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1.
Parasitol Res ; 119(10): 3377-3390, 2020 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-32638100

RESUMEN

The hypersaline lagoons located in evaporation basins or salars (salt flats) in the Atacama Desert are extreme environments harbouring a specialised biota able to survive harsh conditions for life. The knowledge of the parasitic biodiversity of these extreme habitats is still scarce despite their functional importance in regulating relevant non-economic services like habitats of waterbirds. The present study is the first report on the cestode infection of Artemia franciscana Kellogg in Salar de Atacama lagoons in northern Chile. A total of 23 parasite larvae were isolated and identified as belonging to five cestode taxa of the order Cyclophyllidea: two species of the family Hymenolepididae, i.e. Flamingolepis sp. 1 and Flamingolepis sp. 2 (adults parasitic in flamingos); two species of Dilepididae, i.e. Fuhrmannolepis averini (adults parasitic in phalaropes) and Eurycestus avoceti (adult parasitic in charadriforms birds); and one species of Progynotaeniidae, i.e. Gynandrotaenia (?) stammeri (adult parasitic in flamingos). The cysticercoids of each species are described and figured. The study represents the first geographical record of the genera Eurycestus, Gynandrotaenia and Fuhrmannolepis in South America and the first report of Gynandrotaenia and Flamingolepis in A. franciscana in its native range. This survey also contributes to the knowledge of cestodes of Phoenicopteriformes and Charadriiformes and their life cycles in the Neotropical Region. A review of cestodes recorded in brine shrimps of the genus Artemia in the world is provided. Further studies on cestode fauna of aquatic birds and their intermediate hosts in hypersaline habitats of the Neotropical Region are needed to understand their functional role in such extreme and unique ecosystems.


Asunto(s)
Artemia/parasitología , Aves/parasitología , Cestodos/crecimiento & desarrollo , Infecciones por Cestodos/veterinaria , Ambientes Extremos , Animales , Aves/clasificación , Cestodos/clasificación , Cestodos/aislamiento & purificación , Infecciones por Cestodos/parasitología , Chile , Ecosistema , Larva/clasificación , Larva/crecimiento & desarrollo , Estadios del Ciclo de Vida
2.
Andrologia ; 52(11): e13797, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-32870570

RESUMEN

The aim of this study was to evaluate seasonal changes in basic parameters of sperm quality and freezability behaviour of ejaculates from 10 fertile heavy draft stallions. A total of 140 ejaculates were collected, processed and evaluated during both the breeding (September-November) and non-breeding seasons (April-June). Fresh semen was evaluated for volume, concentration, total spermatozoa per ejaculate, plasma membrane integrity and total sperm motility. Cryopreserved samples were evaluated for plasma membrane integrity and sperm motility by the CASA system, and for the freezability index (FI), which was defined as the decreased ratio of viability after freezing-thawing. In fresh ejaculates, only viability showed significantly higher values in the breeding than in the non-breeding season (64.0% ± 15.0% vs. 58.6% ± 12.0%, respectively; p < .05). The sperm post-thawing analysis of viability and total motility parameters showed no significant changes linked to the season. However, the FI analysis showed that the ejaculates collected in the non-breeding season had higher cryoresistance characteristics than those collected in the breeding season. Results suggest that the presence of some cryoprotective factor/s in heavy draft horse ejaculates could be modulated by seasonality, with higher protective effects in the non-breeding season.


Asunto(s)
Análisis de Semen , Preservación de Semen , Animales , Cruzamiento , Chile , Criopreservación/veterinaria , Caballos , Humanos , Masculino , Estaciones del Año , Semen , Análisis de Semen/veterinaria , Preservación de Semen/veterinaria , Motilidad Espermática , Espermatozoides
3.
Ir Vet J ; 72: 5, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31249663

