Hypoglycemic activities of flowers of Xanthoceras sorbifolia and identification of anti-oxidant components by off-line UPLC-QTOF-MS/MS-free radical scavenging detection / 中草药·英文版

OBJECTIVE@#To identify phytochemical constituents present in the extract of flowers of Xanthoceras sorbifolia and evaluate their anti-oxidant and anti-hyperglycemic capacities.@*METHODS@#The AlCl3 colorimetric method and Prussian Blue assay were used to determine the contents of total flavonoids and total phenolic acids in extraction layers, and the bioactive layers was screened through anti - oxidative activity in vitro. The Waters ACQUITY UPLC system and a Waters ACQUITY UPLC BEH C18 column (2.0 mm × 150 mm, 5 μm) were used to identify the ingredients. And anti-oxidative ingredients were screened by off-line UPLC-QTOF-MS/MS-free radical scavenging. The ameliorative role of it was further evaluated in a high-fat, streptozotocin-induced type 2 diabetic rat model and the study was carried out on NADPH oxidase (PDB ID: 2CDU) by molecular docking.@*RESULTS@#Combined with the results of activity screening in vitro, the anti - oxidative part was identified as the ethyl acetate layer. A total of 24 chemical constituents were identified by liquid chromatography-mass spectrometry in the ethyl acetate layer and 13 main anti-oxidative active constituents were preliminarily screened out through off-line UPLC-QTOF-MS/MS-free radical scavenging. In vivo experiments showed that flowers of X. sorbifolia could significantly reduce the blood glucose level of diabetic mice and alleviate liver cell damage. Based on the results of docking analysis related to the identified phytocompounds and oxidase which involved in type 2 diabetes, quercetin 3-O-rutinoside, kaempferol-3-O-rhamnoside, isorhamnetin-3-O-glucoside, and isoquercitrin showed a better inhibitory profile.@*CONCLUSION@#The ethyl acetate layer was rich in flavonoids and phenolic acids and had significant anti-oxidant activity, which could prevent hyperglycemia. This observed activity profile suggested X. sorbifolia flowers as a promising new source of tea to develop alternative natural anti-diabetic products with a high safety margin.

In-vitro Anti-hyperglycemic Evaluation of Hydroalcoholic Extract of Delonix regia Bark

Anti-hyperglycemic agents is a substance that helps a person with diabetes control their level of glucose (sugar) in the blood. It includes insulin and oral anti-hyperglycemic agents. Diabetes is a metabolic disorder characterized by increased blood glucose levels leading to other major complications. Thus, obtaining these anti hyperglycemic agents through easily available flora is necessary. Delonix regia , a tree cultivated worldwide, has also been used as traditional medicine in various disorders. Aim of the project work was to evaluate the anti-hyperglycemic activity in the hydroalcoholic extract of D. regia bark for the treatment of hyperglycemia. The collected bark was dried, powdered and extracted through cold maceration method. The extract was further concentrated to obtain a gummy mass of the hydroalcoholic extract. The extract was subjected to phytochemical analysis through conventional chemical tests and GC-MS. After the identification of the phytoconstituents, they were studied for their clinically proven properties. In-vitro anti-hyperglycemic studies were carried out through assays like alpha-amylase inhibition assay and alpha-glucosidase inhibition assay. The results of the extract were compared with results of standard acarbose. The IC 50 standard values in alpha-amylase inhibition assay and ?-glucosidase inhibition assay were 98.77 and 84.33 ?g/mL, respectively. The IC 50 values of hydroalcoholic extract of D. regia bark in alpha-amylase and alpha-glucosidase inhibition assay were 167 and 116.31 ?g/mL, respectively. From the study, the hydroalcoholic extract of bark of D. regia exhibit anti-hyperglycemic activity compared to standard acarbose.

Anti-hyperglycemic activity of aqueous extracts of cells produced in Ibervillea sonorae (S. Watson) Green cell culture on murine model / Actividad anti-hiperglucémica del extracto acuoso de células producidas en cultivo celular de Ibervillea sonorae (S. Watson) Green en un modelo murino

Ibervillea sonorae (S. Watson) Greene, is a plant native to Mexico, where its roots have been used traditionally for treating Diabetes Mellitus. The aim of this work was to establishment of cell cultures of stem explants of I. sonorae and evaluation of the anti-hyperglycemic activity of cell aqueous extract on a murine model of streptozotocin-induced diabetic rats. Cell extracts had 2.29 mg palmitic acid/g extracted, and other compounds with pharmacological activities like palmitoyl ethanolamide and palmitoyl tryptamine were also identified. Diabetic rats treated with aqueous cell extract decreased glucose levels from 350 mg/dL to 145 mg/dL, AST and ALT from 164 U/L to 49 U/L and 99 U/L to 53 U/L, respectively. Additionally, there were no changes in the cellular morphology of the pancreas, liver, kidneys, and spleen. These results revealed that the cell aqueous extract from stem explants has anti-hyperglycemic activity.

