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Pesquisa : B01.650.940.800.575.912.250.812.666 [Categoria DeCS]
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[PMID]:29320554
[Au] Autor:Choudhary N; Singh V
[Ad] Endereço:Centre for Computational Biology and Bioinformatics, School of Life Sciences, Central University of Himachal Pradesh, Himachal Pradesh, India.
[Ti] Título:A census of P. longum's phytochemicals and their network pharmacological evaluation for identifying novel drug-like molecules against various diseases, with a special focus on neurological disorders.
[So] Source:PLoS One;13(1):e0191006, 2018.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Piper longum (P. longum, also called as long pepper) is one of the common culinary herbs that has been extensively used as a crucial constituent in various indigenous medicines, specifically in traditional Indian medicinal system known as Ayurveda. For exploring the comprehensive effect of its constituents in humans at proteomic and metabolic levels, we have reviewed all of its known phytochemicals and enquired about their regulatory potential against various protein targets by developing high-confidence tripartite networks consisting of phytochemical-protein target-disease association. We have also (i) studied immunomodulatory potency of this herb; (ii) developed subnetwork of human PPI regulated by its phytochemicals and could successfully associate its specific modules playing important role in diseases, and (iii) reported several novel drug targets. P10636 (microtubule-associated protein tau, that is involved in diseases like dementia etc.) was found to be the commonly screened target by about seventy percent of these phytochemicals. We report 20 drug-like phytochemicals in this herb, out of which 7 are found to be the potential regulators of 5 FDA approved drug targets. Multi-targeting capacity of 3 phytochemicals involved in neuroactive ligand receptor interaction pathway was further explored via molecular docking experiments. To investigate the molecular mechanism of P. longum's action against neurological disorders, we have developed a computational framework that can be easily extended to explore its healing potential against other diseases and can also be applied to scrutinize other indigenous herbs for drug-design studies.
[Mh] Termos MeSH primário: Descoberta de Drogas
Doenças do Sistema Nervoso/tratamento farmacológico
Compostos Fitoquímicos/farmacologia
Piper/química
Extratos Vegetais/farmacologia
Mapas de Interação de Proteínas/efeitos dos fármacos
[Mh] Termos MeSH secundário: Bases de Dados Factuais
Seres Humanos
Simulação de Acoplamento Molecular
Doenças do Sistema Nervoso/metabolismo
Fitoterapia
Proteômica
[Pt] Tipo de publicação:EVALUATION STUDIES; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Phytochemicals); 0 (Plant Extracts)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180212
[Lr] Data última revisão:
180212
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180111
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0191006


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[PMID]:29174417
[Au] Autor:Hematpoor A; Paydar M; Liew SY; Sivasothy Y; Mohebali N; Looi CY; Wong WF; Azirun MS; Awang K
[Ad] Endereço:Institute of Biological Sciences, Faculty of Science, University of Malaya, 50603 Kuala Lumpur, Malaysia.
[Ti] Título:Phenylpropanoids isolated from Piper sarmentosum Roxb. induce apoptosis in breast cancer cells through reactive oxygen species and mitochondrial-dependent pathways.
[So] Source:Chem Biol Interact;279:210-218, 2018 Jan 05.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:The aim of the present study is to isolate bioactive compounds from the roots of Piper sarmentosum and examine the mechanism of action using human breast cancer cell line (MDA-MB-231). Bioassay guided-fractionation of methanolic extract led to the isolation of asaricin (1) and isoasarone (2). Asaricin (1) and isoasarone (2) had significant cytotoxicity towards MDA-MB-231. MCF-10A (human normal breast epithelial cells) cells are less sensitive than MDA-MB-231, but they respond to the treatment with the same unit of measurement. Both compounds increase reactive oxygen species (ROS), decrease mitochondrial membrane potential (MMP) and enhance cytochrome c release in treated MDA-MB-231 cells. Isoasarone (2) markedly elevated caspase -8 and -3/7 activities and caused a decline in nuclear NF-κB translocation, suggesting extrinsic, death receptor-linked apoptosis pathway. Quantitative PCR results of MDA-MB-231 treated with asaricin (1) and isoasarone (2) showed altered expression of Bcl-2: Bax level. The inhibitory potency of these isolates may support the therapeutic uses of these compounds in breast cancer.
