Diabetes is a serious, long-term (or chronic) disease that occurs when a person’s blood sugar levels are high because their body cannot produce enough insulin, or does not produce enough insulin or that it cannot eff...Diabetes is a serious, long-term (or chronic) disease that occurs when a person’s blood sugar levels are high because their body cannot produce enough insulin, or does not produce enough insulin or that it cannot effectively use the insulin it produces. According to the literature, this disease has several causes, but certain types of diabetes such as type 2 diabetes are most closely linked to a metabolic disorder due to abdominal obesity. Thus, the number of individuals with type 2 diabetes is increasing. It is with this in mind that we work to improve human health. The aim of this study is to design new derivatives of 1,3,4-thiadiazole with improved antidiabetic activity by the mathematical model of multiple linear regression (MLR) established previously. The analysis of the effect on the substituents influencing the antidiabetic activity, fourteen (14) new molecules coded CDTH were generated and presenting values of the potential of inhibitory concentration higher than that of the base compound (pIC50 = 2.526). But thirteen (13) of these new compounds belong to the domain of applicability of the MLR model established previously. In addition, the thermodynamic quantities of formation formed at 298K have been calculated. Lipinski’s rule and pharmacokinetic properties proved that five (5) (TH4, TH9, TH10, TH13 and TH14) new molecules can be used as diabetes medicine.展开更多
In this study,we presented the isolation and characterization of eight novel seco-guaianolide sesquiterpenoids(1-8)and two known guaianolide derivatives(9 and 10),from the aerial part of Achillea alpina L..Compounds 1...In this study,we presented the isolation and characterization of eight novel seco-guaianolide sesquiterpenoids(1-8)and two known guaianolide derivatives(9 and 10),from the aerial part of Achillea alpina L..Compounds 1-3 were identified as guaianolides bearing an oxygen insertion at the 2,3 position,while compounds 4-8 belonged to a group of special 3-nor guaianolide sesquiterpenoids.The structural elucidation of 1-8,including their absolute configurations,were accomplished by a combination of spectroscopic data analysis and quantum electronic circular dichroism(ECD)calculations.To evaluate the potential antidiabetic activity of compounds 1-10,we investigated their effects on glucose consumption in palmitic acid(PA)-mediated HepG2-insulin resistance(IR)cells.Among the tested compounds,compound 7 demonstrated the most pronounced ability to reverse IR.Moreover,a mechanistic investigation revealed that compound 7 exerted its antidiabetic effect by reducing the production of the pro-inflammatory cytokine IL-1β,which was achieved through the suppression of the NLRP3 pathway.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
The purpose of this study was to investigate the physicochemical properties and bioactivities of rice beans(Vigna umbellata)fermented by Bacillus amyloliquefaciens.The fermentation conditions were optimized on the bas...The purpose of this study was to investigate the physicochemical properties and bioactivities of rice beans(Vigna umbellata)fermented by Bacillus amyloliquefaciens.The fermentation conditions were optimized on the basis of the fibrinolytic activity.Under the optimal fermentation conditions,the fibrinolytic activity reached a maximum of 78.0 FU·g^(-1)(4890 IU·g^(-1),fibrin plate method,FU:fibrin degradation unit).The contents of peptides(which increased from 2.1 to 10.9 g per 100 g),total phenolics(from 116.7 to 388.5 mg gallic acid per 100 g),total flavonoids(from 235.5 to 354.3 mg rutin per 100 g),and anthocyanin(from 20.1 to 47.1 mg per 100 g),as well as the superoxide dismutase activity(from 55.3 to 263.6 U·g^(-1))in rice beans were significantly increased after fermentation.The 2,2-diphenyl-1-picrylhydrazyl(DPPH)and 2,2-azinobis(3-ethylbenzothiazoline-6-sulphonic acid)diammonium salt(ABTS)free radical scavenging activities and ferric reducing antioxidant power(FRAP)of fermented rice beans were 1.9–4.8 times higher than those of unfermented rice beans.Moreover,fermentation induced an increase in the dipeptidyl peptidase IV(DPP-IV)inhibition,a-glucosidase inhibition,and anticoagulant activities of rice beans.Rice beans fermented by Bacillus amyloliquefaciens may serve as a functional food with potential benefits for the prevention of thrombotic diseases.展开更多
