In Vivo and In Vitro Antidiabetic and Anti-Inflammatory Properties of Flax (Linum usitatissimum L.) Seed Polyphenols

Flaxseed is an oilseed (45–50% oil on a dry-weight basis) crop. Its oil has demonstrated multiple health benefits and industrial applications. The goal of this research was to evaluate the antidiabetic and anti-inflammatory potential of the free polyphenol fraction of flax (Linum usitatissimum L.) seeds (PLU), based on their use in traditional medicine. Mice with alloxan-induced diabetes were used to study the antidiabetic activity of PLU in vivo, with an oral administration of 25 and 50 mg/kg over 28 days. Measurements of body weight and fasting blood glucose (FBG) were carried out weekly, and biochemical parameters were evaluated. An oral glucose tolerance test was also performed. Inhibitory activities of PLU on α-amylase and α-glucosidase activities were evaluated in vitro. The anti-inflammatory was evaluated in vivo in Wistar rats using the paw edema induction Test by carrageenan, and in vitro using the hemolysis ratio test. PLU administration to diabetic mice during the study period improved their body weight and FBG levels remarkably. In vitro inhibitory activity of digestive enzymes indicated that they may be involved in the proposed mode of action of PLU extract. Qualitative results of PLU revealed the presence of 18 polyphenols. These findings support daily consumption of flaxseed for people with diabetes, and suggest that polyphenols in flaxseed may serve as dietary supplements or novel phytomedicines to treat diabetes and its complications.

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In vitro, acute and subchronic evaluation of the antidiabetic activity of Atractylis flava Desf n-butanol extract in alloxan-diabetic rats

Future Journal of Pharmaceutical Sciences ◽

10.1186/s43094-021-00358-5 ◽

2021 ◽

Vol 7 (1) ◽

Author(s):

Mohamed Akram Melakhessou ◽

Salah Eddine Marref ◽

Naima Benkiki ◽

Cherine Marref ◽

Imene Becheker ◽

...

Keyword(s):

Blood Glucose ◽

Plant Extract ◽

Fasting Blood Glucose ◽

Folk Medicine ◽

Diabetic Rats ◽

Antidiabetic Activity ◽

Oral Glucose ◽

Butanol Extract

Abstract Background Diabetes mellitus is a serious complex multifactorial disorder that imposes huge health and economic burden on societies. Because the currently available medications have many drawbacks, it's important to look for alternative therapies. Medicinal plants utilized in folk medicine are ideal candidates. Therefore, this work assessed the antidiabetic action of n-butanol extract from the whole plant Atractylis flava Desf (BEAF). These ethnomedicinal properties of BEAF were scientifically validated using in vitro and in vivo assays. In vitro antidiabetic effect of the BEAF was conducted using α-Glucosidase and α-Amylase assays. While the antihyperglycemic activity was assessed using two rat models: Alloxan-induced diabetic rats and oral glucose challenged rats. Experimental diabetes was induced by a single intraperitoneal injection of alloxan at a dose of 150 mg/kg and animals with fasting blood glucose levels (BGL) > 200 mg/dL were considered diabetic. Glibenclamide (5 mg/kg) was used as a typical drug. Results The BEAF at all tested dose levels (100, 250, and 500 mg/kg) showed a significant decrease in blood glucose level in all the two animal models. Besides, the plant extract exhibited a potent inhibitory effect on α-Amylase and α-Glucosidase activity at a concentration of 1000 µg/mL with 76.17% and 89.37%, respectively. Conclusion BEAF exerts in vitro and in vivo antidiabetic effects, these results suggest that the plant extract can be a therapeutic resource in the treatment of diabetes and hyperlipidemia.

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Phytochemical Screening and Anti-Diabetic Efficacy of O. Sanctum Seed Extract on Streptozotocin Induced Diabetic Rats

The Indian Journal of Nutrition and Dietetics ◽

10.21048/ijnd.2017.54.3.14976 ◽

2017 ◽

Vol 54 (3) ◽

pp. 336

Author(s):

Kavitha K. ◽

Ponne S.

Keyword(s):

Body Weight ◽

Digestive Enzymes ◽

Fasting Blood Glucose ◽

Inhibitory Effect ◽

Diabetic Rats ◽

Seed Extract ◽

Phytochemical Screening ◽

Weight Changes

The present study was designed to assess the in vitro and in vivo anti-diabetic efficacy of <em>O. sanctum</em> seed and its phytochemical screening. In vitro inhibitory effect on carbohydrate digestive enzymes like α-amylase and α-glucosidase and in vivo parameters such as fasting blood glucose and body weight changes were studied, a potent inhibitory effect was observed on activities of digestive enzymes and a marked decrease in the glucose level in the <em>O. sanctum</em> seed extract treated streptozotocin induced diabetic rats was noted. Further a marked reduction in body weight was also observed.

