scholarly journals Inhibitory effect of plant extracts on the cytotoxicity of eurytele nematocysts from Pelagia noctiluca

2021 ◽  
Vol 93 (2) ◽  
Author(s):  
Rossana Morabito ◽  
Laura Cornara ◽  
Giuseppina La Spada ◽  
Angela Marino ◽  
Gian Luigi Mariottini ◽  
...  
Keyword(s):  
Cell Survival ◽  
Plant Extracts ◽  
Carica Papaya ◽  
Cultured Cells ◽  
Inhibitory Effect ◽  
Health Problems ◽  
Point Of View ◽  
Ananas Comosus ◽  
Pelagia Noctiluca ◽  
Ic50 Value

Some species of Cnidarians, well known venomous organisms, are able to induce serious health problems as well as economic and social trouble. A lot of data show that cnidarian venoms can be cytotoxic to cultured cells. Therefore, a priority of the research is to find tools which could counteract the damaging activity of venoms. In this connection, the modulatory effects exerted by extracts of plants Ananas comosus (L.) and Carica papaya (L.) on cytotoxicity of heterotrichous microbasic eurytele nematocysts isolated from the jellyfish Pelagia noctiluca was evaluated. The nematocyst extract induced strong cytotoxicity at highest tested doses with reduction of cell survival below 40% and IC50 value of 40×103 nematocysts/mL. Both plant extracts significantly improved the survival of cells, so that the IC50 resulted 74×103 and 100×103 nematocysts/mL in the presence of A. comosus and C. papaya extracts, respectively, both used at 10 and 100 μg/mL. Taking into account that heterotrichous microbasic eurytele nematocysts are present mainly in tentacles, which Pelagia noctiluca utilizes both for predation and defence, this result is particularly interesting from both ecological and sanitary point of view and demonstrates the potential of these plants extracts against cnidarian venoms.

scholarly journals Regulatory volume decrease in isolated nematocytes is affected by crude venom from the jellyfish Pelagia noctiluca

2014 ◽  
Vol 87 (2) ◽  
Author(s):  
Rossana Morabito ◽  
Silvia Dossena ◽  
Giuseppa La Spada ◽  
Angela Marino
Keyword(s):  
Cultured Cells ◽  
Cell Model ◽  
Regulatory Volume Decrease ◽  
Inhibitory Effect ◽  
Crude Venom ◽  
Trypan Blue Exclusion ◽  
Hypotonic Stress ◽  
Pelagia Noctiluca ◽  
Volume Decrease

Crude venom from nematocysts of the Scyphozoan <em>Pelagia noctiluca</em> possesses hemolytic and cytotoxic power on cultured cells and elicits local and systemic inflammation reactions <em>in vivo</em>. The ability of regulating their volume after exposure to an anisosmotic solution is a fundamental feature common to cells from vertebrates and invertebrates, including Cnidarians. The aim of the present work i s to assay whether crude venom from <em>Pelagia noctiluca</em> may affect the regulatory volume decrease (RVD) of nematocytes isolated from the Anthozoan <em>Aiptasia mutabilis</em>, here employed as a cell model. For this purpose, nematocytes were isolated by 605 mM NaSCN plus 0.01 mM Ca2+ application on acontia of <em>Aiptasia mutabilis</em>, while crude venom was obtained by sonication of a population of, respectively, 10, 25 and 50 nematocysts/µL (n/µL). Isolated nematocytes were pre-treated for 30 min with crude venom, submitted to hypotonic stress and their osmotic response and RVD were measured optically. Our results show that, after exposure to crude venom, nematocytes were morphologically intact, as shown by the Trypan blue exclusion test, but did not exhibit RVD. This effect was dose-dependent and reversed by the ionopho re gramicidin. The last observation suggests an inhibitory effect of venom on cell membrane ion transport mechanisms involved in RVD. Further studies are needed to verify this hypothesis and ascertain if a similar effect could be observed in human cells.

