scholarly journals In-Vitro Antidiabetic Effect of Ziziphus mucronata Leave Extracts

2021 ◽  
Vol 11 (6-S) ◽  
pp. 9-13
Author(s):  
Olaitan Kabir Abolaji ◽  
A.N. Ukwuani-Kwaja ◽  
I Sani ◽  
M.N. Sylvester
Keyword(s):  
Glucose Production ◽  
Inhibitory Effect ◽  
Alpha Amylase ◽  
Antidiabetic Activity ◽  
Anthraquinone Glycosides ◽  
Enzymes Inhibition ◽  
Ziziphus Mucronata ◽  
Dose Dependent Increase ◽  
Dose Dependent

Background: Diabetes is a metabolic disorder characterized by hyperglycemia due to the body’s inability to produce insulin or inaction of the produced insulin or a combination of both. One antidiabetic therapeutic approach is to reduce gastrointestinal glucose production and absorption through the inhibition of carbohydrate digesting enzymes such as alpha-amylase as well as through the inhibition of hemoglobin glycosylation. Objective: This study sets out to evaluate the in vitro antidiabetic activity of Ziziphus mucronata extracts for their effect on alpha-amylase and glycosylation of hemoglobin. Methods: Successive gradient maceration of Z. mucronata leaves were carried out using Hexane, Acetone, Methanol and separately with water to obtain four (4) extracts labelled HE, AE, ME, and WE respectively. These were subjected to in vitro studies for their inhibitory effect on alpha-amylase and hemoglobin glycosylation, Standard laboratory methods were used to screen for phytochemicals of the most potent extract. Results: The result showed that AE, ME and WE extract exhibited a dose-dependent increase in percentage inhibition of both alpha-amylase and hemoglobin glycosylation. However, on a stricking note, the AE showed a more potent data result with percentage (%) potency of 71.02 at 1mg/ml, the lowest glucose concentration (of 25mg/ml) at 0.242nm as well as the highest hemoglobin glycosylation inhibitory mean concentration of 3.663nm after 72 hours. The AE of Z. mucronata (the most potent) revealed the presence of alkaloids, anthraquinone, glycosides, flavonoids, phenols, saponin, tanins and terpenoids. Conclusion: Thus, the Acetone extract is more likely to give a lead antidiabetic drug molecule of drug when further explored; which somewhat justify the folkloric claims of Z. mucronata leave as an antidiabetic. Keywords: Heamoglabin glycosylation, Alpha-amylase enzymes, Inhibition, Glucose.

scholarly journals Antidiabetic Activity and Phytochemical Constituents of Syzygium cumini Seeds in Puducherry Region, South India

2018 ◽  
Vol 9 (07) ◽  
Author(s):  
Kandan Prabakaran ◽  
Govindan Shanmugave
Keyword(s):  
Inhibitory Effect ◽  
Seed Extract ◽  
Antidiabetic Activity ◽  
Appreciable Amount ◽  
Syzygium Cumini ◽  
Characteristic Functional ◽  
Infrared Spectral ◽  
Phytochemical Constituents ◽  
Dose Dependent Increase ◽  
Dose Dependent

Syzygium cumini is widely used in traditional medicine to treat diabetes in India. The present study was carried out to evaluate the phytochemical bioactive compounds from Syzygium cumini seed extract and its invitro anti-diabetic activity. The phytochemical screening showed appreciable amount of flavonoid and steroid in the seed extract. The infrared spectral data obtained revealed the presence of characteristic functional groups of alcohol, hydroxyl, aldehydes, alkanes, alkenes, nitro compound and aliphatic amines etc. The extract exhibits the dose-dependent increase in the inhibitory effect on alphaamylase enzyme upto 95.4%. The result suggested that significant amount of flavonoid in Syzygium cumini seed is responsible for antidiabetic properties and it is further confirmed by higher intensity of alpha amylase inhibitory effect.

scholarly journals Assessment of In Vitro Antidiabetic Potential of Purified Anthocyanin Extract from Floral Petals of Wild Balsam Species

