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1.
J Toxicol Environ Health A ; 87(18): 730-751, 2024 Sep 16.
Artículo en Inglés | MEDLINE | ID: mdl-38904345

RESUMEN

Achyrocline satureioides, popularly called "marcela" in Brazil, is used in traditional medicine in South America. A. satureioides, inflorescences are used for many conditions, including to minimize the Sars-Cov-2 symptoms. Therefore, the aim of this study was to determine the toxicity profile of A. satureioides aqueous extract (ASAE), using the Caenorhabditis elegans (C. elegans) alternative model. Survival, reproduction, development, and transgenerational assays were performed. The effects of ASAE were investigated under conditions of thermal stress and presence of oxidant hydrogen peroxide (H2O2). In addition, C. elegans strains containing high antioxidant enzyme levels and elevated lineages of daf-16, skn-1 and daf-2 regulatory pathways were examined. The ASAE LC50 value was found to be 77.3 ± 4 mg/ml. The concentration of ASAE 10 mg/ml (frequently used in humans) did not exhibit a significant reduction in worm survival at either the L1 or L4 stage, after 24 or 72 hr treatment. ASAE did not markedly alter the body area. In N2 strain, ASAE (10 or 25 mg/ml) reversed the damage initiated by H2O2. In addition, ASAE protected the damage produced by H2O2 in strains containing significant levels of sod-3, gst-4 and ctl - 1,2,3, suggesting modulation in these antioxidant systems by this plant extract. ASAE exposure activated daf-16 and skn-1 stress response transcriptional pathways independently of daf-2, even under extreme stress. Data suggest that ASAE, at the concentrations tested in C. elegans, exhibits a reliable toxicity profile, which may contribute to consideration for safe use in humans.


Asunto(s)
Achyrocline , Caenorhabditis elegans , Extractos Vegetales , Animales , Caenorhabditis elegans/efectos de los fármacos , Extractos Vegetales/toxicidad , Extractos Vegetales/farmacología , Achyrocline/química , Proteínas de Caenorhabditis elegans/metabolismo , Proteínas de Caenorhabditis elegans/genética
2.
Phytother Res ; 37(11): 5354-5365, 2023 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-37583121

RESUMEN

We evaluated the impact of an Achyrocline satureioides inflorescence infusion on the clinical outcomes of viral respiratory infections, including those caused by SARS-CoV-2, in a monocentric, randomized, open-label, placebo-controlled clinical trial. Patients with symptoms of viral respiratory infection, including suspected cases of COVID-19, were included and assigned to receive either A. satureioides (n = 57) or Malus domestica (n = 67) infusions twice a day for 14 days. All participants were included before the RT-PCR results, performed using a nasopharyngeal swab. The patients were further divided into subgroups according to real-time polymerase chain reaction results: SARS-CoV-2-positive and SARS-CoV-2-negative subgroups for statistical analyses. We assessed clinical outcomes, such as the latency to resolution of cough, dyspnea, fever, sore throat, chest pain, smell and taste dysfunctions, diarrhea, nausea, abdominal pain, and loss of appetite; hospitalization; and mortality with questionnaires and medical records. The subjects that received early A. satureioides infusion showed a significant reduction in the average number of days with respiratory and neurological symptoms compared with the control group (M. domestica infusion). We conclude that A. satureioides is a safe agent and, in combination with standard care, improves viral respiratory infection symptoms, especially those related to COVID-19.


Asunto(s)
Achyrocline , COVID-19 , Humanos , SARS-CoV-2 , Proyectos de Investigación , Terapia Combinada , Resultado del Tratamiento
3.
J Dairy Res ; 90(4): 376-381, 2023 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-38186216

RESUMEN

This research paper presents the development and evaluation of pioneering nanocomposites (NCs) based on the combination of k-carrageenan and linseed mucilage. When loaded with macela extract nanoemulsion they present an innovative approach for the sustained release of antimicrobial herbal constituents, specifically tailored for bovine mastitis treatment. The NCs, encompassing various ratios of k-carrageenan and linseed mucilage polymers (8:2, 7:3, and 5:5 w/w) with 1.25 mg of macela extract/g of gel, underwent in vitro assessment, emphasizing viscosity, degradation speed, release of herbal actives from macela nanoemulsion and antimicrobial activity. The NCs exhibited thermoreversible characteristics, transitioning from liquid at 60°C to a gel at 25°C. NCs allowed a gradual release of phenolic compounds, reaching approximately 80% of total phenolics release (w/v) within 72 h. NCs inhibited the growth of MRSA (ATCC 33592) until 8 h of incubation. No toxic effect in vitro of NCs was found on MAC-T cells. Thus, the developed materials are relevant for the treatment of bovine mastitis, especially in the dry period, and the data support future evaluations in vivo.


