scholarly journals Bronchodilatory effect of Myxopyrum serratulum in animal model

2017 ◽  
Vol 12 (1) ◽  
pp. 84
Author(s):  
Vijayalakshmi Maruthamuthu ◽  
Ruckmani Kandasamy
Keyword(s):  
Guinea Pig ◽  
Methanolic Extract ◽  
Relaxation Effect ◽  
Inhibitory Effect ◽  
Chlorpheniramine Maleate ◽  
Relaxant Effect ◽  
Significant Inhibitory Effect ◽  
Guinea Pig Model

<p class="Abstract">The plant <em>Myxopyrum </em>serratulum is traditionally claimed to relieve asthma and cough. The present study was undertaken to evaluate the bronchodilatory effect of the methanolic extract of <em>M. </em>serratulum on histamine-induced bronchospasm by <em>in vivo</em> and the inhibitory effect of the extract on histamine-contracted tracheal chain and ileum by <em>in vitro</em> guinea pig model. Additionally, the relaxant effect of four cumulative concentrations of the extract (0.25, 0.5, 0.7 and 1.0 g%) was assessed using precontracted tracheal chain under different conditions. The extract (400 mg/kg) prolonged the preconvulsive time to 102.3 ± 3.8 sec when compared to saline and standard chlorpheniramine maleate as 121.3 ± 4.5 sec (p&lt;0.05). The extract also possessed significant inhibitory effect on histamine-contracted guinea pig ileum and tracheal chain and also exhibited significant relaxation effect on precontracted tracheal chain of guinea pig models contracted by 60 mM KCl (p&lt;0.001) and 10 µM methacholine (p&lt;0.001) when compared with standard theophylline.</p>

Inhibition of Human and Animal Platelet Adhesiveness to Glass Bead Columns by Adenosine, Dipyridamole, Chlorpromazine and Acetylsalicylic Acid

1976 ◽  
Vol 36 (02) ◽  
pp. 401-410 ◽  
Author(s):  
Buichi Fujttani ◽  
Toshimichi Tsuboi ◽  
Kazuko Takeno ◽  
Kouichi Yoshida ◽  
Masanao Shimizu
Keyword(s):  
Guinea Pig ◽  
Acetylsalicylic Acid ◽  
Guinea Pigs ◽  
Glass Bead ◽  
Animal Species ◽  
Inhibitory Effect ◽  
Rabbit Platelet ◽  
Platelet Adhesiveness

SummaryThe differences among human, rabbit and guinea-pig platelet adhesiveness as for inhibitions by adenosine, dipyridamole, chlorpromazine and acetylsalicylic acid are described, and the influence of measurement conditions on platelet adhesiveness is also reported. Platelet adhesiveness of human and animal species decreased with an increase of heparin concentrations and an increase of flow rate of blood passing through a glass bead column. Human and rabbit platelet adhesiveness was inhibited in vitro by adenosine, dipyridamole and chlorpromazine, but not by acetylsalicylic acid. On the other hand, guinea-pig platelet adhesiveness was inhibited by the four drugs including acetylsalicylic acid. In in vivo study, adenosine, dipyridamole and chlorpromazine inhibited platelet adhesiveness in rabbits and guinea-pigs. Acetylsalicylic acid showed the inhibitory effect in guinea-pigs, but not in rabbits.

scholarly journals A novel BRD4 inhibitor suppresses osteoclastogenesis and ovariectomized osteoporosis by blocking RANKL-mediated MAPK and NF-κB pathways

2021 ◽  
Vol 12 (7) ◽  
Author(s):  
Ying Liu ◽  
Wenjie Liu ◽  
Ziqiang Yu ◽  
Yan Zhang ◽  
Yinghua Li ◽  
...  
Keyword(s):  
Bone Loss ◽  
Osteoporosis Treatment ◽  
Inhibitory Effect ◽  
Specific Gene ◽  
Actin Ring ◽  
Treatment Target ◽  
Significant Inhibitory Effect ◽  
Promising Treatment

