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1.
J Agric Food Chem ; 68(1): 17-32, 2020 Jan 08.
Artigo em Inglês | MEDLINE | ID: mdl-31809036

RESUMO

Weeds had caused significant loss for crop production in the process of agriculture. Herbicides have played an important role in securing crop production. However, the high reliance on herbicides has led to environmental issues as well as the evolution of herbicide resistance. Thus, there is an urgent need for new herbicides with safer toxicological profiles and novel modes of action. Actinomycetes produce very diverse bioactive compounds, of which some show potent biopesticidal activity. The herbicidal secondary metabolites from actinomycetes can be classified into several groups, such as amino acids, peptides, nucleosides, macrolides, lactones, amide, amines, etc., some of which have been successfully developed as commercial herbicides. The structure diversity and evolved biological activity of secondary metabolites from actinomycetes can offer opportunities for the development of both directly used bioherbicides and synthetic herbicides with new target sites, and thus, this review focuses on the structure, herbicidal activity, and modes of action of secondary metabolites from actinomycetes.


Assuntos
Actinobacteria/química , Herbicidas/química , Herbicidas/farmacologia , Actinobacteria/metabolismo , Descoberta de Drogas , Herbicidas/metabolismo , Plantas Daninhas/efeitos dos fármacos , Plantas Daninhas/crescimento & desenvolvimento , Metabolismo Secundário , Controle de Plantas Daninhas
2.
Org Biomol Chem ; 17(38): 8721-8725, 2019 10 14.
Artigo em Inglês | MEDLINE | ID: mdl-31402366

RESUMO

Two novel sorbicillinoid adducts containing bicyclo[2.2.2]octane and tetrahydrofuran moieties, named sorbicillfurans A and B (1 and 2), were isolated from the static culture of the marine-derived fungus Penicillium citrinum SCSIO41402. Their structures including absolute configurations were determined by spectroscopic and calculated ECD analyses. Sorbicillfurans A and B (1 and 2) are the first examples of sorbicillinoids possessing a tetrahydrofuran unit. In the proposed biosynthetic pathway, sorbicillfuran B (2), harboring a rare and complex polycyclic framework, is probably formed by two Diels-Alder reactions. Both isolates were evaluated for the cytotoxicity against six human cancer cell lines, only sorbicillfuran B (2) showed weak cytotoxicity against HL-60 cells with an IC50 value of 9.6 µM.


Assuntos
Antineoplásicos/farmacologia , Compostos Heterocíclicos/farmacologia , Penicillium/química , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Células HL-60 , Compostos Heterocíclicos/química , Compostos Heterocíclicos/isolamento & purificação , Humanos , Conformação Molecular , Relação Estrutura-Atividade
3.
Org Biomol Chem ; 17(14): 3635-3639, 2019 04 03.
Artigo em Inglês | MEDLINE | ID: mdl-30916700

RESUMO

Oxazoles are an important class of biologically active metabolites from nature, and exhibit broad biological activities as the lead for drug discovery. Hinduchelins are a class of unusual natural products with an oxazole unit, isolated from Streptoalloteichus hindustanus, and with a potential iron-chelating ability. These compounds are the first identified naturally occurring unusual oxazole derivatives to possess a catechol unit. However, some of these compounds are not abundant in nature, and thus, the efficient syntheses of these compounds are advantageous in exploring their potential applications. This paper reports the efficient synthesis and bio-evaluation of hinduchelins A-D and their derivatives with convenient procedures and high yields.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antineoplásicos/farmacologia , Produtos Biológicos/farmacologia , Inseticidas/farmacologia , Oxazóis/farmacologia , Actinomycetales/química , Animais , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Antineoplásicos/síntese química , Antineoplásicos/química , Afídeos/efeitos dos fármacos , Produtos Biológicos/síntese química , Produtos Biológicos/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Fungos/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Humanos , Inseticidas/síntese química , Inseticidas/química , Testes de Sensibilidade Microbiana , Mariposas , Oxazóis/síntese química , Oxazóis/química
4.
Nat Prod Res ; 32(4): 412-417, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-28441878

RESUMO

Further chemical study of secondary metabolites from the soil actinomycete Streptomyces sp. WS-13394 resulted in the isolation of four new alkylated anthraquinone analogues (5-8). Their structures were elucidated on the basis of extensive spectroscopic analysis, including HR-ESI-MS, 1D and 2D NMR. The new compounds, together with analogues obtained before (1-4), were tested for their in vitro cytotoxicity against Huh-7 and SGC-7901.


