Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 528
Filtrar
1.
Phytochemistry ; 195: 113050, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34906836

RESUMO

Development of the kiwifruit industry has been severely hindered by the canker disease, which is caused by the bacterium Pseudomonas syringae pv. Actinidiae (Psa). However, endophytic fungi associated with healthy kiwi plants may protect host plants through the production of metabolites with potent anti-Psa activity. In the current study, four undescribed isobenzofuranones, namely sporulactones A‒D, two undescribed isocoumarins, namely sporulactones E and F, together with eight known analogs were isolated from the kiwi endophytic fungus Paraphaeosphaeria sporulosa. The structures with absolute configurations were established by extensive spectroscopic methods, quantum chemistry calculations, and X-ray diffraction experiments. In addition, five of the compounds exhibited anti-Psa activity, with minimum inhibitory concentration (MIC) values ranging from 25 to 100 µg/mL. These findings suggest that the small polyketide metabolites produced by P. sporulosa play an important role in the antibacterial properties of the endophyte.


Assuntos
Actinidia , Ascomicetos , Antibacterianos/farmacologia , Isocumarinas/farmacologia , Doenças das Plantas , Pseudomonas syringae
2.
J Org Chem ; 86(15): 10799-10811, 2021 08 06.
Artigo em Inglês | MEDLINE | ID: mdl-34255511

RESUMO

An enantioselective palladium-catalyzed annulation of alkyne-tethered malononitriles for the synthesis of 3,4-ring-fused isocoumarins is described. This cascade strategy involves oxypalladation of ortho-alkynylbenzoates and desymmetrizing addition onto one cyano group of the pendant malononitriles, which enables the concurrent construction of two rings and an all-carbon quaternary stereocenter in a single operation.


Assuntos
Alcinos , Paládio , Catálise , Isocumarinas , Estrutura Molecular , Nitrilas , Estereoisomerismo
3.
Eur J Med Chem ; 221: 113514, 2021 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-33992926

RESUMO

While anti-inflammatory properties of isocoumarins are known their PDE4 inhibitory potential was not explored previously. In our effort the non-PDE4 inhibitor isocoumarins were transformed into the promising inhibitors via introducing an aminosulfonyl/aminocarboxamide moiety to the C-3 benzene ring attached to the isocoumarin framework. This new class of isocoumarins were synthesized via a PdCl2-catalyzed construction of the 4-allyl substituted 3-aryl isocoumarin ring starting from the appropriate 2-alkynyl benzamide derivative. Several compounds showed good inhibition of PDE4B in vitro and the SAR indicated superiority of aminosulfonamide moiety over aminocarboxamide in terms of PDE4B inhibition. Two compounds 3q and 3u with PDE4B IC50 = 0.43 ± 0.11 and 0.54 ± 0.19 µM and ≥ 2-fold selectivity over PDE4D emerged as initial hits. The participation of aminosulfonamide moiety in PDE4B inhibition and the reason for selectivity though moderate shown by 3q and 3u was revealed by the in silico docking studies. In view of potential usefulness of moderately selective PDE4B inhibitors the compound 3u (that showed PDE4 selectivity over other PDEs) was further evaluated in adjuvant induced arthritic rats. At an intraperitoneal dose of 30 mg/kg the compound showed a significant reduction in paw swelling (in a dose dependent manner), inflammation and pannus formation (in the knee joints) as well as pro-inflammatory gene expression/mRNA levels and increase in body weight. Moreover, besides its TNF-α inhibition and no significant toxicity in an MTT assay the compound did not show any adverse effects in a thorough toxicity studies e.g. teratogenicity, hepatotoxicity, cardiotoxicity and apoptosis in zebrafish. Thus, the isocoumarin 3u emerged as a new, safe and moderately selective PDE4B inhibitor could be useful for inflammatory diseases possibly including COVID-19.