Objective:To evaluate the effect of aqueous leaf extract of Cistus ladaniferus(C.ladaniferus) on glycemic and lipidemic status in diabetic rats.Methods:Overnight fasted rats were injected intraperitoneally with strept...Objective:To evaluate the effect of aqueous leaf extract of Cistus ladaniferus(C.ladaniferus) on glycemic and lipidemic status in diabetic rats.Methods:Overnight fasted rats were injected intraperitoneally with streptozotocin(45 mg/kg) to induce experimental diabetes.The aqueous extract of the leaves of C.ladaniferus was administered orally at the dose of 500 mg/kg body weight to diabetic rats for a period of 28 days.Hypoglycemic effect,body weight,oral glucose tolerance,change in lipid parameters,urea,creatinine,aspartate aminotransferase and alanine aminotransferase levels of diabetic rats treated with aqueous extract were evaluated in experimental animals.Results:Administration of 500 mg/kg of C.ladaniferus extract to diabetic rats for 28 days resulted in a significant reduction in the levels of blood glucose,alanine aminotransferase,aspartate aminotransferase,urea and creatinine.Furthermore,the extract of C.ladaniferus improved glucose tolerance in diabetic rats,and its antidiabetic effect was similar to the one obtained with glibenclamide.The hypolipidemic effect was demonstrated by an important decrease in plasma total cholesterol,triglycerides and low density lipoprotein-cholesterol levels.Conclusions:It is concluded that C.ladaniferus leaf extract showed an antidiabetic activity in experimental diabetes which was similar to the one obtained with glibenclamide.展开更多
Objective:To prepare naringenin herbosome and evaluate its antidiabetic activity.Methods:Herbosomes were prepared by the solvent evaporation method.In vitro parameters like particle size,polydispersity index,zeta pote...Objective:To prepare naringenin herbosome and evaluate its antidiabetic activity.Methods:Herbosomes were prepared by the solvent evaporation method.In vitro parameters like particle size,polydispersity index,zeta potential,and entrapment efficiency were estimated and in vitro diffusion study was performed.The in vivo studies were also performed in streptozotocin-induced diabetic male Sprague Dawley rats to evaluate blood glucose,total cholesterol,triglyceride,blood urea nitrogen,total protein,albumin level,aspartate aminotransferase,and alanine aminotransferase levels.Results:The optimized herbosome batch showed a particle size of 564.4 nm,a polydispersity index of 0.412,and zeta potential of−39.3 mV.The percentage entrapment of this formulation was 84.04%,with complete drug release within 8 h.Treatment of diabetic rats with naringenin herbosomes for 28 d significantly reduced the elevated level of plasma glucose as compared to plain naringenin.In biochemical parameters,the treatment showed a significant decrease in total cholesterol,triglyceride,and blood urea nitrogen;while elevated levels of aspartate aminotransferase and alanine aminotransferase were returned to normal.Pure naringenin and herbosome formulation at high dose increased the total protein whereas albumin level significantly increased in naringenin herbosomes at the highest dose but not in the pure naringenin treatment group.Conclusions:Naringenin herbosomes could improve the metabolic profile of diabetic rats,indicating enhanced antidiabetic activity of herbosome formulation.展开更多
The current study used RP-HPLC to compare phytochemicals and estimate the bioactive constituents found in Stevia rebaudiana Bert.(SRB)leaves collected from two different geographical sources.SRB leaves were collected ...The current study used RP-HPLC to compare phytochemicals and estimate the bioactive constituents found in Stevia rebaudiana Bert.(SRB)leaves collected from two different geographical sources.SRB leaves were collected from Bangalore,Karnataka,India,and Reduit,Mauritius.Extracts were prepared using ethanol and aqueous solvents.Proximate analysis was used to evaluate moisture content,ash values,crude fibers,and extractive values.Following that,preliminary phytochemical screening was done on both ethanol leaves extracts,and subsequently total flavonoid content was determined.In addition,TLC chromatograms and RP-HPLC studies were performed on both plant extracts to determine the presence of flavonoid components in both leaves extracts,followed by in vitro anti-diabetic activity was performed with alpha amylase and alpha glucosidase enzymes against Acarbose as standard.Results revealed that both the extracts from two different geographical sources varied significantly with the yield,content of chemicals,and presence of quercetin(flavonoid)content when estimated through the RP-HPLC standardized method.Glycosides,flavonoids,proteins,steroids,saponins,terpenoids,and phenols were found in various concentrations during phytochemical screening.Among both zones,the ethanol leaves extract of SRB taken from Mauritius had a greater content of phytochemicals and a higher yield than other extracts due to the soil nature.The Mauritius sample had greater total flavonoid levels as well as more quercetin(0.92±0.011)than the other extracts.Following that,ethanol extract inhibited enzymes(alpha amylase,alpha glucosidases)more than aqueous extract,and this inhibition was dose dependent.Among them,the Mauritius ethanol sample showed higher anti-diabetic efficacy than the Indian sample,but this difference was not significant.Overall,SRB ethanol leaves extracts outperformed other leaves extracts in terms of yield,phytoconstituents,and total flavonoids.Overall,both SRB samples had high quercetin levels and possessed anti-diabetic potential,but they were greater in the Mauritius sample,demonstrating that plant traits are influenced by geographic location.展开更多