RESUMEN

BACKGROUND: Tamoxifen (TAM), a selective modulator of estrogen receptors (SERMs) has been recently explored as a therapeutic option for the oral treatment of airway inflammation in the horse. The objective of this work was to establish pharmacokinetic parameters of TAM and its main metabolites in equines, as well as to determine its clinical safety in short-term treatments. RESULTS: We determined TAM and its three main metabolites (4-OH tamoxifen, endoxifen, and N-desmethyl tamoxifen) in plasma after single administration of 0.25 mg/kg in healthy adult horses (n = 12). A maximum concentration of TAM was achieved 3 h after the oral administration (4.65 pg/mL ± 1.69); 4-OH tamoxifen was the metabolite that reached the highest concentration (78 pg/mL ± 70), followed by N-desmethyl tamoxifen (0.43 pg / mL ± 0.48), and finally endoxifen (0.17 pg/mL ± 0.17). All metabolites showed peak concentration 2 h after oral administration of the drug. Oral TAM bioavailability was 13,15% ± 4,18, with a steady state volume of distribution of 7831 ± 2922 (L/kg). Elimination half-life was 15.40 ± 5.80 h, and clearance was 5876 ± 699 (mL/kg/min). Clinical safety of TAM was determined over a 7-day course of treatment (0.25 mg/kg, orally q 24 h, n = 20). No adverse effects were observed through clinical examination, blood hematology, serum biochemistry, ophthalmological and reproductive examinations. Endometrial edema observed in some mares was attributed to normal cyclic activity. CONCLUSIONS: Tamoxifen has moderate oral bioavailability and a large volume of distribution, with three main metabolites in horses. Additionally, oral TAM administration over a 7-day treatment period demonstrated to be clinically safe, without adverse effects on clinical, hematological or serum biochemical parameters. These data could contribute to the continued research into this drug's potential for the treatment of different inflammatory conditions in equine species.

4.
Molecules ; 23(8)2018 Aug 16.
Artículo en Inglés | MEDLINE | ID: mdl-30115838

RESUMEN

Herein we report an expeditive C-3 vinylation of unprotected 3-iodoindazoles under microwave irradiation. Ten C-5 substituted 3-vinylindazole derivatives, nine of them novel, were synthesized through this method, which proceeds in moderate to excellent yields starting from C-5 substituted 3-iodoindazole derivatives. In all cases, the C-3 vinylated derivative was the only isolated product. This methodology allows access to 3-vinylated indazoles selectively and directly without the need of N-protection. 3-Vinylindazoles could be interesting synthetic intermediates allowing access to biologically active molecules.


Asunto(s)
Ácidos Borónicos/química , Indazoles/química , Yodo/química , Microondas , Compuestos de Vinilo/química , Catálisis , Glicoles/química , Estructura Molecular , Oxidación-Reducción
5.
Molecules ; 23(7)2018 Jul 19.
Artículo en Inglés | MEDLINE | ID: mdl-30029513

RESUMEN

A rapid emergence of resistant bacteria is occurring worldwide, endangering the efficacy of antibiotics and reducing the therapeutic arsenal available for treatment of infectious diseases. In the present study, we developed a new class of compounds with antibacterial activity obtained by a simple, two step synthesis and screened the products for in vitro antibacterial activity against ATCC® strains using the broth microdilution method. The compounds exhibited minimum inhibitory concentrations (MIC) of 1⁻32 µg/mL against Gram-positive ATCC® strains. The structure⁻activity relationship indicated that the thiophenol ring is essential for antibacterial activity and the substituents on the thiophenol ring module, for antibacterial activity. The most promising compounds detected by screening were tested against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium (VREF) clinical isolates. We found remarkable activity against VREF for compounds 7 and 16, were the MIC50/90 were 2/4 µg/mL and 4/4 µg/mL, respectively, while for vancomycin the MIC50/90 was 256/512 µg/mL. Neither compound affected cell viability in any of the mammalian cell lines at any of the concentrations tested. These in vitro data show that compounds 7 and 16 have an interesting potential to be developed as new antibacterial drugs against infections caused by VREF.


