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番荔枝内酯类化合物基于耐阿霉素肝癌细胞SMMC―7721ADR的构效关系研究
[摘要] 研究12种番荔枝内酯类化合物对耐阿霉素肝癌细胞SMMC-7721/ADR的作用,并初步探究其构效关系。实验利用实时荧光定量PCR法检测12种番荔枝内酯类化合物:annosquamin A(1),annosquamin B(2),annotemoyin-1(3),uvariamicin Ⅱ(4),annosquacin D(5),annosquacin B(6),isodesacetyluvaricin(7),uvarigrandin A(8),squamostatin D(9),squamostatin E(10),squamostatin A(11),12,15-cis-squamostatin A(12)对SMMC-7721/ADR细胞中相关基因NDUFV2的表达量。该研究发现所有受试化合物均使SMMC-7721/ADR中NDUFV2表达量有所下调,邻双四氢呋喃环型番荔枝内酯活性最强,而间双四氢呋喃环型番荔枝内酯活性最弱。内酯环与邻近的四氢呋喃环间碳数越少,作用越强;对于邻双四氢呋喃型番荔枝内酯化合物,链上含有的羟基个数越多,化合物作用可能越强;对于间双四氢呋喃型番荔枝内酯化合物,链上含有的羟基个数越少,化合物作用可能越强;且受试化合物中均是含有3个羟基取代的化合物作用较强;相对构型为苏式的番荔枝内酯的作用比赤式的强,四氢呋喃环为顺式构型的番荔枝内酯的作用比反式的强;在其他基团完全相同的情况下,长链烷基端部与邻近的四氢呋喃环之间的碳数越少,作用越强。
[关键词] 番荔枝内酯;多药耐药;SMMC-7721/ADR;构效关系
[Abstract] The present research was launched to investigate the effects of 12 annonaceous acetogenins (ACGs) on human hepatic carcinoma cell line SMMC-7721/ADR, and to find out their structure-activity relationship. SMMC-7721/ADR cells were treated with 12 ACGs including annosquamin A(1),annosquamin B(2),annotemoyin-1(3),uvariamicin Ⅱ(4),annosquacin D(5),annosquacin B(6),isodesacetyluvaricin(7),uvarigrandin A(8),squamostatin D(9),squamostatin E(10),squamostatin A(11),and 12,15-cis-squamostatin A(12) for 24 h, and the different expression of the target gene NDUFV2 were detected by quantitative real-time PCR. All the tested compounds made the expression of the target gene NDUFV2 decreased on human hepatic carcinoma cell line SMMC-7721/ADR, of which the bistetrahydrofuran ACGs showed the best activity,which the non-adjacent bistetrahydrofuran ACGs displayed the worst activity.The ACGs with the reducing number of carbons between γ-unsaturated lactone and the close tetrahydrofuran (THF) ring are more potent. For bistetrahydrofuran ACGs with the same nucleus skeleton,they would be more active as more hydroxyls on aliphatic chain, which for the non-adjacent bistetrahydrofuran ACGs with less hydroxyls on aliphatic chain that would be more active. ACGs with 3 h
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