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Pesquisa : B01.650.940.800.575.912.250.583.520.051 [Categoria DeCS]
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  1 / 108 MEDLINE  
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[PMID]:28870197
[Au] Autor:Zahra SS; Ahmed M; Qasim M; Gul B; Zia M; Mirza B; Haq IU
[Ad] Endereço:Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, 45320, Pakistan.
[Ti] Título:Polarity based characterization of biologically active extracts of Ajuga bracteosa Wall. ex Benth. and RP-HPLC analysis.
[So] Source:BMC Complement Altern Med;17(1):443, 2017 Sep 05.
[Is] ISSN:1472-6882
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The concept of botanical therapeutics has revitalized due to wide importance of plant derived pharmaceuticals. Therefore, the ameliorative characteristics of Ajuga bracteosa were studied. METHODS: Total phenolic content, flavonoid content, antioxidant capacity, reducing power and free-radical scavenging activity were determined colorimetrically. Specific polyphenols were quantified by RP-HPLC analysis. Preliminary cytotoxicity was tested using brine shrimp lethality assay while antiproliferative activity against THP-1 and Hep-G2 cell lines was determined by MTT and SRB protocols respectively. Antileishmanial potential was assessed via MTT colorimetric method. To investigate antidiabetic prospect, α-amylase inhibition assay was adopted whereas disc diffusion method was used to detect likely protein kinase inhibitory, antibacterial and antifungal activities. RESULTS: Among fifteen different extracts, maximum total phenolic content (10.75 ± 0.70 µg GAE/mg DW), total reducing power (23.90 ± 0.70 µg AAE/mg DW) and total antioxidant capacity (11.30 ± 0.80 µg AAE/mg DW) were exhibited by methanol extract with superlative percent extract recovery (17.50 ± 0.80% w/w). Chloroform-methanol extract demonstrated maximum flavonoid content (4.10 ± 0.40 µg QE/mg DW) and ethanol extract exhibited greatest radical scavenging activity (IC 14.40 ± 0.20 µg/ml). RP-HPLC based quantification confirmed polyphenols such as pyrocatechol, gallic acid, resorcinol, catechin, chlorogenic acid, caffeic acid, syringic acid, p-coumaric acid, ferulic acid, vanillic acid, coumarin, sinapinic acid, trans-cinnamic acid, rutin, quercetin and kaempferol. The brine shrimp lethality assay ranked 78.60% extracts as cytotoxic (LC ≤ 250 µg/ml) whereas significant THP-1 inhibition was shown by methanol-acetone extract (IC 4.70 ± 0.43 µg/ml). The antiproliferative activity against Hep-G2 hepatoma cancer cell line was demonstrated by n-hexane, ethylacetate and methanol-distilled water (IC 8.65-8.95 µg/ml) extracts. Methanol extract displayed prominent protein kinase inhibitory activity (MIC 12.5 µg/disc) while n-hexane extract revealed remarkable antileishmanial activity (IC 4.69 ± 0.01 µg/ml). The antidiabetic potential was confirmed by n-hexane extract (44.70 ± 0.30% α-amylase inhibition at 200 µg/ml concentration) while a moderate antibacterial and antifungal activities were unveiled. CONCLUSION: The variation in biological spectrum resulted due to use of multiple solvent systems for extraction. We also deduce that the valuable information gathered can be utilized for discovery of anticancer, antileishmanial, antioxidant and antidiabetic bioactive lead candidates.
[Mh] Termos MeSH primário: Ajuga/química
Extratos Vegetais/análise
Extratos Vegetais/farmacologia
[Mh] Termos MeSH secundário: Animais
Antioxidantes/análise
Antioxidantes/farmacologia
Artemia
Linhagem Celular
Sobrevivência Celular/efeitos dos fármacos
Cromatografia Líquida de Alta Pressão
Inibidores Enzimáticos/análise
Inibidores Enzimáticos/farmacologia
Flavonoides/análise
Flavonoides/farmacologia
Seres Humanos
Fenóis/análise
Fenóis/farmacologia
alfa-Amilases/antagonistas & inibidores
alfa-Amilases/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Enzyme Inhibitors); 0 (Flavonoids); 0 (Phenols); 0 (Plant Extracts); EC 3.2.1.1 (alpha-Amylases)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170908
[Lr] Data última revisão:
170908
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170906
[St] Status:MEDLINE
[do] DOI:10.1186/s12906-017-1951-5


  2 / 108 MEDLINE  
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[PMID]:28086782
[Au] Autor:Nardos A; Makonnen E
[Ad] Endereço:Pharmacology Unit, School of Medicine, Hawassa University, P O Box 1560, Hawassa, Ethiopia. nant07@yahoo.com.
