scholarly journals Effect of Potentilla Fulgens L. on Selected Enzyme Activities and Altered Tissue Morphology in Diabetic Mice

2018 ◽  
Vol 35 (03) ◽  
pp. 153-160 ◽  
Author(s):  
Suktilang Majaw ◽  
Sooni Challam ◽  
Donkupar Syiem
Keyword(s):  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Eye Lens ◽  
Diabetic Mice ◽  
Ultrastructural Alteration ◽  
Ultrastructural Studies ◽  
Transmission Electron ◽  
Eye Tissues ◽  
Insight Into

Introduction The objective of the present study was to investigate the in vitro inhibitory effect of the Potentilla fulgens extract on amylase, α- and β-glucosidase, and lipase, as well as its effect on the ultrastructure of the liver, of the kidneys, and of the eye tissues in alloxan-induced diabetic mice. The present study was designed to get further insight regarding the action of P. fulgens from what has been previously known and reported about this plant. Materials and Methods Roots of P. fulgens were extracted with 10 volumes of aqueous-methanol solution (1:4), and the prepared extract was used for in vitro inhibitory activity on amylase, α-glucosidase, β-glucosidase, and lipase. Afterwards, the plant extract was intraperitoneally administered for alternated days (250 mg/kg body weight) to diabetic mice for 4 weeks, and an ultrastructural examination of the liver, the kidneys and the eye tissues was performed using a transmission electron microscope (JEM-100 CX II, Jeol Ltd., Tokyo Japan). Results The P. fulgens extract showed inhibitory activity against all the four enzymes (amylase, α- and β-glucosidase, and lipase), with the highest percentage of inhibition (94.57% ± 0.16 at 1 mg/mL) being observed against α-glucosidase when compared with the standard. The ultrastructural studies revealed a distortion in the structure of the nuclei and of the mitochondria in the kidneys and liver tissues of diabetic mice. Distortion of cell shape and disturbed orientation was observed in the eye lens of diabetic mice. The P. fulgens extract reversed/protected/reduced the ultrastructural alteration observed in the tissues (liver, kidney, and eye lens) of diabetic mice. Conclusion The inhibitory effect of the P. fulgens extract against the aforementioned enzymes and its protective effect on the tissues of diabetic mice against alloxan-induced diabetes add further insight into the antidiabetic properties of this plant.

scholarly journals Development of mouthwash with Rosmarinus officinalis extract

2014 ◽  
Vol 50 (4) ◽  
pp. 851-858 ◽  
Author(s):  
Isabela Moreira Baumgratz de Paula ◽  
Flávia Costa Moraes ◽  
Orlando Vieira de Souza ◽  
Célia Hitomi Yamamoto
Keyword(s):  
Sodium Fluoride ◽  
Inhibitory Activity ◽  
Raw Materials ◽  
Ethanol Extract ◽  
Inhibitory Effect ◽  
Rosmarinus Officinalis ◽  
Hexane Fraction ◽  
Diffusion Method ◽  
Oral Infections

Rosmarinus officinalis, which belongs to the Lamiaceaefamily, is a species of medicinal flora with therapeutic properties. In order to exploit the benefits of these properties, a mouthwash formulation was developed, with careful selection of raw materials to meet pharmacotechnical requirements. Extracts of the plant were incorporated into a mouthwash, which was shown to have inhibitory action in vitro against the micro-organisms commonly found in periodontics. Controls for assessing the quality of the drugs were carried out, quantifying phenols and flavonoids as chemical markers. Mouthwash solutions were formulated containing 0.1, 5 and 10% ethanol extract of R. officinalis; and 0.05, 5 and 10% of the hexane fraction of R. officinalis. In order to evaluate synergism, ethanol extract and hexane fraction were also added to formulations containing 0.05% sodium fluoride and 0.12% chlorhexidine digluconate. These formulations were assessed for inhibitory effect against the specific microorganisms involved in the process of bacterial plaque formation, S. mutans(ATCC25175) and C. albicans(ATCC 10231), frequently found in cases of oral infections. The agar diffusion method was used to evaluate the inhibitory activity of extracts and formulations. All mouthwash solutions displayed inhibitory activity having higher sensitivity to S. mutansfor the 5% ethanol extract+0.05% sodium fluoride, and greater sensitivity to C. albicansfor the 10% hexane fraction. Results were characterized by the appearance of a growth inhibition halo, justifying the utilization and association of extracts of R. officinalis.