This is the first report illustrating the extraction of total phenolic compounds(TPC)using the ultrasound-assisted aqueous extraction(USAE)technique from waste Syzygium cumini leaves(WSCL).A kinetic study indicated th...This is the first report illustrating the extraction of total phenolic compounds(TPC)using the ultrasound-assisted aqueous extraction(USAE)technique from waste Syzygium cumini leaves(WSCL).A kinetic study indicated that Peleg’s model was appropriately fitted to the experimental data when the effect of different parameters was checked on extraction with respect to time.Extraction yields of total phenolic contents(TPC)and total flavonoid contents(TFC)were 78.38 mg GAE/g,and 10.15 mg CE/g,respectively,at optimized parameters of 1:25 WSCL:water,35℃ temperature,134 W power,50%duty cycle and in 9 min of sonication time.Cumulative yields of TPC and TFC obtained by 5 sequential stirred batch extraction were 79.36 mg GAE/g and 10 mg CE/g,respectively.The cost and energy requirement of the USAE process was around 3000 times less than that of the Soxhlet technique.SEM images showed the changes in the morphology of the WSCL surface area before and after ultrasonic extraction.FTIR analysis showed the presence of O-H,N-H,C-H,C=C,and halogenated functional groups.The obtained WSCL extract showed antioxidant potential with an IC_(50) value of 15.64μg/mL.IC_(50) values of extract forα-amylase andα-glucosidase inhibitions were 8.3 and 6.64μg/mL.Antiproliferation activity against breast,cervical,and lung cancer showed the potential with GI50 values 252.8,112.5,and 97.8μg/mL,respectively.Aqueous extract of Syzygium cumini leaves can be used to treat oxidative stress,diabetes,and cancer.展开更多
Traditional system of medicine consists of large number of plants with various medicinal and pharmacological importances and hence represents a priceless tank of new bioactive molecules.Coccinia indica belongs to the ...Traditional system of medicine consists of large number of plants with various medicinal and pharmacological importances and hence represents a priceless tank of new bioactive molecules.Coccinia indica belongs to the family Cucurbitaceae.It is a rapidly growing,perennial climber or trailing vine.Traditionally different parts of this plant namely the roots,leaves and fruits are used in folklore medicine for several purposes like jaundice,diabetes,wound healing,ulcers,stomach ache,skin disease,fever,asthma,cough.The leaf and its constituents have been reported to possess hypoglycaemic,hypolipidemic and antioxidant properties.This review provides adequate information to develop suitable therapeutics out of these plant parts.展开更多
Rising consumer concerns with synthetic drugs to treat non-communicable diseases(NCDs)have promoted a shift towards using natural biological active constituents that offer similar health benefits.Hairless canary seed(...Rising consumer concerns with synthetic drugs to treat non-communicable diseases(NCDs)have promoted a shift towards using natural biological active constituents that offer similar health benefits.Hairless canary seed(Phalaris canariensis L)is an emerging crop traditionally used in Mexico to treat NCDs.Peptides liberated during simulated digestion of canary seed protein are believed to be responsible for their biological activity;however,no studies have shown the effect of controlled protein hydrolysis using commercial proteases on canary seed protein’s biological activity.Therefore,this study aimed to explore the in vitro antihypertensive,antidiabetic,and anti-obesity activity of canary seed peptides derived from proteolysis with Alcalase®.Protein fractions were primarily composed of prolamins(54.07±1.8%),glutelins(32.19±3.18%),globulins(5.97±0.52%)and albumins(5.97±0.52%).The<3 kDa and 3–10 kDa peptide fractions showed the highest inhibition capacity(p<0.05)towards angiotensin-converting enzyme(IC50=0.028–0.032 mg/mL)lipase(IC50=2.15–2.27 mg/mL),α-glucosidase(IC50=0.82–1.15 mg/mL),and dipeptidyl-peptidase-IV(IC50=1.27–1.60 mg/mL).Additionally,these peptide fractions showed high antioxidant activity against DPPH(134.22–150.66μmol TE/mg)and ABTS(520.92–813.33μmol TE/mg).These results provide an insight into the potential development of functional foods using commercial enzymatic hydrolysis of canary seed proteins for treating hypertension,type-2 diabetes,and obesity.展开更多
