scholarly journals Evaluating the Inhibitory Effects of Dichloromethane and Methanol Extracts of Salvia macilenta and Salvia officinalis on the Diabetes Marker Enzyme, Alpha-Glucosidase: An Approach for the Treatment of Diabetes

2021 ◽  
Vol In Press (In Press) ◽  
Author(s):  
Hassan Javid ◽  
Soheila Moein ◽  
Mahmood Reza Moein
Keyword(s):  
Glucose Uptake ◽  
Methanol Extract ◽  
Inhibitory Effect ◽  
Salvia Officinalis ◽  
Marker Enzyme ◽  
Inhibitory Effects ◽  
Methanol Extracts ◽  
Treatment Of Diabetes ◽  
Alpha Glucosidase

Background: Diabetes mellitus is believed to be the most serious metabolic disease. One of the treatments for diabetes is to delay glucose uptake by inhibiting carbohydrate-hydrolyzing enzymes. Alpha-glucosidase inhibitors delay glucose uptake. Objectives: The present study was conducted aiming to evaluate the efficacy of Salvia extracts in inhibiting diabetes marker enzymes and their effects on the treatment of diabetes. Methods: This experimental study was performed in vitro. The studied plants included Salvia macilenta and Salvia officinalis. The inhibitory effects of their dichloromethane and methanol extracts were also investigated. After calculating the percentage of inhibition and IC50, Km and Vmax using GraphPad Prism 7 were also calculated. The statistical analysis was performed employing GraphPad Instat 3 software. Results: The results herein showed that the greatest inhibitory effect on alpha-glucosidase belonged to the methanol extract of S. macilenta with IC50 = 8.73 ± 0.26 mg/mL compared to that of acarbose with IC50 = 8.82 ± 0.14 mg/mL as a standard. The IC50 of dichloromethane extract of S. officinalis was 8.95 ± 0.23 mg/mL. Conclusions: The extracts had significant inhibitory effects on alpha-glucosidase. However, methanol extract of S. macilenta and dichloromethane extract of S. officinalis demonstrated the greatest inhibitory effects on alpha-glucosidase compared to acarbose as a standard.

scholarly journals Inhibitory Effect of the Stem Bark Extracts of Albizia chevalieri Harms on the Activity of Alpha-glucosidase Obtained from Aspergillus niger

2019 ◽  
pp. 1-10
Author(s):  
Abdulhafiz Damilola Oso ◽  
Idris Bello ◽  
Yusuf Sa’idu ◽  
Onu Andrew
Keyword(s):  
Ethyl Acetate ◽  
Competitive Inhibition ◽  
Stem Bark ◽  
Inhibitory Effect ◽  
Acetate Buffer ◽  
Bark Extract ◽  
Methanol Extracts ◽  
Glucosidase Activity ◽  
Alpha Glucosidase

The aim of the current study is to evaluate the inhibition of α-glucosidase activity by stem bark extract of Albizia chevalieri. The activity of alpha glucosidase was assayed in vitro using 50 mM acetate buffer pH 6.0 (prepared from acetic acid and sodium acetate) and various concentration of maltose (0.5 mM to 10 mM). Five test tubes, labeled TA – TE, each containing 1.5 ml of acetate buffer, 0.5 ml of alpha glucosidase and 0.5 ml of a known concentration of plant extract and control tubes (CA – CE) were assessed for Alpha glucosidase activity. The results showed that hexane, ethyl acetate and methanol extracts inhibited α-glucosidase activity. The results further indicated that the extracts act by competitive inhibition with inhibition constant of 232 mg/ml, 157 mg/ml and 67 mg/ml for hexane, ethyl acetate and methanol extracts, respectively. The value for the inhibition constants shows that there is a strong binding of the enzyme to the inhibitor as the polarity of solvent increases. The inhibitory activity of Albizia chevalieri may be due one or more of the phytochemicals present in the extracts.