Asunto(s)
Achyrocline , Antiinfecciosos , Enfermedades de los Bovinos , Lino , Mastitis Bovina , Nanocompuestos , Femenino , Bovinos , Animales , Carragenina , Mastitis Bovina/tratamiento farmacológico , Aceite de Linaza , Extractos Vegetales/farmacología
4.
Exp Parasitol ; 236-237: 108252, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35381222

RESUMEN

Although Brazilian livestock is considered one of the most productive in the world, the losses caused by parasites still greatly limit these activities and its incorrect control through traditional synthetic chemicals has caused problems such as parasitic resistance. The present study evaluated the anthelmintic and acaricidal action of ethanolic extract (EE) and essential oil (OE) obtained from Achyrocline satureioides inflorescences against an endo and an ectoparasite of great importance in sheep and cattle. The action against Haemonchus contortus was evaluated by the Larval Development Test (LDT) and the Egg Hatching Test (EHT), while the acaricidal potential against Rhipicephalus (Boophilus) microplus was evaluated by the Adult Immersion Test (AIT) and Larval Package Test (LPT). Chemical analyzes were performed by liquid chromatography coupled to mass of spectrometry (LC-MS) and gas chromatography coupled to mass spectrometry (GC-MS) in order to evaluate the chemical composition of EE and EO, respectively. Luteolin (m/z 285), quercetin (m/z 301) and methyl quercetin (m/z 315) were the major compounds detected in the A. satureioides EE, while 41 compounds were identified in EO. Among them, the major compounds were caryophyllene oxide (15.4%), limonene (10.9%), trans-calamenene + Î´-cadinene (8.0%), (E)-caryophyllene (5.5%), spathulenol (5.1%) and α-pinene (4.5%). Against H. contortus, by EHT, the EE and EO showed LC50 of 83.14 mg mL-1 and 10.42 mg mL-1, respectively. In LDT, LC50 were 0.16 mg mL-1 and 0.42 mg mL-1, respectively by EE and EO. In the AIT assay for R. (B.) microplus tick LC50 obtained for EE and EO were 76.43 mg mL-1 and 114.35 mg mL-1, respectively. EE at 100 mg mL-1 completely inhibited egg laying, while the EO at 50 mg mL-1 completely inhibited larval hatching. No significant larvicidal effect was observed in LPT for both extracts. The EE and EO presented a high efficacy at low concentrations in the inhibition of egg hatching and larval development of H. contortus. Although both extracts did not show consistent larvicidal action, the results were significant in inhibiting the oviposition of R. (B.) microplus engorged females.


Asunto(s)
Acaricidas , Achyrocline , Antihelmínticos , Aceites Volátiles , Rhipicephalus , Acaricidas/farmacología , Animales , Antihelmínticos/farmacología , Bovinos , Femenino , Cromatografía de Gases y Espectrometría de Masas , Larva , Aceites Volátiles/química , Aceites Volátiles/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Quercetina/farmacología , Ovinos
5.
Exp Appl Acarol ; 87(4): 351-363, 2022 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-36001248

RESUMEN

The tick Rhipicephalus microplus (Canestrini) is a major economic hurdle to the global livestock industry. The incorrect and indiscriminate control carried out by synthetic chemical compounds has contributed to the emergence of parasite resistance present today to many products available in the veterinary market. Effective, economically viable and potentially safe alternatives need to be investigated, including herbal medicine and biological control by entomopathogenic fungi. In this study, extracts from Achyrocline satureioides (Lam.) DC. obtained by extraction with solvents of different polarities associated and not associated with the entomopathogenic fungus Beauveria bassiana (Balsamo-Crivelli) Vuillemin were evaluated on different stages of the life cycle of R. microplus. The activity of plant extracts, fungus and their associations in ticks was analyzed in vitro through the adult immersion test, larval packet test and larval immersion test. The highest efficacy on engorged females (43.3%) was reached by the hexanic partition (ASh) at 5 mg/mL + fungus, reducing larval hatchability. ASh associated with B. bassiana also caused high mortality of larvae, reaching LC50 of 6.23 and 2.65 mg/mL in the packet and immersion tests, respectively. The results obtained showed that extracts, when used in combination with the fungus, have their action enhanced, reaching 100% mortality of larvae. Among the evaluated methodologies, it was observed that the larval immersion test allows better assessment, due to the time of contact with the larvae. The results obtained with A. satureioides associated with the fungus are considered promising and open new perspectives for future product development.