The present study was undertaken to evaluate the influence of the methanolic fruit extract of Momordica cymbalaria(MFMC) on PPARγ(Peroxisome Proliferator Activated Receptor gamma) and GLUT-4(Glucose transporter-4) wi...The present study was undertaken to evaluate the influence of the methanolic fruit extract of Momordica cymbalaria(MFMC) on PPARγ(Peroxisome Proliferator Activated Receptor gamma) and GLUT-4(Glucose transporter-4) with respect to glucose transport. Various concentrations of MFMC ranging from 62.5 to 500 μg·mL-1 were evaluated for glucose uptake activity in vitro using L6 myotubes, rosiglitazone was used as a reference standard. The MFMC showed significant and dose-dependent increase in glucose uptake at the tested concentrations, further, the glucose uptake activity of MFMC(500 μg·mL-1) was comparable with rosigilitazone. Furthermore, MFMC has shown up-regulation of GLUT-4 and PPARγ gene expressions in L6 myotubes. In addition, the MFMC when incubated along with cycloheximide(CHX), which is a protein synthesis inhibitor, has shown complete blockade of glucose uptake. This indicates that new protein synthesis is required for increased GLUT-4 translocation. In conclusion, these findings suggest that MFMC is enhancing the glucose uptake significantly and dose dependently through the enhanced expression of PPARγ and GLUT-4 in vitro.展开更多
Objective:Recently,much attention has been paid to natural product-derived compounds for antidiabetic drug discovery.More recent studies are being focused on clarifying the bioactivity of plants and derived products.T...Objective:Recently,much attention has been paid to natural product-derived compounds for antidiabetic drug discovery.More recent studies are being focused on clarifying the bioactivity of plants and derived products.The aim of the present study was to investigate the anti-oxidant and antidiabetic activities of Clerodendrum inerme leaf extract(CILE)in streptozotocin-induced diabetic mice.Methods:C.inerme leaves were analyzed for preliminary phytochemical properties and the content of total phenolic and flavonoid were determined.In vitro anti-oxidant activity was measured using DPPH assay.Streptozotocin-induced diabetic model in mice was applied for in vivo study by the effect of CILE at two dose levels(343 and 686 mg/kg b.w.).Results:The results showed that C.inerme leaves contained the major constituents of flavonoids,alkaloids,tannins,triterpenes,and saponins.CILE exhibited the total polyphenol and flavonoid content with 120.458 mg gallic acid equivalent/g dry weight and 4.494 mg hispidulin equivalent/g dry weight,respectively.The anti-oxidant activity of CILE was expressed with IC50=25.28μg/m L.CILE at the doses of343 mg/kg and 686 mg/kg after 7 d administration exerted a decrease in plasma glucose,protected the liver,kidneys against oxidation stress via increasing glutathione content in the liver,and reduced malondialdehyde content in the liver and kidneys.Pancreatic histological analysis in diabetic mice treated with CILE also showed the pancreaticβ-cells regeneration via increasing the size and number of pancreatic islets.Conclusion:These findings suggested that C.inerme leaves had potent antidiabetic and anti-oxidant activities.The results provide reliable scientific base,which is the premise for further research and development of CILE as supplements.展开更多
Objective:Wild musk melon(Cucumis melo var.agrestis,CMA)is one of the edible plants form Tamil Nadu.Traditionally,this plant was used as diabetic diet(leaves of CMA with Momordica charantia leaves),but there is no sci...Objective:Wild musk melon(Cucumis melo var.agrestis,CMA)is one of the edible plants form Tamil Nadu.Traditionally,this plant was used as diabetic diet(leaves of CMA with Momordica charantia leaves),but there is no scientific report on antidiabetic action of this plant material.Hence,the current research work was designed to evaluate the antihyperglycemic and antihyperlipidemic effect of hydroalcoholic extract of CMA leaves(HALEC)in streptozotocin(STZ)-nicotinamide(NIC)-induced diabetic rats.Methods:Diabetes was induced by administration of STZ(60 mg/kg,i.p.)after 15 min of NIC(120 mg/kg i.p.)administration.The diabetic rats were treated with HALEC(300 and 600 mg/kg,p.o.,respectively)for 21 d.Results:After the management with HALEC,blood glucose,HbA1c levels,total cholesterol,LDL cholesterol,triglycerides levels,glycogen phosphorylase and glucose-6-phosphatase levels were significantly diminished in diabetic rats.However,haemoglobin level,HDL cholesterol,liver glycogen,total protein,hexokinase,glucose-6-phosphate dehydrogenase levels were significantly increased in HALEC treated diabetic rats.The histopathological studies of the pancreas in HALEC-treated diabetic rats showed almost normal appearance.L6 cell line study revealed the increased glucose uptake activity of HALEC.High performance thin layer chromatography(HPTLC)analysis confirms the presence of active principles such as rutin,gallic acid and quercetin in HALEC.Conclusion:The results indicated that HALEC possess significant antihyperglycemic and antihyperlipidemic activity in STZ-NIC-induced typeⅡdiabetic rats with protective effect.This research work will be useful for the isolation of active principles and development of herbal formulation in phytopharmaceuticals.展开更多
