scholarly journals Chemical and biological investigations of Limonium axillare reveal mechanistic evidence for its antidiabetic activity

PLoS ONE ◽  
2021 ◽  
Vol 16 (8) ◽  
pp. e0255904
Author(s):  
Essam Abdel-Sattar ◽  
Manal M. Shams ◽  
Marwa M. Abd-Rabo ◽  
Nehad Mahmoud ◽  
Engy A. Mahrous
Keyword(s):  
Serum Insulin ◽  
Radical Scavenging ◽  
Pancreatic Tissue ◽  
Diabetic Rats ◽  
Antidiabetic Activity ◽  
Scavenging Effect ◽  
Glut4 Expression ◽  
Key Enzyme ◽  
Glycerol 3 Phosphate Dehydrogenase

Root and bark of Limonium axillare (Forssk) Kuntze are used as antidiabetic remedies in parts of East Africa, but this activity has never been fully investigated. To validate its ethnobotanical use, we compared the chemical and pharmacological profiles of the ethanolic extracts of L. axillare root (REE) and aerial parts (AEE). Administration of REE (500 mg kg-1) reduced streptozotocin-induced hyperglycemia by 44%, restored serum insulin levels, reestablished Glut2 and Glut4 expression and ameliorated pancreatic tissue damage in diabetic rats. In vitro studies revealed a strong radical scavenging effect, α-glucosidase, and α-amylase inhibition activity of REE at IC50 at 25.2, 44.8 and 89.1μg/mL, respectively. HPLC analysis identified ten phenolic compounds in REE with umbelliferone as the major constituents at 10 ± 0.081 mg/g of extract. Additionally, six compounds were isolated from REE including, β-sitosterol-3-palmitate, β-sitosterol, myricetin and gallic acids with two new tetrahydrofuran monoterpenes; 2-isopropyl- 3,4,4, trimethyl-tetrahydrofuran (3), and 2-isopropyl-4-methyl-tetrahydrofuran-3,4 dicarboxylic acid (4), the latter was revealed by molecular docking to be a good ligand to glycerol-3-phosphate dehydrogenase a key enzyme in glycolysis.

Synthesis, Characterization and Antidiabetic Activity of Novel Thiazolidine Derivatives

2018 ◽  
Vol 11 (1) ◽  
pp. 3977-3983
Author(s):  
Sumeet Prachand ◽  
Arun K Gupta ◽  
Ritu Gilhotra
Keyword(s):  
Serum Insulin ◽  
Condensation Reaction ◽  
Heterocyclic Ring ◽  
Ring Structure ◽  
Diabetic Rats ◽  
Antidiabetic Activity ◽  
Weight Changes ◽  
Wide Range

Rhodamines are five-member heterocyclic having nitrogen and sulphur atoms in their ring structure respectively and exhibiting potent as well as wide range of pharmacological activities. A series of 4-((4-oxo-2-thioxothiazolidin-5-ylidene) methyl) phenyl substituted benzoate derivatives were synthesized. Benzoic acid derivatives reacted with rhodanine to yield the respective derivatives. This reaction follows the Knoevenagel condensation reaction mechanism by which ethanolamine abstract a proton from heterocyclic ring and a carbanion ion is generated. The structure of synthesize compounds were supported by IR, NMR and mass spectral data. The synthesized compounds were screened for their in vitro antidiabetic activity by α-Amylase, α-Glucosidase inhibition, glucose diffusion inhibitory test and the potential compounds tested for  in vivo activity by blood glucose and body weight changes, serum insulin, Hb, HbA1c, and total protein levels changes, and lipid profiles changes in type 2 diabetic rats.         

Sequoyitol ameliorates diabetic nephropathy in diabetic rats induced with a high-fat diet and a low dose of streptozotocin

2014 ◽  
Vol 92 (5) ◽  
pp. 405-417 ◽  
Author(s):  
Xian-Wei Li ◽  
Yan Liu ◽  
Wei Hao ◽  
Jie-Ren Yang
Keyword(s):  
Diabetic Nephropathy ◽  
Blood Glucose ◽  
High Fat Diet ◽  
Low Dose ◽  
Serum Insulin ◽  
Fasting Blood Glucose ◽  
Diabetic Rats ◽  
High Fat

