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New derivatives of a natural nordentatin
Open Chemistry ( IF 2.1 ) Pub Date : 2020-08-03 , DOI: 10.1515/chem-2020-0149
Tin Myo Thant 1, 2 , Nanik Siti Aminah 1 , Alfinda Novi Kristanti 1 , Rico Ramadhan 1 , Hnin Thanda Aung 3 , Yoshiaki Takaya 4
Affiliation  

Abstract New derivatives were obtained from natural nordentatin (1) previously isolated from the methanol fraction of Clausena excavata by an acylation method. Herein, we report ten new pyranocoumarin derivatives 1a–1j. Their structures were elucidated based on UV-vis, FT-IR, NMR, and DART-MS data. The α-glucosidase inhibition and anticancer activities of nordentatin (1) and its derivatives were also evaluated. The α-glucosidase inhibition assay exhibited that the derivatives 1b, 1d, 1e, 1f, 1h, 1i, and 1j possess higher inhibitory activity for α-glucosidase with IC50 values of 1.54, 9.05, 4.87, 20.25, 12.34, 5.67, and 2.43 mM, whereas acarbose was used as the positive control, IC50 = 7.57 mM. All derivatives exhibited a weak cytotoxicity against a cervical cancer (HeLa) cell line with the IC50 between 0.25 and 1.25 mM. They also showed moderate to low growth inhibition of a breast cancer (T47D) cell line with IC50 values between 0.043 and 1.5 mM, but their activity was lower than that of the parent compound, nordentatin (1) (IC50 = 0.041 mM).

中文翻译:

天然去甲齿素的新衍生物

摘要 从先前通过酰化方法从 Clausena excavata 的甲醇组分中分离的天然去甲齿素 (1) 中获得了新的衍生物。在此,我们报告了十种新的吡喃香豆素衍生物 1a-1j。基于紫外-可见光、傅里叶变换红外、核磁共振和 DART-MS 数据阐明了它们的结构。还评估了去甲牙本质 (1) 及其衍生物的 α-葡萄糖苷酶抑制和抗癌活性。α-葡萄糖苷酶抑制试验表明衍生物1b、1d、1e、1f、1h、1i和1j对α-葡萄糖苷酶具有较高的抑制活性,IC50值为1.54、9.05、4.87、20.25、12.34、5.2673 mM,而阿卡波糖用作阳性对照,IC50 = 7.57 mM。所有衍生物对宫颈癌 (HeLa) 细胞系均表现出微弱的细胞毒性,IC50 介于 0.25 和 1.25 mM 之间。
更新日期:2020-08-03
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