Base de dados : MEDLINE
Pesquisa : B01.650.940.800.575.912.250.859.937.750 [Categoria DeCS]
Referências encontradas : 236 [refinar]
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  1 / 236 MEDLINE  
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[PMID]:28843845
[Au] Autor:Singh R; Kumar V; Bharate SS; Vishwakarma RA
[Ad] Endereço:Preformulation Laboratory, PK-PD, Toxicology and Formulation Division, CSIR-Indian Institute of Integrative Medicine, Canal Road, Jammu 180001, India; Academy of Scientific and Innovative Research (AcSIR), CSIR-Indian Institute of Integrative Medicine, Canal Road, Jammu 180001, India.
[Ti] Título:Synthesis, pH dependent, plasma and enzymatic stability of bergenin prodrugs for potential use against rheumatoid arthritis.
[So] Source:Bioorg Med Chem;25(20):5513-5521, 2017 Oct 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Bergenin is a unique C-glycoside natural product possessing anti-inflammatory and anti-arthritic activity. It is hydrophilic molecule and stable under acidic conditions however is unstable at neutral-basic pH conditions. The rate of degradation is directly proportional to the increase in pH which might be one of the reasons for its low oral bioavailability. Thus, herein our objective was to improve its stability using prodrug strategy. Various ester and ether prodrugs were synthesized and studied for lipophilicity, chemical stability and enzymatic hydrolysis in plasma/esterase. The stability of synthesized prodrugs was evaluated in buffers at different pH, in biorelevant media such as SGF, SIF, rat plasma and in esterase enzyme. All prodrugs displayed significantly improved lipophilicity compared with bergenin, which was in accordance with the criteria of drug-like compounds. Acetyl ester 4a appeared to be the most promising prodrug as it remained stable at gastric/intestinal pH and was completely transformed to the parent compound bergenin in plasma as desired for an ideal prodrug. The data presented herein, will help in designing stable prodrugs of unstable molecules with desired physicochemical properties in structurally similar chemotypes.
[Mh] Termos MeSH primário: Artrite Reumatoide/tratamento farmacológico
Benzopiranos/farmacologia
Esterases/metabolismo
Pró-Fármacos/farmacologia
Saxifragaceae/química
[Mh] Termos MeSH secundário: Animais
Benzopiranos/síntese química
Benzopiranos/metabolismo
Concentração de Íons de Hidrogênio
Fígado/enzimologia
Conformação Molecular
Pró-Fármacos/síntese química
Pró-Fármacos/metabolismo
Ratos
Suínos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzopyrans); 0 (Prodrugs); EC 3.1.- (Esterases); L84RBE4IDC (bergenin)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171108
[Lr] Data última revisão:
171108
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170828
[St] Status:MEDLINE


  2 / 236 MEDLINE  
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[PMID]:28832147
[Au] Autor:Badral D; Odonbayar B; Murata T; Munkhjargal T; Tuvshintulga B; Igarashi I; Suganuma K; Inoue N; Brantner AH; Odontuya G; Sasaki K; Batkhuu J
[Ad] Endereço:School of Engineering and Applied Sciences, National University of Mongolia , Ulaanbaatar 14201, Mongolia.
[Ti] Título:Flavonoid and Galloyl Glycosides Isolated from Saxifraga spinulosa and Their Antioxidative and Inhibitory Activities against Species That Cause Piroplasmosis.
[So] Source:J Nat Prod;80(9):2416-2423, 2017 Sep 22.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Eight new flavonoid-based 3'-O-ß-d-glucopyranosides (1-8) and three new galloyl glucosides (9, 11, 12), were isolated from the aerial parts of Saxifraga spinulosa, along with 25 known compounds. The structures of the new compounds were elucidated by spectroscopic methods. Most of the isolated compounds exhibited potent DPPH radical-scavenging activities. Further, their inhibitory activities were evaluated against Babesia bovis, Babesia bigemina, Babesia caballi, and Theileria equi, protozoan parasites that cause piroplasmosis in livestock. The results indicated that several of these compounds showed growth-inhibitory effects on such organisms that cause piroplasmosis.