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Antidiabetic Activity ofPterospermum acerifoliumFlowers and Glucose Uptake Potential of Bioactive Fraction in L6 Muscle Cell Lines with Its HPLC Fingerprint

BioMed Research International ◽

10.1155/2014/459376 ◽

2014 ◽

Vol 2014 ◽

pp. 1-10 ◽

Cited By ~ 5

Author(s):

Rathinavelusamy Paramaguru ◽

Papiya Mitra Mazumder ◽

Dinakar Sasmal ◽

Venkatesan Jayaprakash

Keyword(s):

Glucose Uptake ◽

Fasting Blood Glucose ◽

Ethanol Extract ◽

Ethyl Acetate Fraction ◽

Diabetic Control ◽

Antidiabetic Activity ◽

Peripheral Tissues ◽

Hplc Fingerprint

The present study was designed to estimate the detailed antidiabetic activity ofPterospermum acerifolium(L.) Willd flowers.In vitroalpha amylase inhibition study was carried out on 50% ethanol extract of flowers (PAFEE) and its various fractions. The active ethyl acetate fraction (PAFEF) was subfractionated into three subfractions (PAFE1, PAFE2, and PAFE3) and subjected to acute toxicity studies followed by antidiabetic screeningin vivoby streptozotocin-nicotinamide induced type II diabetes. Diabetic animals treated with PAFE2 (30 mg/kg) reduced the levels of fasting blood glucose, significantly (P<0.001) compared to that of diabetic control animals. Histological studies on drug treated groups did not show remarkable positive changes inβ-cells. PAFE2 showed32.6±1.93% glucose uptake over control and, in the presence of PI3K inhibitor wortmannin, declined to13.7±2.51%. HPLC analysis of PAFE2 reveals the presence of quercetin and apigenin as major constituents and both are inhibiting the glycogen phosphorylase enzyme in molecular modelling studies. The study evidenced strongly that the probable glucose lowering mechanism of action of active subfraction PAFE2 is by increasing the glucose uptake in peripheral tissues and by inhibition of gluconeogenesis.

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Hyperoside Suppresses Renal Inflammation by Regulating Macrophage Polarization in Mice With Type 2 Diabetes Mellitus

Frontiers in Immunology ◽

10.3389/fimmu.2021.733808 ◽

2021 ◽

Vol 12 ◽

Author(s):

Jialing Liu ◽

Yanmei Zhang ◽

Hongqin Sheng ◽

Chunling Liang ◽

Huazhen Liu ◽

...

Keyword(s):

Bone Marrow ◽

T Cell ◽

Macrophage Polarization ◽

Fasting Blood Glucose ◽

Therapeutic Effects ◽

Protective Effects ◽

Monocyte Chemoattractant Protein 1 ◽

Anti Inflammatory

Accumulating evidence reveals that both inflammation and lymphocyte dysfunction play a vital role in the development of diabetic nephropathy (DN). Hyperoside (HPS) or quercetin-3-O-galactoside is an active flavonoid glycoside mainly found in the Chinese herbal medicine Tu-Si-Zi. Although HPS has a variety of pharmacological effects, including anti-oxidative and anti-apoptotic activities as well as podocyte-protective effects, its underlying anti-inflammatory mechanisms remain unclear. Herein, we investigated the therapeutic effects of HPS on murine DN and the potential mechanisms responsible for its efficacy. We used C57BLKS/6J Lepdb/db mice and a high glucose (HG)-induced bone marrow-derived macrophage (BMDM) polarization system to investigate the potentially protective effects of HPS on DN. Our results showed that HPS markedly reduced diabetes-induced albuminuria and glomerular mesangial matrix expansion, accompanied with a significant improvement of fasting blood glucose level, hyperlipidaemia and body weight. Mechanistically, pretreatment with HPS effectively regulated macrophage polarization by shifting proinflammatory M1 macrophages (F4/80+CD11b+CD86+) to anti-inflammatory M2 ones (F4/80+CD11b+CD206+) in vivo and in bone marrow-derived macrophages (BMDMs) in vitro, resulting in the inhibition of renal proinflammatory macrophage infiltration and the reduction in expression of monocyte chemoattractant protein-1 (MCP-1), tumor necrosis factor (TNF-α) and inducible nitric oxide synthase (iNOS) while increasing expression of anti-inflammatory cytokine Arg-1 and CD163/CD206 surface molecules. Unexpectedly, pretreatment with HPS suppressed CD4+ T cell proliferation in a coculture model of IL-4-induced M2 macrophages and splenic CD4+ T cells while promoting their differentiation into CD4+IL-4+ Th2 and CD4+Foxp3+ Treg cells. Taken together, we demonstrate that HPS ameliorates murine DN via promoting macrophage polarization from an M1 to M2 phenotype and CD4+ T cell differentiation into Th2 and Treg populations. Our findings may be implicated for the treatment of DN in clinic.

