Anti-Tumor and Anti-Diabetic Effects of Sarsasapogenin

In this paper,the pharmacological effects and molecular mechanisms of sarsasapogenin,such as anti-oxidant,anti-inflammatory and anti-diabetic effects,are reviewed in order to provide a theoretical basis for the subsequent development and clinical application of sarsasapogenin.

Access to novel anti-diabetic agents in resource limited settings:A brief commentary

The prevalence of diabetes mellitus is increasing in resource limited settings.Simultaneously,there has been an increase in the number of novel therapies for the management of diabetes mellitus.However,use of novel antidiabetic therapies is limited because of major market access challenges in resource limited settings.Niching products to those patients with the highest absolute risk for major adverse cardiovascular outcomes,and thus most likely to benefit from the therapy,are less likely to have negative budget impact for funders.To improve access,and reduce morbidity and mortality,requires alignment amongst key stakeholders including patient advocacy groups,health care professional councils,national departments of health,the pharmaceutical industry,treasury and finance departments.

Anti-diabetic and anti-cholesterolemic activity of methanol extracts of three species of Amaranthus

Objective:To investigate the anti-diabetic and anti-cholesterolemic activity of methanol extracts of leaves of Amaranthus caudatus,Amaranthus spinosus and Amaranthus viridis in normal and streptozotocin(STZ) induced diabetic rats.Methods:In this study,the anti-diabetic and anti-cholesterolemic activity of methanol extracts of leaves of all three plants was evaluated by using normal and STZ induced diabetic rots at a dose of 200 mg/kg and 400 mg/kg p.o.daily for 21 days.Blood glucose levels and body weight were monitored at specific intervals,and different biochemical parameters,serum cholesterol,serum triglyceride,high density lipoprotein, low density lipoprotein and very low density lipoprotein were also assessed in the experimental animals.Histology of pancreas was performed.Results:It was found that all the three plants at 400 mg/kg dose showed significant anti-diabetic and anti-cholesterolemic activity(P<0.01),while at 200 mg/kg dose less significant anti-diabetic activity(P<0.05) was observed.Concluslons: Methanol extracts of Amaranthus caudatus,Amaranlhus spinosus and Amaranthus viridis showed significant anti-diabetic and anti-cholesterolemic activity,which provides the scientific proof for their traditional claims.

A comprehensive review on anti-diabetic property of rice bran

Rice bran(RB) is one of the nutrient-rich agricultural byproducts. It is a composite of carbohydrates, lipids, proteins, fibers, minerals, and trace elements such as phosphorus, potassium, magnesium, calcium and manganese. The extraction and purification process influences the quality and quantity of rice bran oil, which is rich in tocopherols, tocotrienols, 毭-oryzanol, and unsaturated fatty acids. The bioactive components of RB have been reported for exhibiting antioxidant, anti-inflammatory, hypocholesterolemic, anti-cancer, anti-colitis, and antidiabetic properties. In vitro and in vivo studies, and clinical trials in human volunteers revealed the anti-hyperglycemic activity of RB derived compounds. An updated comprehensive review on the antidiabetic property of RB and its derivative is required to appraise the current knowledge in the particular field. Thus, the present paper covered the composition and bioactivities of RB, and influence of extraction methods on the biological property of rice bran oil and rice bran extract. And the current review also focused on the reported antihyperglycemia activity of rice bran derivatives, and its probable mechanism.

Novel anti-diabetic agents in non-alcoholic fatty liver disease: a mini-review

BACKGROUND:Non-alcoholic fatty liver disease(NAFLD)encompasses a spectrum that ranges from simple steatosis to non-alcoholic steatohepatitis(NASH)and to cirrhosis.The recommended treatment for this disease includes measures that target obesity and insulin resistance.The present review summarizes the role of newer anti-diabetic agents in treatment of NAFLD.DATA SOURCES:PubMed,MEDLINE and Ovid databases were searched to identify human studies between January 1990and January 2013 using specified key words.Original studies that enrolled patients with a diagnosis of NAFLD or NASH and involved use of newer classes of anti-diabetic agents for a duration of at least 3 months were included.RESULTS:Out of the screened articles,four met eligibility criteria and were included in our review.The classes of newer anti-diabetic medications described were dipeptidyl peptidase IV inhibitors and glucagon-like peptide-1 analogues.CONCLUSIONS:Liraglutide and Exenatide showed improvement in transaminases as well as histology in patients with NASH.Sitagliptin showed improvement in transaminases but limited studies are there to access its effect on histology.Further studies are needed to support use of newer anti-diabetic medications in patients with NAFLD.

