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1.
PLoS One ; 18(8): e0269717, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37585472

RESUMEN

Carlsberg subtilisin from Bacillus licheniformis PB1 was investigated as a potential feed supplement, through immobilizing on bentonite for improving the growth rate of broilers. Initially, the pre-optimized and partially-purified protease was extracted and characterized using SDS-PAGE with MW 27.0 KDa. The MALDI-TOF-MS/MS spectrum confirmed a tryptic peptide peak with m/z 1108.496 referring to the Carlsberg subtilisin as a protein-digesting enzyme with alkaline nature. The highest free enzyme activity (30 U/mg) was observed at 50°C, 1 M potassium phosphate, and pH 8.0. the enhanced stability was observed when the enzyme was adsorbed to an inert solid support with 86.39 ± 4.36% activity retention under 20 optimized conditions. Additionally, the dried immobilized enzyme exhibited only a 5% activity loss after two-week storage at room temperature. Structural modeling (Docking) revealed that hydrophobic interactions between bentonite and amino acids surrounding the catalytic triad keep the enzyme structure intact upon drying at RT. The prominent hygroscopic nature of bentonite facilitated protein structure retention upon drying. During a 46-days study, supplementation of boilers' feed with the subtilisin-bentonite complex promoted significant weight gain i.e. 15.03% in contrast to positive control (p = 0.001).


Asunto(s)
Aves de Corral , Subtilisinas , Animales , Subtilisinas/metabolismo , Aves de Corral/metabolismo , Pollos/metabolismo , Bentonita , Espectrometría de Masas en Tándem , Subtilisina , Concentración de Iones de Hidrógeno
2.
Biomed Res Int ; 2023: 4254051, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-36852294

RESUMEN

Traditional Chinese medicines (TCM) play an important role in the control and treatment of several animal diseases. Penthorum chinense Pursh (PCP) is a famous plant for its use in traditional medication practice and therapeutic effects in numerous pathological conditions. In China, PCP is utilized for both food and medication due to numerous bioactivities. PCP is widely administered in prevention and treatment of traumatic injury, edema, and liver diseases with functions of reducing swelling, support diuresis, blood stasis, and mitigation symptoms of excessive alcohol intake. Recently, PCP highlighted for research trials in various fields including pharmacology, pharmacognosy, cosmeceuticals, nutraceuticals, and pharmaceuticals due to medicinal significance with less toxicity and an effective ethnomedicine in veterinary practice. PCP contains diverse important ingredients such as flavonoids, organic acids, coumarins, lignans, polyphenols, and sterols that are important bioactive constituents of PCP exerting the therapeutic benefits and organ-protecting effects. In veterinary, PCP extract, compound, and phytochemicals/biomolecules significantly reversed the liver and kidney injuries, via antioxidation, oxidative stress, apoptosis, mitochondrial signaling pathways, and related genes. PCP water extract and compounds also proved in animal and humans' clinical trial for their hepatoprotective, antiaging, nephroprotective, anti-inflammatory, antidiabetic, antibacterial, antiapoptotic, immune regulation, and antioxidative stress pathways. This updated review spotlighted the current information on efficiency and application of PCP by compiling and reviewing recent publications on animal research. In addition, this review discussed the toxicology, traditional use, comparative, and clinical application of PCP in veterinary practices to authenticate and find out new perspectives on the research and development of this herbal medicine.


Asunto(s)
Enfermedades de los Animales , Animales , Humanos , Antibacterianos , Antioxidantes/farmacología , Apoptosis , Suplementos Dietéticos
3.
J Environ Manage ; 263: 110365, 2020 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-32883473

