scholarly journals Identification of Major α-Glucosidase Inhibitors from Stem Bark of Panamanian Mangrove Plant Pelliciera rhizophorae

2019 ◽  
Vol 14 (1) ◽  
pp. 1934578X1901400
Author(s):  
Lilia Cherigo ◽  
Sergio Martínez-Luis
Keyword(s):  
Stem Bark ◽  
Spectrometric Analysis ◽  
Dependent Manner ◽  
Mangrove Plant ◽  
Concentration Dependent Manner ◽  
Pentacyclic Triterpenes ◽  
Aerial Parts ◽  
Glucosidase Inhibitors ◽  
Pelliciera Rhizophorae ◽  
First Time

In our continuous search for α-glucosidase inhibitors, three active pentacyclic triterpenes were isolated from stem bark samples of the Panamanian mangrove Pelliciera rhizophorae Triana & Planchon. These compounds were identified by both spectroscopic and spectrometric analysis. Of the isolated compounds, only betulinic acid has been previously isolated from P. rhizophorae leaves while both betulin (IC50 2.09 μM) and lupeol (IC50 0.58 μM) were isolated from this plant for the first time. All three pentacyclic triterpenes inhibited the α-glucosidase enzyme in a concentration-dependent manner, and their inhibitory activity was higher than that of the antidiabetic drug acarbose (IC50 241.6 μM). Kinetic analysis established that betulin and lupeol acted as competitive inhibitors. Finally, docking analysis suggested that all three triterpenes bind at the same site as acarbose does in the human intestinal α-glucosidase (PDB: 3TOP). This work contributes further evidence similar to previous studies that point out that the aerial parts of P. rhizophorae might be potential agents in controlling hyperglycemia in diabetic persons.

scholarly journals Brassinolide Enhances the Level of Brassinosteroids, Protein, Pigments, and Monosaccharides in Wolffia arrhiza Treated with Brassinazole

Plants ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1311
Author(s):  
Magdalena Chmur ◽  
Andrzej Bajguz
Keyword(s):  
Plant Growth ◽  
Growth And Development ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Plant Growth And Development ◽  
Concentration Dependent Manner ◽  
Spectrophotometric Methods ◽  
Synthetic Inhibitor ◽  
Wolffia Arrhiza ◽  
First Time

Brassinolide (BL) represents brassinosteroids (BRs)—a group of phytohormones that are essential for plant growth and development. Brassinazole (Brz) is as a synthetic inhibitor of BRs’ biosynthesis. In the present study, the responses of Wolffia arrhiza to the treatment with BL, Brz, and the combination of BL with Brz were analyzed. The analysis of BRs and Brz was performed using LC-MS/MS. The photosynthetic pigments (chlorophylls, carotenes, and xanthophylls) levels were determined using HPLC, but protein and monosaccharides level using spectrophotometric methods. The obtained results indicated that BL and Brz influence W. arrhiza cultures in a concentration-dependent manner. The most stimulatory effects on the growth, level of BRs (BL, 24-epibrassinolide, 28-homobrassinolide, 28-norbrassinolide, catasterone, castasterone, 24-epicastasterone, typhasterol, and 6-deoxytyphasterol), and the content of pigments, protein, and monosaccharides, were observed in plants treated with 0.1 µM BL. Whereas the application of 1 µM and 10 µM Brz caused a significant decrease in duckweed weight and level of targeted compounds. Application of BL caused the mitigation of the Brz inhibitory effect and enhanced the BR level in duckweed treated with Brz. The level of BRs was reported for the first time in duckweed treated with BL and/or Brz.

