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Melipona beecheii pot-pollen is a natural product that has barely been studied, unlike other hive products such as honey and propolis. Its application has been reported since ancient times in traditional Mayan medicine, and it is also a functional food with high nutritional value. In the present study, samples of ethanolic pot-pollen extracts from five locations in the Yucatán Peninsula were analyzed to determine their antibacterial and antioxidant properties. All the extracts showed activity against five medically important bacteria; Pseudomonas aeruginosa and Listeria monocytogenes were the most susceptible bacteria in all samples. The evaluated antioxidant activity was higher than that reported by other studies. Palmitic, linoleic, and linolenic fatty acids and their respective ethyl ethers were detected by Gas Chromatography-Mass Spectrometry (GC-MS) in all samples in different concentrations. Based on these results, pot-pollen extract from Mama, Yucatán exhibited the best biological activities (Minimum Inhibitory Concentrations (MICs) between 6 and 40 mg/mL, EC50 DPPH 28 µg/mL, EC50 RP 30 µg/mL), which could be related to a higher content of unsaturated fatty acids and their ethyl esters. The present study demonstrates that M. beecheii pot-pollen has therapeutic potential in addition to its benefits as a nutritional supplement.
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In this study, we synthesized a series of seven benzimidazole derivatives incorporating the structural acidic framework of angiotensin II (Ang II) type 1 receptor (AT1R) antagonists (ARA-II) employing a three-step reaction sequence. The chemical structures were confirmed by 1H NMR, 13C NMR and mass spectral data. Through biosimulation, compounds 1-7 were identified as computational safe hits, thus, best candidates underwent ex vivo testing against two distinct mechanisms implicated in hypertension: antagonism of the Ang II type 1 receptor and the blockade of calcium channel. Molecular docking studies helped to understand at the molecular level the dual vasorelaxant effects with the recognition sites of the AT1R and the L-type calcium channel. In an in vivo spontaneously hypertensive rat model (SHR), intraperitoneally administration of compound 1 at 20 mg/kg resulted in a 25 % reduction in systolic blood pressure, demonstrating both ex vivo vasorelaxant action and in vivo antihypertensive multitarget efficacy. ©2024 Elsevier.
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Antihipertensivos , Bencimidazoles , Simulación del Acoplamiento Molecular , Ratas Endogámicas SHR , Bencimidazoles/química , Bencimidazoles/farmacología , Bencimidazoles/síntesis química , Animales , Antihipertensivos/farmacología , Antihipertensivos/síntesis química , Antihipertensivos/química , Ratas , Relación Estructura-Actividad , Presión Sanguínea/efectos de los fármacos , Hipertensión/tratamiento farmacológico , Receptor de Angiotensina Tipo 1/metabolismo , Estructura Molecular , Bloqueadores del Receptor Tipo 1 de Angiotensina II/farmacología , Bloqueadores del Receptor Tipo 1 de Angiotensina II/síntesis química , Bloqueadores del Receptor Tipo 1 de Angiotensina II/química , Bloqueadores de los Canales de Calcio/farmacología , Bloqueadores de los Canales de Calcio/síntesis química , Bloqueadores de los Canales de Calcio/química , Canales de Calcio Tipo L/metabolismoRESUMEN
Fungi are a source of a variety of secondary metabolites of importance in different areas of biotechnology. Several compounds have been characterized with antioxidant, antimicrobial, and anti-inflammatory activity from fungi of the division of the Ascomycota, among which is the species Daldinia eschscholtzii, an endophyte fungus of pantropical distribution. In this study, we evaluated the effect of an ointment made with D. eschscholtzii on the wound healing of BALB/c mice. The species was corroborated using a molecular marker Internal Transcribed Spacer (ITS1 and ITS4). The extracts and dust of the fungus were considered nontoxic as they caused a mortality of <15% in the nematode Panagrellus redivivus, and experimental ointments had no adverse effects on the skin of BALB/c mice. Wounds treated with the D. eschscholtzii ointments had 99.9-100% wound contraction after 17 days, which was similar to commercial healing (positive control). As such, the ointment of D. eschscholtzii is a natural alternative to improve wound healing.
