当前位置: X-MOL 学术Phytochemistry › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Azaphilones with protein tyrosine phosphatase inhibitory activity isolated from the fungus Aspergillus deflectus
Phytochemistry ( IF 3.8 ) Pub Date : 2020-02-01 , DOI: 10.1016/j.phytochem.2019.112224
Changhong Huo 1 , Xinhua Lu 2 , Zhihui Zheng 2 , Yeying Li 2 , Yan Xu 2 , Haizhou Zheng 2 , Yuanchen Niu 3
Affiliation  

Six undescribed azaphilones, deflectins C1-C3, deflectins D1-D2, and deflectin E, along with five known azaphilones were obtained from a solid culture of the wild fungus Aspergillus deflectus NCC0415. Their structures were determined by HRESIMS, NMR and ECD analyses, together with the GIAO 13C NMR calculation method. All compounds displayed strong or moderate inhibitory activity against protein tyrosine phosphatases SHP2 and PTP1B. Structure-activity relationship analysis of these azaphilones suggested that the length of the ketone aliphatic side chain would affect their SHP2 and PTP1B inhibitory activity. In addition, the presence of a Δ8(12) double bond on γ-lactone ring and the presence of CH3-2' in fatty chains may increase their inhibitory activity.

中文翻译:

从真菌曲霉中分离的具有蛋白质酪氨酸磷酸酶抑制活性的氮杂菲酮

六个未描述的 azaphilones、deflectins C1-C3、deflectins D1-D2 和 deflectin E,以及五个已知的 azaphilones 从野生真菌 Aspergillus deflectus NCC0415 的固体培养物中获得。它们的结构由 HRESIMS、NMR 和 ECD 分析以及 GIAO 13C NMR 计算方法确定。所有化合物都对蛋白酪氨酸磷酸酶 SHP2 和 PTP1B 显示出强或中度的抑制活性。这些 azaphilones 的构效关系分析表明,酮脂肪族侧链的长度会影响它们的 SHP2 和 PTP1B 抑制活性。此外,γ-内酯环上存在Δ8(12)双键和脂肪链中CH3-2'的存在可能会增加其抑制活性。
更新日期:2020-02-01
down
wechat
bug