Asunto(s)
Antibacterianos/química , Antibacterianos/farmacología , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Enterococcus faecium/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacos , Antibacterianos/síntesis química , Fenómenos Químicos , Humanos , Pruebas de Sensibilidad Microbiana , Modelos Moleculares , Estructura Molecular , Relación Estructura-Actividad , Difracción de Rayos X
6.
Molecules ; 23(5)2018 May 16.
Artículo en Inglés | MEDLINE | ID: mdl-29772697

RESUMEN

The wide tissue distribution of the adrenergic ß3 receptor makes it a potential target for the treatment of multiple pathologies such as diabetes, obesity, depression, overactive bladder (OAB), and cancer. Currently, there is only one drug on the market, mirabegron, approved for the treatment of OAB. In the present study, we have carried out an extensive structure-activity relationship analysis of a series of 41 aryloxypropanolamine compounds based on three-dimensional quantitative structure-activity relationship (3D-QSAR) techniques. This is the first combined comparative molecular field analysis (CoMFA) and comparative molecular similarity index analysis (CoMSIA) study in a series of selective aryloxypropanolamines displaying anti-diabetes and anti-obesity pharmacological profiles. The best CoMFA and CoMSIA models presented values of r²ncv = 0.993 and 0.984 and values of r²test = 0.865 and 0.918, respectively. The results obtained were subjected to extensive external validation (q², r², r²m, etc.) and a final series of compounds was designed and their biological activity was predicted (best pEC50 = 8.561).


Asunto(s)
Agonistas de Receptores Adrenérgicos beta 3/química , Fármacos Antiobesidad/química , Hipoglucemiantes/química , Propanolaminas/química , Agonistas de Receptores Adrenérgicos beta 3/farmacología , Fármacos Antiobesidad/farmacología , Sitios de Unión , Diseño de Fármacos , Humanos , Hipoglucemiantes/farmacología , Modelos Moleculares , Estructura Molecular , Propanolaminas/farmacología , Relación Estructura-Actividad Cuantitativa , Electricidad Estática
7.
Appl Environ Microbiol ; 83(1)2017 01 01.
Artículo en Inglés | MEDLINE | ID: mdl-27795307

RESUMEN

Several bacteria use the plant hormone indole-3-acetic acid (IAA) as a sole carbon and energy source. A cluster of genes (named iac) encoding IAA degradation has been reported in Pseudomonas putida 1290, but the functions of these genes are not completely understood. The plant-growth-promoting rhizobacterium Paraburkholderia phytofirmans PsJN harbors iac gene homologues in its genome, but with a different gene organization and context than those of P. putida 1290. The iac gene functions enable P. phytofirmans to use IAA as a sole carbon and energy source. Employing a heterologous expression system approach, P. phytofirmans iac genes with previously undescribed functions were associated with specific biochemical steps. In addition, two uncharacterized genes, previously unreported in P. putida and found to be related to major facilitator and tautomerase superfamilies, are involved in removal of an IAA metabolite called dioxindole-3-acetate. Similar to the case in strain 1290, IAA degradation proceeds through catechol as intermediate, which is subsequently degraded by ortho-ring cleavage. A putative two-component regulatory system and a LysR-type regulator, which apparently respond to IAA and dioxindole-3-acetate, respectively, are involved in iac gene regulation in P. phytofirmans These results provide new insights about unknown gene functions and complex regulatory mechanisms in IAA bacterial catabolism. IMPORTANCE: This study describes indole-3-acetic acid (auxin phytohormone) degradation in the well-known betaproteobacterium P. phytofirmans PsJN and comprises a complete description of genes, some of them with previously unreported functions, and the general basis of their gene regulation. This work contributes to the understanding of how beneficial bacteria interact with plants, helping them to grow and/or to resist environmental stresses, through a complex set of molecular signals, in this case through degradation of a highly relevant plant hormone.


