Pharmaceutical Organic Chemistry

Research Project

Development of anti-diabetic drugs: structure-activity relationship studies on a novel sulfonium sulfate inner salt, salacinol, a potent a-glucosidase inhibitor from Ayurvedic Traditional medicine, Salacia.
Development of calcium signal modulators: structure-activity relationship studies on a novel glycolipid, acremomannolipin A, a potential calcium signal modulator from the filamentous fungus Acremonium strictum.
Synthetic studies on natural polyphenol glucosides as antitumor agents.
Synthetic studies on aporphine and benzylisoquinoline alkaloids as melanogenesis inhibitors.
Probe design and application for chemical biology research
Nonribosomal synthesis of non-natural products
Biochemical investigations of natural product biosynthetic enzymes fatty acid synthase, polyketide synthase, and nonribosomal peptide synthetase.

Introduction

Our studies focus on the synthesis and structure activity relationships of bioactive natural products which have been isolated by our collaborative research groups. All the projects listed above are also being carried out with the energetic support by of many collaborative groups including pharmaceutical companies. Salacinol-related compound activity synthesized by our division can immediately be evaluated by a bioassay group in the Pharmacognosy Laboratory of Kyoto Pharmaceutical University and/or Pharmaceutical Research and Techonology Institute in this university. The target compounds are designed with the aid of in silico computer calculations conducted in the Laboratory of Computational Drug Design and Discovery in this department. With the support of established pharmaceutical companies, clinical examinations of salacinol extracts were conducted, and now currently salacinol-containing functional foods are on the market for anti-diabetic purposes. Also with the aid of many collaborators we have engaged in successful research and development on acremomannolipin A (as a calcium signal modulator), aporphine and benzylisoquinoline alkaloids (as melanogenesis inhibitors), mangiferin (as an anti-cancer agent), tiliroside (as an anti-obesity agent).
Furthermore, we pursue interdisciplinary research in the fields of synthetic organic chemistry, chemical biology, and natural product biosynthesis.