Assuntos
Anti-Inflamatórios/uso terapêutico , Artrite Experimental/tratamento farmacológico , Isocumarinas/uso terapêutico , Inibidores da Fosfodiesterase 4/uso terapêutico , Sulfonamidas/uso terapêutico , Animais , Anti-Inflamatórios/síntese química , Anti-Inflamatórios/metabolismo , Anti-Inflamatórios/toxicidade , Artrite Experimental/patologia , Catálise , Nucleotídeo Cíclico Fosfodiesterase do Tipo 4/metabolismo , Embrião não Mamífero/efeitos dos fármacos , Feminino , Isocumarinas/síntese química , Isocumarinas/metabolismo , Isocumarinas/toxicidade , Articulação do Joelho/efeitos dos fármacos , Articulação do Joelho/patologia , Masculino , Camundongos , Simulação de Acoplamento Molecular , Estrutura Molecular , Paládio/química , Inibidores da Fosfodiesterase 4/síntese química , Inibidores da Fosfodiesterase 4/metabolismo , Inibidores da Fosfodiesterase 4/toxicidade , Ligação Proteica , Células RAW 264.7 , Ratos Wistar , Relação Estrutura-Atividade , Sulfonamidas/síntese química , Sulfonamidas/metabolismo , Sulfonamidas/toxicidade , Peixe-Zebra
4.
ACS Infect Dis ; 7(6): 1777-1794, 2021 06 11.
Artigo em Inglês | MEDLINE | ID: mdl-33843204

RESUMO

Here we have described a systematic structure activity relationship (SAR) of a set of compounds inspired from cladosporin, a tool compound that targets parasite (Plasmodium falciparum) lysyl tRNA synthetase (KRS). Four sets of analogues, synthesized based on point changes in the chemical scaffold of cladosporin and other logical modifications and hybridizations, were assessed using high throughput enzymatic and parasitic assays along with in vitro pharmacokinetics. Co-crystallization of the most potent compound in our series (CL-2) with PfKRS revealed its structural basis of enzymatic binding and potency. Further, we report that CL-2 has performed better than cladosporin in terms of metabolic stability. It thus represents a new lead for further optimization toward the development of antimalarial drugs. Collectively, along with a lead compound, the series offers insights on how even the slightest chemical modification might play an important role in enhancing or decreasing the potency of a chemical scaffold.


Assuntos
Malária , Parasitos , Animais , Isocumarinas , Plasmodium falciparum
5.
Org Lett ; 23(6): 2337-2341, 2021 03 19.
Artigo em Inglês | MEDLINE | ID: mdl-33688736

RESUMO

A fungal C4-alkylated dihydroisocoumarin pathway was discovered and elucidated. This pathway includes the following (1) a nonreducing polyketide synthase and a P450 collaboratively synthesize hydroxylated C3-methylated isocoumarin 3; (2) a methyltransferase methylates 3 to 8; and (3) importantly, an esterase specifically catalyzes a ring reconstruction process of 8 to C4-alkylated dihydroisocoumarin 10. Our discovery fills the gap in the enzymatic transformation process of natural C4-alkylated isocoumarin derivates.


Assuntos
Fungos/química , Isocumarinas/química , Policetídeo Sintases/química , Alquilantes , Alquilação , Catálise , Fungos/metabolismo , Genoma Fúngico , Estrutura Molecular , Policetídeo Sintases/metabolismo
6.
Angew Chem Int Ed Engl ; 60(20): 11423-11429, 2021 05 10.
Artigo em Inglês | MEDLINE | ID: mdl-33661567

RESUMO

The polyketide synthase (PKS)-like protein TerB, consisting of inactive dehydratase, inactive C-methyltransferase, and functional ketoreductase domains collaborates with the iterative non reducing PKS TerA to produce 6-hydroxymellein, a key pathway intermediate during the biosynthesis of various fungal natural products. The catalytically inactive dehydratase domain of TerB appears to mediate productive interactions with TerA, demonstrating a new mode of trans-interaction between iterative PKS components.


Assuntos
Aldo-Ceto Redutases/metabolismo , Hidroliases/metabolismo , Isocumarinas/metabolismo , Metiltransferases/metabolismo , Aldo-Ceto Redutases/química , Hidroliases/química , Isocumarinas/química , Metiltransferases/química , Estrutura Molecular
7.
J Antibiot (Tokyo) ; 74(4): 280-284, 2021 04.
Artigo em Inglês | MEDLINE | ID: mdl-33526864

RESUMO

A fungal metabolite, isocladosporin was isolated from natural fungus, Cladosporium cladosporioides in the mid of 90s. Due to the lack of optical rotation of isolated natural product sample, the absolute configuration of the natural product remained undetermined for more than two decades. Herein, we demonstrated an SAR study of enantiomers of isocladosporin in herbicidal bio-assay against wheat coleoptile. Using this study as a comparative tool we further proposed the plausible absolute configuration of natural isocladosporin for the first time. The assigned configuration was also supported through biogenetic precursors.