[Mh] Termos MeSH primário: Apoptose/efeitos dos fármacos
Mitocôndrias/efeitos dos fármacos
Fenilpropionatos/farmacologia
Piper/química
Espécies Reativas de Oxigênio/metabolismo
[Mh] Termos MeSH secundário: Antineoplásicos Fitogênicos
Neoplasias da Mama
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Feminino
Seres Humanos
Mitocôndrias/metabolismo
Estrutura Molecular
Fenilpropionatos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents, Phytogenic); 0 (Phenylpropionates); 0 (Reactive Oxygen Species)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180103
[Lr] Data última revisão:
180103
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE


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[PMID]:28851456
[Au] Autor:Moein E; Hajimehdipoor H; Toliyat T; Choopani R; Hamzeloo-Moghadam M
[Ad] Endereço:Department of Traditional Pharmacy, School of Traditional Medicine, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
[Ti] Título:Formulation of an aloe-based product according to Iranian traditional medicine and development of its analysis method.
[So] Source:Daru;25(1):19, 2017 Aug 29.
[Is] ISSN:2008-2231
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Currently, people are more interested to traditional medicine. The traditional formulations should be converted to modern drug delivery systems to be more acceptable for the patients. In the present investigation, a poly herbal medicine "Ayarij-e-Faiqra" (AF) based on Iranian traditional medicine (ITM) has been formulated and its quality control parameters have been developed. METHODS: The main ingredients of AF including barks of Cinnamomum zeylanicum Blume and Cinnamomum cassia J. Presl, the rhizomes of Nardostachys jatamansi DC., the fruits of Piper cubeba L.f., the flowers of Rosa damascena Herrm., the oleo gum resin of Pistacia terebinthus L. and Aloe spp. dried juice were powdered and used for preparing seven tablet formulations of the herbal mixture. Flowability of the different formulated powders was examined and the best formulations were selected (F6&F7). The tablets were prepared from the selected formulations compared according to the physical characteristics and finally, F7 was selected and coated. Physicochemical characters of core and coated AF tablets were determined and the HPLC method for quantitation of aloin as a marker of tablets was selected and verified according to selectivity, linearity, precision, recovery, LOD and LOQ. RESULTS: The results showed that core and coated AF tablets were in agreement with USP requirements for herbal drugs. They had acceptable appearance, disintegration time, friability, hardness, dissolution behavior, weight variation and content uniformity. The amount of aloin in tablets was found 123.1 mg/tab. The HPLC method for aloin determination in AF tablets was verified according to selectivity, linearity (5-500 µg/ml, r :0.9999), precision (RSD: 1.62%), recovery (108.0%), LOD & LOQ (0.0053 & 0.0161 µg/ml). CONCLUSIONS: The formulated tablets could be a good substitute for powder and capsules of AF in ITM clinics with a feasible and precise method for its quality control. Ayarij-e-Faiqra formulation.
[Mh] Termos MeSH primário: Aloe
Medicina Tradicional
Fitoterapia
[Mh] Termos MeSH secundário: Cinnamomum
Composição de Medicamentos
Emodina/análogos & derivados
Emodina/análise
Emodina/uso terapêutico
Flores
Frutas
Medicina Herbária/métodos
Irã (Geográfico)
Medicina Tradicional/métodos
Nardostachys
Fitoterapia/métodos
Piper
Pistacia
Casca de Planta
Rizoma
Rosa
Comprimidos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Tablets); KA46RNI6HN (Emodin); W41H6S09F4 (alloin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171010
[Lr] Data última revisão:
171010
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170831
[St] Status:MEDLINE
[do] DOI:10.1186/s40199-017-0185-x


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[PMID]:28704049
[Au] Autor:Gutiérrez-García K; Neira-González A; Pérez-Gutiérrez RM; Granados-Ramírez G; Zarraga R; Wrobel K; Barona-Gómez F; Flores-Cotera LB
[Ad] Endereço:Evolution of Metabolic Diversity Laboratory, Unidad de Genómica Avanzada (Langebio), Cinvestav-IPN , Irapuato 36821, Guanajuato, Mexico.
[Ti] Título:Phylogenomics of 2,4-Diacetylphloroglucinol-Producing Pseudomonas and Novel Antiglycation Endophytes from Piper auritum.