Stereoselective Inhibition of Renal Basolateral Human Organic Anion Transporter 3 by Lansoprazole Enantiomers

Pharmacology ◽  
2018 ◽  
Vol 101 (3-4) ◽  
pp. 176-183 ◽  
Author(s):  
Yugo Hamada ◽  
Kenji Ikemura ◽  
Takuya Iwamoto ◽  
Masahiro Okuda
Keyword(s):  
Cultured Cells ◽  
Organic Anion ◽  
Inhibitory Effect ◽  
Organic Anion Transporter ◽  
Racemic Mixture ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Anion Transporter ◽  
Ic50 Value ◽  
Organic Anion Transporter 3

Lansoprazole, a proton pump inhibitor, potently inhibits human organic anion transporter, hOAT3 (SLC22A8). Lansoprazole has an asymmetric atom in its structure and is clinically administered as a racemic mixture of (R)-and (S)-enantiomers. However, little is known about the stereoselective inhibitory potencies of lansoprazole against hOAT3 and its homolog, hOAT1. In the present study, the stereoselective inhibitory effect of lansoprazole was evaluated using hOAT1-and hOAT3-expressing cultured cells. hOAT1 and hOAT3 transported [14C]p-aminohippurate and [3H]estrone-3-sulfate (ES) with Michaelis-Menten constants of 29.8 ± 4.0 and 30.1 ± 9.0 µmol/L respectively. Lansoprazole enantiomers inhibited hOAT1- and hOAT3-mediated transport of each substrate in a concentration-dependent manner. The IC50 value of (S)-lansoprazole against hOAT3-mediated transport of [3H]ES (0.61 ± 0.08 µmol/L) was significantly lower than that of (R)-lansoprazole (1.75 ± 0.31 µmol/L). In contrast, stereoselectivity was not demonstrated for the inhibition of hOAT1. Furthermore, (S)-lansoprazole inhibited hOAT3-mediated transport of pemetrexed and methotrexate (hOAT3 substrates) more strongly than the corresponding (R)-lansoprazole. This study is the first to demonstrate that the stereoselective inhibitory potency of (S)-lansoprazole against hOAT3 is greater than that of (R)-lansoprazole. The present findings provide novel information about the drug interactions associated with lansoprazole.

Synthesis and Assessment of Novel Anti-chlamydial Benzylidene Acylhydrazides Derivatives

2018 ◽  
Vol 15 (1) ◽  
pp. 31-36 ◽  
Author(s):  
Xiaofeng Bao ◽  
Ying Xue ◽  
Chao Xia ◽  
Yin Lu ◽  
Ningjing Yang ◽  
...  
Keyword(s):  
Inhibitory Effect ◽  
Dependent Manner ◽  
Iron Starvation ◽  
Hydrochloride Salt ◽  
Obligate Intracellular ◽  
Biphasic Life Cycle ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Dose Dependent ◽  
Better Than

Background: Chlamydiae, characterized by a unique biphasic life cycle, are a group of Gram-negative obligate intracellular bacterial pathogens responsible for diseases in a range of hosts including humans. Benzylidene acylhydrazide CF0001 could inhibit chlamydiae independent of iron starvation and T3SS inhibition. This finding promoted us to design and synthesize more benzylidene acylhydrazides to find novel anti-chlamydial agents. Methods: The carboxylic acids 1a-1d were coupled with Boc-hydrazide inpresence of EDCI and DMAP to obtain the intermediate 2a-2d in 60-62% yields. N-Boc deprotections were performed to obtain hydrazide hydrochloride salt 3a-3d. Nextly, the hydrazides were subjected to condensation with aldehydes to obtain benzylidene acylhydrazides 4a-4g in 30-52% yields in two steps. Results: Compound 4d exhibited best inhibitory effect on the formation and growth of chlamydial inclusions. The IC50 value of compound 4d for infectious progenies was 3.55 µM, better than 7.30 µM of CF0001. Conclusion: To find novel anti-chlamydial agents, we have designed and synthesized benzylidene acylhydrazides 4a-4g. Compounds 4a, 4d, 4g showed inhibitory activity on C. muridarum with the IC50 values from 3.55-12 µM. The 3,5-dibromo-4-hydroxyl substitutes on ring B are critical to keep their anti-chlamydial activity. Compound 4d inhibited C. muridarum in a dose-dependent manner without apparent cytotoxicity.

scholarly journals Combined Luteolin and Indole-3-Carbinol Synergistically Constrains ERα-Positive Breast Cancer by Dual Inhibiting Estrogen Receptor Alpha and Cyclin-Dependent Kinase 4/6 Pathway in Cultured Cells and Xenograft Mice