[Ti] Título:In vivo antiplasmodial activity and toxicological assessment of hydroethanolic crude extract of Ajuga remota.
[So] Source:Malar J;16(1):25, 2017 Jan 13.
[Is] ISSN:1475-2875
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Malaria is one of the most life-threatening health problems worldwide and treatment has been compromised by drug resistance. Identifying lead molecules from natural products might help to find better anti-malarial drugs, since those obtained from natural sources are still effective against malarial parasites. This study aimed at investigating the in vivo antiplasmodial activity of crude extract of the leaves of Ajuga remota together with its safety in mice models. METHODS: In vivo parasite growth inhibitory effect of crude extract was assessed in mice inoculated with Plasmodium berghei (ANKA strain). The in vivo antiplasmodial activity of the test extract was performed against early infection (4-day suppressive test), curative effect against established infection and prophylactic effect against residual infection. Acute and sub-acute toxicity were carried out according to OECD guidelines. RESULTS: In vivo parasite growth inhibition effect of hydroethanolic crude extract of A. remota was evaluated at 30, 50 and 100 mg/kg dose levels. It suppressed parasitaemia by 77.34% at 100 mg/kg dose level in the 4-day test. In curative and prophylactic potential tests, it suppressed parasitaemia by 66.67 and 59.66% at 100 mg/kg dose level, respectively. In vivo toxicity tests revealed no toxicity. All parasitaemia suppressions were statistically significant at P < 0.05 as compared to the vehicle-treated group. The crude extract also prolonged survival time in a dose dependent manner. CONCLUSIONS: The investigation results suggest that the leave extract of Ajuga remota possesses antimalarial activity.
[Mh] Termos MeSH primário: Ajuga/química
Antiprotozoários/administração & dosagem
Misturas Complexas/administração & dosagem
Malária/tratamento farmacológico
Extratos Vegetais/administração & dosagem
Plasmodium berghei/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Antiprotozoários/isolamento & purificação
Antiprotozoários/farmacologia
Misturas Complexas/isolamento & purificação
Misturas Complexas/farmacologia
Modelos Animais de Doenças
Feminino
Malária/parasitologia
Malária/prevenção & controle
Camundongos
Extratos Vegetais/isolamento & purificação
Extratos Vegetais/farmacologia
Análise de Sobrevida
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antiprotozoal Agents); 0 (Complex Mixtures); 0 (Plant Extracts)
[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:170115
[St] Status:MEDLINE
[do] DOI:10.1186/s12936-017-1677-3


  3 / 108 MEDLINE  
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[PMID]:28012983
[Au] Autor:Ganaie HA; Ali MN; Ganai BA; Meraj M; Ahmad M
[Ad] Endereço:Cytogenetics & Molecular Biology Research Laboratory, Centre of Research for Development, University of Kashmir, Srinagar, 190 006, J & K, India; Phytochemistry Research Laboratory, Centre of Research for Development, University of Kashmir, Srinagar, 190 006, J & K, India.
[Ti] Título:Antibacterial activity of 14, 15-dihydroajugapitin and 8-o-acetylharpagide isolated from Ajuga bracteosa Wall ex. Benth against human pathogenic bacteria.
[So] Source:Microb Pathog;103:114-118, 2017 Feb.