In vitro Physicochemical, Phytochemical, Antimicrobial and Antidiabetic studies on Mucuna pruriens (Linn.) DC seeds

2016 ◽  
Vol 5 (06) ◽  
pp. 4650 ◽  
Author(s):  
Srilakshmi Kusuma* ◽  
Aniel Kumar O. ◽  
Lakshmi Narayana K. ◽  
Sudhakar Pola ◽  
Venkata Reddy K.
Keyword(s):  
Developing Countries ◽  
Methanol Extract ◽  
Mucuna Pruriens ◽  
Bioactive Properties ◽  
Treatment Of Diabetes ◽  
Relative Deficiency ◽  
Alpha Glucosidase ◽  
Crude Methanol Extract ◽  
Seed Extracts

Diabetes is one of the most common endocrine diseases characterized by hyperglycemia due to absolute or relative deficiency of insulin which is currently affecting the citizens of both developed and developing countries. According to Williams textbook of endocrinology in 2013 it was estimated that over 382 million people throughout the world had diabetes. Plants have long been used for the treatment of diabetes, particularly in developing countries where most people have limited resources and do not have access to modern treatment. The presented study is aimed to evaluate the Mucuna pruriens seed extracts for its in vitro physiochemical, phytochemical, antioxidant and anti-diabetic studies. From the studies different solvent extracts of hexane and chloroform showed little or no activity on all assays performed whereas methanol extract of Mucuna pruriens showed significant bio properties. The preliminary studies of this plant crude methanol extract exhibited maximum compounds, hence the methanol extracts have under taken for its alpha amylase and alpha glucosidase inhibition activity. On the basis of the results obtained in the present investigation, it can be concluded that methanol extract of Mucuna pruriens had significant bioactive properties and may provide a support to use of the plant in traditional medicine for the management of diabetes.

scholarly journals Inhibition of Haemoglobin Glycosylation, Glucose Uptake and In Vitro Antidiabetic Activities of Solvent Fractions from Daucus carota Seed

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Habibu Tijjani ◽  
Sadiq Adamu Imam
Keyword(s):  
Diabetes Mellitus ◽  
Glucose Uptake ◽  
Daucus Carota ◽  
Inhibitory Activity ◽  
Seed Extract ◽  
Insulin Deficiency ◽  
Inhibitory Effects ◽  
Organ Systems ◽  
Treatment Of Diabetes

Abstract Diabetes mellitus (DM) is a metabolic disorder which result from either absolute or relative insulin deficiency and may lead to dysfunction in some organ systems. Pancreatic α- glucosidase and α- amylase inhibition are an effective strategy to decrease levels of postprandial hyperglycemia through starch control breakdown. The aim of the study is to assess the in vitro antidiabetic activities of fractions from Daucus carota seed extract, a plant used traditionally for the treatment of diabetes mellitus. The aqueous extract (AQE) of Daucus carota seed was partitioned in ethyl acetate (EAE), n – hexane (HEX) and diethyl ether (DEE) to obtain the various fractions. The AQE and EAE expressed significant α – amylase inhibitory activity with IC50 values of 637.0±18.6 μg/mL and 603.0±25.8 μg/mL respectively. AQE, EAE, HEX and DEE expressed α – glucosidase inhibitory activity with IC50 value of 135.85±1.21, 147.59±0.57, 132.64±1.17, and 143.56±0.49 μg/mL respective compared with acarbose (ACA) with 5.42±0.20 μg/mL. Furthermore, DEE fraction expressed inhibitory effects on % glucose uptake in yeast cell comparable with metronidazole. All Daucus carota fractions expressed various inhibitory effects on haemoglobin glycosylation at a concentration of 200 – 1000 μg/mL. The results show that fractions from the aqueous seed extract of Daucus carota possess in vitro antidiabetic potentials with EAE and HEX fractions having most promising inhibitory activities against α-amylase and α-glucosidase respectively.