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Ratones Endogámicos BALB C , Pomadas , Cicatrización de Heridas , Animales , Cicatrización de Heridas/efectos de los fármacos , Ratones , Piel/efectos de los fármacos , Masculino , Modelos Animales de Enfermedad , Humanos , Ascomicetos/química , FemeninoRESUMEN
Parasitic diseases, including giardiasis caused by Giardia lamblia (G. lamblia), present a considerable global health burden. The limited effectiveness and adverse effects of current treatment options underscore the necessity for novel therapeutic compounds. In this study, we employed a rational design strategy to synthesize retroalbendazole (RetroABZ), aiming to address the limitations associated with albendazole, a commonly used drug for giardiasis treatment. RetroABZ exhibited enhanced in vitro activity against G. lamblia trophozoites, demonstrating nanomolar potency (IC50 = 83 nM), outperforming albendazole (189 nM). Moreover, our in vivo murine model of giardiasis displayed a strong correlation, supporting the efficacy of RetroABZ, which exhibited an eleven-fold increase in potency compared to albendazole, with median effective dose (ED50) values of 5 µg/kg and 55 µg/kg, respectively. A notable finding was RetroABZ's significantly improved water solubility (245.74 µg/mL), representing a 23-fold increase compared to albendazole, thereby offering potential opportunities for developing derivatives that effectively target invasive parasites. The molecular docking study revealed that RetroABZ displays an interaction profile with tubulin similar to albendazole, forming hydrogen bonds with Glu198 and Cys236 of the ß-tubulin. Additionally, molecular dynamics studies demonstrated that RetroABZ has a greater number of hydrophobic interactions with the binding site in the ß-tubulin, due to the orientation of the propylthio substituent. Consequently, RetroABZ exhibited a higher affinity compared to albendazole. Overall, our findings underscore RetroABZ's potential as a promising therapeutic candidate not only for giardiasis but also for other parasitic diseases.
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Antiprotozoarios , Giardia lamblia , Giardiasis , Animales , Ratones , Albendazol/química , Giardiasis/tratamiento farmacológico , Giardiasis/parasitología , Antiprotozoarios/farmacología , Antiprotozoarios/uso terapéutico , Tubulina (Proteína) , Simulación del Acoplamiento Molecular , SolubilidadRESUMEN
The aim of this work was to evaluate the vasorelaxant and antihypertensive effects of a standardized precipitate of the hydroalcoholic extract from Agastache mexicana (PPAm), comprising ursolic acid, oleanolic acid, acacetin, luteolin and tilianin, among others. In the ex vivo experiments, preincubation with L-NAME (nonspecific inhibitor of nitric oxide synthases) reduced the relaxation induced by PPAm; nevertheless, preincubation with indomethacin (nonspecific inhibitor of cyclooxygenases) did not generate any change in the vasorelaxation, and an opposed effect was observed to the contraction generated by CaCl2 addition. Oral administration of 100 mg/kg of PPAm induced a significant acute decrease in diastolic (DBP) and systolic (SBP) blood pressure in spontaneously hypertensive rats, without changes in heart rate. Additionally, PPAm showed a sustained antihypertensive subacute effect on both DBP and SBP for 10 days compared to the control group. On the other hand, human umbilical vein cells treated with 10 µg/mL of PPAm showed a significant reduction (p < 0.05) in intracellular adhesion molecule-1, compared to the control, but not on vascular cell adhesion molecule-1. In conclusion, PPAm induces a significant antihypertensive effect in acute- and subacute-period treatments, due to its direct vasorelaxant action on rat aortic rings through NO production and Ca2+ channel blockade.
