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Hyperforin production in Hypericum perforatum root cultures.

Mariam Gaid¹, Paul Haas², Till Beuerle¹

¹Institute of Pharmaceutical Biology, Technische Universität Braunschweig, Braunschweig, Germany; Center of Pharmaceutical Engineering, Technische Universität Braunschweig, Braunschweig, Germany.

Journal of Biotechnology

|February 16, 2016

Summary

In vitro root cultures of Hypericum perforatum produce hyperforin, a key compound for treating depression and skin irritation. This offers a stable, alternative source for medicinal extracts and active pharmaceutical ingredients (APIs).

Keywords:

Adhyperforin (PubChem CID: 90658004)Adlupulone (PubChem CID: 9909740)Adsecohyperforin (PubChem CID: 101442298)Hyperforin (PubChem CID: 441298)Hyperforin dicyclohexylammonium salt (PubChem CID: 46926346)Hyperforins Hypericins Hypericum perforatum Lupulone (PubChem CID: 68051)Lupulones Root cultures Secohyperforin (PubChem CID: 101442297)

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Area of Science:

Plant Biotechnology
Pharmacognosy
Medicinal Chemistry

Background:

Hypericum perforatum extracts are used for depression and skin conditions.
Hyperforin, a major active pharmaceutical ingredient (API), is unstable and difficult to synthesize.
Field-grown plant hyperforin content is variable.

Purpose of the Study:

To establish in vitro root cultures of H. perforatum for hyperforin production.
To characterize the phytochemical profile of these root cultures.
To assess the potential of root cultures as an alternative source for APIs.

Main Methods:

Establishment of auxin-induced H. perforatum root cultures.
High-Performance Liquid Chromatography-Diode Array Detection (HPLC-DAD) and Electrospray Ionization Mass Spectrometry (ESI-MS) for analysis.
Solvent screening and extraction yield optimization.
Dicyclohexylammonium salt formation for stabilization.

Main Results:

Root cultures successfully produced hyperforin, confirmed by HPLC-DAD and ESI-MS.
Extraction yield reached ~5 mg/g DW, with productivity of ~50 mg/L culture.
Secohyperforin and lupulones were detected, but hypericins were absent.
Stabilization and enrichment of hyperforins and lupulones as dicyclohexylammonium salts were achieved.

Conclusions:

H. perforatum root cultures represent a viable in vitro system for hyperforin production.
This platform offers a stable and potentially scalable alternative for obtaining medicinal compounds.
Root cultures provide a unique phytochemical profile, including compounds not found in intact plants.