2020 ◽  
Vol 10 (3) ◽  
pp. 31-35
Author(s):  
R ARATHY ◽  
K MURUGAN ◽  
KV DINESH BABU ◽  
GS MANOJ
Keyword(s):  
International Diabetes Federation ◽  
Inhibitory Effect ◽  
Alpha Amylase ◽  
Herbal Remedies ◽  
Antidiabetic Activity ◽  
Public Health Issue ◽  
Impatiens Balsamina ◽  
Alpha Glucosidase

Diabetes is a notorious and growing clinical and public health issue. The International Diabetes Federation assumes that 592 million had diabetes by 2035 and that by 2040 the number will increase to 642 million. Cardiovascular corollary accounts for four million deaths annually attributable to diabetes. Evidence reveals that certain glucose-lowering phytochemicals can improve vascular outcomes with type 2 diabetes, which, together with better understanding of using multiple therapies concurrently, offers opportunities for beneficial personalization of medication regimens. Anthocyanins are coloured pigments and are natural antioxidants. Keeping this in focus, this study was undertaken to evaluate the in vitro antidiabetic activity in the petals of wild Impatiens balsamina L. The anthocyanin was extracted from floral petals of wild balsam species and purified to homogeneity using chromatographic techniques. Evaluation of in vitro antidiabetic properties of anthocyanin extract revealed a dose-dependent increase in the inhibitory effect on the alpha-glucosidase (200 μg/ml) and alpha-amylase enzymes (500 μg/ml) and was comparable with the standard acarbose drug (189 μg/ml and 50 μg/ml). These results indicated that anthocyanin could be used as a source of functional food and nutraceuticals. This information from wild species will be useful in finding more potent antidiabetic principle from the natural resources for the clinical development of antidiabetic therapeutics. Future studies are planned to substantiate the antidiabetic power of anthocyanin using in vivo animal models. Keywords: Alpha amylase, alpha glucosidase, diabetes, herbal remedies, Impatiens balsamina L.

scholarly journals INHIBITORY EFFECT OF A STANDARDIZED HYDROETHANOLIC EXTRACT OF TERMINALIA ARJUNA BARK ON ALPHA-AMYLASE ENZYMEINHIBITORY EFFECT OF A STANDARDIZED HYDROETHANOLIC EXTRACT OF TERMINALIA ARJUNA BARK ON ALPHA-AMYLASE ENZYME

2018 ◽  
Vol 11 (4) ◽  
pp. 366 ◽  
Author(s):  
Sushant A Shengule ◽  
Sanjay Mishra ◽  
Shweta Bodhale
Keyword(s):  
Inhibitory Activity ◽  
High Performance ◽  
Soxhlet Extraction ◽  
Inhibitory Effect ◽  
Alpha Amylase ◽  
Antidiabetic Activity ◽  
Bark Extract ◽  
Terminalia Arjuna ◽  
Hydroethanolic Extract

 Objective: The present study was initiated to screen the hydroethanolic bark extract for α-amylase inhibitory activity and standardization of the Terminalia arjuna for polyphenolic phytochemicals using high-performance liquid chromatography-photo diode array (HPLC-PDA) method.Methods: The T. arjuna bark sample was extracted with ethanol: water (70:30 v/v) using Soxhlet extraction. A Dionex P680 HPLC system was used to acquire chromatograms. The screening of extract of T. arjuna bark has performed for in vitro α-amylase inhibitory assay. Each experiment was repeated 3 times. All values were expressed mean ± standard deviation.Results: The content of arjunetin, arjungenin, gallic acid, ellagic acid, and quercetin was 0.47, 8.22, 2.443, 7.901, and 3.20 mg/g, respectively, in a hydroethanolic extract of T. arjuna. The hydroethanolic extract of T. arjuna bark and acarbose has shown an inhibitory activity with an IC50 value 145.90 and 62.35 μg/mL, respectively.Conclusion: The hydroethanolic extract T. arjuna bark demonstrates α-amylase inhibitory activity due to a synergistic effect of the phytochemical constituents present in it. This study suggests that one of the mechanisms of this plant for antidiabetic activity is through the inhibition of α-amylase enzyme.

