Constituents of Two DioscoreaSpecies That Potentiate Antibiotic Activity against MRSA

Autor: Sibandze, Gugu F., Stapleton, Paul, Gibbons, Simon
Zdroj: Journal of Natural Products; May 2020, Vol. 83 Issue: 5 p1696-1700, 5p
Abstrakt: The isolation of two diarylnonanoids from Dioscorea cotinifoliapossessing antibiotic-potentiating activity against resistant strains of S. aureusare reported. The diarylnonanoids are a class of natural products similar in structure to the diarylheptanoids, which have a wide spectrum of reported biological activities. One of the diarylnonanoids (1) isolated possesses a chiral center, and to deduce its configuration, the modified Mosher ester method was used. Using both 1D and 2D NMR data, as many protons as possible were assigned to both the R- and S-MTPA esters, and the configuration of the chiral center in 1was determined to be R. Both the chiral and achiral diarylnonanoid (2) exhibited potent antibiotic-potentiating activity with the chiral natural product showing a greater tetracycline-potentiating activity than 2. Interestingly, 2gave a higher norfloxacin-potentiating activity with a resultant higher efflux pump inhibitory activity. Manipulation of the structure of the diarylnonanoids through synthesis could lead to improved biological activity.
Databáze: Supplemental Index