Natural Products Programme, Institute of Fundamental Studies, Kandy, Sri Lanka.
Nat Prod Res. 2013;27(10):938-41. doi: 10.1080/14786419.2012.678348. Epub 2012 Apr 11.
Antibacterial activities of prenylated xanthones from Garcinia mangostana and their synthetic analogues were investigated, and their structure-activity relationships have been studied. γ-Mangostin has shown antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA), methicillin sensitive Staphylococcus aureus (MSSA), vancomycin-resistant Enterococcus (VRE) and vancomycin-sensitive Enterococcus (VSE) strains at MICs 3.13, 6.25, 6.25 and 6.25 µg mL(-1), respectively. In these experiments, gentamicin was used as the positive control. Further, some analogues of γ-mangostin and α-mangostin were synthesised and their activity was tested against MRSA and VRE strains. The analysis of the bioassay results above indicated that, the combination of C-6 and C-3 hydroxyl groups along with the prenyl side chain at C-2 in the 1,3,6,7-tetraoxygenated xanthones from G. mangostana is essential to have a high antibacterial activity.
对藤黄科植物藤黄中具有异戊烯基取代的呫吨酮及其合成类似物的抗菌活性进行了研究,并对其构效关系进行了研究。γ-倒捻子素有抗甲氧西林耐药金黄色葡萄球菌(MRSA)、甲氧西林敏感金黄色葡萄球菌(MSSA)、万古霉素耐药肠球菌(VRE)和万古霉素敏感肠球菌(VSE)的活性,MIC 值分别为 3.13、6.25、6.25 和 6.25μg/ml。在这些实验中,庆大霉素被用作阳性对照。此外,还合成了一些 γ-倒捻子素和 α-倒捻子素的类似物,并测试了它们对 MRSA 和 VRE 菌株的活性。对上述生物测定结果的分析表明,1,3,6,7-四氧基呫吨酮类化合物中 C-6 和 C-3 位的羟基与 C-2 位的异戊烯基侧链的结合对于具有高抗菌活性是必不可少的。