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1.
Biol Trace Elem Res ; 200(1): 339-347, 2022 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-33598892

RESUMEN

The aim of present study was to investigate the beneficial effect of chromium (III) picolinate (CrPic) and chromium (III) picolinate nanoparticles (NCrPic) addition on growth performance, stress-related hormonal changes, and serum levels of various immunity biomarkers, as well as the gene expression of IFN-γ in broilers exposed to heat stress conditions. Treatments included T1 which received the basal diet with no feed additive; T2 exposed to heat stress; T3, T4, and T5 containing 500, 1000, and 1500 ppb CrPic; as well as T6, T7, and T8 containing 500, 1000, and 1500 ppb NCrPic, respectively. After 2 weeks from CrPic and NCrPic supplementation, IFN-γ mRNA expression was assayed using the RT-PCR technique. The results showed that the lower body weight, daily weight gain, daily feed intake by heat stress, and the feed conversion ratio were recovered remarkably by CrPic and NCrPic supplements. The stress-elevated levels of cortisol and immunoglobulin were reduced significantly using CrPic and NCrPic supplementation (P ≤ 0.05). The gene expression profile showed that the upregulated expression of IFN-γ was regulated by the addition of CrPic and NCrPic, in particular, to the diet; however, a full downregulation of IFN-γ expression was observed after week 2 of NCrPic supplementation. In conclusion, the results indicated that nanoparticle supplementation could be effective in reducing heat stress-induced detrimental alterations, thereby attributing to substantial changes to the immune system, including IFN-γ expression.


Asunto(s)
Pollos , Nanopartículas , Alimentación Animal/análisis , Animales , Cromo/farmacología , Dieta , Suplementos Dietéticos , Respuesta al Choque Térmico , Ácidos Picolínicos/farmacología
2.
Nutrients ; 13(10)2021 Sep 24.
Artículo en Inglés | MEDLINE | ID: mdl-34684352

RESUMEN

Magnesium (Mg) deficiency may affect bone metabolism by increasing osteoclasts, decreasing osteoblasts, promoting inflammation/oxidative stress, and result in subsequent bone loss. The objective of the present study was to identify the molecular mechanism underlying the bone protective effect of different forms of Mg (inorganic magnesium oxide (MgO) versus organic magnesium picolinate (MgPic) compound) in rats fed with a high-fat diet (HFD). Forty-two Wistar albino male rats were divided into six group (n = 7): (i) control, (ii) MgO, (iii) MgPic, (iv) HFD, (v) HFD + MgO, and (vi) HFD + MgPic. Bone mineral density (BMD) increased in the Mg supplemented groups, especially MgPic, as compared with the HFD group (p < 0.001). As compared with the HFD + MgO group, the HFD + MgPic group had higher bone P (p < 0.05) and Mg levels (p < 0.001). In addition, as compared to MgO, MgPic improved bone formation by increasing the levels of osteogenetic proteins (COL1A1 (p < 0.001), BMP2 (p < 0.001), Runx2 (p < 0.001), OPG (p < 0.05), and OCN (p < 0.001), IGF-1 (p < 0.001)), while prevented bone resorption by reducing the levels of RANK and RANKL (p < 0.001). In conclusion, the present data showed that the MgPic could increase osteogenic protein levels in bone more effectively than MgO, prevent bone loss, and contribute to bone formation in HFD rats.


Asunto(s)
Proteína Morfogenética Ósea 2/metabolismo , Subunidad alfa 1 del Factor de Unión al Sitio Principal/metabolismo , Conducta Alimentaria , Osteogénesis , Osteoprotegerina/metabolismo , Ácidos Picolínicos/farmacología , Ligando RANK/metabolismo , Receptor Activador del Factor Nuclear kappa-B/metabolismo , Animales , Densidad Ósea/efectos de los fármacos , Huesos/metabolismo , Dieta Alta en Grasa , Elementos Químicos , Masculino , Osteogénesis/efectos de los fármacos , Ratas Wistar , Transducción de Señal/efectos de los fármacos
3.
Theranostics ; 11(14): 6860-6872, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34093858

RESUMEN

Background: Immunotherapy has profoundly changed the landscape of cancer management and represented the most significant breakthrough. Yet, it is a formidable challenge that the majority of cancers - the so-called "cold" tumors - poorly respond to immunotherapy. To find a general immunoregulatory modality that can be applied to a broad spectrum of cancers is an urgent need. Methods: Magnetic hyperthermia (MHT) possesses promise in cancer therapy. We develop a safe and effective therapeutic strategy by using magnetism-mediated targeting MHT-immunotherapy in "cold" colon cancer. A magnetic liposomal system modified with cell-penetrating TAT peptide was developed for targeted delivery of a CSF1R inhibitor (BLZ945), which can block the CSF1-CSF1R pathway and reduce M2 macrophages. The targeted delivery strategy is characterized by its magnetic navigation and TAT-promoting intratumoral penetration. Results: The liposomes (termed TAT-BLZmlips) can induce ICD and cause excessive CRT exposure on the cell surface, which transmits an "eat-me" signal to DCs to elicit immunity. The combination of MHT and BLZ945 can repolarize M2 macrophages in the tumor microenvironment to relieve immunosuppression, normalize the tumor blood vessels, and promote T-lymphocyte infiltration. The antitumor effector CD8+ T cells were increased after treatment. Conclusion: This work demonstrated that TAT-BLZmlips with magnetic navigation and MHT can remodel tumor microenvironment and activate immune responses and memory, thus inhibiting tumor growth and recurrence.