Effect of five fungicides on growth and ochratoxin A production by two Aspergillus carbonarius and Aspergillus niger isolated from Moroccan grapes

2014 ◽  
Vol 4 (3) ◽  
pp. 118-126
Author(s):  
Souad Zouhair ◽  
Souad Qjidaa Qjidaa ◽  
Atar Selouane ◽  
Driss Bouya ◽  
Cony Decock ◽  
...  
Keyword(s):  
Growth Rate ◽  
Ochratoxin A ◽  
Fungal Growth ◽  
Inhibitory Effect ◽  
Aspergillus Carbonarius ◽  
Total Inhibition ◽  
Germination And Growth ◽  
Dose Dependent Increase ◽  
Dose Dependent

Five fungicides azoxystrobin (ortiva), benomyl (benlate), hexaconazole (hexa), pyrimethanil (scala) and thiabendazole (tectocal) were tested sepa-rately in vitro for their ability to inhibit the growth of two ochratoxigenic strains of A. niger and A. carbonarius previously isolated from grapes. All fungicides effectively reduced the growth rate of A. carbonarius and A. niger from 34 to 100% at the recommended dose (RD). Thiabendazole caused total inhibition of spore germination and growth of the two strains, regardless of the doses assayed. Benomyl completely inhibited growth of A. niger whereas for A. carbonarius, concentrations above 0.02xRD were required to prevent the growth. The inhibitory effect of hexaconazole, azoxystrobin and pyrime-thanil was dose-dependent. At sub-lethal concentrations of three fungicides, a dose-dependent increase in in ochratoxin A biosynthesis by two strains was observed. The use of fungicide should be checked for its ability to inhibit fungal growth as well as for their effect in terms of mycotoxins biosynthesis.

scholarly journals PF-06869206 is a selective inhibitor of renal Pi transport: evidence from in vitro and in vivo studies

2020 ◽  
Vol 319 (3) ◽  
pp. F541-F551
Author(s):  
Linto Thomas ◽  
Jianxiang Xue ◽  
Viktor N. Tomilin ◽  
Oleh M. Pochynyuk ◽  
Jessica A. Dominguez Rieg ◽  
...  
Keyword(s):  
Collecting Duct ◽  
Inhibitory Effect ◽  
In Vivo Studies ◽  
Open Probability ◽  
Ok Cells ◽  
Increased Risk ◽  
Dose Dependent Increase ◽  
Dose Dependent

Plasma phosphate (Pi) levels are tightly controlled, and elevated plasma Pi levels are associated with an increased risk of cardiovascular complications and death. Two renal transport proteins mediate the majority of Pi reabsorption: Na+-phosphate cotransporters Npt2a and Npt2c, with Npt2a accounting for 70–80% of Pi reabsorption. The aim of the present study was to determine the in vitro effects of a novel Npt2a inhibitor (PF-06869206) in opossum kidney (OK) cells as well as determine its selectivity in vivo in Npt2a knockout (Npt2a−/−) mice. In OK cells, Npt2a inhibitor caused dose-dependent reductions of Na+-dependent Pi uptake (IC50: ~1.4 μmol/L), whereas the unselective Npt2 inhibitor phosphonoformic acid (PFA) resulted in an ~20% stronger inhibition of Pi uptake. The dose-dependent inhibitory effects were present after 24 h of incubation with both low- and high-Pi media. Michaelis-Menten kinetics in OK cells identified an ~2.4-fold higher Km for Pi in response to Npt2a inhibition with no significant change in apparent Vmax. Higher parathyroid hormone concentrations decreased Pi uptake equivalent to the maximal inhibitory effect of Npt2a inhibitor. In vivo, the Npt2a inhibitor induced a dose-dependent increase in urinary Pi excretion in wild-type mice (ED50: ~23 mg/kg), which was completely absent in Npt2a−/− mice, alongside a lack of decrease in plasma Pi. Of note, the Npt2a inhibitor-induced dose-dependent increase in urinary Na+ excretion was still present in Npt2a−/− mice, a response possibly mediated by an off-target acute inhibitory effect of the Npt2a inhibitor on open probability of the epithelial Na+ channel in the cortical collecting duct.