RESUMEN

Nanoparticles (NPs) application in soil as nano-fertilizers to increase crop yield is getting attention due to their higher efficiency and less environmental risks. This study investigated the interactive effects of variable titanium dioxide nanoparticles (TiO2-NPs) levels (0, 30, 50 and 100 mg kg-1) superimposed to phosphorus (P) fertilizer application in soil at the rates of 0, 25 and 50 mg kg-1 on wheat crop. Physiological parameters of plants, their antioxidant enzymes activities (SOD, POD), and contents of crude protein, H2O2, MDA and metals/nutrients (Al, Ca, Mg, Fe, Zn and Cu) were measured. Data on physiological traits revealed that application of 50 mg kg-1 of TiO2-NPs without P fertilizer significantly enhanced the root and shoot length by 63 and 26%, respectively. Increased contents of nutrients in the shoots, viz., Ca (316%), Cu (296%), Al (171%) and Mg (187%) with 50 mg kg-1 TiO2-NPs treatment reflected improvement in crop growth and grain quality. Furthermore, P contents in plant tissues were raised up to 56% with 50 mg kg-1 of TiO2-NPs even in the absence of P fertilizer. In the soil, concentration of phytoavailable P was significantly increased up to 63.3% in the presence of 50 mg kg-1 TiO2-NPs as compared to control. Contents of crude protein in grain were also enhanced by 22.8% (at P50) and 17.4% (at P25) with 50 mg kg-1 TiO2-NPs application. Along with P application, TiO2-NPs triggered the activities of SOD (2.06-33.97%) and POD (up to 13.19%), and H2O2 production (50.6-138.8%). However, MDA contents were not elevated significantly at any level of TiO2-NPs, and remained at par with control. It was noteworthy that highest level of TiO2-NPs, viz., 100 mg kg-1 exhibited plant and nutrients response lower than that with 50 mg kg-1. Further, TiO2-NPs triggered the bioavailability of micronutrient heavy metals (Zn, Cu and Fe) and Al, which could have toxicity at higher concentrations. These results suggested that TiO2-NPs might have some affinities with phosphate compounds and metal ions in the soil to bring them in soluble form, which enhanced their bioavailability. Although it improved the crop yield and quality, but toxic or negative impact of TiO2-NPs was also apparent at higher dose. Therefore, investigations on the potential interactions of NPs with other nutrients and toxic metals are needed to enhance our understanding for the safer application of nano-fertilizer.


Asunto(s)
Nanopartículas , Contaminantes del Suelo/análisis , Peróxido de Hidrógeno , Fósforo , Suelo , Titanio , Triticum
4.
Phytochemistry ; 170: 112213, 2020 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-31786408

RESUMEN

Clutia lanceolata Forssk. (C. lanceolata) is a medicinal plant native to sub-Saharan Africa and the Arabian Peninsula. Phytochemical investigation of the aerial parts of C. lanceolata yielded twenty-one coumarins including methylthio and methylsulfinyl-coumarins. Thirteen of these compounds are reported here for the first time, named as cluteolin A to M. The remaining eight compounds are known but have not been associated previously with C. lanceolata. The structures of the undescribed compounds were elucidated from their 2D NMR and MS spectra. Single crystal X-ray analyses confirmed the structures of eleven compounds. As, in Saudi Arabian tradition, C. lanceolata has been reported to have anti-diabetic and anti-fungal properties, the coumarins were examined for their biological activity. Seven compounds strongly enhanced the glucose-triggered release of insulin by murine pancreatic islets, with two compounds showing more than two-fold enhancement of insulin secretion, compared with the standard drug glimepiride.


Asunto(s)
Cumarinas/farmacología , Euphorbiaceae/química , Secreción de Insulina/efectos de los fármacos , Insulina/metabolismo , Fitoquímicos/farmacología , Azufre/farmacología , Animales , Cumarinas/química , Cumarinas/aislamiento & purificación , Masculino , Ratones , Ratones Endogámicos BALB C , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Arabia Saudita , Azufre/química , Azufre/aislamiento & purificación
5.
Org Biomol Chem ; 17(5): 1266-1276, 2019 01 31.
Artículo en Inglés | MEDLINE | ID: mdl-30663749

RESUMEN

Retama raetam is a bush which is a member of the family Fabaceae. It is used traditionally in North Africa and Saudi Arabia for the treatment of diabetes. Several flavonoids and alkaloids are already known from this plant. Chromatographic fractionation and purification led to the isolation of three new derivatives of prenylated flavones, retamasin C-E, and four new derivatives of prenylated isoflavones, retamasin F-I, in addition to two isoflavones which have not been previously reported in this plant. Particularly interesting structures included isoflavones containing 3,5-dihydro-2H-2,5-methanobenzo[e][1,4]dioxepine and 3a,8b-dihydro-7-hydroxyfuro[3,2-b]benzo[2,1-d]furan units, both of which are new amongst natural product flavonoids. Five new examples (two flavones and three isoflavones) strongly enhanced the glucose-triggered release of insulin by murine pancreatic islets and one isoflavone was a potent inhibitor of α-glucosidase. This study may rationalise the traditional medicinal use of R. raetam and provide new leads for drug design in the treatment of diabetes.


