含新穎化合物之選擇性殺死口腔癌細胞之醫藥組合物及此化合物之用途

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

108111104

專利證號

I 694990

專利獲證名稱

含新穎化合物之選擇性殺死口腔癌細胞之醫藥組合物及此化合物之用途

專利所屬機關 (申請機關)

高雄醫學大學

獲證日期

2020/06/01

技術說明

本案提供一種新穎磺醯基苯并哌喃-4-酮化合物，以及含有此化合物之用於選擇性殺死口腔癌細胞之醫藥組合物，此醫藥組合物包括：一磺醯基苯并哌喃-4-酮化合物為活性成分；以及一藥學上可接受的載體或鹽類，化合物為2-萘基-1-基甲基-3-(甲苯-4-磺醯基) 苯并哌喃-4-酮，且其具有選擇性殺死該口腔癌細胞之功效。本案另提供一種磺醯基苯并哌喃-4-酮化合物用於製備選擇性殺死一口腔癌細胞之藥物的用途以及一種磺醯基苯并哌喃-4-酮化合物用於製備以氧化壓力為媒介之一癌症治療藥物的用途。 Several functionalized chromones, the key components of naturally occurring oxygenated heterocycles, have anticancer effects but their sulfone compounds are rarely investigated. In this study, we installed a sulfonyl substituent to chromen-4-one skeleton and synthesized CHW09 to evaluate its antioral cancer effect in terms of cell viability, apoptosis, oxidative stress, and DNA damage. In cell viability assay, CHW09 preferentially kills two oral cancer cells (Ca9-22 and CAL 27), less affecting normal oral cells (HGF-1). CHW09 induces apoptosis validated by flow cytometry for annexin V and by western blotting for cleaved poly(ADP-ribose) polymerase (PARP), and caspases 3/8/9. These apoptosis signaling expressions are partly decreased by apoptosis inhibitor (Z-VAD-FMK) or free radical scavenger (N-acetylcysteine). Furthermore, CHW09 induces oxidative stress validated by flow cytometry for the generations of reactive oxygen species (ROS) and mitochondrial superoxide (MitoSOX), and the suppression of mitochondrial membrane potential (MMP). CHW09 also induces DNA damage validated by flow cytometry for the increases of DNA double strand break marker γH2AX and oxidative DNA damage marker 8-oxo-2'-deoxyguanosine (8-oxodG). Therefore, our newly synthesized CHW09 induces apoptosis, oxidative stress, and DNA damage, which may lead to preferential killing of oral cancer cells compared to normal oral cells.

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智財保護與科技管理組

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07-3138030

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