AbstractBromodomain-containing protein 4 (BRD4) has emerged as a promising treatment target for bone-related disorders. (+)-JQ1, a thienotriazolodiazepine compound, has been shown to inhibit pro-osteoclastic activity in a BRD4-dependent approach and impede bone loss caused by ovariectomy (OVX) in vivo. However, clinical trials of (+)-JQ1 are limited because of its poor druggability. In this study, we synthesized a new (+)-JQ1 derivative differing in structure and chirality. One such derivative, (+)-ND, exhibited higher solubility and excellent inhibitory activity against BRD4 compared with its analogue (+)-JQ1. Interestingly, (-)-JQ1 and (-)-ND exhibited low anti-proliferative activity and had no significant inhibitory effect on RANKL-induced osteoclastogenesis as compared with (+)-JQ1 and (+)-ND, suggesting the importance of chirality in the biological activity of compounds. Among these compounds, (+)-ND displayed the most prominent inhibitory effect on RANKL-induced osteoclastogenesis. Moreover, (+)-ND could inhibit osteoclast-specific gene expression, F‐actin ring generation, and bone resorption in vitro and prevent bone loss in OVX mice. Collectively, these findings indicated that (+)-ND represses RANKL‐stimulated osteoclastogenesis and averts OVX-triggered osteoporosis by suppressing MAPK and NF-κB signalling cascades, suggesting that it may be a prospective candidate for osteoporosis treatment.

scholarly journals INHIBITORY EFFECT OF ETHANOLIC EXTRACT OF ERIOBOTRYA JAPONICA LEAVES PRE-INCUBATED WITH THEOPHYLLINE AND ASPIRIN ON ISOLATED GUINEA PIG TRACHEAL

2018 ◽  
Vol 11 (13) ◽  
pp. 46
Author(s):  
Marianne Marianne ◽  
Urip Harahap ◽  
Emil Salim ◽  
Dadang Irfan Husori ◽  
Fahrumsyah Jali Rambe ◽  
...  
Keyword(s):  
Guinea Pig ◽  
Protective Effect ◽  
Contractile Response ◽  
Ethanolic Extract ◽  
Ethanol Extract ◽  
Inhibitory Effect ◽  
Eriobotrya Japonica ◽  
Relaxant Effect ◽  
Significant Difference

 Objectives: The objectives of the study were to examine the inhibitory effect of ethanol extract of Eriobotrya japonica leaves (EEEJL) pre-incubated with theophylline and aspirin on isolated guinea pig tracheal chains against acetylcholine (ACh)-induced contraction.Methods: The effect of EEEJL (1-8 mg/Ml) on the isolated tracheal strips was tested in vitro. Furthermore, the mechanism of relaxant effects of EEEJL was evaluated in the presence of theophylline and aspirin.Results: The contractile response evoked by Ach (1.25 × 10−3 M) was decreased by EEEJL (effective concentration50 = 1.36 mg/mL) and has no significant difference of relaxant effect to that of EEEJL pre-incubated with theophylline and aspirin (p>0.05).Conclusion: The EEEJL decreased the ACh-induced contraction through the inhibition of PDE and the protective effect on prostaglandin E2.

scholarly journals Selective inhibition by antiflamrnin-2 of thromboxane B2release from isolated and perfused guinea-pig lung

1992 ◽  
Vol 1 (4) ◽  
pp. 251-254
Author(s):  
Lidia Sautebin ◽  
Giuseppe Cirino ◽  
Massimo Di Rosa
Keyword(s):  
Guinea Pig ◽  
Histamine Release ◽  
Calcium Ionophore ◽  
Selective Inhibition ◽  
Inhibitory Effect ◽  
Amino Acid Residues ◽  
A 23187 ◽  
Normal Lungs

Antiflammin-2 (AF2) is a nonapeptide corresponding to the amino acid residues 246–254 of lipocortin-1 showing anti-inflammatory activity both in vitro and in vivo. The effect of AF2 on the thromboxane B2(TXB2) and histamine release from isolated and perfused guinea-pig lungs has been studied. AF-2 (10–100 nM) inhibited leukotriene C4- (LTC4) (3 ng) and antigen-induced (ovalbumin, 1 mg) TXB2release in normal and sensitized lungs, respectively. In contrast AF-2 (100 nM) did not modify TXB2release induced by histamine (5 μg) or bradykinin (5 μg) in normal lungs. Antigen-induced histamine release was not affected by 100 nM AF-2 infusion. When tested in chopped lung fragments AF-2 (0.1–25 μM) did not modify the release of histamine and TXB2induced by antigen (ovalbumin, 10 μg ml−1) or calcium ionophore A 23187 (1 μM). Our results show that the inhibitory effect of AF-2 on TXB2release is selective and depends on the stimulus applied. In this respect AF-2 mimics, at least in part, the actions of both glucocorticoids and lipocortin-1.

scholarly journals 672. Activity of Ibrexafungerp (Formerly SCY-078) Against Candida auris: In vitro, In Vivo, and Clinical Case Studies of Candidemia