[So] Source:J Nat Prod;80(7):1955-1963, 2017 Jul 28.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:2,4-Diacetylphloroglucinol (DAPG) (1) is a phenolic polyketide produced by some plant-associated Pseudomonas species, with many biological activities and ecological functions. Here, we aimed at reconstructing the natural history of DAPG using phylogenomics focused at its biosynthetic gene cluster or phl genes. In addition to around 1500 publically available genomes, we obtained and analyzed the sequences of nine novel Pseudomonas endophytes isolated from the antidiabetic medicinal plant Piper auritum. We found that 29 organisms belonging to six Pseudomonas species contain the phl genes at different frequencies depending on the species. The evolution of the phl genes was then reconstructed, leading to at least two clades postulated to correlate with the known chemical diversity surrounding DAPG biosynthesis. Moreover, two of the newly obtained Pseudomonas endophytes with high antiglycation activity were shown to exert their inhibitory activity against the formation of advanced glycation end-products via DAPG and related congeners. Its isomer, 5-hydroxyferulic acid (2), detected during bioactivity-guided fractionation, together with other DAPG congeners, were found to enhance the detected inhibitory activity. This report provides evidence of a link between the evolution and chemical diversity of DAPG and congeners.
[Mh] Termos MeSH primário: Endófitos/química
Floroglucinol/análogos & derivados
Piper/microbiologia
Plantas Medicinais/microbiologia
Policetídeos/isolamento & purificação
Policetídeos/farmacologia
Pseudomonas/química
[Mh] Termos MeSH secundário: Ácidos Cumáricos/química
Ácidos Cumáricos/isolamento & purificação
México
Estrutura Molecular
Família Multigênica
Floroglucinol/química
Floroglucinol/isolamento & purificação
Floroglucinol/farmacologia
Piper/genética
Componentes Aéreos da Planta/química
Plantas Medicinais/genética
Policetídeos/química
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Coumaric Acids); 0 (Polyketides); 1782-55-4 (5-hydroxyferulic acid); 8XV4YYO3WN (2,4-diacetylphloroglucinol); DHD7FFG6YS (Phloroglucinol)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170915
[Lr] Data última revisão:
170915
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170714
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jnatprod.6b00823


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[PMID]:28641835
[Au] Autor:Xin H; Dai Z; Cai J; Ke Y; Shi H; Fu Q; Jin Y; Liang X
[Ad] Endereço:Engineering Research Center of Pharmaceutical Process Chemistry, Ministry of Education, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, PR China.
[Ti] Título:Rapid purification of diastereoisomers from Piper kadsura using supercritical fluid chromatography with chiral stationary phases.
[So] Source:J Chromatogr A;1509:141-146, 2017 Aug 04.
[Is] ISSN:1873-3778
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Supercritical fluid chromatography (SFC) with chiral stationary phases (CSPs) is an advanced solution for the separation of achiral compounds in Piper kadsura. Analogues and stereoisomers are abundant in natural products, but there are obstacles in separation using conventional method. In this paper, four lignan diastereoisomers, (-)-Galbelgin, (-)-Ganschisandrin, Galgravin and (-)-Veraguensin, from Piper kadsura were separated and purified by chiral SFC. Purification strategy was designed, considering of the compound enrichment, sample purity and purification throughput. Two-step achiral purification method on chiral preparative columns with stacked automated injections was developed. Unconventional mobile phase modifier dichloromethane (DCM) was applied to improve the sample solubility. Four diastereoisomers was prepared at the respective weight of 103.1mg, 10.0mg, 152.3mg and 178.6mg from 710mg extract with the purity of greater than 98%.
[Mh] Termos MeSH primário: Cromatografia com Fluido Supercrítico/métodos
Piper/química
Extratos Vegetais/isolamento & purificação
[Mh] Termos MeSH secundário: Cromatografia com Fluido Supercrítico/instrumentação
Extratos Vegetais/química
Solubilidade
Estereoisomerismo
[Pt] Tipo de publicação:EVALUATION STUDIES; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Plant Extracts)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171016
[Lr] Data última revisão:
171016
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170624
[St] Status:MEDLINE


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[PMID]:28603121
[Au] Autor:Ahmed AS; Ahmed Q; Saxena AK; Jamal P
[Ad] Endereço:Department of Basic Medical Sciences, Kulliyyah of Medicine, International Islamic University Malaysia, Kuantan, Pahang Darul Makmur, Malaysia.
[Ti] Título:Evaluation of in vitro antidiabetic and antioxidant characterizations of Elettaria cardamomum (L.) Maton (Zingiberaceae), Piper cubeba L. f. (Piperaceae), and Plumeria rubra L. (Apocynaceae).
[So] Source:Pak J Pharm Sci;30(1):113-126, 2017 Jan.
