Yano Tatsuya, Aoyagi Azusa, Kozuma Shiho, Kawamura Yoko, Tanaka Isshin, Suzuki Yasuhiro, Takamatsu Yasuyuki, Takatsu Toshio, Inukai Masatoshi
Lead Discovery Research Laboratories, Sankyo Co., Ltd., Hiromachi, Tokyo, Japan.
J Antibiot (Tokyo). 2007 Feb;60(2):136-42. doi: 10.1038/ja.2007.13.
In the course of a screening for inositol phosphorylceramide (IPC) synthase inhibitors, the novel inhibitors pleofungins A, B, C, and D were found in a mycelial extract of a fungus, Phoma sp. SANK13899. Purification was performed by 50% methanol and ethyl acetate extraction, reversed phase open-column chromatography, and HPLC separations. Pleofungin A inhibited the IPC synthase of Saccharomyces cerevisiae and Aspergillus fumigatus at IC(50) values of 16 and 1.0 ng/ml, respectively. The inhibitor also suppressed the growth of Candida albicans, Cryptococcus neoformans, and A. fumigatus at MIC values of 2.0, 0.3, and 0.5 mug/ml, respectively. These biological properties indicate that pleofungins belong to a novel class of IPC synthase inhibitors efficacious against A. fumigatus.
在对肌醇磷酸神经酰胺（IPC）合酶抑制剂的筛选过程中，从真菌茎点霉属SANK13899的菌丝体提取物中发现了新型抑制剂多球霉素A、B、C和D。通过50%甲醇和乙酸乙酯萃取、反相开放柱色谱法以及高效液相色谱分离进行纯化。多球霉素A对酿酒酵母和烟曲霉的IPC合酶的IC50值分别为16和1.0 ng/ml。该抑制剂对白色念珠菌、新型隐球菌和烟曲霉的最低抑菌浓度（MIC）值分别为2.0、0.3和0.5 μg/ml时也能抑制其生长。这些生物学特性表明多球霉素属于一类对烟曲霉有效的新型IPC合酶抑制剂。