2019 ◽  
Vol 6 (Supplement_2) ◽  
pp. S307-S307
Author(s):  
Stephen Barat ◽  
Katyna Borroto-Esoda ◽  
Mahmoud Ghannoum ◽  
Elizabeth Berkow ◽  
David A Angulo
Keyword(s):  
Guinea Pig ◽  
Murine Model ◽  
The United States ◽  
In Vitro Studies ◽  
Pig Model ◽  
Cutaneous Infection ◽  
Candida Auris ◽  
Guinea Pig Model

Abstract Background Candida auris is a growing global threat; a pathogen associated with high mortality (up to 60%), multidrug resistance, the ability to spread from person-to-person and surface-to-person, presenting high risk for outbreaks in healthcare facilities. Ibrexafungerp is a novel IV/oral glucan synthase inhibitor (triterpenoid) antifungal with activity against Candida, Aspergillus, and Pneumocystis spp., in Phase 3 development. Methods In vitro studies tested ibrexafungerp against >100 clinical isolates of C. auris. Other in vitro studies evaluated the effects of ibrexafungerp against C. auris biofilms. In vivo activity against C. auris was evaluated using a disseminated murine model and a cutaneous infection guinea pig model. In humans, an ongoing open-label trial of ibrexafungerp for treatment of patients with infections caused by C. auris (the CARES study) has been initiated in the United States and India. Results In vitro and in vivo studies demonstrated that ibrexafungerp is active against C. auris, including MDR strains. The MIC mode for ibrexafungerp was 1 μg/mL and the MIC50 and MIC90 were 0.5 and 1 μg/mL, respectively. Many echinocandin-resistant C. auris isolates have shown susceptibility to ibrexafungerp. Furthermore, ibrexafungerp has been shown to reduce biofilm thickness. In animal models of C. auris infection, treatment with ibrexafungerp resulted in improved survival and reduced fungal burden in both the murine model of disseminated infection and the guinea pig model of cutaneous infection as compared with untreated controls. In humans, two patients with difficult to treat C. auris candidemias were enrolled in the CARES study and responded positively to oral ibrexafungerp with eradication of the infection. Conclusion These data demonstrate that ibrexafungerp possess potent in vitro and in vivo activity as well as promising clinical activity. Therefore, continued clinical evaluation of ibrexafungerp as an option to treat C. auris infections is warranted. Disclosures All authors: No reported disclosures.

Olorofim effectively eradicates dermatophytes in vitro and in vivo

2021 ◽  
Author(s):  
Esmat Mirbzadeh Ardakani ◽  
Atefeh Sharifirad ◽  
Nasrin Pashootan ◽  
Mahsa Nayebhashemi ◽  
Mozhgan Zahmatkesh ◽  
...  
Keyword(s):  
Guinea Pig ◽  
Skin Lesions ◽  
Growth Patterns ◽  
Pig Model ◽  
Antifungal Compound ◽  
Post Inoculation ◽  
Microsporum Gypseum ◽  
Guinea Pig Model

Superficial fungal infections are prevalent worldwide, with dermatophytes, as the most common cause. Various antifungal agents including azoles and allylamines are commonly used to treat dermatophytosis. However, their overuse has yielded drug-resistant strains, calling for the development of novel anti-mycotic compounds. Olorofim, is a newly developed antifungal compound, which targets pyrimidine biosynthesis in molds. The purpose of this study was to determine the in vitro and in vivo antifungal effects of olorofim against common dermatophytes. The in vitro activity of olorofim against dermatophytes was assessed by microtiter broth dilution method. Bioinformatic analysis of olorofim binding to dihydroorotate dehydrogenase (DHODH) of dermatophytes was also performed, using Aspergillus fumigatus DHODH as a template. The in vivo efficacy of the drug was investigated, using a guinea pig model, experimentally infected with Microsporum gypseum. Microtiter assays confirmed the high in vitro sensitivity of dermatophytes to olorofim (MIC= 0.015-0.06 mg/L). Amino acid sequence analysis indicated that DHODH is highly conserved among dermatophytes. The critical residues, in dermatophytes, involved in olorofim binding, were similar to their counterparts in A. fumigatus DHODH, which explains their susceptibility to olorofim. Typical skin lesions of dermatophyte infection, were observed in the guinea pig model, at seven days post-inoculation. Following one week of daily topical administration of olorofim, similar to the clotrimazole group, the skin lesions were resolved and normal hair growth patterns appeared. In light of the in vitro and in vivo activity of olorofim against dermatophytes, this novel agent may be considered as a treatment of choice, against dermatophytosis.

