scholarly journals Effect of L. usitatissimum (Flaxseed/Linseed) Fixed Oil against Distinct Phases of Inflammation

2013 ◽  
Vol 2013 ◽  
pp. 1-4 ◽  
Author(s):  
Gaurav Kaithwas ◽  
Dipak K. Majumdar
Keyword(s):  
Vascular Permeability ◽  
Inflammatory Reaction ◽  
Linum Usitatissimum ◽  
Acid Metabolism ◽  
Capillary Permeability ◽  
Leukocyte Migration ◽  
Dependent Manner ◽  
Dependent Inhibition ◽  
Dose Dependent Inhibition ◽  
Dose Dependent

The present investigation summarizes the effect of Linum usitatissimum fixed oil against different phases of acute inflammatory reaction, namely, protein exudation, peritoneal capillary permeability, and leukocyte migration. The fixed oil exhibited dose-dependent inhibition of protein exudation vascular permeability, comparable to standard aspirin. The oil also inhibited the leukocyte migration in pleural exudates in a dose-dependent manner. Production of less vasodilatory (PGE3) and chemotactic (LTB5) eicosanoids through EPA (derived from linolenic acid) metabolism could account for the above observations.

Prejunctional inhibition of vasoactive intestinal peptide release

1987 ◽  
Vol 253 (1) ◽  
pp. G7-G12 ◽  
Author(s):  
J. R. Grider ◽  
G. M. Makhlouf
Keyword(s):  
Vasoactive Intestinal Peptide ◽  
Muscle Relaxation ◽  
Dependent Manner ◽  
Basal Tone ◽  
Peptide Release ◽  
Dependent Inhibition ◽  
Motor Nerves ◽  
Dose Dependent Inhibition ◽  
Dose Dependent

The role of vasoactive intestinal peptide (VIP) and its homologue, peptide histidine isoleucine (PHI), as neurotransmitters of inhibitory motor nerves of the gut, were examined in strips of guinea pig taenia coli and gastric fundic muscle. The stoichiometry of VIP release and muscle relaxation was determined in the presence and absence of the bee venom peptide, apamin, and the existence of prejunctional VIP/PHI receptors capable of regulating VIP/PHI release was explored. In both types of muscle, relaxation induced by field stimulation was proportional to the amount of VIP released. Apamin inhibited relaxation and VIP release in a dose-dependent manner: maximal relaxation was inhibited by 85–96% at 10(-7)-10(-6) M apamin. Analysis of residual responses showed that apamin did not affect the stoichiometry of VIP release and muscle relaxation. Because apamin had no effect on basal tone or on relaxation induced by exogenous VIP, its effect on neurally induced relaxation was attributed to inhibition of VIP release. Both secretin and PHI inhibited neurally induced VIP release in the two types of muscle. At the optimal concentration of 10(-7) M, secretin inhibited VIP release by 52%, whereas the closer neural homologue, PHI, abolished VIP release. The dose-dependent inhibition of VIP release by PHI, which is cosynthesized and coreleased with VIP, indicates the existence of prejunctional inhibitory VIP/PHI autoreceptors capable of regulating VIP/PHI release.

Anti-nociceptive activity of a few structurally related trimethoxy flavones and possible mechanisms involved

2016 ◽  
Vol 27 (2) ◽  
Author(s):  
Jagan Nadipelly ◽  
Vijaykumar Sayeli ◽  
Parimala Kadhirvelu ◽  
Jaikumar Shanmugasundaram ◽  
Binoy Varghese Cheriyan ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Hot Water ◽  
Dependent Manner ◽  
Tail Immersion ◽  
Dopaminergic Mechanisms ◽  
Dependent Inhibition ◽  
Dose Dependent Inhibition ◽  
Dose Dependent ◽  
Definite Role