Asunto(s)
Fabaceae/química , Flavonoides/aislamiento & purificación , Flavonoides/farmacología , Inhibidores de Glicósido Hidrolasas/farmacología , Insulina/metabolismo , Extractos Vegetales/farmacología , Animales , Cromatografía Líquida de Alta Presión , Flavonoides/química , Masculino , Ratones , Ratones Endogámicos BALB C , Arabia Saudita , Análisis Espectral/métodos
6.
Bioorg Chem ; 87: 857-866, 2019 06.
Artículo en Inglés | MEDLINE | ID: mdl-30551808

RESUMEN

Aldose reductase is an important enzyme in the polyol pathway, where glucose is converted to fructose, and sorbitol is released. Aldose reductase activity increases in diabetes as the glucose levels increase, resulting in increased sorbitol production. Sorbitol, being less cell permeable tends to accumulate in tissues such as eye lenses, peripheral nerves and glomerulus that are not insulin sensitive. This excessive build-up of sorbitol is responsible for diabetes associated complications such as retinopathy and neuropathy. In continuation of our interest to design and discover potent inhibitors of aldo-keto reductases (AKRs; aldehyde reductase ALR1 or AKR1A, and aldose reductase ALR2 or AKR1B), herein we designed and investigated a series of new benzoxazinone-thiosemicarbazones (3a-r) as ALR2 and ALR1 inhibitors. Most compounds exhibited excellent inhibitory activities with IC50 values in lower micro-molar range. Compounds 3b and 3l were found to be most active ALR2 inhibitors with IC50 values of 0.52 ±â€¯0.04 and 0.19 ±â€¯0.03 µM, respectively, both compounds were more effective inhibitors as compared to the standard ALR2 inhibitor (sorbinil, with IC50 value of 3.14 ±â€¯0.02 µM).


Asunto(s)
Aldehído Reductasa/antagonistas & inhibidores , Benzoxazinas/farmacología , Inhibidores Enzimáticos/farmacología , Hipoglucemiantes/farmacología , Simulación del Acoplamiento Molecular , Aldehído Reductasa/química , Aldehído Reductasa/metabolismo , Benzoxazinas/química , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/química , Humanos , Hipoglucemiantes/síntesis química , Hipoglucemiantes/química , Estructura Molecular , Relación Estructura-Actividad
7.
Fitoterapia ; 131: 168-173, 2018 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-30149098

RESUMEN

Phytochemical investigation on the aerial parts of Lyonia ovalifolia (Wall.) Drude led to the isolation of three new iridoids, lyonofolin A (1), lyonofolin B (2), and lyonofolin C (3), and a known iridoid, gelsemiol (4). Structures of compounds 1-4 were determined by extensive spectroscopic analyses, including EI-MS, HREI-MS, UV, IR, and 1D- and 2D-NMR (HMBC, HSQC, COSY, NOESY) spectroscopic methods. The effect of insulin secretion of compounds 1, 2, and 4 were evaluated in mice pancreatic islets cellular model. This insulin secretory assay demonstrated that compound 2 potentiates glucose-induced insulin secretion, and thus can serve as a new insulin secretagogue for the treatment of diabetes. The newly isolated compounds were further evaluated against normal 3 T3 cell lines for cytotoxicity, where they did not show any cytotoxicity.


Asunto(s)
Ericaceae/química , Hipoglucemiantes/farmacología , Iridoides/farmacología , Islotes Pancreáticos/efectos de los fármacos , Células 3T3 , Animales , Hipoglucemiantes/aislamiento & purificación , Insulina/metabolismo , Iridoides/aislamiento & purificación , Islotes Pancreáticos/metabolismo , Masculino , Ratones , Ratones Endogámicos BALB C , Estructura Molecular , Nepal , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Componentes Aéreos de las Plantas/química , Extractos Vegetales/química
8.
Biomed Pharmacother ; 103: 1643-1651, 2018 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-29864953

RESUMEN

Plants have been used as medicinal agents since the origin of mankind. High cost and severe side effects associated with conventional chemotherapy has limited their general acceptability and fuel up the search for alternate options. The alternative treatment options like phytochemicals have come up with ease of availability and cost effectiveness. Owing to their general acceptance, safety, low side effects and multistep targeting in signal transduction pathways, plant derived phyto-constituents have promising anti-carcinogenic potential for skin related cancers. This leads to the surge in research of new phytochemicals for the prevention and cure of a variety of skin cancers which are major cause of morbidity and mortality in present world. Although very limited clinical data involving humans is available in literature to demonstrate favorable eff ;ects of phyto-constituents on various types of skin carcinomas yet the topical treatment with these plant derived anticancer phytochemicals is very promising. There are various mechanisms and pathways responsible for antitumor activity of plant derived medicinal compounds such as loss of mitochondrial membrane potential, release of cytochrome-c, Down regulation of Anti-apoptotic proteins and Up regulation of pro-apoptotic proteins, Activation of Caspase, Fas, FADD, p53 and c-Jun signaling pathway, Inhibition of Akt signaling pathway, phosphorylation of ERK, P13K, Raf, survivin gene, STAT 3 and NF-kB. In-vitro testing of skin cancer cell lines models offers the opportunity for identifying mechanisms of action of compounds from plant origin against variety of skin related cancers. This review thus aims at providing an overview of plant derived anti-cancer compounds which have been reported to show promising anti-carcinogenic effects against various skin cancer cell lines and on animal models. Phytochemicals that are discussed in this review include steroids, coumarines, trepenes, essential oils, alkaloids, esters, ethers, resins, phenols and flavonoids. This review also provides information about marketed formulations developed so far from plant derived compounds for skin cancer prevention and treatment.