scholarly journals In vivo hypotensive effect and in vitro inhibitory activity of some Cyperaceae species

2013 ◽  
Vol 49 (4) ◽  
pp. 803-809
Author(s):  
Monica Lacerda Lopes Martins ◽  
Henrique Poltronieri Pacheco ◽  
Iara Giuberti Perini ◽  
Dominik Lenz ◽  
Tadeu Uggere de Andrade ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Colorimetric Assay ◽  
Hypotensive Effect ◽  
Ace Inhibition ◽  
Inhibitory Effect ◽  
Positive Control ◽  
Total Phenolic ◽  
Before And After

In 1820, French naturalist August Saint Hillaire, during a visit in Espírito Santo (ES), a state in southeastern Brazil, reported a popular use of Cyperaceae species as antidote to snake bites. The plant may even have a hypotensive effect, though it was never properly researched. The in vitro inhibitory of the angiotensin converting enzyme (ACE) activity of eigth ethanolic extracts of Cyperaceae was evaluated by colorimetric assay. Total phenolic and flavonoids were determined using colorimetric assay. The hypotensive effect of the active specie (Rhychonospora exaltata, ERE) and the in vivo ACE assay was measured in vivo using male Wistar Kyoto (ERE, 0.01-100mg/kg), with acetylcholine (ACh) as positive control (5 µg/kg, i.v.). The evaluation of ACE in vivo inhibitory effect was performed comparing the mean arterial pressure before and after ERE (10 mg/kg) in animals which received injection of angiotensin I (ANG I; 0,03, 03 and 300 µg/kg, i.v.). Captopril (30 mg/kg) was used as positive control. Bulbostylis capillaris (86.89 ± 15.20%) and ERE (74.89 ± 11.95%, ERE) were considered active in the in vitro ACE inhibition assay, at 100 µg/mL concentration. ACh lead to a hypotensive effect before and after ERE's curve (-40±5% and -41±3%). ERE showed a dose-dependent hypotensive effect and a in vivo ACE inhibitory effect. Cyperaceae species showed an inhibitory activity of ACE, in vitro, as well as high content of total phenolic and flavonoids. ERE exhibited an inhibitory effect on both in vitro and in vivo ACE. The selection of species used in popular medicine as antidotes, along with the in vitro assay of ACE inhibition, might be a biomonitoring method for the screening of new medicinal plants with hypotensive properties.

IN VITRO STUDIES OF SOME EDIBLE SPICES ON PANCREATIC LIPASE INHIBITORY ACTIVITY

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (02) ◽  
pp. 62-68
Author(s):  
S Mhatre ◽  
◽  
A. Bhagit ◽  
R. P Yadav
Keyword(s):  
Pancreatic Lipase ◽  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Syzygium Aromaticum ◽  
High Potency ◽  
Good Source ◽  
Zanthoxylum Armatum ◽  
Methanolic Extracts ◽  
Cinnamomum Tamala

Pancreatic lipase inhibitory effect of some edible spices in light of percent inhibition, efficacy, reversibility/ irreversibility and effect of pH on inhibition is presented here. Lipase inhibitory activities of methanolic extracts of eighteen spices were evaluated. Extracts of Zanthoxylum armatum, Cinnamomum tamala, Syzygium aromaticum and Myristica fragrans were considered to be of high potency in synthetic substrate assay. Only Syzygium aromaticum showed high potency in natural substrate based lipase assay. Zanthoxylum armatum extract displayed lowest IC50 of 9.0 μg/mL. On dialysis, all extracts lost their lipase inhibitory activity indicating reversible nature of inhibition. pH significantly affected the performance of spice extracts during inhibition of pancreatic lipase. Most of the extracts lost their pancreatic lipase inhibitory activity at pH 3.0 with the exception of Brassica nigra and Cinnamomum tamala. Results showed spice are good source of pancreatic lipase inhibitor and its potential as drug for obesity can be explored by addressing various issues.

scholarly journals Phenolic Acids from Lycium barbarum Leaves: In Vitro and In Silico Studies of the Inhibitory Activity against Porcine Pancreatic α-Amylase

Processes ◽  
2020 ◽  
Vol 8 (11) ◽  
pp. 1388
Author(s):  
Luna Pollini ◽  
Alessandra Riccio ◽  
Cristina Juan ◽  
Carmela Tringaniello ◽  
Federica Ianni ◽  
...  
Keyword(s):  
Phenolic Acids ◽  
Inhibitory Activity ◽  
Leaf Extract ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Lycium Barbarum ◽  
Plant Materials ◽  
Vitro Assay ◽  
In Silico Studies