scholarly journals An In vitro Evaluation of Antidiabetic Activity of Alpinia galangal and Alpinia calcarata

2021 ◽  
pp. 28-35
Author(s):  
V. Miss Revathi ◽  
G. Anuradha ◽  
S. Sumathy
Keyword(s):  
Inhibitory Effect ◽  
Antidiabetic Activity ◽  
Dependent Manner ◽  
In Vitro Evaluation ◽  
Alpinia Galanga ◽  
Phytochemical Content ◽  
The Family ◽  
Potential Alternative ◽  
Dose Dependent

Background: The herbs, genus Alpinia calcarata and Alpinia galanga that underneath the family Zingiberaceae are rhizomatous and extremely aromatic. The study is to investigate the anti-diabetic activity of Alpinia galanga and Alpinia calcarata in-vitro. Material and Methods: The inhibitory effect of Alpinia galanga and Alpinia calcarata on α-amylase and α-glucosidase activities were evaluated. Results: The results revealed that both Alpinia galanga and Alpinia calcarata inhibited α-amylase and α-glucosidase activities in a dose-dependent manner (200–1000 μg/mL). However, Alpinia calcarata possess better antidiabetic activity than Alpinia galangal. Conclusion: The presence of phenolic and other phytochemical content in the herbs might be the reason for their ability to inhibit α-amylase and α-glucosidase activities. Thus, the drug formulating from the herbs, Alpinia galanga and Alpinia calcarata could be part of the potential alternative for synthetic anti-diabetic drug.

scholarly journals IN VITRO STUDIES ON THE ANTIDIABETIC ACTIVITY OF 2-THIOHYDANTOIN USING α-amylase AND α-GLUCOSIDASE

2019 ◽  
pp. 155-157 ◽  
Author(s):  
UMA S ◽  
DEVIKA PT
Keyword(s):  
Therapeutic Approach ◽  
Enzyme Assay ◽  
Inhibitory Concentration ◽  
Glucose Production ◽  
Inhibitory Effect ◽  
In Vitro Studies ◽  
Antidiabetic Activity

Objective: The aim of the present study was to investigate the inhibitory effect of 2-thiohydantoin on the enzymes α-amylase and α-glucosidase in vitro as an antidiabetic therapeutic approach to reduce gastrointestinal glucose production. Methods: Antidiabetic activity of the compound, 2-thiohydantoin was measured using the enzymes α-amylase and α-glucosidase. Results: Half-maximal inhibitory concentration of the antidiabetic α-amylase was found to be 410.35 μg/ml and α-glucosidase was found to be 356.33 μg/ml, respectively. Conclusion: The result obtained in the in vitro enzyme assay suggests the antidiabetic activity of 2-thiohydantoin.

scholarly journals In Vitro Effects of Doxycycline on Replication of Feline Coronavirus

Pathogens ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 312
Author(s):  
Magdalena Dunowska ◽  
Sayani Ghosh
Keyword(s):  
Inhibitory Concentration ◽  
Infectious Virus ◽  
Treatment Options ◽  
Inhibitory Effect ◽  
Virus Titration ◽  
Reverse Transcription Quantitative Pcr ◽  
In Vitro Effects ◽  
Dose Dependent ◽  
Feline Coronavirus

Feline infectious peritonitis (FIP) is a sporadic fatal disease of cats caused by a virulent variant of feline coronavirus (FCoV), referred to as FIP virus (FIPV). Treatment options are limited, and most of the affected cats die or are euthanized. Anecdotally, doxycycline has been used to treat FIP-affected cats, but there are currently no data to support or discourage such treatment. The aim of this study was to establish whether doxycycline inhibits replication of FIPV in vitro. The virus was cultured in Crandell-Rees feline kidney cells with various concentrations of doxycycline (0 to 50 µg/mL). The level of FIPV in cultures was determined by virus titration and FCoV-specific reverse-transcription quantitative PCR. Cell viability was also monitored. There was no difference in the level of infectious virus or viral RNA between doxycycline-treated and untreated cultures at 3, 12- and 18-hours post-infection. However, at 24 h, the growth of FIPV was inhibited by approximately two logs in cultures with >10 µg/mL doxycycline. This inhibition was dose-dependent, with inhibitory concentration 50% (IC50) 4.1 µg/mL and IC90 5.4 µg/mL. Our data suggest that doxycycline has some inhibitory effect on FIPV replication in vitro, which supports future clinical trials of its use for the treatment of FIP-affected cats.