AbstractThe present study was designed to investigate the anti-nociceptive activity of a few structurally related trimethoxy flavones (7,2′,3′-TMF, 7,2′,4′-TMF, 7,3′,4′-TMF and 7,5,4′-TMF) and the possible mechanisms involved.Anti-nociceptive activity was evaluated in mice by employing acetic acid-induced writhing, formalin-induced nociception and hot water tail immersion methods. The involvement of opioid, GABAergic, tryptaminergic, adrenergic and dopaminergic mechanisms and KTrimethoxy flavones exhibited a significant and dose-dependent inhibition of acetic acid writhing. The paw-licking response time was reduced both in the early and late phases of formalin nociception in a dose-dependent manner by trimethoxy flavones. A significant increase in tail withdrawal latency time was also observed after trimethoxy flavones treatment. These observations revealed the potential anti-nociceptive action of the investigated trimethoxy flavones. Pretreatment with naloxone and bicuculline significantly attenuated the reduction of abdominal constrictions produced by all the tested trimethoxy flavones indicating a definite role of opioid and GABAergic mechanisms in the anti-nociceptive effect of trimethoxy flavones. The anti-nociceptive action elicited by various trimethoxy flavones was differently modulated by glibenclamide, ondansetron, yohimbine and sulpiride.The investigated trimethoxy flavones exhibited promising anti-nociceptive activity in various nociceptive models, and multiple mechanisms are involved in the anti-nociceptive activity of these compounds.

scholarly journals Pharmacological Potential of Anti-Inflammatory and Anti Nociceptive Activity of Bioactive Fractions from Leaves of Maytenus emarginata

2021 ◽  
Vol 71 (1) ◽  
Author(s):  
Sunil Kumar ◽  
Mathew George ◽  
Lincy Joseph
Keyword(s):  
Cardiac Glycosides ◽  
Methyl Cellulose ◽  
Dependent Manner ◽  
Dependent Inhibition ◽  
Pure Compounds ◽  
Cotton Pellet Granuloma ◽  
Dose Dependent Inhibition ◽  
Anti Inflammatory ◽  
Pharmacological Potential ◽  
Dose Dependent

The antinociceptive & anti-inflammatory activities of extract were compared to dose of Phenylbutazone. The phytochemical secondary metabolites tested for include alkaloids, cardiac glycosides, flavonoids, phenols, saponins, steroids and terpenoids. Maytenus emarginata leaves extract demonstrated significant antinociceptive and anti- inflammatory effects in a dose-dependent manner. The extract dose at 200mg/kg bw exhibited the highest antinociceptive and anti-inflammatory activities & its activities were comparable to those of the respective reference drugs. BFLME (suspended in 1% carboxy methyl cellulose) in doses of 50, 100 and 200 mg/kg caused a dose-dependent inhibition of swelling caused by carrageenin equivalent to 30.2–63.2% protection (P<0.05– P<0.001) and in cotton pellet granuloma, 47.2–45.4% protection (P<0.01-P<0.001) was observed from inflammation. There was a significant increase in analgesiometer force induced pain in rat equivalent to 98.1–146.5% protection (P<0.01-P<0.001) and 7.19–37.8 % (P<0.05–P<0.001) protection against Acetic acid induced writhing. Phytochemical screening of the extract indicated the presence of alkaloids, cardiac glycosides, flavonoids, phenols, saponins, steroids and terpenoids. The present study therefore demonstrated the antinociceptive and anti-inflammatory properties of bioactive fraction of ethyl acetate extract from leaves of M. emarginata (BFLME), hence providing a basis for further research that may result in pure compounds that can be advanced into drug discovery.