Cancers ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 2116
Author(s):  
Xiaoyong Wang ◽  
Lijuan Zhang ◽  
Qi Dai ◽  
Hongzong Si ◽  
Longyun Zhang ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cell ◽  
Breast Cancer Cells ◽  
Cultured Cells ◽  
Inhibitory Effect ◽  
Cyclin Dependent Kinase ◽  
Xenograft Mice ◽  
The Individual

The high concentrations of individual phytochemicals in vitro studies cannot be physiologically achieved in humans. Our solution for this concentration gap between in vitro and human studies is to combine two or more phytochemicals. We screened 12 phytochemicals by pairwise combining two compounds at a low level to select combinations exerting the synergistic inhibitory effect of breast cancer cell proliferation. A novel combination of luteolin at 30 μM (LUT30) and indole-3-carbinol 40 μM (I3C40) identified that this combination (L30I40) synergistically constrains ERα+ breast cancer cell (MCF7 and T47D) proliferation only, but not triple-negative breast cancer cells. At the same time, the individual LUT30 and I3C40 do not have this anti-proliferative effect in ERα+ breast cancer cells. Moreover, this combination L30I40 does not have toxicity on endothelial cells compared to the current commercial drugs. Similarly, the combination of LUT and I3C (LUT10 mg + I3C10 mg/kg/day) (IP injection) synergistically suppresses tumor growth in MCF7 cells-derived xenograft mice, but the individual LUT (10 mg/kg/day) and I3C (20 mg/kg/day) do not show an inhibitory effect. This combination synergistically downregulates two major therapeutic targets ERα and cyclin dependent kinase (CDK) 4/6/retinoblastoma (Rb) pathway, both in cultured cells and xenograft tumors. These results provide a solid foundation that a combination of LUT and I3C may be a practical approach to treat ERα+ breast cancer cells after clinical trials.

scholarly journals Potential In Vitro Inhibition of Selected Plant Extracts against SARS-CoV-2 Chymotripsin-Like Protease (3CLPro) Activity

Foods ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1503
Author(s):  
Carla Guijarro-Real ◽  
Mariola Plazas ◽  
Adrián Rodríguez-Burruezo ◽  
Jaime Prohens ◽  
Ana Fita
Keyword(s):  
Plant Extracts ◽  
Curcuma Longa ◽  
Hydrolysis Product ◽  
Resonance Energy ◽  
Significant Inhibition ◽  
Main Role ◽  
Turmeric Extract ◽  
Ic50 Value

Antiviral treatments inhibiting Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) replication may represent a strategy complementary to vaccination to fight the ongoing Coronavirus disease 19 (COVID-19) pandemic. Molecules or extracts inhibiting the SARS-CoV-2 chymotripsin-like protease (3CLPro) could contribute to reducing or suppressing SARS-CoV-2 replication. Using a targeted approach, we identified 17 plant products that are included in current and traditional cuisines as promising inhibitors of SARS-CoV-2 3CLPro activity. Methanolic extracts were evaluated in vitro for inhibition of SARS-CoV-2 3CLPro activity using a quenched fluorescence resonance energy transfer (FRET) assay. Extracts from turmeric (Curcuma longa) rhizomes, mustard (Brassica nigra) seeds, and wall rocket (Diplotaxis erucoides subsp. erucoides) at 500 µg mL−1 displayed significant inhibition of the 3CLPro activity, resulting in residual protease activities of 0.0%, 9.4%, and 14.9%, respectively. Using different extract concentrations, an IC50 value of 15.74 µg mL−1 was calculated for turmeric extract. Commercial curcumin inhibited the 3CLPro activity, but did not fully account for the inhibitory effect of turmeric rhizomes extracts, suggesting that other components of the turmeric extract must also play a main role in inhibiting the 3CLPro activity. Sinigrin, a major glucosinolate present in mustard seeds and wall rocket, did not have relevant 3CLPro inhibitory activity; however, its hydrolysis product allyl isothiocyanate had an IC50 value of 41.43 µg mL−1. The current study identifies plant extracts and molecules that can be of interest in the search for treatments against COVID-19, acting as a basis for future chemical, in vivo, and clinical trials.

scholarly journals Heterocyclic Aromatic Amines in Meat: Formation, Isolation, Risk Assessment and Inhibitory Effect of Plant Extracts