Sequoyitol decreases blood glucose, improves glucose intolerance, and enhances insulin signaling in ob/ob mice. The aim of this study was to investigate the effects of sequoyitol on diabetic nephropathy in rats with type 2 diabetes mellitus and the mechanism of action. Diabetic rats, induced with a high-fat diet and a low dose of streptozotocin, and were administered sequoyitol (12.5, 25.0, and 50.0 mg·(kg body mass)−1·d−1) for 6 weeks. The levels of fasting blood glucose (FBG), serum insulin, blood urea nitrogen (BUN), and serum creatinine (SCr) were measured. The expression levels of p22phox, p47phox, NF-κB, and TGF-β1 were measured using immunohistochemisty, real-time PCR, and (or) Western blot. The total antioxidative capacity (T-AOC), as well as the levels of malondialdehyde (MDA) and reactive oxygen species (ROS) were also determined. The results showed that sequoyitol significantly decreased FBG, BUN, and SCr levels, and increased the insulin levels in diabetic rats. The level of T-AOC was significantly increased, while ROS and MDA levels and the expression of p22phox, p47phox, NF-κB, and TGF-β1 were decreased with sequoyitol treatment both in vivo and in vitro. These results suggested that sequoyitol ameliorates the progression of diabetic nephropathy in rats, as induced by a high-fat diet and a low dose of streptozotocin, through its glucose-lowering effects, antioxidant activity, and regulation of TGF-β1 expression.

scholarly journals ANTIOXIDANT PROPERTIES OF SINAPIC ACID: IN VITRO AND IN VIVO APPROACH

2017 ◽  
Vol 10 (6) ◽  
pp. 255 ◽  
Author(s):  
Nithya R ◽  
Subramanian S
Keyword(s):  
Antioxidant Properties ◽  
Intraperitoneal Administration ◽  
Radical Scavenging ◽  
Sinapic Acid ◽  
Lipid Peroxides ◽  
Diabetic Rats ◽  
Antioxidant Potential ◽  
Protein Carbonyls

Objective: This study was aimed to evaluate the antioxidant potential of sinapic acid in both in vitro and in vivo. Recently, we have reported that oral administration of sinapic acid (3,5-dimethoxy 4-hydroxycinnamic acid) an active phyto ingredient widely distributed in rye, mustard, berries, and vegetables has been shown to ameliorate hyperglycemia.Methods: Experimental Type 2 diabetes was induced in male Wistar rats by feeding high-fat diet to induce insulin resistance followed by intraperitoneal administration of a single low dose streptozotocin (35 mg/kg body weight [bw]). Sinapic acid was administered orally at a concentration of 25 mg/kg bw/rat/day for 30 days, and its efficacy was compared with metformin. In vitro, antioxidant scavenging properties of sinapic acid were determined using 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), superoxide, and nitric oxide (NO) assay.Results: Sinapic acid treatment showed a significant decline in the levels of lipid peroxides, hydroperoxides and protein carbonyls in the plasma and vital tissues of diabetic rats. The treatment also improved the antioxidant status in diabetic rats indicating the antioxidant potential of sinapic acid. In addition, the results of DPPH, ABTS, superoxide, and NO radical scavenging assays substantiate the free radical scavenging efficacy of sinapic acid.Conclusion: The results of this study evidenced that sinapic acid possess significant antioxidant properties which in turn may be responsible for its antidiabetic properties.

scholarly journals In vitro inhibitory potentials of ethanolic extract of Moringa oleifera flower against enzymes activities linked to diabetes

2021 ◽  
Vol 10 (4) ◽  
pp. 408-414
Author(s):  
Oluwaseun Ruth Olasehinde ◽  
Olakunle Bamikole Afolabi ◽  
Benjamin Olusola Omiyale ◽  
Oyindamola Adeniyi Olaoye
Keyword(s):  
Free Radical ◽  
Moringa Oleifera ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Ethanolic Extract ◽  
Antidiabetic Activity ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Antioxidant Power

