OBJECTIVE To explore the protective effects of total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja on STZ-stimulated INS-1 cells through regulating of autophagy and apoptosis.METHODS INS-1cells wer...OBJECTIVE To explore the protective effects of total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja on STZ-stimulated INS-1 cells through regulating of autophagy and apoptosis.METHODS INS-1cells were cultured in media containing 3n M STZ and different doses of total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja.The proliferation of cells was examined by MTT assay,ROS content were detected by fluorescence enzyme label.The levels of superoxide dismutase(SOD),glutathione peroxidase(GSH-Px),hydrogen peroxidase(CAT),malondialdehyde(MDA)were also measured by colorimetry.The activities of caspase-3,9 were also observed by Caspase colorimetric assay kit in each group.The expressions of Bcl-2 m RNA and Bax m RNA were detected by Real time PCR,protein expression of LC3-Ⅱand PARP were detected by Western blotting.RESULTS Compared with the control group,total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja could promote the proliferation of INS-1 cells no matter with STZ or not when its concentration lower than 25μg·m L^(-1);but when its concentration higher than 100μg·m L^(-1)(use individually)or 50μg·m L^(-1)(combined use),total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja might significantly inhibite the growth of the cells whether STZ existed or not.Total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja(6.25,12.5,25μg·m L^(-1))might inhibit INS-1cell apoptosis,decrease intra-cellular ROS contents,improve the s upernatant liquid SOD,GSH-PX,CAT activities,decrease MDA level,promote INS-1 cell secreting insulin,decrease the protein expressions of autophagy protein LC3Ⅱand apoptosis regulating protein cleaved PARP protein,up-regulate the anti-apoptotic protein Bcl-2 m RNA expression,down-regulate the pro-apoptotic protein Bax m RNA expression and Bcl-2and Bax,reduce the activity of caspase-9 and caspase-3(P<0.05 or P<0.01).CONCLUSION Total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja has good protective effect on STZ-stimulated INS-1cells.It can inhibit STZ injured INS-1 cells to overproduce ROS production,enhance endogenous antioxidant enzymes(GSH-Px,SOD,CAT activities),reduce the expression of autophagy protein LC3Ⅱand apoptosisregulating protein cleaved PARP,up-reglute the antiapoptosis protein Bcl-2 expression,down-regulate the pro-apoptotic protein Bax expression,decrease the caspase-9 and caspase-3 activities,and improve the INS-1cell survival rate,and then play a protective effect on damaged INS-1 cells.展开更多
[Objectives] To optimize the extraction process and determine the total triterpenoids from Semen Trichosanthis.[Methods]The Box-behnken response surface methodology was applied to optimize the extraction conditions of...[Objectives] To optimize the extraction process and determine the total triterpenoids from Semen Trichosanthis.[Methods]The Box-behnken response surface methodology was applied to optimize the extraction conditions of total triterpenoids in Semen Trichosanthis.And the spectrophotometry was used to determine the content of total triterpenoids in Semen Trichosanthis.[Results] The optimal extraction conditions were solid to liquid ratio of 40∶ 1,ultrasonic time of 20 min,and ultrasonic power of 100 W.Under these conditions,the content of total triterpenoids in Semen Trichosanthis was significantly different among the 10 production areas,among which the No.9 production area(Anhui 1) had the highest total triterpenoids content of 45.71 mg/g,while No.7 production area(Shandong) had the lowest total triterpenoids content of 15.22 mg/g.[Conclusions]The Box-behnken response surface methodology is reliable for the extraction of total triterpenoids in Semen Trichosanthis,and the spectrophotometry is proper for determining the content of total triterpenoids in Semen Trichosanthis.There are large differences in the content of total triterpenoids in Semen Trichosanthis produced in different areas.展开更多