Asunto(s)
Neoplasias del Colon/terapia , Terapia Combinada/métodos , Hipertermia , Inmunoterapia/métodos , Liposomas/química , Magnetoterapia/métodos , Nanopartículas de Magnetita/química , Receptores de Factor Estimulante de Colonias de Granulocitos y Macrófagos/antagonistas & inhibidores , Animales , Apoptosis/efectos de los fármacos , Apoptosis/efectos de la radiación , Benzotiazoles/farmacocinética , Benzotiazoles/farmacología , Linfocitos T CD8-positivos/efectos de los fármacos , Linfocitos T CD8-positivos/metabolismo , Línea Celular Tumoral , Neoplasias del Colon/diagnóstico por imagen , Neoplasias del Colon/inmunología , Femenino , Humanos , Liposomas/metabolismo , Liposomas/efectos de la radiación , Ratones , Ratones Endogámicos BALB C , Ratones Desnudos , Recurrencia Local de Neoplasia/metabolismo , Recurrencia Local de Neoplasia/terapia , Ácidos Picolínicos/farmacocinética , Ácidos Picolínicos/farmacología , Ratas , Microambiente Tumoral/efectos de los fármacos , Macrófagos Asociados a Tumores/efectos de los fármacos , Macrófagos Asociados a Tumores/metabolismo , Ensayos Antitumor por Modelo de Xenoinjerto
4.
Fish Physiol Biochem ; 47(2): 599-616, 2021 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-33611776

RESUMEN

A 60-day feeding experiment was conducted to evaluate the effects of dietary chromium (Cr) on carbohydrate utilization and growth performance of Labeo rohita fingerlings. Fishes were fed with four high carbohydrate (53%), isonitrogenous (crude protein 35%), and isocaloric (415 Kcal, 100 gm-1) experimental diets containing different levels of dietary chromium picolinate (Cr-Pic) viz.0, 400, 800, and 1200 µg kg-1 diet. Weight gain (WG%), specific growth rate (SGR), feed efficiency ratio (FER), and protein efficiency ratio (PER) were significantly increased at 800 µg kg-1 diet chromium supplementation (P < 0.05). Cr-Pic supplementation (800 µg kg-1) also significantly (P < 0.05) enhanced the protein: DNA ratio in muscle, while DNA: RNA and DNA: tissue ratios were significantly (P < 0.05) decreased indicating higher growth. Significantly higher amylase, protease, and lipase activities were recorded in 800 µg Cr-Pic kg-1 diet fed fishes (P < 0.05), while any of the experimental groups showing no significant (P > 0.05) change in hexokinase activity, indicating normal glycolysis in all. Furthermore, significant (P < 0.05) decrease of glucose-6-phospatase activity in 800 µg Cr-Pic kg-1 diet fed group, showcasing an evidence for protein-sparing action with Cr-Pic supplementation. Significantly (P < 0.05) higher serum insulin and liver glycogen in 800 µg Cr-Pic kg-1 diet fed fishes denote an improvement in carbohydrate metabolism. However, significantly (P < 0.05) higher ATPase and SOD activities were also observed when chromium supplementation was more than 800 µg kg-1 diet, indicating stress at higher level. The present study indicates that growth and carbohydrate utilization can significantly (P < 0.05) be improved by feeding the L. rohita fingerlings with Cr-Pic (800 µg kg-1 diet) supplemented diet in laboratory condition.


Asunto(s)
Carpas/crecimiento & desarrollo , Carbohidratos de la Dieta/metabolismo , Ácidos Picolínicos/farmacología , Alimentación Animal/análisis , Animales , Carpas/metabolismo , Dieta/veterinaria , Suplementos Dietéticos , Relación Dosis-Respuesta a Droga , Ácidos Picolínicos/administración & dosificación
5.
J Trace Elem Med Biol ; 63: 126659, 2021 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-33045675

