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寄生蕨Cyclosorus parasiticus 的查尔酮衍生物及其抗增殖活性。

Chalcone derivatives from the fern Cyclosorus parasiticus and their anti-proliferative activity.

机构信息

Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College of Huazhong University of Science and Technology, Wuhan 430030, China; Innovation Institute, Huazhong University of Science and Technology, Wuhan 430074, China.

出版信息

Food Chem Toxicol. 2013 Oct;60:147-52. doi: 10.1016/j.fct.2013.07.045. Epub 2013 Jul 26.

Abstract

Three new chalcone derivatives, named parasiticins A-C (1-3), were isolated from the leaves of Cyclosorus parasiticus, together with four known chalcones, 5,7-dihydroxy-4-phenyl-8-(3-phenyl-trans-acryloyl)-3,4-dihydro-1-benzopyran-2-one (4), 2'-hydroxy-4',6'-dimethoxychalcone (5), 2',4'-dihydroxy-6'-methoxy-3',5'-dimethylchalcone (6), 2',4'-dihydroxy-6'-methoxy-3'-methylchalcone (7). The chemical structures of the new isolated compounds were elucidated unambiguously by spectroscopic data analysis. The cytotoxic activities of compounds 1-7 were evaluated against six human cancer cell lines in vitro. Compounds 3 and 6 exhibited substantial cytotoxicity against all six cell lines, especially toward HepG2 with the IC₅₀ values of 1.60 and 2.82 μM, respectively. Furthermore, we demonstrated that compounds 3 and 6 could induce apoptosis in the HepG2 cell line, which may contribute significantly to their cytotoxicity.

摘要

从寄生 Cyclosorus 叶中分离得到了三种新的查尔酮衍生物,分别命名为寄生素 A-C(1-3),此外还分离得到了四种已知的查尔酮,分别为 5,7-二羟基-4-苯基-8-(3-苯基反式丙烯酰基)-3,4-二氢-1-苯并吡喃-2-酮(4)、2'-羟基-4',6'-二甲氧基查尔酮(5)、2',4'-二羟基-6'-甲氧基-3',5'-二甲基查尔酮(6)和 2',4'-二羟基-6'-甲氧基-3'-甲基查尔酮(7)。通过光谱数据分析,明确了新分离化合物的化学结构。评估了化合物 1-7 对六种人癌细胞系的体外细胞毒性。化合物 3 和 6 对所有六种细胞系均表现出显著的细胞毒性,特别是对 HepG2 的 IC₅₀ 值分别为 1.60 和 2.82 μM。此外,我们证明了化合物 3 和 6 可以诱导 HepG2 细胞系凋亡,这可能对它们的细胞毒性有重要贡献。

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