Asunto(s)
Achyrocline , Beauveria , Rhipicephalus , Animales , Femenino , Larva/microbiología , Control Biológico de Vectores/métodos , Extractos Vegetales/farmacología
6.
J Org Chem ; 86(18): 12813-12820, 2021 09 17.
Artículo en Inglés | MEDLINE | ID: mdl-34464127

RESUMEN

Two novel derivatives of 2-methyl-1-(2,3,4,6-tetrahydroxyphenyl)propan-1-one and (S)-2-methyl-1-(2,3,4,6-tetrahydroxyphenyl)butan-1-one (1 and 2), four novel six-membered lactone phenols (3-6), and a nor-ursane type triterpenoid (7) named Achroacid, were isolated from the aerial part of Achyrocline satureioides. The absolute configurations of 1-7 are presented by spectroscopic data and X-ray crystallographic analysis. A DP4plus evaluation was applied to determine the final stereochemistry for 1 and 2. The biosynthesis pathway of 1 and 2 was proposed. 1 has potential on anti-Gram-negative bacteria. Both 1 and 2 exhibited a significant impact on anti-H1299 cells. Compounds 3-7 showed moderate cancer cell lethality and significant anti-inflammatory activities.


Asunto(s)
Achyrocline , Triterpenos , Lactonas , Polifenoles , Esqueleto , Triterpenos/farmacología
7.
Planta Med ; 86(2): 151-159, 2020 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-31777054

RESUMEN

The biological properties of Achyrocline satureioides have been mostly ascribed to its major flavonoids quercetin (QCT), luteolin (LUT), and 3-O-methylquercetin (3OMQ). The present study aimed to optimize the extraction by dynamic maceration of the major phenolic compounds in order to obtain in a subsequent step a flavonoid-enriched fraction (FEF) using high performance countercurrent chromatography (HPCCC). A 3-level Box-Behnken design (BBD) was applied to maximize the extraction of the substances, using the plant : solvent ratio (X1 ), extraction time (X2 ), and ethanol concentration (X3 ) as factors. One-step HPCCC semipreparative separation with a solvent system composed of hexane : ethyl acetate : methanol : water (0.9 : 0.9 : 0.8 : 1.0, v/v) was employed to obtain the FEF. The second-order polynomial model was able to fit the experimental data adequately. The linear and quadratic terms of X3 were the most significant factors that affected all the responses. The positive linear term of X3 indicated a substantial increase in extraction yield, while the negative quadratic term showed a nonlinear tendency. Linear terms of X1 suggested a tendency to solvent saturation, except for QCT. The terms of X2 did not affect the responses substantially. The HPCCC method was found to be efficient and rapid for separating the FEF with 71% (w/w) flavonoid content. Overall, the developed extraction procedure coupled with HPCCC proved to be efficient for obtaining an enriched fraction with a very high content of flavonoids from A. satureioides.


Asunto(s)
Achyrocline/química , Distribución en Contracorriente/métodos , Flavonoides/aislamiento & purificación , Extractos Vegetales/aislamiento & purificación
8.
An Acad Bras Cienc ; 92(4): e20191066, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-33206785

RESUMEN

Inflammatory dermatoses are prevalent worldwide, with impacts on the quality of life of patients and their families. The aim of this study was to determine the anti-inflammatory effects of Achyrocline satureioides oily extracts and nanocapsules on the skin using a mouse model of irritant contact dermatitis induced by croton oil, and a skin inflammation model induced by ultraviolet B (UVB) radiation. The mice were treated with 15 mg/ear oily extract (HG-OLAS) or nanocapsules (HG-NCAS) of A. satureioides incorporated into Carbopol® 940 hydrogels. We found that HG-OLAS and HG-NCAS formulations reduced ear edema in croton oil-induced lesions with maximum inhibitions of 54±7% and 74±3%, respectively. HG-OLAS and HG-NCAS formulations decreased ear edema induced by UVB radiation (0.5 J/cm2), with maximum inhibitions of 68±6% and 76±2% compared to the UVB radiation group, respectively. HG-OLAS and HG-NCAS modulated myeloperoxidase (MPO) activity after croton oil induction. Furthermore, croton oil and UVB radiation for 6 and 24 h, respectively, stimulated polymorphonuclear cells infiltration. The topical treatments reduced inflammatory processes, as shown by histological analysis. Together, the data suggest that topical application of A. satureioides oily extracts and nanocapsules produced antiedematogenic and anti-inflammatory effects. They constitute a compelling alternative for treatment of skin injuries.


