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1.
Molecules ; 29(8)2024 Apr 20.
Artículo en Inglés | MEDLINE | ID: mdl-38675702

RESUMEN

The goal of this study was to apply the principles of analytical quality by design (AQbD) to the analytical method for determining the radiochemical purity (PQR) of the radiopharmaceutical sodium iodide 131I oral solution, utilizing thin-layer chromatography (TLC) with a radio-TLC scanner, which also enables the evaluation of product quality. For AQbD, the analytical target profile (ATP), critical quality attributes (CQA), risk management, and the method operable design region (MODR) were defined through response surface methodology to optimize the method using MINITAB® 19 software. This study encompassed the establishment of a control strategy and the validation of the method, including the assessment of selectivity, linearity, precision, robustness, detection limit, quantification limit, range, and the stability of the sample solution. Under the experimental conditions, the method parameters of the TLC scanner were experimentally demonstrated and optimized with an injection volume of 3 µL, a radioactive concentration of 10 mCi/mL, and a carrier volume of 40 µL. Statistical analysis confirmed the method's selectivity for the 131I iodide band Rf of 0.8, a radiochemical impurity IO3- Rf of 0.6, a linearity from 6.0 to 22.0 mCi/mL, and an intermediate precision with a global relative standard deviation (RSD) of 0.624%. The method also exhibited robustness, with a global RSD of 0.101%, a detection limit of 0.09 mCi/mL, and a quantification limit of 0.53 Ci/mL, meeting the prescribed range and displaying stability over time (at 0, 2, and 20 h) with a global RSD of 0.362%, resulting in consistent outcomes. The development of a method based on AQbD facilitated the creation of a design space and an operational space, with comprehensive knowledge of the method's characteristics and limitations. Additionally, throughout all operations, compliance with the acceptance criteria was verified. The method's validity was confirmed under the established conditions, making it suitable for use in the manufacturing process of sodium iodide 131I and application in nuclear medicine services.


Asunto(s)
Radioisótopos de Yodo , Radiofármacos , Yoduro de Sodio , Cromatografía en Capa Delgada/métodos , Radiofármacos/química , Radiofármacos/análisis , Radioisótopos de Yodo/análisis , Yoduro de Sodio/química , Administración Oral , Reproducibilidad de los Resultados
2.
Molecules ; 29(6)2024 Mar 20.
Artículo en Inglés | MEDLINE | ID: mdl-38543016

RESUMEN

Moringa oleifera Lam, commonly known as moringa, is a plant widely used both as a human food and for medicinal purposes around the world. This research aimed to evaluate the efficacy of the aqueous extract of Moringa oleifera leaves (MoAE) and benzyl isothiocyanate (BIT) in rats with induced breast cancer. Cancer was induced with 7,12-dimethylbenz[a]anthracene (DMBA) at a dose of 60 mg/kg by orogastric gavage once only. Forty-eight rats were randomly assigned to eight groups, each consisting of six individuals. The control group (healthy) was called Group I. Group II received DMBA plus saline. In addition to DMBA, Groups III, IV, and V received MoAE at 100, 250, and 500 mg/kg/day, respectively, while Groups VI, VII, and VIII received BIT at 5, 10, and 20 mg/kg/day, respectively. Treatment was carried out for 13 weeks. Secondary metabolite analysis results identified predominantly quercetin, caffeoylquinic acid, neochlorogenic acid, vitexin, and kaempferol, as well as tropone, betaine, loliolide, and vitexin. The administration of MoAE at a dose of 500 mg/kg and BIT at 20 mg/kg exhibited a notable decrease in both the total tumor count and the cumulative tumor weight, along with a delay in their onset. Furthermore, they improved the histological grade. A significant decrease in serum levels of VEGF and IL-1ß levels was observed (p < 0.001) with a better effect demonstrated with MoAE at 500 mg/kg and BIT at 20 mg/kg. In conclusion, this study suggests that both the aqueous extract of Moringa oleifera leaves and the benzyl isothiocyanate possess antitumor properties against mammary carcinogenesis, and this effect could be due, at least in part, to the flavonoids and isothiocyanates present in the extract.


