2-(4-胺苯)苯幷噻唑衍生物的合成與用途

專利類型

發明

專利國別 (專利申請國家)

中華民國

專利申請案號

099137211

專利證號

I 444371

專利獲證名稱

2-(4-胺苯)苯幷噻唑衍生物的合成與用途

專利所屬機關 (申請機關)

高雄醫學大學

獲證日期

2014/07/11

技術說明

光動力療法(PDT)使用外源性光敏劑是被批准用於治療基底細胞癌(BCC) 2-(4-Aminophenyl)benzothiazoles (6)含有發色團的結構和吸收光線中的紫外線(315-400 nm)。這個結果鼓勵我們的設計和合成多樣的2-phenylbenzothiazoles (6)。UVA-activated 6在BCC細胞中，產生光敏效應誘導細胞產生凋亡機制。6-UVA-treated cells顯示幾個凋亡的特點，像是sub-G1 population的提高，明顯增加Annexin V的結合和caspase-3的活化。6-UVA引起粒線體膜電位(△mt)下降，和ATP經由增強活性氧的產生，和促進細胞外信號調節激酶(ERK)的磷酸化，和p38 MAPK的表現。這些結果顯示6-UVA在mitochondria processes中引起的光敏效應涉及ERK和p38的活性化最終導致BCC的凋亡。 Photodynamic therapy (PDT) employing exogenous photosensitizers is currently being approved for treatment of basal cell carcinoma (BCC). 2-(4-Aminophenyl)benzothiazoles (6) consist of chromophoric structure and absorb light in the UVA (315-400 nm). Studies on the apoptotic mechanism involved in photosensitive effects induced by UVA-activated 6 in BCC cells are carried out in the present article. 6-UVA-treated cells displayed several features of apoptosis, including an increase in the sub-G1 population, a significantly increased annexin V binding, and activation of caspase-3. 6-UVA induced a decrease in mitochondrial membrane potential and ATP via enhanced ROS generation and promoted phosphorylation of extracellular signal-regulated kinase and p38 MAPK expression. These results suggest that 6-UVA elicits photosensitive effects in mitochondria processes which involve ERK and p38 activation, and ultimately lead to BCC cell apoptosis.

備註

本部(發文號1100044017)同意貴校110年1月28日高醫產學字第1101100305號函申請終止維護專利。(高醫)

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