Anti-diabetic and anti-hyperlipidemic effects of sea cucumber(Cucumaria frondosa) gonad hydrolysates in type Ⅱ diabetic rats

The present study investigated the anti-diabetic activity and potential mechanisms of sea cucumber gonad hydrolysates(SCGH)in a rat model of type II diabetes induced by streptozotocin(STZ)combined with high-fat diet(HFD).Results showed that SCGH significantly reduced water intake,fasting blood glucose level and glycated hemoglobin level.Moreover,the oral glucose tolerance,insulin resistance and plasma lipid level in diabetic rats were also alleviated.Furthermore,histological analysis showed that SCGH effectively protected the tissue structure of liver.In addition,mechanism studies showed that SCGH improved glucose metabolism via activating the IRS/Akt signaling pathway,and promoted lipid metabolism via activating the AMPK signaling pathway.In summary,these findings suggested that SCGH have potential anti-diabetic effects by improving insulin resistance and lipid metabolism disorders.

Anti-diabetic potential of Urena lobata leaf extract through inhibition of dipeptidyl peptidase IV activity

Objective: To evaluate the anti-diabetic potential of leaf extract from Urena lobata(U. lobata) through dipeptidyl peptidase IV(DPP-IV) inhibitory activity.Methods: U. lobata leaf was extracted in hot water and ethanol. The activity of DPPIV inhibitor was tested by in vitro study using gly-pro-p-nitroanilide as substrat of DPPIV and vildagliptin, as standard reference. A product of the reactions between gly-pro-pnitroanilide and DPP-IV, was observed by microplate readers with λ = 405 nm. All data were expressed as mean ± SD and the IC50 value was determined by non linear regression curve fit. Active substances in leaf extract of U. lobata was analyzed by liquid chromatography-mass spectrometry. DPP-IV inhibitory activity of active compounds was evaluated in silico using docking server. Results: The ethanolic extract of U. lobata showed stronger DPP-IV inhibitor activity than water extract with the IC50 values of 1 654.64 and 6 489.88 μg/mL, respectively. Vildagliptin, based on standard reference for DPP-IV inhibitor activity, has IC50 value of 57.44 μg/mL. Based on in silico analysis, mangiferin, stigmasterol and β-sitosterol in U. lobata extract have a strong inhibitory activity on DPP-IV. Conclusions: The results showed that DPP-IV inhibitory activity of U. lobata is related to its active compounds such as mangiferin, stigmasterol and β-sitosterol.

The neuroprotective effects of the anti-diabetic drug linagliptin against Aβ-induced neurotoxicity

Impaired insulin signaling in Alzheimer’s disease（AD）brains：The insulin signaling pathway is a fundamental physiological mechanism that presents in nearly all vertebrate cells.However,sometimes cells stop responding properly to insulin stimulation.This condition is known as insulin resistance,which is a hallmark of two very common conditions,metabolic syndrome and type 2 diabetes（T2D）.

Effects of anti-diabetic drugs on sarcopenia: Best treatment options for elderly patients with type 2 diabetes mellitus and sarcopenia

Human life expectancy increases as society becomes more developed.This increased life expectancy poses challenges associated with the rapid aging of the population.Sarcopenia,an age-related disease,has become a worldwide health issue.Patients with sarcopenia experience decreases in muscle mass and function,becoming frail and eventually bedridden.Type 2 diabetes mellitus(T2DM)is also a major health issue;the incidence of T2DM increases with aging.T2DM is associated with reduced muscle strength and poor muscle quality and may contribute to acceleration of the aging process,augmenting age-related sarcopenia.Recent studies indicate that elderly patients with diabetes are at an increased risk for sarcopenia.Therefore,these older diabetic patients with sarcopenia need specific anti-diabetic therapies targeting not only glycemic control but also sarcopenia,with the goal of preventing sarcopenia in presarcopenic patients.Presently,various types of hypoglycemic drugs are available,but which hypoglycemic drugs are better suited for geriatric T2DM patients with sarcopenia remains undetermined.In this review,we discuss the association between diabetes and sarcopenia in geriatric patients,and how anti-diabetic drugs may influence sarcopenia outcomes.This review will guide clinical workers in the selection of drugs best suited for this patient population.

