Inhibition of sortase, a bacterial surface protein anchoring transpeptidase, by β-sitosterol-3-O-glucopyranoside from Fritillaria verticillata
Inhibition of sortase, a bacterial surface protein anchoring transpeptidase, by β-sitosterol-3-O-glucopyranoside from Fritillaria verticillata
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DOI：
10.1271/bbb.67.2477
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发表时间：
2003-11-01
影响因子：
1.6
通讯作者：
Oh, KB
中科院分区：
文献类型：
--
作者：
Kim, SH;Shin, DS;Oh, KB
从贝母鳞茎中分离得到一种具有分选酶抑制作用的糖基甾醇-β-谷甾醇-3-O-葡萄糖苷。该分离物是一种有效的分选酶抑制剂，IC 50值为18.3 μ g/ml，对枯草芽孢杆菌、金黄色葡萄球菌和白色微球菌具有抗菌活性，MIC值分别为50、200和400 μ g/ml，表明该化合物是开发细菌分选酶抑制剂的可能候选物。此外，发现谷甾醇对分选酶和细菌细胞生长无活性。这些结果表明，谷甾醇-3-O-吡喃葡萄糖苷的抑制效力敏感地依赖于吡喃葡萄糖苷侧链部分。
A glucosylsterol, beta-sitosterol-3-O-glueopyranoside, has been isolated as an active principle with sortase inhibitory effect from the bulbs of Fritillaria verticillata by bioassay-guided chromatographic fractionation. The isolate was a potent inhibitor of sortase, with an IC50 value of 18.3 mug/ml and had antibacterial activity against Bacillus subtilis, Staphylococcus aureus, and Micrococcus leuteus with MIC values of 50, 200, and 400 mug/ml, respectively, indicating that this compound is a possible candidate for the development of a bacterial sortase inhibitor. In addition, sitosterol was found to be inactive upon sortase and bacterial cell growth. These results suggest that the inhibitory potency of flsitosterol-3-O-glucopyranoside is sensitively dependent upon the glucopyranoside side chain moiety.