Assuntos
Herbicidas/química , Herbicidas/farmacologia , Isocumarinas/química , Isocumarinas/farmacologia , Animais , Cladosporium/química , Besouros/efeitos dos fármacos , Estereoisomerismo , Relação Estrutura-Atividade , Triticum
8.
Nutrients ; 13(1)2021 Jan 17.
Artigo em Inglês | MEDLINE | ID: mdl-33477276

RESUMO

Alzheimer's disease (AD) is a neurodegenerative disease conceptualized as a clinical-biological neurodegenerative construct where amyloid-beta pathophysiology is supposed to play a role. The loss of cognitive functions is mostly characterized by the rapid hydrolysis of acetylcholine by cholinesterases including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Moreover, both enzymes are responsible for non-catalytic actions such as interacting with amyloid ß peptide (Aß) which further leads to promote senile plaque formation. In searching for a natural cholinesterase inhibitor, the present study focused on two isocoumarines from hydrangea, thunberginol C (TC) and hydrangenol 8-O-glucoside pentaacetate (HGP). Hydrangea-derived compounds were demonstrated to act as dual inhibitors of both AChE and BChE. Furthermore, the compounds exerted selective and non-competitive mode of inhibition via hydrophobic interaction with peripheral anionic site (PAS) of the enzymes. Overall results demonstrated that these natural hydrangea-derived compounds acted as selective dual inhibitors of AChE and BChE, which provides the possibility of potential source of new type of anti-cholinesterases with non-competitive binding property with PAS.


Assuntos
Inibidores da Colinesterase/farmacologia , Hydrangea/química , Acetilcolinesterase/metabolismo , Doença de Alzheimer/enzimologia , Peptídeos beta-Amiloides/metabolismo , Sítios de Ligação , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/química , Humanos , Interações Hidrofóbicas e Hidrofílicas , Isocumarinas , Cinética , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Relação Estrutura-Atividade
9.
Nat Prod Res ; 35(22): 4380-4387, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31960706

RESUMO

A new isocoumarin (1) named fraxicoumarin was isolated from the bark of Fraxinus chinensis subsp. rhynchophylla along with three known compounds (2-4). The structure of the new compound was established by extensive spectroscopic studies and chemical evidence. The anti-inflammatory effects of the isolated compounds (1-4) on lipopolysaccharide (LPS)-induced RAW 264.7 macrophage cells were evaluated in vitro. Of the compounds tested, compounds 1 and 3 inhibited LPS-induced nitric oxide (NO) production in RAW 264.7 cells. Consistent with these findings, they also suppressed LPS-induced expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) at the protein level in RAW 264.7 cells.


Assuntos
Fraxinus , Anti-Inflamatórios/farmacologia , Ciclo-Oxigenase 2/metabolismo , Isocumarinas/farmacologia , Lipopolissacarídeos/farmacologia , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Casca de Planta
10.
Nat Prod Res ; 35(21): 3644-3651, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32000518

RESUMO

Two new 2H-pyranones (1 and 2), two new isocoumarins (4 and 5), and two known compounds (3 and 6) were obtained from solid cultures of the endophytic fungus Pestalotiopsis microspora SC3082. Their structures and revision of the absolute stereochemistry of 6 were established by spectroscopic analyses and computational calculations. Compounds 2, 4 and 6 displayed moderate antifungal activities against Candida albicans ATCC 10321 with MIC values of 25.0, 25.0, and 12.5 µg/mL, respectively.


