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从西方梧桐(美国梧桐)中提取的耐甲氧西林金黄色葡萄球菌(MRSA)活性代谢物。

Methicillin-resistant Staphylococcus aureus (MRSA)-active metabolites from Platanus occidentalis (American Sycamore).

机构信息

Departments of Pharmacognosy, Pharmacology, Chemistry, and Biochemistry and National Center for Natural Products Research, School of Pharmacy, The University of Mississippi, University, Mississippi 38677, USA.

出版信息

J Nat Prod. 2009 Dec;72(12):2141-4. doi: 10.1021/np900499q.

Abstract

One known and three new potent, selective, and nontoxic anti-MRSA metabolites, kaempferol 3-O-alpha-l-(2'',3''-di-E-p-coumaroyl)rhamnoside (1) (IC(50) 2.0 microg/mL), kaempferol 3-O-alpha-l-(2''-E-p-coumaroyl-3''-Z-p-coumaroyl)rhamnoside (2) (IC(50) 0.8 microg/mL), kaempferol 3-O-alpha-l-(2''-Z-p-coumaroyl-3''-E-p-coumaroyl)rhamnoside (3) (IC(50) 0.7 microg/mL), and kaempferol 3-O-alpha-l-(2'',3''-di-Z-p-coumaroyl)rhamnoside (4) (IC(50) 0.4 microg/mL), were isolated from the leaves of the common American sycamore, Platanus occidentalis. Compounds 2-4 are new. Due to the unusual selectivity, potency, and safety of the pure compounds and the semipure glycoside mixture against MRSA, it is clear that this represents a viable class of inhibitors to prevent growth of MRSA on surfaces and systemically.

摘要

从普通美国梧桐(Platanus occidentalis)的叶子中分离得到了 1 种已知的和 3 种新的强效、选择性和无毒的抗耐甲氧西林金黄色葡萄球菌(MRSA)代谢产物:山柰酚 3-O-α-l-(2'',3''-二-E-对香豆酰基)鼠李糖苷(1)(IC50 为 2.0 μg/mL)、山柰酚 3-O-α-l-(2''-E-对香豆酰基-3''-Z-对香豆酰基)鼠李糖苷(2)(IC50 为 0.8 μg/mL)、山柰酚 3-O-α-l-(2''-Z-对香豆酰基-3''-E-对香豆酰基)鼠李糖苷(3)(IC50 为 0.7 μg/mL)和山柰酚 3-O-α-l-(2'',3''-二-Z-对香豆酰基)鼠李糖苷(4)(IC50 为 0.4 μg/mL)。化合物 2-4 为新化合物。由于纯化合物和半纯糖苷混合物对 MRSA 的选择性、效力和安全性不同寻常,因此很明显,这代表了一类可防止 MRSA 在表面和系统中生长的可行抑制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9c9a/4883668/b02cf75c80db/nihms788212f1.jpg

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