Scale-Up Preparation of Crocins I and II from Gardeniajasminoides by a Two-Step Chromatographic Approach and Their Inhibitory Activity Against ATP Citrate Lyase

Molecules. 2021 May 24;26(11):3137. doi: 10.3390/molecules26113137.

Abstract

Crocins are highly valuable natural compounds for treating human disorders, and they are also high-end spices and colorants in the food industry. Due to the limitation of obtaining this type of highly polar compound, the commercial prices of crocins I and II are expensive. In this study, macroporous resin column chromatography combined with high-speed counter-current chromatography (HSCCC) was used to purify crocins I and II from natural sources. With only two chromatographic steps, both compounds were simultaneously isolated from the dry fruit of Gardenia jasminoides, which is a cheap herbal medicine distributed in a number of countries. In an effort to shorten the isolation time and reduce solvent usage, forward and reverse rotations were successively utilized in the HSCCC isolation procedure. Crocins I and II were simultaneously obtained from a herbal resource with high recoveries of 0.5% and 0.1%, respectively, and high purities of 98.7% and 99.1%, respectively, by HPLC analysis. The optimized preparation method was proven to be highly efficient, convenient, and cost-effective. Crocins I and II exhibited inhibitory activity against ATP citrate lyase, and their IC50 values were determined to be 36.3 ± 6.24 and 29.7 ± 7.41 μM, respectively.

Keywords: crocins; high-speed counter-current chromatography; inhibitory activity on ATP citrate lyase; macroporous resin column chromatography; preparation method.

MeSH terms

  • ATP Citrate (pro-S)-Lyase / antagonists & inhibitors*
  • Carotenoids / isolation & purification*
  • Carotenoids / pharmacology
  • Countercurrent Distribution / methods*
  • Enzyme Inhibitors / pharmacology*
  • Gardenia / chemistry*
  • Spectrum Analysis / methods

Substances

  • Enzyme Inhibitors
  • Carotenoids
  • crocin
  • ATP Citrate (pro-S)-Lyase