RESUMO
Four new tirucallane-type triterpenoids, polystanins H-K (1-4), were obtained from the stems and leaves of Aphanamixis polystachya. Their structures were elucidated by analysis of the spectroscopic data and comparison with literature data. Compounds 1 and 2 showed week inhibitory effects against NO production in LPS-stimulated RAW264.7 cells. All the isolates were investigated for their antifungal activities against drug-resistant Candida albicans.
Assuntos
Antifúngicos , Candida albicans , Óxido Nítrico , Triterpenos , Triterpenos/química , Triterpenos/farmacologia , Triterpenos/isolamento & purificação , Camundongos , Animais , Estrutura Molecular , Candida albicans/efeitos dos fármacos , Células RAW 264.7 , Óxido Nítrico/biossíntese , Óxido Nítrico/antagonistas & inibidores , Antifúngicos/farmacologia , Antifúngicos/química , Antifúngicos/isolamento & purificação , Folhas de Planta/química , Testes de Sensibilidade Microbiana , Lipopolissacarídeos/farmacologia , Meliaceae/química , Caules de Planta/química , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/isolamento & purificaçãoRESUMO
Nineteen triterpenoids, including five previously unknown (four triucallane-type derivatives and one highly oxidized A, B-seco limonoids), together with fourteen known triterpenoids, were isolated from the fruits of Aphanamixis polystachya. Their structures were elucidated by extensive spectroscopic analysis. All isolates were evaluated their anti-inflammatory activities. The result showed that all compounds inhibit LPS-induced nitric oxide production in RAW264.7 macrophages with their IC50 value ranging from 95 to 1332 uM, and compound 6 exhibited obvious anti-inflammatory activity comparable to that of the positive control, with IC50 values of 94.96 uM.
Assuntos
Meliaceae , Triterpenos , Frutas/química , Triterpenos/farmacologia , Óxido Nítrico , Estrutura Molecular , Meliaceae/química , Anti-Inflamatórios/farmacologiaRESUMO
Two new triucallane triterpenoids, polystanin F (1) and polystanin G (2), along with eight known compounds (3-10) were isolated from the fruits of Aphanamixis polystachya. Their structures were established on the basis of extensive spectroscopic analysis. Moreover, eight compounds were evaluated for their in vitro cytotoxicity against three cancer cell lines (liver cancer RT112, colon cancer HCT-116 and breast cancer M231) using the MTT method. Compound 7 showed significant cytotoxic activity against HCT-116 with IC50 1.27 µM.
Assuntos
Limoninas , Meliaceae , Triterpenos , Frutas/química , Limoninas/química , Meliaceae/química , Estrutura Molecular , Triterpenos/análise , Triterpenos/farmacologiaRESUMO
MicroRNA (miR)138 serves an important role in the proliferation, differentiation and apoptosis of human pulmonary artery smooth muscle cells (HPASMCs), indi-cating the involvement of miR138 in the development and progression of pulmonary artery hypertension (PAH). Potassium channel subfamily K member 3 (TASK1), a twopore domain K+ channel, is expressed in HPASMCs and is associated with hypoxic PAH. However, whether miR138 mediates PAH through targeting TASK1 is not known. In the present study, HPASMCs were transfected with miR138 mimic to establish a PAH model in vitro, and the effects of a miR138 inhibitor and a TASK1 inhibitor (A293) were examined. Cell proliferation and mitochondrial membrane potential (MMP) were measured by CCK8 assay and flow cytometry, respectively. Reverse transcription-quantitative polymerase chain reaction and western blotting were performed to examine the expression of miR138, TASK1, Bcl2, caspase3 and activation of extracellular signalregulated kinase 1/2 (ERK1/2). A dualluciferase reporter assay was also used to analyse the expression level of TASK1 in HPASMCs. The results of the present study demonstrated that the miR138 mimic promoted proliferation and MMP level, which was similar to the effect of A293 treatment on HPASMCs. However, the miR138 inhibitor inhibited the effects induced by miR138 mimic or A293 treatment, as demonstrated by a decrease in proliferation and MMP level in HPASMCs, accompanied by a decrease of Bcl2 and an increase of caspase3 expression levels, as well as ERK1/2 activation. The dualluciferase reporter assay indicated that TASK1 expression was negatively regulated by miR138. The results of the present study suggested that miR138 promoted proliferation and suppressed mitochondrial depolarization of HPASMCs by targeting TASK1.