[Is] ISSN:1096-1208
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Ajuga bracteosa Wall ex. Benth. (Lamiaceae) commonly known as Bungle Weed has been in use since ancient times and is mentioned Ayurvedic literature. The upper ground parts of the plant are used for treatment of various diseases. The weed is credited with astringent, febrifugal, stimulant, aperient, tonic, diuretic and depurative properties and is used for the treatment of gout and rheumatism, palsy and amenorrhoea. Two compounds 1) 14, 15-dihydroajugapitin and 2) 8-o-acetylharpagide were isolated from the aerial parts of the plant and tested for antibacterial activity against various pathogenic bacteria by agar well diffusion method. Compound 1 and 2 showed maximum antibacterial activity against Escherichia coli with zone of inhibitions of 25. 0 ± 1.4 mm and 22.6 ± 0.9 mm respectively. The MIC value of compound 1 and 2 ranged between 500 and 1000 µg/ml. It could be concluded that both compounds isolated from the aerial parts of Ajuga bracteosa possess antibacterial activity against pathogens.
[Mh] Termos MeSH primário: Ajuga/química
Antibacterianos/farmacologia
Bactérias/efeitos dos fármacos
Extratos Vegetais/farmacologia
Piranos/farmacologia
[Mh] Termos MeSH secundário: Antibacterianos/química
Antibacterianos/isolamento & purificação
Seres Humanos
Testes de Sensibilidade Microbiana
Compostos Fitoquímicos/química
Extratos Vegetais/química
Extratos Vegetais/isolamento & purificação
Piranos/química
Piranos/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Phytochemicals); 0 (Plant Extracts); 0 (Pyrans); 6926-14-3 (8-O-acetylharpagide)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170406
[Lr] Data última revisão:
170406
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161226
[St] Status:MEDLINE


  4 / 108 MEDLINE  
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[PMID]:27653644
[Au] Autor:Karami A
[Ad] Endereço:a Department of Horticultural Science, School of Agriculture , Shiraz University , Shiraz , Iran.
[Ti] Título:Essential oil composition of Ajuga comata Stapf. from Southern Zagros, Iran.
[So] Source:Nat Prod Res;31(3):359-361, 2017 Feb.
[Is] ISSN:1478-6427
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The chemical composition of essential oil obtained from the aerial parts of Ajuga comata Stapf. was analyzed by GC and GC/MS. Thirty-seven components were identified in the oil. (E)-ß-caryophyllene (30.9%), caryophyllene oxide (24.9%), (E)-ß-farnesene (12.6%), ß-eudesmol (3.2%), δ-cadinene (3.1%) and germacrene D (3.0%) were the main compounds in the EOs. The chemical composition of A. comata Stapf. from the Southern Zagros of Iran is reported for the first time.
[Mh] Termos MeSH primário: Ajuga/química
Óleos Voláteis/análise
[Mh] Termos MeSH secundário: Cromatografia Gasosa-Espectrometria de Massas
Irã (Geográfico)
Óleos Voláteis/química
Sesquiterpenos/análise
Sesquiterpenos/química
Sesquiterpenos de Eudesmano/análise
Sesquiterpenos de Germacrano/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Oils, Volatile); 0 (Sesquiterpenes); 0 (Sesquiterpenes, Eudesmane); 0 (Sesquiterpenes, Germacrane); 0 (delta-cadinene); 18794-84-8 (beta-farnesene); 473-15-4 (beta-eudesmol); BHW853AU9H (caryophyllene); S2XU9K448U (caryophyllene oxide); V2I9ATG34E (germacrene D)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160923
[St] Status:MEDLINE


  5 / 108 MEDLINE  
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[PMID]:27492580
[Au] Autor:Frezza C; Venditti A; Di Cecco M; Ciaschetti G; Serafini M; Bianco A
[Ad] Endereço:b Dipartimento di Biologia Ambientale , Università di Roma 'La Sapienza' , Roma , Italy.
[Ti] Título:Iridoids and phenylethanoid glycosides from the aerial parts of Ajuga tenorei, an endemic Italian species.
[So] Source:Nat Prod Res;31(2):218-223, 2017 Jan.
