New bioactive compounds from aquatic endophyte Chaetomium globosum

Two new oxidation products-related aureonitol and cytochalasan were isolated from Chaetomium globosum fermented in Chinese yam (Dioscorea opposita)and determined as 10,11-dihydroxyl- aureonitol (1) and yamchaetoglobosin A (2). Compound 2 indicated significant inhibitory effect on nitric oxide production in LPS-activated macrophages, anti-acetylcholinesterase activity with the inhibition ratios of 92.5, 38.2% at 50M, and cytotoxicity to HL-60, A-549, SMMC-7721, MCF-7 and SW480 with the range of inhibition ratio at 51-96% for a concentration of 40M. Compounds 1, 2 showed weak anticoagulant activity with PT at 16.8 s. Few work was reported on the anti-acetylcholinesterase, and anticoagulant activities of aureonitol, and cytochalasan derivatives. The preliminary structure-activity relationship stated that the oxidation ring-opening in yamchaetoglobosin A can retain the inhibitory effect against NO production and tumor cell.[GRAPHICS].

从山药（Dioscorea opposita）中发酵的球毛壳菌（Chaetomium globosum）中分离出两种新的氧化产物相关的金黄糖醇和细胞松弛素，分别鉴定为10,11 - 二羟基金黄糖醇（1）和山药球毛壳甲素A（2）。化合物2对脂多糖激活的巨噬细胞中一氧化氮的产生有显著抑制作用，在50μM时对乙酰胆碱酯酶的抑制率分别为92.5%、38.2%，对HL - 60、A - 549、SMMC - 7721、MCF - 7和SW480细胞在40μM浓度下的抑制率范围为51 - 96%。化合物1、2的凝血酶原时间（PT）为16.8秒，显示出较弱的抗凝活性。关于金黄糖醇和细胞松弛素衍生物的抗乙酰胆碱酯酶和抗凝活性的报道较少。初步的构效关系表明，山药球毛壳甲素A的氧化开环能保留对一氧化氮产生和肿瘤细胞的抑制作用。[图表]