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Antidiabetic Effect of Noodles Containing Fermented Lettuce Extracts

Metabolites ◽

10.3390/metabo11080520 ◽

2021 ◽

Vol 11 (8) ◽

pp. 520

Author(s):

Soon Yeon Jeong ◽

Eunjin Kim ◽

Ming Zhang ◽

Yun-Seong Lee ◽

Byeongjun Ji ◽

...

Keyword(s):

Blood Glucose ◽

Fasting Blood Glucose ◽

Diabetic Mouse ◽

Antidiabetic Activity ◽

Oral Glucose ◽

Antidiabetic Effect ◽

In Vivo Experiments ◽

Gaba Content ◽

Tof Ms

The aim of the current study was to examine the antidiabetic effect of noodle containing fermented lettuce extract (FLE) on diabetic mice as a pre-clinical study. The γ-aminobutyric acid (GABA) content, antioxidant capacity, and total polyphenol content of the FLE noodles were analyzed and compared with those of standard noodles. In addition, oral glucose and sucrose tolerance, and fasting blood glucose tests were performed using a high-fat diet/streptozotocin-mediated diabetic mouse model. Serum metabolite profiling of mice feed standard or FLE noodles was performed using gas chromatography–time-of-flight mass spectrometry (GC–TOF-MS) to understand the mechanism changes induced by the FLE noodles. The GABA content, total polyphenols, and antioxidant activity were high in FLE noodles compared with those in the standard noodles. In vivo experiments also showed that mice fed FLE noodles had lower blood glucose levels and insulin resistance than those fed standard noodles. Moreover, glycolysis, purine metabolism, and amino acid metabolism were altered by FLE as determined by GC–TOF-MS-based metabolomics. These results demonstrate that FLE noodles possess significant antidiabetic activity, suggesting the applicability of fermented lettuce extract as a potential food additive for diabetic food products.

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Investigation of the In Vitro Antioxidant Potential Of Polyphenolic-Rich Extract of Artocarpus heterophyllus Lam Stem Bark and Its Antidiabetic Activity In Streptozotocin-Induced Diabetic Rats

Journal of Evidence-Based Integrative Medicine ◽

10.1177/2515690x20916123 ◽

2020 ◽

Vol 25 ◽

pp. 2515690X2091612 ◽

Cited By ~ 1

Author(s):

Basiru Olaitan Ajiboye ◽

Oluwafemi Adeleke Ojo ◽

Babatunji Emmanuel Oyinloye ◽

Mary Abiola Okesola ◽

Adeyonu Oluwatosin ◽

...

Keyword(s):

Diabetes Mellitus ◽

Fasting Blood Glucose ◽

Stem Bark ◽

Diabetic Rats ◽

Antioxidant Potential ◽

Antidiabetic Activity ◽

Artocarpus Heterophyllus ◽

Inflammatory Parameters ◽

Anti Inflammatory

Artocarpus heterophyllus Lam (Moraceae) stem bark has been used locally in managing diabetes mellitus with sparse scientific information. This study investigates the in vitro antioxidant potential of polyphenolic-rich extract of A heterophyllus stem bark as well as its antidiabetic activity in streptozotocin-induced diabetic rats. Fifty male Wistar rats were used with the induction of diabetes by a single intraperitoneal injection of streptozotocin (45 mg/kg body weight) and were orally administered 400 mg/kg free and bound phenols of A heterophyllus stem bark. The animals were sacrificed on the 28th day of the experiment using the cervical dislocation method; antihyperglycemia and anti-inflammatory parameters were subsequently assessed. The polyphenolic extracts demonstrated antioxidant potentials (such as hydrogen peroxide and diphenyl-1-picrylhydrazyl), as well as strong inhibitory activity against amylase and glucosidase. There was a significant ( P < .05) increase in glycogen, insulin concentration, pancreatic β-cell scores (HOMA-β), antioxidant enzymes and hexokinase activities, as well as glucose transporter concentration in diabetic animals administered the extracts and metformin. Also, a significant ( P < .05) reduction in fasting blood glucose, lipid peroxidation, glucose-6-phosphatase, and all anti-inflammatory parameters were observed in diabetic rats administered the extracts and metformin. The extracts demonstrated antidiabetic potential, which may be useful in the management of diabetes mellitus