[Is] ISSN:1478-6427
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:We report the first analysis in absolute, and in particular, concerning the phytochemical pattern, about an endemic Italian species, Ajuga tenorei C. Presl. The analysis, performed by means of techniques such as Column Chromatography and NMR spectroscopy and Mass spectrometry, led to the isolation and the identification of five compounds namely verbascoside (1), echinacoside (2), ajugoside (3), harpagide (4) and 8-O-acetylharpagide (5). The presence of these compounds is important from both chemotaxonomic and ethno-pharmacological point of view. For what concerns the first point is confirmed the correct botanical classification of the species. The isolated compounds are also known to exert peculiar pharmacological activities and their presence may give a rationale to the historical medicinal properties associated to the Ajuga genus in general, since these plants have a long traditional use in many parts of the world. Such fact might suggest the use of also this species in this sense.
[Mh] Termos MeSH primário: Ajuga/química
Glicosídeos/isolamento & purificação
Iridoides/isolamento & purificação
[Mh] Termos MeSH secundário: Glucosídeos/isolamento & purificação
Glicosídeos/química
Glicosídeos Iridoides/isolamento & purificação
Iridoides/química
Itália
Espectrometria de Massas
Fenóis/isolamento & purificação
Componentes Aéreos da Planta/química
Extratos Vegetais/química
Plantas Medicinais/química
Piranos/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Glucosides); 0 (Glycosides); 0 (Iridoid Glycosides); 0 (Iridoids); 0 (Phenols); 0 (Plant Extracts); 0 (Pyrans); 3TGX09BD5B (acteoside); 52916-96-8 (ajugoside); 6926-14-3 (8-O-acetylharpagide); I04O1DT48T (echinacoside); OF59XHX7SR (harpagide)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160806
[St] Status:MEDLINE


  6 / 108 MEDLINE  
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[PMID]:27396203
[Au] Autor:Fan GX; Zhi DJ; Ren H; Li ZY; Hu QL; Liu YH; Zhang ZX; Fei DQ
[Ti] Título:A New Succinate Derivative from Ajuga decumbens.
[So] Source:Nat Prod Commun;11(4):497-8, 2016 Apr.
[Is] ISSN:1934-578X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A new succinate derivative, ethyl (5-formylfuran-2-yl)methyl succinate (1), along with three known compounds (2-4) have been isolated from the whole plants of Ajuga decumbens Thunb. Their structures were elucidated by extensive spectroscopic (1D and 2D NMR) and HR-ESI-MS data analysis, and literature values. Compound 1 was isolated as a new succinate derivative, and compounds 2 and 3 were for the first time separated from A. decumbens.
[Mh] Termos MeSH primário: Ajuga/química
Succinatos/isolamento & purificação
[Mh] Termos MeSH secundário: Testes de Sensibilidade Microbiana
Estrutura Molecular
Fitol/isolamento & purificação
Succinatos/química
Ácido Vanílico/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Succinates); 0 (ethyl (5-formylfuran-2-yl)methylsuccinate); 150-86-7 (Phytol); GM8Q3JM2Y8 (Vanillic Acid)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:160711
[Lr] Data última revisão:
160711
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160712
[St] Status:MEDLINE


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[PMID]:27373875
[Au] Autor:Venditti A; Frezza C; Maggi F; Lupidi G; Bramucci M; Quassinti L; Giuliani C; Cianfaglione K; Papa F; Serafini M; Bianco A
[Ad] Endereço:Dipartimento di Chimica, Università di Roma "La Sapienza", Rome, Italy; Dipartimento di Biologia Ambientale, Università di Roma "La Sapienza", Rome, Italy. Electronic address: alessandro.venditti@uniroma1.it.
[Ti] Título:Phytochemistry, micromorphology and bioactivities of Ajuga chamaepitys (L.) Schreb. (Lamiaceae, Ajugoideae): Two new harpagide derivatives and an unusual iridoid glycosides pattern.
[So] Source:Fitoterapia;113:35-43, 2016 Sep.