Asunto(s)
Moringa oleifera , Ratones , Ratas , Humanos , Animales , Moringa oleifera/química , Extractos Vegetales/química , Cromatografía Líquida de Alta Presión , Isotiocianatos/química , Fitoquímicos/farmacología , Fitoquímicos/análisis , Carcinogénesis , Hojas de la Planta/química
3.
Molecules ; 27(19)2022 Oct 02.
Artículo en Inglés | MEDLINE | ID: mdl-36235047

RESUMEN

Brunfelsia grandiflora is an ancient plant widely used for its promising medicinal properties, although little explored scientifically. Despite being a rich source of phenolic compounds responsible in part for the proven anti-inflammatory activity, its characterization has not been carried out to date. The present work deals with the exhaustive identification and quantification of its phenolic fraction, along with its antioxidant activity. Decoction resulting from the bark as fine powder was filtered and lyophilized, and polyphenols were extracted from the resulting product by aqueous-organic solvents. Seventy-nine polyphenols were identified using LC-MSn. Hydroxycinnamates was the most abundant group of compounds (up to 66.8%), followed by hydroxycoumarins (15.5%), lignans (6.1%), flavonols (5.7%), phenolic simples (3.1), gallates (2.3%), flavanols (0.3%), and flavanones (0.2%). About 64% of the characterized phenols were in their glycosylated forms. The quantification of these phytochemicals by LC-QToF showed that this medicinal plant contained 2014.71 mg of phenolic compounds in 100 g dry matter, which evidences a great antioxidant potency determined by ABTS and DPPH assays. Therefore, Brunfelsia grandiflora represents an important source of polyphenols which supports its therapeutic properties scientifically proven.


Asunto(s)
Flavanonas , Lignanos , Antioxidantes/química , Antioxidantes/farmacología , Flavonoides , Flavonoles , Fenoles , Extractos Vegetales/química , Extractos Vegetales/farmacología , Polifenoles/química , Polifenoles/farmacología , Polvos , Solventes/química
4.
Molecules ; 27(6)2022 Mar 10.
Artículo en Inglés | MEDLINE | ID: mdl-35335182

RESUMEN

Annona muricata leaves are traditionally used as an anticancer plant in the world. The aim of this study was to evaluate the ameliorative effect of the essential oil from Annona muricata leaves (EOAm) in an experimental model of breast cancer and to determine the volatile constituents with gas chromatography-mass spectrometry (GC-MS). Thirty female rats were assigned to five groups: the control group; the DMBA (7,12-dimethylbenz[α]anthracene) group; and three groups received daily EOAm doses of 50, 100, and 200 mg/kg/day, plus DMBA, respectively. After 13 weeks of treatment, tumors were analyzed pathologically and biochemical markers in serum were noted. As a result, in GC-MS analysis, 40 compounds were identified and 4 of them were abundant: Z-caryophyllene (40.22%), followed by α-selinene (9.94%), ß-pinene (8.92%), and ß-elemene (7.48%). Furthermore, EOAm in a dose-dependent form produced a reduction in tumor frequency and the accumulated tumor volume was reduced by 50% and 71% with doses of 100 and 200 mg/kg, respectively. Serum levels of reduced glutathione (GSH) increased and malondialdehyde (MDA) decreased significantly compared to the DMBA group. Serum levels of vascular endothelial growth factor (VEGF) decreased significantly from 70.75 ± 7.15 pg/mL in the DMBA group to 46.50 ± 9.00 and 34.13 ± 11.50 pg/mL in groups treated with doses of 100 and 200 mg/kg, respectively. This study concludes that the EOAm leaves showed an ameliorative effect in a murine model of breast cancer.


Asunto(s)
Annona , Neoplasias , Aceites Volátiles , Animales , Modelos Animales de Enfermedad , Femenino , Ratones , Aceites Volátiles/química , Fitoquímicos/análisis , Fitoquímicos/farmacología , Hojas de la Planta/química , Ratas , Factor A de Crecimiento Endotelial Vascular
5.
Molecules ; 25(14)2020 Jul 20.
Artículo en Inglés | MEDLINE | ID: mdl-32698395

