総説および総合論文
Chemically Engineered Extractsからの新規医薬シーズ探索
2019 年 77 巻 9 号 p. 895-903
詳細
2019 年 77 巻 9 号 p. 895-903
In the development of drugs, the structural diversity of natural compounds plays a pivotal role and is extensive but not unlimited. Semisynthetic compounds produced by diversification of a natural product through the chemical transformation was valuable as new medicinal seeds. Chemically Engineered Extracts (CEEs) are an ideal tool for obtaining semisynthetic natural compounds. CEEs are natural crude extracts directly derivatized by chemical reactions and thus can yield various novel compounds at once. Coumarins and coumarin dimers (including the unprecedented tetracyclic coumarin derivatives) were isolated from CEEs of the marine-derived fungus Eurotium rubrum. The structures of these compounds were established using NMR, MS and IR methods. The absolute configuration of tetracyclic coumarin structure was determined by Electronic Circular Dichroism (ECD) calculations. Isolated coumarins and coumarin dimers showed stronger activity for anti-melanogenesis. These results showed that chemically engineered extract generated medicinal seeds for new drugs.