Asunto(s)
Achyrocline , Dermatitis por Contacto , Nanocápsulas , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Dermatitis por Contacto/tratamiento farmacológico , Edema/tratamiento farmacológico , Humanos , Hidrogeles , Irritantes/uso terapéutico , Nanocápsulas/uso terapéutico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Calidad de Vida
9.
Phytochem Anal ; 31(6): 905-914, 2020 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-32573881

RESUMEN

INTRODUCTION: Achyrocline satureioides (marcela or macela) is a plant widely used in folk medicine in South America. Recently, there has been increasing interest for the development of skin care products containing A. satureoides extracts, due to its well-documented antioxidant, antiherpetic, and wound healing properties. OBJECTIVES: The present study aimed to develop and validate a yet unexplored stability-indicating and robust ultra-fast liquid chromatography (UFLC) method for the simultaneous quantification of the main flavonoids of A. satureioides in extracts, nanoemulsions, and porcine skin layers. MATERIAL AND METHODS: The chromatographic separation of flavonoids quercetin, luteolin, and 3-O-methylquercetin was performed on a Luna C18 analytical column (100 mm × 2.0 mm i.d.; particle size 2.5 µm) using isocratic elution with methanol/phosphoric acid 1% (48:52 v/v) with a flow rate of 0.3 mL/min at 40°C. RESULTS: The method was found to be specific, linear (R > 0.998), precise, accurate, and robust for all flavonoids assayed in A. satureioides extract, nanoemulsions, and porcine ear skin. A low matrix effect was noted for all complex matrices. The stability-indicating UFLC method was evaluated by submitting isolated flavonoids, a mixture of standards, and A. satureioides extract to acidic, alkaline, oxidative, UV-A/UV-C light, and thermal stress conditions. No peaks were found co-eluting with the flavonoids of interest in all matrices. The robustness of the method was confirmed using Plackett-Burman experimental design. CONCLUSION: The short run time (8 min) and reliability of the method could be useful for the determination of A. satureioides flavonoids in topical product development since extracts of this medicinal plant have been used to treat various skin disorders.


Asunto(s)
Achyrocline , Animales , Cromatografía Líquida de Alta Presión , Cromatografía Liquida , Flavonoides/análisis , Extractos Vegetales , Reproducibilidad de los Resultados , Proyectos de Investigación , Piel/química , Porcinos
10.
Bioorg Med Chem ; 27(12): 2579-2591, 2019 06 15.
Artículo en Inglés | MEDLINE | ID: mdl-30935792

RESUMEN

Achyrocline satureioides (Lam) D.C (Compositae) is a native medicinal plant of South America traditionally utilized for its anti-inflammatory, sedative and anti-atherosclerotic properties among others. Neuroprotective effects have been reported in vivo and could be associated to its elevated content of flavonoid aglycones. In the present study we performed the isolation and structure elucidation of the major individual flavonoids of A. satureioides along with the in vitro characterization of their individual antioxidant and neuroprotective properties in order to see their putative relevance for treating neurodegeneration. Exact mass, HPLC-MS/MS and 1H NMR identified dicaffeoyl quinic acid isomers, quercetin, luteolin, isoquercitrin, and 3-O-methylquercetin as the mayor polyphenols. Flavonoids intrinsic redox properties were evaluated in the presence of the endogenous antioxidants GSH and Ascorbate. Density Functional Theory (DFT) molecular modeling and electron density studies showed a theoretical basis for their different redox properties. Finally, in vitro neuroprotective effect of each isolated flavonoid was evaluated against hydrogen peroxide-induced toxicity in a primary neuronal culture paradigm. Our results showed that quercetin was more efficacious than luteolin and isoquercitrin, while 3-O-methylquercetin was unable to afford neuroprotection significantly. This was in accordance with the susceptibility of each flavonoid to be oxidized and to react with GSH. Overall our results shed light on chemical and molecular mechanisms underlying bioactive actions of A. satureioides main flavonoids that could contribute to its neuroprotective effects and support the positive association between the consumption of A. satureioides as a natural dietary source of polyphenols, and beneficial health effect.