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Salvia hispanica L., commonly known as chía, and its seeds have been used since ancient times to prepare different beverages. Due to its nutritional content, it is considered a dietary ingredient and has been reported with many health benefits. Chia seed components are helpful in cardiovascular disease (CVD) by reducing blood pressure, platelet aggregation, cholesterol, and oxidation. Still, its vasodilator effects on the vascular system were not reported yet. The hexanic (HESh), dichloromethanic (DESh), and methanolic (MESh) extracts obtained from chía seeds were evaluated on an aortic ring ex-vivo experimental model. The vasorelaxant efficacy and mechanism of action were determined. Also, phytochemical data was obtained through 13C NMR-based dereplication. The MESh extract showed the highest efficacy (Emax = 87%), and its effect was partially endothelium-dependent. The mechanism of action was determined experimentally, and the vasorelaxant curves were modified in the presence of L-NAME, ODQ, and potassium channel blockers. MESh caused a relaxing effect on KCl 80 mM-induced contraction and was less potent than nifedipine. The CaCl2-induced contraction was significantly decreased compared with the control curve. Phytochemical analysis of MESh suggests the presence of mannitol, previously reported as a vasodilator on aortic rings. Our findings suggest NO-cGMP pathway participation as a vasodilator mechanism of action of S. hispanica seeds; this effect can be attributed, in part, to the mannitol presence. S. hispanica could be used in future research focused on antihypertensive therapies.
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Salvia hispanica , Vasodilatadores , Vasodilatadores/farmacología , Óxido Nítrico , NifedipinoRESUMEN
Lomentospora prolificans is a pathogenic and multidrug-resistant fungus that can infect both immunocompetent and immunocompromised patients, with mortality rates up to 87%. The World Health Organization (WHO) included this fungal species in its first list of 19 priority fungal pathogens, which focused on fungal pathogens that can cause invasive acute and subacute systemic fungal infections. Therefore, there is a growing interest in finding new therapeutic alternatives. In this work, the synthesis of twelve α-aminophosphonates by the microwave-assisted Kabachnik-Fields reaction and twelve α-aminophosphonic acids by a monohydrolysis reaction is reported. All compounds were evaluated by the agar diffusion method as a preliminary screening in comparison with voriconazole, showing inhibition halos for compounds 7, 11, 13, 22 and 27. The five active compounds in the preliminary tests were evaluated against five strains of L. prolificans following protocol M38-A2 from CLSI. The results showed that these compounds exhibit antifungal activity in the concentration range of 900->900 µg/mL. Cytotoxicity against healthy COS-7 cells was also evaluated by the MTT assay, and it was shown that compound 22 was the least cytotoxic, with a viability of 67.91%, comparable to the viability exhibited by voriconazole (68.55%). Docking studies showed that the possible mechanism of action of the active compounds could be through the inhibition of the enzyme lanosterol-14-alpha-demethylase in an allosteric hydrophobic cavity.
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Micosis , Scedosporium , Humanos , Antifúngicos/farmacología , Antifúngicos/uso terapéutico , Voriconazol/farmacología , Microondas , Micosis/tratamiento farmacológico , Pruebas de Sensibilidad MicrobianaRESUMEN
Microbial degradation of aromatic hydrocarbons is an emerging technology, and it is well recognized for its economic methods, efficiency, and safety; however, its exploration is still scarce and greater emphasis on cyanobacteria-bacterial mutualistic interactions is needed. We evaluated and characterized the phenanthrene biodegradation capacity of consortium dominated by Fischerella sp. under holoxenic conditions with aerobic heterotrophic bacteria and their molecular identification through 16S rRNA Illumina sequencing. Results indicated that our microbial consortium can degrade up to 92% of phenanthrene in five days. Bioinformatic analyses revealed that consortium was dominated by Fischerella sp., however different members of Nostocaceae and Weeksellaceae, as well as several other bacteria, such as Chryseobacterium, and Porphyrobacter, were found to be putatively involved in the biological degradation of phenanthrene. This work contributes to a better understanding of biodegradation of phenanthrene by cyanobacteria and identify the microbial diversity related.