Ibervillea sonorae (S. Watson) Greene, es una planta originaria de México, donde sus raíces se han utilizado tradicionalmente para el tratamiento de la Diabetes Mellitus. El objetivo de este trabajo fue el establecimiento de cultivos celulares de explantes de tallo de I. sonorae y la evaluación de la actividad anti-hiperglucémica del extracto acuoso celular en un modelo de ratas diabéticas inducidas con estreptozotocina. El extracto celular contiene 2.29 mg de ácido palmítico/g extracto y se identificaron otros compuestos como palmitoil etanolamida y palmitoil triptamina. Las ratas diabéticas tratadas con extracto celular disminuyeron los niveles de glucosa de 350 mg/dL a 145 mg/dL, AST y ALT de 164 U/L a 49 U/L y 99 U/L a 53 U/L, respectivamente. Además, no hubo cambios en la morfología celular del páncreas, hígado, riñones y bazo. Estos resultados indican que el extracto de células de explantes de tallo de I. sonorae tiene actividad anti-hiperglucémica.

Research on hypoglycemic activity of Osmanthus fragrans var. thunbergii extract / 药学学报

This study aimed to assess the hypoglycemic activity, and in vitro inhibition of α-glucosidase, inhibition of the advanced glycation end products (AGEs), and total antioxidant capacity were used to clarify its bioactivity. Furthermore, the potential hypoglycemic active chemical constituents in the aqueous extract of Osmanthus fragrans var. thunbergii flower were characterized using high performance liquid chromatography-electrospray ionization-quadruple time-of-flight mass spectrometry (HPLC-ESI-QTOF-MS) method. The result showed that in vitro inhibition of α-glucosidase of the extract (IC50 = 2.11 ± 0.26 mg·mL-1) were similar to acarbose (IC50 = 2.88 ± 0.32 mg·mL-1), and it inhibited the AGEs formation and the total antioxidant capacity in a certain extent. Based on the MS fragmentation pathway analysis of reference chemical acteoside contained in this extract, and related references, 73 constituents were tentatively identified from the aqueous extract of Osmanthus fragrans var. thunbergii flower, including 58 phenylethanoids, 8 caffeoylquinic acids, 1 flavonoid vicenin-2, and 6 common organic chemicals in plant. Furthermore, 8 unknown alkaloids were characterized in this work. Among of these chemicals, 61 phenylethanoids were supposed to be detected for the first time. In conclusion, this work disclosed the potential hypoglycemic active constituents of Osmanthus fragrans var. thunbergii flower.

Anti-hyperglycemic fraction from Alternanthera sessilis L. leaves gets elucidated following bioassay-guided isolation and mass spectrometry

Abstract The anecdotal use of Alternanthera sessilis L. as a relief for diabetes has been known in the Philippines for generations, and antidiabetic activity of similar varieties in other countries is likewise documented. However, the compounds responsible for this activity remain unclear. This study aims to isolate the anti-hyperglycemic fraction of local A. sessilis leaves and identify the compounds in this fraction. Methanol extract of A. sessilis leaves and its hexane, ethyl acetate (ASE), and water fractions were administered to alloxan-induced diabetic mice. ASE (250mg/kg) had the highest anti-hyperglycemic activity at 6-h post-treatment (25.81%±12.72%), with almost similar blood glucose reduction rate as metformin (30.13±3.75%, p=0.767). Repeated fractionation employing chromatographic separation techniques followed by in vivo anti-hyperglycemic assay yielded partially purified subfractions. A. sessilis ethyl acetate subfraction 4-2 (100mg/kg) displayed remarkable suppression of blood glucose rise in diabetic mice at 6-h post-treatment (26.45±3.75%, p<0.0001), with comparable activity with metformin (100mg/kg, 27.87±5.65%, p=0.652). Liquid chromatography/mass spectrometry showed eight distinct peaks, with four peaks annotated via the Traditional Chinese Medicine library and custom library for A. sessilis. Among these, luteolin, apigenin, ononin, and sophorabioside were identified as putative compounds responsible for the anti-hyperglycemic activity. This result provided basis for the reported anecdotal claims and potential utility of the local variety of A. sessilis leaves as sources of anti-hyperglycemic agents