[Is] ISSN:1873-6971
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Ajuga chamaepitys (L.) Schreb, well-known as Camaepitium or Ground Pine, is an annual herb typical of the Mediterranean area accounting several uses in the traditional medicine. In this work we have, analyzed the plant iridoid fraction together with the essential oil composition and study of the plant indumentum. Finally, we assayed the polar extracts and essential oil obtained from the aerial parts for antioxidant activity and cytotoxicity on tumor cells. The analysis of the monoterpene glycosides allowed us to isolate from roots and aerial parts and to structurally elucidate by NMR and MS the following compounds: ajugoside (1), reptoside (2), 8-O-acetylharpagide (3), harpagide (4), 5-O-ß-d-glucopyranosyl-harpagide (5), asperulosidic acid (6), deacetyl asperulosidic acid (7) and 5-O-ß-d-glucopyranosyl-8-O-acetylharpagide (8), among which 5 and 8 were two new natural products. Chemotaxomic relevance of these constituents was discussed. The chemical analysis of A. chamaepitys essential oil by GC-FID and GC-MS showed ethyl linoleate (13.7%), germacrene D (13.4%), kaurene (8.4%), ß-pinene (6.8%), and (E)-phytol (5.3%) as the major volatile components. The micromorphological and histochemical study showed that iridoids and essential oil are mainly produced in the type III capitates and peltate trichomes of leaves and flowers. Biological evaluations of A. chamaepitys polar extracts and essential oil showed that the former were more potent as radical scavengers than the latter. MTT assay revealed that essential oil and ethanolic extracts were moderately cytotoxic on tumor cells with IC50 of 36.88 and 59.24µg/mL on MDA-MB 231 cell line, respectively, and IC50 of 60.48 and 64.12µg/mL on HCT116, respectively.
[Mh] Termos MeSH primário: Ajuga/química
Glicosídeos Iridoides/química
Óleos Voláteis/química
Óleos Vegetais/química
Piranos/química
[Mh] Termos MeSH secundário: Antineoplásicos Fitogênicos/química
Antineoplásicos Fitogênicos/isolamento & purificação
Linhagem Celular Tumoral
Depuradores de Radicais Livres/química
Depuradores de Radicais Livres/isolamento & purificação
Seres Humanos
Glicosídeos Iridoides/isolamento & purificação
Extratos Vegetais/química
Piranos/isolamento & purificação
Tricomas/química
Compostos Orgânicos Voláteis/química
Compostos Orgânicos Voláteis/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents, Phytogenic); 0 (Free Radical Scavengers); 0 (Iridoid Glycosides); 0 (Oils, Volatile); 0 (Plant Extracts); 0 (Plant Oils); 0 (Pyrans); 0 (Volatile Organic Compounds); OF59XHX7SR (harpagide)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170131
[Lr] Data última revisão:
170131
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160705
[St] Status:MEDLINE


  8 / 108 MEDLINE  
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[PMID]:27017303
[Au] Autor:Tsukagoshi Y; Ohyama K; Seki H; Akashi T; Muranaka T; Suzuki H; Fujimoto Y
[Ad] Endereço:Department of Chemistry and Materials Science, Tokyo Institute of Technology, O-okayama, Meguro, Tokyo 152-8551, Japan.
[Ti] Título:Functional characterization of CYP71D443, a cytochrome P450 catalyzing C-22 hydroxylation in the 20-hydroxyecdysone biosynthesis of Ajuga hairy roots.
[So] Source:Phytochemistry;127:23-8, 2016 Jul.
[Is] ISSN:1873-3700
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:20-Hydroxyecdysone (20HE), a molting hormone of insects, is also distributed among a variety of plant families. 20HE is thought to play a role in protecting plants from insect herbivores. In insects, biosynthesis of 20HE from cholesterol proceeds via 7-dehydrocholesterol and 3ß,14α-dihydroxy-5ß-cholest-7-en-6-one (5ß-ketodiol), the latter being converted to 20HE through sequential hydroxylation catalyzed by four P450 enzymes, which have been cloned and identified. In contrast, little is known about plant 20HE biosynthesis, and no biosynthetic 20HE gene has been reported thus far. We recently proposed involvement of 3ß-hydroxy-5ß-cholestan-6-one (5ß-ketone) in 20HE biosynthesis in the hairy roots of Ajuga reptans var. atropurpurea (Lamiaceae). In this study, an Ajuga EST library was generated from the hairy roots and P450 genes were deduced from the library. Five genes with a high expression level (CYP71D443, CYP76AH19, CYP76AH20, CYP76AH21 and CYP716D27) were screened for a possible involvement in 20HE biosynthesis. As a result, CYP71D443 was shown to have C-22 hydroxylation activity for the 5ß-ketone substrate using a yeast expression system. The hydroxylated product, 22-hydroxy-5ß-ketone, had a 22R configuration in agreement with that of 20HE. Furthermore, labeling experiments indicated that (22R)-22-hydroxy-5ß-ketone was converted to 20HE in Ajuga hairy roots. Based on the present results, a possible 20HE biosynthetic pathway in Ajuga plants involved CYP71D443 is proposed.
