigs per replicate.Group A was the control group,in which the pigs were fed basal diet;in group B,0.8%arginine and 0.60%glutamate were added to the basal diet;in group C,75 g of soybean phospholipid,20 g of vitamin E and 8 g of yeast selenium were added to every 100 kg of the basal diet.The trial period was 60 d.After the experiment was ended,one test pig with similar body weight was selected from each replicate for slaughter and meat determination.[Results]The average weight gain and eye muscle area of the pigs in group B were significantly higher than those in group C(P<0.05),and also showed an increasing trend compared with group A,but there was no statistically significant difference(P>0.05);there was no significant difference between group B or C and group A in the average weight gain and eye muscle area(P>0.05).There was no significant difference in other slaughter performance between the three groups(P>0.05).Besides,there was also no significant difference in the content of various amino acids,total amino acids and total umami amino acids between the three groups(P>0.05).The inosine content in the longissimus dorsi muscle and muscle cooking loss of binary hybrid pigs in group C were significantly better than those in group B(P<0.05),and also had a tendency to be better than those in group A,but there was no significant difference(P>0.05);there was no significant difference between group B or C and group A in the inosine content and muscle cooking loss of the pigs(P>0.05).In addition,there was no significant difference in other meat traits and chemical composition of the longissimus dorsi muscle between group B or C and group A(P>0.05).[Conclusions]The addition of arginine and glutamic acid or soybean phospholipid,vitamin E and yeast selenium in diet had no significant effect on the growth rate,slaughter performance and meat traits of long×large binary hybrid pigs.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
文摘Objective:To evaluate the antitumor activity both in vitro and in vivo of saponin–phospholipid complex of Panax notoginseng.Methods:The in vitro cytotoxic effect of saponins extract and saponin–phospholipid complex against human lung cancer NCI-H460 and breast cancer cell lines BT474 was examined using MTS assay.For in vivo evaluation of antitumor potential,saponin and saponin–phospholipid complex were administered orally in rats induced mammary carcinogenesis by 7,12-dimethylbenz(a)anthracene,for 30 days.Results:Our data showed that saponin–phospholipid complex had stronger anticancer effect compared to saponin extract.The IC50 values of saponin–phospholipid complex and saponin extract for NCI-H460 cell lines were 28.47 mg/m L and 47.97 mg/mL,respectively and these values for BT474 cells were 53.18 mg/mL and 86.24 mg/mL,respectively.In vivo experiments,administration of saponin,saponin–phospholipid complex and paclitaxel(positive control) effectively suppressed 7,12-dimethylbenz(a) anthracene-induced breast cancer evidenced by a decrease in tumor volume,the reduction of lipid peroxidation level and increase in the body weight,and elevated the enzymatic antioxidant activities of superoxide dismutase,catalase,glutathione peroxidase in rat breast tissue.Conclusions:Our study suggests that saponin extract from Panax notoginseng and saponin–phospholipid complex have potential to prevent cancer,especially breast cancer.
基金funded by Young and Middle Aged Teachers’Career Development Support Project of Shenyang Pharmaceutical University(ZQN2019005).
文摘Kaempferol(KA),as one of the flavonoids,has extensive pharmacological properties.However,the poor solubility of KA severely limits its clinical application.In our study,the kaempferol phospholipid complex(KA-PC)has been prepared by solvent evaporation for the enhancement of the bioavailability of KA.KA-PC was verified by scanning electron microscope characterization methods.Drug loading,solubility and long-term stability were measured.The characterization results showed that KA-PC was formed through the intermolecular interaction between KA and phospholipids.The solubility of KA-PC in water was 189 times higher than that of KA,and the solubility in n-octanol was also significantly improved.Besides,pharmacodynamic studies showed that KA-PC can significantly reduce the level of serum uric acid in mice without causing renal injury.This study expanded the clinical application of KA by preparing KA-PC.
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.
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.
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 Self-funded Project of Agricultural Science and Technology of Guangxi(Z2022114).
文摘[Objectives]The study aims to discuss the effects of addition of arginine and glutamic acid or soybean phospholipid,vitamin E and yeast selenium in diet on the slaughter performance and meat quality of long(white)×large(York)binary hybrid pigs.[Methods]27 long×large castrated hybrid boars with the body weight of(54.4±0.15)kg were randomly divided into 3 groups,with 3 replicates per group and 3 pigs per replicate.Group A was the control group,in which the pigs were fed basal diet;in group B,0.8%arginine and 0.60%glutamate were added to the basal diet;in group C,75 g of soybean phospholipid,20 g of vitamin E and 8 g of yeast selenium were added to every 100 kg of the basal diet.The trial period was 60 d.After the experiment was ended,one test pig with similar body weight was selected from each replicate for slaughter and meat determination.[Results]The average weight gain and eye muscle area of the pigs in group B were significantly higher than those in group C(P<0.05),and also showed an increasing trend compared with group A,but there was no statistically significant difference(P>0.05);there was no significant difference between group B or C and group A in the average weight gain and eye muscle area(P>0.05).There was no significant difference in other slaughter performance between the three groups(P>0.05).Besides,there was also no significant difference in the content of various amino acids,total amino acids and total umami amino acids between the three groups(P>0.05).The inosine content in the longissimus dorsi muscle and muscle cooking loss of binary hybrid pigs in group C were significantly better than those in group B(P<0.05),and also had a tendency to be better than those in group A,but there was no significant difference(P>0.05);there was no significant difference between group B or C and group A in the inosine content and muscle cooking loss of the pigs(P>0.05).In addition,there was no significant difference in other meat traits and chemical composition of the longissimus dorsi muscle between group B or C and group A(P>0.05).[Conclusions]The addition of arginine and glutamic acid or soybean phospholipid,vitamin E and yeast selenium in diet had no significant effect on the growth rate,slaughter performance and meat traits of long×large binary hybrid pigs.
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.