Cytokine modulation of inhibin secretion in cultured rat granulosa cells

1996 ◽  
Vol 151 (3) ◽  
pp. 449-457 ◽  
Author(s):  
M Imai ◽  
M Yamoto ◽  
H Otani ◽  
R Nakano
Keyword(s):  
Enzyme Immunoassay ◽  
Granulosa Cells ◽  
Dependent Manner ◽  
Inhibin A ◽  
Α Subunit ◽  
Cytokine Modulation ◽  
Dependent Inhibition ◽  
Dose Dependent Inhibition ◽  
Factor Α ◽  
Dose Dependent

Abstract In the present study, we examined the effects of tumour necrosis factor α (TNFα) and interleukin-1β (IL-1β) on inhibin secretion by cultured rat granulosa cells using immunoblotting and two-site enzyme immunoassay for inhibin A (α-βA dimer). FSH stimulated the secretion of the inhibin α-βA dimer (32 kDa) by the cells in a dose-dependent manner. In addition to the predominant 32 kDa inhibin α-βA dimer staining, staining of minor immunoreactive bands was also enhanced by FSH. TNFα alone did not have any effect on inhibin secretion. Immunoblot analyses using an antiserum against α-subunit and an antiserum against βA-subunit revealed a dose-dependent inhibition by TNFα of FSH-stimulated secretion of inhibin by rat granulosa cells. Similarly, TNFα inhibited in a dose-dependent manner FSH-stimulated inhibin secretion when measured using a two-site enzyme immunoassay. IL-1β alone did not exert any effect on inhibin secretion but it inhibited FSH-stimulated inhibin release in a dose-dependent manner (using both immunoblotting and a two-site assay for inhibin A). The present observations suggest that TNFα and IL-1β inhibit gonadotrophin-stimulated inhibin production by cultured rat granulosa cells. Journal of Endocrinology (1996) 151, 449–457

Synthesis and antitumor activities of piperazine- and cyclen-conjugated dehydroabietylamine derivatives

2015 ◽  
Vol 21 (4) ◽  
pp. 233-237 ◽  
Author(s):  
Xinbin Yang ◽  
Xiaolin Qin ◽  
Qin Wang ◽  
Yu Huang
Keyword(s):  
Positive Control ◽  
Dependent Manner ◽  
Antitumor Activities ◽  
H Nmr ◽  
Flow Cytometric ◽  
Dependent Inhibition ◽  
Dose Dependent Inhibition ◽  
Dose Dependent ◽  
Mcf 7

AbstractA series of piperazine- and cyclen-conjugated dehydroabietylamine derivatives were synthesized and characterized by 1H NMR, 13C NMR, and HRMS. The in vitro antitumor activities of conjugates 10–13 against MCF-7 and HepG-2 tumor cell lines were evaluated using CCK-8 assay. The results show that the synthesized compounds cause a dose-dependent inhibition of cell proliferation and display different antitumor activities with the IC50 values ranging from 23.56 to 78.92 μm. Moreover, the antitumor activity of conjugate 10 against the MCF-7 cell line is superior to that of the positive control 5-fluorouracil. In addition, flow cytometric assay revealed that the representative conjugate 10 could induce apoptosis in MCF-7 tumor cells in a dose-dependent manner.

Retardation of cation channel deactivation by mitochondrial dysfunction in adrenal medullary cells

2000 ◽  
Vol 278 (1) ◽  
pp. C26-C32 ◽  
Author(s):  
M. Inoue ◽  
N. Fujishiro ◽  
I. Imanaga
Keyword(s):  
Kinase Inhibitor ◽  
Dependent Manner ◽  
Induced Current ◽  
Bath Application ◽  
Muscarinic Stimulation ◽  
Pump Activity ◽  
Dependent Inhibition ◽  
Relative Production ◽  
Dose Dependent Inhibition ◽  
Dose Dependent

The mechanism for cyanide (CN) activation of a nonselective cation (NS) channel coupled with a muscarinic receptor in a guinea pig chromaffin cell was studied with the perforated-patch method. Bath application of a protein kinase inhibitor resulted in a dose-dependent inhibition of muscarine-induced current ( I M) but had no apparent effect on the CN-induced current ( I CN). On the other hand, production of I CN occluded muscarine activation of NS channels in an amplitude-dependent manner. Deactivation of I M after washout was retarded while I CN was also active, and the extent of the retardation increased with an increase in the relative production of I CN on muscarinic stimulation. Restoration of Na+ pump activity from CN suppression was conspicuously retarded below 19–20°C, and the apparent diminution of I M and I CN after washout was retarded in parallel with a decrease in temperature. The results suggest that CN activation of NS channels is due to suppression of deactivation of the channel.

