Shi Zhen-Ting, Bao Hai-Ying, Feng Shuang
College of Chinese Medicine Material, Jilin Agricultural University, Changchun 130118, China.
Engineering Research Center of Chinese Ministry of Education for Edible and Medicinal Fungi, Jilin Agricultural University, Changchun 130118, China.
Zhongguo Zhong Yao Za Zhi. 2017 Mar;42(5):915-922. doi: 10.19540/j.cnki.cjcmm.20170121.017.
Seven lanostane-type triterpenes including fomitopsin C(1),3-keto-dehydrosulfurenic acid(2),dehydroeburiconic acid(3),3-acetyloxylanosta-8, 24-dien-21-oic acid(4),pinicolic acid A(5),trametenolic acid B(6),and eburicoic acid(7),were isolated from the fruitbodies of Fomitopsis pinicola and F. officinalis. In vitro assay, all compounds were evaluated against MCF-7, HeLa, HepG2 and A549 cells lines using the MTT assay and the structure-activity relationship of antitumor activity was discussed. The results showed that the seven compounds were more sensitive to MCF-7 cells.The IC₅₀ value for MCF-7 was 2<5<4<1<3<6<7. H22 tumor mouse model was used to assay compounds 2, 3, 4 and 5 in vivo. Compounds 2 and 4 had obvious effect and the necrosis area and measurement were positively correlated. The results showed that compounds 2, 4 and 5 had significant antitumor activities at a dose of 20 mg•L⁻¹ with 65.31%, 56.71%, 58.72% suppression, respectively, approaching to CTX group with 69.19% suppression in subcutaneous H22-implanted mice.The results showed that these compounds had significant against the expression of VEGF, cytokines IL-4 and IFN-γ tumor, additionally, the structure-activity relationship of lanostane-type triterpenes indicated that the acetoxyl or carbonyl at C-3 and hydroxy at C-15 can enhance the antitumor activity.
从松杉灵芝和药用拟层孔菌子实体中分离出7种羊毛甾烷型三萜，包括硫黄多孔菌素C（1）、3-酮-脱氢硫黄酸（2）、脱氢齿孔酸（3）、3-乙酰氧基羊毛甾-8,24-二烯-21-酸（4）、松萝酸A（5）、雷尼酸B（6）和齿孔酸（7）。体外实验中，采用MTT法对所有化合物针对MCF-7、HeLa、HepG2和A549细胞系进行了评估，并讨论了其抗肿瘤活性的构效关系。结果表明，这7种化合物对MCF-7细胞更为敏感。MCF-7的IC₅₀值为2<5<4<1<3<6<7。利用H22肿瘤小鼠模型对化合物2、3、4和5进行体内实验。化合物2和4有明显效果，坏死面积与测量值呈正相关。结果表明，化合物2、4和5在剂量为20 mg•L⁻¹时具有显著的抗肿瘤活性，抑制率分别为65.31%、56.71%、58.72%，接近CTX组在皮下接种H22小鼠中的69.19%抑制率。结果表明，这些化合物对VEGF、细胞因子IL-4和肿瘤IFN-γ的表达有显著抑制作用，此外，羊毛甾烷型三萜的构效关系表明，C-3位的乙酰氧基或羰基以及C-15位的羟基可增强抗肿瘤活性。