Chemical and biological assessment of high value pharmaceutical raw material from Egyptian orange peel

In Egypt, orange juice industries generate huge amount of waste peel that could be a source of raw materials with high value and economic return. Here, we explored a better model for waste management of citrus processing waste in Egypt by developing an ecofriendly method for preparation of value added materials. A high grade pectin (HGP) was obtained from the crude acidic water extract of the peel after passing through Diaion HP20 column. The HGP showed potent antidiabetic activity at lower dose than those reported in literature. It possessed significant effect on blood glucose (BG) level, as well as parameters relevant to liver and kidney functions in streptozotocin (STZ) induced diabetic rats. On the other hand, the essential oil (EO) prepared by cold press showed the highest yield (0.72% w/w) and it is the most applicable method of isolate orange oil on pilot scale. EO showed significant antimicrobial activity against the tested food borne pathogens. In conclusion, high value materials — HGP and EO were prepared on pilot scale from the waste orange peel. While the HGP can be included in food supplement for diabetic patients, EO can be used as a natural food preservative.

Efficacy of antihyperglycemic drugs and inositol on polycystic ovary syndrome: A network meta-analysis / 中华内分泌代谢杂志

Objective:The study was designed to evaluate the efficacy in polycystic ovary syndrome (PCOS) of glucagon-like peptide-1 receptor agonists (GLP-1RA), metformin combined with thiazolidinediones, α-glucosidase inhibitor, and inositol.Methods:Eligible studies were searched in databases of PubMed, EMBase, Cochrane Library, Wanfang data, and CNKI based on population, interventions, comparisons, outcomes, and study design (PICOS) principle (inception to Nov 2020). Two researchers independently screened randomized controlled trials in strict accordance with the inclusion and exclusion criteria, extracted basic information and outcomes of included studies, and used Cochrane risk of bias tool to evaluate the methodological quality of the literature. Network meta-analysis was conducted by STATA 14.0. Continuous variables without dimensional differences were calculated by weighted mean difference and 95% CI, and continuous variables with dimensional differences were calculated using standardized mean difference and 95% CI. Results:A total of 27 studies with 1 445 patients were included in this study. Network meta-analysis showed that acarbose presented a better efficacy than other interventions in reducing total testosterone [surface under the cumulative ranking curve (SUCRA): 89.4%]. GLP-1RAs may have the best efficacy in reducing body mass index and homeostasis model assessment for insulin resistance (HOMA-IR; SUCRA: 99.1%, 89.2%, respectively), while using inositol may be a good choice to reduce serum fasting insulin, HOMA-IR, blood total cholesterol, and blood triglycerides (SUCRA: 94.5%, 85.4%, 96.6%, and 82.8%, respectively).Conclusions:Acarbose may have advantages over other antihyperglycemic drugs in lowering blood testosterone. GLP-1RAs are more helpful to improve body mass index and HOMA-IR in PCOS patients. Inositol, as an insulin sensitizer, has a favorable effect on reducing fasting insulin, HOMA-IR, blood total cholesterol, and blood triglycerides, and there are no reports of side effects in current researches. Further study is still needed to confirm its efficacy.

Consideraciones sobre el efecto cardiovascular de algunos antidiabéticos orales / Considerations on the cardiovascular effect of some oral antidiabetics

RESUMEN La diabetes mellitus tipo 2 se asocia a un elevado riesgo cardiovascular, dadas las proporciones epidémicas a las que está llegando; las guías de tratamiento ponen de relieve la necesidad de prevenir y reducir las complicaciones cardiovasculares y mejorar el control glucémico, especialmente en las etapas precoces de la enfermedad. Los fármacos que disminuyen o regulan la glucosa se han incrementado en los últimos años y, a consecuencia de ello, el tratamiento de la diabetes mellitus tipo 2 se ha vuelto cada vez más complejo y cambiante; por tanto, es importante conocer los diferentes medicamentos que existen hoy para el tratamiento de la diabetes mellitus y sus efectos, tanto positivos como negativos, a nivel cardiovascular. Las actuales recomendaciones hacen hincapié en la individualización de los objetivos glucémicos.

ABSTRACT Type 2 diabetes mellitus is associated to high cardiovascular risk. Given the epidemic proportions it is reaching, treatment guidelines emphasize the need of preventing and reducing major adverse cardiovascular events as well as improving glycemic control, especially in the early stages of the disease. The drugs that decrease or regulate glucose have increased in recent years and, as a result, the treatment of type 2 diabetes mellitus has become increasingly changing and complex; therefore, it is important to know the different drugs that exist nowadays for the treatment of diabetes mellitus and their effects, both positive and negative, at a cardiovascular level. The current recommendations emphasize the individualization of glycemic targets.