Differences between antigenic determinants of pig and cat zona pellucida proteins

Reproduction ◽  
2000 ◽  
pp. 15-23 ◽  
Author(s):  
K Jewgenow ◽  
M Rohleder ◽  
I Wegner
Keyword(s):  
In Vitro Fertilization ◽  
Zona Pellucida ◽  
Antigenic Determinants ◽  
Vitro Fertilization ◽  
Contraceptive Vaccine ◽  
Sperm Binding ◽  
Dependent Inhibition ◽  
Dose Dependent Inhibition ◽  
Dose Dependent

Despite many efforts, the control of reproduction in feral cat populations is still a problem in urban regions around the world. Immunocontraception is a promising approach; thus the present study examined the suitability of the widely used pig zona pellucida proteins (pZP) for contraception in feral domestic cats. Purified zona pellucida proteins obtained from pig and cat ovaries were used to produce highly specific antisera in rabbits. Antibodies against pZP raised in rabbits or lions were not effective inhibitors of either in vitro sperm binding (cat spermatozoa to cat oocytes) or in vitro fertilization in cats, whereas antibodies against feline zona pellucida proteins (fZP) raised in rabbits showed a dose-dependent inhibition of in vitro fertilization. Immunoelectrophoresis, ELISA and immunohistology of ovaries confirmed these results, showing crossreactivity of anti-fZP sera to fZP and to a lesser extent to pZP, but no interaction of anti-pZP sera with fZP. It is concluded that cat and pig zonae pellucidae express a very small number of shared antigenic determinants, making the use of pZP vaccine in cats questionable. A contraceptive vaccine based on feline zona pellucida determinants will be a better choice for the control of reproduction in feral cats if immunogenity can be achieved.

Antioxidant effects and in vitro cytotoxicity on human cancer cell lines of flavonoid-rich Flamboyant (Delonix regia (Bojer) Raf.) flower extract

2020 ◽  
Vol 21 ◽  
Author(s):  
Putthiporn Khongkaew ◽  
Phanphen Wattanaarsakit ◽  
Konstantinos I. Papadopoulos ◽  
Watcharaphong Chaemsawang
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Leukemia Cell ◽  
Leukemia Cell Line ◽  
Flower Extract ◽  
Dependent Inhibition ◽  
Dose Dependent Inhibition ◽  
Murine Leukemia Cell ◽  
Dose Dependent

Background: Cancer is a noncommunicable disease with increasing incidence and mortality rates both worldwide and in Thailand. Its apparent lack of effective treatments is posing challenging public health issues. Introduction: Encouraging research results indicating probable anti-cancer properties of the Delonix regia flower extract (DRE) have prompted us to evaluate the feasibility of developing a type of product for future cancer prevention or treatment. Methods and Results: In the present report, using High Performance Liquid Chromatography (HPLC), we demonstrate in the DRE, the presence of high concentrations of three identifiable flavonoids, namely rutin 4.15±0.30 % w/w, isoquercitrin 3.04±0.02 %w/w, and myricetin 2.61±0.01 % w/w respectively while the IC50 of DPPH and ABTS assay antioxidation activity was 66.88±6.30 µg/ml and 53.65±7.24 µg/ml respectively. Discussion: Our cancer cell line studies using the MTT assay demonstrated DREs potent and dose dependent inhibition of murine leukemia cell line (P-388: 35.28±4.07% of cell viability remaining), as well as of human breast adenocarcinoma (MCF-7), human cervical carcinoma (HeLa), human oral cavity carcinoma (KB), and human colon carcinoma (HT-29) cell lines in that order of magnitude. Conclusion: Three identifiable flavonoids (rutin, isoquercitrin and myricetin) with high antioxidation activity and potent and dose dependent inhibition of murine leukemia cell line and five other cancer cell lines were documented in the DRE. The extract’s lack of cytotoxicity in 3 normal cell lines is a rare advantage not usually seen in current antineoplastic agents. Yet another challenge of the DRE was its low dissolution rate and long-term storage stability, issues to be resolved before a future product can be formulated.

