Wulff Jeremy E, Herzon Seth B, Siegrist Romain, Myers Andrew G
Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, USA.
J Am Chem Soc. 2007 Apr 25;129(16):4898-9. doi: 10.1021/ja0690971. Epub 2007 Mar 31.
We report that the dimeric alkaloid stephacidin B () and the monomeric alkaloid avrainvillamide () function equivalently within experimental error to inhibit the growth of four different cultured human cancer cell lines. We also show that the proportion of the monomer greatly outweighs that of the dimer in the medium of incubation, and that the half-life for the transformation of to is short relative to the half-life of cell division. Finally, using a monomer-based affinity reagent, we provide evidence that the monomer () interacts with intracellular thiol-containing proteins, likely by covalent modification.
我们报告称，二聚体生物碱stephacidin B（）和单体生物碱avrainvillamide（）在实验误差范围内具有同等功能，可抑制四种不同培养的人类癌细胞系的生长。我们还表明，在孵育培养基中单体的比例大大超过二聚体，并且从转化为的半衰期相对于细胞分裂的半衰期较短。最后，使用基于单体的亲和试剂，我们提供证据表明单体（）可能通过共价修饰与细胞内含硫醇的蛋白质相互作用。