Anti-hyperglycemic Effects of Diacerein in Alloxan-Induced Diabetes Mellitus in Wistar Albino Rats

Objective: To determine the anti-hyperglycemic effects of interleukin-1 inhibitor (diacerein) in alloxan induced diabetic albino wistar rats. This experimental study was performed at the Department of Animal Husbandry and Veterinary Sciences, Sindh Agriculture University, Tando Jam within 6 months from April 2016 to September 2016. Total of 160 adult Albino Wistar Rats having an average of 200 to 300 grams body weights were selected. Animals were categorized into 4 groups as;  Group A (n=15): Control rats – receive 0.9% normal saline as placebo Experimental Groups  Group B (n=15): Experimental Control (Diabetic rats) - Alloxan50 mg/kg body weight intraperitoneal.  Group C (n=15): Diabetic rats + Diacerein (30 mg/kg/day) orally daily.  Group D (n=15): Diabetic rats + Diacerein (50 mg/kg/day) orally daily. Animals were kept and treated as per the NIH Guideline for Use and Care of Laboratory Animals. Diabetes mellitus was induced via a single intraperitoneal injection of 50 milligram/kg alloxan monohydrated dissolved in aseptic 0.9% saline. After 72 hours, blood specimens were taken from the caudal vein of the rats and glucose level>200 mg/dL was taken as diabetes. Experimental rats were given diacerein approximately 30 and 50 mg orally for 6 weeks. At the completion of experiment the body weight was measured of each animal by electronic measuring balance and blood sample was taken from each animal of all groups to assess the blood glucose level and HbA1c level. Data were recorded via self-made proforma and analysis was done by using SPSS version 20. Results: Average body weight of Diabetic control (Group B) was 193.33±22.50 grams, which was lower in contrast to Diacerein treated group C 202.47±25.70 grams and significantly lower as compared to Diacerein treated group D as 212.6±23.43 grams. A significant increase in blood glucose levels 182.07±10.63 mg/dl was noted in the Diabetic control (Group B) compared to Diacerein treated group C (110.13± 8.54 mg/dl) and group D (85.87±8.41 mg/dl) (P=0.001). HbA1c was markedly raised in the Group B- diabetic controls, while diacerein treated diabetic rats (groups C and D) showed a significant decrease in HbA1c (P=0.001). Conclusion: It was concluded that Diacerein achieves the Euglycemic state by reducing the levels of blood glucose and glycated hemoglobin (HbA1c) in Alloxan-Induced diabetes mellitus in Wistar Albino Rats

Hematological Changes and Antidiabetic Activities of Colocasia esculenta (L.) Schatt Stem Tuber Aqueous Extract in Alloxan Induced Diabetic Rats

Managementofbloodglucoselevelisthehallmarkinthetreatmentofdiabetes.MuchworkhasnotbeendoneonthemanagementofdiabetesusingthestemtuberextractofColocasiaesculenta.TheobjectiveofthisstudywastoevaluatetheantihyperglycemicandhematologicalparameteronColocasiaesculentaaqueousstemextractinalloxaninduceddiabeticrats.Sixty(60)maleratswereusedinthestudy.Sevendaysofacclimatization,theratsweredividedrandomlyintosixgroupsoffiveineachgroup.Group1:Servedasnormalcontrol,Group2:Diabeticcontrolgroup(negativecontrol),Group3:Diabeticgroupand“Glucinorm-M80”(positivecontrol),Group4:Diabeticgroupandextractat200mg/kgbodyweight,Group5:Diabeticgroupandextractat400mg/kg,Group6:Diabeticgroupandextractat600mg/kg.Diabeteswasinducedinalbinoratsby intraperitonealinjectionofalloxanatasingledoseof120mg/kgbodyweightingroups2to6afterstarvingthemfor24hrs.Theanimalsweregivenfeedandwateradlibitum.ThealbinoratswereadministeredfortwentyeightdayswiththeaqueousColocasiaesculentastemtuber,afterwhichtheywerefastedovernight,anaesthetizedwithchloroformandsacrificed.Theresultshowedthattherewasasignificantincrease(p<0.05)inmeanbodyweightofthepositivecontrolandthetreatmentgroups(200mg/kgto600mg/kg)whencomparedwiththenegativecontrolwhichhasasignificantdecrease(p<0.05)inmeanbodyweight.Theresultalsoshowedasignificantincrease(P<0.05)intheconcentrationsofRBC,PCV,HB,whilePLTandMCHshowedsignificantdecrease(P<0.05)inthetreatmentgroupsandnegativecontrolgroupwhencomparedwiththenormalcontrolgroup.Alsotherewasanosignificant(P<0.05)differenceinMCHCofthetreatmentgroupswhencomparedwiththecontrolgroupandnegativecontrolgroup.Alsotherewasasignificantdifferenceinglycosylatehemoglobinofthetreatmentgroupswhencomparedwiththecontrolgroupandnegativegroup.ThisstudyhasdemonstratedthataqueousstemtuberextractofColocasiaesculentahasasignificantincreaseonbodyweightwhichmayhavearoleofimprovingthestatesofpossibleweightlossfollowingcomplicateddiabetes.Also,aqueousstemtuberextractofColocasiaesculentahasanameliorativeeffectonsugarlevelandsomehematologicalparametersofalloxaninduceddiabeticratsshowingeffectivediabeticcontrolandmanagementofdiabetes