Asunto(s)
Proteínas Bacterianas/genética , Burkholderiaceae/genética , Burkholderiaceae/metabolismo , Regulación Bacteriana de la Expresión Génica , Ácidos Indolacéticos/metabolismo , Reguladores del Crecimiento de las Plantas/metabolismo , Proteínas Bacterianas/metabolismo , Burkholderiaceae/fisiología , Genes Bacterianos , Desarrollo de la Planta , Reguladores del Crecimiento de las Plantas/química , Pseudomonas putida/genética , Pseudomonas putida/metabolismo , Estrés Fisiológico/genética
8.
Molecules ; 21(8)2016 Aug 16.
Artículo en Inglés | MEDLINE | ID: mdl-27537868

RESUMEN

Based on a known pharmacophore model for 5-HT6 receptor antagonists, a series of novel extended derivatives of the N-arylsulfonyindole scaffold were designed and identified as a new class of 5-HT6 receptor modulators. Eight of the compounds exhibited moderate to high binding affinities and displayed antagonist profile in 5-HT6 receptor functional assays. Compounds 2-(4-(2-methoxyphenyl)piperazin-1-yl)-1-(1-tosyl-1H-indol-3-yl)ethanol (4b), 1-(1-(4-iodophenylsulfonyl)-1H-indol-3-yl)-2-(4-(2-methoxyphenyl)piperazin-1-yl)ethanol (4g) and 2-(4-(2-methoxyphenyl)piperazin-1-yl)-1-(1-(naphthalen-1-ylsulfonyl)-1H-indol-3-yl)ethanol (4j) showed the best binding affinity (4b pKi = 7.87; 4g pKi = 7.73; 4j pKi = 7.83). Additionally, compound 4j was identified as a highly potent antagonist (IC50 = 32 nM) in calcium mobilisation functional assay.


Asunto(s)
Arilsulfonatos/química , Indoles/síntesis química , Receptores de Serotonina/metabolismo , Antagonistas de la Serotonina/síntesis química , Sitios de Unión , Humanos , Indoles/química , Indoles/farmacología , Modelos Moleculares , Estructura Molecular , Unión Proteica , Receptores de Serotonina/química , Antagonistas de la Serotonina/química , Antagonistas de la Serotonina/farmacología , Relación Estructura-Actividad
9.
Extremophiles ; 19(1): 135-47, 2015 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-25239570

RESUMEN

The brine shrimp Artemia (Crustacea) and a diversity of halophilic microorganisms coexist in natural brines, salterns and laboratory cultures; part of such environmental microbial diversity is represented in the gut of Artemia individuals. Bacterial diversity in these environments was assessed by 16S rRNA gene denaturing gradient gel electrophoresis (DGGE) fingerprinting. Eight natural locations in Chile, where A. franciscana or A. persimilis occur, were sampled for analysis of free-living and gut-associated bacteria in water from nature and laboratory cultures. The highest ecological diversity (Shannon's index, H') was found in brines, it decreased in the gut of wild and laboratory animals, and in laboratory water. Significant differences in H' existed between brines and laboratory water, and between brines and gut of wild animals. The greatest similarity of bacterial community composition was between brines and the gut of field animals, suggesting a transient state of the gut microbiota. Sequences retrieved from DGGE patterns (n = 83) exhibited an average of 97.8% identity with 41 bacterial genera from the phyla Proteobacteria (55.4% of sequences match), Bacteroidetes (22.9%), Actinobacteria (16.9%) and Firmicutes (4.8%). Environment-exclusive genera distribution was seen in Sphingomonas and Paenibacillus (gut of field animals), Amaricoccus and Ornithinimicrobium (gut of laboratory animals), and Hydrogenophaga (water of laboratory cultures). The reported ecological and physiological capabilities of such bacteria can help to understand Artemia adaptation to natural and laboratory conditions.


Asunto(s)
Artemia/microbiología , Bacterias/clasificación , Intestinos/microbiología , Microbiota , Microbiología del Agua , Animales , Artemia/fisiología , Bacterias/aislamiento & purificación , Biodiversidad , Chile , ADN Bacteriano/genética , Ecosistema , Electroforesis , Metagenoma , Filogenia , Reacción en Cadena de la Polimerasa , Proteobacteria/genética , ARN Ribosómico 16S/genética , Salinidad , Análisis de Secuencia de ADN
10.
Arch Pharm (Weinheim) ; 348(2): 81-8, 2015 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-25641513

RESUMEN

A series of N-acyl-2,5-dimethoxyphenyl-1H-benzimidazoles were designed based on a CoMFA model for cannabinoid receptor type 1 (CB1) ligands. Compounds were synthesized and radioligand binding affinity assays were performed. Eight novel benzimidazoles exhibited affinity for the CB1 receptor in the nanomolar range, and the most promising derivative compound 5 displayed a K(i) value of 1.2 nM when compared to CP55,940. These results confirm our previously reported QSAR model on benzimidazole derivatives, providing new information for the development of small molecules with high CB1 affinity.


