Suppr超能文献

镰刀硫酰胺B,一种从内生真菌厚垣镰刀菌中分离得到的新型苯甲酰胺衍生物,具有强大的细胞毒性和抗菌活性。

Fusarithioamide B, a new benzamide derivative from the endophytic fungus Fusarium chlamydosporium with potent cytotoxic and antimicrobial activities.

作者信息

Ibrahim Sabrin R M, Mohamed Gamal A, Al Haidari Rwaida A, Zayed Mohamed F, El-Kholy Amal A, Elkhayat Ehab S, Ross Samir A

机构信息

Department of Pharmacognosy and Pharmaceutical Chemistry, College of Pharmacy, Taibah University, Al Madinah Al Munawwarah 30078, Saudi Arabia; Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt.

Department of Natural Products and Alternative Medicine, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia; Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Assiut Branch, Assiut 71524, Egypt.

出版信息

Bioorg Med Chem. 2018 Feb 1;26(3):786-790. doi: 10.1016/j.bmc.2017.12.049. Epub 2017 Dec 30.

Abstract

Fusarithioamide B (6), a new aminobenzamide derivative with unprecedented carbon skeleton and five known metabolites: stigmast-4-ene-3-one (1), stigmasta-4,6,8(14),22-tetraen-3-one (2), p-hydroxyacetophenone (3), tyrosol (4), and fusarithioamide A (5) were separated from Fusarium chlamydosporium EtOAc extract isolated from Anvillea garcinii (Burm.f.) DC. leaves (Asteraceae). The structure elucidation and completeassignment of the isolated metabolites were performed mainly by the aid of various NMR and MS data. Fusarithioamide B (6) has been assessed for antibacterial and antifungal activities towards various microbial strains by disc diffusion assay. It exhibited selective antifungal activity towards C. albicans (MIC 1.9 µg/ml and IZD 14.5 mm), comparing to clotrimazole (MIC 2.8 µg/ml and IZD 17.9 mm). Also, it possessed high antibacterial potential towards E. coli, B. cereus, and S. aureus compared to ciprofloxacin. Furthermore, 6 was tested for the in vitro cytotoxic effect against KB, HCT-116, BT-549, MCF-7, SKOV-3, and SK-MEL cell lines. It had selective and potent effect towards BT-549, MCF-7, SKOV-3, and HCT-116 cell lines with ICs 0.09, 0.21, 1.23, and 0.59 μM, respectively compared to doxorubicin (ICs 0.046, 0.05, 0.321, and 0.24 μM, respectively). Fusarithioamide B may provide a lead molecule for future developing of antitumor and antimicrobial agents.

摘要

镰刀硫酰胺B(6)是一种具有前所未有的碳骨架的新型氨基苯甲酰胺衍生物,以及五种已知代谢产物:豆甾-4-烯-3-酮(1)、豆甾-4,6,8(14),22-四烯-3-酮(2)、对羟基苯乙酮(3)、酪醇(4)和镰刀硫酰胺A(5),它们是从菊科植物加氏安维尔草(Anvillea garcinii (Burm.f.) DC.)叶片中分离得到的镰刀菌厚垣孢子乙酸乙酯提取物中分离出来的。分离得到的代谢产物的结构解析和完全归属主要借助各种核磁共振和质谱数据完成。通过纸片扩散法评估了镰刀硫酰胺B(6)对多种微生物菌株的抗菌和抗真菌活性。与克霉唑(MIC 2.8 μg/ml,IZD 17.9 mm)相比,它对白色念珠菌表现出选择性抗真菌活性(MIC 1.9 μg/ml,IZD 14.5 mm)。此外,与环丙沙星相比,它对大肠杆菌、蜡样芽孢杆菌和金黄色葡萄球菌具有较高的抗菌潜力。此外,对6进行了针对KB、HCT-116、BT-549、MCF-7、SKOV-3和SK-MEL细胞系的体外细胞毒性作用测试。与阿霉素(IC50分别为0.046、0.05、0.321和0.24 μM)相比,它对BT-549、MCF-7、SKOV-3和HCT-116细胞系具有选择性和强效作用,IC50分别为0.09、0.21、1.23和0.

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验