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In the present study, the nematicidal and acaricidal activity of three biosurfactants (BS) produced by strains of the Bacillus genus was evaluated. The BS produced by the Bacillus ROSS2 strain presented a mortality of 39.29% in juveniles (J2) of Nacobbus aberrans at a concentration of 30 mg/mL, this same strain is the one that presented the highest mortality in Tyrophagus putrescentiae, which was 57.97% at a concentration of 39 mg/mL. The BS were qualitatively identified by thin layer chromatography and are lipid in nature based on the retention factor (Rf). While the GC-MS analysis identified two main compounds that are 4,7-Methano-1H-indene-2,6-dicarboxylic acid, 3a,4,7,7a-tetrahydro-1, and Methyl 4-(pyrrol-1-yl)-1,2,5-oxadiazole-3-carboxylate1, which is the polar part indicated by the presence of dicarboxylic acid and carboxylate groups; while the non-polar portion can be interpreted as a hydrocarbon chain of variable length. Based on the present results, BS can be an alternative for the biocontrol of the root-knot nematode N. aberrans and the mite T. putrescentiae.
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Acaricidas , Bacillus , Tylenchoidea , Animales , Acaricidas/farmacología , PyroglyphidaeRESUMEN
Flavonoids are naturally occurring compounds widely distributed in the Citrus genus. These natural compounds have many health benefits, mainly for metabolic and cardiovascular diseases. In fact, some these compounds are components of drug products with approved indications for peripheral vascular insufficiency and hemorrhoids. However, information on pharmacological effects of these compounds remains disperse and there is scarce comprehensive analysis of whole data and evidence. These kinds of evidence analyses could be necessary in drug design and the development of novel and innovate drug products in diabetes and hypertension. We aimed to systematically search for evidence on the efficacy of citroflavonoids in diabetes and hypertension in in vivo models. We searched four literature databases based on a PICO strategy. After database curation, twenty-nine articles were retrieved to analyze experimental data. There was high heterogeneity in both outcomes and methodology. Naringenin and hesperetin derivates were the most studied citroflavonoids in both experimental models. More investigation is still needed to determine its potential for drug design and development.
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Citrus , Diabetes Mellitus , Hipertensión , Hipertensión/tratamiento farmacológico , Diabetes Mellitus/tratamiento farmacológico , Descubrimiento de Drogas , Flavonoides/farmacología , Flavonoides/uso terapéuticoRESUMEN
Panulirus argus virus 1 (PaV1) (Family Mininucleoviridae) causes chronic and systemic infection in wild juvenile spiny lobsters Panulirus argus (Latreille, 1804), ending in death by starvation and metabolic wasting. In marine decapods, the antennal gland is involved in osmoregulation and excretion. In this compact organ, fluid is filtered from the hemolymph, and ions are reabsorbed to produce a hypotonic urine. Although PaV1 is released with the urine in infected individuals, little is known regarding the metabolic effect of PaV1 in the antennal gland. The objective of this study was to perform a comparative evaluation of the metabolic profile of the antennal gland of clinically PaV1-infected lobsters versus those with no clinical signs of infection, using proton nuclear magnetic resonance analysis. Overall, 48 compounds were identified, and the most represented metabolites were those involved in carbohydrate, amino acid, energy, and nucleotide metabolism. Most of the metabolites that were down-regulated in the infected group were essential and non-essential amino acids. Some metabolites involved in the urea cycle and carbohydrate metabolism were also altered. This study represents a first approach to the metabolic evaluation of the antennal gland. We broadly discuss alterations in the content of several proteinogenic and non-proteinogenic amino acids and other key metabolites involved in energetic and nucleotide metabolism.
