A practical, biomimetic, one-pot synthesis of firefly luciferin

Sci Rep. 2024 Dec 25;14(1):30461. doi: 10.1038/s41598-024-82996-2.

Abstract

The bioluminescence reaction of firefly luciferase with D-luciferin has become an indispensable imaging technique in modern biology and life science experiments, but the high cost of D-luciferin is limiting its further application. Here, we report a practical, one-pot synthesis of D-luciferin from p-benzoquinone (p-BQ), L-cysteine methyl ester and D-cysteine, with an overall yield of 46%. Our route, which is six steps in length and proceeds via 2-cyano-6-hydroxybenzothiazole, is inspired by the mechanistic study of our previously reported biomimetic, non-enzymatic, one-pot formation of L-luciferin from p-BQ and L-cysteine. Advantages of our route include its high yield, low cost, use of only inexpensive, commercially available reagents, without requiring strictly anhydrous and oxygen-free conditions, and elevated temperatures.

Keywords: p-benzoquinone; Bioluminescence; Cysteine; D-firefly luciferin; One-pot synthesis.

MeSH terms

  • Animals
  • Benzoquinones / chemistry
  • Benzothiazoles / chemical synthesis
  • Benzothiazoles / chemistry
  • Biomimetics / methods
  • Cysteine / analogs & derivatives
  • Cysteine / chemistry
  • Fireflies
  • Firefly Luciferin* / chemistry
  • Firefly Luciferin* / metabolism
  • Luciferases, Firefly / metabolism

Substances

  • Firefly Luciferin
  • Benzoquinones
  • Benzothiazoles
  • Cysteine
  • quinone
  • Luciferases, Firefly
  • D-luciferin