Exploration Of Bioactive Components Of Thunbergia Coccinea, Its Pharmacognostic, Antioxidant, Gcms And Antihyperglycemic Studies

Objective: An effort currently made to appraise the preliminary phytochemical, pharmacognostic criteria, antioxidant, GCMS and antihyperglycemic investigations of the Thunbergia coccinea leaves. Thunbergia coccinea (T. coccinea) is an ornamental plant considerably practiced by the tribes of forest areas of Assam (INDIA) as an analgesic, antipyretic, anti-inflammatory, antidote, hepatoprotective, antidiabetic and detoxificant substance. Methods: A comprehensive literature survey was conducted to recognize the ethnomedicinal value of T. coccinea, which is currently grown practically in all provinces. The physicochemical constants like moisture content, ash values especially total ash, insoluble acid ash, water-soluble ash and foreign organic matter were determined for the assessment of the drug. Pharmacognostic parameters like fluorescence examination and microscopic characters of the leaf were studied that would serve to verify for contamination. The extract secured by maceration was subjected to the phytochemical inquiry to determine the existence of substances and their antioxidant activity. The antihyperglycemic characteristic of alcoholic extract of the leaf was examined with the inhibition of α-amylase and α-glucosidase enzymes. Gas Chromatography-Mass Spectrometry (GCMS) studies of alcoholic extract of the plant leaf have undertaken to get an insight into the therapeutic properties of the molecules present based on online PASS prediction. Results: Various physicochemical, microscopic parameters studied gave a clear distinguishing and identifying features of T. coccinea leaf. Phytochemical screening gave an insight into the secondary metabolites existing in the plant leaf through picturizing its therapeutic properties against various ailments. Both extracts of T. coccinea leaf showed enhanced antioxidant activities. Nevertheless, the alcoholic leaf extract has shown significant antioxidant activity with an IC50 of 171.38±2.51 μg/ml and AQTC an IC50 value of 206.29±4.5 μg/ml respectively by DPPH method. Further, ACTC showed a better-reducing potential with an IC50 value of 105.74±0.61 μg/ml in comparison with AQTC IC50 value of 203.702±0.97 μg/ml by FRP method. The inhibition potentiality of α-amylase and α-glucosidase was found to be 71.66 % and 83.74 %, respectively at 500 µg/ml that rationally an adequate remedy in the treatment of type-2 diabetes. GCMS studies of the alcoholic extract unveiled the presence of different molecules like Glycerol, tris (trimethylsilyl) ether, 3,7,11,15-Tetramethyl-2-hexadecen-1-ol, Undecanoic acid, Ethyl ester, Phytol in comparison with NIST library, thereby giving its predicted therapeutic properties like sugar phosphatase inhibitor, antifungal, phobic disorders treatment, antiviral and so on. Conclusion: The selected plant had many proven therapeutic traits and, possibly, successively united on to the sort of potential therapeutic plants. Besides, isolation and discoveries will lead to the detection of certain novel compounds, which will be of potential medicinal value.