Introduction: Diabetes mellitus (DM) has been recognized as the seventh leading cause of global mortality; however, researchers seek alternative means to manage the menace. The current study sought to investigate antioxidant potentials, α-amylase, and α-glucosidase inhibitory activities of ethanolic extract of Moringa oleifera flower in vitro. Methods: Antioxidant properties of the extract were appraised by assessing its inhibition against 1,1-diphenyl-2-picrylhydrazyl (DPPH), hydroxyl (OH•), and hydrogen peroxide (H2O2) free radicals, as well as ferric reducing antioxidant power (FRAP), the antidiabetic activity was evaluated by α-amylase and α-glucosidase inhibition.Results: In this study, ethanolic extract of M. oleifera flower demonstrated a significant (P < 0.05) inhibition against DPPH free radical (43.57–83.56%) in a concentration-dependent manner, while FRAP (101.76 ± 1.63 mg/100 g), OH• scavenging ability (71.62 ± 0.95 mg/100 g), and H2O2 free radical scavenging capacity (15.33 ± 1.20 mg/100 g) were also observed. In the same manner, ethanolic extract of M. oleifera flower revealed a significant (P < 0.05) inhibition against α-amylase (IC50= 37.63 mg/mL) and α-glucosidase activities (IC50= 38.30 mg/mL) in the presence of their respective substrates in a concentration-dependent manner in comparison with acarbose. Conclusion: Ethanoic extract of M. oleifera flower could be useful as an alternative phytotherapy in the management of DM, having shown a strong antioxidative capacity and substantial inhibition against the activities of key enzymes involved in carbohydrate hydrolysis in vitro.

scholarly journals Synthesis and Antioxidant Properties of Novel 2-(2,4-Dioxothiazolidin-5-ylidene)-Acetamides Containing 1,3,4-Thia/Oxadiazole Moieties

2021 ◽  
Vol 12 (5) ◽  
pp. 6710-6722
Keyword(s):  
Ascorbic Acid ◽  
Acetyl Chloride ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Scavenging Effect ◽  
Highly Active ◽  
Ethanol Medium ◽  
Ic50 Value ◽  
Radical Scavenging Ability

A series of novel 1,3,4-thia(oxa)diazole substituted 2-(2,4-dioxothiazolidine-5-ylidene)-acetamides 3a-c, 4 and 5a-k have been synthesized following the acylation reaction of 2-amino-5-aryl-1,3,4-oxadiazoles, 5-amino-1,3,4-thiadiazole-2-thiol and it’s S-alkylated derivatives with 2-(2,4-dioxothiazolidine-5-ylidene)acetyl chloride in dioxane medium. The functionalization of compounds 3b, 3c, 5d and 5e was carried out on their N3 position under N-alkylation conditions with N-aryl-2-chloroacetamides in DMF/ethanol medium yielded the corresponding 2,4-dioxothiazolidine-3,5-diacetic acid diamides 6a-e and 7a-b. The structures of target compounds were confirmed by using 1H NMR spectroscopy and elemental analysis. The antioxidant activity evaluation in vitro of the synthesized compounds was performed by the method of scavenging effect on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals. As a result, the highly active compound 4, namely 2-(2,4-dioxothiazolidin-5-ylidene)-N-(5-mercapto-[1,3,4]thiadiazol-2-yl)acetamide was found to be the most efficient candidate among all compounds with a radical scavenging ability of 88.9%, which was comparable that for ascorbic acid (92.7%). The experimentally calculated IC50 value of 43.1 µM for compound 4 was lower than for ascorbic acid (50.5 µM).

scholarly journals IN VITRO ANTIOXIDANT AND IN VIVO ANTIDIABETIC ACTIVITY OF TWO POTENTIAL PROBIOTIC ENTEROCOCCUS SPP. ON ALLOXAN-INDUCED DIABETIC RATS

2021 ◽  
pp. 94-98
Author(s):  
KAMNI RAJPUT ◽  
RAMESH CHANDRA DUBEY
Keyword(s):  
Diabetic Rats ◽  
Antidiabetic Activity ◽  
Control Group ◽  
Albino Rats ◽  
Bacterial Cells ◽  
Bacterial Strains ◽  
Animal Group ◽  
Enterococcus Spp

Objective: In vitro antioxidant activity, in vivo antidiabetic property and intestinal attachment by two potential probiotic bacterial strains, namely, Enterococcus faecium and Enterococcus hirae were studied using albino rats. Methods: Antioxidant the activity was assessed using 2,2-Diphenyl-1-picrylhydrazyl radicals scavenging assay. Alloxan was administered intraperitoneally to induce diabetic conditions in experimental rats. Animals were treated with oral administration of Enterococcus spp., such as E. faecium, and E. hirae isolated from goat and sheep milk. The control animal group received normal saline for the same days. Glibenclamide drug was used as a positive control against probiotic bacterial cells. Results: However, administration of probiotic bacterial strains E. faecium and E. hirae, in albino rats significantly (p<0.05) at varying doses lowered blood glucose levels in diabetic rats as compared to the diabetic control group. Both the species of Enterococcus increased the bodyweight of experimental rats. However, E. faecium was the best antidiabetic strain having the antioxidant activities also in comparison to E. hirae. The attachment of probiotic bacterial cells E. faecium on the rat’s intestine wall against pathogens was examined. Furthermore, E. faecium showed its aggregation with pathogens by attachment of the intestines of albino rats. This showed that both the bacterial strains exhibited in vivo antidiabetic effect. Conclusion: The results of this study showed that probiotic bacteria possess antioxidant, antidiabetic activities, and attachment of intestine.