Cytotoxic Effects of Ferula Latisecta on Human Glioma U87 Cells

Drug Research ◽  
2019 ◽  
Vol 69 (12) ◽  
pp. 665-670 ◽  
Author(s):  
Mohammad Jalili-Nik ◽  
Hamed Sabri ◽  
Ehsan Zamiri ◽  
Mohammad Soukhtanloo ◽  
Mostafa Karimi Roshan ◽  
...  
Keyword(s):  
Enzymatic Activity ◽  
Gelatin Zymography ◽  
Annexin V ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Ic50 Values ◽  
Induced Apoptosis ◽  
Natural Herb ◽  
First Time ◽  
U87 Cells

AbstractGlioblastoma multiforme (GBM) is the fatal type of astrocytic tumors with a survival rate of 12 months. The present study, for the first time, evaluated the cytotoxic impacts of Ferula latisecta (F. latisecta) hydroalcoholic extract on U87 GBM cell line. The MTT assay measured the cellular toxicity following 24- and 48 h treatment with various doses of F. latisecta (0–800 μg/mL). Apoptosis was evaluated by an Annexin V/propidium iodide (PI) staining 24 h after treatment by F. latisecta. Moreover, to determine the cellular metastasis of U87 cells, we used a gelatin zymography assay (matrix metalloproteinase [MMP]-2/-9 enzymatic activity). The outcomes showed that F. latisecta mitigated the viability of U87 cells in a concentration- and time-dependent manner with IC50 values of 145.3 and 192.3 μg/mL obtained for 24- and 48 h treatments, respectively. F. latisecta induced apoptosis in a concentration-dependent manner after 24 h. Also, MMP-9 activity was significantly decreased following 24 h after treatment concentration-dependently with no change in MMP-2 enzymatic activity. This study showed that F. latisecta induced cytotoxicity and apoptosis, and mitigated metastasis of U87 GBM cells. Hence, F. latisecta could be beneficial as a promising natural herb against GBM after further studies.

In Vitro Attenuation of Thermal-Induced Protein Denaturation by Aerial Parts of Artemisia scoparia

2014 ◽  
Vol 20 (1) ◽  
pp. 9-12 ◽  
Author(s):  
Murad Ali Khan ◽  
Haroon Khan ◽  
Shafiq Ahmad Tariq ◽  
Samreen Pervez
Keyword(s):  
Crude Extract ◽  
Protein Denaturation ◽  
Total Flavonoid ◽  
Significant Activity ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Aqueous Fraction ◽  
Denatured Protein ◽  
Aerial Parts ◽  
Artemisia Scoparia

The goal of this study was to explore the aerial parts of Artemisia scoparia (crude extract, total flavonoid contents, and aqueous fraction) for protein denaturation potential. The crude extract provoked marked attenuation of thermal-induced denatured protein in a concentration-dependent manner with maximum inhibition of 54.05 μg/mL at 500 μg/mL and IC50 of 449.66 μg/mL. When total flavonoid contents were studied, it illustrated most dominant activity concentration dependently with maximum amelioration of 62.16 μg/mL at 500 μg/mL and IC50 of 378.35 μg/mL. The aqueous fraction also exhibited significant activity with maximum of 56.75% inhibition at 500 μg/mL and IC50 of 445.10 μg/mL. It can be concluded on the basis of the results that the crude extract, flavonoid contents, and aqueous fraction of the plant possessed significant inhibition on thermal-induced denatured protein.

Small Molecule Constituents of Periplaneta americana and Their IL-6 Inhibitory Activities

2021 ◽  
Vol 16 (9) ◽  
pp. 1934578X2110331
Author(s):  
Hua-Sheng Zhang ◽  
Yong-Ming Yan ◽  
Dai-Wei Wang ◽  
Qing Lv ◽  
Yong-Xian Cheng ◽  
...  
Keyword(s):  
High Performance Liquid Chromatography ◽  
High Performance ◽  
Periplaneta Americana ◽  
Ethanol Extract ◽  
Biological Evaluation ◽  
Dependent Manner ◽  
Chemical Methods ◽  
Concentration Dependent Manner ◽  
Inhibitory Activities ◽  
First Time

Two new glycosides, periplanosides A (1) and B (2), 3 compounds reported from a natural source for the first time (3 − 5), and 6 known compounds 6 − 11 were isolated from the ethanol extract of Periplaneta americana (Linnaeus). Their structures, including absolute configurations, were unambiguously identified by comprehensive spectroscopic and chemical methods. Compound 3 is a racemate whose enantiomers were purified by chiral high-performance liquid chromatography . The biological evaluation results showed that compound 7 (0 − 20 μM) did not affect the viability of RAW264.7 cells and could effectively inhibit the production of interleukin-6 stimulated by lipopolysaccharide in a concentration-dependent manner, indicating the potential to develop novel agents against inflammation-related diseases.