In Vitro Effects of Ethanol on Rabbit Platelet Aggregation, Secretion of Granule Contents, and Cyclic AMP Levels in the Presence of Prostacyclin

1989 ◽  
Vol 61 (02) ◽  
pp. 254-258 ◽  
Author(s):  
Margaret L Rand ◽  
Peter L Gross ◽  
Donna M Jakowec ◽  
Marian A Packham ◽  
J Fraser Mustard
Keyword(s):  
Cyclic Amp ◽  
Inhibitory Effect ◽  
Rabbit Platelet ◽  
Inhibitory Effects ◽  
Low Concentrations ◽  
Rabbit Platelets ◽  
High Concentrations ◽  
In Vitro Effects ◽  
Aggregation Of Platelets

SummaryEthanol, at physiologically tolerable concentrations, inhibits platelet responses to low concentrations of collagen or thrombin, but does not inhibit responses of washed rabbit platelets stimulated with high concentrations of ADP, collagen, or thrombin. However, when platelet responses to high concentrations of collagen or thrombin had been partially inhibited by prostacyclin (PGI2), ethanol had additional inhibitory effects on aggregation and secretion. These effects were also observed with aspirin- treated platelets stimulated with thrombin. Ethanol had no further inhibitory effect on aggregation of platelets stimulated with ADP, or the combination of ADP and epinephrine. Thus, the inhibitory effects of ethanol on platelet responses in the presence of PGI2 were very similar to its inhibitory effects in the absence of PGI2, when platelets were stimulated with lower concentrations of collagen or thrombin. Ethanol did not appear to exert its inhibitory effects by increasing cyclic AMP above basal levels and the additional inhibitory effects of ethanol in the presence of PGI2 did not appear to be brought about by further increases in platelet cyclic AMP levels.

scholarly journals Identification of 3-chymotrypsin like protease (3CLPro) inhibitors as potential anti-SARS-CoV-2 agents

2021 ◽  
Vol 4 (1) ◽  
Author(s):  
Vicky Mody ◽  
Joanna Ho ◽  
Savannah Wills ◽  
Ahmed Mawri ◽  
Latasha Lawson ◽  
...  
Keyword(s):  
Inhibitory Effect ◽  
Dynamics Simulation ◽  
Simulation Studies ◽  
Inhibitory Effects ◽  
Major Threat ◽  
Main Protease ◽  
Approved Drugs ◽  
Fda Approved Drugs ◽  
Computational Molecular Modeling

AbstractEmerging outbreak of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) infection is a major threat to public health. The morbidity is increasing due to lack of SARS-CoV-2 specific drugs. Herein, we have identified potential drugs that target the 3-chymotrypsin like protease (3CLpro), the main protease that is pivotal for the replication of SARS-CoV-2. Computational molecular modeling was used to screen 3987 FDA approved drugs, and 47 drugs were selected to study their inhibitory effects on SARS-CoV-2 specific 3CLpro enzyme in vitro. Our results indicate that boceprevir, ombitasvir, paritaprevir, tipranavir, ivermectin, and micafungin exhibited inhibitory effect towards 3CLpro enzymatic activity. The 100 ns molecular dynamics simulation studies showed that ivermectin may require homodimeric form of 3CLpro enzyme for its inhibitory activity. In summary, these molecules could be useful to develop highly specific therapeutically viable drugs to inhibit the SARS-CoV-2 replication either alone or in combination with drugs specific for other SARS-CoV-2 viral targets.

scholarly journals Amphetamine-Decreased Progesterone and Estradiol Release in Rat Granulosa Cells: The Regulatory Role of cAMP- and Ca2+-Mediated Signaling Pathways

Biomedicines ◽  
2021 ◽  
Vol 9 (5) ◽  
pp. 493
Author(s):  
 Chung-Yu Chen ◽  
Chien-Rung Chen ◽  
Chiao-Nan Chen ◽  
Paulus S. Wang ◽  
Toby Mündel ◽  
...  
Keyword(s):  
Granulosa Cells ◽  
Prostaglandin F2α ◽  
Inhibitory Effect ◽  
Inhibitory Effects ◽  
Steroidogenic Enzyme ◽  
Estradiol Secretion ◽  
Basal Release ◽  
Ca2 Channels

