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Name

Novel substance having DGAT inhibitory activities and therapeutic agent for treating metabolic diseases using the same

Organization name

PVA Saarland

Profile

Technical Summary

  • The present invention relates to a novel indole derivative or pharmaceutically available salts thereof, a method of preparing the same and a composition for preventing and treating metabolic diseases such as obesity, diabetes, hyperlipemia, arteriosclerosis and fatty liver, including the indole derivative as an effective component
  • The present invention may provide a health food composition for preventing or improving diseases such as obesity, diabetes, hyperlipemia, arteriosclerosis and fatty liver
  • Effective therapeutic effects have been confirmed through experiments using a simple animal model

Major Technical Data

Excellent effects of inhibiting DGAT enzymatic activities

  • It has been confirmed that the compounds significantly inhibit DGAT enzymatic activities in a concentration-dependent manner.
  • It has been confirmed that compounds 15, 27 and 32 have excellent effects of inhibiting DGAT enzymatic activities.

Inhibiting the biosynthesis of neutral fat in cells

  • DGAT enzymatic activities are measured using human-derived liver cells, HepG2

Toxicity Test

  • An Acute Toxicity Test was performedthrough an animal experiment

Technical Superiority

Effects of inhibiting DGAT enzymatic activities

  • The biosynthesis of neutral fat is inhibited by inhibiting DGAT associated with the synthesis of neutral fat
  • An increase in body weight induced by a high fat diet is suppressed.
  • Insulin resistance is improved and insulin sensitivity is enhanced
  • Biosynthesis of neutral fat in cells is inhibited.

Stability

  • No toxicity was found in experiments using an animal model
  • It may be used as a therapeutic agent for treating metabolic diseases since it has no toxicity to human bodies

 Applications

  • It may be used as a therapeutic agent for treating metabolic diseases such as obesity, diabetes, hyperlipemia, arteriosclerosis and fatty liver
  • It may be formulated into pharmaceutical preparations

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