scholarly journals A C21-Steroidal Glycoside from Cynanchum atratum Attenuates Concanavalin A-Induced Liver Injury in Mice

Molecules ◽  
2019 ◽  
Vol 24 (6) ◽  
pp. 1087 ◽  
Author(s):  
Jian Yang ◽  
Bin Wang ◽  
Chao-feng Zhang ◽  
Xiang-hong Xu ◽  
Mian Zhang
Keyword(s):  
T Lymphocytes ◽  
Concanavalin A ◽  
Underlying Mechanism ◽  
Dependent Manner ◽  
Histopathological Changes ◽  
Con A ◽  
Concentration Dependent Manner ◽  
Steroidal Glycoside ◽  
First Time

Cynatratoside A (CyA) is a C21 Steroidal glycoside with pregnane skeleton isolated from the root of Cynanchum atratum Bunge (Asclepiadaceae). This study aimed to investigate the effects of CyA on concanavalin A (Con A)-induced autoimmune hepatitis (AIH) and the underlying mechanism. CyA was orally administered to mice at 10 and 40 mg/kg 8 h before and 1 h after Con A treatment. The effects of CyA on Con A-induced spleen and liver in mice were assessed via histopathological changes, T lymphocyte amounts and the expressions of IL-1β and ICAM-1. Con A-induced L-02 hepatocytes were used to evaluate whether CyA (0.1–10 μM) can directly protect hepatocytes from cytotoxicity and the possible mechanism. The results revealed that CyA treatment could significantly improve the histopathological changes of spleen and liver, reduce the proliferation of splenic T lymphocytes, and decrease the expressions of IL-1β and ICAM-1 in liver. The experiment in vitro showed that CyA inhibited Con A-induced hepatotoxicity in a concentration-dependent manner. CyA (10 μM) significantly increased/decreased the expression of Bcl-2/Bax and reduced the levels of cleaved caspases-9 and -3. Our study demonstrated for the first time that CyA has a significant protective effect on Con A-induced AIH by inhibiting the activation and adhesion of T lymphocytes and blocking hepatocyte apoptosis.

The cytoprotective effects of bilirubin and biliverdin on rat hepatocytes and human erythrocytes and the impact of albumin

1991 ◽  
Vol 69 (12) ◽  
pp. 828-834 ◽  
Author(s):  
Tai-Wing Wu ◽  
Doug Carey ◽  
Jun Wu ◽  
Hiroshi Sugiyama
Keyword(s):  
Rat Hepatocytes ◽  
Human Erythrocytes ◽  
Red Cells ◽  
Peroxyl Radicals ◽  
Blood Levels ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Hepatocyte Necrosis ◽  
The Impact ◽  
First Time

The hypothesis that unconjugated bilirubin and biliverdin are cytoprotective antioxidants has been examined for the first time in systems containing cells. In primary rat hepatocytes exposed to xanthine oxidase and hypoxanthine, bilirubin (0–60 μM) failed to prolong cell survival. In contrast, biliverdin (20–100 μM) markedly delayed hepatocyte necrosis in a concentration-dependent manner. When 0.3 mM of albumin was present, bilirubin (0–50 μM) became protective of hepatocytes, while biliverdin was less dramatically enhanced in its cytoprotective effect. In human erythrocytes exposed to peroxyl radicals, bilirubin and biliverdin inhibited 50% cell lysis at lower concentrations than Trolox and ascorbate, respectively. Albumin alone appeared less cytoprotective in red cells than in hepatocytes, but its presence enhanced the effects of both pigments on erythrocytes. Of probable physiologic relevance, bilirubin with albumin present or biliverdin alone protected hepatocytes substantially (and to a lesser extent red cells) at the normal blood levels of bilirubin (3.4–26 μM). Moreover, the fact that the pigments are cytoprotective at higher bilirubin levels (e.g., 50–100 μM) tempts the speculation that they may be circulating cytoprotectors of overlooked importance in jaundice.Key words: cytoprotection, biliverdin, bilirubin, albumin.