Asunto(s)
Bencimidazoles/síntesis química , Bencimidazoles/metabolismo , Agonistas de Receptores de Cannabinoides/síntesis química , Agonistas de Receptores de Cannabinoides/metabolismo , Diseño de Fármacos , Receptor Cannabinoide CB1/metabolismo , Bencimidazoles/farmacología , Sitios de Unión , Unión Competitiva , Agonistas de Receptores de Cannabinoides/farmacología , Diseño Asistido por Computadora , Ciclohexanoles/metabolismo , Ligandos , Simulación del Acoplamiento Molecular , Estructura Molecular , Unión Proteica , Conformación Proteica , Relación Estructura-Actividad Cuantitativa , Receptor Cannabinoide CB1/agonistas , Receptor Cannabinoide CB1/química
11.
Arch Pharm (Weinheim) ; 347(3): 174-84, 2014 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-24339227

RESUMEN

A series of functionalized indolylalkylarenes 3-16(a and b) were synthesized and their affinities for the serotonin transporter were investigated in vitro. Compounds 3-12(a and b) were obtained by nucleophilic substitution of 3-(1H-indol-3-yl)propyl-4-methylbenzenesulfonates 2(a and b) with a series of azaheterocycles. Compounds 14-16(a and b) were prepared in a two-step sequence by reaction of 3-(1H-indol-3-yl)-2-methylpropanal with substituted 1,2-phenylenediamines. Compounds 3b, 4b, and 5b showed good binding affinities (K(i) = 33.0, 48.0, and 17 nM, respectively). The other synthesized compounds showed moderate or no affinity in the binding studies.


Asunto(s)
Indoles/síntesis química , Indoles/metabolismo , Inhibidores Selectivos de la Recaptación de Serotonina/síntesis química , Inhibidores Selectivos de la Recaptación de Serotonina/metabolismo , Proteínas de Transporte de Serotonina en la Membrana Plasmática/metabolismo , Células HEK293 , Humanos , Indoles/farmacología , Estructura Molecular , Proteínas de Transporte de Serotonina en la Membrana Plasmática/efectos de los fármacos , Proteínas de Transporte de Serotonina en la Membrana Plasmática/genética , Inhibidores Selectivos de la Recaptación de Serotonina/farmacología , Relación Estructura-Actividad , Transfección
12.
Heliyon ; 10(1): e23695, 2024 Jan 15.
Artículo en Inglés | MEDLINE | ID: mdl-38205306

RESUMEN

Epigenetic variation affects gene expression without altering the underlying DNA sequence of genes controlling ecologically relevant phenotypes through different mechanisms, one of which is long non-coding RNAs (lncRNAs). This study identified and evaluated the gene expression of lncRNAs in the gill and mantle tissues of Mytilus chilensis individuals from two ecologically different sites: Cochamó (41°S) and Yaldad (43°S), southern Chile, both impacted by climatic-related conditions and by mussel farming given their use as seedbeds. Sequences identified as lncRNAs exhibited tissue-specific differences, mapping to 3.54 % of the gill transcriptome and 1.96 % of the mantle transcriptome, representing an average of 2.76 % of the whole transcriptome. Using a high fold change value (≥|100|), we identified 43 and 47 differentially expressed lncRNAs (DE-lncRNAs) in the gill and mantle tissue of individuals sampled from Cochamó and 21 and 17 in the gill and mantle tissue of individuals sampled from Yaldad. Location-specific DE-lncRNAs were also detected in Cochamó (65) and Yaldad (94) samples. Via analysis of the differential expression of neighboring protein-coding genes, we identified enriched GO terms related to metabolic, genetic, and environmental information processing and immune system functions, reflecting how the impact of local ecological conditions may influence the M. chilensis (epi)genome expression. These DE-lncRNAs represent complementary biomarkers to DNA sequence variation for maintaining adaptive differences and phenotypic plasticity to cope with natural and human-driven perturbations.