Assuntos
Antraquinonas/química , Antraquinonas/farmacologia , Antineoplásicos/farmacologia , Streptomyces/química , Alquilação , Antineoplásicos/química , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Microbiologia do Solo , Espectrometria de Massas por Ionização por Electrospray , Relação Estrutura-Atividade
5.
Arch Virol ; 161(11): 3061-72, 2016 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-27518401

RESUMO

The antiviral activity of dehydroepiandrosterone (DHEA) and 21 synthetic derivatives against influenza A virus (IAV) replication was investigated in vitro in cell culture. Our results revealed that three DHEA analogues were potent inhibitors of IAV multiplication in MDCK cells and mainly blocked the post-attachment stage of viral infection. Among these derivatives, one containing a 2-OH-Ph moiety (3i) exhibited the best inhibitory effects against H1N1 and H3N2 IAV in a dose-dependent manner. Moreover, treatment with compound 3i decreased progeny virus yields, viral RNA synthesis and protein expression. Orally administered compound 3i at 25 or 50 mg/kg/day for 5 days protected mice from lethal A/FM/1/47 (H1N1) challenge by reducing the viral titers in the lungs and promoting survival of infected mice. Our results suggest that DHEA-dihydrazone derivatives may provide promising lead scaffolds for further design and synthesis of potential antiviral agents.


Assuntos
Antivirais/farmacologia , Desidroepiandrosterona/análogos & derivados , Desidroepiandrosterona/farmacologia , Vírus da Influenza A/efeitos dos fármacos , Vírus da Influenza A/fisiologia , Animais , Antivirais/uso terapêutico , Desidroepiandrosterona/uso terapêutico , Modelos Animais de Doenças , Cães , Humanos , Células Madin Darby de Rim Canino , Camundongos Endogâmicos BALB C , Infecções por Orthomyxoviridae/tratamento farmacológico , Análise de Sobrevida , Resultado do Tratamento , Replicação Viral/efeitos dos fármacos
6.
J Antibiot (Tokyo) ; 68(3): 185-90, 2015 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-25204346

RESUMO

Two new 32-membered macrolide compounds, named Novonestmycins A (1) and B (2), were isolated from the soil strain Streptomyces phytohabitans HBERC-20821. Their structures were elucidated by using spectroscopic methods, including 1D, 2D-NMR and MS spectrometry. The two compounds showed strong activities against the phytophathogenic fungi Corynespora cassiicola, Rhizoctonia solani and Septoria nodorum, with MIC values of 0.78, 0.39 and 0.78 µg ml(-1), respectively. In addition, the two compounds exhibited potent inhibitory activities against four different human tumor cell lines as well as one 5-FU-resistant human hepatocellular carcinoma cell line, with IC50 of 0.15-0.48 µg ml(-1) and 0.24-1.34 µg ml(-1), respectively.


Assuntos
Antibacterianos/isolamento & purificação , Macrolídeos/isolamento & purificação , Microbiologia do Solo , Antibacterianos/química , Antibacterianos/farmacologia , Antibióticos Antineoplásicos/química , Antibióticos Antineoplásicos/isolamento & purificação , Antibióticos Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Humanos , Macrolídeos/química , Macrolídeos/farmacologia , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Streptomyces/metabolismo
7.
Chem Pharm Bull (Tokyo) ; 62(1): 118-21, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24390501

RESUMO

Four new alkylated anthraquinone analogues (1-4) were isolated from a soil actimomycete Streptomyces sp. WS-13394. The structures of compounds 1-4 were elucidated to be 1,4,6-trihydroxy-8-alkylanthraquinones by means of spectroscopic methods, including UV, one dimensional (1D), 2D-NMR and MS spectrometry. All compounds showed activities against BGC-823 and MCF-7 with IC50 from 0.99 to 3.54 µg/mL, while 2 exhibited cytotoxicity against HepG2, A875, BGC-823 and MCF-7 with IC50 2.29, 4.90, 0.99, and 1.66 µg/mL, respectively.


Assuntos
Actinobacteria/química , Antraquinonas/química , Antraquinonas/farmacologia , Solo/química , Streptomyces/química , Alquilação , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Células Hep G2 , Humanos , Concentração Inibidora 50 , Células MCF-7
8.
Chem Biodivers ; 10(6): 1061-71, 2013 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-23776021

RESUMO

Four highly acylated diterpenoids, designated as pierisformotoxins A-D (1-4, resp.), along with 26 known compounds, were isolated from the flowers of Pieris formosa. Among them, pierisformotoxins A and B (1 and 2, resp.) were new highly acylated grayanane diterpenoids, of which the five-membered ring A has undergone an oxidative cleavage between C(3) and C(4), followed by lactonization, to give rise to a five-membered lactone ring between C(3) and C(5), differing from the previously reported grayanane diterpenoids with a 5/7/6/5 ring system. Results of the cAMP-regulation-activity assay showed that pierisformotoxin C (3) at 10 µM (inhibitory ratio (IR): 10.1%) or 2 µM (9.8%), and pierisformotoxin B (2) at 50 µM (13.9%) significantly decreased the cAMP level in N1E-115 neuroblastoma cells (p<0.05).