A review of five traditionally used anti-diabetic plants of Bangladesh and their pharmacological activities

Plants are used traditionally throughout the globe to treat various diseases.Traditionally used medicinal plants are an essential part of the health sector in Bangladesh due to its abundance of a vast source of ethno-medicine.Rural people from developing country like Bangladesh are greatly dependent on traditional source of medicine.The prevalence of diabetes mellitus is increasing from recent years; therefore various researches are going on to discover better medicine to treat this disease.This study has focused on five plants which are Andrographis paniculata, Ageratum conyzoides, Swertia chirata, Terminalia arjuna, and Azadirachta indica to find out their traditional formulation as anti-diabetic medicine and their pharmacological activity has also been explored through literature search.The available information about traditional anti-diabetic uses of these plants and their pharmacological activities were collected from various electronic sources like Pubmed, Sci Finder, Elsevier, Springer, Scopus, Scirus, Science Direct, Google Scholar and Web of Science apart from these locally available books and peer reviewed journal were also used to collect information.This study will help to strengthen the relation between traditional medicine, pharmacology and drug development.A clue may be found from the information provided this review to discover new and better anti-diabetic drugs.

Anti-diabetics and antimicrobials:Harmony of mutual interplay

Diabetes is one of the four major non-communicable diseases,and appointed by the world health organization as the seventh leading cause of death worldwide.The scientists have turned over every rock in the corners of medical sciences in order to come up with better understanding and hence more effective treatments of diabetes.The continuous research on the subject has elucidated the role of immune disorders and inflammation as definitive factors in the trajectory of diabetes,assuring that blood glucose adjustments would result in a relief in the systemic stress leading to minimizing inflammation.On a parallel basis,microbial infections usually take advantage of immunity disorders and propagate creating a pro-inflammatory environment,all of which can be reversed by antimicrobial treatment.Standing at the crossroads between diabetes,immunity and infection,we aim in this review at projecting the interplay between immunity and diabetes,shedding the light on the overlapping playgrounds for the activity of some antimicrobial and anti-diabetic agents.Furthermore,we focused on the antidiabetic drugs that can confer antimicrobial or anti-virulence activities.

Antioxidants, anti-proliferative, anti-inflammatory, anti-diabetic and anti-microbial effects of isolated compounds from Swertia corymbosa (Grieb.) Wight ex C.B. Clark – An in vitro approach

The present study,antioxidant,enzyme inhibitory,anti-inflammatory and antimicrobial activity of isolated compounds such as Decussatin(1),Gentiacaulein(2),Swertianin(3),1,8-dihydroxy-2,6-dimethoxy xanthone(methylswertianin)(4)8-hydroxy-1,2,4,6-tetramethoxyxanthone(5)and 1,2-dihydroxy-6-methoxyxanthone-8-O--d-xylopyranosyl(6)were investigated using an in vitro model.Results of antioxidant studies revealed that the compound 6 possessed an efficient 2,2-diphenyl-1-picryl-hydrazyl(DPPH•)(IC5007.19±4.56μmol/mL),2,2-azinobis(3-ethylbenzothiozoline-6-sulfonic acid)(ABTS•^+)(42.62±0.25 mmol/L TE/g),superoxide(57.89±3.45μmol/mL),nitric oxide(18.45±1.23μmol/mL)and hydroxyl(12.13±2.76μmol/mL)radical scavenging activities,ferric reducing antioxidant power(14.76±0.10 molar Fe(II)/g),metal chelating(213.85±27.18 mg EDTA/g)ability.Compounds 6 and 3 exhibited significant anti-proliferative activity.Compound 6 displayed strongest antibacterial activity against Streptococcus pneumoniae and Escherichia coli with MIC value of 3.90μg/mL and 21.21±0.25 and 20.27±0.11 mm zone of inhibition at 25μg/mL concentration respectively.In the membrane stabilization and protein denaturation test 3 was the most potent with an IC50 value of 12.57,18.75μmol/mL respectively.