scholarly journals Protective effects of Trigonella foenum-graecum crude extract over damage induced by Sreptozotocin diabetes rats

2020 ◽  
Vol 10 (4-s) ◽  
pp. 138-141
Author(s):  
Dalila Bencheikh ◽  
Seddik Khennouf ◽  
Saliha Dahamna
Keyword(s):  
Streptozotocin Diabetes ◽  
Diabetic Rats ◽  
Antidiabetic Activity ◽  
Protective Effects ◽  
Traditional Use ◽  
Orogastric Tube ◽  
Trigonella Foenum Graecum ◽  
Male Wistar Rats ◽  
Treatment Of Diabetes

The seeds of Trigonella foenum-graecum (fenugreek) are used for treatment of diabetes mellitus in traditional medicine. This paper examines the protection effects of fenugreek from the damage induced by streptozotocin diabetes rats. Tannins content of T. foenum-graecum was also estimated in vitro. Normoglycemic male Wistar rats, weighing 170-250 g, were selected and randomly divided into five groups (n= 6): normal control, diabetic + TFGE (200mg/kg), diabetic+ TFGE (600mg/kg), diabetic + Glibil (3mg/kg), untreated group. Diabetes was induced after a single intraperitoneal injection of streptozotocin (50 mg/kg body weight) and Fenugreek was given every day via orogastric tube for 18 days. At the end of experiment, rats were sacarificed. Organ weight was estimated of all groups. Trigonella foenum-graecum administration significantly improved the polydipsia, polyphagia, and it also compensated weight loss of diabetic rats (P<0.05, P < 0.01). Moreover, fenugreek had a significant concentration of tannins (806.22 ±0.036 µg TAE/gE). The results revealed that fenugreek improves the damage in diabetic rats that in some ways validates the traditional use of this plant in treatment of diabetes. Keywords: Antidiabetic activity, Protective effect, Streptozotocin, Tannins, Trigonella foenum-graecum

IN-SILICO AND IN VITRO ASSESSMENT OF SYNTHESIZED DIAZENYLSULFONAMIDES AS APOPTOSIS INDUCERS AND RADICAL SCAVENGERS

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (06) ◽  
pp. 49-59
Author(s):  
Priyambada Kshiroda Nandini Sarangi ◽  
Jyotirmaya Sahoo ◽  
Chita Ranjan Sahoo ◽  
Sudhir Kumar Paidesetty ◽  
Guru Prasad Mohanta
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Radical Scavenging ◽  
Cancer Cell Line ◽  
Scavenging Effect ◽  
Ic50 Values ◽  
Radical Scavenging Effect ◽  
The Individual ◽  
Mcf 7

A series of eight quinoline-thiazole hybrid-bearing diazenylsulfonamides, 4a-4h, were synthesized and characterized by UV-Vis, FT/IR, 1H NMR and lC-MS. These compounds were formed when two prepared intermediate precursors of Schiff-base compounds, (E)-N-((2-chloroquinolin-3-yl)methylene)-4phenylthiazol-2-amine (3a) and (E)-N-((2-chloroquinolin-3-yl)methylene)-4-chlorophenylthiazol-2-amine (3b) were converted to the corresponding diazenyl compounds 4a-4h by treating and coupling with the individual diazonium salts of sulfa-drugs. The results of in vitro cytotoxic activity of the synthesized compounds in two cancer cell lines MCF 7 (human breast cancer cell line) and K562 (myelogenousleukemia cell line) have shown the IC50 values as given: 4b against MCF 7 19.52 and against K562 20.55µM; 4d against MCF 7 15.96 and against K562 13.05µM. Moreover, the compound 4-(((Z)-(2-chloroquinolin-3yl)(4-phenylthiazol-2-ylimino)methyl)diazenyl)benzenesulfonic acid (4d) induced maximum percentage of apoptosis. Furthermore, the in vitro antioxidant activity study revealed that among all the synthesized compounds, compound 4d has an excellent radical scavenging effect. Molecular docking was additionally performed to investigate the binding affinity of H-bonding interaction of synthesized compounds with a targeted enzyme and to compare it with the anticancer drugs, dasatinib, bosutinib and dacarbazine.