Asunto(s)
Antineoplásicos/uso terapéutico , Plantas/química , Neoplasias Cutáneas/tratamiento farmacológico , Animales , Línea Celular Tumoral , Humanos , Fitoquímicos/uso terapéutico , Fitoterapia , Neoplasias Cutáneas/patología
9.
Science ; 360(6396)2018 06 29.
Artículo en Inglés | MEDLINE | ID: mdl-29743352

RESUMEN

The Yamnaya expansions from the western steppe into Europe and Asia during the Early Bronze Age (~3000 BCE) are believed to have brought with them Indo-European languages and possibly horse husbandry. We analyzed 74 ancient whole-genome sequences from across Inner Asia and Anatolia and show that the Botai people associated with the earliest horse husbandry derived from a hunter-gatherer population deeply diverged from the Yamnaya. Our results also suggest distinct migrations bringing West Eurasian ancestry into South Asia before and after, but not at the time of, Yamnaya culture. We find no evidence of steppe ancestry in Bronze Age Anatolia from when Indo-European languages are attested there. Thus, in contrast to Europe, Early Bronze Age Yamnaya-related migrations had limited direct genetic impact in Asia.


Asunto(s)
Pueblo Asiatico/genética , Domesticación , Flujo Genético , Genoma Humano , Caballos , Migración Humana/historia , Animales , Asia , Cromosomas Humanos Y/genética , ADN Antiguo , ADN Mitocondrial/genética , Europa (Continente) , Pradera , Historia Antigua , Humanos , Lenguaje , Secuenciación Completa del Genoma
10.
Acta Pharm ; 68(1): 47-60, 2018 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-29453917

RESUMEN

In the present study, berries of two different species of Solanaceae family, Withania somnifera (WS) and Solanum nigrum (SN), were extracted in methanol and then fractionated with solvents, ranging from non-polar to polar, for their phytochemical profiling and investigation of antioxidant and tyrosinase enzyme inhibition capacity. The methanolic extract and n-hexane, ethyl acetate (WSEA, SNEA) and aqueous fractions were chemically analyzed and evaluated for biological activity. Total flavonoids and total phenolics were quantified in WSEA (96.91 ± 1.56 µg QE mg-1 sample and 178.45 ± 2.78 µg GAE mg-1 s ample, r esp.) and S NEA (89.58 ± 0.98 µg QE mg-1 sample and 120.15 ± 2.33 µg GAE mg-1 sample, resp.). HPLC-DAD analysis of ethyl acetate fractions of WS and SN measured 13.74 and 5.34 µg GAE mg-1 dry fraction and 3.72 and 3.41 µg QE mg-1 dry fraction, resp. WSEA and SNEA fractions showed the highest 2,2-diphenyl-2-picryl hydrazyl (DPPH) radical scavenging, total antioxidant capacity and iron reducing power activity. The highest inhibition of tyrosinase enzyme was also exhibited by WSEA and SNEA (59.6 and 58.7 %) resp. This investigation justifies the medicinal value of W. somnifera and S. nigrum berry extracts as potential and readily available sources of natural antioxidants. Marked tyrosinase enzyme inhibition activity and antioxidant activity of both plant extracts might be due to polyphenols and flavonoids.


Asunto(s)
Antioxidantes/química , Monofenol Monooxigenasa/antagonistas & inhibidores , Extractos Vegetales/química , Extractos Vegetales/farmacología , Solanum nigrum/química , Withania/química , Flavonoides/química , Flavonoides/farmacología , Frutas/química , Fenoles/química , Polifenoles/química
11.
Bioorg Chem ; 75: 62-70, 2017 12.
Artículo en Inglés | MEDLINE | ID: mdl-28917123

