Tsukamoto Sachiko, Tatsuno Mayu, van Soest Rob W M, Yokosawa Hideyoshi, Ohta Tomihisa
Faculty of Pharmaceutical Sciences, Kanazawa University, Takara-machi, Kanazawa 920-0934, Japan.
J Nat Prod. 2003 Sep;66(9):1181-5. doi: 10.1021/np030120v.
Seven new polyhydroxylated sterols, as well as the known agosterols A, C, and D2 (8-10), were isolated from a marine sponge Acanthodendrilla sp. as proteasome inhibitors. Their structures were elucidated on the basis of their spectral data, and they were characterized as agosterol congeners, which had been initially isolated from a marine sponge Spongia sp. and reported to reverse multidrug resistance in tumor cells. Among them, agosterol C (9) most strongly inhibited chymotrypsin-like activity of the proteasome with an IC50 value of 10 microg/mL.
从海洋海绵Acanthodendrilla sp.中分离出七种新的多羟基化甾醇以及已知的阿戈甾醇A、C和D2(8 - 10),作为蛋白酶体抑制剂。根据它们的光谱数据阐明了其结构,并将它们表征为阿戈甾醇同系物,这些同系物最初是从海洋海绵Spongia sp.中分离出来的,据报道可逆转肿瘤细胞中的多药耐药性。其中,阿戈甾醇C(9)对蛋白酶体的胰凝乳蛋白酶样活性抑制作用最强,IC50值为10微克/毫升。