IN VITRO ANTIOXIDANT AND ALPHA-AMYLASE, ALPHA-GLUCOSIDASE INHIBITORY ACTIVITY OF FLOWERS OF CALOTROPIS GIGANTEA

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (10) ◽  
pp. 38-42
Author(s):  
N. K Choudhary ◽  
◽  
J Dwivedi ◽  
S Sharma
Keyword(s):  
Nitric Oxide ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Chloroform Extract ◽  
Antidiabetic Activity ◽  
Scavenging Activity ◽  
Dpph Radical ◽  
Dpph Radical Scavenging Activity ◽  
Dpph Radical Scavenging

The present investigations were carried out to evaluate the in vitro antioxidant as well as antidiabetic activity of flowers of Calotropis gigantea. Different extracts (petroleum ether, chloroform and ethanolic extract) were prepared using successive solvent extraction method (soxhlet) and screened for its in vitro antioxidant activity using Diphenyl picryl hydrazyl (DPPH) radical scavenging activity, ABT S radical cation decolorization assay and nitric oxide (NO) radical scavenging activity and IC50 were calculated. In vitro antidiabetic activity was studied using α – amylase and α – glucosidase inhibitory assay. Chloroform extract, among the three extracts (i.e. petroleum ether, chloroform and ethanolic), showed maximum antioxidant activity with IC50 value of 151.23µg/ml, 73.56 µg/ml and 158.92µg/ml against DPPH radical scavenging activity, ABTS radical cation decolorization assay and nitric oxide (NO) radical scavenging activity respectively. The chloroform extract produced a significant in vitro antidiabetic activity with IC50 of 52.3µg/ml 18.2µg/ml against α – amylase and α – glucosidase enzymes but less inhibitory effect than standard acarbose.

scholarly journals Effects of Antioxidants in Reducing Accumulation of Fat in Hepatocyte

2018 ◽  
Vol 19 (9) ◽  
pp. 2563 ◽  
Author(s):  
Jung-Pyo Yang ◽  
Ji-Hun Shin ◽  
Seung-Hwan Seo ◽  
Sang-Gyun Kim ◽  
Sang Lee ◽  
...  
Keyword(s):  
Er Stress ◽  
Inflammatory Responses ◽  
Radical Scavenging ◽  
Gene Expressions ◽  
Fat Accumulation ◽  
Scavenging Effect ◽  
Radical Scavenging Effect ◽  
Vitro Model ◽  
Liver Hepatocellular Carcinoma

The progress of the hepatic steatosis (HS), a clinicopathological status, is influenced by cellular oxidative stress, lipogenesis, fatty acid (FA) oxidation, and inflammatory responses. Because antioxidants are gaining attention as potent preventive agents for HS, we aimed to investigate anti-lipogenic effects of the antioxidants vitamin C (VC), N-acetylcysteine (NAC), and astaxanthin (ATX) using hepatocytes. For this, we established an in vitro model using 1 mM oleic acid (OA) and human liver hepatocellular carcinoma (HepG2) cells; 10 μM antioxidants were evaluated for their ability to reduce fat accumulation in hepatocytes. Our results showed that all three antioxidants were effective to reduce fat accumulation for the molecular targets such as reduction in lipid droplets, triglyceride (TG) concentration, reactive oxygen species (ROS) production, and cell apoptosis, as well as in gene expressions of endoplasmic reticulum (ER) stress-related effectors, lipogenesis, and inflammatory cytokines. There were simultaneous increases in diphenyl-1-picrylhydrazyl (DPPH) radical scavenging effect, cell survival, AMPK phosphorylation, NRF2-related gene expression for cellular defense, and FA β-oxidation. However, among these, ATX more effectively inhibited ER stress and lipogenesis at the intracellular level than VC or NAC. Consequently, ATX was also more effective in inhibiting cell death, lipotoxicity, and inflammation. Our result emphasizes that ATX achieved greater lipotoxicity reduction than VC and NAC.

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