Isolation and characterization of an antibacterial biflavonoid from an African chewing stick Garcinia kola Heckel (Clusiaceae).
Isolation and characterization of an antibacterial biflavonoid from an African chewing stick Garcinia kola Heckel (Clusiaceae).
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从非洲咀嚼棒 Garcinia kola Heckel（Clusiaceae）中分离和表征抗菌双黄酮类化合物。
DOI：
10.1016/j.jep.2013.03.047
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发表时间：
2013
影响因子：
5.4
通讯作者：
S. Lee
中科院分区：
文献类型：
--
作者：
Hong;S. Mughal;O. Taiwo;S. Lee
非洲咀嚼棒在维持口腔健康方面的使用在非洲国家得到了广泛的实践。据报道，使用咀嚼棒的人患龋齿的几率比不使用咀嚼棒的人低，总体口腔健康状况也较好。一般认为，咀嚼棒的有益作用是由于其机械清洁作用和抗菌物质的存在。然而，活性抗菌物质仍未被表征。研究目的为了为非洲咀嚼棒的抗龋作用提供科学依据，作者从尼日利亚咀嚼棒Garcinia kola Heckel中纯化了一种活性抗菌化合物，并检测了该化合物对致龋细菌变形链球菌的抗菌活性。材料与方法以藤黄为原料制备乙醇提取物，采用溶剂萃取法进行分馏。采用硅胶层析法从活性部位分离纯化抗菌化合物。通过核磁共振分析确定了纯化化合物的性质。用标准微生物学方法检测纯化化合物的抑菌活性。结果分离得到的活性化合物为一种双黄酮，命名为GB1。GB1对变形链球菌等口腔细菌有抑制作用，最小抑制浓度（MIC）为32 ~ 64μg/ml。以变形链球菌为靶点，探讨了GB1抗菌作用的基础。在256μg/ml浓度下，GB1对变形链球菌具有一定的杀菌活性，并诱导变形链球菌聚集。GB1对蛋白质合成和DNA合成无明显影响，但对变形链球菌的葡萄糖摄取和利用有抑制作用，说明GB1的抑菌作用是通过抑制代谢发挥的。GB1还以剂量依赖性的方式抑制变形链球菌胞外糖基转移酶对水不溶性葡聚糖的形成。在双黄酮含量低于mic水平的情况下，变形链球菌在继代培养中没有对GB1产生抗性。结论该双黄酮的抗菌作用和抑制葡聚糖合成的特性可能是咀嚼棒使用者报告的一些有益作用的原因。
ETHNOPHARMACOLOGICAL RELEVANCEThe use of African chewing sticks in maintaining oral health is widely practiced in African countries. It has been reported that chewing stick users have a lower rate of dental caries and a better general oral health than non-users. It is generally thought that the beneficial effect of chewing stick is attributed to the mechanical cleansing effect and antimicrobial substances present in the stick. However, the active antimicrobial substances remain uncharacterized.AIM OF THE STUDYTo provide a scientific basis for the anti-caries effect of African chewing sticks, the authors purify an active antibacterial compound from Garcinia kola Heckel, a Nigerian chewing stick and examined the antibacterial activity of this compound against the cariogenic bacterium Streptococcus mutans.MATERIALS AND METHODSMethanol extract was prepared from Garcinia kola and was further fractionated by solvent extractions. Silica gel chromatography was used to purify the antibacterial compound from the active fraction. The identity of the purified compound was determined by NMR analysis. The antibacterial activity of the purified compound was examined by standard microbiological assays.RESULTSThe antibacterial activity was found in the ether fraction and the active compound was isolated and determined to be a biflavonoid named GB1. GB1 was active against Streptococcus mutans and other oral bacteria with minimum inhibitory concentration (MIC) values of 32–64μg/ml. The basis for the antibacterial effect of GB1 was investigated using Streptococcus mutans as the target. At 256μg/ml, GB1 exhibited some bacteriocidal activity against Streptococcus mutans and induced the aggregation of Streptococcus mutans. GB1 has no apparent effects on protein synthesis and DNA synthesis but inhibited glucose uptake and utilization by Streptococcus mutans suggesting that GB1 exerts its antibacterial effect by inhibiting metabolism. GB1 also inhibited the formation of water-insoluble glucan by the extracellular glucosyltransferases from Streptococcus mutans in a dose-dependent manner. Streptococcus mutans did not develop resistance to GB1 upon subculturing in the presence of sub-MIC level of the biflavonoid.CONCLUSIONThe antibacterial effect and glucan synthesis-inhibition property of this biflavonoid may account for some of the beneficial effects reported in the chewing stick users.
八种尼日利亚咀嚼棒的水提取物对有利于牙菌斑形成的细菌特性的抑制作用。
影响因子：
4.2
作者：
Wolinsky,LE;Sote,EO
通讯作者：
Sote,EO
从“尼日利亚咀嚼棒”中分离出天然牙菌斑抑制物质。
影响因子：
4.2
作者：
Wolinsky,LE;Sote,EO
通讯作者：
Sote,EO