Nowadays, bioactive compounds from vegetable food and waste are of great interest for their inhibitory potential against digestive enzymes. In the present study, the inhibitory activity of methanolic extract from Lycium barbarum leaves on porcine pancreas α-amylase has been studied. The α-amylase inhibitory activity of the constituent phenolic acids was also investigated. The leaves were extracted by ultrasound-assisted method, one of the most efficient techniques for bioactive extraction from plant materials, and then the phenolic acids were identified by Accurate-Mass Quadrupole Time-of-Flight (Q-TOF) Liquid Chromatography/Mass Spectrometry (LC/MS). Chlorogenic and salicylic acids were the most abundant phenolic acids in L. barbarum leaf extract. The inhibitory effect against α-amylase, determined for individual compounds by in vitro assay, was higher for chlorogenic, salicylic, and caffeic acids. L. barbarum leaf extract showed an appreciable α-amylase inhibitory effect in a concentration-dependent manner. Docking studies of the considered phenolic acids into the active site of α-amylase suggested a conserved binding mode that is mainly stabilized through H-bonds and π-π stacking interactions.

Synthesis of Novel Benzimidazole and Benzothiazole Derivatives Bearing a 1,2,3-triazole Ring System and their Acetylcholinesterase Inhibitory Activity

2017 ◽  
Vol 41 (1) ◽  
pp. 30-35 ◽  
Author(s):  
Laleh Faraji ◽  
Shiva Shahkarami ◽  
Hamid Nadri ◽  
Alireza Moradi ◽  
Mina Saeedi ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Docking Simulation ◽  
Triazole Ring ◽  
Copper Catalysts ◽  
Inhibitory Effect ◽  
Ring System ◽  
Benzothiazole Derivatives ◽  
Ache Inhibitory Activity ◽  
Group A

A series of 20 novel benzimidazole and benzothiazole derivatives linked to a 1,2,3-triazole ring system was synthesised, characterised and evaluated for in vitro acetylcholinesterase (AChE) inhibitory activity. Several copper catalysts and solvents were screened to establish the optimal conditions for the preparation of the target compounds. Three different linkers were used to optimise the enzyme inhibitory effect. Out of the 20 compounds, 13 showed some AChE inhibition. The most potent compound, which showed 84% inhibition at 100 μM, contained a 1-(2-fluorobenzyl)-1,2,3-triazole linked to a benzimidazole group. A docking simulation study showed that the most active compound bound preferentially to the catalytic anionic subsite of the AChE enzyme.

Ce-Based Nanoparticles Loaded with Cisplatin for Tumour Radiotherapy

2020 ◽  
Vol 16 (10) ◽  
pp. 1482-1494
Author(s):  
Li Sun ◽  
Chang Jiang ◽  
Wenhai Li ◽  
Zelai He ◽  
Gengming Wang ◽  
...  
Keyword(s):  
Photoelectric Effect ◽  
Inhibitory Effect ◽  
Precipitation Method ◽  
Treatment Mode ◽  
X Ray ◽  
Transmission Electron ◽  
Good Biocompatibility ◽  
Synergistic Inhibitory Effect

The combination of radiotherapy and chemotherapy is a common and useful treatment mode for tumours. But traditional methods inevitably lead to a variety of side effects. A drug delivery system (DDS), which has good biocompatibility and strong anti-tumour ability, is expected to solve this problem. Studies have shown that Ce-based nanoparticles (NPs) have good radiosensitization effect through the photoelectric effect. Hence, cisplatin-loaded LiLuF4 :Ce3+scintillation NPs (NP + Cis) were first constructed in this study, which was synthesized by the crystal precipitation method and characterized by transmission electron microscopy (TEM). Subsequently, its toxicity was verified, and the radiosensitization effect and basic radiosensitization mechanism on tumour cells and tumour-bearing mice were researched. Results showed that NP + Cis triggered massive DNA damage and effectively inhibited cell viability in vitro under the exposure of X-ray irradiation (IR). Moreover, the experiments in vivo showed that the NP + Cis had higher biosafety, which could absorb enough irradiation and produce a synergistic inhibitory effect on tumours through the releasing of Cis. NP + Cis can improve the performance of DDS in chemoradiotherapy.

