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- Sitosterol-doxorubicin derivatives for radiotherapy amplification and composition for preventing or treating cancer diseases comprising the same
专利权人:
경북대학교 산학협력단;한국원자력의학원;영남대학교 산학협력단
发明人:
서영배,도경오,최종수,김광석,김병길,박재원
申请号:
KR1020190002872
公开号:
KR1020200086541A
申请日:
2019.01.09
申请国别(地区):
KR
年份:
2020
代理人:
摘要:
The present invention relates to a composition for preventing or treating cancer diseases comprising a cytosterol-doxorubicin derivative for amplifying radiation therapy and an active ingredient thereof, in the present invention, Sito-dox A and Sito as a doxorubicin derivative using β-cytosterol -dox B was synthesized, and the Sito-dox A exhibited superior anticancer effects than doxorubicin and a synergistic effect in combination therapy with radiation therapy, and Sito-dox B did not show cytotoxicity, but in combination therapy with radiation therapy It was confirmed that the tumor collapse phenomenon was observed. That is, the doxorubicin derivatives synthesized using the β-cytosterol of the present invention can amplify the anti-cancer treatment effect when used in combination with radiation therapy, and overcome the shortcomings of doxorubicin in the body and shortcomings of rapid dissolution. , It can be useful as a more effective cancer disease prevention or treatment pharmaceutical composition, radiation treatment sensitizer pharmaceutical composition, and the like. In addition, citric acid, glycoic acid, taurocollic acid, dioxycholic acid, kenodeoxycholic acid, glycokenodioxycholic acid, taurocenodeoxycholic acid, cholesterol and ritoh are similar in structure and properties to cytosterol. It is expected that doxorubicin derivatives substituted with lipids such as cholic acid will have similar cancer treatment effects to doxorubicin derivatives substituted with cytosterols.본 발명은 방사선 치료 증폭을 위한 사이토스테롤-독소루비신 유도체 및 이를 유효성분으로 포함하는 암 질환 예방 또는 치료용 조성물에 관한 것으로, 본 발명에서는 β-사이토스테롤을 이용하여 독소루비신 유도체로서 Sito-dox A 및 Sito-dox B를 합성하였으며, 상기 Sito-dox A는 독소루비신 보다 우수한 항암 효과, 및 방사선 요법과의 병용 치료에서 시너지 효과를 나타내고, Sito-dox B는 세포 독성을 나타내지 않았으나, 방사선 요법과의 병용 치료에서 종양 붕괴 현상을 나타내는 것을 확인하였다. 즉, 본 발명의 β-사이토스테롤을 이용하여 합성된 독소루비신 유도체는 방사선 요법과 병용 치료 시, 항암 치료 효과를 증폭시킬 수 있고, 독소루비신의 체내 짧은 체류 시간과 빠른 용출의 단점을 극복할 수 있는 바, 보다 효과적인 암 질환 예방 또는 치료용 약학 조성물, 방사선 치료 민감제용 약학 조성물 등으로 유용하게 활용될 수 있다. 더불어, 사이토스테롤과 구
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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