scholarly journals Chemical Composition, Antimicrobial and Antiparasitic Screening of the Essential Oil from Phania matricarioides (Spreng.) Griseb.

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1615 ◽  
Author(s):  
Yamilet Gutiérrez ◽  
Ramón Scull ◽  
Anabel Villa ◽  
Prabodh Satyal ◽  
Paul Cos ◽  
...  
Keyword(s):  
Fungal Growth ◽  
Chemical Characterization ◽  
Peritoneal Macrophages ◽  
In Vivo Studies ◽  
Parasitic Protozoa ◽  
Reference Drug ◽  
Ic50 Values

Essential oils (EOs) have gained increasing attention due to their pharmacological effectiveness, and they also constitute some of the most popular natural products. In this study, we present the chemical characterization of the EO from Phania matricarioides and the in vitro activity/selectivity against a wide panel of bacteria, fungi and parasitic protozoa. Forty-five compounds were identified in the studied EO, of which lavandulyl acetate (40.1%) and thymyl isobutyrate (13.9%) were the major components. The EO did not inhibit bacterial or fungal growth at the maximum concentration tested (64 µg/mL), although it displayed activity on all evaluated protozoa (IC50 values ranging from 2.2 to 56.6 µg/mL). In parallel, the EO demonstrated a noteworthy cytotoxic activity against peritoneal macrophages (CC50 values of 28.0 µg/mL). The most sensitive microorganism was Trypanosoma cruzi, which had a superior activity (IC50 = 2.2 µg/mL) and selectivity (SI = 13) in respect to other parasitic protozoa and the reference drug (p < 0.05). Further in vivo studies are needed to evaluate the potential use of this EO and the main compounds as antitrypanosomal agents. To our knowledge, this is the first report of chemical characterization and antimicrobial assessment of the EO from P. matricarioides.

scholarly journals Biological and Inflammatory Effects of Antigen 5 from Polybia paulista (Hymenoptera, Vespidae) Venom in Mouse Intraperitoneal Macrophages

Toxins ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 850
Author(s):  
Murilo Luiz Bazon ◽  
Luis Gustavo Romani Fernandes ◽  
Isabela Oliveira Sandrini Assugeni ◽  
Lucas Machado Pinto ◽  
Patrícia Ucelli Simioni ◽  
...  
Keyword(s):  
Peritoneal Macrophages ◽  
In Vivo Studies ◽  
M2 Macrophage ◽  
No Production ◽  
Activated Macrophages ◽  
In Vitro Production ◽  
Polybia Paulista ◽  
Antigen 5

The social wasp Polybia paulista (Hymenoptera, Vespidae) is highly aggressive, being responsible for many medical occurrences. One of the most allergenic components of this venom is Antigen 5 (Poly p 5). The possible modulation of the in vitro immune response induced by antigen 5 from P. paulista venom, expressed recombinantly (rPoly p 5), on BALB/c mice peritoneal macrophages, activated or not with LPS, was assessed. Here, we analyzed cell viability changes, expression of the phosphorylated form of p65 NF-κB subunit, nitric oxide (NO), proinflammatory cytokines production, and co-stimulatory molecules (CD80, CD86). The results suggest that rPoly p 5 does not affect NO production nor the expression of co-stimulatory molecules in mouse peritoneal macrophages. On the other hand, rPoly p 5 induced an increase in IL-1β production in non-activated macrophages and a reduction in the production of TNF-α and MCP-1 cytokines in activated macrophages. rPoly p 5 decreased the in vitro production of the phosphorylated p65 NF-κB subunit in non-activated macrophages. These findings suggest an essential role of this allergen in the polarization of functional M2 macrophage phenotypes, when analyzed in previously activated macrophages. Further investigations, mainly in in vivo studies, should be conducted to elucidate Polybia paulista Ag5 biological role in the macrophage functional profile modulation.

Activity profile of two 5-nitroindazole derivatives over the moderately drug-resistant Trypanosoma cruzi Y strain (DTU TcII): in vitro and in vivo studies

Parasitology ◽  
2020 ◽  
Vol 147 (11) ◽  
pp. 1216-1228
Author(s):  
Cristina Fonseca-Berzal ◽  
Cristiane França da Silva ◽  
Denise da Gama Jaen Batista ◽  
Gabriel Melo de Oliveira ◽  
José Cumella ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Positive Impact ◽  
Cardiac Cells ◽  
In Vivo Studies ◽  
Drug Resistant ◽  
Activity Profile ◽  
Reference Drug ◽  
Novel Drugs