Inhibitory Effect of Hydroxyapatite Nanoparticles on K562 Cells

2011 ◽  
Vol 685 ◽  
pp. 352-356 ◽  
Author(s):  
Hong Lian Dai ◽  
Pei Chen ◽  
Yin Chao Han ◽  
Xin Yu Wang ◽  
Shi Pu Li
Keyword(s):  
Myeloid Leukemia ◽  
K562 Cells ◽  
Inhibitory Effect ◽  
Inhibition Mechanism ◽  
Hydroxyapatite Nanoparticles ◽  
X Ray Diffraction ◽  
Transmission Electron ◽  
Cell Changes ◽  
Crystallization Degree

HAP Nanoparticles Was Synthesized by Homogeneous Precipitation. the Size Distribution, Crystallization Degree and Morphology of the Precipitation Were Characterized by Laser Granularity Instrument, X-Ray Diffraction (XRD), and Transmission Electron Microscope (TEM) Respectively. the Prepared HAP Nanoparticles Were Used for the Treatment of Human Chronic Myeloid Leukemia K562 Cells. the Inhibition Effect of the Nanoparticles on the Proliferation of K562 Cells Was Measured by MTT Assay and Growth Curve Test. the Results Showed that the HAP Nanoparticles Inhibit the Proliferation of K562 Cells Dramatically in Vitro. the Likely Inhibition Mechanism of HAP Nanoparticles on the K562 Cells Is that the Nanoparticles Entered into the Dells, Induced a Series of Cell Changes, through Cell Death of Apoptosis, Oncosis and Autoschizis, Thus Led to the Death of K562 Cells.

Essential role of follicle stimulating hormone in the maintenance of caprine preantral follicle viability in vitro

Zygote ◽  
2007 ◽  
Vol 15 (2) ◽  
pp. 173-182 ◽  
Author(s):  
M.H.T. Matos ◽  
I.B. Lima-Verde ◽  
M.C.A. Luque ◽  
J.E. Maia Jr ◽  
J.R.V. Silva ◽  
...  
Keyword(s):  
Ovarian Tissue ◽  
Follicle Stimulating Hormone ◽  
Control Medium ◽  
Primordial Follicles ◽  
Ultrastructural Studies ◽  
Follicle Diameter ◽  
Transmission Electron ◽  
Stimulating Hormone

SummaryThe aims of the present study were to investigate the effects of follicle-stimulating hormone (FSH) on survival, activation and growth of caprine primordial follicles using histological and ultrastructural studies. Pieces of caprine ovarian cortex were cultured for 1 or 7 days in minimum essential medium (MEM – control medium) supplemented with different concentrations of FSH (0, 10, 50 or 100 ng/ml). Small fragments from non-cultured ovarian tissue and from those cultured for 1 or 7 days in a specific medium were processed for classical histology and transmission electron microscopy (TEM). Additionally, effects of FSH on oocyte and follicle diameter of cultured follicles were evaluated. The results showed that the lowest percentage of normal follicles was observed after 7 days of culture in control medium. After 1 day of culture, a higher percentage of growing follicles was observed in the medium supplemented with 50 ng/ml of FSH. In the presence of 10 and 50 ng/ml of FSH, an increase in diameter of both oocyte and follicle on day 7 of culture was observed. TEM showed ultrastructural integrity of follicles after 1 day of culture in MEM and after 7 days in MEM plus 50 ng/ml FSH, but did not confirm the integrity of those follicles cultured for 7 days in MEM. In conclusion, this study demonstrated that FSH at concentration of 50 ng/ml not only maintains the morphological integrity of 7 days cultured caprine preantral follicles, but also stimulate the activation of primordial follicles and the growth of activated follicles.

scholarly journals Investigating crosstalk among PTMs provides novel insight into the structural basis underlying the differential effects of Nt17 PTMs on mutant Httex1 aggregation

2021 ◽  
Author(s):  
Anass Chiki ◽  
Zhidian Zhang ◽  
Kolla Rajasekhar ◽  
Luciano A. Abriata ◽  
Iman Rostami ◽  
...  
Keyword(s):  
Inhibitory Effect ◽  
Dynamics Simulation ◽  
Helical Conformation ◽  
Structural Basis ◽  
Similar Distribution ◽  
Post Translational Modifications ◽  
Differential Effects ◽  
The Impact ◽  
Insight Into