[Objectives]To study the immediate-release mechanism of dehydrotrametenolic acid and dehydroeburicoic acid in Poriae Cutis total triterpenoids tablets by liquid-solid compacts technique.[Methods] Taking dehydrotramete...[Objectives]To study the immediate-release mechanism of dehydrotrametenolic acid and dehydroeburicoic acid in Poriae Cutis total triterpenoids tablets by liquid-solid compacts technique.[Methods] Taking dehydrotrametenolic acid and dehydroeburicoic acid as indicators,differences in dissolution were compared between liquid-solid compressed tablets and crude drug of total triterpenoids in Poriae Cutis;crude drug,powder of liquid-solid compressed tablets and excipients of liquid-solid compressed tablets were characterized by differential scanning calorimetry( DSC).[Results]Liquid-solid compact technique could significantly improve dissolution rate of dehydrotrametenolic acid and dehydroeburicoic acid. The total dissolution rate of dehydrotrametenolic acid and dehydroeburicoic acid in Poriae Cutis total triterpenoids tablets was 92%,t50( time for 50% total dissolution rate) and t_D( time for 63. 2% total dissolution rate) were 11. 18 min and 22. 71 min; the total dissolution rate of dehydrotrametenolic acid and dehydroeburicoic acid in crude drug of total triterpenoids was 29%,and t50 and t_D were231. 06 min and 359. 23 min. DSC showed that there was no mutual interaction between excipients and total triterpenoids in Poriae Cutis; on the DSC curve for powder of liquid-solid compressed tablets,the absorption peak vanished completely,indicating that the drug exists in the amorphous form in the liquid-solid powder.[Conclusions] Liquid-solid compact technique can increase the dissolution rate of total triterpenoids in Poriae Cutis and allow rapid release of poorly water soluble drugs.展开更多
This study was to investigate the decoloration effects of activated clay, activated carbon, diatomite, Ca group bentonite, kaolin, activated aluminum oxide, magnesium oxide and attapulgite. Ultraviolet-visible spectro...This study was to investigate the decoloration effects of activated clay, activated carbon, diatomite, Ca group bentonite, kaolin, activated aluminum oxide, magnesium oxide and attapulgite. Ultraviolet-visible spectroscopywas adopted to de- tect the absorbanees of the extracts of Schisandra chinensis fruit and rattan stems, the contents of total triterpenoids in S. chinensis fruit and rattan stems were deter- mined, and the decoloration rate and the retention rate of total triterpenoids of S. chi- nensis fruit and rattan stems were calculated. The results indicated that, attapulgite exhibited the best decoloration effect on the extract of S. chinensis fruit, with a de- coloration rate up to 60.47%, activated carbon exhibited a better decoloration effect on the extract of S. chinensis rattan stems, with a decoloration rate up to 69.24%, and they had relatively higher retention rates of total triterpenoids. In the eight de- colorants, attapulgite showed the best decoloration effect on the extract of S. chi- nensis fruit, and activated carbon exhibited the best decoloration effect on the ex- tract of S. chinensisrattan stems.展开更多
OBJECTIVE Gastric ulcers affect people of all ages and half of the world's population,which is being considered as the new"plague of the 21st century".As is well known,gastric mucosa is known as the firs...OBJECTIVE Gastric ulcers affect people of all ages and half of the world's population,which is being considered as the new"plague of the 21st century".As is well known,gastric mucosa is known as the first guard to protect the stomach from ulcer injury,while the aetiology of gastric ulcer is relative to imbalances between gastric mucosal protective and aggressive factors.Therefore,reducing or eliminating the aggressive factors,returning to the balance of between mucosal protective and aggressive factors,and then restoring the normal functional of gastric mucosal barrier could be crucial for treating the gastric ulcer.The fruits of Chaenomeles speciosa(TCS),also known as"mugua",might be processed into edible and health care derived products,and used as a commonly used traditional medicine in China for thousands of years.In China folk,there is a saying that"apricot one benefit,pear two benefits,mgua hundred benefits",so it has a"hundred-benefit"fruit reputation.Tujia nationality inhabitants in Southwestern China should have rheumatic diseases and peptic ulcers for living in the damp environments and bingeing on spicy and pungent foods.For the exis⁃tence of the fruit derived products of Chaenomeles speciosa as their complementary foods or snacks,the habit makes them rarely suffer from the two kinds of diseases.Enlightened by these,we had investigated the structure-activity rela⁃tionships,screened out CSTT with gastroprotective activity.Our previous studies demonstrated that TCS owned effec⁃tively therapeutic effects on gastric ulcer patients and animals,and further confirmed that TFF1 and apoptotic pathway were closely interrelated with