scholarly journals Toxicity and disruption of quorum sensing in Aliivibrio fisheri by environmental chemicals: Impacts of selected contaminants and microplastics

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
François Gagné
Keyword(s):  
Quorum Sensing ◽  
Fourier Transformation ◽  
Effective Concentration ◽  
Environmental Chemicals ◽  
Dependent Manner ◽  
Luminescent Bacterium ◽  
Concentration Dependent Manner ◽  
20 Nm ◽  
Toxic Concentrations ◽  
First Time

The purpose of this study was to examine the effects of dissolved and particulate compounds on quorum sensing in the marine luminescent bacterium Aliivibrio fisheri. Bacteria were exposed to increasing concentrations of CuSO4 (Cu2+), gadolinium chloride (Gd3+), 20-nm silver nanoparticles (nanoAg) and 1-3 μm microplastic polyethylene beads for 250 min. During this period, luminescence measurements were taken at 5-min intervals. Toxicity was first examined by measuring luminescence output at 5-min and 30-min incubation time. Based on the effective concentration that decreases luminescence by 20% (EC20), the compounds were toxic at the following concentrations in decreasing toxicity: Cu2+ (3.2 mg/L) < nanoAg (3.4 mg/L, reported) < Gd3+ (34 mg/L) < microplastics (2.6 g/L). The data revealed that luminescence changed non-linearly over time. In control bacteria, luminescence changed at eight specific major frequencies between 0.04 and 0.27 cycle/min after Fourier transformation of time-dependent luminescence data. The addition of dissolved Cu2+ and Gd3+ eliminated the amplitude changes at these frequencies in a concentration-dependent manner, indicating loss of quorum sensing between bacteria at concentrations below EC20. In the presence of nanoAg and microplastic beads, the decreases in amplitudes were modest but compressed the luminescence profiles, with shorter frequencies appearing at concentrations well below EC20. Thus, loss of communication between bacteria occurs at non-toxic concentrations. In addition, with exposure to a mixture of the above compounds at concentrations that do not produce effects for Gd3+, nanoAg and microplastics, Cu2+ toxicity was significantly enhanced, suggesting synergy. This study revealed for the first time that small microplastic particles and nanoparticles can disrupt quorum sensing in marine bacteria.

scholarly journals Uridine Triphosphate Thio-analogues Inhibit Platelet P2Y12 Receptors and Aggregation

2016 ◽  
Author(s):  
Dursun Guenduez ◽  
Christian Tanislav ◽  
Daniel Sedding ◽  
Mariana Parahuleva ◽  
Sentot Santoso ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Inhibitory Activity ◽  
Platelet Rich Plasma ◽  
P2y12 Receptor ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Uridine Triphosphate ◽  
Ic50 Value ◽  
Adp Receptor ◽  
First Time

Platelet P2Y12 is an important ADP receptor that is involved in agonist-induced platelet aggregation and is a valuable target for the development of anti-platelet drugs. Here we characterise the effects of thio-analogues of uridine triphosphate (UTP) on ADP-induced platelet aggregation. Using human platelet-rich plasma we demonstrate that UTP inhibits P2Y12 but not P2Y1 receptors and antagonises 10 &mu;M ADP-induced platelet aggregation in a concentration-dependent manner with an IC50 value of ~250 &mu;M. An 8-fold higher platelet inhibitory activity was observed with a 2-thio analogue of UTP (2S-UTP), with an IC50 of 30 &mu;M. The 4-thio analogue (4S-UTP) with an IC50 of 7.5 &mu;M was 33-fold more effective. A 3-fold decrease in inhibitory activity, however, was observed by introducing an isobutyl group at the 4S- position. A complete loss of inhibition was observed with thio-modification of the&nbsp;&gamma; phosphate of the sugar moiety, which yields an enzymatically stable analogue. The interaction of UTP analogues with P2Y12 receptors was verified by P2Y12 receptor binding and cAMP assays. These novel data demonstrate for the first time that 2- and 4-thio analogues of UTP are potent P2Y12 receptor antagonists that may be useful for therapeutic intervention.

