Sakagami Hiroshi, Watanabe Taihei, Hoshino Tomonori, Suda Naoto, Mori Kazumasa, Yasui Toshikazu, Yamauchi Naoki, Kashiwagi Harutsugu, Gomi Tsuneaki, Oizumi Takaaki, Nagai Junko, Uesawa Yoshihiro, Takao Koichi, Sugita Yoshiaki
Meikai University Research Institute of Odontology (M-RIO), 1-1 Keyakidai, Sakado, Saitama 350-0283, Japan.
Division of Pediatric Dentistry, Meikai University School of Dentistry, 1-1 Keyakidai, Sakado, Saitama 350-0283, Japan.
Medicines (Basel). 2018 Dec 25;6(1):4. doi: 10.3390/medicines6010004.
The present article reviews the research progress of three major polyphenols (tannins, flavonoids and lignin carbohydrate complexes), chromone (backbone structure of flavonoids) and herbal extracts. Chemical modified chromone derivatives showed highly specific toxicity against human oral squamous cell carcinoma cell lines, with much lower toxicity against human oral keratinocytes, as compared with various anticancer drugs. QSAR analysis suggests the possible correlation between their tumor-specificity and three-dimensional molecular shape. Condensed tannins in the tea extracts inactivated the glucosyltransferase enzymes, involved in the biofilm formation. Lignin-carbohydrate complexes (prepared by alkaline extraction and acid-precipitation) and crude alkaline extract of the leaves of species (SE, available as an over-the-counter drug) showed much higher anti-HIV activity, than tannins, flavonoids and Japanese traditional medicine (Kampo). Long-term treatment with SE and several Kampo medicines showed an anti-inflammatory and anti-oxidant effects in small size of clinical trials. Although the anti-periodontitis activity of synthetic angiotensin II blockers has been suggested in many papers, natural angiotensin II blockers has not yet been tested for their possible anti-periodontitis activity. There should be still many unknown substances that are useful for treating the oral diseases in the natural kingdom.
本文综述了三种主要多酚（单宁、黄酮类化合物和木质素碳水化合物复合物）、色酮（黄酮类化合物的骨架结构）和草药提取物的研究进展。与各种抗癌药物相比，化学修饰的色酮衍生物对人口腔鳞状细胞癌细胞系表现出高度特异性毒性，而对人口腔角质形成细胞的毒性则低得多。定量构效关系分析表明它们的肿瘤特异性与三维分子形状之间可能存在相关性。茶提取物中的缩合单宁使参与生物膜形成的葡糖基转移酶失活。木质素-碳水化合物复合物（通过碱性提取和酸沉淀制备）和某物种叶片的粗碱性提取物（SE，作为非处方药可得）显示出比单宁、黄酮类化合物和日本传统药物（汉方）更高的抗HIV活性。在小规模临床试验中，长期使用SE和几种汉方药物显示出抗炎和抗氧化作用。尽管许多论文都提出了合成血管紧张素II阻滞剂的抗牙周炎活性，但天然血管紧张素II阻滞剂尚未测试其可能的抗牙周炎活性。自然界中应该仍有许多未知物质可用于治疗口腔疾病。