Assuntos
Isocumarinas , Magnoliopsida , Antifúngicos/farmacologia , Candida albicans , Isocumarinas/farmacologia , Estrutura Molecular , Pestalotiopsis
11.
Nat Prod Res ; 35(22): 4616-4620, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31782665

RESUMO

Five chromone derivatives, including 2,6-dimethyl-5-methoxyl-7-hydroxylchromone (1), 6-hydroxymethyleugenin (2), 6-methoxymethyleugenin (3), chaetoquadrin D (4), and isoeugenitol (5), and three isocoumarin congeners, namely diaporthin (6), 8-hydroxy-6-methoxy-3-methylisocoumarin (7), and 6-methoxymellein (8), were isolated from the culture of the endophytic fungus Xylomelasma sp. Samif07 derived from the medicinal plant Salvia miltiorrhiza Bunge. Among them, compound 1 was a new natural product. Their structures were determined by spectroscopic methods and comparison with the literature. The isolated compounds were evaluated for their antibacterial and antioxidant activities. Compound 5 showed notable antitubercular activity against Mycobacterium tuberculosis with MIC value of 10.31 µg/mL, while compounds 1-3, and 5-7 displayed inhibitory activities against the other bacteria with MIC range of 25 ∼ 100 µg/mL. Meanwhile, compound 6 showed potent hydroxyl radical-scavenging activity with EC50 value of 15.1 µg/mL, while compounds 5-7 showed certain ferric reducing ability.


Assuntos
Antioxidantes , Ascomicetos , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Antituberculosos , Cromonas/farmacologia , Isocumarinas/farmacologia , Testes de Sensibilidade Microbiana , Estrutura Molecular
12.
Nat Prod Res ; 35(9): 1445-1451, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-31460795

RESUMO

Two new dihydroisocoumarins (1 and 2), together with six known compounds (3-8), were isolated from the fungus Penicillium sp. XR046 collected from the Xinren coal area of Guizhou province in China. Their structures were elucidated on the basis of spectroscopic analysis. The absolute configurations of C-3 in 1 and 2 were established by comparison of their CD data with those of known compounds. Compounds 1-6 showed anti-microbial activities with MIC values in the range of 50∼100 µg/mL against Candida albicans, Staphylococcus epidermidis, Bacillus subtilis, and Escherichia coli.


Assuntos
Anti-Infecciosos/farmacologia , Carvão Mineral/microbiologia , Isocumarinas/farmacologia , Penicillium/química , Anti-Infecciosos/química , Bactérias/efeitos dos fármacos , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , China , Fungos/efeitos dos fármacos , Isocumarinas/química , Testes de Sensibilidade Microbiana , Espectroscopia de Prótons por Ressonância Magnética
13.
Nat Prod Res ; 35(7): 1115-1121, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31307232

RESUMO

Cladosporine A (1), a new indole diterpenoid alkaloid, was isolated from the extract of a fungal strain Cladosporium sp. JNU17DTH12-9-01. Its structure was elucidated by extensive spectroscopic analysis, and the absolute configurations were determined by electronic circular dichroism (ECD) experiments. This is the first report of the presence of indole diterpenoid alkaloid in the genus Cladosporium. The antimicrobial activities against Staphylococcus aureus 209P, Escherichia coli ATCC0111, Aspergillus niger R330, and Candida albicans FIM709 were evaluated. Compound 1 showed MICs of 4 µg/mL and 16 µg/mL against S. aureus 209P and C. albicans FIM709, respectively.


Assuntos
Anti-Infecciosos/farmacologia , Cladosporium/química , Diterpenos/farmacologia , Alcaloides Indólicos/farmacologia , Isocumarinas/farmacologia , Anti-Infecciosos/química , Bactérias/efeitos dos fármacos , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Dicroísmo Circular , Fungos/efeitos dos fármacos , Alcaloides Indólicos/química , Isocumarinas/química , Testes de Sensibilidade Microbiana , Espectroscopia de Prótons por Ressonância Magnética
14.
Nat Prod Res ; 35(7): 1122-1126, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31313599

RESUMO

A novel 3,4-dihydroisocoumarin, lindermyrrhin (1), along with three known compounds, quercetin (2), northalifoline (3) and N-formyl-laurolitsine (4) were isolated from the roots of Lindera myrrha. The structure of compound 1 was identified by interpretation of their spectroscopic data as well as comparison with those reported in the literature. The novel compound 1 represents the first 3,4-dihydroisocoumarin bearing a 2-hydroxyisopropyl substituent at C-3.