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Crangonidae , Palinuridae , Aminoácidos , Animales , Región del Caribe , Virus ADN , NucleótidosRESUMEN
In this paper, we report the synthesis of block and random copolymers of 2-acrylamido-2-methyl-1-propane sulfonic acid (AMPS) and methyl methacrylate (MMA), with different AMPS feed ratios. These solution-processable copolymers with strongly sulfonated acid groups resulted in membranes with tunable ion exchange (IEC) and water absorption capacities. AFM images confirmed the microphase separation of PAMPS-b-PMMA-1:1 block copolymer membrane, annealed under the appropriate conditions. The resulting copolymers from the random combination of a 1:1 molar ratio of AMPS and MMA monomers are effective at enhancing the esterification conversion of acetic acid, when compared with a reaction catalyzed by PAMPS-b-PMMA block copolymers and the previously studied catalytic membranes. With the PAMPS-co-PMMA-1:1 membrane, the esterification reaction using acetic acid achieved 85% isopropyl acetate. These results are closely correlated with the increase in IEC (2.63 mmol H+g-1) and the relationship between weight loss (20.3%) and swelling degree (68%) in 2-propanol.
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Low-cost substrates are an exciting alternative for bioprocesses; however, their complexity can affect microorganism metabolism with non-desirable outcomes. This work evaluated banana peel extract (BPE) as a growth medium compared to commercial Yeast-Malt (YM) broth in the native and non-conventional yeast Rhodotorula mucilaginosa UANL-001L. The production of carotenoids, fatty acids, and exopolysaccharides (EPS) was also analyzed. Biomass concentration (3.9 g/L) and growth rate (0.069 g/h) of Rhodotorula mucilaginosa UANL-001L were obtained at 200 g/L of BPE. Yields per gram of dry biomass for carotenoids (317 µg/g) and fatty acids (0.55 g/g) showed the best results in 150 g/L of BPE, while 298 µg/g and 0.46 mg/g, respectively, were obtained in the YM broth. The highest yield of EPS was observed in 50 g/L of BPE, a two-fold increase (160.1 mg/g) compared to the YM broth (76.3 mg/g). The fatty acid characterization showed that 100 g/L of BPE produced 400% more unsaturated compounds (e.g., oleic and ricinoleic acid) than the YM broth. Altogether, these results indicate that BPE is a suitable medium for producing high-value products with potential industrial applications.
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Musa , Rhodotorula , Carotenoides/metabolismo , Medios de Cultivo/metabolismo , Ácidos Grasos/metabolismo , Rhodotorula/metabolismo , LevadurasRESUMEN
The Scedosporium genus is an emerging pathogen with worldwide prevalence and high mortality rates that gives multidrug resistance to antifungals; therefore, pharmacological alternatives must be sought for the treatment of diseases caused by this fungus. In the present project, six new α-aminophosphates were synthesized by the Kabachnik-Fields multicomponent reaction by vortex agitation, and six new monohydrolyzed α-aminophosphonic acids were synthesized by an alkaline hydrolysis reaction. Antifungal activity was evaluated using the agar diffusion method as an initial screening to determine the most active compound compared to voriconazole; then it was evaluated against 23 strains of the genus Scedosporium following the M38-A2 protocol from CLSI (activity range: 648.76-700 µg/mL). Results showed that compound 5f exhibited the highest antifungal activity according to the agar diffusion method (≤1 mg/mL). Cytotoxicity against healthy COS-7 cells was also evaluated by the MTT assay and it was shown that compound 5f exhibits a lower toxicity in comparison to voriconazole at the same concentration (1000 µM). A docking study was conducted afterwards, showing that the possible mechanism of action of the compound is through the inhibition of allosteric 14-α-demethylase. Taking these results as a basis, 5f is presented as a compound with attractive properties for further studies.