Foods ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1466
Author(s):  
Hafiz Rehan Nadeem ◽  
Saeed Akhtar ◽  
Tariq Ismail ◽  
Piero Sestili ◽  
Jose Manuel Lorenzo ◽  
...  
Keyword(s):  
Risk Assessment ◽  
Plant Extracts ◽  
Aromatic Amines ◽  
Extraction Procedure ◽  
Inhibitory Effect ◽  
Heating Time ◽  
Raw Material ◽  
Heterocyclic Aromatic Amines ◽  
Isolation And Identification ◽  
Cooked Meats

Heterocyclic aromatic amines (HAAs) are potent carcinogenic compounds induced by the Maillard reaction in well-done cooked meats. Free amino acids, protein, creatinine, reducing sugars and nucleosides are major precursors involved in the production of polar and non-polar HAAs. The variety and yield of HAAs are linked with various factors such as meat type, heating time and temperature, cooking method and equipment, fresh meat storage time, raw material and additives, precursor’s presence, water activity, and pH level. For the isolation and identification of HAAs, advanced chromatography and spectroscopy techniques have been employed. These potent mutagens are the etiology of several types of human cancers at the ng/g level and are 100- to 2000-fold stronger than that of aflatoxins and benzopyrene, respectively. This review summarizes previous studies on the formation and types of potent mutagenic and/or carcinogenic HAAs in cooked meats. Furthermore, occurrence, risk assessment, and factors affecting HAA formation are discussed in detail. Additionally, sample extraction procedure and quantification techniques to determine these compounds are analyzed and described. Finally, an overview is presented on the promising strategy to mitigate the risk of HAAs by natural compounds and the effect of plant extracts containing antioxidants to reduce or inhibit the formation of these carcinogenic substances in cooked meats.

scholarly journals Diadenosine polyphosphate hydrolase from presynaptic plasma membranes of Torpedo electric organ

1997 ◽  
Vol 323 (3) ◽  
pp. 677-684 ◽  
Author(s):  
Jesús MATEO ◽  
Pedro ROTLLAN ◽  
Eulalia MARTI ◽  
Inmaculada GOMEZ DE ARANDA ◽  
Carles SOLSONA ◽  
...  
Keyword(s):  
Plasma Membranes ◽  
Pyridoxal Phosphate ◽  
Electric Organ ◽  
Competitive Inhibitor ◽  
Inhibitory Effect ◽  
Ic50 Value ◽  
Neural Origin ◽  
Disulphonic Acid ◽  
Torpedo Electric Organ ◽  
Enzyme Activators

The diadenosine polyphosphate hydrolase present in presynaptic plasma membranes from the Torpedo electric organ has been characterized using fluorogenic substrates of the form di-(1,N6-ethenoadenosine) 5´,5‴-P1,Pn-polyphosphate. The enzyme hydrolyses diadenosine polyphosphates (Apn A, where n = 3–5), producing AMP and the corresponding adenosine (n-1) 5´-phosphate, Ap(n-1). The Km values of the enzyme were 0.543± 0.015, 0.478±0.043 and 0.520±0.026 μM, and the Vmax values were 633±4, 592±18 and 576±45 pmol/min per mg of protein, for the etheno derivatives of Ap3A (adenosine 5´,5‴-P1,P3-triphosphate), Ap4A (adenosine 5´,5‴-P1,P4 -tetraphosphate) and Ap5A (adenosine 5´,5‴-P1,P5-pentaphosphate) respectively. Ca2+, Mg2+ and Mn2+ are enzyme activators, with EC50 values of 0.86±0.11, 1.35±0.24 and 0.58±0.10 mM respectively. The fluoride ion is an inhibitor with an IC50 value of 1.38±0.19 mM. The ATP analogues adenosine 5´-tetraphosphate and adenosine 5´-[γ-thio]triphosphate are potent competitive inhibitors and adenosine 5´-[α,β-methylene]diphosphate is a less potent competitive inhibitor, the Ki values being 0.29±0.03, 0.43±0.05 and 7.18±0.8 μM respectively. The P2-receptor antagonist pyridoxal phosphate 6-azophenyl-2´,4´-disulphonic acid behaves as a non-competitive inhibitor with a Ki value of 29.7±3.1 μM, and also exhibits a significant inhibitory effect on Torpedo apyrase activity. The effect of pH on the Km and Vmax values, together with inhibition by diethyl pyrocarbonate, strongly suggests the presence of functional histidine residues in Torpedo diadenosine polyphosphate hydrolase. The enzyme from Torpedo shows similarities with that of neural origin from neurochromaffin cells, and significant differences compared with that from endothelial vascular cells.

