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1.
J Nat Prod ; 83(6): 1766-1777, 2020 06 26.
Artigo em Inglês | MEDLINE | ID: mdl-32479076

RESUMO

Fourteen new terpenoids plagicosins A-N (1-14), including seven sesquiterpenoids (1-7) consisting of six ent-bicyclogermacrenes and one ent-2,3-seco-aromadendrane, as well as seven diterpenoids (8-14) comprising five fusicoccanes, a eunicellane, and a rare gersemiane, were isolated from the Chinese liverwort Plagiochila fruticosa Mitt. The structures of these terpenoids were determined on the basis of comprehensive analysis of MS and NMR spectroscopic data coupled with electronic circular dichroism (ECD) and coupling constant calculations. Plagicosin F (6) displayed potent antivirulence activity through inhibiting the hyphal morphogenesis, adhesion, and biofilm formation of Candida albicans. The genes related to hyphal formation were regulated by 6.


Assuntos
Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Hepatófitas/química , Terpenos/farmacologia , Biofilmes/efeitos dos fármacos , Dicroísmo Circular , Diterpenos/química , Hifas/efeitos dos fármacos , Hifas/crescimento & desenvolvimento , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Estrutura Molecular , Sesquiterpenos/química , Terpenos/química , Virulência/efeitos dos fármacos
2.
Phytochemistry ; 174: 112341, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32240851

RESUMO

Eight undescribed terpenoids, namely, odongrossins A-H, together with two known terpenoids were isolated from Odontoschisma grosseverrucosum Stephani (Cephaloziaceae). Their structures were established based on NMR data, electronic circular dichroism (ECD) calculations, and single-crystal X-ray diffraction measurements. Odongrossin A and odongrossin G displayed moderate anti-virulence activities against CDR1-and CDR2-efflux-pump-deficient Candida albicans DSY654. Further investigation of odongrossin A revealed that it inhibited adhesion and biofilm formation on C. albicans DSY654. The results regarding the transcription levels of genes demonstrated that odongrossin A could regulate the expression of genes that are associated with the virulence of C. albicans DSY654.


Assuntos
Antifúngicos , Hepatófitas , Biofilmes , Candida albicans , Proteínas Fúngicas , Terpenos , Virulência
3.
Phytochemistry ; 174: 112324, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32163786

RESUMO

In this study, 14 previously undescribed terpenoids were isolated from the Chinese liverwort Heteroscyphus coalitus (Hook.) Schiffner, including a rare harziane type diterpenoid, heteroscyphsic acid A; eight ent-clerodane diterpenoids, heteroscyphsic acids B-I; four labdane diterpenoids, heteroscyphins A-D; and one guaiane sesquiterpene, heteroscyphin E; as well as a known ent-junceic acid. Their structures were determined by a combination of MS, NMR spectroscopy, electronic circular dichroism (ECD) and single crystal X-ray diffraction analyses. The anti-virulence activity of the isolated compounds against Candida albicans DSY654 demonstrated that most of them could block hyphal growth at concentrations ranging from 4-32 µg/ml. Further investigation of the most active compound, heteroscyphin D, revealed that it could suppress the ability of C. albicans DSY654 to adhere to A549 cells and form biofilms, and modulate the transcription of related genes in this fungus.


Assuntos
Diterpenos Clerodânicos , Hepatófitas , Sesquiterpenos , Candida albicans , Terpenos
4.
Org Lett ; 20(20): 6550-6553, 2018 10 19.
Artigo em Inglês | MEDLINE | ID: mdl-30289265

RESUMO

Two novel ent-aromadendrane derivatives, plagiochianin A (1), possessing an unprecedented 2,3:6,7-di- seco-6,8-cyclo-aromadendrane carbon scaffold conjugated with three cyclic acetals, and plagiochianin B (2), an exceptional pyridine type aromadendrane alkaloid, were isolated from the Chinese liverwort Plagiochila duthiana. Their structures were established by comprehensive spectroscopic analysis coupled with single-crystal X-ray diffraction and electronic circular dichroism calculations. A plausible biogenetic pathway of these two compounds is presented, and their acetylcholinesterase inhibitory activities are preliminarily tested using TLC-bioautographic assays.

5.
Bioorg Med Chem Lett ; 28(9): 1545-1549, 2018 05 15.
Artigo em Inglês | MEDLINE | ID: mdl-29606575

RESUMO

Diversity-oriented synthesis of derivatives of natural products is an important approach for the discovery of novel drugs. In this paper, a series of novel 3,4-diaryl-1H-pyrazoles and 3,5-diaryl-1H-pyrazoles derivatives were synthesized through the one-pot reaction of flavones and isoflavones with the hydrazine hydrate and substituted hydrazine hydrate. Some of these novel compounds exhibited antifungal effects against Candida albicans SC5314, and displayed more potent inhibitory activities against the efflux-pump-deficient strain DSY654. In addition, compounds 25, 28 and 32a displayed outstanding reversal activity of azole resistance against clinical azole-resistant Candida albicans in combination with fluconazole (FLC), with FICI values ranging from 0.012 to 0.141. The preliminary structure-activity relationship (SAR) of these compounds was also discussed. In conclusion, this study provides several novel agents that displayed potent antifungal activities alone or together with fluconazole, which makes progress for development of antifungal drugs.


Assuntos
Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Descoberta de Drogas , Farmacorresistência Fúngica/efeitos dos fármacos , Flavonas/farmacologia , Isoflavonas/farmacologia , Pirazóis/farmacologia , Antifúngicos/síntese química , Antifúngicos/química , Relação Dose-Resposta a Droga , Flavonas/química , Fluconazol/química , Fluconazol/farmacologia , Isoflavonas/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Pirazóis/síntese química , Pirazóis/química , Relação Estrutura-Atividade
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