[Mh] Termos MeSH primário: Antioxidantes/farmacologia
Babesia/química
Flavonoides/farmacologia
Glicosídeos/farmacologia
Saxifragaceae/química
Theileria/química
[Mh] Termos MeSH secundário: Animais
Antioxidantes/química
Flavonoides/química
Glicosídeos/química
Estrutura Molecular
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Flavonoids); 0 (Glycosides)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170824
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jnatprod.7b00142


  3 / 236 MEDLINE  
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[PMID]:28749965
[Au] Autor:Pandey R; Kumar B; Meena B; Srivastava M; Mishra T; Tiwari V; Pal M; Nair NK; Upreti DK; Rana TS
[Ad] Endereço:Sophisticated Analytical Instrument Facility, CSIR-Central Drug Research Institute, Lucknow, India.
[Ti] Título:Major bioactive phenolics in Bergenia species from the Indian Himalayan region: Method development, validation and quantitative estimation using UHPLC-QqQLIT-MS/MS.
[So] Source:PLoS One;12(7):e0180950, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Bergenia species are important medicinal plants used in indigenous systems of medicine for their antilithiatic and diuretic properties. An ultra-high performance liquid chromatography coupled to hybrid linear ion trap triple quadrupole mass spectrometry (UHPLC-QqQLIT-MS/MS) method has been developed and validated for the estimation of quantitative variation of eight major bioactive phenolics in the rhizomes (150 samples) of four species of this herb, Bergenia (B. ciliata, B. ligulata, B. purpurascens and B. stracheyi). Chromatographic separation was obtained on a Waters ACQUITY UPLCTM BEH (ethylene bridged hybrid) C18 column with a mobile phase consisting of 0.1% (v/v) formic acid aqueous solution and acetonitrile under a gradient elution manner. A hybrid linear ion trap triple quadrupole mass spectrometer was operated in negative electrospray ionization mode with multiple reactions monitoring for detection and quantification of the eight compounds. The validated method demonstrated good linearity (r2 ≥ 0.9991), precision (RSD ≤ 1.87%) and accuracy (95.16-102.11%, RSD ≤ 1.83%) for all reference analytes. The quantitative results revealed that B. ligulata contains the highest amount of the major active marker-bergenin. The results also suggest that sensitive UHPLC-QqQLIT-MS/MS method, a sensitive, accurate and convenient one, could be helpful in identification of potential accession(s), rapid quality control and establishing authenticity of Bergenia species as raw material for pharmaceutical industries.
[Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/métodos
Fenóis/análise
Saxifragaceae/química
Espectrometria de Massas em Tandem/métodos
[Mh] Termos MeSH secundário: Índia
Análise de Componente Principal
Padrões de Referência
Reprodutibilidade dos Testes
Especificidade da Espécie
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Phenols)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170929
[Lr] Data última revisão:
170929
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170728
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0180950


  4 / 236 MEDLINE  
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[PMID]:28562649
[Au] Autor:Jin Y; Wang Y; Zhang D; Shen X; Liu W; Chen F
[Ad] Endereço:Biotechnology Research Center, China Three Gorges University, Yichang, Hubei Province, P. R. China.
[Ti] Título:Floral organ MADS-box genes in Cercidiphyllum japonicum (Cercidiphyllaceae): Implications for systematic evolution and bracts definition.
[So] Source:PLoS One;12(5):e0178382, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The dioecious relic Cercidiphyllum japonicum is one of two species of the sole genus Cercidiphyllum, with a tight inflorescence lacking an apparent perianth structure. In addition, its systematic place has been much debated and, so far researches have mainly focused on its morphology and chloroplast genes. In our investigation, we identified 10 floral organ identity genes, including four A-class, three B-class, two C-class and one D-class. Phylogenetic analyses showed that all ten genes are grouped with Saxifragales plants, which confirmed the phylogenetic place of C. japonicum. Expression patterns of those genes were examined by quantitative reverse transcriptase PCR, with some variations that did not completely coincide with the ABCDE model, suggesting some subfunctionalization. As well, our research supported the idea that thebract actually is perianth according to our morphological and molecular analyses in Cercidiphyllum japonicum.