[Mh] Termos MeSH primário: Ajuga/química
Sistema Enzimático do Citocromo P-450/metabolismo
Ecdisterona/biossíntese
Ecdisterona/metabolismo
Lamiaceae/química
[Mh] Termos MeSH secundário: Ajuga/genética
Colestanonas/metabolismo
Colesterol/química
Citocromo P-450 CYP1A1/metabolismo
Sistema Enzimático do Citocromo P-450/genética
Desidrocolesteróis/metabolismo
Ecdisteroides/química
Lamiaceae/metabolismo
Estrutura Molecular
Raízes de Plantas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (3beta-hydroxy-5beta-cholestan-6-one); 0 (Cholestanones); 0 (Dehydrocholesterols); 0 (Ecdysteroids); 5289-74-7 (Ecdysterone); 9035-51-2 (Cytochrome P-450 Enzyme System); 97C5T2UQ7J (Cholesterol); BK1IU07GKF (7-dehydrocholesterol); EC 1.14.14.1 (CYP1A1 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP1A1)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170213
[Lr] Data última revisão:
170213
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160328
[St] Status:MEDLINE


  9 / 108 MEDLINE  
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[PMID]:26872973
[Au] Autor:Tsukagoshi Y; Suzuki H; Seki H; Muranaka T; Ohyama K; Fujimoto Y
[Ad] Endereço:From the Department of Chemistry and Materials Science, Tokyo Institute of Technology, O-okayama, Meguro-ku, Tokyo 152-8551, Japan.
[Ti] Título:Ajuga Δ24-Sterol Reductase Catalyzes the Direct Reductive Conversion of 24-Methylenecholesterol to Campesterol.
[So] Source:J Biol Chem;291(15):8189-98, 2016 Apr 08.
[Is] ISSN:1083-351X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Dimunito/Dwarf1 (DWF1) is an oxidoreductase enzyme that is responsible for the conversion of C28- and C29-Δ(24(28))-olefinic sterols to 24-methyl- and 24-ethylcholesterols. Generally, the reaction proceeds in two steps via the Δ(24(25))intermediate. In this study, we characterized theArDWF1gene from an expression sequence tag library ofAjuga reptansvar.atropurpureahairy roots. The gene was functionally expressed in the yeast T21 strain. Thein vivoandin vitrostudy of the transformed yeast indicated that ArDWF1 catalyzes the conversion of 24-methylenecholesterol to campesterol. A labeling study followed by GC-MS analysis suggested that the reaction proceeded with retention of the C-25 hydrogen. The 25-H retention was established by the incubation of the enzyme with (23,23,25-(2)H3,28-(13)C)-24-methylenecholesterol, followed by(13)C NMR analysis of the resulting campesterol. Thus, it has been concluded that ArDWF1 directly reduces 24-methylenecholesterol to produce campesterol without passing through a Δ(24(25))intermediate. This is the first characterization of such a unique DWF1 enzyme. For comparison purposes,Oryza sativa DWF1(OsDWF1) was similarly expressed in yeast. Anin vivoassay of OsDWF1 supported the generally accepted two-step mechanism because the C-25 hydrogen of 24-methylenecholesterol was eliminated during its conversion to 24-methylcholesterol. As expected, the 24-methylcholesterol produced by OsDWF1 was a mixture of campesterol and dihydrobrassicasterol. Furthermore, the 24-methylcholesterol contained in theAjugahairy roots was determined to be solely campesterol through its analysis using chiral GC-MS. Therefore, ArDWF1 has another unique property in that only campesterol is formed by the direct reduction catalyzed by the enzyme.