The purpose of this study is to evaluate the amphetamine effects on progesterone and estradiol production in rat granulosa cells and the underlying cellular regulatory mechanisms. Freshly dispersed rat granulosa cells were cultured with various test drugs in the presence of amphetamine, and the estradiol/progesterone production and the cytosolic cAMP level were measured. Additionally, the cytosolic-free Ca2+ concentrations ([Ca2+]i) were measured to examine the role of Ca2+ influx in the presence of amphetamine. Amphetamine in vitro inhibited both basal and porcine follicle-stimulating hormone-stimulated estradiol/progesterone release, and amphetamine significantly decreased steroidogenic enzyme activities. Adding 8-Bromo-cAMP did not recover the inhibitory effects of amphetamine on progesterone and estradiol release. H89 significantly decreased progesterone and estradiol basal release but failed to enhance a further amphetamine inhibitory effect. Amphetamine was capable of further suppressing the release of estradiol release under the presence of nifedipine. Pretreatment with the amphetamine for 2 h decreased the basal [Ca2+]i and prostaglandin F2α-stimulated increase of [Ca2+]i. Amphetamine inhibits progesterone and estradiol secretion in rat granulosa cells through a mechanism involving decreased PKA-downstream steroidogenic enzyme activity and L-type Ca2+ channels. Our current findings show that it is necessary to study the possibility of amphetamine perturbing reproduction in females.

scholarly journals In Vitro α-Glucosidase and α-Amylase Inhibitory Activities of Free and Bound Phenolic Extracts from the Bran and Kernel Fractions of Five Sorghum Grain Genotypes

Foods ◽  
2020 ◽  
Vol 9 (9) ◽  
pp. 1301
Author(s):  
Yun Xiong ◽  
Ken Ng ◽  
Pangzhen Zhang ◽  
Robyn Dorothy Warner ◽  
Shuibao Shen ◽  
...  
Keyword(s):  
Digestive System ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Inhibitory Effects ◽  
Phenolic Contents ◽  
Inhibitory Activities ◽  
Sorghum Grain ◽  
Global Health Challenge ◽  
Phenolic Extracts

Diabetes is a global health challenge. Currently, an effective treatment for diabetes is to reduce the postprandial hyperglycaemia by inhibiting the carbohydrate hydrolysing enzymes in the digestive system. In this study, we investigated the in vitro α-glucosidase and α-amylase inhibitory effects of free and bound phenolic extracts, from the bran and kernel fractions of five sorghum grain genotypes. The results showed that the inhibitory effect of sorghum phenolic extracts depended on the phenolic concentration and composition. Sorghum with higher phenolic contents generally had higher inhibitory activity. Among the tested extracts, the brown sorghum (IS131C)-bran-free extract (BR-bran-free, half-maximal inhibitory concentration (IC50) = 18 ± 11 mg sorghum/mL) showed the strongest inhibition against α-glucosidase which was comparable to that of acarbose (IC50 = 1.39 ± 0.23 mg acarbose/mL). The red sorghum (Mr-Buster)-kernel-bound extract (RM-kernel-bound, IC50 = 160 ± 12 mg sorghum/mL) was the most potent in inhibiting α-amylase but was much weaker compared to acarbose (IC50 = 0.50 ± 0.03 mg acarbose/mL).

A STUDY OF THE INHIBITORY EFFECTS OF CHICK WHOLE EYE EXTRACT ON THE DEVELOPMENT OF THE LENS OF THE CHICK EMBRYO IN VITRO

1966 ◽  
Vol 44 (4) ◽  
pp. 661-676 ◽  
Author(s):  
Robert P. Thompson
Keyword(s):  
Chick Embryo ◽  
Nutrient Medium ◽  
Inhibitory Effect ◽  
Reactive System ◽  
Vesicle Formation ◽  
Inhibitory Effects ◽  
Muscle Extract ◽  
Lens Vesicle ◽  
And Control