[Is] ISSN:1011-601X
[Cp] País de publicação:Pakistan
[La] Idioma:eng
[Ab] Resumo:Inhibition of intestinal α-amylase and α-glucosidase is an important strategy to regulate diabetes mellitus (DM). Antioxidants from plants are widely regarded in the prevention of diabetes. Fruits of Elettaria cardamomum (L.) Maton (Zingiberaceae) and Piper cubeba L. f. (Piperaceae) and flowers of Plumeria rubra L. (Apocynaceae) are traditionally used to cure DM in different countries. However, the role of these plants has been grossly under reported and is yet to receive proper scientific evaluation with respect to understand their traditional role in the management of diabetes especially as digestive enzymes inhibitors. Hence, methanol and aqueous extracts of the aforementioned plants were evaluated for their in vitro α-glucosidase and α-amylase inhibition at 1 mg/mL and quantification of their antioxidant properties (DPPH, FRAP tests, total phenolic and total flavonoids contents). In vitro optimization studies for the extracts were also performed to enhance in vitro biological activities. The % inhibition of α-glucosidase by the aqueous extracts of the fruits of E. cardamomum, P. cubeba and flowers of P. rubra were 10.41 (0.03), 95.19 (0.01), and -2.92 (0.03), while the methanol extracts exhibited % inhibition 13.73 (0.02), 92.77 (0.01), and -0.98 (0.01), respectively. The % inhibition of α-amylase by the aqueous extracts were 82.99 (0.01), 64.35 (0.01), and 20.28 (0.02), while the methanol extracts displayed % inhibition 39.93 (0.01), 31.06 (0.02), and 39.40 (0.01), respectively. Aqueous extracts displayed good in vitro antidiabetic and antioxidant activities. Moreover, in vitro optimization experiments helped to increase the α-glucosidase inhibitory activity of E. cardamomum. Our findings further justify the traditional claims of these plants as folk medicines to manage diabetes, however, through digestive enzymes inhibition effect.
[Mh] Termos MeSH primário: Antioxidantes/farmacologia
Apocynaceae/química
Hipoglicemiantes/farmacologia
Lignanas/farmacologia
Piper/química
Extratos Vegetais/farmacologia
Zingiberaceae/química
[Mh] Termos MeSH secundário: Antioxidantes/química
Antioxidantes/isolamento & purificação
Compostos de Bifenilo/química
Cloretos/química
Compostos Férricos/química
Flores/química
Frutas/química
Inibidores de Glicosídeo Hidrolases/isolamento & purificação
Inibidores de Glicosídeo Hidrolases/farmacologia
Hipoglicemiantes/química
Hipoglicemiantes/isolamento & purificação
Lignanas/química
Lignanas/isolamento & purificação
Metanol/química
Oxirredução
Fitoterapia
Picratos/química
Extratos Vegetais/química
Extratos Vegetais/isolamento & purificação
Plantas Medicinais
Solventes/química
Água/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Biphenyl Compounds); 0 (Chlorides); 0 (Ferric Compounds); 0 (Glycoside Hydrolase Inhibitors); 0 (Hypoglycemic Agents); 0 (Lignans); 0 (Picrates); 0 (Piper cubeba extract); 0 (Plant Extracts); 0 (Solvents); 059QF0KO0R (Water); DFD3H4VGDH (1,1-diphenyl-2-picrylhydrazyl); U38V3ZVV3V (ferric chloride); Y4S76JWI15 (Methanol)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171103
[Lr] Data última revisão:
171103
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170613
[St] Status:MEDLINE


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[PMID]:28500884
[Au] Autor:Lee J; Kim J; Ok YS; Kwon EE
[Ad] Endereço:Department of Environment and Energy, Sejong University, Seoul 05006, Republic of Korea.
[Ti] Título:Rapid biodiesel synthesis from waste pepper seeds without lipid isolation step.
[So] Source:Bioresour Technol;239:17-20, 2017 Sep.
[Is] ISSN:1873-2976
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:In situ transformation of lipid in waste pepper seeds into biodiesel (i.e., fatty acid methyl esters: FAMEs) via thermally-induced transmethylation on silica was mainly investigated in this study. This study reported that waste pepper seeds contained 26.9wt% of lipid and that 94.1% of the total lipid in waste pepper seeds could be converted into biodiesel without lipid extraction step for only ∼1min reaction time. This study also suggested that the optimal temperature for in situ transmethylation was identified as 390°C. Moreover, comparison of in situ process via the conventional transmethylation catalyzed by H SO showed that the introduced biodiesel conversion in this study had a higher tolerance against impurities, thereby being technically feasible. The in situ biodiesel production from other oil-bearing food wastes can be studied.
