RESUMO
The phytochemical study of Euphorbia resinifera afforded 18 structurally diverse diterpenoids, including 14 new ingol-type diterpenoids, euphorblins A-N (1-14), a new rhamnofolane diterpenoid, euphorblin O (15), and three known analogues (16-18). The structures of these compounds were deduced using 2D NMR spectroscopy and NOE experiments. The structure of compound 1 was confirmed by single-crystal X-ray crystallography. The abilities of the compounds to enhance lysosomal biosynthesis were evaluated through LysoTracker Red staining. Among the 10 active compounds, compounds 2, 4, and 18 showed remarkable immunofluorescence strength, and their LysoTracker staining intensities were 155.9%, 143.5%, and 140.7%, respectively, greater than that of the control. A series of lysosomal genes were also found to be upregulated by these compounds, which further confirms their ability to induce lysosome biosynthesis and suggests that these diterpenoids have potential as lead compounds for the development of drugs for the treatment of lysosome-related diseases.
Assuntos
Diterpenos/química , Diterpenos/farmacologia , Euphorbia/química , Lisossomos/efeitos dos fármacos , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Cristalografia por Raios X/métodos , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Células HeLa , Humanos , Espectroscopia de Ressonância Magnética/métodos , Ressonância Magnética Nuclear Biomolecular/métodosRESUMO
Ten new nortriterpenes, euphorbiumrins A-J (1-10), together with three known analogues (11-13) were isolated from the latex of Euphorbia resinifera. Their structures were established on the basis of extensive spectroscopic analyses (IR, UV, HRESIMS, 1D and 2D NMR). Their inhibitions on tomato yellow leaf curl virus (TYLCV) were evaluated and compound 5 exhibited significant anti-TYLCV activity with an inhibition rate of 71.7% at concentration of 40 µg/mL.
Assuntos
Begomovirus/efeitos dos fármacos , Euphorbia/química , Doenças das Plantas/prevenção & controle , Triterpenos/farmacologia , China , Látex/química , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Doenças das Plantas/virologia , Nicotiana/virologia , Triterpenos/isolamento & purificaçãoRESUMO
Twenty-two diterpenoids (1-22), including two new ones (1, a tigliane-type diterpenoid and 8, an abietane-type diterpenoid) were isolated from the roots of Euphorbia fischeriana Steud. Among them, compounds 4, 7, 12, 14-16, 19-21 are isolated from this plant for the first time. Their structures were elucidated through extensive 1D, 2D NMR and the HRESIMS data. The 13C data of 4 is hereby presented for the first time. The macrocyclic diterpenes 1 and 2 showed marked enhancement of lysosomal biosynthesis after evaluation using lysoTracker staining method.