文摘Diabetes is a serious, long-term (or chronic) disease that occurs when a person’s blood sugar levels are high because their body cannot produce enough insulin, or does not produce enough insulin or that it cannot effectively use the insulin it produces. According to the literature, this disease has several causes, but certain types of diabetes such as type 2 diabetes are most closely linked to a metabolic disorder due to abdominal obesity. Thus, the number of individuals with type 2 diabetes is increasing. It is with this in mind that we work to improve human health. The aim of this study is to design new derivatives of 1,3,4-thiadiazole with improved antidiabetic activity by the mathematical model of multiple linear regression (MLR) established previously. The analysis of the effect on the substituents influencing the antidiabetic activity, fourteen (14) new molecules coded CDTH were generated and presenting values of the potential of inhibitory concentration higher than that of the base compound (pIC50 = 2.526). But thirteen (13) of these new compounds belong to the domain of applicability of the MLR model established previously. In addition, the thermodynamic quantities of formation formed at 298K have been calculated. Lipinski’s rule and pharmacokinetic properties proved that five (5) (TH4, TH9, TH10, TH13 and TH14) new molecules can be used as diabetes medicine.
基金supported by the National Natural Science Foundation of China(No.82003606)the Scientific and Technological Key Project in Henan Province(No.212102311093)the Scientific Research Nursery Project(No.MP2020-29).
文摘In this study,we presented the isolation and characterization of eight novel seco-guaianolide sesquiterpenoids(1-8)and two known guaianolide derivatives(9 and 10),from the aerial part of Achillea alpina L..Compounds 1-3 were identified as guaianolides bearing an oxygen insertion at the 2,3 position,while compounds 4-8 belonged to a group of special 3-nor guaianolide sesquiterpenoids.The structural elucidation of 1-8,including their absolute configurations,were accomplished by a combination of spectroscopic data analysis and quantum electronic circular dichroism(ECD)calculations.To evaluate the potential antidiabetic activity of compounds 1-10,we investigated their effects on glucose consumption in palmitic acid(PA)-mediated HepG2-insulin resistance(IR)cells.Among the tested compounds,compound 7 demonstrated the most pronounced ability to reverse IR.Moreover,a mechanistic investigation revealed that compound 7 exerted its antidiabetic effect by reducing the production of the pro-inflammatory cytokine IL-1β,which was achieved through the suppression of the NLRP3 pathway.
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 work was supported by The National Key Research and Development Program of China(2018YFD0400404).
文摘The purpose of this study was to investigate the physicochemical properties and bioactivities of rice beans(Vigna umbellata)fermented by Bacillus amyloliquefaciens.The fermentation conditions were optimized on the basis of the fibrinolytic activity.Under the optimal fermentation conditions,the fibrinolytic activity reached a maximum of 78.0 FU·g^(-1)(4890 IU·g^(-1),fibrin plate method,FU:fibrin degradation unit).The contents of peptides(which increased from 2.1 to 10.9 g per 100 g),total phenolics(from 116.7 to 388.5 mg gallic acid per 100 g),total flavonoids(from 235.5 to 354.3 mg rutin per 100 g),and anthocyanin(from 20.1 to 47.1 mg per 100 g),as well as the superoxide dismutase activity(from 55.3 to 263.6 U·g^(-1))in rice beans were significantly increased after fermentation.The 2,2-diphenyl-1-picrylhydrazyl(DPPH)and 2,2-azinobis(3-ethylbenzothiazoline-6-sulphonic acid)diammonium salt(ABTS)free radical scavenging activities and ferric reducing antioxidant power(FRAP)of fermented rice beans were 1.9–4.8 times higher than those of unfermented rice beans.Moreover,fermentation induced an increase in the dipeptidyl peptidase IV(DPP-IV)inhibition,a-glucosidase inhibition,and anticoagulant activities of rice beans.Rice beans fermented by Bacillus amyloliquefaciens may serve as a functional food with potential benefits for the prevention of thrombotic diseases.