Morphological, phytochemical and anti-hyperglycemic evaluation of Brachychiton populneus

Abstract Brachychiton populneus (Schott & Endl.) R.Br., Malvaceae, is one of five Brachychiton species cultivated in Egypt. Little information was found concerning the morphological, phytochemical and biological investigations of B. populneus. Morphological investigations of B. populneus were performed on fresh and dried leaves. Air-dried, ground leafy branches were extracted with 70% methanol/water yielding B. populneus extract. Seventeen flavonoids were isolated and identified using different chromatographic and spectroscopic techniques; eleven of them were reported for the first time from this plant. Potential activity of B. populneus extract against alloxan inducing oxidative stress and diabetes in male rats was preliminary investigated (four groups of ten rats /group). B. populneus extract (500 mg/kg bw i.p.) exhibited significant acute anti-hyperglycemic activity with blood glucose levels of 227.3 and 157.6 mg/dl after 4 and 24 h, respectively, compared to alloxan and standard Diamicron (5 mg/kg bw p.o.) groups, as well as to a normoglycemic control group at p < 0.05. The extract reverted the body weight values of the alloxan-induced diabetic rats to that of control animals after 24 h. In addition, B. populneus extract counteracted the effect of the oxidative stress induced by alloxan causing significantly increase in the glutathione content level (2.35 mmol/l) and relative decrease in the malondialdehyde level (21.31 nmol/l) and nitric oxide content (1.98 µmol/l) in serum after 24 h of treatment compared to alloxan-induced diabetic rats (1.01 mmol/l, 118.9 nmol/l, 4.69 µmol/l, respectively) and to normoglycemic control at p < 0.05. These effects appear to be related to the flavonoid principles. The intergeneric relationship of the genus Brachychiton and other related genera assessed well-supported differentiation between them. Furthermore, a significant dissimilarity was observed at interspecific level.

Anti-Hyperglycemic and Anti-Hyperlipidemic Potentials of Methanol Leaf Extracts of Aframomum melegueta and Piper guineense

Aim: The study investigated the anti-hyperglycemic and anti-hyperlipidemic potentials of methanol extracts of Piper guineense and Aframomum melegueta leaves with a view to utilizing the plants in the treatment and management of cardiovascular disorders. Methodology: Twenty-eight healthy albino rats were randomly divided into seven equal groups: Group I received normal saline (2 ml/kg bwt); Group II received a single dose of alloxan(150 mg/kg bwt) intraperitoneally; Group III received alloxan (150 mg/kg bwt) + glibenclamide (5 mg/kg bwt);Group IV received alloxan (150 mg/kg bwt) +PG (200 mg/kg bwt); Group V received alloxan (150 mg/kg bwt) + PG (400 mg/kg bwt); Group VI received alloxan (150 mg/kg bwt) + AM 200 (mg/kg bwt); Group VII received alloxan (150 mg/kg bwt) + AM (400 mg/kg bwt). The blood glucose level was determined before and after treatment with the extracts. The lipid: (total cholesterol (TC), triglycerides (TG), high density lipoprotein (HDL) and low density lipoprotein (LDL) were estimated using the Randox diagnostic kits. Results: The results revealed that alloxan was able to induce hyperglycemia at 150 mg/kg bwt and post-treatment with P. guineense and A. melegueta at 200 mg/kg and 400 mg/ kg bwt were able to significantly lower the blood glucose level which was quite apparent in AM treated groups. Also, the extracts at 200 mg/kg and 400 mg/kg were able to bring a significant (p < 0.05) reduction in TC, TG and LDL concentrations when compared to the alloxan treated group with the highest reduction in AM treated groups. Conclusion: These results revealed that the methanol extract of P. guineense and A. melegueta elicited anti-hyperglycemic and anti-hyperlipidemic potentials of the extracts with the highest effect observed in A. melegueta treated rats.

Bioactivity of methanolic extract of Brassica juncea in animal model of diabetes mellitus / 中草药·英文版

Objective: To study the bioactivity of methanolic extract of Brassica juncea on animal model of diabetes mellitus along with its effect on diabetic and metabolic parameters. Methods: Diabetes mellitus was induced in rats by injecting streptozotocin (60 mg/kg) intraperitonealy. Blood glucose was measured on day 3 by GOD-POD method to confirm the diabetes mellitus. Rats having fasting blood glucose > 250 mg/dL were further selected for study and they were divided into four groups, control, control + streptozotocin, streptozotocin + metformin (75 mg/kg) and streptozotocin+ extract of B. juncea (450 mg/kg). Each group consisted of six rats of either sex. Metformin and experimental extract were administered for 21 d. Triglyceride, cholesterol level were measured on day 21 by commercially available kit. Blood glucose was measured on days 7 and 21. Anti-oxidant potential was assessed by estimating extent of lipid peroxidation (LPO) by malondialdehyde (MDA), nitric oxide (NO), superoxide dismutase (SOD) and glutathione (GSH) in liver, kidney, pancreas, muscle tissues on day 21. Unpaired and paired student's t-test was applied for statistical analysis. Results: The extract of B. juncea showed significant decrease in blood glucose level on day 21. The treatment group showed significant difference in oxidative stress by increasing SOD and GSH and decreasing LPO and NO activity on day 21. The treatment did not show statistically significant difference of cholesterol, and triglycerides level on day 21. Conclusion: The study showed anti-hyperglycemic and anti-oxidative properties of methanolic extract of B. juncea.