<i>In Vitro</i>Anti-Diabetic Activities and Phytochemical Analysis of Bioactive Fractions Present in <i>Meriandra dianthera, Aloe camperi</i>and a Polyherb

This paper reports the in vitro anti-diabetic profile of certain medicinal plants traditionally used in Eritrea for the management of type 2 diabetes. The crude methanolic extracts and fractions of Meriandra dianthera, Aloe camperi, a Polyherb and their fractions were investigated. The in vitro screening of the crude extracts has generally elicited a dose dependent α-glucosidase and α-amylase inhibition activities. M. dianthera displayed the highest α-glucosidase inhibitory activity (IC50: 0.074 ± 0.032 mg/mL) at the highest concentration tested (0.800 mg/mL) relative to A. camperi, the Polyherb and Acarbose (IC50: 0.37 ± 0.052, 0.56 ± 0.024 and 0.55 ± 0.029 respectively). The α-glucosidase inhibition activities of A. camperi and M. dianthera, except for the Polyherb and Acarbose, were significantly different (P < 0.05) at various ranges of concentrations (0.025 - 0.800 mg/mL). The percentage α-amylase inhibitions of M. dianthera, A. camperi, the Polyherb and Acarbose, at the highest concentrations (0.800 mg/mL), were 78.3%, 15.9%, 16.4%, and 82.9% respectively. A. camperi and the Polyherb displayed lower α-amylase inhibitory activities (IC50: 1.72 ± 0.06 and 2.57 ± 0.07 mg/mL respectively) compared to Acarbose and M. dianthera (IC50: 0.31 ± 0.01 and 0.43 ± 0.02 mg/mL respectively). For the α-amylase inhibition activity, even at lower concentrations (0.025 mg/mL), there were statistically significant differences (P < 0.01) among the values generated for all the extracts. The in vitro anti-diabetic screening of the fractions, at 0.800 mg/ml, displayed characteristic enzyme inhibition activities. Generally, the non-polar fractions showed higher enzyme inhibitory activities compared to the polar fractions. The most bioactive non-polar fractions, thus, were subjected to GC-MS analysis and presented various essential oils, fatty acid methyl esters (FAMEs) and benzoic acid derivatives in those plants.

Anti-diabetic effects of cold and hot extracted virgin coconut oil

Virgin coconut oil (VCO) has been shown to possess insulinotropic effects shown in isolated perfused mouse islet with hypolipidemic effects. Hot extracted virgin coconut oil (HEVCO) has been shown to possess better antioxidant properties than cold extracted virgin coconut oil (CEVCO). These properties were exploited to study the anti-diabetic effects of HEVCO and CEVCO in diabetic rats. Four groups 8 rats each, first group served as non-diabetic control remaining groups were made diabetic and force fed with 2ml alcoholic extracts of commercial coconut oil (CCO), CEVCO and HEVCO for 21 days. Blood glucose once in 5 days, body weight gain, food intake once in a week and water intake and urine output daily, were monitored. Animals were sacrificed at the end of 21 days. The results indicated HEVCO reduced blood glucose and lipids viz total cholesterol (TC), triglycerides (TG), High density lipoproteins (HDL), Low and Very Low Density Lipoprotein (LDL+ VLDL) and thiobarbutyric acid reactive substances (TBARS) increased the antioxidant status by elevating activities of antioxidant enzymes such as superoxide dismutase (SOD), catalase, glutathione peroxidase (GSH-Px), glutathione (GSH) concentration and decresed lipid peroxidation in liver than CEVCO. These beneficial effects may be attributed to increased polyphenolic and other antioxidants content present in HEVCO.