Asunto(s)
Achyrocline/química , Antioxidantes/química , Polifenoles/química , Sustancias Protectoras/química , Achyrocline/metabolismo , Animales , Cromatografía Líquida de Alta Presión , Teoría Funcional de la Densidad , Flavonoides/química , Flavonoides/aislamiento & purificación , Modelos Moleculares , Conformación Molecular , Neuronas/citología , Neuronas/efectos de los fármacos , Neuronas/metabolismo , Extractos Vegetales/química , Plantas Medicinales/química , Plantas Medicinales/metabolismo , Polifenoles/aislamiento & purificación , Polifenoles/farmacología , Sustancias Protectoras/aislamiento & purificación , Sustancias Protectoras/farmacología , Ratas , Ratas Sprague-Dawley , Espectrometría de Masas en Tándem
11.
J Toxicol Environ Health A ; 82(5): 321-330, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-30940006

RESUMEN

Achyrocline satureioides (LAM) D.C. is a species plant used in folk medicine with several medicinal properties; however, few studies have focused on its potential adverse effects. The aim of this study was to examine the effects of ethanolic extract of A. satureioides flowers administered during pre-mating, mating, pregnancy and postpartum period on reproductive and developmental parameters in rats. Male and female rats received by gavage 0, 250, 500 or 750 mg/kg of extract. The animals were treated from pre-mating until 13 days post-partum. Phytochemical analysis revealed the presence of important flavonoids (quercetin, luteolin, caffeic acid, rutin, and ferulic acid). In females, biochemical, hematological or gestational parameters were not markedly altered by the extract. However, an increase in calcium and thyroid stimulating hormone (TSH) levels was found in treated-dams. Although TSH and T4 levels were not significantly altered in pups, there was a rise in body weight of pups whose mothers were treated with the extract. All males treated were able to successfully copulate with treated-females. However, rats exposed to 500 and 750 mg/kg of extract exhibited a significant decrease in daily testicular sperm production and delay in sperm transit time in the epididymis. The ethanolic extract of A. satureioides flowers produced adverse effects in the male reproductive system as evidenced by diminished sperm production and transport. In addition, the extract elevated TSH levels of exposed mothers which may consequently affect the development of pups but this requires further evaluation.


Asunto(s)
Achyrocline/química , Extractos Vegetales/toxicidad , Reproducción/efectos de los fármacos , Animales , Femenino , Flores/química , Masculino , Ratas/crecimiento & desarrollo , Ratas Wistar , Pruebas de Toxicidad
12.
Phytochem Anal ; 30(2): 182-192, 2019 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-30565775

RESUMEN

INTRODUCTION: Phenolic compounds present in Achyrocline satureioides are known to have therapeutic benefits like antioxidant, anti-inflammatory, and antitumour properties. The main polyphenols present in the plant are quercetin (QCT), luteolin (LUT), 3-O-methylquercetin (3OMQ), and achyrobichalcone (ACB). However, the effective isolation and purification of these compounds from A. satureioides inflorescences are not an easy task. OBJECTIVE: To develop an efficient high-performance counter-current chromatography (HPCCC) method for quick separation and purification of naturally occurring phenolic compounds from the extract of A. satureioides. METHODOLOGY: A two-step HPCCC semi-preparative isolation method was developed using a solvent system composed of n-hexane/ethyl acetate/methanol/water (0.8:1.0:0.8:1.0) and dichloromethane/methanol/water (3.5:3.5:2.5). RESULTS: The HPCCC method was used to obtain two fractions. The first fraction (F1 ) contained high levels of ACB, among other constituents, while the second fraction (F2 ) contained mostly QCT, LUT, and 3OMQ. Besides the high ACB content, F1 contained three other flavonoid-aglycones (kaempferol, 97.3%; isokaempferide, 92.4%; and 3,3'-di-O-methylquercetin, 95.2%) identified by an ultra-performance liquid chromatography system coupled to a quadrupole time-of-flight with high-definition mass spectrometry (UPLC-QTOF/HDMS) and nuclear magnetic resonance (NMR) analysis. Purity levels of ACB, 3OMQ, QCT, and LUT were 98.0, 97.0, 97.5, and 90.2%, respectively. CONCLUSION: This is the first time that high purity ACB and six other flavonoids were obtained from A. satureioides inflorescences by HPCCC. These excellent results reveal the potential and versatility of HPCCC as a technique to produce different types of products from this plant species on a semi-preparative scale: enriched fractions, new metabolites, or high purity compounds.