Daphnetin methylation stabilizes the activity of phosphoribulokinase in wheat during cold acclimation

2012 ◽  
Vol 90 (5) ◽  
pp. 657-666
Author(s):  
Khalil Kane ◽  
Amira Moheb ◽  
Yukihara Fukushi ◽  
René Roy ◽  
Norman P.A Hüner ◽  
...  
Keyword(s):  
Cold Acclimation ◽  
Calvin Cycle ◽  
Biological Significance ◽  
Deae Cellulose ◽  
Triticum Aestivum L ◽  
Spectrometric Analysis ◽  
Dependent Manner ◽  
Aerial Parts ◽  
Dose Dependent ◽  
Excitation Pressure

The methylation of daphnetin (7,8-dihydroxycoumarin) to its 8-methyl derivative is catalyzed by a wheat (Triticum aestivum L.) O-methyltransferase (TaOMT1). This enzyme is regulated by cold and photosystem II excitation pressure (plastid redox state). Here, we investigated the biological significance of this methylation and its potential role in modulating the activity of kinases in wheat. To identify the potential kinases that may interact with daphnetin in wheat, the soluble protein extract from aerial parts of cold-acclimated wheat was purified by DEAE-cellulose separation and affinity chromatography on a daphnetin derivative (7,8-dihydroxy-4-coumarin acetic acid)-EAH sepharose column. Mass spectrometric analysis indicated that wheat phosphoribulokinase (TaPRK) is the major kinase that binds to daphnetin. This TaPRK plays an important role in regulating the flow of carbon through the Calvin cycle, by catalyzing the final step in the regeneration of ribulose 1,5-bisphosphate from ribulose-5-phosphate (Ru5P) and ATP. The activities of TaPRK, endogenous or recombinant, are inhibited by daphnetin in a specific and dose-dependent manner, but not by its monomethyl derivative (7-methyl, 8-hydroxycoumarin). Furthermore, HPLC-MS analysis of wheat extracts reveals that 7,8-dimethoxycoumarin is more abundant than its monomethyl derivative. The results also show that cold acclimation does not alter the level of TaPRK mRNA or its enzyme activity, and thus ensures the stable generation of ribulose 1,5-biphosphate.

scholarly journals Constituents of Coreopsis lanceolata Flower and Their Dipeptidyl Peptidase IV Inhibitory Effects

Molecules ◽  
2020 ◽  
Vol 25 (19) ◽  
pp. 4370 ◽  
Author(s):  
Bo-Ram Kim ◽  
Sunil Paudel ◽  
Joo-Won Nam ◽  
Chang Jin ◽  
Ik-Soo Lee ◽  
...  
Keyword(s):  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Mass Spectrometry Data ◽  
Ionization Mass ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Dpp Iv ◽  
Ic50 Values ◽  
First Time

A new polyacetylene glycoside, (5R)-6E-tetradecene-8,10,12-triyne-1-ol-5-O-β-glucoside (1), was isolated from the flower of Coreopsis lanceolata (Compositae), together with two known compounds, bidenoside C (10) and (3S,4S)-5E-trideca-1,5-dien-7,9,11-triyne-3,4-diol-4-O-β-glucopyranoside (11), which were found in Coreopsis species for the first time. The other known compounds, lanceoletin (2), 3,2′-dihydroxy-4-3′-dimethoxychalcone-4′-glucoside (3), 4-methoxylanceoletin (4), lanceolin (5), leptosidin (6), (2R)-8-methoxybutin (7), luteolin (8) and quercetin (9), were isolated in this study and reported previously from this plant. The structure of 1 was elucidated by analyzing one-dimensional and two-dimensional nuclear magnetic resonance and high resolution-electrospray ionization-mass spectrometry data. All compounds were tested for their dipeptidyl peptidase IV (DPP-IV) inhibitory activity and compounds 2–4, 6 and 7 inhibited DPP-IV activity in a concentration-dependent manner, with IC50 values from 9.6 to 64.9 μM. These results suggest that C. lanceolata flower and its active constituents show potential as therapeutic agents for diseases associated with type 2 diabetes mellitus.

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