[Mh] Termos MeSH primário: Evolução Molecular
Genes de Plantas
Proteínas de Domínio MADS/fisiologia
Saxifragaceae/genética
[Mh] Termos MeSH secundário: Proteínas de Domínio MADS/genética
Filogenia
Saxifragaceae/classificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (MADS Domain Proteins)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170921
[Lr] Data última revisão:
170921
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170601
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0178382


  5 / 236 MEDLINE  
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[PMID]:28545386
[Au] Autor:Ebersbach J; Schnitzler J; Favre A; Muellner-Riehl AN
[Ad] Endereço:Department of Molecular Evolution and Plant Systematics & Herbarium (LZ), Institute of Biology, Leipzig University, Johannisallee 21-23, D-04103, Leipzig, Germany. ebersbach.jana@gmail.com.
[Ti] Título:Evolutionary radiations in the species-rich mountain genus Saxifraga L.
[So] Source:BMC Evol Biol;17(1):119, 2017 May 25.
[Is] ISSN:1471-2148
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: A large number of taxa have undergone evolutionary radiations in mountainous areas, rendering alpine systems particularly suitable to study the extrinsic and intrinsic factors that have shaped diversification patterns in plants. The species-rich genus Saxifraga L. is widely distributed throughout the Northern Hemisphere, with high species numbers in the regions adjacent to the Qinghai-Tibet Plateau (QTP) in particular the Hengduan Mountains and the Himalayas. Using a dataset of 297 taxa (representing at least 60% of extant Saxifraga species), we explored the variation of infrageneric diversification rates. In addition, we used state-dependent speciation and extinction models to test the effects of geographic distribution in the Hengduan Mountains and the entire QTP region as well as of two morphological traits (cushion habit and specialized lime-secreting glands, so-called hydathodes) on the diversification of this genus. RESULTS: We detected two to three rate shifts across the Saxifraga phylogeny and two of these shifts led to radiations within two large subclades of Saxifraga, sect. Ciliatae Haworth subsect. Hirculoideae Engl. & Irmsch. and sect. Porphyrion Tausch subsect. Kabschia Engl. GEOSSE analyses showed that presence in the Hengduan Mountains had a positive effect on diversification across Saxifraga. Influence of these mountains was strongest in Saxifraga sect. Ciliatae subsect. Hirculoideae given its pronounced distribution there, and thus the radiation in this group can be classified at least partially as geographic. In contrast, the evolution of the cushion life form and lime-secreting hydathodes had positive effects on diversification only in selected Saxifraga sections, including sect. Porphyrion subsect. Kabschia. We therefore argue that radiation in this group was likely adaptive. CONCLUSIONS: Our study underlines the complexity of processes and factors underpinning plant radiations: Even in closely related lineages occupying the same life zone, shifts in diversification are not necessarily governed by similar factors. In conclusion, alpine plant radiations result from a complex interaction among geographical settings and/or climatic modifications providing key opportunities for diversification as well as the evolution of key innovations.
[Mh] Termos MeSH primário: Saxifragaceae/classificação
Saxifragaceae/genética
[Mh] Termos MeSH secundário: Evolução Biológica
Mudança Climática
Geografia
Filogenia
Saxifragaceae/anatomia & histologia
Tibet
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170901
[Lr] Data última revisão:
170901
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170527
[St] Status:MEDLINE
[do] DOI:10.1186/s12862-017-0967-2


  6 / 236 MEDLINE  
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[PMID]:28421612
[Au] Autor:Tiwary BK; Ghosh R; Moktan S; Ranjan VK; Dey P; Choudhury D; Dutta S; Deb D; Das AP; Chakraborty R
[Ad] Endereço:Omics Laboratory, Department of Biotechnology, University of North Bengal, Siliguri, India.
[Ti] Título:Prospective bacterial quorum sensing inhibitors from Indian medicinal plant extracts.
[So] Source:Lett Appl Microbiol;65(1):2-10, 2017 Jul.
