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 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.

Genomic and nongenomic dose-dependent biphasic effect of aldosterone on Na+/H+ exchanger in proximal S3 segment: role of cytosolic calcium

2008 ◽  
Vol 295 (5) ◽  
pp. F1342-F1352 ◽  
Author(s):  
D. C. A. Leite-Dellova ◽  
M. Oliveira-Souza ◽  
G. Malnic ◽  
M. Mello-Aires
Keyword(s):  
Actinomycin D ◽  
Cytosolic Calcium ◽  
Inhibitory Effect ◽  
Ru 486 ◽  
Nongenomic Action ◽  
Biphasic Effect ◽  
S3 Segment ◽  
Dose Dependent Increase ◽  
Dose Dependent

The effects of aldosterone on the intracellular pH recovery rate (pHirr) via Na+/H+ exchanger and on the [Ca2+]i were investigated in isolated rat S3 segment. Aldosterone [10−12, 10−10, or 10−8 M with 1-h, 15- or 2-min preincubation (pi)] caused a dose-dependent increase in the pHirr, but aldosterone (10−6 M with 1-h, 15- or 2-min pi) decreased it (these effects were prevented by HOE694 but not by S3226). After 1 min of aldosterone pi, there was a transient and dose-dependent increase of the [Ca2+]i and after 6-min pi there was a new increase of [Ca2+]i that persisted after 1 h. Spironolactone, actinomycin D, or cycloheximide did not affect the effects of aldosterone (15- or 2-min pi) but inhibited the effects of aldosterone (1-h pi) on pHirr and on [Ca2+]i. RU 486 prevented the stimulatory effect of aldosterone (10−12 M, 15- or 2-min pi) on both parameters and maintained the inhibitory effect of aldosterone (10−6 M, 15- or 2-min pi) on the pHirr but reversed its stimulatory effect on the [Ca2+]i to an inhibitory effect. The data indicate a genomic (1 h, via MR) and a nongenomic action (15 or 2 min, probably via GR) on [Ca2+]i and on the basolateral NHE1 and are compatible with stimulation of the NHE1 by increases in [Ca2+]i in the lower range (at 10−12 M aldosterone) and inhibition by increases at high levels (at 10−6 M aldosterone) or decreases in [Ca2+]i (at 10−6 M aldosterone plus RU 486).

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.

Antidiabetic Activity and Phytochemical Constituents of Syzygium cumini Leave in Kadipaten, Central Java Indonesia, Indonesia

2021 ◽  
Vol 13 (6) ◽  
pp. 1502-1508
Author(s):  
Zahra Fadhilah ◽  
Berna Elya ◽  
Heri Setiawan ◽  
Gumilar Adhi Nugroho ◽  
Febrika Wediasari ◽  
...  
Keyword(s):  
Antidiabetic Activity ◽  
Syzygium Cumini ◽  
Central Java ◽  
Phytochemical Constituents

5-Methylnicotinamide inhibits renal brush-border phosphate transport with no change in NAD

1986 ◽  
Vol 251 (3) ◽  
pp. F520-F527
Author(s):  
S. A. Kempson
Keyword(s):  
Brush Border ◽  
Phosphate Transport ◽  
Inhibitory Effect ◽  
Renal Brush Border Membrane ◽  
Sodium Gradient ◽  
Nad Synthesis ◽  
Hydrolyzing Enzymes ◽  
Dose Dependent Increase ◽  
Dose Dependent ◽  
Renal Brush Border

Administration of nicotinamide to rats produces a dose-dependent increase in nicotinamide adenine dinucleotide (NAD) content in the renal cortex and specific inhibition of sodium gradient-dependent phosphate transport across the renal brush-border membrane (BBM). Nicotinamide acts both as a precursor for NAD synthesis and as an inhibitor of NAD hydrolysis. To determine if the latter effect contributes to the change in phosphate transport, a nicotinamide analogue was used in the present study. 5-Methylnicotinamide (5MN) cannot support NAD synthesis, but it is an equipotent inhibitor of NAD-hydrolyzing enzymes. The characteristics of the specific inhibitory effect of nicotinamide on sodium gradient-dependent phosphate transport were reproduced by an equimolar dose (4 mmol/kg body wt) of 5MN. Unlike nicotinamide, the action of 5MN did not involve a change in renal cortical NAD content. These data indicate that inhibition of NAD hydrolyzing enzymes may be associated with inhibition of BBM phosphate transport, and this effect occurs independently of changes in NAD levels. These conclusions are supported by the finding that BBM phosphate transport was not inhibited by administration of nicotinic acid, an analogue that does not inhibit NAD hydrolysis.

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.