AbstractPost-translational modifications (PTMs) within the first 17 amino acids (Nt17) of the Huntingtin protein (Htt) have been shown to inhibit the aggregation and attenuate the toxicity of mutant Htt proteins in vitro and in various models of Huntington’s disease. Our group’s previous studies suggested that the Nt17 PTM code is a combinatorial code that involves a complex interplay between different PTMs. Here, we expand on these studies by investigating the effect of methionine 8 oxidation (oxM8) and crosstalk between this PTM and either lysine 6 acetylation (AcK6) or threonine 3 phosphorylation (pT3) on the aggregation of mutant Httex1. We show that M8 oxidation delays but does not inhibit the aggregation and has no effect on the final morphologies of mutant Httex1 aggregates. This delay in aggregation kinetics could be attributed to the transient accumulation of oligomeric aggregates, which disappear upon the formation of Httex1 oxM8 fibrils. Interestingly, the presence of both oxM8 and AcK6 resulted in dramatic inhibition of Httex1 fibrillization, whereas the presence of oxM8 did not influence the aggregation inhibitory effect of pT3. To gain insight into the structural basis underlying these proteins’ aggregation properties, we investigated the impact of each PTM and the combination of these PTMs on the conformational properties of the Nt17 peptide by circular dichroism spectroscopy and molecular dynamics simulation. These studies show that M8 oxidation decreases the helicity of the Nt17 in the presence or absence of PTMs and provides novel insight into the structural basis underlying the effects of different PTMs on mutant Httex1 aggregation. PTMs that lower the mutant Httex1 aggregation rate (oxM8, AcK6/oxM8, pT3, pT3/oxM8, and phosphorylation at Serine 13) result in stabilization and increased population of a short N-terminal helix (first eight residues) in Nt17 or decreased abundance of other helical forms, including long helix and short C-terminal helix. PTMs that did not alter the aggregation of mutant Httex1 exhibit a similar distribution of helical conformation as the unmodified peptides. These results show that the relative abundance of N- vs. C-terminal helical conformations and long helices, rather than the overall helicity of Nt17, better explains the effect of different Nt17 PTMs on mutant Httex1; thus, explaining the lack of correlation between the effect of PTMs on the overall helicity of Nt17 and mutant Httex1 aggregation in vitro. Taken together, our results provide novel structural insight into the differential effects of single PTMs and crosstalk between different PTMs in regulating mutant Httex1 aggregation.TOC Figure

scholarly journals α-Glucosidase Inhibitory Activity of Phenolic Rich Extracts Obtained from the Seeds of Melastoma saigonense (Kuntze) Merr.

2019 ◽  
Vol 31 (12) ◽  
pp. 2964-2968 ◽  
Author(s):  
Nutthamon Prajudtasri ◽  
Mongkol Nontakitticharoen ◽  
Sujint Anguravirutt
Keyword(s):  
Ethyl Acetate ◽  
Inhibitory Activity ◽  
Total Phenolic Content ◽  
Phenolic Content ◽  
Inhibitory Effect ◽  
Total Phenolic ◽  
Phytochemical Analysis ◽  
Antidiabetic Agent ◽  
Seed Extracts

The aim of this study was to perform a phytochemical analysis of Melastoma saigonense seed extracts and to determine their α-glucosidase inhibitory activity. The extracts from seeds of M. saigonense indicated that the total phenolic content was in the range between 233.46 and 967.22 mg GAE/g DE, whereas the flavonoids content was in the range between 359.96 and 850.84 mg QE/g DE. The present study of antidiabetic inhibitory activity by in vitro α-glucosidase revealed that the crude extracts using ethyl acetate (EA), butanol (BU) and final aqueous residue extracts (AQ) exhibited a strong α-glucosidase inhibitory effect (IC50 4.42-11.95 μg/mL). The ethyl acetate and butanol extracts of seeds of Melastoma saigonense (Kuntze) Merr. were further fractionated by silica gel column chromatography into four fractions (EAF1−EAF4) and five fractions (BUF1−BUF5), respectively and their bioactivities were investigated. The nine fractions exhibited significant α-glucosidase inhibitory activity (p < 0.05) with an IC50 between 3.42-34.77 μg/mL which is less than the IC50 for standard acarbose (IC50 = 507.26 μg/mL). Among all the fractions, BUF1 and EAF1 exhibited high inhibitory activity against α-glucosidase with BUF1 showing the highest inhibitory activity (IC50 = 3.42 μg/mL). The dominant phenolic acids were sinapic, gallic, ferrulic, syringic, gallic and caffeic acids and the prominent flavonoids were myricetin and quercetin. These findings suggest that the seeds of M. saigonense have potential as a source of antidiabetic agent (s).

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