Inhibitory effect of silibinin on Amadori-albumin in diabetes mellitus: A multi-spectroscopic and biochemical approach

2019 ◽  
Vol 209 ◽  
pp. 217-222
Author(s):  
Km Neelofar ◽  
Zarina Arif ◽  
Jamal Ahmad ◽  
Khursheed Alam
Keyword(s):  
Diabetes Mellitus ◽  
Inhibitory Effect ◽  
Biochemical Approach

scholarly journals Investigation on the Enzymatic Profile of Mulberry Alkaloids by Enzymatic Study and Molecular Docking

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1776 ◽  
Author(s):  
Zhihua Liu ◽  
Ying Yang ◽  
Wujun Dong ◽  
Quan Liu ◽  
Renyun Wang ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Molecular Docking ◽  
Side Effects ◽  
Inhibitory Effect ◽  
Active Ingredients ◽  
Wide Range ◽  
Consensus Score

α-glucosidase inhibitors (AGIs) have been an important category of oral antidiabetic drugs being widely exploited for the effective management of type 2 diabetes mellitus. However, the marketed AGIs not only inhibited the disaccharidases, but also exhibited an excessive inhibitory effect on α-amylase, resulting in undesirable gastrointestinal side effects. Compared to these agents, Ramulus Mori alkaloids (SZ-A), was a group of effective alkaloids from natural Morus alba L., and showed excellent hypoglycemic effect and fewer side effects in the Phase II/III clinical trials. Thus, this paper aims to investigate the selective inhibitory effect and mechanism of SZ-A and its major active ingredients (1-DNJ, FA and DAB) on different α-glucosidases (α-amylase and disaccharidases) by using a combination of kinetic analysis and molecular docking approaches. From the results, SZ-A displayed a strong inhibitory effect on maltase and sucrase with an IC50 of 0.06 μg/mL and 0.03 μg/mL, respectively, which was similar to the positive control of acarbose with an IC50 of 0.07 μg/mL and 0.68 μg/mL. With regard to α-amylase, SZ-A exhibited no inhibitory activity at 100 μg/mL, while acarbose showed an obvious inhibitory effect with an IC50 of 1.74 μg/mL. The above analysis demonstrated that SZ-A could selectively inhibit disaccharidase to reduce hyperglycemia with a reversible competitive inhibition, which was primarily attributed to the three major active ingredients of SZ-A, especially 1-DNJ molecule. In the light of these findings, molecular docking study was utilized to analyze their inhibition mechanisms at molecular level. It pointed out that acarbose with a four-ring structure could perform desirable interactions with various α-glucosidases, while the three active ingredients of SZ-A, belonging to monocyclic compounds, had a high affinity to the active site of disaccharidases through forming a wide range of hydrogen bonds, whose affinity and consensus score with α-amylase was significantly lower than that of acarbose. Our study illustrates the selective inhibition mechanism of SZ-A on α-glucosidase for the first time, which is of great importance for the treatment of type 2 diabetes mellitus.

scholarly journals In vitro glycoxidation alters the interactions between collagens and human polymorphonuclear leucocytes

2000 ◽  
Vol 350 (3) ◽  
pp. 777-783 ◽  
Author(s):  
Jean-Claude MONBOISSE ◽  
Laure RITTIE ◽  
Hasnae LAMFARRAJ ◽  
Roselyne GARNOTEL ◽  
Philippe GILLERY
Keyword(s):  
Diabetes Mellitus ◽  
Type I Collagen ◽  
Inhibitory Effect ◽  
Type I ◽  
Polymorphonuclear Leucocytes ◽  
Type Iv ◽  
And Migration ◽  
Significant Stimulatory Effect

Glycation and glycoxidation processes, which are increased in diabetes mellitus, are generally considered causative mechanisms of long-term complications. With reference to our previous studies, type-I and -IV collagens could induce differentially the adhesion and stimulation of polymorphonuclear leucocytes (PMNs). As PMNs play a role in sustained diabetic oxidative stress, the present study was designed to determine whether in vitro glycoxidation of these macromolecules could alter PMN adhesion, activation and migration. The adhesion of PMNs to in vitro-glycoxidized collagens was significantly increased when compared with control collagens: +37% (P < 0.05) and +99% (P < 0.01) for collagens I and IV, respectively. Glycoxidized type-I collagen increased the chemotactic properties of PMNs without significant stimulatory effect on respiratory burst, whereas pre-incubation of PMNs with glycoxidized type-I collagen induced a priming on subsequent stimulation by N-formyl-methionyl-leucyl-phenylalanine. Glycoxidation of type-IV collagen suppressed its inhibitory effect on further PMN stimulation or migration. Collectively, these results indicate that glycoxidation of two major extracellular-matrix collagens considerably alters their ability to modulate PMN migration and production of reactive oxygen species. This imbalance in PMN metabolism may be a major event in the increased oxidative status that characterizes diabetes mellitus.