AbstractIn previous studies, we have identified several families of 5-nitroindazole derivatives as promising antichagasic prototypes. Among them, 1-(2-aminoethyl)-2-benzyl-5-nitro-1,2-dihydro-3H-indazol-3-one, (hydrochloride) and 1-(2-acetoxyethyl)-2-benzyl-5-nitro-1,2-dihydro-3H-indazol-3-one (compounds 16 and 24, respectively) have recently shown outstanding activity in vitro over the drug-sensitive Trypanosoma cruzi CL strain (DTU TcVI). Here, we explored the activity of these derivatives against the moderately drug-resistant Y strain (DTU TcII), in vitro and in vivo. The outcomes confirmed their activity over replicative forms, showing IC50 values of 0.49 (16) and 5.75 μm (24) towards epimastigotes, 0.41 (16) and 1.17 μm (24) against intracellular amastigotes. These results, supported by the lack of toxicity on cardiac cells, led to better selectivities than benznidazole (BZ). Otherwise, they were not as active as BZ in vitro against the non-replicative form of the parasite, i.e. bloodstream trypomastigotes. In vivo, acute toxicity assays revealed the absence of toxic events when administered to mice. Moreover, different therapeutic schemes pointed to their capability for decreasing the parasitaemia of T. cruzi Y acute infected mice, reaching up to 60% of reduction at the peak day as monotherapy (16), 79.24 and 91.11% when 16 and 24 were co-administered with BZ. These combined therapies had also a positive impact over the mortality, yielding survivals of 83.33 and 66.67%, respectively, while untreated animals reached a cumulative mortality of 100%. These findings confirm the 5-nitroindazole scaffold as a putative prototype for developing novel drugs potentially applicable to the treatment of Chagas disease and introduce their suitability to act in combination with the reference drug.

Development and characterization of highly selective target-sensitive liposomes for the delivery of streptokinase: in vitro/in vivo studies

Drug Delivery ◽  
2014 ◽  
Vol 23 (3) ◽  
pp. 791-797 ◽  
Author(s):  
Bhuvaneshwar Vaidya ◽  
Manasa K. Nayak ◽  
Debabrata Dash ◽  
Govind P. Agrawal ◽  
Suresh P. Vyas
Keyword(s):  
In Vivo Studies ◽  
Selective Target

Characterization of nociceptin receptors in the periphery: in vitro and in vivo studies

1999 ◽  
Vol 359 (3) ◽  
pp. 160-167 ◽  
Author(s):  
Raffaella Bigoni ◽  
Sandro Giuliani ◽  
G. Calo’ ◽  
Anna Rizzi ◽  
Remo Guerrini ◽  
...  
Keyword(s):  
In Vivo Studies

scholarly journals ENHANCED FLUORESCENCE IMAGING WITH DMSO-MEDIATED OPTICAL CLEARING

2010 ◽  
Vol 03 (03) ◽  
pp. 153-158 ◽  
Author(s):  
SANJEEV KARMA ◽  
JAMES HOMAN ◽  
CHARLES STOIANOVICI ◽  
BERNARD CHOI
Keyword(s):  
Fluorescence Emission ◽  
Model Systems ◽  
In Vivo Studies ◽  
In Vivo Model ◽  
Fluorescence Signal ◽  
Optical Clearing ◽  
Treated Site

Recent studies have demonstrated that topical application of glycerol on intact skin does not affect its optical scattering properties. Investigators from our research group recently revisited the use of dimethyl sulfoxide (DMSO) as an agent with optical clearing potential. We address the use of optical clearing to enhance quantitation of subsurface fluorescence emission. We employed both in vitro and in vivo model systems to study the effect of topical DMSO application on fluorescence emission. Our in vitro experiments performed on a tissue-simulating phantom suggest that DMSO-mediated optical clearing enables enhanced characterization of subsurface fluorophores. With topical DMSO application, a marked increase in fluorescence emission was observed. After 30 min, the fluorescence signal at the DMSO-treated site was 9× greater than the contralateral saline-treated site. This ratio increased to 13× at 105 min after agent application. In summary, DMSO is an effective optical clearing agent for improved fluorescence emission quantitation and warrants further study in preclinical in vivo studies. Based on outcomes from previous clinical studies on the toxicity profile of DMSO, we postulate that clinical application of DMSO as an optical clearing agent, can be performed safely, although further study is warranted.

scholarly journals In silico screening leads to novel scaffolds with both antifungal and anti-NLRP3 inflammasome activity

2021 ◽  
Vol 3 (12) ◽  
Author(s):  
David Lowes ◽  
Rand Al-waqfi ◽  
Kirk Hevener ◽  
Brian Peters
Keyword(s):  
Nlrp3 Inflammasome ◽  
In Silico ◽  
Fungal Growth ◽  
Hyphal Growth ◽  
Acetohydroxyacid Synthase ◽  
In Silico Screening ◽  
Chemical Structures ◽  
Ic50 Values