Assuntos
Isocumarinas/farmacologia , Lindera/química , Raízes de Plantas/química , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Isocumarinas/química , Espectroscopia de Prótons por Ressonância Magnética
15.
Nat Prod Res ; 35(10): 1573-1581, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-31170816

RESUMO

Chemical characterization of ethyl acetate extract of Exophiala sp. has afforded the isolation of three compounds including a new isocoumarin named exophiarin (1). Exophiala sp. was obtained from the soil containing dumped organic waste (litter). Initially, LC-UV-MS analysis of the extract of Exophiala sp. revealed the presence of a new compound having molecular weight 438 (1) and previously reported TPI-2 and TPI-5. The novelty was established using advanced database search comprising of biological source, molecular weight and UV profile. 1D, 2D NMR and HRMS data have been used for structure elucidation. Exophiarin with TPI-2 and TPI-5 have displayed moderate improvement in glucose uptake activity when tested in rat skeletal muscle cell line L6.


Assuntos
Exophiala/química , Hipoglicemiantes/farmacologia , Isocumarinas/farmacologia , Animais , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Isocumarinas/química , Isocumarinas/isolamento & purificação , Camundongos , Peso Molecular , Filogenia , Espectroscopia de Prótons por Ressonância Magnética
16.
Nat Prod Res ; 35(13): 2232-2238, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31564133

RESUMO

A new epimer of azaphilone derivative pinophilin B, epi-pinophilin B (1), and three known analogues (2-4) were obtained from the culture of the gorgonian-derived fungus Aspergillus fumigatus 14-27. The structures of 1-4, including their relative configurations were determined by extensive spectroscopic analysis and comparing with literature data. The absolute configuration of 1 was determined by electronic circular dichroism (ECD) and optical rotatory (OR) calculations methods. Compounds 1-4 were isolated from A. fumigatus for the first time. Their antibacterial and cytotoxic activities were also evaluated.


Assuntos
Aspergillus fumigatus/química , Benzopiranos/química , Isocumarinas/química , Pigmentos Biológicos/química , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Benzopiranos/isolamento & purificação , Benzopiranos/farmacologia , Isocumarinas/isolamento & purificação , Isocumarinas/farmacologia , Pigmentos Biológicos/isolamento & purificação , Pigmentos Biológicos/farmacologia , Espectroscopia de Prótons por Ressonância Magnética
17.
Phytochemistry ; 181: 112568, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-33166749

RESUMO

Isocoumarins and dihydroisocoumarins are lactonic phytochemicals plentiful in microbes and higher plants. These are an amazing small scaffolds consecrated with all types of pharmacological applications. Our previous review covered the period 2000-2016, documenting the then known natural products of this class; the current article is a critical account of discovery of known as well as undescribed structural types and pharmacological activities reported in the course of 2016-2020. The classification revealed in our previous review based on the biogenetic origin is further buttressed by discovery of new members of each class and some new structural types hitherto unknown have also been identified. Similarly, the biological activities and SAR conclusions identified were found to be valid as well, nonetheless with new accompaniments. The most recent available literature on the structural diversity and biological activity of these natural products has been included. The information documented in this article are collected from scientific journals, books, electronic search engines and scientific databases.


Assuntos
Produtos Biológicos , Isocumarinas , Produtos Biológicos/farmacologia , Compostos Fitoquímicos
18.
Med Chem ; 17(8): 820-833, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32484772

RESUMO

BACKGROUND: Malaria greatly affects the world health, having caused more than 228 million cases only in 2018. The emergence of drug resistance is one of the main problems in its treatment, demonstrating the need for the development of new antimalarial drugs. OBJECTIVE: Synthesis and in vitro antiplasmodial evaluation of triazole compounds derived from isocoumarins and a 3,4-dihydroisocoumarin. METHODS: The compounds were synthesized in 4 to 6-step reactions with the formation of the triazole ring via the Copper(I)-catalyzed 1,3-dipolar cycloaddition between isocoumarin or 3,4- dihydroisocoumarin azides and terminal alkynes. This key reaction provided compounds with an unprecedented connection of isocoumarin or 3,4-dihydroisocoumarin and the 1,2,3-triazole ring. The products were tested for their antiplasmodial activity against a Plasmodium falciparum chloroquine resistant and sensitive strains (W2 and 3D7, respectively). RESULTS: Thirty-one substances were efficiently obtained by the proposed routes with an overall yield of 25-53%. The active substances in the antiplasmodial test displayed IC50 values ranging from 0.68-2.89 µM and 0.85-2.07 µM against W2 and 3D7 strains, respectively. CONCLUSION: This study demonstrated the great potential of isocoumarin or 3,4-dihydroisocoumarin derivatives because practically all the tested substances were active against Plasmodium falciparum.


