Synthesis of Pseudo-Phospholipids by Phospholipase D-Catalyzed Transphosphatidylation.

DOI DOI Web Site 2 Citations 48 References Open Access

Bibliographic Information

Other Title
  • ホスホリパーゼＤの触媒するホスファチジル基転移反応による機能性リン脂質誘導体の合成
  • ホスホリパーゼ D ノ ショクバイスル ホスファチジルキ テンイ ハンノウ ニ

Search this article

Description

We found that phospholipase D from Streptomyces sp. (PLDP) effectively catalyzed transphosphatidylation, i.e., the regiospecific transfer of the phosphatidyl residue from phosphatidylcholines to alkanols. The scope of this enzymatic reaction was investigated in detail to develop an efficient method for preparing various phospholipid derivatives. Using this enzymatic method, 5'-Ο-phosphatidyl derivatives of antitumor nucleosides were successfully synthesized to identify potent antitumor drugs. 5'-Ο-Phosphatidyl derivatives of DMDC (2'-deoxy-2'-methylenecytidine) and CNDAC [1- (2-C -cyano-2-deoxy-β-arabino-pentofuranosyl) cytosine], antitumor nucleosides developed by us, showed significant antitumor effects in mice which clearly surpassed those of parent compounds. We have also demonstrated that 5'-Ο-phosphatidylnucleosides can be used as a drug delivery system for lymph : 5'-Ο-phosphatidyl-5-fluorouridine given orally is absorbed via the deacylation-reacylation cycle, a specific pathway for natural phospholipids, to be transported selectively to the lymph.

Journal

Citations (2)*help

See more

References(48)*help

See more

Keywords

Details 詳細情報について

Report a problem

Back to top