its exerting gastroprotection.However,its underlying molecular mechanisms involved have not been fully elucidated.The current study was to further investigate its protective effect on indomethacin(IND)-damaged RGM-1 cells and rats and its underlying mechanisms through modulating TFF1-mediated EGF/EGFR and apoptotic pathways.METHODS The gastroprotection of TCS was evaluated with IND-induced gastric lesions model in RGM-1 cells and rats.In vitro,the proliferation,migration,mitochondrial viability and apoptosis were assessed,In vivo,ulcer index,ulcer inhibition rate,gastric juice acidity,gastric wall mucus(GWM),histopathology of gastric mucosa were detected.The gastroprotective effects of TCS through the TFF1-mediated EGFR/EGFR and apoptotic pathways were presented and measured by qRT-PCR and Western blotting assays.RESULTS TCS had gastroprotective function,which was related to the amelioration in promoting IND-damaged RGM-1 cell proliferation and migration,hoisting gastric juice acidity and GWM,improving ulcer index and ulcer inhibition rate,attenuating the hemorrhage,edema,epithelial cell loss and inflammatory cell infiltration of gastric mucosa,upregulating proliferation cell nuclear antigen,Bcl-2,Bcl-xl mRNA and TFF1,EGF,p-EGFR,p-Src,pro-caspase-3,pro-caspase-9 protein expressions,mitochondrial viability,mitochondrial cytochrome C concentration and p-EGFR/EGFR,p-Src/Src,Bcl-2/Bax,Bcl-xl/Bad ratioes,downregulating Bax,Bad,Apaf-1 mRNA and cleaved-caspase-3,cleaved-caspase-9,cleaved-PARP-1 protein expressions,cytosol cytochrome C concentration.CONCLUSION TCS′s gastroprotective effect was closely connected with boosting TFF1 expression,acti⁃vating TFF1-mediated EGF/EGFR pathway,thus restraining mitochondrial-dependent apoptosis,which provided new insights into interpreting its underlying mechanism and promised to act as a candidate drug to treat gastric mucosal injury.展开更多
基金The project supported by National Natural and Science Foundation of China(81341141)Yichang Qingqianliu Biotechnology Co.,Ltd.(SDHZ201602)Science and Technology Bureau of Yichang city(A15301-25)
文摘OBJECTIVE To explore the protective effects of total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja on STZ-stimulated INS-1 cells through regulating of autophagy and apoptosis.METHODS INS-1cells were cultured in media containing 3n M STZ and different doses of total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja.The proliferation of cells was examined by MTT assay,ROS content were detected by fluorescence enzyme label.The levels of superoxide dismutase(SOD),glutathione peroxidase(GSH-Px),hydrogen peroxidase(CAT),malondialdehyde(MDA)were also measured by colorimetry.The activities of caspase-3,9 were also observed by Caspase colorimetric assay kit in each group.The expressions of Bcl-2 m RNA and Bax m RNA were detected by Real time PCR,protein expression of LC3-Ⅱand PARP were detected by Western blotting.RESULTS Compared with the control group,total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja could promote the proliferation of INS-1 cells no matter with STZ or not when its concentration lower than 25μg·m L^(-1);but when its concentration higher than 100μg·m L^(-1)(use individually)or 50μg·m L^(-1)(combined use),total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja might significantly inhibite the growth of the cells whether STZ existed or not.Total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja(6.25,12.5,25μg·m L^(-1))might inhibit INS-1cell apoptosis,decrease intra-cellular ROS contents,improve the s upernatant liquid SOD,GSH-PX,CAT activities,decrease MDA level,promote INS-1 cell secreting insulin,decrease the protein expressions of autophagy protein LC3Ⅱand apoptosis regulating protein cleaved PARP protein,up-regulate the anti-apoptotic protein Bcl-2 m RNA expression,down-regulate the pro-apoptotic protein Bax m RNA expression and Bcl-2and Bax,reduce the activity of caspase-9 and caspase-3(P<0.05 or P<0.01).CONCLUSION Total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja has good protective effect on STZ-stimulated INS-1cells.It can inhibit STZ injured INS-1 cells to overproduce ROS production,enhance endogenous antioxidant enzymes(GSH-Px,SOD,CAT activities),reduce the expression of autophagy protein LC3Ⅱand apoptosisregulating protein cleaved PARP,up-reglute the antiapoptosis protein Bcl-2 expression,down-regulate the pro-apoptotic protein Bax expression,decrease the caspase-9 and caspase-3 activities,and improve the INS-1cell survival rate,and then play a protective effect on damaged INS-1 cells.