RESUMEN

C. citratus essential oil and carvacrol have shown an antitumor effect on breast tumor cell lines; the main objective of this research was to evaluate the antitumor effect of the essential oil of Cymbopogon citratus (EOCc) and carvacrol on 7,12-dimethylbenz [a] anthracene (DMBA)-induced breast cancer in female rats. Cancer was induced by a single administration of DMBA at dose of 80 mg/kg body weight (BW). A total of 54 female Holtzman rats were randomly assigned into 9 groups (n = 6). Group I: PS (Physiological saline); Group II: DMBA; Groups III, IV, and V: DMBA + EOCc at doses of 50, 100 and 200 mg/kg/day BW, respectively; Groups VI, VII, and VIII: DMBA + carvacrol at doses of 50, 100 and 200 mg/kg/day BW, respectively; and group IX: DMBA + EOCc + carvacrol at doses of 100 mg/kg/day BW. The treatment lasted 14 weeks. As results, EOCc showed a reduction in tumors as well as necrosis and mitosis. Animals treated with carvacrol did not show necrosis, mitosis, or infiltration. Carvacrol at dose of 100 mg/kg/day BW revealed a significant decrease in the cumulative tumor volume down to 0.11 ± 0.05 cm3 compared to 0.38 ± 0.04 cm3 of the DMBA group (p < 0.01). It is concluded that EOCc and carvacrol had an antitumor effect on DMBA-induced breast cancer in female rats.


Asunto(s)
Cymbopogon/química , Cimenos/uso terapéutico , Neoplasias Mamarias Experimentales/inducido químicamente , Neoplasias Mamarias Experimentales/tratamiento farmacológico , Aceites Volátiles/uso terapéutico , 9,10-Dimetil-1,2-benzantraceno , Animales , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Compuestos de Bifenilo/química , Peso Corporal/efectos de los fármacos , Carcinogénesis/efectos de los fármacos , Carcinogénesis/patología , Femenino , Neoplasias Mamarias Experimentales/patología , Aceites Volátiles/análisis , Aceites Volátiles/farmacología , Picratos/química , Ratas Sprague-Dawley
6.
Artículo en Inglés | MEDLINE | ID: mdl-32565864

RESUMEN

The objective of this study was to evaluate the chemopreventive effect of the ethanolic extract of Cordia lutea flowers (EECL) on N-methyl-N-nitrosourea- (MNU), cyproterone-, and testosterone-induced prostate cancer in rats. 40 Holtzman male rats were used and assigned to 5 groups (n = 8). In Group I, rats received normal saline (10 mL/Kg); Group II: rats were induced for prostate cancer with cyproterone, testosterone, and NMU; Groups III, IV, and V: rats received EECL daily, at doses of 50, 250, and 500 mg/kg body weight, respectively. After the period of treatment, animals were sacrificed by an overdose of pentobarbital and blood samples were collected for determination of prostate-specific antigen (PSA). The prostate was dissected and weighed accurately. The ventral lobe of the prostate was processed for histopathology analysis. The somatic prostate index decreased with EECL at dependent dose, from 0.34 ± 0.04 to 0.23 ± 0.05 (P < 0.05). The PSA levels also decreased significantly at doses of 250 and 500 mg/kg. Histopathological analysis showed a decrease in the number of prostatic layers with high-grade prostatic intraepithelial neoplasia (HG-PIN) and low-grade prostatic intraepithelial neoplasia (LG-PIN) at the dose of 500 mg/kg. The ethanolic extract of Cordia lutea flowers had a chemopreventive effect on induced prostate cancer in rats.

7.
Toxicol Res ; 35(3): 225-232, 2019 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-31341551

RESUMEN

Thymus vulgaris L. is widely used as an ingredient in cooking and in herbal medicine. However, there is little information about its toxicity. The present study was performed to evaluate the acute and repeated 28-day oral dose toxicity of thyme essential oil in rats. For the acute toxicity test, two groups of three rats were used. The rats received a single dose of essential oil: 300 or 2,000 mg/kg of body weight (bw). The rats were observed individually during the first four hours, and then daily until day 14. For the toxicity test with repeated doses, four groups of 10 rats were used. Doses of 100, 250, and 500 mg/kg/day were tested for 28 days. At the end of the experiment, blood was collected and the animals were sacrificed. Histopathological examination showed that in the lungs of rats given the 2,000 mg/kg bw dose, polymorph nuclear infiltrates, hemosiderin macrophages, and interstitial space thickening were present. In the repeated dose study, all rats survived the 28-day treatment period and apparently showed no signs of toxicity. The hematological and biochemical parameters were not altered. The histopathological study of the organs showed severe changes in the lung, with the dose of 500 mg/kg/day; in the other organs, no alterations were observed or the changes were slight. The body weight was only altered in male rats given the 500 mg/kg dose. The relative weight of the organs did not show any significant changes. Our studies revealed that the essential oil of Thymus vulgaris has moderate oral toxicity according to the results of the acute test, whereas the results of the 28-day oral toxicity test suggest that the no-observed-adverse effect level (NOAEL) is greater than 250 mg/kg/day.