scholarly journals In vitro study on the effect of cornin on the activity of cytochrome P450 enzymes

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Qun Zhang ◽  
Zengqiang Qu ◽  
Yanqing Zhou ◽  
Jin Zhou ◽  
Junwei Yang ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interaction ◽  
Liver Microsomes ◽  
In Vitro Study ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Cytochrome P450 Enzymes ◽  
Drug Drug Interaction ◽  
Dose Dependent

Abstract Background Cornin is a commonly used herb in cardiology for its cardioprotective effect. The effect of herbs on the activity of cytochrome P450 enzymes (CYP450s) can induce adverse drug-drug interaction even treatment failure. Therefore, it is necessary to investigate the effect of cornin on the activity of CYP450s, which can provide more guidance for the clinical application of cornin. Methods Cornin (100 μM) was incubated with eight isoforms of CYP450s, including CYP1A2, 2A6, 3A4, 2C8, 2C9, 2C19, 2D6, and 2E1, in pooled human liver microsomes. The inhibition model and corresponding parameters were also investigated. Results Cornin exerted significant inhibitory effect on the activity of CYP3A4, 2C9, and 2E1 in a dose-dependent manner with the IC50 values of 9.20, 22.91, and 14.28 μM, respectively (p < 0.05). Cornin inhibited the activity of CYP3A4 non-competitively with the Ki value of 4.69 μM, while the inhibition of CYP2C9 and 2E1 by cornin was competitive with the Ki value of 11.31 and 6.54 μM, respectively. Additionally, the inhibition of CYP3A4 by cornin was found to be time-dependent with the KI/Kinact value of 6.40/0.055 min− 1·μM− 1. Conclusions The inhibitory effect of cornin on the activity of CYP3A4, 2C9, and 2E1 indicated the potential drug-drug interaction between cornin and drugs metabolized by these CYP450s, which needs further investigation and validation.

Immunomodulatory activities of whey fractions in efferent prefemoral lymph of sheep

1996 ◽  
Vol 63 (2) ◽  
pp. 257-267 ◽  
Author(s):  
Chun W. Wong ◽  
Geoffrey O. Regester ◽  
Geoffrey L. Francis ◽  
Dennis L. Watson
Keyword(s):  
Immune Responses ◽  
Bovine Milk ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Milk Whey ◽  
Significant Difference ◽  
Lymphocyte Phenotypes ◽  
Dose Dependent

SummaryStudies on the immunomodulatory activities of ruminant milk and colostral whey fractions were undertaken. By comparing with boiled colostral whey in a preliminary experiment, a putative heat-labile immunostimulatory factor for antibody responses was found to be present in ovine colostral whey. Studies were then undertaken in sheep in which the efferent prefemoral lymphatic ducts were cannulated bilaterally, and immune responses in the node were measured following subcutaneous injection in the flank fold of whey protein preparations of various purities. A significant sustained decline of efferent lymphocyte output was observed following injection with autologous crude milk whey or colostral whey preparations, but no changes were observed in interferon-gamma levels in lymph plasma. Two bovine milk whey fractions (lactoperoxidase and lactoferrin) of high purity were compared in bilaterally cannulated sheep. A transient decline over the first 6 h was seen in the efferent lymphocyte output and lymph flow rate after injection of both fractions. A significant difference was seen between the two fractions in interferongamma levels in lymph at 6 h after injection. However, no significant changes in the proportion of the various efferent lymphocyte phenotypes were seen following either treatment. Whereas both fractions showed a significant inhibitory effect in a dose-dependent manner on the proliferative response of T lymphocytes, but not B lymphocytes, to mitogenic stimulation in vitro, no similar changes were seen following in vivo stimulation with these two fractions.

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