基金Supported by University of Sidi Mohamed Ben Abdellah(USMBA)grant from the National Center for Scientific and Technical Research of Morocco(CNRST)to Mohamed El Kabbaoui(Fellowship number N°:021USMBA2014)
文摘Objective:To evaluate the effect of aqueous leaf extract of Cistus ladaniferus(C.ladaniferus) on glycemic and lipidemic status in diabetic rats.Methods:Overnight fasted rats were injected intraperitoneally with streptozotocin(45 mg/kg) to induce experimental diabetes.The aqueous extract of the leaves of C.ladaniferus was administered orally at the dose of 500 mg/kg body weight to diabetic rats for a period of 28 days.Hypoglycemic effect,body weight,oral glucose tolerance,change in lipid parameters,urea,creatinine,aspartate aminotransferase and alanine aminotransferase levels of diabetic rats treated with aqueous extract were evaluated in experimental animals.Results:Administration of 500 mg/kg of C.ladaniferus extract to diabetic rats for 28 days resulted in a significant reduction in the levels of blood glucose,alanine aminotransferase,aspartate aminotransferase,urea and creatinine.Furthermore,the extract of C.ladaniferus improved glucose tolerance in diabetic rats,and its antidiabetic effect was similar to the one obtained with glibenclamide.The hypolipidemic effect was demonstrated by an important decrease in plasma total cholesterol,triglycerides and low density lipoprotein-cholesterol levels.Conclusions:It is concluded that C.ladaniferus leaf extract showed an antidiabetic activity in experimental diabetes which was similar to the one obtained with glibenclamide.
文摘Objective:To prepare naringenin herbosome and evaluate its antidiabetic activity.Methods:Herbosomes were prepared by the solvent evaporation method.In vitro parameters like particle size,polydispersity index,zeta potential,and entrapment efficiency were estimated and in vitro diffusion study was performed.The in vivo studies were also performed in streptozotocin-induced diabetic male Sprague Dawley rats to evaluate blood glucose,total cholesterol,triglyceride,blood urea nitrogen,total protein,albumin level,aspartate aminotransferase,and alanine aminotransferase levels.Results:The optimized herbosome batch showed a particle size of 564.4 nm,a polydispersity index of 0.412,and zeta potential of−39.3 mV.The percentage entrapment of this formulation was 84.04%,with complete drug release within 8 h.Treatment of diabetic rats with naringenin herbosomes for 28 d significantly reduced the elevated level of plasma glucose as compared to plain naringenin.In biochemical parameters,the treatment showed a significant decrease in total cholesterol,triglyceride,and blood urea nitrogen;while elevated levels of aspartate aminotransferase and alanine aminotransferase were returned to normal.Pure naringenin and herbosome formulation at high dose increased the total protein whereas albumin level significantly increased in naringenin herbosomes at the highest dose but not in the pure naringenin treatment group.Conclusions:Naringenin herbosomes could improve the metabolic profile of diabetic rats,indicating enhanced antidiabetic activity of herbosome formulation.
基金Walaa F.Alsanie would like to acknowledge Taif University for support No.TURSP(2020/53)Syed Mohammed Basheeruddin Asdaq,would like to thank AlMaarefa University,Riyadh,Saudi Arabia for extending support(TUMA-2021-1)to do this research.
文摘The current study used RP-HPLC to compare phytochemicals and estimate the bioactive constituents found in Stevia rebaudiana Bert.(SRB)leaves collected from two different geographical sources.SRB leaves were collected from Bangalore,Karnataka,India,and Reduit,Mauritius.Extracts were prepared using ethanol and aqueous solvents.Proximate analysis was used to evaluate moisture content,ash values,crude fibers,and extractive values.Following that,preliminary phytochemical screening was done on both ethanol leaves extracts,and subsequently total flavonoid content was determined.In addition,TLC chromatograms and RP-HPLC studies were performed on both plant extracts to determine the presence of flavonoid components in both leaves extracts,followed by in vitro anti-diabetic activity was performed with alpha amylase and alpha glucosidase enzymes against Acarbose as standard.Results revealed that both the extracts from two different geographical sources varied significantly with the yield,content of chemicals,and presence of quercetin(flavonoid)content when estimated through the RP-HPLC standardized method.Glycosides,flavonoids,proteins,steroids,saponins,terpenoids,and phenols were found in various concentrations during phytochemical screening.Among both zones,the ethanol leaves extract of SRB taken from Mauritius had a greater content of phytochemicals and a higher yield than other extracts due to the soil nature.The Mauritius sample had greater total flavonoid levels as well as more quercetin(0.92±0.011)than the other extracts.Following that,ethanol extract inhibited enzymes(alpha amylase,alpha glucosidases)more than aqueous extract,and this inhibition was dose dependent.Among them,the Mauritius ethanol sample showed higher anti-diabetic efficacy than the Indian sample,but this difference was not significant.Overall,SRB ethanol leaves extracts outperformed other leaves extracts in terms of yield,phytoconstituents,and total flavonoids.Overall,both SRB samples had high quercetin levels and possessed anti-diabetic potential,but they were greater in the Mauritius sample,demonstrating that plant traits are influenced by geographic location.
