Objective To analyze the chemical constituents of Shanxiangyuanye(Turpiniae Folium)through liquid chromatography-tandem mass spectrometry(LC-MS/MS)method,and to evaluate their anti-oxidant,hypoglycemic,and anti-glycat...Objective To analyze the chemical constituents of Shanxiangyuanye(Turpiniae Folium)through liquid chromatography-tandem mass spectrometry(LC-MS/MS)method,and to evaluate their anti-oxidant,hypoglycemic,and anti-glycation activities related to diabetic complications.Methods The supernatant of Shanxiangyuanye(Turpiniae Folium)(TFS),obtained following water extraction and alcohol precipitation,was analyzed by LC-MS/MS.Antioxidant activity of TFS in vitro was evaluated using three experimental approaches:the 1,1-diphenyl-2-picrylhydrazyl(DPPH)radical scavenging assay,the 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)(ABTS+)radical cation decolorization assay,and the hydroxyl(·OH)radical scavenging assay.To comprehensively evaluate hypoglycemic potential,α-glucosidase inhibition was measured to analyze in vitro hypoglycemic activity.Subsequently,in vitro models were developed to examine anti-glycation activity through the bovine serum albumin(BSA)-fructose(Fru),BSA-methylglyoxal(MGO),BSA-glyoxal(GO),and D-arginine(Arg)-MGO systems,with particular attention to the inhibitory effects of TFS.Furthermore,the concentrations of fructosamine,protein carbonyls,sulfhydryl groups,andβ-amyloid in the glycation solution were quantified using the BSA-Fru model following 7-d of incubation at 37°C.Results Using LC-MS/MS analysis in both positive and negative ion modes,we identified 750 chemical components in TFS,primarily including organic acids,amino acids,and their derivatives.In vitro activity studies demonstrated that TFS exhibited remarkable free radical scavenging capacity,with half-maximal inhibitory concentrations(IC_(50))of 0.47,1.56,and 0.36 mg/mL against DPPH,ABTS+,and·OH radicals,respectively.Regarding hypoglycemic activity,TFS dose-dependently inhibitedα-glucosidase activity(IC_(50)=0.21 mg/mL),displaying comparable efficacy to the clinical drug acarbose(IC_(50)=0.23 mg/mL).Notably,TFS intervened in the glycation process:IC_(50) values were 0.22,1.91–4.96,and 4.09 mg/mL in the BSAFru,BSA-MGO/GO,and Arg-MGO models,respectively,with the most prominent inhibitory effects observed in the BSA-Fru model.Furthermore,although TFS may not effectively preserve thiol groups in BSA or reduce thiol oxidation during glycation,it significantly reduces fructosamine levels(in a dose-dependent manner),decreasesβ-amyloid formation,and inhibits protein carbonylation(P<0.0001).Conclusion The findings demonstrate that TFS exhibits a complex chemical composition with potent antioxidant,hypoglycemic,and anti-glycation activities.These results provide compelling scientific evidence supporting TFS’s potential as a natural adjuvant for diabetes prevention and complication management,while laying a solid foundation for its applications in functional food development and adjunctive antidiabetic therapeutics.展开更多
Flavonoids,the key active compounds in Epimedii Folium,have both protective and toxic effects on the liver.Their hepatoprotective effects are associated with reducing lipid accumulation and oxidative stress,which cont...Flavonoids,the key active compounds in Epimedii Folium,have both protective and toxic effects on the liver.Their hepatoprotective effects are associated with reducing lipid accumulation and oxidative stress,which contribute to the management of various liver conditions.In contrast,the mechanisms driving Epimedii Folium-induced hepatotoxicity are less understood but likely involve oxidative stress and pyroptosis.Pharmacokinetic studies,especially on icaritin,indicate that it undergoes isopentenyl dehydrogenation,glycosylation,and glucuronidation in vivo,contributing to its pharmacological effects.However,intermediate metabolites of icaritin may interact with biomolecules,potentially leading to liver toxicity.This review offers a detailed examination of the dual effects of Epimedii Folium flavonoids on liver function,emphasizing recent discoveries in their hepatoprotective and hepatotoxic pathways.We also summarize and discuss the pharmacokinetics of these flavonoids,highlighting how their meta-bolism affects therapeutic efficacy and toxicity.Lastly,we propose strategies to mitigate liver injury,providing new perspectives on the safe use of Epimedii Folium.展开更多
[Objective] To extract the effective component rosmarinic acid from Folium perillae,study preparation technology and quality control of rosmarinic acid injection and provide test basis for hemorheological drug develop...[Objective] To extract the effective component rosmarinic acid from Folium perillae,study preparation technology and quality control of rosmarinic acid injection and provide test basis for hemorheological drug development and clinic application.[Method]The coarse powder of Folium perillae(40 μm)was lixiviated with hot water and acidized to make aqueous extracts.Rosmarinic acid from the aqueous mixture was extracted with Ethyl Acetate.And Et Ac was evaporated to obtain primary product.The injection was purified by pH adjustment.Concentration of rosmarinic acid in the injection was detected by high performance liquid chromatography(HPLC).Contents of tannin,resin and oxalate were eliminated according to the Chinese Pharmacopeia(2005 edition).Stability,irritation,haemolyticus,LD50 and thermogenic substance of this injection were also detected.[Result]The content of rosmarinic acid in Folium perillae injection is 2.81 mg/ml,and the content of LD50 was 406.82 mg/kg.This injection was consistent with the stipulation of Chinese Pharmacopeia(2005 edition).[Conclusion]The preparation technology of this experiment was reasonable.The stable qualities of the prepared injection meet the injection requirement.展开更多
