College of Pharmacy, Catholic University of Daegu, Gyeongsan, Gyeongbuk 712-702, Korea.
Arch Pharm Res. 2009 Nov;32(11):1573-9. doi: 10.1007/s12272-009-2109-x.
To determine the anti-complement activity of natural triterpenes, chromatographic separation of the EtOAc-soluble fraction from the fruiting body of Ganoderma lucidum led to the isolation of three steroids and five triterpenoids. They were identified as ergosterol peroxide (1), ergosterol (2), genoderic acid Sz (3), stella sterol (4), ganoderic aic C1 (5), ganoderic acid A (6), methyl ganoderate A (7), and lucidenic acid A (8) based on spectroscopic evidence and physicochemical properties. These compounds were examined for their anti-complement activity against the classical pathway of the complement system. Compounds 2 and 3 showed potent anti-complement activity with IC50 values of 52.0 and 44.6 microM, respectively. Compound 1 exhibited significant inhibitory activity with an IC50 value of 126.8 microM, whereas compounds 4-8 were inactive. Our findings suggested that in addition to the ketone group at C-3, the delta7(8), delta9(11)-lanostadiene type triterpene also plays an important role in inhibiting the hemolytic activity of human serum against erythrocytes.
为了确定天然三萜的抗补体活性,从灵芝子实体的乙酸乙酯可溶部分进行色谱分离,导致分离出三种甾体和五种三萜。它们被鉴定为麦角甾醇过氧化物(1)、麦角甾醇(2)、灵芝酸 Sz(3)、星状甾醇(4)、灵芝酸 C1(5)、灵芝酸 A(6)、甲基灵芝酸 A(7)和灵芝酸 A(8)基于光谱证据和物理化学性质。这些化合物被检测其对补体系统经典途径的抗补体活性。化合物 2 和 3 表现出很强的抗补体活性,IC50 值分别为 52.0 和 44.6 microM。化合物 1 表现出显著的抑制活性,IC50 值为 126.8 microM,而化合物 4-8 则没有活性。我们的研究结果表明,除了 C-3 上的酮基外,delta7(8), delta9(11)-lanostadiene 型三萜还在抑制人血清对红细胞的溶血活性方面发挥重要作用。