基金The authors gratefully acknowledge the University Grants Commission(UGC)India for providing financial assistance in the research work.‘In vitro testing for anticancer activity evaluation of drugs,was done at Anti-Cancer Drug screening facility(ACDSF)at ACTREC,Tata Memorial Centre,Navi Mumbai’.
文摘This is the first report illustrating the extraction of total phenolic compounds(TPC)using the ultrasound-assisted aqueous extraction(USAE)technique from waste Syzygium cumini leaves(WSCL).A kinetic study indicated that Peleg’s model was appropriately fitted to the experimental data when the effect of different parameters was checked on extraction with respect to time.Extraction yields of total phenolic contents(TPC)and total flavonoid contents(TFC)were 78.38 mg GAE/g,and 10.15 mg CE/g,respectively,at optimized parameters of 1:25 WSCL:water,35℃ temperature,134 W power,50%duty cycle and in 9 min of sonication time.Cumulative yields of TPC and TFC obtained by 5 sequential stirred batch extraction were 79.36 mg GAE/g and 10 mg CE/g,respectively.The cost and energy requirement of the USAE process was around 3000 times less than that of the Soxhlet technique.SEM images showed the changes in the morphology of the WSCL surface area before and after ultrasonic extraction.FTIR analysis showed the presence of O-H,N-H,C-H,C=C,and halogenated functional groups.The obtained WSCL extract showed antioxidant potential with an IC_(50) value of 15.64μg/mL.IC_(50) values of extract forα-amylase andα-glucosidase inhibitions were 8.3 and 6.64μg/mL.Antiproliferation activity against breast,cervical,and lung cancer showed the potential with GI50 values 252.8,112.5,and 97.8μg/mL,respectively.Aqueous extract of Syzygium cumini leaves can be used to treat oxidative stress,diabetes,and cancer.
文摘Traditional system of medicine consists of large number of plants with various medicinal and pharmacological importances and hence represents a priceless tank of new bioactive molecules.Coccinia indica belongs to the family Cucurbitaceae.It is a rapidly growing,perennial climber or trailing vine.Traditionally different parts of this plant namely the roots,leaves and fruits are used in folklore medicine for several purposes like jaundice,diabetes,wound healing,ulcers,stomach ache,skin disease,fever,asthma,cough.The leaf and its constituents have been reported to possess hypoglycaemic,hypolipidemic and antioxidant properties.This review provides adequate information to develop suitable therapeutics out of these plant parts.
基金supported by the USDA National Institute of Food and Agriculture,Hatch Act formula funds project 1019794.
文摘Rising consumer concerns with synthetic drugs to treat non-communicable diseases(NCDs)have promoted a shift towards using natural biological active constituents that offer similar health benefits.Hairless canary seed(Phalaris canariensis L)is an emerging crop traditionally used in Mexico to treat NCDs.Peptides liberated during simulated digestion of canary seed protein are believed to be responsible for their biological activity;however,no studies have shown the effect of controlled protein hydrolysis using commercial proteases on canary seed protein’s biological activity.Therefore,this study aimed to explore the in vitro antihypertensive,antidiabetic,and anti-obesity activity of canary seed peptides derived from proteolysis with Alcalase®.Protein fractions were primarily composed of prolamins(54.07±1.8%),glutelins(32.19±3.18%),globulins(5.97±0.52%)and albumins(5.97±0.52%).The<3 kDa and 3–10 kDa peptide fractions showed the highest inhibition capacity(p<0.05)towards angiotensin-converting enzyme(IC50=0.028–0.032 mg/mL)lipase(IC50=2.15–2.27 mg/mL),α-glucosidase(IC50=0.82–1.15 mg/mL),and dipeptidyl-peptidase-IV(IC50=1.27–1.60 mg/mL).Additionally,these peptide fractions showed high antioxidant activity against DPPH(134.22–150.66μmol TE/mg)and ABTS(520.92–813.33μmol TE/mg).These results provide an insight into the potential development of functional foods using commercial enzymatic hydrolysis of canary seed proteins for treating hypertension,type-2 diabetes,and obesity.
