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Prenylated chromones and flavonoids from Artocarpus heterophyllus with their potential antiproliferative and anti-inflammatory activities.
Bioorganic Chemistry ( IF 5.1 ) Pub Date : 2020-06-20 , DOI: 10.1016/j.bioorg.2020.104030
Yan-Ping Liu 1 , Xiao-Mei Yu 1 , Wei Zhang 1 , Ting Wang 1 , Bo Jiang 1 , Hao-Xuan Tang 1 , Qin-Ting Su 1 , Yan-Hui Fu 1
Affiliation  

Two new prenylated chromones, artoheterophines A (1) and B (2), five known prenylated chromones (37), as well as five known biogenetically related prenylated flavonoids (812) were isolated and characterized from the stems and leaves of A. heterophyllus. Their chemical structures were unambiguously determined through comprehensive spectral data analyses. The antiproliferative and anti-inflammatory effects of all these isolated prenylated chromones and flavonoids were evaluated in vitro. As a result, compounds 112 showed notable inhibitory effects against various human cancer cell lines with IC50 values ranging from 0.36 ± 0.02 to 22.09 ± 0.16 μM. Meanwhile, compounds 112 exhibited significant inhibitory activities on nitric oxide (NO) production holding IC50 values in the range of 0.48 ± 0.05–19.87 ± 0.21 µM. These research results suggest that the isolation and characterization of these prenylated chromones (17) and flavonoids (812) holding significant antiproliferative and anti-inflammatory activities could be significant to the discovery and development of new natural anti-tumor and anti-inflammatory drugs. The findings also provides a phytochemical evidence for further development and utilization of the stems and leaves of A. heterophyllus in health and pharmaceutical products.



中文翻译:

面包果的异戊烯基色酮和类黄酮具有潜在的抗增殖和抗炎活性。

两个新的异戊烯化色酮类,artoheterophines A(1)和B(2),5个已知异戊二烯化色酮(3 - 7),以及5种已知biogenetically相关异戊二烯化黄酮类化合物(8 - 12)的分离和表征从茎和叶A.太子参。通过全面的光谱数据分析明确确定了它们的化学结构。在体外评估了所有这些分离的异戊二烯酮色酮和类黄酮的抗增殖和抗炎作用。结果,化合物112表现出对各种人类癌细胞系的显着抑制作用,IC 50值为0.36±0.02至22.09±0.16μM。同时,化合物112对一氧化氮(NO)的生产表现出显着的抑制活性,保持IC 50值为0.48±0.05–19.87±0.21 µM。这些研究结果表明,这些烯丙基化色酮(17)和类黄酮(812)的分离和表征)具有重要的抗增殖和抗炎活性,对于发现和开发新的天然抗肿瘤和抗炎药物可能具有重要意义。该发现还为进一步开发和利用健康和医药产品中农杆菌的茎和叶提供了植物化学证据。

更新日期:2020-06-29
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