[Mh] Termos MeSH primário: Biocombustíveis
Sementes
[Mh] Termos MeSH secundário: Ácidos Graxos
Lipídeos
Piper
Temperatura Ambiente
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biofuels); 0 (Fatty Acids); 0 (Lipids)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171118
[Lr] Data última revisão:
171118
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170514
[St] Status:MEDLINE


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[PMID]:28480386
[Au] Autor:Sanubol A; Chaveerach A; Tanee T; Sudmoon R
[Ad] Endereço:Department of Biology, Faculty of Science, Khon Kaen University, Thailand.
[Ti] Título:PRE-CLINICAL EVALUATION OF EXTRACTS AND ESSENTIAL OILS FROM BETEL-LIKE SCENT SPECIES IDENTIFIED POTENTIAL CANCER TREATMENT.
[So] Source:Afr J Tradit Complement Altern Med;14(1):89-102, 2017.
[Is] ISSN:2505-0044
[Cp] País de publicação:Nigeria
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Nine species with betel-like scents are sources of industrial and medicinal aromatic chemicals, but there is lack of information on cytotoxicity and genotoxicity for human safety, including how these plants impact human cervical cancer cell line. METHODS: Plant leaves were extracted with hexane and hydro-distilled for essential oils. The extracts and oils were pre-clinically studied based on cyto - and genotoxicity using microculture tetrazolium (MTT) and comet assays. RESULTS: The crude extracts showed an IC in leukocytes and HeLa cells of 58.59-97.31 mg/ml and 34.91-101.79 mg/ml, the LD is higher than 5000 mg/kg. With lower values than the crude extracts, the essential oils showed an IC in leukocytes and HeLa cells of 0.023-0.059 µg/ml and 0.025-0.043 µg/ml the LD is less than 50 mg/kg. IC values showed that the essential oils were highly toxic than the crude extracts. At the level of human genetic materials, the crude extracts of two species, including and , showed a significant toxicity ( < 0.05) in leukocytes. The other samples were non-toxic. The crude extracts of all samples showed significant genotoxicity in HeLa cells. The essential oils of all studied species showed insignificant toxicity in leukocytes. For HeLa cells, the eight-studied species showed significant toxicity in HeLa cells, whereas only showed insignificant toxicity. CONCLUSION: The crude extracts and essential oils should be tested as putative cervical cancer treatments due to less toxicity in human normal cells.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Óleos Voláteis/farmacologia
Piper/química
Óleos Vegetais/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Avaliação Pré-Clínica de Medicamentos
Seres Humanos
Neoplasias/tratamento farmacológico
Neoplasias/fisiopatologia
Óleos Voláteis/química
Piper/classificação
Extratos Vegetais/química
Extratos Vegetais/farmacologia
Folhas de Planta/química
Óleos Vegetais/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Oils, Volatile); 0 (Plant Extracts); 0 (Plant Oils)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170626
[Lr] Data última revisão:
170626
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170509
[St] Status:MEDLINE
[do] DOI:10.21010/ajtcam.v14i1.10


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[PMID]:28436658
[Au] Autor:Xiang CP; Han JX; Li XC; Li YH; Zhang Y; Chen L; Qu Y; Hao CY; Li HZ; Yang CR; Zhao SJ; Xu M
[Ad] Endereço:Center for Pharmaceutical Sciences, Faculty of Life Science and Technology, Kunming University of Science and Technology , Chenggong Campus, Kunming 650500, P. R. China.
[Ti] Título:Chemical Composition and Acetylcholinesterase Inhibitory Activity of Essential Oils from Piper Species.
[So] Source:J Agric Food Chem;65(18):3702-3710, 2017 May 10.
[Is] ISSN:1520-5118
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The essential oils (EOs) derived from aromatic plants such as Piper species are considered to play a role in alleviating neuronal ailments that are associated with inhibition of acetylcholinesterase (AChE). The chemical compositions of 23 EOs prepared from 16 Piper spp. were analyzed by both gas chromatography with a flame ionization detector (GC-FID) and gas chromatography-mass spectrometry (GC-MS). A total of 76 compounds were identified in the EOs from the leaves and stems of 19 samples, while 30 compounds were detected in the EOs from the fruits of four samples. Sesquiterpenes and phenylpropanoids were found to be rich in these EOs, of which asaricin, caryophyllene, caryophyllene oxide, isospathulenol, (+)-spathulenol, and ß-bisabolene are the major constituents. The EOs from the leaves and stems of Piper austrosinense, P. puberulum, P. flaviflorum, P. betle, and P. hispidimervium showed strong AChE inhibitory activity with IC values in the range of 1.51 to 13.9 mg/mL. A thin-layer chromatography (TLC) bioautography assay was employed to identify active compound(s) in the most active EO from P. hispidimervium. The active compound was isolated and identified as asaricin, which gave an IC value of 0.44 ± 0.02 mg/mL against AChE, comparable to galantamine with an IC 0.15 ± 0.01 mg/mL.