基金Key Project of Hunan Provincial Education Bureau(23A0307)Natural Science Foundation of Hunan Province (2025JJ80089)。
文摘Objective To analyze the chemical constituents of Shanxiangyuanye(Turpiniae Folium)through liquid chromatography-tandem mass spectrometry(LC-MS/MS)method,and to evaluate their anti-oxidant,hypoglycemic,and anti-glycation activities related to diabetic complications.Methods The supernatant of Shanxiangyuanye(Turpiniae Folium)(TFS),obtained following water extraction and alcohol precipitation,was analyzed by LC-MS/MS.Antioxidant activity of TFS in vitro was evaluated using three experimental approaches:the 1,1-diphenyl-2-picrylhydrazyl(DPPH)radical scavenging assay,the 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)(ABTS+)radical cation decolorization assay,and the hydroxyl(·OH)radical scavenging assay.To comprehensively evaluate hypoglycemic potential,α-glucosidase inhibition was measured to analyze in vitro hypoglycemic activity.Subsequently,in vitro models were developed to examine anti-glycation activity through the bovine serum albumin(BSA)-fructose(Fru),BSA-methylglyoxal(MGO),BSA-glyoxal(GO),and D-arginine(Arg)-MGO systems,with particular attention to the inhibitory effects of TFS.Furthermore,the concentrations of fructosamine,protein carbonyls,sulfhydryl groups,andβ-amyloid in the glycation solution were quantified using the BSA-Fru model following 7-d of incubation at 37°C.Results Using LC-MS/MS analysis in both positive and negative ion modes,we identified 750 chemical components in TFS,primarily including organic acids,amino acids,and their derivatives.In vitro activity studies demonstrated that TFS exhibited remarkable free radical scavenging capacity,with half-maximal inhibitory concentrations(IC_(50))of 0.47,1.56,and 0.36 mg/mL against DPPH,ABTS+,and·OH radicals,respectively.Regarding hypoglycemic activity,TFS dose-dependently inhibitedα-glucosidase activity(IC_(50)=0.21 mg/mL),displaying comparable efficacy to the clinical drug acarbose(IC_(50)=0.23 mg/mL).Notably,TFS intervened in the glycation process:IC_(50) values were 0.22,1.91–4.96,and 4.09 mg/mL in the BSAFru,BSA-MGO/GO,and Arg-MGO models,respectively,with the most prominent inhibitory effects observed in the BSA-Fru model.Furthermore,although TFS may not effectively preserve thiol groups in BSA or reduce thiol oxidation during glycation,it significantly reduces fructosamine levels(in a dose-dependent manner),decreasesβ-amyloid formation,and inhibits protein carbonylation(P<0.0001).Conclusion The findings demonstrate that TFS exhibits a complex chemical composition with potent antioxidant,hypoglycemic,and anti-glycation activities.These results provide compelling scientific evidence supporting TFS’s potential as a natural adjuvant for diabetes prevention and complication management,while laying a solid foundation for its applications in functional food development and adjunctive antidiabetic therapeutics.
基金the National Natural Science Foundation of China(Grant No.:82174071).
文摘Flavonoids,the key active compounds in Epimedii Folium,have both protective and toxic effects on the liver.Their hepatoprotective effects are associated with reducing lipid accumulation and oxidative stress,which contribute to the management of various liver conditions.In contrast,the mechanisms driving Epimedii Folium-induced hepatotoxicity are less understood but likely involve oxidative stress and pyroptosis.Pharmacokinetic studies,especially on icaritin,indicate that it undergoes isopentenyl dehydrogenation,glycosylation,and glucuronidation in vivo,contributing to its pharmacological effects.However,intermediate metabolites of icaritin may interact with biomolecules,potentially leading to liver toxicity.This review offers a detailed examination of the dual effects of Epimedii Folium flavonoids on liver function,emphasizing recent discoveries in their hepatoprotective and hepatotoxic pathways.We also summarize and discuss the pharmacokinetics of these flavonoids,highlighting how their meta-bolism affects therapeutic efficacy and toxicity.Lastly,we propose strategies to mitigate liver injury,providing new perspectives on the safe use of Epimedii Folium.
基金Supported by National Natural Science Foundation Project(10572029,10772054)Key Project of National Natural Science Foundation(10632010)~~
文摘[Objective] To extract the effective component rosmarinic acid from Folium perillae,study preparation technology and quality control of rosmarinic acid injection and provide test basis for hemorheological drug development and clinic application.[Method]The coarse powder of Folium perillae(40 μm)was lixiviated with hot water and acidized to make aqueous extracts.Rosmarinic acid from the aqueous mixture was extracted with Ethyl Acetate.And Et Ac was evaporated to obtain primary product.The injection was purified by pH adjustment.Concentration of rosmarinic acid in the injection was detected by high performance liquid chromatography(HPLC).Contents of tannin,resin and oxalate were eliminated according to the Chinese Pharmacopeia(2005 edition).Stability,irritation,haemolyticus,LD50 and thermogenic substance of this injection were also detected.[Result]The content of rosmarinic acid in Folium perillae injection is 2.81 mg/ml,and the content of LD50 was 406.82 mg/kg.This injection was consistent with the stipulation of Chinese Pharmacopeia(2005 edition).[Conclusion]The preparation technology of this experiment was reasonable.The stable qualities of the prepared injection meet the injection requirement.
