七种先前未描述的羊毛甾烷三萜类化合物,灵芝酸M1(1),M2(2),M3(3),M4(4),M5(5),M6(6),M7(7)连同八种已知的化合物,从担子菌灵芝(Ganoderedaceae)的菌丝体中分离。通过光谱分析阐明了所有化合物的结构。提出了这15种三萜类化合物可能的生物合成途径。通过测量一氧化氮(NO)的产生来评估某些化合物的抗炎活性。TNF-α,脂多糖诱导的RAW264.7巨噬细胞和IL-6。Lanosta-7,9(11),24-三en-3β,15α,22β-三乙酰氧基-26-酸(14)对NO产生的抑制作用最强,IC50为0.6±0.1μM,在10μM时完全抑制TNF-α和IL-6的分泌。讨论了抗炎活性的构效关系。
Seven previously undescribed lanostane triterpenoids, ganoderic acid M1 (1), M2 (2), M3 (3), M4 (4), M5 (5), M6 (6), and M7 (7), together with eight known compounds, were isolated from mycelia of the basidiomycete Ganoderma sinense (
Ganodermataceae). The structures of all compounds were elucidated by spectroscopic analysis. The possible biosynthetic pathway of these fifteen triterpenoids was proposed. Some of the compounds were evaluated for their anti-inflammatory activity by measuring the production of nitric oxide (NO), TNF-α, and IL-6 in RAW264.7 macrophage cells induced by lipopolysaccharide. Lanosta-7,9(11),24-trien-3β,15α,22β-triacetoxy-26-oic acid (14) exhibited the strongest inhibition of NO production with an IC50 of 0.6 ± 0.1 μM and completely inhibited the secretion of TNF-α and IL-6 at 10 μM. The structure-activity relationship of the anti-inflammatory activity is discussed.