Short Lecture 12 “Isolation of ecdysteroids from Cyanotis arachnoidea using scalable and sustainable centrifugal partition chromatography (CPC)”

Ecdysteroids are a special group of steroids that play an important role in regulating the molting and development of arthropods. This structurally diverse, non-toxic group of steroids has several beneficial bioactivities in mammals; hence they are widely consumed as dietary supplements. Some derivatives were shown to have cholesterol-lowering [1], antioxidant and neuroprotective [2] effects among others, and a recent in silico study suggests a probable anti-COVID-19 activity of an ecdysteroid (calonysterone) [3].

Our aim was to develop a scalable and cost-effective preparative CPC purification method that can tackle the increasing needs on both consumer and research sides.

After the LC-MS analysis of a commercial C. arachnoidea extract, we targeted 20-hydroxyecdysone; (20E) and 5 minor ecdysteroid components for preparation. Afterwards, their partitioning properties were studied in 43 two-phase liquid-liquid chromatographic solvent systems. Then, a laboratory-scale (250 mL rotor volume) and a pilot-scale CPC (2100 mL rotor volume) instrument was used to test 8 selected ternary systems in ascending or descending modes. The optimized method allowed us to achieve a sustainable, economic, and green isolation of 20E on a 10 g scale. Additionally, we performed economic semi-synthesis and purification of the minor ecdysteroid calonysterone.

The developed method is also applicable for the cost-effective and scalable fractionation of several minor natural ecdysteroid other than 20E from a variety of plant starting materials. This is expected to greatly contribute to future R&D activities in the utilization of ecdysteroids.

Acknowledgments

The NKFIH grant K134704 is acknowledged.

Publikationsverlauf

Artikel online veröffentlicht:
12. Dezember 2022

• References

• 1 Yahya Al N. et al. Phytoecdysteroids: Isolation and Biological Applications. American Journal of Science 2017; 5: 7-10
• 2 Hu J. et al. 20-Hydroxyecdysone Protects against Oxidative Stress-Induced Neuronal Injury by Scavenging Free Radicals and Modulating NF-κB and JNK Pathways. PLoS One 2012; 7 (12) e50764
• 3 Mubarak A. et al. Structure-based virtual screening and molecular dynamics of phytochemicals derived from Saudi medicinal plants to identify potential COVID-19 therapeutics. Arab J Chem 2020; 13: 7224-7234