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Evaluation of Aqueous Extract of Alphonsea sclerocarpa for in vivo and in vitro Antidiabetic Potentials in Wistar Rats

International Journal of Pharmaceutical Sciences Review and Research ◽

10.47583/ijpsrr.2021.v70i02.029 ◽

2021 ◽

Vol 70 (2) ◽

Author(s):

Ravi Shankar N ◽

Ram Kishore ◽

Puranik SB

Keyword(s):

Blood Glucose ◽

Glucose Uptake ◽

Aqueous Extract ◽

Insulin Level ◽

Antidiabetic Activity ◽

Albino Rats ◽

Oral Glucose ◽

In Vivo Evaluation

The purpose of current investigation was to investigate in vivo and in vitro anti-diabetic potentials of aqueous extract of Alphonsea sclerocarpa leaves against alloxan induced diabetes in albino rats. Two in vivo and one in vitro methods were performed for the evaluation of aqueous extract for antidiabetic activity. For in-vivo evaluation, diabetes was induced in albino rats by administering a single dose of alloxan. The study was designed to test the acute effect of aqueous extract of Alphonsea sclerocarpa (AEAS) to reduce blood glucose in OGTT. The chronic study of 21 days was performed against diabetic rats and blood glucose was determined at 1st , 7 th, 14th and 21st day. In chronic in vivo study, serum parameters insulin, urea, creatinine, total cholesterol, triglycerides, ALT and AST were also estimated at 21st day to determine the effects of aqueous and aqueous extracts on complications of diabetes mellitus. Glucose uptake by hemidiaphragm assay was performed to test the ability of extract to utilize glucose. In Oral Glucose Tolerance Test, standard glibenclamide and aqueous extract (200mg/kg and 400mg/kg) treated animals have shown significant reduction in blood glucose at 90 mins but at 120 mins. In chronic model the aqueous extract effectively reduced blood glucose levels (P<0.001) at 14th and 21st day of study in therapeutic groups and effect was comparable to that of standard. The extract could also significantly (P<0.001) reduce concentrations of SGOT, triglycerides, cholesterol and urea in serum and significantly (P<0.001) increased the insulin level in blood which proves beneficial effects of the extract in diabetes. The change in concentrations of SGPT and urea were less significant (P>0.01). The presence of extract in glucose uptake assay could significantly increase utilization of the glucose by rat hemidiaphragm. The aqueous extract of Alphonsea sclerocarpa possess significant antidiabetic properties against alloxan induced diabetic animals.

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In Vitro Alpha-Amylase and Alpha-Glucosidase Inhibitory Activity and In Vivo Antidiabetic Activity of Withania frutescens L. Foliar Extract

Molecules ◽

10.3390/molecules26020293 ◽

2021 ◽

Vol 26 (2) ◽

pp. 293

Author(s):

Hamza Mechchate ◽

Imane Es-safi ◽

Abdelhadi Louba ◽

Ali S. Alqahtani ◽

Fahd A. Nasr ◽

...

Keyword(s):

Local Population ◽

Fasting Blood Glucose ◽

Continuous Treatment ◽

Alpha Amylase ◽

Antidiabetic Activity ◽

In Vitro Assays ◽

Diabetic Mice ◽

Alpha Glucosidase

Withania frutescens L. is a wild perennial woody plant used by the local population for diverse therapeutic purposes. This work aims to study for the first time the potential inhibitory effect of this plant hydroethanolic extract on α-amylase and α-glucosidase activities using in vitro methods and its antidiabetic and antihyperglycemic activities using alloxan-induced diabetic mice as a model for experimental diabetes. Two doses were selected for the in vivo study (200 and 400 mg/kg) and glibenclamide, a well-known antidiabetic drug (positive control) in a subacute study (28 days) where the antihyperglycemic activity was also assessed over a period of 12 h on diabetic mice. The continuous treatment of diabetic mice with the extract of Withania frutescens for 4 weeks succeeded to slowly manage their high fasting blood glucose levels (after two weeks), while the antihyperglycemic test result revealed that the extract of this plant did not control hyperglycemia in the short term. No toxicity signs or death were noted for the groups treated with the plant extract, and it shows a protective effect on the liver and kidney. The in vitro assays demonstrated that the inhibition of alpha-amylase and alpha-glucosidase might be one of the mechanisms of action exhibited by the extract of this plant to control and prevent postprandial hyperglycemia. This work indicates that W. frutescens have an important long term antidiabetic effect that can be well established to treat diabetes.