RESUMEN

BACKGROUND: Evaluating the impact of chromium picolinate supplementation on glycemic status, lipid profile, inflammatory markers and fetuin-A in patients with non-alcoholic fatty liver disease (NAFLD). METHODS: In present research, participants (N = 46) were randomized to (400 mcg/day, n = 23) chromium picolinate and placebo (n = 23) for 3 months. RESULTS: Glucose indices, and lipid profiles, inflammatory biomarker and fetuin-A were measured before and after the intervention. Chromium reduced triglyceride (TG), atherogenic index of plasma (AIP), very-low-density lipoprotein (VLDL), insulin, homeostatic model assessment for insulin resistance (HOMA-IR), high-sensitivity C-reactive protein (hs-CRP), interleukin (IL) -6, tumor necrosis factor-alpha (TNF-α) and fetuin-A significantly compared to placebo group (p < 0.05). Furthermore, chromium significantly increased the quantitative insulin sensitivity check index (QUICKI). There were no significant differences in total cholesterol (TC), high-density lipoprotein cholesterol (HDL), low-density lipoprotein cholesterol (LDL), fasting blood sugar (FBS), Hemoglobin A1c (HbA1C), interleukin (IL)-17 between the two groups (p < 0.05). CONCLUSION: Chromium picolinate significantly decreased TG, insulin, HOMA-IR, fetuin-A, the number of inflammatory factors, and increased QUICKI without changing FBS, HbA1C, TC, LDL, HDL, IL-17 levels and liver steatosis intensity in patients with NAFLD. Further studies by examining the effect of different doses of chromium and mechanisms of cellular action, would help further clarify the subject.


Asunto(s)
Enfermedad del Hígado Graso no Alcohólico/tratamiento farmacológico , Ácidos Picolínicos/farmacología , alfa-2-Glicoproteína-HS/antagonistas & inhibidores , Adulto , Biomarcadores/sangre , Proteína C-Reactiva/análisis , Proteína C-Reactiva/antagonistas & inhibidores , Suplementos Dietéticos , Método Doble Ciego , Femenino , Humanos , Resistencia a la Insulina , Interleucina-6/antagonistas & inhibidores , Interleucina-6/sangre , Masculino , Persona de Mediana Edad , Enfermedad del Hígado Graso no Alcohólico/sangre , Enfermedad del Hígado Graso no Alcohólico/metabolismo , Ácidos Picolínicos/administración & dosificación , Proyectos Piloto , Factor de Necrosis Tumoral alfa/antagonistas & inhibidores , Factor de Necrosis Tumoral alfa/sangre , Adulto Joven , alfa-2-Glicoproteína-HS/análisis
6.
PLoS One ; 15(11): e0242820, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-33237949

RESUMEN

The aim of the study was to determine whether the level and form of Cr in the diet of chickens influences its accumulation in tissues as well as intestinal absorption of P and its deposition in tissues. The experiment was carried out on 405 one-day-old male Ross 308 chickens that were randomly divided into five treatment groups. Control group was fed the diet without supplemental chromium; experimental groups were fed the diet with 3 or 6 mg/kg chromium picolinate (Cr-Pic) and with 3 or 6 mg/kg chromium nanoparticles (Cr-NP). Chromium was found to accumulate in the tissues of the ileum, liver, breast muscle, bones skin and in feathers of chickens. Chromium deposited in the ileum of chickens does not affect the ex vivo estimated intestinal absorption of P. The use of Cr in the diet of chickens carries the risk of lowering P levels in femur.


Asunto(s)
Huesos/efectos de los fármacos , Absorción Intestinal/efectos de los fármacos , Fósforo/farmacología , Ácidos Picolínicos/farmacología , Animales , Glucemia/efectos de los fármacos , Pollos , Plumas/efectos de los fármacos , Hígado/efectos de los fármacos , Fósforo/química , Distribución Tisular/efectos de los fármacos
7.
Biomolecules ; 10(3)2020 03 04.
Artículo en Inglés | MEDLINE | ID: mdl-32143429

RESUMEN

Diabetic nephropathy (DN) is one of the most important complications of diabetes, and the leading cause of end-stage renal disease (ESRD). While Chromium picolinate (CrPic) supplementation has been found to be effective in treating diabetes, its effects on diabetic-induced nephropathy have not been studied. Therefore, in this study, CrPic (1 mg kg -1 d -1) was administered to a DN rat model by oral gavage for eight weeks to investigate its effects. The results show that CrPic supplementation caused a decrease in levels of blood glucose, serum insulin, blood urea nitrogen (BUN), serum creatinine, and urinary albumin in DN rats. It also reversed renal pathological changes, including renal glomerular sclerosis and interstitial fibrosis. In addition, the oxidative defense system in the kidneys of DN rats was found to be improved; the biological activities of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPX) increased; and the content of malondialdehyde (MDA) lowered. Immunohistochemical results reveal that the expression levels of renal transforming growth factor-ß1 (TGF-ß1), Smad 2, and Smad 3 decreased significantly in the kidneys of rats in the CrPic-treated group. CrPic administration was thus found to ameliorate diabetic nephropathy in SD rats via an antioxidative stress mechanism, as well the ability to inhibit TGF-ß1/Smad2/3 expression. This study suggests that CrPic could be a potential renal-protective nutrient against diabetic nephropathy.


Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Nefropatías Diabéticas/tratamiento farmacológico , Ácidos Picolínicos/farmacología , Animales , Biomarcadores/metabolismo , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Experimental/patología , Nefropatías Diabéticas/metabolismo , Nefropatías Diabéticas/patología , Fibrosis , Regulación de la Expresión Génica/efectos de los fármacos , Masculino , Estrés Oxidativo/efectos de los fármacos , Ratas , Ratas Sprague-Dawley
8.
Biol Trace Elem Res ; 193(2): 414-421, 2020 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-31079328

RESUMEN

Chromium (Cr) is a micromineral that is involved in the metabolism of carbohydrates, lipids, ammonia, and nucleic acids; thus, its supplementation can influence the nutritional status of ruminants, and consequently, colostrum profile, since this secretion depends on products secreted by the mammary gland and elements of the maternal bloodstream. The present study investigated the influence of supplementation with Cr bound to organic molecule on the nutritional, immune, and antioxidant quality of ewe colostrum. Thirty-two multiparous Santa Ines ewes (55.3 ± 8.00 kg body weight) were randomly assigned into four groups: T1 (0.0 mg of chromium picolinate (CrPic) supplementation per ewe, n = 8), T2 (0.15 mg of CrPic per ewe, n = 9), T3 (0.30 mg of CrPic per ewe, n = 7), and T4 (0.45 mg of CrPic per ewe, n = 8). Supplementation was supplied during the breeding season, pregnancy, and lactation. Shortly after calving, the first milking colostrum was collected to determine its chemical composition, activity of lysozyme, lactoperoxidase, ceruloplasmin, catalase, glutathione peroxidase, and oxygen radical absorbance capacity. The results show that lactoperoxidase activity decreased with CrPic supplementation (P < 0.01), revealing that this micromineral reduces an important component of defense mechanism in the body. Therefore, the results of this work show that supplementation with chromium picolinate influences colostrum quality.


Asunto(s)
Cromo/farmacología , Calostro/efectos de los fármacos , Lactoperoxidasa/metabolismo , Ácidos Picolínicos/farmacología , Animales , Animales Recién Nacidos , Catalasa/metabolismo , Ceruloplasmina/metabolismo , Cromo/administración & dosificación , Cromo/análisis , Calostro/química , Calostro/metabolismo , Suplementos Dietéticos , Femenino , Glutatión Peroxidasa/metabolismo , Muramidasa/metabolismo , Ácidos Picolínicos/administración & dosificación , Embarazo , Ovinos
9.
J Trace Elem Med Biol ; 58: 126434, 2020 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-31778961

RESUMEN

BACKGROUND: Chromium picolinate (CrPic) is commonly used to reduce muscle fatigue after exercise. We aimed to elucidate the effects of CrPic on glucose and lipid metabolism and the expression of glucose transporters in exercised rats. METHODS: Forty-two male Wistar rats (8-week-old) were distributed into six groups (n = 7) as follows: Control, CrPic, Chronic Exercise (CEx), CEx + CrPic, Acute Exercise (AEx), and AEx + CrPic. CEx consists of 30 m/min, 30 min/day, and 5 days/week for 6 weeks. CrPic was supplemented at 400 µg elemental Cr/kg of diet for 6 weeks. In the AEx groups, animals were run on the treadmill at 30 m/min until exhaustion. RESULTS: CEx significantly lowered blood glucose (BG), total cholesterol (TC) and triglyceride (TG) levels, but elevated insulin concentration (IC), compared with control (P < 0.05). CEx significantly decreased the level of malondialdehyde (MDA) in the serum, liver, and muscle while AEx elevated it (P < 0.001 for all). CrPic significantly decreased BG, TC, TG levels, and increased IC with a remarkable effect in CEx rats (P < 0.01). CrPic also significantly reduced serum, liver, and muscle MDA levels (P < 0.001). Both AEx and CEx increased the expression of liver glucose transporter 2 (GLUT-2) and muscle GLUT-4 with the highest level in CEx rats (P < 0.05). Moreover, CrPic supplementation significantly elevated GLUT-2 and GLUT-4 expressions in the liver and muscle of sedentary and exercise-treated rats (P < 0.05). CONCLUSION: CrPic improves various metabolic parameters and reduces oxidative stress in CEx and AEx rats by decreasing BG, TC, TG, MDA levels in serum and elevating GLUT-2 and GLUT-4 expression in the liver and muscle samples. The efficacy of CrPic was more pronounced in CEx rats.


Asunto(s)
Glucosa/metabolismo , Metabolismo de los Lípidos/efectos de los fármacos , Condicionamiento Físico Animal , Ácidos Picolínicos/farmacología , Animales , Peso Corporal/efectos de los fármacos , Conducta Alimentaria/efectos de los fármacos , Regulación de la Expresión Génica/efectos de los fármacos , Transportador de Glucosa de Tipo 2/genética , Transportador de Glucosa de Tipo 2/metabolismo , Transportador de Glucosa de Tipo 4/genética , Transportador de Glucosa de Tipo 4/metabolismo , Metabolismo de los Lípidos/genética , Hígado/efectos de los fármacos , Hígado/metabolismo , Masculino , Malondialdehído/sangre , Malondialdehído/metabolismo , Músculos/efectos de los fármacos , Músculos/metabolismo , Ratas Wistar
10.
J Mater Chem B ; 7(40): 6210-6223, 2019 10 16.
Artículo en Inglés | MEDLINE | ID: mdl-31566200