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Scedosporium , Agar , Antifúngicos/farmacología , Pruebas de Sensibilidad Microbiana , Simulación del Acoplamiento Molecular , Triazoles/farmacología , Voriconazol/farmacologíaRESUMEN
In current work, we prepared a series of nine 4-benzyloxy-5-benzylidene-1,3-thiazolidine-2,4-diones using a two-step pathway. Compounds 1-9 were tested in vitro using a set of three proteins recognized as important targets in diabetes and related diseases: PPARα, PPARγ, and GLUT-4. Compounds 1-3, 5, and 7 showed significant increases in the mRNA expression of PPARγ and GLUT-4, whereas compounds 1-3 did it over PPARα. Compounds 1-3 were identified as a dual PPAR α/γ modulators and were selected for evaluating the in vivo antidiabetic action at 100 mg/kg dose, being orally actives and decreasing blood glucose concentration in a hyperglycemic mice model, as well as reducing the triacylglycerides levels in normolipidemic rats. Docking and molecular dynamics studies were conducted to clarify the dual effect and binding mode of compounds 1-3 on both PPARs. Compounds 2 and 3 exhibited robust in vitro and in vivo efficacy and could be considered dual PPAR modulators with antidiabetic and antidyslipidemic effects.
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Hipoglucemiantes , PPAR gamma , Animales , Hipoglucemiantes/química , Hipoglucemiantes/farmacología , Hipoglucemiantes/uso terapéutico , Lípidos , Ratones , PPAR alfa/metabolismo , PPAR gamma/metabolismo , Ratas , Tiazolidinas/farmacologíaRESUMEN
This study was performed to evaluate and compare the pharmacokinetic parameters between two dosage formulations of hesperidin and naringenin: mixture and tablet. Our objective was to determine that the flavonoid tablet does not significantly modify the pharmacokinetic parameters compared with the mixture. For this study, we administered 161 mg/kg of either mixture (Mix-160) or tablet composed of hesperidin and by intragastric administration. Blood microsamples were collected from tail vein up to 24 h. Serum flavonoid extraction was performed by solid phase extraction and analyzed by LC-MS/MS of triple quadrupole (QqQ). Serum concentration vs. time plot showed that data fitted for a first-order model. The pharmacokinetic parameters were calculated by a noncompartmental model. The results showed that the absorption constant is higher than the elimination constant. The first concentration was found at five minutes, and minimal concentration at 24 h after administration, suggesting a enterohepatic recirculation phenomena and regulation of liver cytochromes' activity. We did not find meaningful differences between the pharmacokinetic parameters of both samples. We concluded that tablet form did not interfere with the bioavailability of hesperidin and naringenin, and it could be a suitable candidate for developing a drug product.
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Disponibilidad BiológicaRESUMEN
Several 4H-pyran derivatives were designed and synthesized previously as vasorelaxant agents for potential antihypertensive drugs. In this context, the objective of the present investigation was to determine the functional mechanism of vasorelaxant action of 6-amino-3-methyl-4-(2-nitrophenyl)-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile (1: ) and its in vivo antihypertensive effect. Thus, compound 1: showed significant vasorelaxant action on isolated aorta rat rings pre-contracted with serotonin or noradrenaline, and the effect was not endothelium-dependent. Compound 1: induced a significant relaxant effect when aortic rings were contracted with KCl (80 mM), indicating that the main mechanism of action is related to L-type calcium channel blockade. Last was corroborated since compound 1: induced a significant concentration-dependent lowering of contraction provoked by cumulative CaCl2 adding. Moreover, compound 1: was capable to block the contraction induced by FPL 64176, a specific L-type calcium channel agonist, in a concentration-dependent manner. On the other hand, docking studies revealed that compound 1: interacts on two possible sites of the L-type calcium channel and it had better affinity energy (-7.80+/-0.00 kcal/mol on the best poses) than nifedipine (-6.86+/-0.14 kcal/mol). Finally, compound 1: (50 mg/kg) showed significant antihypertensive activity, lowering the systolic and diastolic blood pressure on spontaneously hypertensive rats (SHR) without modifying heart rate.
