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Atalantiaphyllines A-G, prenylated acridones from Atalantia monophylla DC. and their aromatase inhibition and cytotoxic activities
Phytochemistry ( IF 3.8 ) Pub Date : 2020-12-01 , DOI: 10.1016/j.phytochem.2020.112525
Phanruethai Pailee , Hunsa Prawat , Poonsakdi Ploypradith , Chulabhorn Mahidol , Somsak Ruchirawat , Vilailak Prachyawarakorn

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 IC50 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 IC50 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 IC50 value of 22.4 μM.

中文翻译:

Atalantiaphyllines AG,​​来自 Atalantia monophylla DC 的异戊二烯化吖啶酮。以及它们的芳香化酶抑制和细胞毒活性

从 Atalantia monophylla DC 的根和茎的二氯甲烷提取物中分离出 7 种以前未描述的吖啶酮,命名为 atalantiaphyllines AG,​​以及 26 种已知化合物。它们的结构通过对大量 NMR 和 HRMS 数据的分析得到阐明。评估了芳香酶抑制、对 MOLT-3、HepG2、A549 和 HuCCA-1 细胞系的细胞毒性以及这些化合物的 DPPH 自由基清除活性。大多数测试的吖啶酮在抑制芳香酶方面表现出比阳性对照酮康唑更高的效力,IC50 值在 0.08-2.0 μM 的范围内。在细胞毒性试验中,cycloataphylline A、N-methylbuxifoliadine E 和 atalantiaphylline G 对 MOLT-3 细胞系具有选择性的细胞毒性,IC50 值分别为 8.0、5.4 和 9.8 μM,
更新日期:2020-12-01
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