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Antiproliferative Dimeric Aporphinoid Alkaloids from the Roots of Thalictrum cultratum
Journal of Natural Products ( IF 3.3 ) Pub Date : 2017-11-13 00:00:00 , DOI: 10.1021/acs.jnatprod.7b00387 Da-Hong Li 1 , Jian-Yong Li 1 , Chun-Mei Xue 1 , Tong Han 1 , Chun-Mei Sai 1 , Kai-Bo Wang 1 , Jin-Cai Lu 1 , Yong-Kui Jing 1 , Hui-Ming Hua 1 , Zhan-Lin Li 1
Journal of Natural Products ( IF 3.3 ) Pub Date : 2017-11-13 00:00:00 , DOI: 10.1021/acs.jnatprod.7b00387 Da-Hong Li 1 , Jian-Yong Li 1 , Chun-Mei Xue 1 , Tong Han 1 , Chun-Mei Sai 1 , Kai-Bo Wang 1 , Jin-Cai Lu 1 , Yong-Kui Jing 1 , Hui-Ming Hua 1 , Zhan-Lin Li 1
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Inspired by the intriguing structures and bioactivities of dimeric alkaloids, 11 new thalifaberine-type aporphine-benzylisoquinoline alkaloids, thalicultratines A–K, a tetrahydroprotoberberine-aporphine alkaloid, thalicultratine L, and five known ones were isolated from the roots of Thalictrum cultratum. Their structures were defined on the basis of NMR and HRESIMS data. The antiproliferative activities of compounds 1–17 were evaluated against human leukemia HL-60 and prostate cancer PC-3 cells. Most alkaloids showed potent cytotoxicity against selected cancer cells. Preliminary SARs are discussed. The most active new compound (3), with an IC50 value of 1.06 μM against HL-60 cells, was selected for mechanism of action studies. The results revealed that compound 3 induced apoptosis and arrested the HL-60 cell cycle at the S phase with the loss of mitochondria membrane potential. The nuclear morphological Hoechst 33258 staining assay was also carried out, and the results confirmed apoptosis.
中文翻译：
从根细胞增殖的二聚Aporphinoid生物碱唐松cultratum
通过错综复杂的结构和二聚体生物碱，11个新thalifaberine型阿朴啡-苄基异生物碱，生物活性的启发thalicultratines A-K，一个tetrahydroprotoberberine-阿朴啡生物碱，thalicultratine L，和五个公知的是从根部分离唐松cultratum。它们的结构是根据NMR和HRESIMS数据定义的。评估了化合物1 – 17对人白血病HL-60和前列腺癌PC-3细胞的抗增殖活性。大多数生物碱对选定的癌细胞显示出强力的细胞毒性。初步讨论了SAR。最具活性的新化合物（3），IC 50选择了针对HL-60细胞的1.06μM的值作为作用机理研究。结果表明，化合物3诱导细胞凋亡并在S期停止了HL-60细胞周期，并丧失了线粒体膜电位。还进行了核形态学的Hoechst 33258染色测定，结果证实了细胞凋亡。
更新日期：2017-11-13
中文翻译：
从根细胞增殖的二聚Aporphinoid生物碱唐松cultratum
通过错综复杂的结构和二聚体生物碱，11个新thalifaberine型阿朴啡-苄基异生物碱，生物活性的启发thalicultratines A-K，一个tetrahydroprotoberberine-阿朴啡生物碱，thalicultratine L，和五个公知的是从根部分离唐松cultratum。它们的结构是根据NMR和HRESIMS数据定义的。评估了化合物1 – 17对人白血病HL-60和前列腺癌PC-3细胞的抗增殖活性。大多数生物碱对选定的癌细胞显示出强力的细胞毒性。初步讨论了SAR。最具活性的新化合物（3），IC 50选择了针对HL-60细胞的1.06μM的值作为作用机理研究。结果表明，化合物3诱导细胞凋亡并在S期停止了HL-60细胞周期，并丧失了线粒体膜电位。还进行了核形态学的Hoechst 33258染色测定，结果证实了细胞凋亡。
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