基金Supported by Project of Department of Education of Liaoning Province(L2017lkyfwdf-05)Natural Science Foundation Project of Department of Education of Liaoning Province(20180551223&2016003003)
文摘[Objectives] To optimize the extraction process and determine the total triterpenoids from Semen Trichosanthis.[Methods]The Box-behnken response surface methodology was applied to optimize the extraction conditions of total triterpenoids in Semen Trichosanthis.And the spectrophotometry was used to determine the content of total triterpenoids in Semen Trichosanthis.[Results] The optimal extraction conditions were solid to liquid ratio of 40∶ 1,ultrasonic time of 20 min,and ultrasonic power of 100 W.Under these conditions,the content of total triterpenoids in Semen Trichosanthis was significantly different among the 10 production areas,among which the No.9 production area(Anhui 1) had the highest total triterpenoids content of 45.71 mg/g,while No.7 production area(Shandong) had the lowest total triterpenoids content of 15.22 mg/g.[Conclusions]The Box-behnken response surface methodology is reliable for the extraction of total triterpenoids in Semen Trichosanthis,and the spectrophotometry is proper for determining the content of total triterpenoids in Semen Trichosanthis.There are large differences in the content of total triterpenoids in Semen Trichosanthis produced in different areas.
基金Supported by Project of National Natural Science Foundation of Shandong Province(ZR2015PH015)
文摘[Objectives]To study the immediate-release mechanism of dehydrotrametenolic acid and dehydroeburicoic acid in Poriae Cutis total triterpenoids tablets by liquid-solid compacts technique.[Methods] Taking dehydrotrametenolic acid and dehydroeburicoic acid as indicators,differences in dissolution were compared between liquid-solid compressed tablets and crude drug of total triterpenoids in Poriae Cutis;crude drug,powder of liquid-solid compressed tablets and excipients of liquid-solid compressed tablets were characterized by differential scanning calorimetry( DSC).[Results]Liquid-solid compact technique could significantly improve dissolution rate of dehydrotrametenolic acid and dehydroeburicoic acid. The total dissolution rate of dehydrotrametenolic acid and dehydroeburicoic acid in Poriae Cutis total triterpenoids tablets was 92%,t50( time for 50% total dissolution rate) and t_D( time for 63. 2% total dissolution rate) were 11. 18 min and 22. 71 min; the total dissolution rate of dehydrotrametenolic acid and dehydroeburicoic acid in crude drug of total triterpenoids was 29%,and t50 and t_D were231. 06 min and 359. 23 min. DSC showed that there was no mutual interaction between excipients and total triterpenoids in Poriae Cutis; on the DSC curve for powder of liquid-solid compressed tablets,the absorption peak vanished completely,indicating that the drug exists in the amorphous form in the liquid-solid powder.[Conclusions] Liquid-solid compact technique can increase the dissolution rate of total triterpenoids in Poriae Cutis and allow rapid release of poorly water soluble drugs.
基金Supported by Key Science and Technology Research and Development Program of Jilin Province(20140204068YY,20140204062YY)Special Fund for Pharmaceutical Industry Development of Jilin Province(YYZW201246)~~
文摘This study was to investigate the decoloration effects of activated clay, activated carbon, diatomite, Ca group bentonite, kaolin, activated aluminum oxide, magnesium oxide and attapulgite. Ultraviolet-visible spectroscopywas adopted to de- tect the absorbanees of the extracts of Schisandra chinensis fruit and rattan stems, the contents of total triterpenoids in S. chinensis fruit and rattan stems were deter- mined, and the decoloration rate and the retention rate of total triterpenoids of S. chi- nensis fruit and rattan stems were calculated. The results indicated that, attapulgite exhibited the best decoloration effect on the extract of S. chinensis fruit, with a de- coloration rate up to 60.47%, activated carbon exhibited a better decoloration effect on the extract of S. chinensis rattan stems, with a decoloration rate up to 69.24%, and they had relatively higher retention rates of total triterpenoids. In the eight de- colorants, attapulgite showed the best decoloration effect on the extract of S. chi- nensis fruit, and activated carbon exhibited the best decoloration effect on the ex- tract of S. chinensisrattan stems.
