Chen Shuqiang, Dong Guoqiang, Wu Shanchao, Liu Na, Zhang Wannian, Sheng Chunquan
School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
Acta Pharm Sin B. 2019 Jan;9(1):144-156. doi: 10.1016/j.apsb.2018.08.003. Epub 2018 Aug 20.
Natural product evodiamine and its derivatives represent a promising class of multi-target antitumor agents. However, the clinical development of these compounds has been hampered by a poor understanding of their antitumor mechanisms. To tackle this obstacle, herein, novel fluorescent probes were designed to elucidate the antitumor mode of action of 10-hydroxyevodiamine. This compound was proven to be distributed in the mitochondria and lysosomes and to act by autophagy and apoptosis mechanisms.
天然产物吴茱萸碱及其衍生物是一类很有前景的多靶点抗肿瘤药物。然而,由于对其抗肿瘤机制了解不足,这些化合物的临床开发受到了阻碍。为克服这一障碍,本文设计了新型荧光探针以阐明10-羟基吴茱萸碱的抗肿瘤作用模式。该化合物被证明分布于线粒体和溶酶体中,并通过自噬和凋亡机制发挥作用。