Due to structural similarities that exist between established inhibitors of the NLRP3-inflammasome, sulfonylureas Glyburide and MCC-950, and herbicidal-sulfonylureas, that specifically target fungal acetohydroxyacid synthase (AHAS), we sought to determine the potential for compounds to block both inflammation and inhibit fungal growth. In silico screening of ∼250,000 compounds was used to identify a prioritized list of chemical structures capable of inhibiting both targets. Prioritization of the top 1% of scores identified ∼70 compounds with a diverse set of scaffolds for testing in vitro. Selected hits were used to assess anti-inflammatory function in a THP-1 challenge model with LPS+ATP and resulting IC50 values were obtained. MIC and hyphal-growth assays were conducted to determine potential antifungal activity using media depleted of branched chain amino acids isoleucine and valine, to confirm on target AHAS inhibition. Identification of hits that exhibited low micromolar activity for NLRP3 and AHAS inhibition were selected for SAR study. In vitro testing of the analogs along with molecular docking led to increased knowledge for lead optimization of the potential hits. In silico screening has resulted in IC50 (IL-1β release) and MIC50 (fungal growth) values with low μM potency against several Candida species. In vivo validation will further confirm the potential of the scaffolds for further synthetic-modification for the rationale design of novel dual-purpose drugs

scholarly journals Chemical Characterization of the Lichen-symbiont Microalga Asterochloris erici and Study of Its Cytostatic Effect on the L929 Murine Fibrosarcoma Cell Line

2021 ◽  
Author(s):  
M. Concepción Matesanz ◽  
Mercedes Villa-Carvajal ◽  
Javier Linares ◽  
Sonia Morante-Zarcero ◽  
Isabel Sierra ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Chemical Characterization ◽  
Human Consumption ◽  
Cytostatic Effect ◽  
In Vitro Biocompatibility ◽  
Murine Fibrosarcoma ◽  
Terrestrial Lichen

New resources of food, pharmaceuticals or biotechnological products are needed. The huge biodiversity of aero-terrestrial lichen-symbiont microalgae remains unexplored. Viability of these for human consumption demands the demonstration of the absence of toxic effects. In vitro biocompatibility of crude homogenates of axenic microalga Asterochloris erici, symbiotic in the lichen Cladonia cristatella, was analyzed after treatment of cultured L929 fibroblasts with different doses of microalgal homogenates. The results show that crude homogenates of A. erici do not induce fibroblast cytotoxicity but seem to have some cytostatic effect inducing slight cell cycle alterations and intracellular reactive oxygen species (ROS) increase at the highest dose. Carotenoid analysis demonstrates high content of lutein, a xanthophyll with antioxidant and cytostatic properties in vivo. These findings confirm that Asterochloris erici can be considered suitable for the development of alimentary or pharmaceutical applications. The cytostatic effects should be further investigated for antitumor agents.

scholarly journals 1,4-Disubstituted-1,2,3-Triazole Compounds Induce Ultrastructural Alterations in Leishmania amazonensis Promastigote: An in Vitro Antileishmanial and in Silico Pharmacokinetic Study

2020 ◽  
Vol 21 (18) ◽  
pp. 6839 ◽  
Author(s):  
Fernando Almeida-Souza ◽  
Verônica Diniz da Silva ◽  
Gabriel Xavier Silva ◽  
Noemi Nosomi Taniwaki ◽  
Daiana de Jesus Hardoim ◽  
...  
Keyword(s):  
In Silico ◽  
Peritoneal Macrophages ◽  
In Vivo Studies ◽  
Topical Formulation ◽  
Current Standard ◽  
Current Standard Treatment ◽  
Predictive Study ◽  
Leishmania Parasites

The current standard treatment for leishmaniasis has remained the same for over 100 years, despite inducing several adverse effects and increasing cases of resistance. In this study we evaluated the in vitro antileishmanial activity of 1,4-disubstituted-1,2,3 triazole compounds and carried out in silico predictive study of their pharmacokinetic and toxicity properties. Ten compounds were analyzed, with compound 6 notably presenting IC50: 14.64 ± 4.392 µM against promastigotes, IC50: 17.78 ± 3.257 µM against intracellular amastigotes, CC50: 547.88 ± 3.256 µM against BALB/c peritoneal macrophages, and 30.81-fold selectivity for the parasite over the cells. It also resulted in a remarkable decrease in all the parameters of in vitro infection. Ultrastructural analysis revealed lipid corpuscles, a nucleus with discontinuity of the nuclear membrane, a change in nuclear chromatin, and kinetoplast swelling with breakdown of the mitochondrial cristae and electron-density loss induced by 1,4-disubstituted-1,2,3-triazole treatment. In addition, compound 6 enhanced 2.3-fold the nitrite levels in the Leishmania-stimulated macrophages. In silico pharmacokinetic prediction of compound 6 revealed that it is not recommended for topical formulation cutaneous leishmaniasis treatment, however the other properties exhibited results that were similar or even better than miltefosine, making it a good candidate for further in vivo studies against Leishmania parasites.

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