Target screening and antihyperglycemic activity on SGLT2 and α-glucosidase in vitro and in vivo of TSG from Polygonum multiflorum / 中草药

Objective: To study the mechanism that TSG can reduce plasma glucose level by inhibiting sodium-dependent glucose cotransporters 2 (SGLT2) and α-glucosidase in vitro and in vivo. Methods: Molecular docking method was used to study the binding affinities of TSG and diabetes related targets. The structures of targets were taken from Protein Data Bank or references. 1-NBDG and PNPG were used as the substrates for the inhibition assays of TSG against SGLT2 and α-glucosidase respectively in vitro. The antihyperglycemic activity of TSG was operated by oral glucose tolerance test (OGTT) and urinary glucose excretion (UGE) test in rats. Results: TSG was identified as the inhibitors of SGLT2 with the docking score of -9.35 less than -9.79 of dapagliflozin as the positive control and α-glucosidase with the docking score of -5.44 compared to -5.58 of acarbose as the positive control. TSG showed the inhibitory rate of 21.6% at the dose of 10 μmol/L against SGLT2 and 32.5% at the dose of 100 μmol/L in vitro test. Compared with model group, the group of 120 mg/kg dose had significant difference (P < 0.05) but the overall effect was not as strong as dapagliflozin in OGTT and UGE test. The result of rat in vivo test showed that glucose inhibition rate of TSG (120 mg/kg) was (9.3 ± 1.0)%, urinary glucose content was (435.5 ± 84.0) mg/kg, which showed certain hypoglycemic effect. Conclusion: TSG exhibited antiglycemic activity through inhibiting SGLT2 and α-glucosidase, which was considered to be a new lead compound of dual target inhibitors.

In vivo hypoglycemic investigation, antihyperglycemic and antihyperlipidemic potentials of Pereskia bleo Kunth. In normal and streptozotocin-induced diabetic rats

Objective: To elucidate the in vivo hypoglycemic capability, antihyperglycemic and antihyperlipidemic activities of Pereskia bleo (Kunth) leaves extracts and bioactive fraction. Methods: The various solvent extracts of Pereskia bleo were investigated for the hypoglycemic and antihyperglycemic activities using a relevant in vivo normal rat model and streptozotocin-induced diabetic rat model with glibenclamide and metformin utilized as positive controls. The effects of the most potent extract and its bioactive fraction on the insulin level, lipid profile and body weight of the diabetic rats were also analyzed. Results: All the extracts showed no hypoglycemic effect while petroleum ether, chloroform and aqueous extracts demonstrated significant (P<0.05) reduction in blood sugar level in the intraperitoneal glucose tolerance test. Aqueous extract and aqueous fraction significantly (P<0.05) reduced the blood glucose level in streptozotocin-induced diabetic rats as early as day 6 compared to the diabetic control as well as significantly restored the serum insulin of diabetic rats. Moreover, the aqueous extract and aqueous fraction disclosed a significant (P<0.05) reduction in total cholesterol, triglycerides, and low-density lipoprotein levels. An elevation in high-density lipoprotein as well as improved body weight loss of the diabetic rats were also observed. Conclusions: In summary, Pereskia bleo appears effective in the management of diabetes and correlated impairments arising from high blood sugar level. Further studies will possibly bring about the discovery of effective and secure plant derived antidiabetic drugs.

In vivo hypoglycemic investigation, antihyperglycemic and antihyperlipidemic potentials of Pereskia bleo Kunth. in normal and streptozotocin-induced diabetic rats