RESUMEN

Recent efforts to develop cure for chronic diabetic complications have led to the discovery of potent inhibitors against aldose reductase (AKR1B1, EC 1.1.1.21) whose role in diabetes is well-evident. In the present work, two new natural products were isolated from the ariel part of Ocimum basilicum; 7-(3-hydroxypropyl)-3-methyl-8-ß-O-d-glucoside-2H-chromen-2-one (1) and E-4-(6'-hydroxyhex-3'-en-1-yl)phenyl propionate (2) and confirmed their structures with different spectroscopic techniques including NMR spectroscopy etc. The isolated compounds (1, 2) were evaluated for in vitro inhibitory activity against aldose reductase (AKR1B1) and aldehyde reductase (AKR1A1). The natural product (1) showed better inhibitory activity for AKR1B1 with IC50 value of 2.095±0.77µM compare to standard sorbinil (IC50=3.14±0.02µM). Moreover, the compound (1) also showed multifolds higher activity (IC50=0.783±0.07µM) against AKR1A1 as compared to standard valproic acid (IC50=57.4±0.89µM). However, the natural product (2) showed slightly lower activity for AKR1B1 (IC50=4.324±1.25µM). Moreover, the molecular docking studies of the potent inhibitors were also performed to identify the putative binding modes within the active site of aldose/aldehyde reductases.


Asunto(s)
Aldehído Reductasa/antagonistas & inhibidores , Benzopiranos/química , Inhibidores Enzimáticos/química , Glucósidos/química , Ocimum basilicum/química , Fenilpropionatos/química , Aldehído Reductasa/metabolismo , Benzopiranos/aislamiento & purificación , Benzopiranos/metabolismo , Benzopiranos/farmacología , Sitios de Unión , Activación Enzimática/efectos de los fármacos , Inhibidores Enzimáticos/aislamiento & purificación , Inhibidores Enzimáticos/metabolismo , Inhibidores Enzimáticos/farmacología , Glucósidos/aislamiento & purificación , Glucósidos/metabolismo , Glucósidos/farmacología , Concentración 50 Inhibidora , Espectroscopía de Resonancia Magnética , Conformación Molecular , Simulación del Acoplamiento Molecular , Ocimum basilicum/metabolismo , Fenilpropionatos/aislamiento & purificación , Fenilpropionatos/metabolismo , Fenilpropionatos/farmacología , Componentes Aéreos de las Plantas/química , Componentes Aéreos de las Plantas/metabolismo , Extractos Vegetales/química , Extractos Vegetales/farmacología , Estructura Terciaria de Proteína
12.
Biomed Pharmacother ; 94: 446-457, 2017 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-28779706

RESUMEN

Over the past few years, it was suggested that a rational approach to treat cancer in clinical settings requires a multipronged approach that augments improvement in systemic efficiency along with modification in cellular phenotype leads to more efficient cell death response. Recently, the combinatory delivery of traditional chemotherapeutic drugs with natural compounds proved to be astonishing to deal with a variety of cancers, especially that are resistant to chemotherapeutic drugs. The natural compounds not only synergize the effects of chemotherapeutics but also minimize drug associated systemic toxicity. In this review, our primary focus was on antitumor effects of natural compounds. Previously, the drugs from natural sources are highly precise and safer than drugs of synthetic origins. Many natural compounds exhibit anti-cancer potentials by inducing apoptosis in different tumor models, in-vitro and in-vivo. Furthermore, natural compounds are also found equally useful in chemotherapeutic drug resistant tumors. Moreover, these Phyto-compounds also possess numerous other pharmacological properties such as antifungal, antimicrobial, antiprotozoal, and hepatoprotection. Aglycone solasodine and solanidine derivatives are the utmost important steroidal glycoalkaloids that are present in various Solanum species, are discussed here. These natural compounds are highly cytotoxic against different tumor cell lines. As the molecular weight is concerned; these are smaller molecular weight chemotherapeutic agents that induce cell death response by initiating apoptosis through both extrinsic and intrinsic pathways.


Asunto(s)
Diosgenina/uso terapéutico , Neoplasias/tratamiento farmacológico , Neoplasias/patología , Alcaloides Solanáceos/uso terapéutico , Animales , Antineoplásicos/química , Antineoplásicos/uso terapéutico , Línea Celular Tumoral , Diosgenina/química , Humanos , Modelos Biológicos , Alcaloides Solanáceos/química
13.
Eur J Nutr ; 56(2): 591-601, 2017 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-26593435