Investigation on the antibacterial activity of electronic cigarette liquids (ECLs): a proof of concept study

2020 ◽  
Vol 21 ◽  
Author(s):  
Virginia Fuochi ◽  
Massimo Caruso ◽  
Rosalia Emma ◽  
Aldo Stivala ◽  
Riccardo Polosa ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Bacterial Species ◽  
A549 Cells ◽  
Bactericidal Effect ◽  
Minimal Bactericidal Concentration ◽  
Viability Assay ◽  
Dependent Inhibition ◽  
Dose Dependent Inhibition ◽  
Dose Dependent

Background: The key ingredients of e-cigarettes liquid are commonly propane-1,2-diol (also called propylene glycol) and propane-1,2,3-triol (vegetal glycerol) and their antimicrobial effects are already established. The nicotine and flavors which are often present in e-liquids can interfere with the growth of some microorganisms. Objective: The effect of the combining these elements in e-liquids is unknown. The aim of the study was to investigate the possible effects of these liquids on bacterial growth in the presence or absence of nicotine and flavors. Methods: Susceptibilities of pathogenic strains (Klebsiella pneumoniae, Staphylococcus aureus, Pseudomonas aeruginosa, Acinetobacter baumannii, Escherichia coli, Enterococcus faecalis and Sarcina lutea) were studied by means of a multidisciplinary approach. Cell viability and antioxidant assays were also evaluated. Results: All e-liquids investigated showed antibacterial activity against at least one pathogenic strain. A higher activity was correlated to the presence of flavors and nicotine. Discussion: In most cases the value of minimal bactericidal concentration is equal to the value of minimal inhibitory concentration showing that these substances have a bactericidal effect. This effect was observed in concentrations up to 6.25% v/v. Antioxidant activity was also correlated to presence of flavors. Over time, the viability assay in human epithelial lung A549 cells showed a dose-dependent inhibition of cell growth. Conclusion: Our results have shown that flavors considerably enhance the antibacterial activity of propane-1,2-diol and propane-1,2,3-triol. This study provides important evidence that should be taken into consideration in further investigative approaches, to clarify the different sensitivity of the various bacterial species to e-liquids, including the respiratory microbiota, to highlight the possible role of flavors and nicotine.

scholarly journals In VitroActivities of Hexaazatrinaphthylenes against Leishmania spp.

2015 ◽  
Vol 59 (5) ◽  
pp. 2867-2874 ◽  
Author(s):  
Atteneri López-Arencibia ◽  
Daniel García-Velázquez ◽  
Carmen M. Martín-Navarro ◽  
Ines Sifaoui ◽  
María Reyes-Batlle ◽  
...  
Keyword(s):  
Therapeutic Agents ◽  
Content Type ◽  
Inhibition Effect ◽  
Intracellular Amastigotes ◽  
Dependent Inhibition ◽  
Leishmania Spp ◽  
Dose Dependent Inhibition ◽  
Dose Dependent ◽  
Potential Use

ABSTRACTThein vitroactivity of a novel group of compounds, hexaazatrinaphthylene derivatives, against two species ofLeishmaniais described in this study. These compounds showed a significant dose-dependent inhibition effect on the proliferation of the parasites, with 50% inhibitory concentrations (IC50s) ranging from 1.23 to 25.05 μM against the promastigote stage and 0.5 to 0.7 μM against intracellular amastigotes. Also, a cytotoxicity assay was carried out to in order to evaluate the possible toxic effects of these compounds. Moreover, different assays were performed to determine the type of cell death induced after incubation with these compounds. The obtained results highlight the potential use of hexaazatrinaphthylene derivatives againstLeishmaniaspecies, and further studies should be undertaken to establish them as novel leishmanicidal therapeutic agents.

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