Shipley Paul R, Donnelly Caitlin C A, Le Cuong H, Bernauer Ashley D, Klegeris Andis
Department of Chemistry, Irving K. Barber School of Arts and Sciences, University of British Columbia Okanagan, Kelowna, BC, V1V 1V7, Canada.
Int J Mol Med. 2009 Nov;24(5):711-5. doi: 10.3892/ijmm_00000283.
Asukamycin, a manumycin-type metabolite, was isolated by a rapid and easily scalable purification scheme. Thus far, studies on the biological activity of asukamycin have been limited to its role as an antibacterial and antifungal agent. By using five different tumor cell lines we demonstrate antineoplastic activity of asukamycin. It inhibited cell growth at concentrations similar to other members of the manumycin family (IC50 1-5 microM). Cytotoxicity of asukamycin was accompanied by activation of caspases 8 and 3 and was diminished by SB 202190, a specific p38 mitogen-activated protein kinase (MAPK) inhibitor. These data, in combination with earlier observations showing its low in vivo toxicity, indicate that further studies on the potential antitumor activity of asukamycin are warranted.
阿苏卡霉素是一种马红霉素型代谢产物，通过一种快速且易于扩大规模的纯化方案分离得到。迄今为止，关于阿苏卡霉素生物活性的研究仅限于其作为抗菌和抗真菌剂的作用。通过使用五种不同的肿瘤细胞系，我们证明了阿苏卡霉素具有抗肿瘤活性。它在与马红霉素家族其他成员相似的浓度下抑制细胞生长（半数抑制浓度为1 - 5微摩尔）。阿苏卡霉素的细胞毒性伴随着半胱天冬酶8和3的激活，并被特异性p38丝裂原活化蛋白激酶（MAPK）抑制剂SB 202190减弱。这些数据，结合早期显示其体内低毒性的观察结果，表明有必要进一步研究阿苏卡霉素的潜在抗肿瘤活性。