In vivo induction of neutrophil extracellular traps by Mycobacterium tuberculosis in a guinea pig model

2017 ◽  
Vol 23 (7) ◽  
pp. 625-637 ◽  
Author(s):  
Georgina Filio-Rodríguez ◽  
Iris Estrada-García ◽  
Patricia Arce-Paredes ◽  
María M Moreno-Altamirano ◽  
Sergio Islas-Trujillo ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Guinea Pig ◽  
Neutrophil Extracellular Traps ◽  
Post Inoculation ◽  
Extracellular Traps ◽  
Guinea Pig Model ◽  
In Vivo Induction ◽  
Proteins And Peptides

In 2004, a novel mechanism of cellular death, called ‘NETosis’, was described in neutrophils. This mechanism, different from necrosis and apoptosis, is characterized by the release of chromatin webs admixed with microbicidal granular proteins and peptides (NETs). NETs trap and kill a variety of microorganisms. Diverse microorganisms, including Mycobacterium tuberculosis, are NET inducers in vitro. The aim of this study was to examine whether M. tuberculosis can also induce NETs in vivo and if the NETs are bactericidal to the microorganism. Guinea pigs were intradermally inoculated with M. tuberculosis H37Rv, and the production of NETs was investigated at several time points thereafter. NETs were detected as early as 30 min post-inoculation and were clearly evident by 4 h post-inoculation. NETs produced in vivo contained DNA, myeloperoxidase, elastase, histones, ROS and acid-fast bacilli. Viable and heat-killed M. tuberculosis, as well as Mycobacterium bovis BCG were efficient NET inducers, as were unilamellar liposomes prepared with lipids from M. tuberculosis. In vitro, guinea pig neutrophils also produced NETs in response to M. tuberculosis. However, neither the in vivo nor the in vitro-produced NETs were able to kill M. tuberculosis. Nevertheless, in vivo, neutrophils might propitiate recruitment and activation of more efficient microbicidal cells.

Schistosoma mansoni: in vivoandin vitrostudies of immunity using the guinea-pig model

Parasitology ◽  
1983 ◽  
Vol 87 (3) ◽  
pp. 465-479 ◽  
Author(s):  
E. J. Pearce ◽  
Diane J. McLaren
Keyword(s):  
Guinea Pig ◽  
Schistosoma Mansoni ◽  
Guinea Pigs ◽  
Time Course ◽  
Immune Status ◽  
Challenge Infection ◽  
Cytotoxicity Assays ◽  
Guinea Pig Model

SummaryIn vivoandin vitroparameters of immunity have been assessed in guinea-pigs sensitized with 500 normal or 500 radiation-attenuated cercariae ofSchistosoma mansoni. High levels of resistance to a challenge infection developed in both the chronic and irradiated vaccine model, but immunity was expressed earlier (week 4) and reached higher levels (90%) in the latter case. Vaccinated guinea-pigs have thus been shown to achieve greater resistance than the more commonly used rodent hosts.In vitrocytotoxicity assays have demonstrated that antibodies capable of participating in complement-dependent (lethal antibody) or eosinophil-mediated schistosomular killing, develop in the serum of guinea-pigs immunized with either normal or irradiated cercariae. The time course of development of the eosinophil adherence promoting antibody approximated in both models, the development of immunityin vivo, but the lethal antibody response paralleled the immune status of the animal only in the irradiated vaccine model

Evaluation of antinociceptive and anti-inflammatory properties of methanolic crude extract of Lophopetalum javanicum (bark)

2016 ◽  
Vol 0 (0) ◽  
Author(s):  
Prawej Ansari ◽  
Sanjeeda Sarmin Badhan ◽  
Shofiul Azam ◽  
Nasrin Sultana ◽  
Sabbir Anwar ◽  
...  
Keyword(s):  
Methanolic Extract ◽  
Inhibitory Effect ◽  
Scientific Basis ◽  
Dose Increase ◽  
Hot Plate ◽  
Plate Method ◽  
Preliminary Screening ◽  
Significant Inhibitory Effect ◽  
Anti Inflammatory

AbstractThe aim of the current study was to investigate the scientific basis of the traditional application ofPresent study includes the preliminary screening of the phytochemical composition and in vivo analgesic and anti-inflammatory activity of methanolic extract ofOne hour after the administration of carrageenan, rat’s paw was inflamed, and after treating it with 500 mg/kg dose, increase in the significant inhibitory effect on paw was observed. At the third hour after carrageenan injection, extreme inhibition (55.61%±0.015%; p<0.001) resulted by methanolic extract. By using hot plate method, it was found thatThis study manifested that the methanolic extract of

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