Asunto(s)
Achyrocline/química , Distribución en Contracorriente/métodos , Polifenoles/aislamiento & purificación , Biflavonoides/análisis , Espectroscopía de Resonancia Magnética con Carbono-13/métodos , Luteolina/análisis , Extractos Vegetales/química , Polifenoles/normas , Espectroscopía de Protones por Resonancia Magnética/métodos , Quercetina/análogos & derivados , Quercetina/análisis , Estándares de Referencia , Espectrofotometría Ultravioleta/métodos
13.
Microb Pathog ; 105: 30-36, 2017 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-28185949

RESUMEN

Oxidative stress has been considered as a pathological mechanism that contributes to initiation and progression of cardiac injury during the Trypanosoma evansi infection. In this sense, the natural compounds with antioxidant and free radical scavenger abilities, such the Achyrocline satureioides essential oil loaded in nanocapsules (AS-NC), may be considered important approach to minimize the cardiac damage. Thus, the aim of this study was to investigate whether AS-NC treatment is able to prevents or reduce the cardiac oxidative damage in infected rats with T. evansi. Heart samples from rats infected by T. evansi showed increased reactive oxygen species (ROS), thiobarbituric reactive-acid substances (TBARS) and glutathione reduced (GSH) levels, while catalase (CAT), superoxide dismutase (SOD) and glutathione peroxidase (GPx) activities decreased compared with uninfected and untreated animals. Also, the seric biomarkers of cardiac function increased in the infected animals compared with uninfected animals. AS-NC treatment reduced ROS and TBARS levels, ameliorate cardiac CAT and SOD activities of infected rats, and reduced seric biomarkers of cardiac function. AS-NC treatment protected the heart from oxidative stress caused by T. evansi, which might be due to its antioxidant properties. AS-NC might be considered a promising therapeutic agent against oxidative stress, when associated with nanotechnology.


Asunto(s)
Achyrocline/química , Antioxidantes/farmacología , Miocardio/patología , Nanocápsulas/administración & dosificación , Aceites Volátiles/farmacología , Tripanosomiasis/tratamiento farmacológico , Animales , Antioxidantes/administración & dosificación , Catalasa/análisis , Femenino , Aceites Volátiles/administración & dosificación , Oxidantes , Ratas Wistar , Superóxido Dismutasa/análisis , Resultado del Tratamiento
14.
Microb Pathog ; 103: 149-154, 2017 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-28027942

RESUMEN

The aim of this study was to evaluate whether the treatment with Achyrocline satureioides essential oil-loaded in nanocapsules (AS-NC) is able to protect the hepatic tissue against cytotoxic damage caused by Trypanosoma evansi. Thus, the rats were divided into four groups (n = 6 per group): uninfected/saline, uninfected/AS-NC, infected/saline, and infected/AS-NC. At day 4 post-infection (PI), the animals were euthanized and liver and sera samples were collected to perform the hepatic cell viability assay, and to determine seric levels of reactive oxygen species (ROS) and nitric oxide metabolites (NOx). Cell viability decreased (p < 0.05) in the infected/saline group compared to uninfected/saline group, while the treatment with AS-NC avoided this alteration in infected rats. Seric ROS and NOx levels increased (p < 0.05) in the infected/saline group compared to uninfected/saline group, while the treatment with AS-NC avoided this effect on ROS levels of infected rats. In summary, the treatment with AS-NC was able to protect the liver tissue against the cytotoxic effect caused by the parasite by avoiding exacerbated production of ROS.


Asunto(s)
Achyrocline/química , Hígado/patología , Hígado/parasitología , Nanocápsulas/administración & dosificación , Aceites Volátiles/administración & dosificación , Trypanosoma/efectos de los fármacos , Tripanosomiasis/patología , Tripanosomiasis/parasitología , Animales , Femenino , Hígado/efectos de los fármacos , Nanocápsulas/química , Nanocápsulas/toxicidad , Nanocápsulas/ultraestructura , Óxido Nítrico/metabolismo , Aceites Volátiles/química , Aceites Volátiles/toxicidad , Extractos Vegetales/química , Ratas , Especies Reactivas de Oxígeno/metabolismo , Tripanosomiasis/tratamiento farmacológico , Tripanosomiasis/metabolismo
16.
J Tissue Viability ; 26(4): 289-299, 2017 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-29031657

RESUMEN

Plants of the Asteraceae family have been traditionally used as medicinal plants. The species Achyrocline satureioides and Achyrocline alata present anti-inflammatory properties and great chemical similarity. However, no study has been performed to evaluate the influence of these plants on skin wound healing in vivo. Here, we have assessed the effect of these plants extracts on skin wound healing in mice. Mice were randomly arranged into three groups (n = 10), an injury was performed on the dorsal area of the animals, which received the following topical treatment: group 1, control (ointment base); group 2, A. satureioides extract; group 3, A. alata extract. The solution for treatment was prepared as 10% (w/w) concentration. The wound area was measured on days 1, 4, 9, 15 and 17 after treatment and tissues of local lesion were collected on the ninth day for histological analysis. A. alata was more effective since it induced earlier wound closure associated with decreasing initial inflammatory response, faster reepithelialization and collagen remodeling. A. satureioides improved the collagen renovation, but induced slower closure, which may be due to different concentrations of phenolic compounds among the plants here studied. Both plants did not alter the ultrastructural characteristics of cells in the healing process. In conclusion, our findings suggest the potent wound healing capacity of A. alata extracts, as demonstrated by more efficient and faster induction of wound closure. We believe this plant is a potential wound healing treatment for humans and further studies are necessary to assess its clinical practice.


