RESUMO
Three new cyclohexapeptides, petrosamides A-C (1-3), were isolated from the sponge-derived fungus Aspergillus sp. 151304. Their structures were elucidated by detailed 1D and 2D spectroscopic analyses, and the absolute configurations of the amino acid residues were determined by the advanced Marfey's method. These peptides displayed significant and dose-dependent pancreatic lipase (PL) inhibitory activities, with IC50 values of 7.6 ± 1.5, 1.8 ± 0.3, and 0.5 ± 0.1 µM, respectively. Further inhibition kinetics analyses showed that compound 3 inhibited PL in a noncompetitive manner, while molecular dynamics simulation revealed that it could bind to PL at the entrance of the catalytic pocket.
Assuntos
Aspergillus/isolamento & purificação , Inibidores Enzimáticos/farmacologia , Lipase/antagonistas & inibidores , Biologia Marinha , Oligopeptídeos/farmacologia , Pâncreas/enzimologia , Peptídeos Cíclicos/farmacologia , Poríferos/microbiologia , Animais , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Inibidores Enzimáticos/química , Humanos , Simulação de Acoplamento Molecular , Estrutura Molecular , Oligopeptídeos/química , Peptídeos Cíclicos/químicaRESUMO
Two new sorbicillinoids, 13-hydroxy-dihydrotrichodermolide (1) and 10,11,27,28-tetrahydrotrisorbicillinone C (2), were isolated from the sponge-derived fungus Penicillium chrysogenum 581F1. Their structures were determined on the basis of spectroscopic analysis. Compounds 1 and 2 displayed high affinities to target proteins GLP-1R (diabetes) and eEF2K (cancer) with Kd values of 0.0285 µM, 0.0162 µM for GLP-1R and 0.118 µM, 0.0746 µM for eEF2K, respectively.
Assuntos
Cicloexanonas/química , Quinase do Fator 2 de Elongação/metabolismo , Receptor do Peptídeo Semelhante ao Glucagon 1/metabolismo , Penicillium chrysogenum/química , Animais , Cicloexanonas/isolamento & purificação , Cicloexanonas/metabolismo , Humanos , Estrutura Molecular , Poríferos/microbiologiaRESUMO
A new trienic α-pyrone derivative asteltoxin G (1) bearing a tetrahydrofuran ring and a new ochratoxin derivative named ochratoxin A1 (5), along with seven known compounds, were isolated from a sponge-derived fungus Aspergillus ochraceopetaliformis. The compounds (1-9) were evaluated on the basis of spectroscopic analyses and comparison with those of the reported data. The new compound ochratoxin A1 (5) exhibited anti-inflammatory activity against IL-6 and TNF-α expression of the LPS-induced THP-1 cells with inhibitory rates of 74.4 and 67.7% at concentration of 10 µM, respectively.
Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Aspergillus/química , Ocratoxinas/química , Pironas/química , Animais , Anti-Inflamatórios não Esteroides/química , Linhagem Celular , Avaliação Pré-Clínica de Medicamentos , Humanos , Interleucina-6/metabolismo , Lipopolissacarídeos/farmacologia , Estrutura Molecular , Ocratoxinas/farmacologia , Poríferos/microbiologia , Pironas/farmacologia , Fator de Necrose Tumoral alfaRESUMO
Three new cytochalasins Z24 , Z25 , Z26 (1-3, resp.) and one known compound, scoparasin B (4), were isolated from the fungus Eutypella sp. D-1 isolated from the soil of high latitude of the Arctic. The structures of 1-3 were elucidated from spectroscopic data (NMR, MS). These compounds were evaluated for cytotoxic activities against several human tumor cell lines. Among them, compound 1 exhibited moderate cytotoxicity toward human breast cancer MCF-7 cell line with IC50 of 9.33 µM.
Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Citocalasinas/química , Citocalasinas/farmacologia , Xylariales/química , Antineoplásicos/isolamento & purificação , Linhagem Celular Tumoral , Citocalasinas/isolamento & purificação , Humanos , Células MCF-7 , Neoplasias/tratamento farmacológico , Tirosina/químicaRESUMO
Two new diterpenes, libertellenone G(1) and libertellenone H(2) were isolated from the fungus Eutypella sp. D-1 isolated from the soil of high latitude of Arctic, together with two known pimarane diterpenes (3-4). The structures of 1 and 2 were elucidated from spectroscopic data (nuclear magnetic resonance, mass spectrometry and infrared). These compounds were evaluated for cytotoxic activity against seven human tumor cell lines. Compound 2 showed a range of cytotoxicity between 3.31 and 44.1 µM. Compound 1 exhibited antibacterial activity against Escherichia coli, Bacillus subtilis and Staphylococcus aureus.
Assuntos
Abietanos/farmacologia , Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Diterpenos/farmacologia , Xylariales/química , Abietanos/química , Abietanos/isolamento & purificação , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Regiões Árticas , Bacillus subtilis/efeitos dos fármacos , Linhagem Celular Tumoral , Diterpenos/química , Diterpenos/isolamento & purificação , Descoberta de Drogas , Escherichia coli/efeitos dos fármacos , Humanos , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Testes de Sensibilidade Microbiana , Estrutura Molecular , Microbiologia do Solo , Staphylococcus aureus/efeitos dos fármacosRESUMO
Polar regions are remote and challenging areas on the earth. In view of the unique environment and the severe competition in polar regions, it's considered that the ecological system might be the producer of new compounds with diversity biological activities. This review is an attempt to consolidate the studies about 97 natural products isolated from Antarctic and Arctic organisms including microbes, algae, sponges, bryozoans, and tunicates and so on published in the recent years. The emphasis is mainly about the new compounds, source organisms and biological activities, which signifies the immense competence of Antarctic and Arctic organisms as bioactive natural products producers.