[Is] ISSN:1472-765X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:As virulence of many pathogenic bacteria is regulated by the phenomenon of quorum sensing (QS), the present study aimed to find the QS-inhibiting (QS-I) property (if any) in 61 Indian medicinal plants. The presence of QS-I compound in the leaf extract was evaluated by its ability to inhibit production of pigment in Chromobacterium violaceum MTCC 2656 (violacein) and Pseudomonas aeruginosa MTCC 2297 (pyocyanin) or swarming of P. aeruginosa MTCC 2297. Extracts of three plants, Astilbe rivularis, Fragaria nubicola and Osbeckia nepalensis, have shown a dose-dependent inhibition of violacein production with no negative effect on bacterial growth. Inhibition of pyocyanin pigment production and swarming motility in P. aeruginosa MTCC 2297 was also shown. Based on the results obtained by gas chromatography-mass spectroscopy (GC-MS) and thin-layer chromatography-direct bioautography (TLC-DB), it was concluded that triterpenes and flavonoid compounds found in the three plant extracts could have QS-I activity. SIGNIFICANCE AND IMPACT OF THE STUDY: A novel alternative prospect to prevent bacterial infections without inhibiting the growth is to apply chemicals that inhibit quorum sensing mechanism of the pathogens. Antiquorum property of 61 medicinal plants was evaluated by the ability of their leaf extract(s) to inhibit production of pigment (violacein in Chromobacterium violaceum MTCC 2656, pyocyanin in Pseudomonas aeruginosa MTCC 2297) or swarming in P. aeruginosa MTCC 2297. The most prospective plants (for the development of quorum sensing inhibitor), showing inhibition of violacein production without affecting bacterial growth, were Astilbe rivularis, Fragaria nubicola and Osbeckia nepalensis.
[Mh] Termos MeSH primário: Chromobacterium/efeitos dos fármacos
Flavonoides/farmacologia
Indóis/metabolismo
Pseudomonas aeruginosa/efeitos dos fármacos
Piocianina/biossíntese
Percepção de Quorum/efeitos dos fármacos
Triterpenos/farmacologia
[Mh] Termos MeSH secundário: Antibacterianos/farmacologia
Fragaria/química
Medicina Tradicional
Melastomataceae/química
Extratos Vegetais/farmacologia
Folhas de Planta/química
Plantas Medicinais/química
Estudos Prospectivos
Saxifragaceae/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Flavonoids); 0 (Indoles); 0 (Plant Extracts); 0 (Triterpenes); 9OQM399341 (Pyocyanine); QJH0DSQ3SG (violacein)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170420
[St] Status:MEDLINE
[do] DOI:10.1111/lam.12748


  7 / 236 MEDLINE  
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[PMID]:28361347
[Au] Autor:Koethe S; Bloemer J; Lunau K
[Ad] Endereço:Institute of Sensory Ecology, Heinrich-Heine-University Düsseldorf, Düsseldorf, Germany.
[Ti] Título:Testing the influence of gravity on flower symmetry in five Saxifraga species.
[So] Source:Naturwissenschaften;104(3-4):37, 2017 Apr.
[Is] ISSN:1432-1904
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Flower symmetry is considered a species-specific trait and is categorized in asymmetry, actinomorphic symmetry, bisymmetry and zygomorphic symmetry. Here we report on the intra-individual variation of flower symmetry in the genus Saxifraga and the influence of light, gravity and intrinsic factors on the development of flower symmetry. We tested five species-Saxifraga cuneifolia, Saxifraga imparilis, Saxifraga rotundifolia, Saxifraga stolonifera and Saxifraga umbrosa-concerning six flower parameters-angles between petals, petal length, petal pigmentation, angular position of carpels, movement of stamens and (only for S. imparilis and S. stolonifera) the length of the two lower elongated petals in regard to their position towards the stem. Specimens of all species were tested on a vertical clinostat as a gravity compensator, on a horizontal clinostat as a light incidence compensator and on a stationary control. The results show that the angle of incident light has no apparent impact on flower symmetry, whereas gravity affects the angular position of petals in S. cuneifolia and S. umbrosa and the petal colouration in S. rotundifolia. In S. cuneifolia and S. umbrosa, the absence of directional gravity resulted in the development of actinomorphic flowers, whereas the corresponding control flowers were zygomorphic. The development of flowers in S. rotundifolia was not altered by this treatment. The length of the two elongated petals in S. stolonifera and S. imparilis was not affected by gravity, but rather was determined by position of the flower within the inflorescence and resulted in asymmetrical flowers.