Asunto(s)
Achyrocline/metabolismo , Reparación del ADN/efectos de los fármacos , Fitoquímicos/farmacología , Piel/efectos de los fármacos , Piel/lesiones , Animales , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Ratones , Fitoquímicos/uso terapéutico
17.
AAPS PharmSciTech ; 17(4): 844-50, 2016 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-26361953

RESUMEN

Ethanolic extracts of Achyrocline satureioides have pronounced antioxidant activity mainly due to the presence of the flavonoid quercetin. However, direct topical application of the extract is not possible due to the presence of high amounts of ethanol. In this sense, nanoemulsions arise as an alternative for topical formulation associating molecules with limited aqueous solubility. This article describes the development of topical nanoemulsions containing either A. satureioides extract or one of its most abundant flavonoid, quercetin. Nanoemulsions composed of octyldodecanol, egg lecithin, water and extract (NEE), or quercetin (NEQ) were prepared by spontaneous emulsification. This process led to monodisperse nanoemulsions presenting a mean droplet size of approximately 200-300 nm, negative zeta potential, and high association efficiency. A study of quercetin skin retention using porcine skin which was performed using a Franz diffusion cell revealed a higher accumulation of quercetin in skin for NEE when compared to NEQ. Finally, the antioxidant activity of formulations was measured by thiobarbituric acid-reactive species and the APPH model. A lower lipoperoxidation for the extract in respect to quercetin solution was observed. However, no difference between NEQ and NEE lipoperoxidation could be seen. The protection against lipoperoxidation by the formulations was also measured in the skin, where lower formation of reactive species was observed after treatment with NEE. In conclusion, this study shows the formulation effect on the physicochemical properties of nanoemulsions as well as on the skin retention and antioxidant activity of quercetin.


Asunto(s)
Achyrocline/química , Antioxidantes/farmacología , Asteraceae/química , Emulsiones/farmacología , Nanopartículas/administración & dosificación , Extractos Vegetales/farmacología , Animales , Antioxidantes/química , Química Farmacéutica/métodos , Emulsiones/química , Alcoholes Grasos/química , Flavonoides/química , Flavonoides/farmacología , Nanopartículas/química , Extractos Vegetales/química , Quercetina/química , Quercetina/farmacología , Piel/metabolismo , Absorción Cutánea/efectos de los fármacos , Solubilidad , Porcinos
18.
J Nat Prod ; 78(1): 93-102, 2015 Jan 23.
Artículo en Inglés | MEDLINE | ID: mdl-25517209

RESUMEN

The new prenylated phloroglucinol α-pyrones 1-3 and the new dibenzofuran 4, together with the known 23-methyl-6-O-demethylauricepyrone (5), achyrofuran (6), and 5,7-dihydroxy-3,8-dimethoxyflavone (gnaphaliin A), were isolated from the aerial parts of Achyrocline satureioides. Their structures were determined by 1D and 2D NMR spectroscopic studies, while the absolute configuration of the sole stereogenic center of 1 was established by vibrational circular dichroism measurements in comparison to density functional theory calculated data. The same (S) absolute configuration of the α-methylbutyryl chain attached to the phloroglucinol nucleus was assumed for compounds 2-6 based on biogenetic considerations. Derivatives 7-16 were prepared from 1 and 5, and the antimicrobial activities of the isolated metabolites and some of the semisynthetic derivatives against a selected panel of Gram-positive and Gram-negative bacteria, as well as a set of yeast molds, were determined.