[Mh] Termos MeSH primário: Ajuga/metabolismo
Colesterol/análogos & derivados
Oxirredutases/metabolismo
Fitosteróis/metabolismo
Proteínas de Plantas/metabolismo
[Mh] Termos MeSH secundário: Ajuga/química
Ajuga/genética
Sequência de Aminoácidos
Colesterol/análise
Colesterol/genética
Colesterol/metabolismo
Dados de Sequência Molecular
Oxirredutases/química
Filogenia
Fitosteróis/análise
Fitosteróis/genética
Proteínas de Plantas/química
Proteínas de Plantas/genética
Alinhamento de Sequência
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Phytosterols); 0 (Plant Proteins); 5L5O665639 (campesterol); 97C5T2UQ7J (Cholesterol); EC 1.- (Oxidoreductases); SJ0718OYKX (24-methylenecholesterol)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:170408
[Lr] Data última revisão:
170408
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160214
[St] Status:MEDLINE
[do] DOI:10.1074/jbc.M115.703470


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[PMID]:26734766
[Au] Autor:Atay I; Kirmizibekmez H; Kaiser M; Akaydin G; Yesilada E; Tasdemir D
[Ad] Endereço:a Department of Pharmacognosy , School of Pharmacy, Istanbul Medipol University , Istanbul , 34810 , Turkey ;
[Ti] Título:Evaluation of in vitro antiprotozoal activity of Ajuga laxmannii and its secondary metabolites.
[So] Source:Pharm Biol;54(9):1808-14, 2016 Sep.
[Is] ISSN:1744-5116
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Context Some Ajuga L. (Lamiaceae) species are traditionally used for the treatment of malaria, as well as fever, which is a common symptom of many parasitic diseases. Objective In the continuation of our studies on the identification of antiprotozoal secondary metabolites of Turkish Lamiaceae species, we have investigated the aerial parts of Ajuga laxmannii. Materials and methods The aerial parts of A. laxmannii were extracted with MeOH. The H2O subextract was subjected to polyamide, C18-MPLC and SiO2 CCs to yield eight metabolites. The structures of the isolates were elucidated by NMR spectroscopy and MS analyses. The extract, subextracts as well as the isolates were tested for their in vitro antiprotozoal activities against Plasmodium falciparum, Trypanasoma brucei rhodesiense, T. cruzi and Leishmania donovani at concentrations of 90-0.123 µg/mL. Results Two iridoid glycosides harpagide (1) and 8-O-acetylharpagide (2), three o-coumaric acid derivatives cis-melilotoside (3), trans-melilotoside (4) and dihydromelilotoside (5), two phenylethanoid glycosides verbascoside (6) and galactosylmartynoside (7) and a flavone-C-glycoside, isoorientin (8) were isolated. Many compounds showed moderate to good antiparasitic activity, with isoorientin (8) displaying the most significant antimalarial potential (an IC50 value of 9.7 µg/mL). Discussion and conclusion This is the first report on the antiprotozoal evaluation of A. laxmannii extracts and isolates. Furthermore, isoorientin and dihydromelilotoside are being reported for the first time from the genus Ajuga.
[Mh] Termos MeSH primário: Ajuga
Antiprotozoários/farmacologia
Extratos Vegetais/farmacologia
[Mh] Termos MeSH secundário: Ajuga/metabolismo
Animais
Antiprotozoários/isolamento & purificação
Linhagem Celular
Seres Humanos
Leishmania donovani/efeitos dos fármacos
Leishmania donovani/crescimento & desenvolvimento
Estrutura Molecular
Testes de Sensibilidade Parasitária
Fitoterapia
Componentes Aéreos da Planta
Extratos Vegetais/isolamento & purificação
Plantas Medicinais
Plasmodium falciparum/efeitos dos fármacos
Plasmodium falciparum/crescimento & desenvolvimento
Ratos
Trypanosoma brucei rhodesiense/efeitos dos fármacos
Trypanosoma brucei rhodesiense/crescimento & desenvolvimento
Trypanosoma cruzi/efeitos dos fármacos
Trypanosoma cruzi/crescimento & desenvolvimento
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antiprotozoal Agents); 0 (Plant Extracts)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170213
[Lr] Data última revisão:
170213
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160107
[St] Status:MEDLINE
[do] DOI:10.3109/13880209.2015.1129542



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