RESUMEN

Due to the complexity and heterogeneity of solid tumors, traditional clinical treatments often only achieve limited therapeutic effects. Tumor-associated macrophages (TAMs) play a key role in the development of solid tumors, and the elimination of solid tumors based on the tumor microenvironment has proven to be an effective therapeutic strategy. Here, we successfully developed Ru-based nanoparticles, Ru@ICG-BLZ NPs, with inflammation-responsive release ability, which could repolarize TAMs into M1 macrophages (with an antitumor role) and further produce hyperthermia and ROS to eliminate cancer cells. In vitro experiments showed that Ru@ICG-BLZ NPs had superior drug (ICG and BLZ-945) loading capacity and sensitive inflammation-responsive drug release behavior, which enhanced CT26 cell uptake and penetration ability. Furthermore, in vivo experiments showed that Ru@ICG-BLZ NPs could effectively up-regulate the expression of M1 markers (iNOS, and IL-12) and exert phototherapy to ablate solid tumor, without causing obvious damage to the surrounding tissues of the tumor. The lower toxicity and excellent antitumor ability of Ru@ICG-BLZ NPs could provide new ideas for the clinical transformation of nanomedicine.


Asunto(s)
Benzotiazoles/farmacología , Neoplasias Colorrectales/terapia , Inflamación/fisiopatología , Macrófagos/inmunología , Nanopartículas/administración & dosificación , Fototerapia , Ácidos Picolínicos/farmacología , Rutenio/química , Animales , Apoptosis , Benzotiazoles/administración & dosificación , Benzotiazoles/química , Proliferación Celular , Neoplasias Colorrectales/patología , Liberación de Fármacos , Femenino , Humanos , Macrófagos/patología , Ratones , Ratones Endogámicos BALB C , Nanopartículas/química , Ácidos Picolínicos/administración & dosificación , Ácidos Picolínicos/química , Nanomedicina Teranóstica , Células Tumorales Cultivadas , Microambiente Tumoral , Ensayos Antitumor por Modelo de Xenoinjerto
11.
Molecules ; 24(8)2019 Apr 22.
Artículo en Inglés | MEDLINE | ID: mdl-31013675

RESUMEN

Two near-infrared fluorescent probes (A and B) containing hemicyanine structures appended to dipicolylamine (DPA), and a dipicolylamine derivative where one pyridine was substituted with pyrazine, respectively, were synthesized and tested for the identification of Zn(II) ions in live cells. In both probes, an acetyl group is attached to the phenolic oxygen atom of the hemicyanine platform to decrease the probe fluorescence background. Probe A displays sensitive fluorescence responses and binds preferentially to Zn(II) ions over other metal ions such as Cd2+ ions with a low detection limit of 0.45 nM. In contrast, the emission spectra of probe B is not significantly affected if Zn(II) ions are added. Probe A possesses excellent membrane permeability and low cytotoxicity, allowing for sensitive imaging of both exogenously supplemented Zn(II) ions in live cells, and endogenously releases Zn(II) ions in cells after treatment of 2,2-dithiodipyridine.


Asunto(s)
Aminas , Carbocianinas , Colorantes Fluorescentes , Ácidos Picolínicos , Zinc/metabolismo , Aminas/química , Aminas/farmacología , Carbocianinas/química , Carbocianinas/farmacología , Colorantes Fluorescentes/química , Colorantes Fluorescentes/farmacología , Células HeLa , Humanos , Microscopía Fluorescente , Ácidos Picolínicos/química , Ácidos Picolínicos/farmacología
12.
ACS Infect Dis ; 5(1): 131-140, 2019 01 11.
Artículo en Inglés | MEDLINE | ID: mdl-30427656

RESUMEN

The clinical effectiveness of carbapenem antibiotics such as meropenem is becoming increasingly compromised by the spread of both metallo-ß-lactamase (MBL) and serine-ß-lactamase (SBL) enzymes on mobile genetic elements, stimulating research to find new ß-lactamase inhibitors to be used in conjunction with carbapenems and other ß-lactam antibiotics. Herein, we describe our initial exploration of a novel chemical series of metallo-ß-lactamase inhibitors, from concept to efficacy, in a survival model using an advanced tool compound (ANT431) in conjunction with meropenem.


Asunto(s)
Antibacterianos/farmacología , Enterobacteriaceae Resistentes a los Carbapenémicos/efectos de los fármacos , Farmacorresistencia Bacteriana Múltiple , Infecciones por Enterobacteriaceae/tratamiento farmacológico , Inhibidores de beta-Lactamasas/química , Carbapenémicos/farmacología , Cristalografía por Rayos X , Concentración 50 Inhibidora , Meropenem/farmacología , Pruebas de Sensibilidad Microbiana , Ácidos Picolínicos/química , Ácidos Picolínicos/farmacología , Unión Proteica , Relación Estructura-Actividad , Inhibidores de beta-Lactamasas/farmacología , beta-Lactamasas
13.
Curr Microbiol ; 76(2): 178-186, 2019 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-30498942