Objective: To elucidate the in vivo hypoglycemic capability, antihyperglycemic and antihyperlipidemic activities of Pereskia bleo (Kunth) leaves extracts and bioactive fraction. Methods: The various solvent extracts of Pereskia bleo were investigated for the hypoglycemic and antihyperglycemic activities using a relevant in vivo normal rat model and streptozotocin-induced diabetic rat model with glibenclamide and metformin utilized as positive controls. The effects of the most potent extract and its bioactive fraction on the insulin level, lipid profile and body weight of the diabetic rats were also analyzed. Results: All the extracts showed no hypoglycemic effect while petroleum ether, chloroform and aqueous extracts demonstrated significant (P<0.05) reduction in blood sugar level in the intraperitoneal glucose tolerance test. Aqueous extract and aqueous fraction significantly (P<0.05) reduced the blood glucose level in streptozotocin-induced diabetic rats as early as day 6 compared to the diabetic control as well as significantly restored the serum insulin of diabetic rats. Moreover, the aqueous extract and aqueous fraction disclosed a significant (P<0.05) reduction in total cholesterol, triglycerides, and low-density lipoprotein levels. An elevation in high-density lipoprotein as well as improved body weight loss of the diabetic rats were also observed. Conclusions: In summary, Pereskia bleo appears effective in the management of diabetes and correlated impairments arising from high blood sugar level. Further studies will possibly bring about the discovery of effective and secure plant derived antidiabetic drugs.

Utilization Pattern Study Of Oral Antihyperglycemic Drugs In Type 2 Diabetes Mellitus In Diabetic Outpatient Care

Aim:The Aim of the present study is to analyze prescription pattern of the antihyperglycemic drugs in patients with type 2 diabetes mellitus (T2DM). Methodology:The study included 620 T2DM out patients aged between 41 to 60 years. Sociodemographic data included mean age, educational status, marital status, duration of diabetes mellitus and BMI. Results:Women (54.8%) shared higher percentage in study population. Metformin (44.1%) was prescribed significantly in higher cases than other antihyperglycemic drugs. Glimepiride (30%) is second most common drug prescribed in monotherapy followed by glibenclamide (9.3%), gliclazide (6.6%) in treatment of T2DM. Conclusion:The prescription pattern study of antihyperglycemic drugs in T2DM can serve as a guide to clinicians to select the monotherapy drug, combination drugs and insulin preparations. The findings of current study also help to the phar-maceutical companies to understand the percentage of utilization of antidiabetic drugs before developing and mar-keting any new drug.

Evaluation of antihyperglycemic activities of Bangladeshi medicinal plant Cinnamomum tamala Leaf extracts in alloxan treated Albino Rats

Background: Diabetic mellitus is a multifactorial disorder associated with its devastating consequences has assumed epidemic proportion in Bangladesh.Methods: The study evaluates the anti-hyperglycemic activity of the aqueous extracts of C. tamala (CTLEt) leaves in blood glucose of albino rats. Type II diabetes mellitus was induced by injecting alloxan at the concentration of 100mg/kg body weight in male albino rats. The diabetic rats were administered orally with aqueous CTLEt at the amount of 1.0ml, 1.5ml and 2.0ml with lab diet and glibenclamide (5mg/kg of body weight). Then blood glucose levels were estimated in all groups after 2 hours, 4 hours, 6 hours, 12 hours and 18 hours of the treatment with CTLEt and a known antidiabetic drug glibenclamide.Results: A comparison was made between the action of CTLEt and glibenclamide. Blood glucose levels of the CTLEt on 18th hours of the study were 8.6 to 5.1mmol/L (1ml CTLEt with lab diet), 10.4 to 4.9mmol/L (1.5ml CTLEt with lab diet), 14.7 to 4.3mmol/L (2.0ml CTLEt with lab diet) in comparison of diabetic control (9.5 to 8.5, 8.7 to 7.8, 7.7 to 7.1mmol/L) and glibenclamide (13.9 to 6.5, 16.3 to 6.1, 9.5 to 5.1mmol/L). Among the sample level, the 2.0ml CTLEt showed a higher efficiency of hypoglycemic effect on alloxan induced diabetic rats.Conclusions: Till date, there is no specific experimental work in Bangladesh about the evolution of antidiabetic activity of C. tamala plant in animal model. Further studies should be undertaken to find out the molecular mechanism of the leaf powder of C. tamala medicinal plant.

New advances in research of pharmacological effects of hesperetin and its derivatives / 中草药

Hesperetin is a dihydrogen flavonoid extracted from the Citrus fruits of the Rutaceae plants. It has many pharmacological effects, such as antibacterial, anti-inflammatory, anti-oxidant, antiviral, anti-allergy, regulating blood lipid, enhancing immunity, etc. In recent years, it is reported that hesperetin and its derivatives had anti-Alzheimer’s disease, anti-Parkinson’s disease, antihyperglycemic effect, inhibiting the venom thrombin, anti-fibrosis, ect. This paper mainly reviews some new pharmacological effects of hesperetin and its derivatives in the past five years, aiming to provide reference for further development and utilization of hesperidin and make it achieve better curative effect in other diseases.