13.
ACS Chem Neurosci ; 15(18): 3257-3269, 2024 Sep 18.
Artículo en Inglés | MEDLINE | ID: mdl-39254100

RESUMEN

Muscimol (3) is a psychoactive isoxazole present in various Amanita mushrooms, along with ibotenic acid and muscarine. It is structurally related to GABA and acts as a GABAA agonist with great affinity. Muscimol use dates back to Siberian shamanic cultures as an entheogen, where it was ingested orally to exert psychoactive effects. Although not approved for clinical use, its potential and use as a research tool in neuroscience is of immense value, with 3H-muscimol being used as a radioligand in GABA receptor research. Since its discovery in the early 60s, many research groups have worked on the synthesis of the compound. Recent research suggests the potential use of muscimol in neuropathic pain relief and other potential uses are also being studied. In this review, we will cover the history, chemistry, pharmacology and overall importance of the compound.


Asunto(s)
Muscimol , Muscimol/farmacología , Humanos , Animales , Historia del Siglo XX , Agonistas de Receptores de GABA-A/farmacología , Agonistas de Receptores de GABA-A/química , Neurociencias , Agonistas del GABA/farmacología , Agonistas del GABA/química , Historia del Siglo XXI
14.
Animals (Basel) ; 14(3)2024 Jan 25.
Artículo en Inglés | MEDLINE | ID: mdl-38338040

RESUMEN

Determining molecular markers for parasites provides a useful tool for their identification, particularly for larval stages with few distinguishable diagnostic characters. Avian cestodes play a key role in the food webs and biodiversity of hypersaline wetlands, yet they remain understudied. Using naturally infected Artemia, we identified cestode larvae (cysticercoids), assessed their genetic diversity, and explored phylogenetic relationships in relation to larval morphology and waterbird final hosts. We obtained partial 18S rDNA sequences for 60 cysticercoids of the family Hymenolepidae infecting Artemia spp. from seven localities and three countries (Spain, the USA, and Chile). We present the first DNA sequences for six taxa: Confluaria podicipina, Fimbriarioides sp., Flamingolepis liguloides, Flamingolepis sp. 1, Flamingolepis sp. 2, and Hymenolepis californicus. Intraspecific sequence variation (0.00-0.19% diversity) was lower than intergroup genetic distance (0.7-14.75%). Phylogenetic analysis revealed three main clades: 1-Flamingolepis, 2-Fimbriarioides, 3-Confluaria and Hymenolepis, all of which separated from hymenolepidids from mammals and terrestrial birds. This clear separation among taxa is congruent with previous morphological identification, validating the 18S gene as a useful marker to discriminate at generic/species level. Working with intermediate hosts allows the expansion of knowledge of taxonomic and genetic diversity of cestodes in wildlife, as well as elucidation of their life cycles.

15.
Molecules ; 18(4): 3972-4001, 2013 Apr 04.
Artículo en Inglés | MEDLINE | ID: mdl-23558540

RESUMEN

A series of novel 2-pyridylbenzimidazole derivatives was rationally designed and synthesized based on our previous studies on benzimidazole 14, a CB1 agonist used as a template for optimization. In the present series, 21 compounds displayed high affinities with Ki values in the nanomolar range. JM-39 (compound 39) was the most active of the series (KiCB1 = 0.53 nM), while compounds 31 and 44 exhibited similar affinities to WIN 55212-2. CoMFA analysis was performed based on the biological data obtained and resulted in a statistically significant CoMFA model with high predictive value (q2 = 0.710, r2 = 0.998, r2pred = 0.823).