RESUMEN

Bioactive natural compounds play pivotal roles in drug discovery and the emergence of multi-drug resistance pathogens demands the development of better/new drugs. Paenibacillus amylolyticus KMCLE06 endophytic bacterium isolated from the medicinal plant Coix lachryma-jobi were analyzed for the potential bioactive secondary metabolite compounds and its gene responsible within polyketide synthases (PKS) clusters. Ethyl acetate extraction of P. amylolyticus KMCLE06 showed significant antibacterial activity which was further processed to partial purification and characterization for bioactive compound. The foremost bioactive component in extraction was found to be dipicolinic acid (DPA). The antibacterial activity showed remarkable activity compared to the commercial standard DPA against both gram-positive and gram-negative pathogens. The MIC and MBC concentrations for partially purified extracted DPA ranged from 62.5 to 125 µg/ml and MBC from 208 to 250 µg/ml, respectively. Sequence analysis of gene amplified using degenerative primer, amplified 543 bp DNA region, revealing conserved putative open reading frame for dipicolinic acid synthetase (DpsA) key gene to produce DPA in most endospore forming bacteria. A search in the structural database for DpsA revealed significant homologous match with enoyl reductase one of the PKS type 1 module protein. This emphasizes endophytic P. amylolyticus KMCLE06 bacteria has presence of spoVF operon producing DPA via dipicolinic acid synthetase and lacks the polyketide synthase type 1 module cluster gene in its genome. And the bioactive compound DPA extracted acts as a stable remarkable antibacterial agent which can be potent compound for multi-resistance pathogens.


Asunto(s)
Antibacterianos/farmacología , Proteínas Bacterianas/genética , Ligasas/genética , Paenibacillus/química , Paenibacillus/enzimología , Ácidos Picolínicos/farmacología , Antibacterianos/aislamiento & purificación , Coix/microbiología , Descubrimiento de Drogas , Endófitos , Genoma Bacteriano , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Familia de Multigenes , Operón , Paenibacillus/genética , Ácidos Picolínicos/aislamiento & purificación , Plantas Medicinales/microbiología
14.
Nutrients ; 10(12)2018 Dec 03.
Artículo en Inglés | MEDLINE | ID: mdl-30513859

RESUMEN

With over two-thirds (71.6%) of the US adult population either overweight or obese, many strategies have been suggested for weight loss. While many are successful, the weight loss is often accompanied by a loss in lean body mass. This loss in lean body mass has multiple negative health implications. Therefore, weight loss strategies that protect lean body mass are of value. It is challenging to consume a significant caloric deficit while maintaining lean body mass regardless of macronutrient distribution. Therefore, the efficacy of various dietary supplements on body weight and body composition have been a topic of research interest. Chromium picolinate has been shown to improve body composition by maintaining lean body mass. In this paper we review some common weight loss strategies and dietary supplements with a focus on their impact on body composition and compare them to the effect of chromium picolinate.


Asunto(s)
Composición Corporal , Pérdida de Peso , Composición Corporal/efectos de los fármacos , Dieta Reductora , Humanos , Quelantes del Hierro/farmacología , Ácidos Picolínicos/farmacología , Pérdida de Peso/efectos de los fármacos
15.
Anal Bioanal Chem ; 410(28): 7441-7448, 2018 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-30218128

RESUMEN

Matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI TOF MS) is a well-established method with a unique set of qualities including sensitivity, minute sample consumption, and label-free detection, all of which are highly desired in enzyme assays. On the other hand, the application of MALDI TOF MS is usually limited by high concentrations of MS-incompatible compounds in the reaction mixture such as salts or organic solvents. Here, we introduce kinetic and inhibition studies of ß-secretase (BACE1), a key enzyme of the progression of Alzheimer's disease. Compatibility of the enzyme assay with MALDI TOF MS was achieved, providing both a complex protocol including a desalting step designed for rigorous kinetic studies and a simple mix-and-measure protocol designed for high-throughput inhibitor screening. In comparison with fluorescent or colorimetric assays, MALDI TOF MS represents a sensitive, fast, and label-free technique with minimal sample preparation. In contrast to other MS-based methodological approaches typically used in drug discovery processes, such as a direct injection MS or MS-coupled liquid chromatography or capillary electrophoresis, MALDI TOF MS enables direct analysis and is a highly suitable approach for high-throughput screening. The method's applicability is strongly supported by the high correlation of the acquired kinetic and inhibition parameters with data from the literature as well as from our previous research. Graphical abstract ᅟ.


Asunto(s)
Enfermedad de Alzheimer/enzimología , Secretasas de la Proteína Precursora del Amiloide/antagonistas & inhibidores , Espectrometría de Masa por Láser de Matriz Asistida de Ionización Desorción/métodos , Aminoácidos/antagonistas & inhibidores , Secretasas de la Proteína Precursora del Amiloide/metabolismo , Evaluación Preclínica de Medicamentos/métodos , Células HEK293 , Compuestos Heterocíclicos con 2 Anillos/farmacología , Humanos , Cinética , Ácidos Picolínicos/farmacología , Pirimidinonas/farmacología
16.
Fish Physiol Biochem ; 44(5): 1265-1274, 2018 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-29961187