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Antihipertensivos , Vasodilatadores , Animales , Antihipertensivos/farmacología , Antihipertensivos/uso terapéutico , Calcio/metabolismo , Canales de Calcio , Pirazoles/farmacología , Ratas , Ratas Wistar , Vasodilatadores/farmacologíaRESUMEN
We report the chemical characterisation and toxic effects of municipal solid waste landfill leachates on the embryonic development of Danio rerio. The results of the Fourier transform infrared spectroscopy (FTIR) revealed the presence of nitrogen-containing groups and aromatic functional groups associated with highly toxic pollutants such as ammonia and heavy metal-humic complexes. Mortalities of up to 93 and 100% were observed in 1:64 and 1:32 landfill leachate dilutions, v/v, respectively. The hatching percentages of the fish were also severely affected, with very low percentages ranging from 0 to 33.3% for 1:32, 1:64 and 1:128 dilutions, v/v. Morphologically, a developmental arrest was evident for all treatments. This study reveals the high toxicity of landfill leachates that could contaminate the aquifer of the Yucatan Peninsula and threaten the health of living organisms.
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Eliminación de Residuos , Contaminantes Químicos del Agua , Animales , Desarrollo Embrionario , México , Residuos Sólidos , Instalaciones de Eliminación de Residuos , Contaminantes Químicos del Agua/análisis , Pez CebraRESUMEN
Degradation efficiency of a heavy crude oil by a marine microbial consortium was evaluated in this study, with and without the addition of a chemical dispersant (Nokomis 3-F4). 15.50% of total petroleum hydrocarbons (TPH) were removed after 15 days of incubation without dispersant, with a degradation rate of 2.39 ± 0.22 mg L-1 day-1. In contrast, the addition of Nokomis 3-F4 increased TPH degradation up to 30.81% with a degradation rate of 5.07 ± 0.37 mg L-1 day-1. 16S rRNA gene sequencing indicated a dominance of the consortium by Achromobacter and Alcanivorax. Nonetheless, significant increases in the relative abundance of Martelella and Ochrobactrum were observed with the addition of Nokomis 3-F4. These results will contribute to further environmental studies of the Gulf of Mexico, where Nokomis 3-F4 can be used as chemical dispersant.
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Contaminación por Petróleo , Petróleo , Contaminantes Químicos del Agua , Biodegradación Ambiental , Consorcios Microbianos , Contaminación por Petróleo/análisis , ARN Ribosómico 16S/genética , Agua , Contaminantes Químicos del Agua/análisisRESUMEN
Benzo[α]pyrene (BaP), a lipophilic polycyclic aromatic hydrocarbon (PAH), is a contaminant widely distributed in aquatic systems. Its presence in freshwater organisms is of great concern; particularly in Nile tilapia (Oreochromis niloticus), due to its economic relevance. The aim of this study is to evaluate the effects of acute and sub-chronic BaP exposures on molecular growth/development responses, toxicity to DNA pathways and xenobiotic metabolism. Negative morphometric changes (the growth condition factor, hepatosomatic and gonadosomatic indices), the fluorescent aromatic compounds (FACs) in bile were also studied in order to understand the mechanisms of action of BaP. Genes involved in the growth hormone GH/insulin-like growth factor 1 (IGF-1) were measured, such as IGF1-2 with the growth hormone receptor gene expression GHR1-2, and the endocrine disruption biomarker vitellogenin (VTG). Acute exposure elicited changes in the GH/IGF axis, mainly in the GHR1 and in IGF1 mRNA levels without affecting the GHR2 expression. While sub-chronic exposure had less effect on both GHR and IGF genes. The most notable tissue-specific effects and morphometric endpoints were observed upon sub-chronic exposure, such as changes in key genes involved in detoxification, DNA damage, and altered reproductive morphological endpoints; showing that sub-chronic BaP doses have longer-lasting toxic effects. This study shows that sub-chronic BaP exposure may compromise the health of Nile tilapia and sheds light on the changes of the GH/IGF axis and the biotransformation of the xenobiotics due to the presence of this contaminant.