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Antidiabetic activity, alpha-amylase, and alpha-glucosidase inhibitory effect of Tradescantia spathacea Swartz extract

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v11ispl4.4343 ◽

2020 ◽

Vol 11 (SPL4) ◽

pp. 1594-1599

Author(s):

Nagaraju Jesetti ◽

Rajasekhar Reddy Alavala ◽

Subhakar Raju Rapaka ◽

Umasankar Kulandaivelu ◽

Koteswara Rao GSN

Keyword(s):

Methanolic Extract ◽

Amylase Activity ◽

Inhibitory Effect ◽

Antidiabetic Activity ◽

Oral Glucose ◽

Diabetic Patients ◽

Diabetic Model ◽

Alpha Glucosidase

Tradescantia spathacea Swartz belongs to the genus Commelinaceae, a tropical tree used in many countries as an herbal drug for the care of diabetic patients. The aim of this study was to examine anti-diabetic activity of the Tradescantia spathacea Swartz methanolic extract (METSW) and the in-vitro activity of α-amylase, and α-glucosidase was carried out. METSW compared with acarbose inhibition of the α-amylase and α-glucosidase enzyme, METSW exhibited IC50 less than 100μg/mL would be considered as healthy. The METSW showed IC50 66.22 ± 0.52μg/mL α-amylase activity, acarbose revealed an IC50 of 83.25 ± 1.28μg/mL. METSW demonstrated IC50 levels of 85.37 ± 0.72 μg/mL (y= 0.095x+41.89) inhibition of the α-Glucosidase enzymes. METSW at 400 mg/kg greatly decreased the region under the blood glucose level curve in a typical rat test for oral glucose tolerance. The single dose of the extract decreased dramatically from 211 mg/dl to 89.22 mg/dl at 400 mg/kg METSW in the alloxan induced diabetic model. METSW possesses strong antidiabetic activity in vivo and in vitro. Besides, the extract has also been shown to have a significant inhibitory activity of α-amylase and α-glucosidase which may lead to its anti-hyperglycemic function when used in diabetic patients.

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The optimization of ultrasonic-microwave assisted synergistic extraction of Lotus plumule extract rich in flavonoids and its hypoglycemic activity

Food Production, Processing and Nutrition ◽

10.1186/s43014-021-00063-z ◽

2021 ◽

Vol 3 (1) ◽

Author(s):

Qiuzhe Li ◽

Xiaoqing Li ◽

Baodong Zheng ◽

Chao Zhao

Keyword(s):

Body Weight ◽

Fasting Blood Glucose ◽

The Body ◽

Hypoglycemic Activity ◽

Synergistic Extraction ◽

Antidiabetic Activity ◽

Oral Glucose ◽

Ultrasonic Power ◽

Mice Model ◽

Microwave Assisted

AbstractLotus (Nelumbo nucifera Gaertn), a kind of perennial aquatic plant, is widely cultivated and consumed by people in Asian countries. Lotus plumule flavonoids (LPF) have been recognized as a hypoglycemic agent. LPF was optimally obtained using novel ultrasonic-microwave assisted synergistic extraction (UMSE) method by response surface methodology (RSM) on the basis of the results of single-factor experiments. Furthermore, the hypoglycemic activity of LPF was investigated by measuring the body weight, fasting blood glucose (FBG) level, and oral glucose tolerance test (OGTT) and analyzing the physiological indexes in streptozotocin-diabetic mice model. The optimum extraction conditions consisted of microwave power 355 W, ultrasonic power 423 W, extraction time 15 min, solid-liquid ratio 1:40, ultrasound/interval time 1/0, and ethanol concentration 70% with the maximum LPF yield of 2.62%. LPF supplementation significantly decreased the body weight, FBG, OGTT, serum total cholesterol (TC), serum total triglycerides (TG), and insulin levels, indicating the antidiabetic activity of LPF. This research verified that the UMSE technique was highly efficient to extract LPF to the maximum extent and the flavonoids from L. plumule exhibited hypoglycemic activity, which showed broad development and application prospects.

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