RESUMEN

PURPOSE: The present study was undertaken to explore the possible anti-diabetic mechanism(s) of Emblica officinalis (EO) and its active constituent, ellagic acid (EA), in vitro and in vivo. METHOD: Neonatal streptozotocin-induced non-obese type 2 diabetic rats were treated with a methanolic extract of EO (250 or 500 mg/kg) for 28 days, and blood glucose, serum insulin, and plasma antioxidant status were measured. Insulin and glucagon immunostaining and morphometry were performed in pancreatic section, and liver TBARS and GSH levels were measured. Additionally, EA was tested for glucose-stimulated insulin secretion and glucose tolerance test. RESULTS: Treatment with EO extract resulted in a significant decrease in the fasting blood glucose in a dose- and time-dependent manner in the diabetic rats. It significantly increased serum insulin in the diabetic rats in a dose-dependent manner. Insulin-to-glucose ratio was also increased by EO treatment. Immunostaining of pancreas showed that EO250 increased ß-cell size, but EO500 increased ß-cells number in diabetic rats. EO significantly increased plasma total antioxidants and liver GSH and decreased liver TBARS. EA stimulated glucose-stimulated insulin secretion from isolated islets and decreased glucose intolerance in diabetic rats. CONCLUSION: Ellagic acid in EO exerts anti-diabetic activity through the action on ß-cells of pancreas that stimulates insulin secretion and decreases glucose intolerance.


Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Ácido Elágico/administración & dosificación , Hipoglucemiantes , Células Secretoras de Insulina/efectos de los fármacos , Phyllanthus emblica/química , Animales , Antioxidantes , Glucemia/análisis , Frutas/química , Glucagón/análisis , Glutatión/análisis , Insulina/análisis , Insulina/sangre , Células Secretoras de Insulina/química , Células Secretoras de Insulina/citología , Hígado/química , Hígado/efectos de los fármacos , Fitoterapia , Extractos Vegetales/administración & dosificación , Ratas , Sustancias Reactivas al Ácido Tiobarbitúrico/análisis
14.
Nat Prod Commun ; 11(5): 615-20, 2016 May.
Artículo en Inglés | MEDLINE | ID: mdl-27319132

RESUMEN

A new ceramide and a new biflavonoid named parinaramide (1) and sparinaritin (2), respectively, have been isolated along with ten known compounds, kaempferol, quercetin, taxifolin, taxifolin-3-O-rhamnoside, lupeol, betulinic acid, ursolic acid, 2α-hydroxy-ursolic acid, 2,3-dihydroxy-1-(4-hydroxy-3,5-dimethoxyphenyl)-1-propanone, and sucrose, from the leaves of Parinari hypochrysea (Chrysobalanaceae). Structures were determined using 1D- and 2D-NMR, MS and by chemical analysis. The methanol extract of leaves, stem bark and roots of P. hypochrysea were screened for their antioxidant and lipoxygenase inhibition potential and found to be inactive.


Asunto(s)
Biflavonoides/aislamiento & purificación , Ceramidas/aislamiento & purificación , Chrysobalanaceae/química , Biflavonoides/química , Ceramidas/química , Estructura Molecular , Hojas de la Planta/química
15.
Int J Mol Sci ; 16(9): 20290-307, 2015 Aug 27.
Artículo en Inglés | MEDLINE | ID: mdl-26343638

RESUMEN

Plant extracts are complex matrices and, although crude extracts are widely in use, purified compounds are pivotal in drug discovery. This study describes the application of automated preparative-HPLC combined with a rapid off-line bacterial bioassay, using reduction of a tetrazolium salt as an indicator of bacterial metabolism. This approach enabled the identification of fractions from Dodonaea viscosa that were active against Staphylococcus aureus and Escherichia coli, which, ultimately, resulted in the identification of a clerodane type diterpenoid, 6ß-hydroxy-15,16-epoxy-5ß, 8ß, 9ß, 10α-cleroda-3, 13(16), 14-trien-18-oic acid, showing bacteriostatic activity (minimum inhibitory concentration (MIC) = 64-128 µg/mL) against test bacteria. To the best of our knowledge, this is the first report on antibacterial activity of this metabolite from D. viscosa.


Asunto(s)
Antibacterianos/farmacología , Diterpenos de Tipo Clerodano/farmacología , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/farmacología , Sapindaceae/química , Antibacterianos/química , Diterpenos de Tipo Clerodano/química , Pruebas de Sensibilidad Microbiana/métodos , Estructura Molecular , Extractos Vegetales/química
16.
Phytother Res ; 29(10): 1672-5, 2015 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-26178652

RESUMEN

Ethno-botanical inspired isolation from plant Scoparia dulcis Linn. (Sweet Broomweed) yielded six compounds, coixol (1), glutinol (2), glutinone (3), friedelin (4), betulinic acid (5), and tetratriacontan-1-ol (6). There structures were identified using mass and 1D- and 2D-NMR spectroscopy techniques. Compounds 1-6 were evaluated for their insulin secretory activity on isolated mice islets and MIN-6 pancreatic ß-cell line, and compounds 1 and 2 were found to be potent and mildly active, respectively. Compound 1 was further evaluated for insulin secretory activity on MIN-6 cells. Compound 1 was subjected to in vitro cytotoxicity assay against MIN-6, 3T3 cell lines, and islet cells, and in vivo acute toxicity test in mice that was found to be non-toxic. The insulin secretory activity of compounds 1 and 2 supported the ethno-botanic uses of S. dulcis as an anti-diabetic agent.


Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/farmacología , Extractos Vegetales/uso terapéutico , Scoparia , Células 3T3 , Animales , Insulina , Islotes Pancreáticos , Masculino , Ratones , Nepal , Ratas , Ratas Wistar
17.
Nat Genet ; 47(7): 814-7, 2015 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-26005865

RESUMEN

The major pathway by which the brain obtains essential omega-3 fatty acids from the circulation is through a sodium-dependent lysophosphatidylcholine (LPC) transporter (MFSD2A), expressed in the endothelium of the blood-brain barrier. Here we show that a homozygous mutation affecting a highly conserved MFSD2A residue (p.Ser339Leu) is associated with a progressive microcephaly syndrome characterized by intellectual disability, spasticity and absent speech. We show that the p.Ser339Leu alteration does not affect protein or cell surface expression but rather significantly reduces, although not completely abolishes, transporter activity. Notably, affected individuals displayed significantly increased plasma concentrations of LPCs containing mono- and polyunsaturated fatty acyl chains, indicative of reduced brain uptake, confirming the specificity of MFSD2A for LPCs having mono- and polyunsaturated fatty acyl chains. Together, these findings indicate an essential role for LPCs in human brain development and function and provide the first description of disease associated with aberrant brain LPC transport in humans.


Asunto(s)
Ácidos Grasos Omega-3/metabolismo , Microcefalia/genética , Proteínas Supresoras de Tumor/genética , Adolescente , Animales , Secuencia de Bases , Transporte Biológico , Barrera Hematoencefálica/metabolismo , Estudios de Casos y Controles , Niño , Preescolar , Femenino , Estudios de Asociación Genética , Células HEK293 , Humanos , Lactante , Lisofosfatidilcolinas/sangre , Masculino , Microcefalia/sangre , Mutación Missense , Linaje , Análisis de Secuencia de ADN , Simportadores , Síndrome
18.
Phytomedicine ; 22(2): 297-300, 2015 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-25765836

RESUMEN

Although the anti-diabetic activity of cinnamic acid, a pure compound from cinnamon, has been reported but its mechanism(s) is not yet clear. The present study was designed to explore the possible mechanism(s) of anti-diabetic activity of cinnamic acid in in vitro and in vivo non-obese type 2 diabetic rats. Non-obese type 2 diabetes was developed by injecting 90 mg/kg streptozotocin in 2-day-old Wistar pups. Cinnamic acid and cinnamaldehyde were administered orally to diabetic rats for assessing acute blood glucose lowering effect and improvement of glucose tolerance. Additionally, insulin secretory activity of cinnamic acid and cinnamaldehyde was evaluated in isolated mice islets. Cinnamic acid, but not cinnamaldehyde, decreased blood glucose levels in diabetic rats in a time- and dose-dependent manner. Oral administration of cinnamic acid with 5 and 10 mg/kg doses to diabetic rats improved glucose tolerance in a dose-dependent manner. The improvement by 10 mg/kg cinnamic acid was comparable to that of standard drug glibenclamide (5 mg/kg). Further in vitro studies showed that cinnamaldehyde has little or no effect on glucose-stimulated insulin secretion; however, cinnamic acid significantly enhanced glucose-stimulated insulin secretion in isolated islets. In conclusion, it can be said that cinnamic acid exerts anti-diabetic activity by improving glucose tolerance in vivo and stimulating insulin secretion in vitro.


Asunto(s)
Cinamatos/farmacología , Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/farmacología , Insulina/metabolismo , Islotes Pancreáticos/efectos de los fármacos , Acroleína/análogos & derivados , Acroleína/farmacología , Animales , Glucemia/metabolismo , Células Cultivadas , Diabetes Mellitus Experimental/inducido químicamente , Femenino , Prueba de Tolerancia a la Glucosa , Secreción de Insulina , Masculino , Ratones Endogámicos BALB C , Ratas Wistar
19.
J Ethnopharmacol ; 152(3): 561-7, 2014 Mar 28.
Artículo en Inglés | MEDLINE | ID: mdl-24534525