scholarly journals Growth response of Spirulina platensis in papaya skin extract and antimicrobial activities of Spirulina extracts in different culture media

2012 ◽  
Vol 47 (2) ◽  
pp. 147-152 ◽  
Author(s):  
Nasima Akhtar ◽  
Monzur Morshed Ahmeda ◽  
Nishat Sarker ◽  
Khandaker Rayhan Mahbuba ◽  
Abdul Matin Sarker
Keyword(s):  
Antimicrobial Activity ◽  
Spirulina Platensis ◽  
Growth Response ◽  
Carica Papaya ◽  
Culture Media ◽  
Antimicrobial Activities ◽  
Inhibitory Effect ◽  
Skin Extract ◽  
Freeze Dried ◽  
Powder Extract

Growth response of Spirulina platensis in papaya skin extract media and their antimicrobial activity were studied. Five different concentrations  e.g. 10gm/L, 8gm/L, 6 gm/L, 4 gm/L and 2gm/L of Papaya (Carica papaya) skin extract media and BD1 (control) medium were used  in this study. After 8 days of cultivation, the optical density (0.33) was recorded in BD1 medium and among the five different concentrations  of papaya skin extract media the maximum was found (0.31) in 6gm/L. Antimicrobial activity of Spirulina platensis grown in three  media namely Zarrouk, BD1 media and media made from papaya skin extract was also studied. Only freeze dried Spirulina platensis powder  extract showed inhibitory effect against bacteria and no antifungal activity was observed. DOI: http://dx.doi.org/10.3329/bjsir.v47i2.11445 Bangladesh J. Sci. Ind. Res. 47(2), 147-152, 2012  

scholarly journals Potential Effect of Pomegranate Peels Extract (Punica Granatum.) against Covid-19 Virus .

2021 ◽  
Author(s):  
Ashraf fawzy mosa ◽  
Mostafa abo Elhoda Mohamed
Keyword(s):  
Tissue Culture ◽  
Water Extract ◽  
Punica Granatum ◽  
Inhibitory Effect ◽  
Potential Effect ◽  
Laboratory Methods ◽  
Global Epidemic ◽  
Ic50 Value ◽  
The World

Abstract Background: Covid-19 Virus infection poses significant global health challenges and considered a global epidemic sweeping all countries of the world Which prompted scientists around the world to search for a quick or safe treatment to preserve people's lives .So far, options for controlling and treating the disease have not been revealed. The current study was conducted to evaluate the effectiveness of pomegranate peels extract against the Covid-19 virus in the laboratory. Methods: In this research, tow methods of extraction are carried out ethyl alcohol and distal water extract of pomegranate peels . activity of the extract assessed using 50% Tissue Culture Infectious Doses (TCID50) method in Vero E6 cells. Results: Pomegranate peels extract had the highest inhibitory effect against Covid -19 virus with IC50 value of 0.125, 0.0625 and 0.031256 μl in Vero E6 cells. Conclusion: Based on our results, the aqueous extract of pomegranate peels can inhibit Covid-19 virus replication in vitro.

scholarly journals EFFICIENCY OF SOME PLANT EXTRACTS TO CONTROL OF PENICILLIUM ITALICUM WEHMER CAUSING BLUE MOLD ON LEMON FRUITS IN IRAQ

2019 ◽  
Vol 31 (1) ◽  
pp. 01-05
Author(s):  
Ahed A.H. Matloob ◽  
Hamid A A. Khafaji
Keyword(s):  
Plant Extracts ◽  
Water Extract ◽  
Inhibitory Effect ◽  
Penicillium Italicum ◽  
Blue Mold ◽  
Lemon Fruit ◽  
Water Extracts ◽  
Wild Mustard ◽  
First Time ◽  
High Inhibitory Effect

The study aimed to evaluate the efficacy of the water extract of Propolis, Wild mustard and dates vinegar in the inhibition of Penicillium italicum causal agent of Blue mold on a lemon fruits. The results showed that all tested extracts with concentrations 5, 10 and 15% had a high inhibitory effect against P. italicum. Dates vinegar is highly effective and showed 100% inhibition of P. italicum and protected lemon fruit from infection. First time this type of natural inhibitory water extracts are used in Iraq which resulted that the dates vinegar is the best suitable option for the management of lemon blue mold disease in post-harvest.

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