Section of Gastroenterology, Boston University School of Medicine, Boston, MA 02118-2518, USA.
Biochem Biophys Res Commun. 2011 Dec 16;416(3-4):397-402. doi: 10.1016/j.bbrc.2011.11.052. Epub 2011 Nov 19.
A number of cyclohexenyl chalcone Diels-Alder natural products possess promising biological properties including strong cytotoxicity in various human cancer cells. Herein, we show that natural products in this class including panduratin A and nicolaioidesin C inhibit cysteine cathepsins as indicated by protease profiling assays and cell-free cathepsin L enzyme assays. Owing to the critical roles of cathepsins in the biology of human tumor progression, invasion, and metastasis, these findings should pave the way for development of novel antitumor agents for use in clinical settings.
一些环己烯基查耳酮 Diels-Alder 天然产物具有有前途的生物特性，包括在各种人类癌细胞中具有强细胞毒性。在此，我们表明该类天然产物，包括 panduratin A 和 nicolaioidesin C，如蛋白酶谱分析和无细胞组织蛋白酶 L 酶测定所示，抑制半胱氨酸组织蛋白酶。由于组织蛋白酶在人类肿瘤进展、侵袭和转移的生物学中起着关键作用，这些发现应该为开发新型抗肿瘤药物用于临床环境铺平道路。