scholarly journals Inhibition of Growth Hormone Receptor Gene Expression by Saturated Fatty Acids: Role of Krüppel-Like Zinc Finger Factor, ZBP-89

2006 ◽  
Vol 20 (11) ◽  
pp. 2747-2760 ◽  
Author(s):  
Jamuna Thimmarayappa ◽  
Jinhong Sun ◽  
Laura E. Schultz ◽  
Prapai Dejkhamron ◽  
Chunxia Lu ◽  
...  
Keyword(s):  
Gene Expression ◽  
Diabetes Mellitus ◽  
Palmitic Acid ◽  
Receptor Gene ◽  
Inhibitory Effect ◽  
Cis Elements ◽  
Gh Receptor ◽  
Steady State Levels ◽  
Receptor Gene Expression

Abstract The expression and function of the GH receptor is critical for the actions of pituitary GH in the intact animal. The role of systemic factors in the reduced expression of the GH receptor and consequent GH insensitivity in pathological states such as sepsis, malnutrition, and poorly controlled diabetes mellitus is unclear. In the current study, we demonstrate that saturated (palmitic and myristic; 50 μm) fatty acids (FA) inhibit activity of the promoter of the major (L2) transcript of the GH receptor gene; unsaturated (oleic and linoleic) FA (200 μm) do not alter activity of the promoter. Comparable effects with palmitic acid and the nonmetabolizable analog bromo-palmitic acid, and failure of triacsin C to abrogate palmitic acids effects on GH receptor expression indicate that this effect is due to direct action(s) of FA. Palmitic acid, but not the unsaturated FA linoleic acid, decreased steady-state levels of endogenous L2 mRNA and GHR protein in 3T3-L1 preadipocytes. The effect of FA was localized to two cis elements located approximately 600 bp apart on the L2 promoter. EMSA and chromatin immunoprecipitation assays established that both these cis elements bind the Krüppel-type zinc finger transcription factor, ZBP-89. Ectopic expression of ZBP-89 amplified the inhibitory effect of FA on L2 promoter activity and on steady-state levels of endogenous L2 mRNA in 3T3-L1 preadipocytes. Mutational analyses of the two ZBP-89 binding sites revealed that both the sites are essential for palmitic acid’s inhibitory effect on the L2 promoter and for the enhancing effect of ZBP-89 on palmitic acid-induced inhibition of the L2 promoter. Our results establish a molecular basis for FA-induced inhibition of GH receptor gene expression in the pathogenesis of acquired GH insensitivity in pathological states such as poorly controlled diabetes mellitus and small for gestational age.

scholarly journals Chemical Composition andα-Glucosidase Inhibitory Activity of VietnameseCitrusPeels Essential Oils

2016 ◽  
Vol 2016 ◽  
pp. 1-5 ◽  
Author(s):  
Nguyen Hai Dang ◽  
Pham Huong Nhung ◽  
Bui Thi Mai Anh ◽  
Dinh Thi Thu Thuy ◽  
Chau Van Minh ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Chemical Composition ◽  
Essential Oil ◽  
Essential Oils ◽  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Potential Use

Background. Inhibition ofα-glucosidase is an important factor to control postprandial hyperglycemia in type 2 diabetes mellitus.Citrusessential oils (CEO) are among the most widely used essential oils, and some of them exhibited promising antidiabetic effect. However, theα-glucosidase inhibition of CEO has not been investigated so far. The present work aims to evaluate theα-glucosidase inhibition of essential oils from six VietnameseCitruspeels.Methods. The chemical composition of essential oils obtained by hydrodistillation from sixCitruspeels was analyzed by GC-MS. All essential oils were tested for their inhibitory activity onα-glucosidase usingp-nitrophenyl-α-D-glucopyranoside as substrate.Results. In Buddha’s hand and lime peels, the major components were limonene (59.0–61.31%) andγ-terpinene (13.98–23.84%) while limonene (90.95–95.74%) was most abundant in pomelo, orange, tangerine, and calamondin peels. Among the essential oils, the Buddha’s hand oil showed the most significantα-glucosidase inhibitory effect with the IC50value of 412.2 μg/mL. The combination of the Buddha’s hand essential oil and the antidiabetic drug acarbose increased the inhibitory effect.Conclusions. The results suggested the potential use of Buddha’s hand essential oil as an alternative in treatment of type 2 diabetes mellitus.

scholarly journals Modes of Inhibition ofα-Amylase andα-Glucosidase by Aqueous Extract ofMorinda lucidaBenth Leaf

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
M. I. Kazeem ◽  
J. O. Adamson ◽  
I. A. Ogunwande
Keyword(s):  
Diabetes Mellitus ◽  
Aqueous Extract ◽  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Leaf Extracts ◽  
Glucosidase Inhibitors ◽  
Ethanolic Extracts ◽  
Insulin Secretagogues ◽  
Percentage Yield ◽  
Oral Hypoglycemic Drugs

