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从 K. Schum 茎皮中分离得到的一种新三萜烷衍生物的细胞毒性。

Cytotoxicity of a new tirucallane derivative isolated from K. Schum stem bark.

机构信息

Department of Chemistry, Faculty of Science, University of Maroua, Maroua, Cameroon.

Department of Chemistry, Higher Teachers' Training College, University of Maroua, Maroua, Cameroon.

出版信息

Nat Prod Res. 2021 Nov;35(22):4417-4422. doi: 10.1080/14786419.2020.1723085. Epub 2020 Feb 3.

Abstract

One new tirucallan derivative, leutcharic acid () was isolated from stem bark together with the known compounds 3-oxo-22-hydroxyhopane (), 3,4-secotirucalla-4(28),7,24-trien-3,21-dioic acid (), 3-oxotirucalla-7,24-dien-21-oic acid (), lupeol (), -sitosterol () and stigmasterol (). The structures of the isolated compounds were elucidated using 1 D and 2 D NMR spectroscopy in combination with literature data. To the best of our knowledge, this is the first report on the cytotoxic properties' constituents of . Cytotoxicity of compounds and was assessed with the WST-1 assay on human lung adenocarcinoma A549 and THP-1 human monocytic leukaemia cell lines. Both compounds showed antiproliferative activity on the cancer cells. Compound was more active against THP-1 with an IC value of 26.83 µM. The sensitivity of THP-1 cells to compounds and indicated that these compounds might be potential leads for anticancer agent development against leukaemia.

摘要

从 茎皮中分离得到一个新的 Tirucallan 衍生物,即 leutcharic 酸(),以及已知化合物 3-oxo-22-hydroxyhopane()、3,4-secotirucalla-4(28),7,24-trien-3,21-dioic acid()、3-oxotirucalla-7,24-dien-21-oic acid()、羽扇豆醇()、β-谷甾醇()和豆甾醇()。通过 1D 和 2D NMR 光谱结合文献数据阐明了分离化合物的结构。据我们所知,这是首次报道 Tirucalla 的细胞毒性成分。通过 WST-1 测定法在人肺腺癌细胞 A549 和 THP-1 人单核白血病细胞系上评估了化合物 和 的细胞毒性。这两种化合物对癌细胞均表现出增殖抑制活性。化合物 对 THP-1 的活性更强,IC 值为 26.83µM。THP-1 细胞对化合物 和 的敏感性表明,这些化合物可能是开发针对白血病的抗癌药物的潜在先导化合物。

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