8.
Artículo en Español | LILACS | ID: biblio-959757

RESUMEN

RESUMEN: Se realizó una revisión bibliográfica cuyo objetivo es dar a conocer los beneficios de los probióticos en su posible uso en la periodontitis crónica. En la actualidad han aparecido nuevos enfoque terapéuticos, que podrían complementar el tratamiento de la periodontitis crónica. Es bien sabido que el gold estándar en el tratamiento no quirúrgico, es el raspado y alisado radicular y que en su apoyo pueden haber coadyuvantes, como lo podrían ser los probióticos. Estos son microorganismos comensales de la microflora bucal que siendo administrados de forma adecuada, brindarían beneficios a la persona, como la mejora de su salud periodontal. Los probióticos son productores de sustancias antimicrobianas, tienen un mecanismo competitivo con las bacterias patógenas, así como moduladores de la respuesta inmune. En esta revisión se detallan sus múltiples beneficios así como su apoyo al tratamiento de la periodontitis crónica.


ABSTRACT A bibliographic review was carried out to present the benefits of probiotics in their possible use in chronic periodontitis. At present, new therapeutic approaches have appeared, which could complement the treatment of chronic periodontitis. It is well known that the gold standard in non-surgical treatment is scaling and root planing and that adjuvants, such as probiotics may support it. These commensal microorganisms of the oral microflora , when administered properly, would provide benefits to the individual, such as improving their periodontal health. Probiotics are producers of antimicrobial substances and have a competitive mechanism with pathogenic bacteria, as well as being modulators of the immune response. This review details their multiple benefits and their support in the treatment of chronic periodontitis.


Asunto(s)
Terapéutica , Bacterias , Probióticos , Periodontitis Crónica
9.
Cienc. invest ; 9(1): 41-46, ene-jun. 2006. ilus, tab
Artículo en Español | LIPECS | ID: biblio-1107405

RESUMEN

Se realizó la evaluación comparativa de tres fármacos de síntesis utilizados como hipoglicemiantes orales con el extracto acuoso obtenido por infusión de las hojas de Smallanthus sochifolius (Poepp) Rob. "yacón", utilizando un biomodelo experimental por hiperglicemia en ratas nomoglucémicas de la especie Rattus norvegicus var. Albina. El objetivo de la investigación fue observa el efecto de extracto acuoso al 10 por ciento de las hojas de "yacon" en el descenso de la glicemia frente a la glibenclamida, clorpropamida y metformina, que tienen amplio uso en el tratamiento de la diabetes mellitus tipo 2 (DM2). El material vegetal fue colectado en el disco se realizó con 36 ratas albinas hembras, cepa Holtzman con un peso promedio de 240 g, que estuvieron sometidas a una alimentación controlada y agua ad libitum, hasta el momento de experimento. Se determinó la curva de tolerancia a la glucosa y la administración de las drogas se hizo por vía intragástrica. Los resultados obtenidos muestran un descenso significativo de glicemia con el extracto acuoso utilizado. Con la aplicación del extracto y los fármacos en e biomodelo experimenta, se concluye que las hojas de yacón producen en efecto de disminución significa de glicemia.


It was carried out the comparative evaluation of three synthetic drugs used as oral hypoglycemiants, against the aqueous obtained by infusion of leaves from Smallathus sonchifolius (Popp) Rob. Yacon, using a experimental biomodel by hypoglycemia in normogycemic rats of species Rattus norvegicus var. Albine. The object of the research was to observe the 10 per cent aqueous extract effect of Smallanthus sonchifolius (Poepp) Rob. Yacon in the decay of glycemia against glibenclamide, clorprofamide and metformine drugs that have great usage in the treatment of type 2 diabets mellitus (DM2). The vegetal material vas collected in the Huancbamba district, province of Oxapampa in Cerro de Pasco department. The pharmacological assay was taken with 36 female albine rats of Holtzman strain, with a average weight of 240 g that were fed by a controlled food and water ad libitum until the moment od experiment. Is was determined the glucose tolerance curve and the administration of drugs was made by intragastric via. The obtained results show a significant decay of glycemia with the used aqueous extact and the drugs used in the experimental biomodel, it was concluded that the Yacon leaves Produce an affect of signifcant decay of glycemia.


Asunto(s)
Ratas , Clorpropamida , Gliburida , Hipoglucemia , Metformina , Plantas Medicinales , Ratas
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