RESUMO
The phytochemical investigation of the EtOAc extract from the aerial parts of Isodon eriocalyx afforded seventeen diterpenoids, including eight undescribed compounds. Eriocalyxins H-L have unique structural characteristics featuring a 5-epi-ent-kaurane diterpenoid scaffold with eriocalyxins H-K also possess an unusual 6,11-epoxyspiro-lactone ring while eriocalyxin L, a 1,7:3,20-diepoxy-ent kaurene, features an 1,7-oxygen linkage. The structures of these compounds were elucidated by spectroscopic data interpretation, and the absolute configurations of eriocalyxins H, I, L, and M were confirmed by single-crystal X-ray diffraction. The isolates were screened for their inhibitory activities against VCAM-1 and ICAM-1 at 5 µM. While eriocalyxin O, coetsoidin A and laxiflorin P were found to significantly inhibit both VCAM-1 and ICAM-1, 8 (17),13-ent-labdadien-15 â 16-lactone-19-oic acid displayed evidently inhibitory effect against ICAM-1.
Assuntos
Antineoplásicos Fitogênicos , Diterpenos do Tipo Caurano , Diterpenos , Isodon , Diterpenos do Tipo Caurano/farmacologia , Diterpenos do Tipo Caurano/química , Isodon/química , Molécula 1 de Adesão Intercelular/análise , Molécula 1 de Adesão de Célula Vascular/análise , Antineoplásicos Fitogênicos/química , Diterpenos/química , Componentes Aéreos da Planta/química , Estrutura Molecular , Ensaios de Seleção de Medicamentos AntitumoraisRESUMO
Two previously undescribed 7, 20-epoxy-ent-kauranes along with six known ent-kauranoids, were isolated from the aerial parts of Isodon eriocalyx. The structures of new compounds were established on the basis of extensive spectroscopic analyses. Compound 2 could inhibit the production of interleukin - 1ß (IL - 1ß) in monosodium urate (MSU) and lipopolysaccharide (LPS) induced macrophages.