Asunto(s)
Bencimidazoles/síntesis química , Bencimidazoles/farmacología , Cannabinoides/química , Receptor Cannabinoide CB1/metabolismo , Benzoxazinas/química , Humanos , Ligandos , Modelos Biológicos , Morfolinas/química , Naftalenos/química , Conformación Proteica , Relación Estructura-Actividad Cuantitativa
16.
Animals (Basel) ; 13(4)2023 Feb 05.
Artículo en Inglés | MEDLINE | ID: mdl-36830341

RESUMEN

The establishment of a state of immunotolerance in the female reproductive tract is important for embryo development, implantation and placentation. Llamas are induced ovulators and more than 98% of pregnancies occur in the left uterine horn. The objective of this study was to determine the uterine immune response of llamas in different stages of the reproductive cycle. Adult llamas (n = 20) were examined daily by transrectal ultrasonography to determine follicular growth and then randomly assigned to four groups: Follicular phase (n = 5); Luteal phase induced by an intramuscular administration of 50 ug of GnRH analogue (n = 5); Luteal phase induced by intrauterine infusion of seminal plasma (n = 5); and Luteal phase induced by mating (n = 5). Uterine fluid was collected separately from both uterine horns by non-surgical flushing to determine the presence of cells, total proteins and concentration of IL-1ß, IL-6, IL-8, IFN γ, TNF-α and PGE2. Inflammatory cells were not observed in the uterine fluid and total protein pattern and inflammatory mediators did not differ between the left and the right horn amongst groups. Llamas treated with an intrauterine infusion of seminal plasma showed the highest concentration of total proteins, inflammatory cytokines PGE2, IL-8 and IL-1ß in the uterine fluid. In conclusion, seminal plasma is made up of significant numbers of signaling molecules that are able to modify the uterine immune response in llamas.

17.
Genes (Basel) ; 14(4)2023 04 07.
Artículo en Inglés | MEDLINE | ID: mdl-37107634

RESUMEN

The blue mussel Mytilus chilensis is an endemic and key socioeconomic species inhabiting the southern coast of Chile. This bivalve species supports a booming aquaculture industry, which entirely relies on artificially collected seeds from natural beds that are translocated to diverse physical-chemical ocean farming conditions. Furthermore, mussel production is threatened by a broad range of microorganisms, pollution, and environmental stressors that eventually impact its survival and growth. Herein, understanding the genomic basis of the local adaption is pivotal to developing sustainable shellfish aquaculture. We present a high-quality reference genome of M. chilensis, which is the first chromosome-level genome for a Mytilidae member in South America. The assembled genome size was 1.93 Gb, with a contig N50 of 134 Mb. Through Hi-C proximity ligation, 11,868 contigs were clustered, ordered, and assembled into 14 chromosomes in congruence with the karyological evidence. The M. chilensis genome comprises 34,530 genes and 4795 non-coding RNAs. A total of 57% of the genome contains repetitive sequences with predominancy of LTR-retrotransposons and unknown elements. Comparative genome analysis of M. chilensis and M. coruscus was conducted, revealing genic rearrangements distributed into the whole genome. Notably, transposable Steamer-like elements associated with horizontal transmissible cancer were explored in reference genomes, suggesting putative relationships at the chromosome level in Bivalvia. Genome expression analysis was also conducted, showing putative genomic differences between two ecologically different mussel populations. The evidence suggests that local genome adaptation and physiological plasticity can be analyzed to develop sustainable mussel production. The genome of M. chilensis provides pivotal molecular knowledge for the Mytilus complex.


Asunto(s)
Mytilus edulis , Mytilus , Animales , Mytilus/genética , Chile , Acuicultura , Cromosomas/genética
18.
Animals (Basel) ; 13(6)2023 Mar 09.
Artículo en Inglés | MEDLINE | ID: mdl-36978545