[Mh] Termos MeSH primário: Flores/anatomia & histologia
Gravitação
Saxifragaceae/anatomia & histologia
Saxifragaceae/fisiologia
[Mh] Termos MeSH secundário: Especificidade da Espécie
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170916
[Lr] Data última revisão:
170916
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170401
[St] Status:MEDLINE
[do] DOI:10.1007/s00114-017-1458-4


  8 / 236 MEDLINE  
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[PMID]:28349055
[Au] Autor:Sharma I; Khan W; Parveen R; Alam MJ; Ahmad I; Ansari MH; Ahmad S
[Ad] Endereço:Bioactive Natural Product Laboratory, Department of Pharmacognosy and Phytochemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi 110062, India.
[Ti] Título:Antiurolithiasis Activity of Bioactivity Guided Fraction of against Ethylene Glycol Induced Renal Calculi in Rat.
[So] Source:Biomed Res Int;2017:1969525, 2017.
[Is] ISSN:2314-6141
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Dried rhizome of (pashanbhed) is commonly used as a traditional herbal medicine with a wide range of therapeutic applications including urolithiasis. Aqueous extract of was prepared through maceration followed by decoction (mother extract, 35.9% w/w). Further, polarity based fractions were prepared successively from mother extract which yielded 3.4, 2.9, 5.4, 7.5, and 11.3% w/w of hexane, toluene, dichloromethane (DCM), -butanol, and water fractions, respectively. The in vitro, ex vivo, and real-time antiurolithiasis activity of mother extract and fractions were carried out using aggregation assay in synthetic urine and in rat plasma. The study revealed that DCM fraction has significantly ( < 0.05) greater inhibitory potential than other fractions. Ethylene glycol in drinking water (0.75%, v/v) for 28 days was used for induction of urolithiasis and the curative effects of mother extract and DCM fraction were checked for the level of oxalate, calcium, creatinine, uric acid, and urea of both urine and serum. Treatment with mother extract and DCM fraction at a dose of 185 mg/kg and 7 mg/kg, respectively, in ethylene glycol induced rats resulted in a significant ( < 0.05) decrease in serum and urine markers. Histological study revealed lower number of calcium oxalate deposits with minimum damage in the kidneys of mother extract and DCM fraction treated rats. This result provides a scientific basis for its traditional claims.
[Mh] Termos MeSH primário: Antioxidantes/administração & dosagem
Cálculos Renais/tratamento farmacológico
Extratos Vegetais/administração & dosagem
Saxifragaceae/química
Urolitíase/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Antioxidantes/química
Modelos Animais de Doenças
Etilenoglicol/toxicidade
Seres Humanos
Cálculos Renais/induzido quimicamente
Cálculos Renais/patologia
Extratos Vegetais/química
Plantas Medicinais/química
Ratos
Urolitíase/induzido quimicamente
Urolitíase/patologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Plant Extracts); FC72KVT52F (Ethylene Glycol)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170428
[Lr] Data última revisão:
170428
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170329
[St] Status:MEDLINE
[do] DOI:10.1155/2017/1969525


  9 / 236 MEDLINE  
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[PMID]:28205435
[Au] Autor:Chattopadhyay AK; Hanessian S
[Ad] Endereço:Department of Chemistry, Université de Montréal , Post Office Box 6128, Station Centre Ville, Montreal, Quebec H3C 3J7, Canada.
[Ti] Título:Recent Progress in the Chemistry of Daphniphyllum Alkaloids †.
[So] Source:Chem Rev;117(5):4104-4146, 2017 Mar 08.
[Is] ISSN:1520-6890
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Daphniphyllum is an evergreen species known since 1826. After initial systematic investigations, more than 320 members of this family have been isolated, which comprise complex and fascinating structures. Unique azapolycyclic architectures containing one or more quaternary stereocenters render these alkaloids synthetically challenging. This review covers efforts toward the synthesis of Daphniphyllum alkaloids spanning the period from 2005 to the beginning of 2016, including reported biological activities as well as the isolation of new members of this genus.
