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首页> 外文期刊>Natural product communications >Methicillin-resistant Staphylococcus aureus, Vancomycin-resistant Enterococcus faecalis and Enterococcus faecium active Dimeric Isobutyrylphloroglucinol from Ivesia gordonii
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Methicillin-resistant Staphylococcus aureus, Vancomycin-resistant Enterococcus faecalis and Enterococcus faecium active Dimeric Isobutyrylphloroglucinol from Ivesia gordonii

机译：耐甲氧西林金黄色葡萄球菌，粪便对万古霉素的粪便肠球菌和粪肠球菌的活性二聚异丁酰间苯二酚

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摘要

Bioassay-guided fractionation of the chloroform soluble fraction of stem, leaf, and flower extracts of the American plant Ivesia gordonii led to the isolation of a new dimeric acylphloroglucinol, 3,3'-diisobutyryl-2,6'-dimethoxy-4,6,2',4'-tetrahydroxy-5,5'dimethyldiphenyl methane (1), to which we have assigned the trivial name of ivesinol (1), together with a known monomeric acylphloroglucinol, l,5-dihydroxy-2-(2'-methylpropionyl)-3-methoxy-6-methylbenzene (2). The structures of the isolated compounds were characterized using 1D- and 2D- NMR spectroscopy, including COSY, HMQC, HMBC, and ROESY experiments, as well as mass spectrometry. Ivesinol (1) showed potent activity against Staphylococcus aureus (SA) and methicillin-resistant S. aureus (MRSA) with IC_(50)/MIC/MBC values of 0.10/1.25/>20 μg/mL and 0.05/0.31/>20 μg/mL, respectively (vs. IC_(50)/MIC/MBC 0.13/0.5/1.0 μg/mL and 0.13/0.5/1.0 μg/mL of ciprofloxacin), while the corresponding monomer 2 was found to be less active. Compound 1 also demonstrated strong activity against vancomycin-resistant Enterococcus faecium (VRE) with IC_(50)/MIC/MBC values of 0.22/1.25/>20 μg/mL, whereas the reference standard ciprofloxacin was found to be inactive against this strain. In addition, compound 2 showed moderate activity against two species of Candida and Cryptococcus neoformans, while 1 was inactive against these fungi. In order to evaluate the influence of the acyl group(s) in phloroglucinol (3) as a ligand, the mono- (4) and diacetylphloroglucinol (5) were prepared from 3, and evaluated for their in vitro SA, MRSA, and VRE activities; 2,4-diacetylphloroglucinol (5) showed potent activity, like 1, against SA, MRSA, and VRE (ATCC 700221) with IC_(50)/ MIC values of 0.3/2.5, 0.23/2.5, and 0.86/2.5 μg/mL, respectively, while 4 was inactive.
机译：生物测定指导下的美国植物伊维西亚戈登氏茎，叶和花提取物的氯仿可溶性部分的分馏导致分离出新的二聚酰基间苯三酚，3,3'-diisobutyryl-2,6'-dimethoxy-4,6 ，2'，4'-四羟基-5,5'二甲基二苯基甲烷（1），我们为其赋予了普通的名字伊维诺尔（1），以及一个已知的单体酰基间苯三酚，1,5-二羟基-2-（2 （-甲基丙酰基）-3-甲氧基-6-甲基苯（2）。使用1D和2D NMR光谱，包括COSY，HMQC，HMBC和ROESY实验以及质谱，对分离出的化合物的结构进行了表征。伊维素醇（1）对金黄色葡萄球菌（SA）和耐甲氧西林金黄色葡萄球菌（MRSA）表现出强效活性，IC_（50）/ MIC / MBC值为0.10 / 1.25 /> 20μg/ mL和0.05 / 0.31 /> 20分别为μg/ mL（vs. IC_（50）/ MIC / MBC 0.13 / 0.5 / 1.0μg/ mL和0.13 / 0.5 / 1.0μg/ mL环丙沙星），而发现相应的单体2活性较低。化合物1还显示出抗万古霉素粪便肠球菌（VRE）的强大活性，IC_（50）/ MIC / MBC值为0.22 / 1.25 /> 20μg/ mL，而环丙沙星的参考标准品对该菌株无活性。此外，化合物2对两种假丝酵母和新型隐球菌显示中等活性，而化合物1对这些真菌无活性。为了评估酰基在间苯三酚（3）中作为配体的影响，由3制备了单（4）和二乙酰基间苯三酚（5），并对其体外SA，MRSA和VRE进行了评估活动; 2,4-二乙酰基间苯三酚（5）表现出与SA，MRSA和VRE（ATCC 700221）相似的有效活性，IC_（50）/ MIC值为0.3 / 2.5、0.23 / 2.5和0.86 / 2.5μg/ mL ，而4个处于非活动状态。

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