[Mh] Termos MeSH primário: Acetilcolinesterase/química
Inibidores da Colinesterase/química
Proteínas de Peixes/antagonistas & inibidores
Óleos Voláteis/química
Piper/química
Extratos Vegetais/química
[Mh] Termos MeSH secundário: Animais
Cromatografia em Camada Delgada
Enguias
Proteínas de Peixes/química
Cromatografia Gasosa-Espectrometria de Massas
Folhas de Planta/química
Óleos Vegetais/química
Caules de Planta/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cholinesterase Inhibitors); 0 (Fish Proteins); 0 (Oils, Volatile); 0 (Plant Extracts); 0 (Plant Oils); EC 3.1.1.7 (Acetylcholinesterase)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170608
[Lr] Data última revisão:
170608
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170425
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jafc.7b01350


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[PMID]:28371557
[Au] Autor:Varela MT; Lima ML; Galuppo MK; Tempone AG; de Oliveira A; Lago JHG; Fernandes JPS
[Ad] Endereço:Departamento de Ciências Farmacêuticas, Universidade Federal de São Paulo, Diadema, SP, Brazil.
[Ti] Título:New alkenyl derivative from Piper malacophyllum and analogues: Antiparasitic activity against Trypanosoma cruzi and Leishmania infantum.
[So] Source:Chem Biol Drug Des;90(5):1007-1011, 2017 Nov.
[Is] ISSN:1747-0285
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Alkylphenols isolated from Piper malacophyllum (Piperaceae), gibbilimbols A and B, showed interesting activity against the parasites Trypanosoma cruzi and Leishmania infantum. In continuation to our previous work, a new natural product from the essential oil of the leaves of P. malacophyllum was isolated, the 5-[(3E)-oct-3-en-1-il]-1,3-benzodioxole, and also a new set of five compounds was prepared. The antiparasitic activity of the natural product was evaluated in vitro against these parasites, indicating potential against the promastigote/trypomastigote/amastigote forms (IC 32-83 µm) of the parasites and low toxicity (CC  > 200 µm) to mammalian cells. The results obtained to the synthetic compounds indicated that the new derivatives maintained the promising antiparasitic activity, but the cytotoxicity was considerably lowered. The amine derivative LINS03011 displayed the most potent IC values (13.3 and 16.7 µm) against amastigotes of T. cruzi and L. infantum, respectively, indicating comparable activity to the phenolic prototype LINS03003, with threefold decreased (CC 73.5 µm) cytotoxicity, leading the selectivity index (SI) towards the parasites up to 24.5. In counterpart, LINS03011 has not shown membrane disruptor activity in SYTOX Green model. In summary, this new set showed the hydroxyl is not essential for the antiparasitic activity, and its substitution could decrease the toxicity to mammalian cells.
[Mh] Termos MeSH primário: Dioxóis/química
Dioxóis/farmacologia
Leishmania infantum/efeitos dos fármacos
Piper/química
Tripanossomicidas/química
Tripanossomicidas/farmacologia
Trypanosoma cruzi/efeitos dos fármacos
[Mh] Termos MeSH secundário: Doença de Chagas/tratamento farmacológico
Dioxóis/isolamento & purificação
Seres Humanos
Leishmaniose Visceral/tratamento farmacológico
Óleos Voláteis/química
Fenóis/química
Fenóis/farmacologia
Tripanossomicidas/isolamento & purificação
[Pt] Tipo de publicação:LETTER
[Nm] Nome de substância:
0 (Dioxoles); 0 (Oils, Volatile); 0 (Phenols); 0 (Trypanocidal Agents); 0 (gibbilimbol A); F0XLL582B8 (1,3-benzodioxole)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171113
[Lr] Data última revisão:
171113
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170404
[St] Status:MEDLINE
[do] DOI:10.1111/cbdd.12986



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