Nukoolkarn Veena S, Saen-oon Suwipa, Rungrotmongkol Thanyada, Hannongbua Supot, Ingkaninan Kornkanok, Suwanborirux Khanit
Department of Pharmacognosy, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand.
Bioorg Med Chem. 2008 Jul 1;16(13):6560-7. doi: 10.1016/j.bmc.2008.05.027. Epub 2008 May 15.
Two pyridoacridine alkaloids, including a known petrosamine and a new 2-bromoamphimedine were isolated from a Thai marine sponge Petrosia n. sp. The alkaloids were characterized on the basis of 1D and 2D NMR, MS, and IR spectroscopy. Only petrosamine showed strong acetylcholinesterase inhibitory activity approximately six times higher than that of the reference galanthamine. A computational docking study of petrosamine with the enzyme from the electric eel Torpedo californica (TcAChE) showed the major contribution to the petrosamine-TcAChE interaction to be arising from the quaternary ammonium group of petrosamine.
从泰国海洋海绵新种Petrosia中分离出两种吡啶吖啶生物碱，包括一种已知的石蒜胺和一种新的2-溴海绵胺。通过一维和二维核磁共振、质谱和红外光谱对这些生物碱进行了表征。只有石蒜胺表现出较强的乙酰胆碱酯酶抑制活性，约为参比加兰他敏的六倍。对石蒜胺与电鳗（Torpedo californica，TcAChE）的酶进行的计算对接研究表明，石蒜胺与TcAChE相互作用的主要贡献来自石蒜胺的季铵基团。