Evaluation of extraction protocols for anti-diabetic phytochemical substances from medicinal plants

AIM To examine the efficacy of three extraction techniques: Soxhlet-extraction(SE), cold-maceration(CM) and microwave-assisted-extraction(MAE) using 80% methanol as solvent. METHODS The study was performed on each of 50 g of Vernonia amygdalina(VA) and Occimum gratissimum(OG) leaves respectively. The percentage yield, duration of extraction, volume of solvent used, qualitative and quantitative phytoconstituents present was compared. The biological activities(hypoglycemic effect) were investigated using albino wistar rat model of diabetes mellitus(n = 36) with a combined dose(1:1) of the two plants leaf extracts(250 mg/kg b.w.) from the three methods. Theextracts were administered orally, once daily for 21 d.RESULTS In this report, the percentage VA extract yield from MAE was highest(20.9% ± 1.05%) within 39 min using 250 m L of solvent, when compared to the CM(14.35% ± 0.28%) within 4320 min using 900 m L of solvent and SE(15.75% ± 0.71%) within 265 min using 500 m L of solvent. The percentage differences in OG extract yield between: MAE vs SE was 41.05%; MAE vs CM was 46.81% and SE vs CM was 9.77%. The qualitative chemical analysis of the two plants showed no difference in the various phytoconstituents tested, but differs quantitatively in the amount of the individual phytoconstituents, as MAE had significantly high yield(P > 0.05) on phenolics, saponins and tannins. SE technique gave significantly high yield(P > 0.05) on alkaloid, while CM gave significant high yield on flavonoids. The extracts from CM exhibited a significantly(P > 0.05) better hypoglycemic activity within the first 14-d of treatment(43.3% ± 3.62%) when compared to MAE(36.5% ± 0.08%) and SE methods(33.3% ± 1.60%). However, the percentage hypoglycemic activity, 21 d post-treatment with 250 mg/kg b.w. extract from MAE was 72.6% ± 1.03% and it was more comparable to 10 mg/kg b.w. glibenclamide treated group(75.0% ± 0.73%), unlike the SE(69.5% ± 0.71%) and CM(69.1% ± 1.03%). CONCLUSION CM technique produces extract with better hypoglycemic activity, whereas; MAE is a better option for high yield of phytoconstituents using less solvent within a short time.

A new anti-diabetic sesquiterpenoid from Acorus calamus

A new sesquiterpenoid, 1β,5α-guaiane-4β,10α-diol-6-one （1）, was isolated from 70% EtOH extract of the rhizomes of Acorus calamus. The structure was determined on spectroscopic methods, especially 2D NMR techniques. The absolute configuration of 1 was confirmed by TDDFT quantum chemical calculation of its ECD spectrum. Compound 1 showed promising anti-diabetic activity on a insulin-mediated glucose consumption model of HepG2 cells.

Antioxidant and anti-diabetic activities in commercial and homemade pomegranate molasses in Lebanon

Pomegranate fruit and its derived products are rich sources of bioactive compounds.They have many biological activities.Pomegranate molasses(PM)is a thick,traditional Middle Eastern syrup used in many recipes for Lebanese and international cuisines.It is a highly nutritious product which makes it of great interest.The purpose of this study was to assess the phytochemical composition,antioxidant and anti-diabetic properties of homemade and commercial PM consumed in Lebanon using samples collected from households in rural areas(n=4)and the market(n=28).The objectives of this study were to determine their total phenolic content using the Follin-Ciocalteu method,their total flavonoid content using aluminum chloride method,their antioxidant activity using DPPH radical scavenging as well as ferrous ion chelating assays and their anti-diabetic activity usingα-amylase andα-glucosidase inhibitory activities with acarbose,a known anti-diabetic drug,used as the standard reference.Homemade PM samples exhibited a higher antioxidant activity than commercial samples,with the most active homemade PM sample having IC_(50)values of 0.09 mg/mL(DPPH radical scavenging assay)and 46.78%ferrous ion chelating assay).Homemade PM samples also showed higher anti-diabetic activity than commercial samples,with the most active homemade PM sample having an IC_(50)values of 0.63 mg/mL(α-amylase inhibitory activity)and of 0.41 mg/mL(α-glucosidase inhibitory activity)and being almost as active as acarbose with both enzymes(1.5 times).Significant inverse strong/moderate correlations were observed between total phenolic content/total flavonoid content and the IC_(50)value of DPPH radical scavenging assay,indicating positive associations between total phenolic and flavonoid contents and antioxidant activity.In addition,significant negative moderate correlations were observed between total phenolic/flavonoid contents andα-amylase inhibitory activity,indicating positive associations between total phenolic and flavonoid contents and anti-diabetic activity.