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Bergenia himalaica Boriss is mainly distributed in the temperate Himalayas between altitudes of 900 and 3000m ranging from the southeastern regions in central Asia and northern regions in South Asia. The plant has a long history of its use in traditional medicine for the treatment of various diseases such as diabetes, urinary complaints, kidney stones, hemorrhagic diseases and epilepsy. The aim of this study is to isolate pure compounds from Bergenia himalaica Boriss, elucidate their structures and determine their blood glucose lowering activity to obtain additional scientific evidence for its usage in traditional medicine for the management of diabetes. MATERIALS AND METHODS: The crude methanolic extract from the aerial parts of Bergenia himalaica Boriss was separated into EtOAc and water sub-extracts and the EtOAc sub-extract was further divided into petroleum ether soluble and insoluble fractions. The pet-ether insoluble fraction was subjected to fractionation through column chromatography followed by prep. TLC. The blood glucose lowering activity of the 2 new compounds was evaluated in streptozotocin-nicotinamide induced diabetic rats. Additionally, glucose-stimulated insulin secretion was measured on isolated mice islets. RESULTS: Two new compounds bergenicin and bergelin were isolated and their structures determined on the basis of spectral analysis. Significant decrease of blood glucose was observed at 1-h (1.0mg/kg) and 2-h (0.5mg/kg), after bergenicin administration to the diabetic rats and at 2-h (1.0mg/kg) and 3-h (0.5mg/kg), after bergelin administration. Bergenicin, but not bergelin, enhanced glucose-stimulated insulin secretion in isolated pancreatic islets. CONCLUSIONS: In the present studies two new compounds, bergenicin and bergelin were isolated from Bergenia himalaica Boriss and their structures were elucidated. Both the compounds showed anti-hyperglycemic effects in streptozotocin-nicotinamide induced diabetic rats. Bergenicin showed insulinotropic effect; suggesting that the anti-hyperglycemic effect is mostly due to enhancement of insulin secretion from pancreatic ß-cells.


Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/farmacología , Extractos Vegetales/farmacología , Saxifragaceae/química , Animales , Glucemia/efectos de los fármacos , Diabetes Mellitus Experimental/patología , Femenino , Furanos/química , Furanos/aislamiento & purificación , Furanos/farmacología , Compuestos Heterocíclicos de 4 o más Anillos/química , Compuestos Heterocíclicos de 4 o más Anillos/aislamiento & purificación , Compuestos Heterocíclicos de 4 o más Anillos/farmacología , Hipoglucemiantes/aislamiento & purificación , Insulina/metabolismo , Secreción de Insulina , Células Secretoras de Insulina/efectos de los fármacos , Células Secretoras de Insulina/metabolismo , Islotes Pancreáticos/efectos de los fármacos , Islotes Pancreáticos/metabolismo , Masculino , Medicina Tradicional , Ratones , Ratones Endogámicos BALB C , Niacinamida/toxicidad , Componentes Aéreos de las Plantas , Extractos Vegetales/química , Ratas , Ratas Wistar , Análisis Espectral , Estreptozocina/toxicidad , Factores de Tiempo
20.
Pak J Pharm Sci ; 26(2): 251-4, 2013 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-23455192

RESUMEN

This work aimed to evaluate the inhibitory effects of Olea ferruginea crude leaves extract that are commonly used as remedy to cure infections in the tribal (Khyber Agency) areas of Pakistan against some of bacterial and fungal pathogens. The crude n-hexane fraction was appreciably active against both gram positive and negative microorganisms (MIC ranged from 7.5 to 15 mg/ml) followed by butanol fraction (MIC 15 to 30 mg/ml). Conversely least biological activity was shown by chloroform (30mg/ml) and methanol (15 to 30mg/ml) crude fractions. The MBC observed for all crude fractions was same or 2 times higher when compared with MIC for all crude extract fractions. Likewise all the fractions showed activity against Aspergillus niger and maximum zones of inhibition were shown by the n-hexane fraction (14 ± (0.02), butanol (13 ± (0.02) followed by methanol (9 ± (0.05) and chloroform fractions (7 ± (0.02). These results clearly imitate the antibacterial and antifungal potential of Olea ferruginea and hence we recommend the whole plant for further futuristic studies.


Asunto(s)
Antibacterianos/farmacología , Antifúngicos/farmacología , Olea/química , Extractos Vegetales/farmacología , Antibacterianos/aislamiento & purificación , Antifúngicos/aislamiento & purificación , Aspergillus niger/efectos de los fármacos , Aspergillus niger/crecimiento & desarrollo , Cloroformo/química , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Gramnegativas/crecimiento & desarrollo , Bacterias Grampositivas/efectos de los fármacos , Bacterias Grampositivas/crecimiento & desarrollo , Hexanos/química , Metanol/química , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/aislamiento & purificación , Hojas de la Planta , Plantas Medicinales , Solventes/química
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