Department of Preventive Medicine and Public Health, National Defense Medical College, Namiki, Tokorozawa, Japan.
Pharm Biol. 2013 Feb;51(2):267-70. doi: 10.3109/13880209.2012.717227. Epub 2012 Nov 2.
Dental caries are an infectious oral bacterial disease caused by cariogenic streptococci. These streptococci inhabit dental biofilms which comprise insoluble glucans.
To prevent dental caries, nisin, a suitable agent active against Gram-positive bacteria, was examined in vitro for its ability to suppress insoluble glucan-biofilm synthesis by cariogenic streptococci.
To investigate glucan-biofilm synthesis by a typical cariogenic streptococcus, Streptococcus mutans 10449, the naked form of nisin was loaded onto a 96-well microplate in vitro model. To prolong the efficacy of nisin as a preventive agent, liposome-encapsulated nisin (nisin-liposome) was examined for its ability to inhibit the synthesis of glucan-biofilms on microplates.
Naked nisin (100 pmol) completely suppressed insoluble glucan-biofilm synthesis by S. mutans 10449 following 1 h cultivation in 96-well microplates. The concentration of nisin-liposome required for the efficacious inhibition of glucan-biofilm synthesis was four times lower than that of naked nisin following 2 h cultivation. In particular, nisin-liposome (30 pmol nisin equivalent) prolonged the inhibitory activity of nisin against glucan-biofilm synthesis by S. mutans 10449 for up to 6 h, while naked nisin (30 pmol) gradually lost this inhibitory activity over the same period. In vitro release assay of nisin from the liposome showed that 76% nisin was released within 6 h.
The findings indicate the usefulness of nisin-liposome for the sustained release of nisin. Thus, nisin-liposome could play a potential role in preventive medicine as an inhibitor of the glucan-biofilm synthesis.
龋齿是一种由致龋链球菌引起的传染性口腔细菌性疾病。这些链球菌栖息在由不溶性葡聚糖组成的牙菌斑中。
为了预防龋齿,研究了乳链菌肽(nisin),一种对革兰氏阳性菌有活性的合适药物,以研究其抑制致龋链球菌合成不溶性葡聚糖生物膜的能力。
为了研究典型致龋链球菌——变形链球菌 10449 的葡聚糖生物膜合成,将乳链菌肽的裸形式加载到体外 96 孔微量滴定板模型中。为了延长乳链菌肽作为预防剂的功效,研究了脂质体包封的乳链菌肽(nisin-liposome)抑制微板上葡聚糖生物膜合成的能力。
裸形式的乳链菌肽(100 pmol)在 96 孔微量滴定板中培养 1 小时后完全抑制了 S. mutans 10449 的不溶性葡聚糖生物膜合成。在培养 2 小时后,有效抑制葡聚糖生物膜合成所需的 nisin-liposome 的浓度比裸形式的乳链菌肽低四倍。特别是,nisin-liposome(30 pmol 乳链菌肽当量)可将乳链菌肽抑制 S. mutans 10449 葡聚糖生物膜合成的抑制活性延长至 6 小时,而裸形式的乳链菌肽(30 pmol)在同一时期逐渐失去这种抑制活性。从脂质体中释放乳链菌肽的体外释放试验表明,76%的乳链菌肽在 6 小时内释放。
这些发现表明乳链菌肽脂质体在乳链菌肽的持续释放方面具有实用性。因此,乳链菌肽脂质体可能在预防医学中作为葡聚糖生物膜合成抑制剂发挥作用。