RESUMO
Three new cyclopentenone derivatives (1-3) were isolated from the rare actinomycete Actinoalloteichus nanshanensis NEAU 119. Their structures were elucidated by extensive spectroscopic analysis. Compound 1 showed moderate cytotoxic activity against human lung adenocarcinoma cell line A549, human leukemia cell line K562, and human renal carcinoma cell line ACHN with an IC50 of 14.67, 11.87, and 23.36 µg ml(-1), respectively.
Assuntos
Actinobacteria/química , Antineoplásicos/isolamento & purificação , Ciclopentanos/isolamento & purificação , Adenocarcinoma/tratamento farmacológico , Adenocarcinoma de Pulmão , Antineoplásicos/química , Antineoplásicos/farmacologia , Ciclopentanos/química , Ciclopentanos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Ficus/microbiologia , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Estrutura Molecular , RizosferaRESUMO
Four novel cyclopentenone derivatives (1-4), characterising a cyclopentenone ring conjugated with a 1,8-dioxadecalin, were isolated from rare actinobacterial strain Actinoalloteichus nanshanensis sp. nov. NEAU 119. The structures of these compounds were elucidated on the basis of extensive spectroscopic analysis. Bioassays indicated that compounds 1-4 showed low cytotoxicities against human leukaemia cell line K562 and human renal carcinoma cell line ACHN. To the best of our knowledge, this is the first example of isolation of C11 cyclopentenones from actinomycetes.
Assuntos
Actinomycetales/química , Anti-Infecciosos/isolamento & purificação , Ciclopentanos/isolamento & purificação , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Candida albicans/efeitos dos fármacos , Linhagem Celular Tumoral , Ciclopentanos/química , Ciclopentanos/farmacologia , Humanos , Estrutura Molecular , Rhizoctonia/efeitos dos fármacos , Especificidade da Espécie , Análise Espectral , Staphylococcus epidermidis/efeitos dos fármacosRESUMO
Two new metabolites, pyrenocine J (1) and pyrenochaetic acid D (2), together with two known metabolites, pyrenocine A (3) and pyrenochaetic acid A (4), were isolated from a soil fungus, Curvularia affinis strain HS-FG-196. Their structures were established by extensive spectroscopic analysis. Compound 1 showed cytotoxic activity against the human hepatic cancer cell line HepG2 with an IC(50) value of 28.5 µg/ml.
Assuntos
Antineoplásicos/isolamento & purificação , Ascomicetos/química , Pironas/isolamento & purificação , Antineoplásicos/química , Antineoplásicos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Células Hep G2 , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Pironas/química , Pironas/farmacologiaRESUMO
In this study, an endophytic Streptomyces sp. neau-D50 with strong antifungal activity against Phytophthora sojae was isolated from healthy soybean root, using an in vitro screening technique. A bioactivity-guided approach was then employed to isolate and determine the chemical identity of bioactive constituents with antifungal activity from strain neau-D50. The structure of the antifungal metabolite was elucidated as borrelidin on the basis of spectral analysis. To our knowledge, this is the first report that borrelidin has strong antifungal activity against dominant race 1 of P. sojae with EC(50) and EC(95) of 0.0056 and 0.026 mg/L, respectively. The values were respectively 62.5- and 262.3-fold lower than those of the commercial fungicide metalaxyl, which has been used to treat soybean seed for the control of P. sojae . The in situ bioassays demonstrated that borrelidin at 10 mg/L reduced P. sojae race 1 lesions on soybean seedlings by 94.72% without affecting root growth. Thus, borrelidin might be a promising candidate for new antifungal agents against P. sojae.