基金supported by Padmashree Institute of Information Sciences,Bangalore
文摘The present study was undertaken to evaluate the influence of the methanolic fruit extract of Momordica cymbalaria(MFMC) on PPARγ(Peroxisome Proliferator Activated Receptor gamma) and GLUT-4(Glucose transporter-4) with respect to glucose transport. Various concentrations of MFMC ranging from 62.5 to 500 μg·mL-1 were evaluated for glucose uptake activity in vitro using L6 myotubes, rosiglitazone was used as a reference standard. The MFMC showed significant and dose-dependent increase in glucose uptake at the tested concentrations, further, the glucose uptake activity of MFMC(500 μg·mL-1) was comparable with rosigilitazone. Furthermore, MFMC has shown up-regulation of GLUT-4 and PPARγ gene expressions in L6 myotubes. In addition, the MFMC when incubated along with cycloheximide(CHX), which is a protein synthesis inhibitor, has shown complete blockade of glucose uptake. This indicates that new protein synthesis is required for increased GLUT-4 translocation. In conclusion, these findings suggest that MFMC is enhancing the glucose uptake significantly and dose dependently through the enhanced expression of PPARγ and GLUT-4 in vitro.
基金supported by Center for Science and Technology Development for Youth in Ho Chi Minh City(26/2017/HD-KHCN-VU)supported in part by Kien Giang Department of Science and Technology(28/HD-SKHCN).
文摘Objective:Recently,much attention has been paid to natural product-derived compounds for antidiabetic drug discovery.More recent studies are being focused on clarifying the bioactivity of plants and derived products.The aim of the present study was to investigate the anti-oxidant and antidiabetic activities of Clerodendrum inerme leaf extract(CILE)in streptozotocin-induced diabetic mice.Methods:C.inerme leaves were analyzed for preliminary phytochemical properties and the content of total phenolic and flavonoid were determined.In vitro anti-oxidant activity was measured using DPPH assay.Streptozotocin-induced diabetic model in mice was applied for in vivo study by the effect of CILE at two dose levels(343 and 686 mg/kg b.w.).Results:The results showed that C.inerme leaves contained the major constituents of flavonoids,alkaloids,tannins,triterpenes,and saponins.CILE exhibited the total polyphenol and flavonoid content with 120.458 mg gallic acid equivalent/g dry weight and 4.494 mg hispidulin equivalent/g dry weight,respectively.The anti-oxidant activity of CILE was expressed with IC50=25.28μg/m L.CILE at the doses of343 mg/kg and 686 mg/kg after 7 d administration exerted a decrease in plasma glucose,protected the liver,kidneys against oxidation stress via increasing glutathione content in the liver,and reduced malondialdehyde content in the liver and kidneys.Pancreatic histological analysis in diabetic mice treated with CILE also showed the pancreaticβ-cells regeneration via increasing the size and number of pancreatic islets.Conclusion:These findings suggested that C.inerme leaves had potent antidiabetic and anti-oxidant activities.The results provide reliable scientific base,which is the premise for further research and development of CILE as supplements.
文摘Objective:Wild musk melon(Cucumis melo var.agrestis,CMA)is one of the edible plants form Tamil Nadu.Traditionally,this plant was used as diabetic diet(leaves of CMA with Momordica charantia leaves),but there is no scientific report on antidiabetic action of this plant material.Hence,the current research work was designed to evaluate the antihyperglycemic and antihyperlipidemic effect of hydroalcoholic extract of CMA leaves(HALEC)in streptozotocin(STZ)-nicotinamide(NIC)-induced diabetic rats.Methods:Diabetes was induced by administration of STZ(60 mg/kg,i.p.)after 15 min of NIC(120 mg/kg i.p.)administration.The diabetic rats were treated with HALEC(300 and 600 mg/kg,p.o.,respectively)for 21 d.Results:After the management with HALEC,blood glucose,HbA1c levels,total cholesterol,LDL cholesterol,triglycerides levels,glycogen phosphorylase and glucose-6-phosphatase levels were significantly diminished in diabetic rats.However,haemoglobin level,HDL cholesterol,liver glycogen,total protein,hexokinase,glucose-6-phosphate dehydrogenase levels were significantly increased in HALEC treated diabetic rats.The histopathological studies of the pancreas in HALEC-treated diabetic rats showed almost normal appearance.L6 cell line study revealed the increased glucose uptake activity of HALEC.High performance thin layer chromatography(HPTLC)analysis confirms the presence of active principles such as rutin,gallic acid and quercetin in HALEC.Conclusion:The results indicated that HALEC possess significant antihyperglycemic and antihyperlipidemic activity in STZ-NIC-induced typeⅡdiabetic rats with protective effect.This research work will be useful for the isolation of active principles and development of herbal formulation in phytopharmaceuticals.
