Open Access

ARTICLE

In Vitro and in Silico Insights on the Biological Activities, Phenolic Compounds Composition of Hypericum perforatum L. Hairy Root Cultures

Oliver Tusevski^1,*, Marija Todorovska¹, Jasmina Petreska Stanoeva², Marina Stefova², Sonja Gadzovska Simic¹

1 Institute of Biology, Faculty of Natural Sciences and Mathematics, University “Ss. Cyril and Methodius”, Skopje, 1000, Republic of North Macedonia
2 Institute of Chemistry, Faculty of Natural Sciences and Mathematics, University “Ss. Cyril and Methodius”, Skopje, 1000, Republic of North Macedonia

* Corresponding Author: Oliver Tusevski. Email:

(This article belongs to the Special Issue: Plant Bioactive Compounds-Chemotaxonomic Significance, Antioxidant Properties, Potential Application as Food Ingredients as well as Therapeutics, and the Analytical Technology in Their Efficient Discovery)

Phyton-International Journal of Experimental Botany 2023, 92(3), 921-941. https://doi.org/10.32604/phyton.2023.024995

Received 16 June 2022; Accepted 07 September 2022; Issue published 29 November 2022

Abstract

Three Hypericum perforatum hairy root lines (HR B, HR F and HR H) along with non-transformed roots were analyzed for phenolic compounds composition and in vitro enzyme inhibitory properties. In silico molecular modeling was performed to predict the interactions of the most representative phenolic compounds in HR clones with enzymes related to depression, neurodegeneration and diabetes. Chromatographic analyses revealed that HR clones represent an efficient source of quinic acid and hydroxybenzoic acids, epicatechin and procyanidin derivatives, quercetin and kaempferol glycosides, as well numerous xanthones. In vitro antidepressant activity of HR extracts through monoamine oxidase A (MAO-A) inhibition was attributed to the production of oxygenated and prenylated xanthones. The neuroprotective potential of HR extracts was related to the accumulation of quercetin 6-C-glucoside, epicatechin, procyanidins and γ-mangostin isomers as potential inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Vanillic acid and prenylated xanthones in HR clones as promising inhibitors of tyrosinase additionally contributed to the neuroprotective activity. Five preeminent xanthones in HR (γ-mangostin, mangiferin, garcinone C, garcinone E and 1,3,7-trihydroxy-6-metoxy-8-prenyl xanthone) along with the flavonol quercetin 6-C-glucoside effectively inhibited α-amylase and α-glucosidase indicating the antidiabetic properties of HR extracts. Transgenic roots of H. perforatum can be exploited for the preparation of novel phytoproducts with multi-biological activities.

---

Keywords

---