New bioactive compounds from aquatic endophyte <i>Chaetomium globosum</i>

<p>Two new oxidation products-related aureonitol and cytochalasan were isolated from <i>Chaetomium globosum</i> fermented in Chinese yam (<i>Dioscorea opposita</i>) and determined as 10,11-dihydroxyl- aureonitol (<b>1</b>) and yamchaetoglobosin A (<b>2</b>). Compound <b>2</b> 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 50 μM, 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 40 μM. Compounds <b>1</b>, <b>2</b> 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.</p