RESUMEN

A feeding trial was conducted to evaluate the effects of chromium picolinate (Cr-Pic) on growth performance, body composition, and biochemical parameters in Nile tilapia Oreochromis niloticus. Five experimental diets were formulated with high-protein diet (HP), low-protein diet (LP), and LP + 0.6, 1.2, or 1.8 mg kg-1 Cr, respectively. Each diet was randomly assigned to four replicate groups of 30 fish per aquarium in a water-circulated rearing system for 60 days. Dietary 1.2 or 1.8 mg kg-1 Cr inclusion significantly affects the final body weight, weight gain rate, specific growth rate, feed efficiency rate, and protein efficiency ratio of tilapia compare to the LP diet. The Cr inclusion significantly decreased the content of blood urea nitrogen and the blood glucose level generally with increasing Cr inclusion levels. The Cr content of gill tissue was higher than that of back muscle in all treatments, and the addition of 1.2 or 1.8 mg kg-1 Cr significantly enhanced the Cr contents of back muscle. The cold stress test results showed that adding Cr significantly enhanced the serum T3 concentration and reduced the activity of serum creatine kinase and the serum cortisol level. These results indicated that the supplementation of chromium picolinate can improve the growth performance and reshape the serum protein and carbohydrate metabolism profile and has the potentiality to alleviate the detrimental effects of cold stress in Nile tilapia. The low-protein diet with 1.8 mg kg-1 Cr obtained the same growth performance as the high-protein diet.


Asunto(s)
Alimentación Animal/análisis , Composición Corporal/efectos de los fármacos , Cíclidos/crecimiento & desarrollo , Suplementos Dietéticos , Ácidos Picolínicos/farmacología , Fenómenos Fisiológicos Nutricionales de los Animales , Animales , Acuicultura , Cíclidos/sangre , Dieta/veterinaria , Relación Dosis-Respuesta a Droga , Ácidos Picolínicos/administración & dosificación
17.
Redox Rep ; 23(1): 146-152, 2018 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-29776315

RESUMEN

OBJECTIVE: The purpose of this study was to investigate the effects of chromium picolinate (CrPic) supplementation associated with aerobic exercise using measures of oxidative stress in rats exposed to air pollution. METHODS: Sixty-one male Wistar rats were divided into eight groups: residual oil fly ash (ROFA) exposure and sedentary (ROFA-SED); ROFA exposure, sedentary and supplemented (ROFA-SED-CrPic); ROFA exposure and trained (ROFA-AT); ROFA exposure, supplemented and trained (ROFA-AT-CrPic); sedentary (Sal-SED); sedentary and supplemented (Sal-SED-CrPic); trained (Sal-AT); and supplemented and trained (Sal-AT-CrPic). Rats exposed to ROFA (air pollution) received 50 µg of ROFA daily via intranasal instillation. Supplemented rats received CrPic (1 mg/kg/day) daily by oral gavage. Exercise training was performed on a rat treadmill (5×/week). Oxidative parameters were evaluated at the end of protocols. RESULTS: Trained groups demonstrated lower gain of body mass (P < .001) and increased exercise tolerance (P < .0001). In the gastrocnemius, trained groups demonstrated increased SOD activity (P < .0001) and decrease levels of TBARS (P = .0014), although CAT activity did not differ among groups (P = .4487). CONCLUSION: Air pollution exposure did not lead to alterations in oxidative markers in lungs and heart, and exercise training was responsible for decreasing oxidative stress of the gastrocnemius.


Asunto(s)
Contaminación del Aire/efectos adversos , Músculo Esquelético/efectos de los fármacos , Músculo Esquelético/metabolismo , Estrés Oxidativo/fisiología , Ácidos Picolínicos/farmacología , Aerobiosis , Animales , Masculino , Condicionamiento Físico Animal , Ratas , Ratas Wistar , Superóxido Dismutasa/metabolismo , Sustancias Reactivas al Ácido Tiobarbitúrico/metabolismo
18.
Biol Trace Elem Res ; 185(2): 448-455, 2018 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-29380257

RESUMEN

To investigate the effect of chromium picolinate (CrPic) on egg production performance, egg quality, blood indices, and immune function of laying hens, 270 23-week-old Beijing Red brown-egg laying hens were randomly assigned to one of three treatments with six replicates of 15 birds per replicate for each treatment in a completely randomized design. Laying hens were fed a Cr-unsupplemented corn-soybean meal basal diet (control, containing 0.45 mg Cr/kg by analysis) or the basal diet supplemented with 0.4 or 0.6 mg Cr/kg from CrPic for 10 weeks. Laying hens fed diets supplemented with CrPic had a lower (P < 0.05) serum glucose (GLU) concentration and higher (P < 0.03) serum antibody titer against Newcastle disease than those fed the control diet at 33 weeks of age. However, supplemental CrPic had no effect (P > 0.05) on egg production and egg quality of brown-egg laying hens from 24 to 33 weeks of age. The results from this study indicated that supplemental CrPic decreased serum GLU and enhanced the immune function of brown-egg laying hens.