To demonstrate the phenomenon of homologous inhibition by clearly interpretable results in a readily reactive system, experiments were carried out to study the effect of chick whole eye extract on the development of the vesicular lens of the chick embryo in vitro. The heads of embryos of 11 through 13 somites were explanted onto nutrient medium diluted with varying amounts of the extract, and cultured for 30 hours. A total of 35 embryos exposed to concentrations of 1:1, 1:2, and 1:4 (extract to medium) showed complete inhibition of lens vesicle formation. Of a total of 53 embryos on concentrations of 1:8, 1:16, 1:32, and 1:64, more than 50% showed inhibition of vesicle formation. The inhibitory effect disappeared at a concentration of 1:128. Control material exposed to some equivalent concentrations of nutrient medium – saline mixtures showed inhibition of vesicle formation in only 15% of 33 embryos. Of a total of 27 control embryos exposed to ventricular muscle extract, approximately one-third showed inhibition of vesicle formation at concentrations of 1:8 and 1:16, with the inhibitory effect disappearing at 1:32. The implications of this result are discussed. Other factors and control experiments are described and their value is assessed.

scholarly journals In Vitro Efficacy of Aqueous and Methanol Extract of Cassia siamea Against the Motility of Caenorhabditis elegans

2020 ◽  
Vol 31 (3) ◽  
pp. 145-159
Author(s):  
Haladu Ali Gagman ◽  
Nik Ahmad Irwan Izzauddin Nik Him ◽  
Hamdan Ahmad ◽  
Shaida Fariza Sulaiman ◽  
Rahmad Zakaria ◽  
...  
Keyword(s):  
Caenorhabditis Elegans ◽  
Methanol Extract ◽  
Anthelmintic Resistance ◽  
Gastrointestinal Nematode ◽  
Parasitic Nematodes ◽  
Cassia Siamea ◽  
Methanol Extracts ◽  
C Elegans ◽  
Significant Difference

Gastrointestinal nematode infections can cause great losses in revenue due to decrease livestock production and animal death. The use of anthelmintic to control gastrointestinal nematode put a selection pressure on nematode populations which led to emergence of anthelmintic resistance. Because of that, this study was carried out to investigate the efficacy of aqueous and methanol extract of Cassia siamea against the motility of C. elegans Bristol N2 and C. elegans DA1316. Caenorhabditis elegans Bristol N2 is a susceptible strain and C. elegans DA1316 is an ivermectin resistant strain. In vitro bioassay of various concentrations of (0.2, 0.6, 0.8, 1.0 and 2.0 mg mL–1) aqueous and methanol extracts of C. siamea was conducted against the motility of L4 larvae of C. elegans Bristol N2 and C. elegans DA1316. The L4 larvae were treated with 0.02 μg mL–1 of ivermectin served as positive control while those in M9 solution served as negative control. The activity of the extracts was observed after 24 h and 48 h. A significant difference was recorded in the extract performance compared to control at (P < 0.001) after 48 h against the motility of the larvae of both strains. The methanol extracts inhibited the motility of C. elegans Bristol N2 by 86.7% as well as DA1316 up to 84.9% at 2.0 mg mL–1 after 48 h. The methanol extract was more efficient than aqueous extract (P < 0.05) against the motility of both strains of C. elegans. Cassia siamea may be used as a natural source of lead compounds for the development of alternative anthelmintic against parasitic nematodes as well ivermectin resistant strains of nematodes.

scholarly journals Inhibitory effects of pentamidine analogues on protein biosynthesis in vitro.

2000 ◽  
Vol 47 (1) ◽  
pp. 113-120 ◽  
Author(s):  
K Bielawski ◽  
A Galicka ◽  
A Bielawska ◽  
K Sredzińska
Keyword(s):  
Protein Biosynthesis ◽  
Elongation Factor ◽  
Inhibitory Effect ◽  
New Drugs ◽  
Clinical Use ◽  
Inhibitory Effects ◽  
Inhibit Protein Synthesis ◽  
Primary Target ◽  
Eukaryotic Elongation Factor

Pentamidine despite its rather high toxicity, is currently in clinical use. For development of new drugs of this type it is important to know the mechanism of their action. Two new amidines (I and II) and 4',6-diamidino-2-phenylindole (DAPI) were found in preliminary experiments to inhibit protein synthesis in vitro in the cell-free rat liver system. The three compounds differed in the precise mode of action. The inhibitory effect of I on the activity of the eukaryotic elongation factor eEF-2 and ribosomes seems to suggest that the binding site of eEF-2 on the ribosome was blocked by this compound. eEF-2 has been identified as the primary target of II and eEF-1 as the primary target of DAPI in the system studied.

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