Modulation of Nitric Oxide Production by Tetracyclines and Chemically Modified Tetracyclines

1998 ◽  
Vol 12 (1) ◽  
pp. 126-130 ◽  
Author(s):  
E. Cillari ◽  
S. Milano ◽  
P. D'Agostino ◽  
G. Di Bella ◽  
M. La Rosa ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Inhibitory Effect ◽  
Inos Mrna ◽  
Mrna Accumulation ◽  
Chemically Modified ◽  
No Formation ◽  
Oxide Synthase ◽  
Chemically Modified Tetracyclines ◽  
Dose Dependent Increase ◽  
Dose Dependent

Chemically modified tetracyclines (CMTs) dose-dependently decreased inducible nitric oxide synthase (iNOS) and, consequently, nitric oxide (NO) formation by the lipopolysaccharide (LPS)-stimulated J774 line. The inhibitory effect was due to a specific reduction in the iNOS protein content in the cells, as attested by Western blot analysis and by the inhibition of iNOS mRNA accumulation. Furthermore, CMTs cause a dose-dependent increase in cell death in the J774 line mediated by the NO-independent apoptotic mechanism.

Plasma growth hormone, somatostatin, insulin and glucagon inter-relationships during infusion of human pancreatic growth hormone-releasing factor in young and adult ducks (Anas platyrhynchos)

1987 ◽  
Vol 114 (1) ◽  
pp. 25-32 ◽  
Author(s):  
Ch. Foltzer-Jourdainne ◽  
S. Harvey ◽  
H. Karmann ◽  
P. Mialhe
Keyword(s):  
Growth Hormone ◽  
Inhibitory Effect ◽  
Insulin Levels ◽  
Gh Secretion ◽  
Plasma Gh ◽  
Glucagon And Insulin ◽  
Rebound Increase ◽  
Dose Dependent Increase ◽  
Dose Dependent ◽  
Infusion Period

ABSTRACT Human pancreatic GH-releasing factor (hpGRF) increased the concentrations of plasma GH when infused i.v. into immature ducks. A dose-dependent increase in plasma GH was observed within 10 min of the start of infusion and was maintained during the 30-min infusion period. Simultaneous infusion of somatostatin S-14 prevented the increase in plasma GH induced by hpGRF, but when the infusion had finished there was a rebound increase in plasma GH. Infusion of the highest dose of hpGRF (800 ng/kg per min) in adult ducks had no significant effect on plasma GH. Plasma somatostatin concentrations were reduced during the infusion of hpGRF in young but not in adult ducks. This observation suggests that the stimulatory effect of hpGRF on GH secretion may be partly due to its inhibitory effect on somatostatin secretion. Infusion of hpGRF in ducklings also increased the concentrations of glucagon and decreased levels of insulin in the plasma. Peripheral plasma glucagon and insulin levels in adult ducks were unaffected by hpGRF infusion. These results indicate that in ducklings, hpGRF increases plasma GH and glucagon concentrations and lowers plasma somatostatin and insulin levels. In the adult, these hormonal responses to hpGRF are not maintained. The highly stimulatory effect of hpGRF on GH secretion in ducklings may explain why plasma GH concentrations are high in these birds. J. Endocr. (1987) 114, 25–32

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.

Increased Expression of u-PA and u-PAR on Monocytes by LDL and Lp(a) Lipoproteins – Consequences for Plasmin Generation and Monocyte Adhesion

1999 ◽  
Vol 81 (04) ◽  
pp. 594-560 ◽  
Author(s):  
Florence Ganné ◽  
Marc Vasse ◽  
Jean-Louis Beaudeu ◽  
Jacqueline Peynet ◽  
Arnaud François ◽  
...  
Keyword(s):  
Fold Increase ◽  
Surface Expression ◽  
Cell Surface Expression ◽  
Atheromatous Plaque ◽  
Monocyte Adhesion ◽  
Blood Monocytes ◽  
Proteolytic Cascade ◽  
Ecm Degradation ◽  
Dose Dependent Increase ◽  
Dose Dependent

SummaryMonocyte-derived foam cells figure prominently in rupture-prone regions of atherosclerotic plaque. As urokinase/urokinase-receptor (u-PA/u-PAR) is the trigger of a proteolytic cascade responsible for ECM degradation, we have examined the effect of atherogenic lipoproteins on monocyte surface expression of u-PAR and u-PA. Peripheral blood monocytes, isolated from 10 healthy volunteers, were incubated with 10 to 200 µg/ml of native or oxidised (ox-) atherogenous lipoproteins for 18 h and cell surface expression of u-PA and u-PAR was analysed by flow cytometry. Both LDL and Lp(a) induced a dose-dependent increase in u-PA (1.6-fold increase with 200 μg/ml of ox-LDL) and u-PAR [1.7-fold increase with 200 μg/ml of ox-Lp(a)]. There is a great variability of the response among the donors, some of them remaining non-responders (absence of increase of u-PA or u-PAR) even at 200 μg/ml of lipoproteins. In positive responders, enhanced u-PA/u-PAR is associated with a significant increase of plasmin generation (1.9-fold increase with 200 μg/ml of ox-LDL), as determined by an amidolytic assay. Furthermore, monocyte adhesion to vitronectin and fibrinogen was significantly enhanced by the lipoproteins [respectively 2-fold and 1.7-fold increase with 200 μg/ml of ox-Lp(a)], due to the increase of u-PAR and ICAM-1, which are receptors for vitronectin and fibrinogen. These data suggest that atherogenous lipoproteins could contribute to the development of atheromatous plaque by increasing monocyte adhesion and trigger plaque weakening by inducing ECM degradation.

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