Asunto(s)
Achyrocline/química , Antibacterianos/aislamiento & purificación , Antibacterianos/farmacología , Floroglucinol/aislamiento & purificación , Floroglucinol/farmacología , Pironas/aislamiento & purificación , Pironas/farmacología , Antibacterianos/química , Argentina , Flavonoides/química , Flavonoides/aislamiento & purificación , Furanos/química , Furanos/aislamiento & purificación , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Floroglucinol/química , Pironas/química
19.
Exp Parasitol ; 149: 39-46, 2015 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-25499512

RESUMEN

This study aimed to verify the effect of the treatment with A. satureioides essential oil (free and nanoencapsulated forms) and diminazene aceturate on hematological and biochemical variables in rats infected by Trypanosoma evansi. The 56 rats were divided into seven groups with eight rats each. Groups A, C and D were composed by uninfected animals, and groups B, E, F and G were formed by infected rats with T. evansi. Rats from groups A and B were used as negative and positive control, respectively. Rats from the groups C and E were treated with A. satureioides essential oil, and groups D and F were treated with A. satureioides nanoencapsulated essential oil. Groups C, D, E and F received one dose of oil (1.5 mL kg(-1)) during five consecutive days orally. Group G was treated with diminazene aceturate (D.A.) in therapeutic dose (3.5 mg kg(-1)) in an only dose. The blood samples were collected on day 5 PI for analyses of hematological (erythrocytes and leukocytes count, hemoglobin concentration, hematocrit, mean corpuscular and mean corpuscular hemoglobin concentration) and biochemical (glucose, triglycerides, cholesterol, alanine aminotransferase (ALT), aspartate aminotransferase (AST), albumin, urea and creatinine) variables. A. satureioides administered was able to maintain low parasitemia, mainly the nanoencapsulated form, on 5 days post infection. On the infected animals with T. evansi treated with A. satureioides essential oil (free and nanocapsules) the number of total leucocytes, lymphocytes and monocytes present was similar to uninfected rats, and different from infected and not-treated animals (leukocytosis). Treatment with A. satureioides in free form elevated levels of ALT and AST, demonstrating liver damage; however, treatment with nanoencapsulated form did not cause elevation of these enzymes. Finally, treatments inhibited the increase in creatinine levels caused by infection for T. evansi. In summary, the nanoencapsulated form showed better activity on the trypanosome; it did not cause liver toxicity and prevented renal damage.


Asunto(s)
Achyrocline/química , Diminazeno/análogos & derivados , Aceites Volátiles/uso terapéutico , Aceites de Plantas/uso terapéutico , Tripanocidas/uso terapéutico , Tripanosomiasis/tratamiento farmacológico , Animales , Biomarcadores/sangre , Análisis Químico de la Sangre , Diminazeno/administración & dosificación , Diminazeno/uso terapéutico , Perros , Femenino , Pruebas Hematológicas , Riñón/fisiología , Hígado/fisiología , Nanocápsulas , Aceites Volátiles/administración & dosificación , Aceites Volátiles/química , Parasitemia/parasitología , Aceites de Plantas/administración & dosificación , Aceites de Plantas/química , Ratas , Ratas Wistar , Tripanocidas/administración & dosificación , Trypanosoma/efectos de los fármacos , Tripanosomiasis/sangre
20.
BMC Complement Altern Med ; 15(1): 428, 2015 Dec 03.
Artículo en Inglés | MEDLINE | ID: mdl-26630872

RESUMEN

BACKGROUND: Achyrocline bogotensis has been traditionally used to treat infections of skin, respiratory, tract urinary and other infections, but not to treat viral gastrointestinal disease. In this study, this Colombian native medicinal plant was investigated by its in vitro anti-rotavirus and anti-astrovirus activity. METHODS: Several extracts and fractions phytochemically obtained from A. bogotensis were evaluated initially for their cell toxicity on MA104 and Caco2 cells and then for their anti-rotavirus (RRV) and anti-astrovirus (Yuc8) activity following three strategies: pre-treatment of cells (blocking effect), direct viral activity (virucidal effect) and post-treatment of infected cells (reduction of viral yield post-infection). In addition qualitative chemical studies were developed for the active compounds. RESULTS: Non-toxic concentrations of a fraction obtained exhibited antiviral activity against both viruses characterized by a virucidal effect and by the reduction of the infectious particles produced post-infection. Steroids, sterols, terpenes, phenols, flavonoids and sesquiterpenlactones were identified qualitatively in the active fraction. CONCLUSIONS: A. bogotensis contains substances with in vitro antiviral activity against rotavirus and astrovirus. This study confirms their anti-microbial properties and describes by the first time its antiviral activity in vitro.


Asunto(s)
Achyrocline , Antivirales/farmacología , Astroviridae/efectos de los fármacos , Extractos Vegetales/farmacología , Infecciones por Virus ARN/tratamiento farmacológico , Rotavirus/efectos de los fármacos , Achyrocline/química , Achyrocline/toxicidad , Línea Celular , Supervivencia Celular , Humanos , Fitoterapia , Componentes Aéreos de las Plantas/química , Extractos Vegetales/toxicidad , Plantas Medicinales/química , Plantas Medicinales/toxicidad
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