Assuntos
Diterpenos/química , Ericaceae/química , Animais , Linhagem Celular Tumoral , AMP Cíclico/metabolismo , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Flores/química , Espectroscopia de Ressonância Magnética , Camundongos , Conformação Molecular , Neurônios/efeitos dos fármacos
9.
Chem Biodivers ; 8(6): 1182-7, 2011 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-21674790

RESUMO

Phytochemical studies on the branches and leaves of Lyonia ovalifolia yielded a new grayanane diterpenoid, lyonin A (1), together with two known compounds, secorhodomollolides A and D (2 and 3, resp.). The structure of 1 was elucidated by combination of 1D- and 2D-NMR, and MS analyses. Compound 1 turned out to be a new, highly O-acylated grayanane diterpenoid, of which ring B has undergone an oxidative cleavage between C(9) and C(10), yielding a system differing from the previously reported grayanane type with a 5/7/6/5 ring system. Results of the cAMP regulation activity assay showed that compounds 2 and 3 at 50 µM induced a significantly decreased cAMP level in N1E-115 neuroblastoma cells (p<0.001), indicating neuropharmacological potential.


Assuntos
Diterpenos/química , Ericaceae/química , Linhagem Celular Tumoral , AMP Cíclico/metabolismo , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Humanos , Espectroscopia de Ressonância Magnética , Conformação Molecular , Folhas de Planta/química , Caules de Planta/química
10.
Chem Pharm Bull (Tokyo) ; 59(4): 492-5, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-21467681

RESUMO

Phytochemical investigation on the fruits of Pieris formosa resulted in the isolation of three new highly acylated 3,4-seco-grayanane diterpenoids, pierisformotoxins E-G (1-3). Their structures were elucidated on the basis of extensive spectroscopic analysis, including 1D-, 2D-NMR, electrospray ionization-mass spectra (ESI-MS) and high resolution (HR)-MS.


Assuntos
Diterpenos/química , Ericaceae/química , Diterpenos/isolamento & purificação , Frutas/química , Espectroscopia de Ressonância Magnética , Conformação Molecular
11.
J Asian Nat Prod Res ; 12(1): 70-5, 2010 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-20390746

RESUMO

A new grayanol diterpenoid, grayanotoxin XXII (1), and a new phenolic glucoside, benzyl 2-hydroxy-4-O-[beta-xylopyranosyl(1'' --> 6')-beta-glucopyranosyl]-benzoate (2), were isolated from the flowers of Pieris formosa. Their structures were determined on the basis of spectroscopic analysis and chemical methods.


Assuntos
Diterpenos/isolamento & purificação , Medicamentos de Ervas Chinesas/isolamento & purificação , Ericaceae/química , Glucosídeos/isolamento & purificação , Fenóis/isolamento & purificação , Diterpenos/química , Medicamentos de Ervas Chinesas/química , Flores/química , Glucosídeos/química , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Fenóis/química
12.
Planta Med ; 75(8): 843-7, 2009 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-19242901

RESUMO

In an attempt to search for bioactive natural products, two new prenylflavonols, 2''-hydroxy-3''-en-anhydroicaritin (1) and 2''-hydroxy-beta-anhydroicaritin (2), were isolated from the Chinese medicinal herb Epimedium brevicornum. Their structures were determined by 1D and 2D NMR spectroscopic analysis. The effects of compounds 1 and 2 on cytokine production in vitro were investigated. Compound 1 could significantly downregulate tumor necrosis factor-alpha (TNF-alpha) production and increase interleukin-10 (IL-10) production. These results suggested that compound 1 may have anti-inflammatory activity in lipopolysaccharide (LPS)-stimulated mouse macrophages. In addition, the biogenetic relationships among compounds 1 and 2 are discussed.


Assuntos
Anti-Inflamatórios/farmacologia , Epimedium/química , Flavonóis/farmacologia , Interleucina-10/metabolismo , Macrófagos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Fator de Necrose Tumoral alfa/metabolismo , Animais , Anti-Inflamatórios/isolamento & purificação , Células Cultivadas , Regulação para Baixo , Flavonóis/química , Flavonóis/isolamento & purificação , Lipopolissacarídeos , Camundongos , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Prenilação
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