[Mh] Termos MeSH primário: Alcaloides/química
Saxifragaceae/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Alkaloids)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170622
[Lr] Data última revisão:
170622
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170217
[St] Status:MEDLINE
[do] DOI:10.1021/acs.chemrev.6b00412


  10 / 236 MEDLINE  
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[PMID]:27887929
[Au] Autor:Kang H; Ku SK; Kim J; Chung J; Kim SC; Zhou W; Na M; Bae JS
[Ad] Endereço:College of Pharmacy, CMRI, Research Institute of Pharmaceutical Sciences, BK21 Plus KNU Multi-Omics Based Creative Drug Research Team, Kyungpook National University, Daegu 41566, Republic of Korea.
[Ti] Título:Anti-vascular inflammatory effects of pentacyclic triterpenoids from Astilbe rivularis in vitro and in vivo.
[So] Source:Chem Biol Interact;261:127-138, 2017 Jan 05.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:Sepsis is a systemic inflammatory condition resulting from bacterial infections. It is associated with high mortality rates, and its therapeutic options are limited. Transforming growth factor ß induced protein (TGFBIp) is an extracellular matrix protein that functions as a mediator of experimental sepsis. C-27-carboxylated pentacyclic triterpenoids are specifically found in species of the genus Astilbe, and show several biological effects. Given the anti-inflammatory effects of pentacyclic triterpenoids, we investigated the effects of 3ß-trans-p-coumaroyloxy-olean-12-en-27-oic acid (1) and 6ß-hydroxy-3-oxoolean-12-en-27-oic acid (2) on TGFBIp-mediated vascular inflammatory responses. The anti-inflammatory activities of compounds 1 and 2 were determined by measuring the permeability, leukocyte adhesion and migration, and activation of pro-inflammatory proteins in TGFBIp-activated human umbilical vein endothelial cells (HUVECs) and mice. We found that compounds 1 and 2 inhibited lipopolysaccharide (LPS)-induced TGFBIp secretion, TGFBIp-induced barrier disruption, expression of cell adhesion molecules (CAMs), and the adhesion/transendothelial migration of the neutrophils to the human endothelial cells. Compounds 1 and 2 also suppressed TGFBIp-induced hyperpermeability and leukocyte migration in vivo. These results suggested that C-27-carboxylated pentacyclic triterpenoids 1 and 2 have anti-inflammatory functions by inhibiting hyperpermeability, CAM expression, and leukocyte adhesion/migration. Therefore, these compounds can be considered as a potential therapy for vascular inflammatory diseases.
[Mh] Termos MeSH primário: Anti-Inflamatórios/farmacologia
Triterpenos Pentacíclicos/farmacologia
Saxifragaceae/química
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios/química
Anti-Inflamatórios/uso terapêutico
Ceco/patologia
Adesão Celular/efeitos dos fármacos
Moléculas de Adesão Celular/metabolismo
Movimento Celular/efeitos dos fármacos
Proteínas da Matriz Extracelular/metabolismo
Células Endoteliais da Veia Umbilical Humana/efeitos dos fármacos
Células Endoteliais da Veia Umbilical Humana/patologia
Seres Humanos
Inflamação/patologia
Interleucina-6/metabolismo
Ligadura
Lipopolissacarídeos/farmacologia
Pulmão/efeitos dos fármacos
Pulmão/patologia
Masculino
Camundongos Endogâmicos C57BL
NF-kappa B/metabolismo
Neutrófilos/citologia
Neutrófilos/efeitos dos fármacos
Triterpenos Pentacíclicos/química
Triterpenos Pentacíclicos/uso terapêutico
Permeabilidade/efeitos dos fármacos
Substâncias Protetoras/farmacologia
Substâncias Protetoras/uso terapêutico
Punções
Sepse/tratamento farmacológico
Sepse/patologia
Fator de Crescimento Transformador beta/metabolismo
Fator de Necrose Tumoral alfa/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Cell Adhesion Molecules); 0 (Extracellular Matrix Proteins); 0 (Interleukin-6); 0 (Lipopolysaccharides); 0 (NF-kappa B); 0 (Pentacyclic Triterpenes); 0 (Protective Agents); 0 (Transforming Growth Factor beta); 0 (Tumor Necrosis Factor-alpha); 148710-76-3 (betaIG-H3 protein)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170207
[Lr] Data última revisão:
170207
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161127
[St] Status:MEDLINE



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