新型川芎嗪衍生物的合成及其抗癌活性研究
신형천궁진연생물적합성급기항암활성연구
Synthesis and anti-tumor activity evaluation of new ligustrazine derivatives
  • 万方数据
    西北药学杂志 서북약학잡지

    2014年 1期 58-63,64 ,共7页

    王鹏龙%徐昕%李国梁%褚福浩%林锦璇%绪扩%周燊%龚晏%张宇忠%李强%雷海民

    왕붕룡%서흔%리국량%저복호%림금선%서확%주신%공안%장우충%리강%뢰해민

    川芎嗪衍生物%拼合原理%抗肿瘤%先导化合物 川芎嗪衍生物%拼閤原理%抗腫瘤%先導化閤物
    천궁진연생물%병합원리%항종류%선도화합물
    ligustrazine derivatives%combination principle%anti-tumor effect%leading compound
    目的：合成新型川芎嗪衍生物并对其抗癌活性和毒性进行评价。方法以中医经典方药中抗癌活性成分为原料，利用拼合原理，设计、合成川芎嗪衍生物，并采用四甲基偶氮唑蓝(MTT)法体外检测川芎嗪衍生物对 Hela(人宫颈癌)细胞模型的抗癌活性和对正常细胞 MDCK(犬肾上皮细胞)的毒性。结果获得4个未见报道的川芎嗪类新化合物，均经光谱方法鉴定了结构，其中化合物10和12能明显抑制 Hela细胞的增殖，抗癌活性显著高于其合成前体；且对 MDCK 细胞的毒性明显小于顺铂。结论该结果进一步验证以拼合原理为指导，从经典方药中发现新型低毒抗癌先导化合物的研究思路是可行的。
    목적：합성신형천궁진연생물병대기항암활성화독성진행평개。방법이중의경전방약중항암활성성분위원료，이용병합원리，설계、합성천궁진연생물，병채용사갑기우담서람(MTT)법체외검측천궁진연생물대 Hela(인궁경암)세포모형적항암활성화대정상세포 MDCK(견신상피세포)적독성。결과획득4개미견보도적천궁진류신화합물，균경광보방법감정료결구，기중화합물10화12능명현억제 Hela세포적증식，항암활성현저고우기합성전체；차대 MDCK 세포적독성명현소우순박。결론해결과진일보험증이병합원리위지도，종경전방약중발현신형저독항암선도화합물적연구사로시가행적。
    Obj ective To discover new anti-cancer agents with low toxicity,four new ligustrazine derivatives were synthesized by u-sing anti-tumor ingredients of the classic Chinese medicine as starting materials.Methods Our idea was enlightened by the combi-nation principle in drug discovery.The ligustrazine derivatives′anti-tumor activities were evaluated on the Hela human cancer cell line and their toxicities were evaluated on MDCK (Madin-Darby canine kidney)cell line.Results The structure of the intermediate and four new ligustrazine derivatives were characterized by 1 H NMR,13 C NMR and IR techniques.Compound 10 and 12 displayed more antiproliferative activities on Hela cell than their starting materials;moreover ligustrazine derivatives showed much lower toxicity on MDCK cell than DDP.Conclusion The results suggest that it is feasible to discover new anti-cancer lead compounds from classic formula via combination principle.
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