Faculty of Science, Josai University, Sakado, Saitama 350-0295, Japan.
In Vivo. 2011 Jan-Feb;25(1):41-8.
We have previously reported a possible anti-inflammatory activity of azulene-, tropolone- and azulenequinone-related compounds. To further pursue the newly discovered biological activity of these compounds, five compounds that inhibited nitric oxide production by activated macrophages were investigated for their possible hormetic and anti-radiation effects.
Viable cell number of human oral normal cells (gingival fibroblast, pulp cell and periodontal ligament fibroblast) and three oral squamous cell carcinoma cell lines on treatment with various concentrations of each azulene-related compound was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. Apoptosis induction was monitored by caspase-3 activation and DNA fragmentation.
Among five compounds, only benzo[b]cyclohepta[e][1,4]thiazine slightly stimulated the growth of all three normal cell types, but not tumor cell lines, at concentrations slightly higher than cytotoxic concentrations. Using a newly established evaluation system for UV-induced cellular damage, we found that this compound slightly but significantly protected the cells from UV-induced cellular injury, and its effect was synergistically enhanced by sodium ascorbate.
These data suggest the possible application of benzo[b]cyclohepta[e][1,4]thiazine in UV protection therapy.
我们之前曾报道过薁类、三酮类和薁醌类化合物具有抗炎活性。为了进一步探索这些化合物新发现的生物学活性，我们研究了五种能抑制活化巨噬细胞产生一氧化氮的化合物，以探讨它们是否具有适应原和抗辐射作用。
采用 3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐（MTT）法检测不同浓度薁类相关化合物对人口腔正常细胞（牙龈成纤维细胞、牙髓细胞和牙周膜成纤维细胞）和三种口腔鳞状细胞癌细胞系存活细胞数的影响。通过 caspase-3 激活和 DNA 片段化监测细胞凋亡诱导。
在这 5 种化合物中，只有苯并[b]环庚[e][1,4]噻嗪在略高于细胞毒性浓度的浓度下，略微刺激所有三种正常细胞类型（而非肿瘤细胞系）的生长。使用新建立的用于评估 UV 诱导细胞损伤的评价系统，我们发现该化合物能略微但显著地保护细胞免受 UV 诱导的细胞损伤，其作用通过抗坏血酸钠协同增强。
这些数据表明苯并[b]环庚[e][1,4]噻嗪可能应用于 UV 防护治疗。
