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A novel sesquiterpene lactone from Centaurea pullata: structure elucidation, antimicrobial activity, and prediction of pharmacokinetic properties.
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2008 Apr 1 , DOI: 10.1016/j.bmc.2008.01.056
Samah Djeddi , Anastasia Karioti , Marina Sokovic , Catherine Koukoulitsa , Helen Skaltsa

A novel elemanolide with an alpha-methyl-gamma-lactone moiety, 8alpha-O-(4-hydroxy-2-methylenebutanoyloxy)melitensine, in addition to four known sesquiterpene lactones also bearing the same lactone ring, melitensin, 11beta,13 dihydrosalonitenolide, 8alpha-hydroxy-11beta,13-dihydro-4-epi-sonchucarpolide, and 8alpha-hydroxy-11beta,13-dihydro-onopordaldehyde have been isolated from the aerial parts of Centaurea pullata. The in vitro antibacterial and antifungal activities of the isolated sesquiterpene lactones were tested against six bacteria and eight fungal species, using a microdilution method. All compounds tested showed greater antibacterial and antifungal activities than the positive controls used. Moreover, the pharmacokinetic profile of these compounds was investigated using computational methods.

中文翻译:

一种来自矢车菊的倍半萜内酯:结构阐明,抗菌活性和药代动力学特性的预测。

除了具有四个已知具有相同内酯环的倍半萜内酯外,一种具有α-甲基-γ-内酯部分,8alpha-O-(4-羟基-2-亚甲基丁酸酰)melitensine的新型香叶内酯,降压素,11beta,13 dihydrosalonitenolide,从矢车菊的地上部分中分离出8alpha-hydroxy-11beta,13-dihydro-4-epi-sonchucarpolide和8alpha-hydroxy-11beta,13-dihydro-onopordaldehyde 使用微稀释法测试了分离出的倍半萜内酯对六种细菌和八种真菌的体外抗菌和抗真菌活性。与所使用的阳性对照相比,所有测试的化合物均显示出更大的抗菌和抗真菌活性。此外,使用计算方法研究了这些化合物的药代动力学特征。
更新日期:2017-01-31
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