RESUMEN

The neurotrophin beta-nerve growth factor (NGF), which is present in the semen of different mammals, elicits potent ovulatory and luteotrophic actions in llamas following systemic administration. Here, we determine if purified NGF given intramuscularly (IM) during the preovulatory stage affects the corpus luteum (CL), hormone production, endometrial gene expression, and pregnancy rate of dairy heifers. Holstein-Friesian heifers were estrus-synchronized using estradiol benzoate (EB) plus an intravaginal progesterone (P4) device (DIB). After eight days, the device was removed and cloprostenol was given IM; the next day (day 9), heifers received EB IM plus one of the following: (i) 1 mg of NGF (NGF D9 group), (ii) 1 mg of NGF 32 h after EB (NGF D10 group), or (iii) phosphate buffer saline (control group). To measure pregnancy rates, heifers were treated similarly, then artificially inseminated with sexed semen 48-52 h after DIB removal, then an ultrasound was conducted 30 days after insemination. The females given NGF along with EB (NGF D9) showed significantly higher luteinizing hormone (LH) concentrations, larger CL vascular areas, and higher plasma P4 concentrations than the NGF D10 and control animals. Downregulation of the P4 receptor (PGR), and upregulation of both lipoprotein lipase (LPL) and Solute Carrier Family 6 member 14 (SLC6A14) endometrial genes, were detected in NGF D9 heifers. Furthermore, these heifers had a 10% higher pregnancy rate than the control group. We conclude that the higher P4 output, in response to the early NGF administration, led to the enhanced gene expression of transcripts related to uterine receptivity that may result in enhanced pregnancy rates.

19.
Molecules ; 17(2): 1388-407, 2012 Feb 03.
Artículo en Inglés | MEDLINE | ID: mdl-22306829

RESUMEN

A series of novel benzo[b]thiophen-2-yl-3-(4-arylpiperazin-1-yl)-propan-1-one derivatives 6a-f, 7a-f and their corresponding alcohols 8a-f were synthesized and evaluated for their affinity towards 5-HT(1A) receptors. The influence of arylpiperazine moiety and benzo[b]thiophene ring substitutions on binding affinity was studied. The most promising analogue, 1-(benzo[b]thiophen-2-yl)-3-(4-(pyridin-2-yl)piperazin-1-yl)propan-1-one (7e) displayed micromolar affinity (K(i) = 2.30 µM) toward 5-HT(1A) sites. Docking studies shed light on the relevant electrostatic interactions which could explain the observed affinity for this compound.


Asunto(s)
Piperazinas/síntesis química , Piperazinas/farmacología , Receptor de Serotonina 5-HT1A/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Modelos Moleculares , Piperazinas/química , Espectrometría de Masa por Ionización de Electrospray
20.
Artículo en Inglés | MEDLINE | ID: mdl-35065314

RESUMEN

We assessed the adaptive contribution of the mitochondrial genes involved with the respiratory chain and oxidative phosphorylation of the blue mussel Mytilus chilensis, a native and heavily exploited species in the inner sea of Chiloé Island, southern Chile. The assembled mitochondrial transcriptome of individuals from two ecologically different farm-impacted natural seedbeds, Cochamó (41°S) and Yaldad (42°S), represented about 4.5% of the whole de novo transcriptome of the species and showed location and tissue (gills, mantle) specific expression differences in 13 protein-coding mitochondrial genes. The RNA-Seq analysis detected differences in the number of up-regulated mitogenes between individuals from Cochamó (7) and Yaldad (11), some being tissue-specific (ND4L and COX2). However, the analysis did not detect transcripts-per-million (TPM = 0) of ND2 and ND5 in gills and ATP6 in mantle samples from Cochamó. Likewise, for ND6 and ATP8 in any sample. Several monomorphic location-specific mitochondrial genetic variants were detected in samples from Cochamó (78) and Yaldad (207), representing standing genetic variability to optimize mitochondrial functioning under local habitats. Overall, these mitochondrial transcriptomic differences reflect the impact of environmental conditions on the mitochondrial genome functioning and offer new markers to assess the effects on mussel fitness of habitat translocations, a routine industry practice. Likewise, these mitochondrial markers should help monitor and maintain adaptive population differences in this keystone and heavily exploited native species.


Asunto(s)
Genoma Mitocondrial , Mytilus , Animales , Branquias , Humanos , Mytilus/genética , RNA-Seq , Transcriptoma
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