Effects of compounds found in propolis on Streptococcus mutans growth and on glucosyltransferase activity
Effects of compounds found in propolis on Streptococcus mutans growth and on glucosyltransferase activity
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DOI：
10.1128/aac.46.5.1302-1309.2002
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发表时间：
2002-05-01
影响因子：
4.9
通讯作者：
Bowen, WH
中科院分区：
文献类型：
--
作者：
Koo, H;Rosalen, PL;Bowen, WH
蜂胶，一种树脂状的蜂产品，已被证明能抑制口腔微生物的生长以及细菌来源的葡糖基转移酶（GTFs）的活性。在这种天然产物中已鉴定出几种化合物，主要是多酚类物质。本研究评估了蜂胶中不同化学基团对溶液中以及唾液包被的羟基磷灰石（sHA）珠表面的GTF酶活性的影响。对30种化合物，包括黄酮类、肉桂酸衍生物和萜类化合物，测试了其抑制变形链球菌的GTFs B、C和D以及血链球菌的GTF（GTF Ss）的能力。黄酮和黄酮醇是溶液中GTF活性的强效抑制剂；对不溶性酶的作用较小。芹菜素，一种4',5,7 - 三羟基黄酮，是GTFs最有效的抑制剂，在溶液中（浓度为135μg/ml时抑制率为90.5% - 95%）以及在sHA珠表面（135μg/ml时为30% - 60%）均是如此。通过最小抑菌浓度（MICs）、最小杀菌浓度（MBCs）和时间 - 杀菌研究来确定抗菌活性。黄烷酮和一些二氢黄酮醇，以及倍半萜tt - 法尼醇，抑制了变形链球菌和远缘链球菌的生长；tt - 法尼醇是最有效的抗菌化合物（MICs为14 - 28μg/ml，MBCs为56 - 112μg/ml）。tt - 法尼醇（56 - 112μg/ml）在培养4小时后使细菌数量减少了3个对数级。肉桂酸衍生物的生物活性可忽略不计。蜂胶中鉴定出的几种化合物抑制GTF活性和细菌生长。芹菜素是一种新型且强效的GTF活性抑制剂，并且发现tt - 法尼醇是一种有效的抗菌剂。
Propolis, a resinous bee product, has been shown to inhibit the growth of oral microorganisms and the activity of bacterium-derived glucosyltransferases (GTFs). Several compounds, mainly polyphenolics, have been identified in this natural product. The present study evaluated the effects of distinct chemical groups found in propolis on the activity of GTF enzymes in solution and on the surface of saliva-coated hydroxyapatite (sHA) beads. Thirty compounds, including flavonoids, cinnamic acid derivatives, and terpenoids, were tested for the ability to inhibit GTFs B, C, and D from Streptococcus mutans and GTF from S. sanguinis (GTF Ss). Flavones and flavonols were potent inhibitors of GTF activity in solution; lesser effects were noted on insolubilized enzymes. Apigenin, a 4',5,7-trihydroxyflavone, was the most effective inhibitor of GTFs, both in solution (90.5 to 95% inhibition at a concentration of 135 mug/ml) and on the surface of sHA beads (30 to 60% at 135 mug/ml). Antibacterial activity was determined by using MICs, minimum bactericidal concentrations (MBCs), and time-kill studies. Flavanones and some dihydroflavonols, as well as the sesquiterpene tt-farnesol, inhibited the growth of S. mutans and S. sobrinus; tt-farnesol was the most effective antibacterial compound (MICs of 14 to 28 mug/ml and MBCs of 56 to 112 mug/ml). tt-Farnesol (56 to 112 mug/ml) produced a 3-log-fold reduction in the bacterial population after 4 h of incubation. Cinnamic acid derivatives had negligible biological activities. Several of the compounds identified in propolis inhibit GTF activities and bacterial growth. Apigenin is a novel and potent inhibitor of GTF activity, and tt-farnesol was found to be an effective antibacterial agent.