Asunto(s)
Anticuerpos/inmunología , Glucemia/efectos de los fármacos , Pollos/sangre , Pollos/inmunología , Suplementos Dietéticos , Oviposición/fisiología , Ácidos Picolínicos/administración & dosificación , Ácidos Picolínicos/farmacología , Animales , Anticuerpos/sangre , Glucemia/inmunología , Huevos , Femenino , Distribución Aleatoria
19.
Biol Trace Elem Res ; 185(1): 205-215, 2018 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-29344818

RESUMEN

An 11-week feeding trial was carried out to investigate the effects of supplemented chromium picolinate (Cr-Pic) on the growth, whole-body composition, and relative mRNA expression related to lipogenesis and glucose metabolism in juvenile blunt snout bream. Seven isonitrogenous and isoenergetic diets with graded Cr supplementation levels were fed to triplicate groups. The final weight (FW), feed conversion ratio (FCR), and specific growth rate (SGR) were improved with increasing dietary Cr supplementation levels up to 0.4 mg/kg, and thereafter showed relatively constant. However, 12.0 mg/kg dietary Cr supplementation decreased growth and feed utilization. Based on SGR and FCR, the optimal dietary Cr supplementation level for the juvenile was estimated to be 0.28 mg/kg. Significantly higher plasma insulin levels were found in juvenile fed diets with 0.4 and 0.8 mg/kg Cr supplementation compared to those fed diet sans supplemented Cr. Plasma glucose levels decreased with increasing dietary Cr supplementation, and the lowest value was remarked in the group added 3.2 mg/kg of Cr. Adding 0.4-0.8 mg/kg Cr enhanced insulin receptor substrate 1 (IRS-1), phosphoinositide-3-kinase (PI3K), and pyruvate kinase (PK) and inhibited expression of phosphoenolpyruvate carboxykinase (PEPCK), glucose-6-phosphatase (G6Pase), and glycogen synthase (GS) mRNA levels. High dietary Cr (12.0 mg/kg) supplementation resulted in high G6Pase and PEPCK expression. The highest content of whole-body lipid was remarked in fish fed with 0.4 mg/kg dietary Cr, which related to the enhanced gene expression related to lipogenesis; thereafter, mRNA levels showed a diminishing trend. These findings indicate that optimum dietary Cr-Pic supplementation has a positive effect on growth and blood glucose homeostasis by modifying the mRNA levels related to glucose metabolism and lipogenesis in juvenile blunt snout bream.


Asunto(s)
Composición Corporal/efectos de los fármacos , Cromo/farmacología , Glucosa/metabolismo , Lipogénesis/efectos de los fármacos , Ácidos Picolínicos/farmacología , Alimentación Animal , Animales , Cyprinidae , Suplementos Dietéticos , Expresión Génica/efectos de los fármacos
20.
Cell Mol Biol (Noisy-le-grand) ; 63(10): 93-98, 2017 Oct 31.
Artículo en Inglés | MEDLINE | ID: mdl-29096748

RESUMEN

In this study, the effect of the supplemental organic chromium (Cr) forms on the expression of ovarian orexin(hypocretin), glucose transporters (GLUTs), heat shock proteins (HSPs) andnuclear factor-kappaB (NF-κB)were investigated in laying hens (HS). Laying hens (n=1800; 16-wk-old; Lohmann LSL-Lite) were allocated to 6 random groups according to a 2 × 3 factorial trial scheme with two different environmental temperatures [Thermoneutral (TN groups; at either 22±2 °C 24 h/d)  and heat stress (HS groups; at 34±2 °C for 8 h/d, 08:00 to 17:00 h, followed by 22°C for 16 h for a period of 12 wks)], andhens reared under both environmental conditions were fed either a basal diet or the basal diet supplemented with 1.600 mg of chromium-picolinate (CrPic, 12.43% Cr) and 0.788 mg of chromium-histidinate (CrHis, 25.22% Cr) per kg of diet, delivering 200 µg elemental Cr per kg diet. HS groups showed decreased levels of orexin and GLUTs(GLUT1, GLUT4), and increased NFκB, HSP60, HSP70 and HSP90 levels compared to the TN groups in ovarian tissue of hens (P < 0.0001 for all).However, dietary chromium supplementation (CrPic-CrHis) increasedorexin and GLUTs levels and significantly reduced the NF-κB and HSPs levels making them closer to those of thermoneutral group (P < 0.0001).In conclusion, CrPic and CrHis showed supported the relief and treatment of stress complications.


Asunto(s)
Pollos/metabolismo , Proteínas Facilitadoras del Transporte de la Glucosa/metabolismo , Histidina/análogos & derivados , Orexinas/metabolismo , Compuestos Organometálicos/farmacología , Ovario/metabolismo , Ácidos Picolínicos/farmacología , Regulación hacia Arriba/efectos de los fármacos , Animales , Suplementos Dietéticos , Femenino , Proteínas Facilitadoras del Transporte de la Glucosa/genética , Proteínas de Choque Térmico/metabolismo , Histidina/farmacología , FN-kappa B/metabolismo , Orexinas/genética , Ovario/efectos de los fármacos , Estrés Fisiológico , Temperatura
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