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Atalantiaphyllines A-G,来自于单叶吴茱萸 Atalantia monophylla DC. 的 苯丙素 acridones 及其芳香酶抑制和细胞毒性活性。

Atalantiaphyllines A-G, prenylated acridones from Atalantia monophylla DC. and their aromatase inhibition and cytotoxic activities.

机构信息

Laboratory of Natural Products, Chulabhorn Research Institute, Kamphaeng Phet 6 Road, Laksi, Bangkok, 10210, Thailand.

Laboratory of Medicinal chemistry, Chulabhorn Research Institute, Kamphaeng Phet 6 Road, Laksi, Bangkok, 10210, Thailand; Program in Chemical Sciences, Chulabhorn Graduate Institute, Chulabhorn Royal Academy, Kamphaeng Phet 6 Road, Laksi, Bangkok, 10210, Thailand; Center of Excellence on Environmental Health and Toxicology (EHT), CHE, Ministry of Education, Bangkok, 10400, Thailand.

出版信息

Phytochemistry. 2020 Dec;180:112525. doi: 10.1016/j.phytochem.2020.112525. Epub 2020 Oct 1.

Abstract

Seven previously undescribed acridones, named atalantiaphyllines A-G, along with twenty-six known compounds were isolated from the dichloromethane extracts of roots and stems of Atalantia monophylla DC. Their structures were elucidated by analysis of extensive NMR and HRMS data. Aromatase inhibition, cytotoxicity against MOLT-3, HepG2, A549 and HuCCA-1 cell lines and DPPH radical scavenging activity of these compounds were evaluated. Most of the tested acridones exhibited higher potency in inhibiting aromatase than the positive control, ketoconazole, with IC values in the range of 0.08-2.0 μM. In the cytotoxicity assay, cycloataphylline A, N-methylbuxifoliadine E and atalantiaphylline G were selectively cytotoxic against MOLT-3 cell line with IC values of 8.0, 5.4 and 9.8 μM, respectively, while only atalaphyllidine exhibited highest antioxidant activity as evaluated by DPPH free radical scavenging assay with an IC value of 22.4 μM.

摘要

从萝藦科娃儿藤属植物南山藤的根和茎的二氯甲烷提取物中分离得到了 7 个以前未描述的吖啶酮类化合物,命名为阿塔拉烯 A-G,以及 26 个已知化合物。通过分析广泛的 NMR 和 HRMS 数据阐明了它们的结构。评估了这些化合物对芳香酶的抑制作用、对 MOLT-3、HepG2、A549 和 HuCCA-1 细胞系的细胞毒性以及 DPPH 自由基清除活性。大多数测试的吖啶酮类化合物对芳香酶的抑制活性均高于阳性对照酮康唑,IC 值范围为 0.08-2.0 μM。在细胞毒性测定中,环阿塔菲林 A、N-甲基布西非利定 E 和阿塔拉烯 G 对 MOLT-3 细胞系具有选择性细胞毒性,IC 值分别为 8.0、5.4 和 9.8 μM,而只有阿塔拉定具有最高的抗氧化活性,DPPH 自由基清除试验的 IC 值为 22.4 μM。

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