Assessment of anti-diabetic activity of peanut shell polyphenol extracts

The present study aimed to evaluate the anti-diabetic property of peanut shell polyphenol extracts （PSPEs）. Diabetic rats were oral-administrated with PSPE at doses of 50, 100, and 200 mg/kg body weight （BW） per day for 28 consecutive days, with metformin （Met） as a positive control. The results showed that, similar to the Met treatment, administration of PSPE caused significant decreases in food intake, water intake, fasting blood glucose, total cholesterol, triglyceride, low-density lipoprotein cholesterol, and methane dicarboxylic aldehyde in serum, and significant increases in BW, insulin level, high-density lipoprotein cholesterol, superoxide dismutase, glutathione, and liver gly- cogen. Further, glucose tolerance was markedly improved in the PSPE-treated diabetic groups. Histopathological results showed that PSPE improved cellular structural and pathological changes in liver, kidney, and pancreatic islets. Collectively, the results indicated that the hypoglycemic effects of PSPE on high-fat diet/streptozotocin （HFD/STZ）induced diabetes are comparable to Met, though their exact mechanism actions are still under investigation. Therefore, the current study suggests that PSPE could be a potential health-care food supplement in the management of diabetes.

Anti-diabetic related health food properties of traditional rice(Oryza sativa L.)in Sri Lanka

Objective:To evaluate a range of anti-diabetic related properties and some consumer preferred physicochemical properties of selected Sri Lankan traditional rice varieties.Methods:Sudu Heeneti,Goda Heeneti,Masuran and Dik Wee varieties were used in this study.Anti-diabetic related properties of bran extracts of selected varieties were studied for methylglyoxal mediated protein glycation inhibition,acetyl and butyryl-cholinesterase inhibition in vitro and anti-hyperglycemic activity in vivo.Further,selected varieties were studied for starch hydrolysis rate in vitro.Physicochemical properties including grain color,size,shape,crude protein,crude fat,ash,dietary fiber and total carbohydrate contents were studied.Results:Brans of selected varieties had significant(P<0.05)and dose dependent methylglyoxal mediated protein glycation inhibition[IC_(50):(174.77±6.65)to(342.87±0.43)μg/mL]and acetyl[IC_(50):(37.00±0.68)to(291.00±3.54)μg/mL]and butyryl-cholinesterase[IC_(50):(18.50±0.60)to(96.60±0.56)μg/mL]inhibitory activities.Further,Sudu Heeneti,Masuran and Dik Wee had low starch digestion rate(52.40±1.44 to 53.76±1.19)indicating that these varieties may be low glycemic index rices.Brans of Masuran tested in rat model showed anti-hyperglycemic activity.Physicochemical properties studied showed that selected varieties were red in color and grain size and shape were mostly medium and bold respectively.Moisture,crude protein,crude fat,ash and total carbohydrate contents varied significantly(P<0.05)among the varieties.Conclusions:It is concluded that selected varieties could be promoted as physicochemically sound rices with a range of anti-diabetic related properties in the management of diabetes and its complications.

Anti-diabetic effects of linarin from Chrysanthemi Indici Flos via AMPK activation

Objective:The purpose of this study is to investigate the anti-diabetic effects of linarin,a flavonoid extracted from Chrysanthemi Indici Flos(CIF),and its potential mechanisms.Methods:The effects of linarin on cell viability and glucose consumption in Hep G2 cells were measured.Meanwhile,monosodium glutamate(MSG) mouse model was constructed to monitor the changes of insulin tolerance,glucose tolerance,triglyceride and cholesterol.The protein expression levels of pAMPK,p-ACC,PEPCK and p-GS were detected by Western blot.Results:Linarin could increase the relative glucose consumption of Hep G2 cells,improve insulin tolerance and glucose tolerance,and decrease the levels of triglyceride and cholesterol of MSG mice.Simultaneously,the expression levels of p-AMPK and p-ACC in Hep G2 cells and the liver tissue of MSG mice were increased,while the expression levels of PEPCK and p-GS were decreased after treatment with linarin.Conclusion:Insulin resistance could be ameliorated by linarin in type 2 diabetes,and its mechanism may be related to AMPK signaling pathway.