Diabetes mellitus is a metabolic disorder of glucose metabolism. The management of blood glucose level is the hallmark in the treatment of this disease. This may be achieved through the use of oral hypoglycemic drugs such as biguanides, insulin secretagogues, andα-glucosidase inhibitors. The purpose of the present study was to investigate the inhibitory effect ofMorinda lucidaleaf extracts on the activities ofα-amylase andα-glucosidase. This was performed usingα-amylase fromAspergillus oryzaeandα-glucosidase fromSaccharomyces cerevisiae.Aqueous extract ofMorinda lucidagave the highest percentage yield (9.99%) of the plant out of the three extracts (compared to acetone and ethanolic extracts) and possesses the highest inhibitory activity againstα-amylase (IC50value of 2.30 mg/mL) andα-glucosidase (IC50value of 2.00 mg/mL). Kinetic analysis revealed that the aqueous extract of this plant leaf inhibited theα-amylase competitively but displayed mixed noncompetitive mode of inhibition towardsα-glucosidase. It can be concluded that aqueous extract ofMorinda lucidaexhibited the best inhibitory activity on the two enzymes studied and the presence of phytochemicals like flavonoids, saponins, and tannins may have contributed greatly to the inhibitory activity of the plant extract.

Inhibitory effect of gymnemic acid on intestinal absorption of oleic acid in rats

1998 ◽  
Vol 76 (10-11) ◽  
pp. 1017-1023 ◽  
Author(s):  
L F Wang ◽  
H Luo ◽  
M Miyoshi ◽  
T Imoto ◽  
Y Hiji ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Oleic Acid ◽  
Intestinal Absorption ◽  
Inhibitory Effect ◽  
Glucose Absorption ◽  
Gymnema Sylvestre ◽  
Gymnemic Acid ◽  
Acid Absorption ◽  
New Findings ◽  
Dose Dependent

Gymnemic acid, a mixture of triterpene glycosides extracted from the leaves of Gymnema sylvestre, is known to inhibit the intestinal absorption of glucose in human and rats. This work examined the effect of gymnemic acid on oleic acid absorption by the method of intestinal perfusion in rats. The results showed the following. (i) Gymnemic acid potently inhibited the absorption of oleic acid in intestine. (ii) This inhibition was dose dependent and reversible. (iii) The extent of inhibition and the recovery progress were extremely similar to that of glucose absorption. (iv) Taurocholate did not affect the inhibitory effect of gymnemic acid on oleic acid absorption, but lowering its concentration facilitated the recovery from the inhibition. (v) The absorption of oleic acid was not affected by other glycosides such as phloridzin, stevioside, and glycyrrhizin. These new findings are important for understanding the roles of gymnemic acid in therapy of diabetes mellitus and obesity.Key words: gymnemic acid, oleic acid, glucose, intestinal absorption, rat.

scholarly journals The Effect of Bioactive Polyphenols from Anacardium occidentale Linn. Leaves on α-Amylase and Dipeptidyl Peptidase IV Activities

2020 ◽  
Vol 20 (5) ◽  
pp. 1010
Author(s):  
Nur Imanina Abdullah Thaidi ◽  
Hanapi Mat Jusoh ◽  
Ahmad Badruddin Ghazali ◽  
Deny Susanti ◽  
Normah Haron
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Dipeptidyl Peptidase ◽  
Inhibitory Effect ◽  
Dipeptidyl Peptidase Iv ◽  
Anacardium Occidentale ◽  
Mature Leaves ◽  
Young Leaves ◽  
Amylase Inhibitors

Anacardium occidentale Linn. (A. occidentale L.) leaves possess bioactive polyphenols which are associated with antidiabetic potency for the management of type 2 diabetes mellitus (T2DM). In this study, free, soluble ester, and insoluble-bound phenolic fractions from young and mature leaves of A. occidentale L. were extracted. Subsequently, all fractions were investigated for their inhibitory effect on α-amylase and dipeptidyl peptidase IV (DPPIV) activities. Both free (72.45 ± 3.6%) and soluble ester (83.40 ± 4.7%) phenolic fractions in the mature leaves extracts had significantly demonstrated greater α-amylase inhibitors than the young leaves. Likewise, soluble ester (4.09 ± 0.34 µg/mL) and insoluble-bound (4.87 ± 0.32 µg/mL) phenolic fractions in the mature leaves extracts were significantly more effective in inhibiting DPPIV than the young leaves. As for fractions comparison, insoluble-bound derived from the young leaves extract was a more potent α-amylase inhibitor than free and soluble ester phenolic fractions (p < 0.0001). Besides, soluble ester and insoluble-bound phenolic fractions showed a stronger inhibitor of DPPIV than the free phenolic (p < 0.001), irrespective of the maturity of the leaves. In conclusion, this study showed that A. occidentale L. extracts possessed antidiabetic properties, which may potentially be used as an alternative treatment for T2DM management.

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