Assuntos
Antimaláricos/síntese química , Antimaláricos/farmacologia , Isocumarinas/síntese química , Isocumarinas/farmacologia , Triazóis/química , Alcinos , Antimaláricos/química , Técnicas de Química Sintética , Reação de Cicloadição , Isocumarinas/química , Plasmodium falciparum/efeitos dos fármacos , Relação Estrutura-Atividade
19.
Chin J Nat Med ; 18(11): 855-859, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33308608

RESUMO

Four new compounds, asperisocoumarin G (1), asperisocoumarin H (2), (±)-asperisocoumarin I [(±)-3], along with the known pergillin (4) and penicisochroman L (5) were isolated from a mangrove endophytic fungus Aspergillus sp. 085242 by further chemical investigation. The structures of the new compounds, including their absolute configurations, were established by analysis of HR-ESI-MS and NMR spectroscopic data, and ECD calculation. Asperisocoumarins G-I (1-3) were new isocoumarins belonging to the class of furo[3, 2-h]isocoumarins which are rarely found in natural sources. All of the isolated compounds were evaluated for their α-glucosidase inhibitory effects, and compounds 1 and 4 showed moderate α-glucosidase inhibitory activity, respectively. In an antimicrobial test, the racemate of 3 showed antibacterial activity against Salmonella.


Assuntos
Antibacterianos/farmacologia , Aspergillus/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Isocumarinas/química , Isocumarinas/isolamento & purificação , Isocumarinas/farmacologia , Estrutura Molecular
20.
Bioorg Chem ; 105: 104443, 2020 12.
Artigo em Inglês | MEDLINE | ID: mdl-33197853

RESUMO

In the course of our continuing search for biologically active compounds from medicinal sources, we investigated the MeOH extract of the aerial parts of Coriandrum sativum Linn. An extended phytochemical investigation of the aerial parts of C. sativum led to the isolation and identification of seven compounds (1-7) including two new isocoumarin glycosides (1-2) and a new phenolic glycoside (5). The chemical structures of the new compounds (1, 2, and 5) were elucidated by analysis of 1D and 2D NMR (1H and 13C NMR, COSY, HSQC, and HMBC) and HRESIMS data as well as by using chemical methods. All the isolates were evaluated not only for their potential neurotrophic activity by means of induction of nerve growth factor (NGF) in C6 glioma cells but also for production of nitric oxide (NO) levels in lipopolysaccharide (LPS)-activated murine microglia BV-2 cells to assess their anti-neuroinflammatory activity. Compounds 1-3 and 7 were stimulants of NGF release, with levels of NGF stimulated at 127.23 ± 1.89%, 128.22 ± 5.45%, 121.23 ± 6.66%, and 120.94 ± 3.97%, respectively. Furthermore, the aglycones of 1 and 2 (1a and 2a) showed more potent NGF secretion activity and anti-neuroinflammatory effect than did their glycosides (1a : 130.81 ± 5.45% and 2a : 134.44 ± 5.45%).


Assuntos
Anti-Inflamatórios não Esteroides/química , Coriandrum/química , Glicosídeos/química , Fármacos Neuroprotetores/química , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Animais , Anti-Inflamatórios não Esteroides/farmacologia , Linhagem Celular , Glicosídeos/farmacologia , Humanos , Isocumarinas/química , Lipopolissacarídeos/metabolismo , Macrófagos/citologia , Camundongos , Fator de Crescimento Neural/metabolismo , Fármacos Neuroprotetores/farmacologia , Óxido Nítrico/metabolismo , Fenóis/química , Extratos Vegetais/farmacologia
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...