Bioevaluation of Hybrid Based uponPyrrolo[2,1-c][1,4]benzodiazepine A-ring Linked with Triazole

• Main Authors: Yong-Yong Lin, 林詠詠
• Other Authors: Wan-Ping Hu
• Format: Others
• Language: zh-TW
• Published: 2012
• Online Access: http://ndltd.ncl.edu.tw/handle/64912572249325264071

碩士 === 高雄醫學大學 === 生物科技學系碩士班 === 100 === The malignant melanoma is much more dangerous if it is not found early. It causes the majority (75%) of deaths related to skin cancer. It is more common in women than in men. There are high rates of incidence in Australia, New Zealand, North America (especially Texas and Florida), Latin America and Northern Europe, with a paradoxical decrease in southern Italy and Sicily. This geographic pattern reflects the primary cause, ultraviolet light (UV) exposure crossed with the amount of skin pigmentation in the population. It will be easy to treat if it was recognized in the early stages. The natural compound PBD has been shown to possess the most potential activity towards the melanocytes along with the triazole derivatives compared to the previously available compounds. We have observed that these compounds were following the apoptosis pathway. The MTT and SRB results also proved that they may inhibit the melanoma growth. Further, the flow cytometry data have shown that the G1 arrest was occurred. In addition, we have performed real-time PCR and western blotting experiments to demonstrate that the apoptosis related gene (Bcl-2, Bcl-cL, Bax, Bad, P27, P21 and P53) have been changed their expression by treatment with the following compounds. In conclusion, these results suggest that PBD-linked triazoles have potential therapeutic ability towards the human malignant melanoma.