基金Research Foundation of Hubei Biological Enzyme Engineering Technology Research Center(JS2018-06)
文摘OBJECTIVE Gastric ulcers affect people of all ages and half of the world's population,which is being considered as the new"plague of the 21st century".As is well known,gastric mucosa is known as the first guard to protect the stomach from ulcer injury,while the aetiology of gastric ulcer is relative to imbalances between gastric mucosal protective and aggressive factors.Therefore,reducing or eliminating the aggressive factors,returning to the balance of between mucosal protective and aggressive factors,and then restoring the normal functional of gastric mucosal barrier could be crucial for treating the gastric ulcer.The fruits of Chaenomeles speciosa(TCS),also known as"mugua",might be processed into edible and health care derived products,and used as a commonly used traditional medicine in China for thousands of years.In China folk,there is a saying that"apricot one benefit,pear two benefits,mgua hundred benefits",so it has a"hundred-benefit"fruit reputation.Tujia nationality inhabitants in Southwestern China should have rheumatic diseases and peptic ulcers for living in the damp environments and bingeing on spicy and pungent foods.For the exis⁃tence of the fruit derived products of Chaenomeles speciosa as their complementary foods or snacks,the habit makes them rarely suffer from the two kinds of diseases.Enlightened by these,we had investigated the structure-activity rela⁃tionships,screened out CSTT with gastroprotective activity.Our previous studies demonstrated that TCS owned effec⁃tively therapeutic effects on gastric ulcer patients and animals,and further confirmed that TFF1 and apoptotic pathway were closely interrelated with its exerting gastroprotection.However,its underlying molecular mechanisms involved have not been fully elucidated.The current study was to further investigate its protective effect on indomethacin(IND)-damaged RGM-1 cells and rats and its underlying mechanisms through modulating TFF1-mediated EGF/EGFR and apoptotic pathways.METHODS The gastroprotection of TCS was evaluated with IND-induced gastric lesions model in RGM-1 cells and rats.In vitro,the proliferation,migration,mitochondrial viability and apoptosis were assessed,In vivo,ulcer index,ulcer inhibition rate,gastric juice acidity,gastric wall mucus(GWM),histopathology of gastric mucosa were detected.The gastroprotective effects of TCS through the TFF1-mediated EGFR/EGFR and apoptotic pathways were presented and measured by qRT-PCR and Western blotting assays.RESULTS TCS had gastroprotective function,which was related to the amelioration in promoting IND-damaged RGM-1 cell proliferation and migration,hoisting gastric juice acidity and GWM,improving ulcer index and ulcer inhibition rate,attenuating the hemorrhage,edema,epithelial cell loss and inflammatory cell infiltration of gastric mucosa,upregulating proliferation cell nuclear antigen,Bcl-2,Bcl-xl mRNA and TFF1,EGF,p-EGFR,p-Src,pro-caspase-3,pro-caspase-9 protein expressions,mitochondrial viability,mitochondrial cytochrome C concentration and p-EGFR/EGFR,p-Src/Src,Bcl-2/Bax,Bcl-xl/Bad ratioes,downregulating Bax,Bad,Apaf-1 mRNA and cleaved-caspase-3,cleaved-caspase-9,cleaved-PARP-1 protein expressions,cytosol cytochrome C concentration.CONCLUSION TCS′s gastroprotective effect was closely connected with boosting TFF1 expression,acti⁃vating TFF1-mediated EGF/EGFR pathway,thus restraining mitochondrial-dependent apoptosis,which provided new insights into interpreting its underlying mechanism and promised to act as a candidate drug to treat gastric mucosal injury.
