title: Hyperforin production in Hypericum perforatum root cultures.
abstract: Extracts of the medicinal plant Hypericum perforatum are used to treat depression and skin irritation. A major API is hyperforin, characterized by sensitivity to light, oxygen and temperature. Total synthesis of hyperforin is challenging and its content in field-grown plants is variable. We have established in vitro cultures of auxin-induced roots, which are capable of producing hyperforin, as indicated by HPLC-DAD and ESI-MS analyses. The extraction yield and the productivity upon use of petroleum ether after solvent screening were ∼5 mg/g DW and ∼50 mg/L culture after six weeks of cultivation. The root cultures also contained secohyperforin and lupulones, which were not yet detected in intact plants. In contrast, they lacked another class of typical H. perforatum constituents, hypericins, as indicated by the analysis of methanolic extracts. Hyperforins and lupulones were stabilized and enriched as dicyclohexylammonium salts. Upon up-scaling of biomass production and downstream processing, H. perforatum root cultures may provide an alternative platform for the preparation of medicinal extracts and the isolation of APIs.
authors.affiliation: Institute of Pharmaceutical Biology, Technische Universität Braunschweig, Braunschweig, Germany; Center of Pharmaceutical Engineering, Technische Universität Braunschweig, Braunschweig, Germany. Electronic address: m.gaid@tu-bs.de.
authors.forename: Mariam
authors.initials: M
authors.lastname: Gaid
authors.affiliation: Institute of Chemical and Thermal Process Engineering, Technische Universität Braunschweig, Braunschweig, Germany; Center of Pharmaceutical Engineering, Technische Universität Braunschweig, Braunschweig, Germany. Electronic address: p.haas@tu-bs.de.
authors.forename: Paul
authors.initials: P
authors.lastname: Haas
authors.affiliation: Institute of Pharmaceutical Biology, Technische Universität Braunschweig, Braunschweig, Germany; Center of Pharmaceutical Engineering, Technische Universität Braunschweig, Braunschweig, Germany. Electronic address: t.beuerle@tu-bs.de.
authors.forename: Till
authors.initials: T
authors.lastname: Beuerle
authors.affiliation: Institute of Chemical and Thermal Process Engineering, Technische Universität Braunschweig, Braunschweig, Germany; Center of Pharmaceutical Engineering, Technische Universität Braunschweig, Braunschweig, Germany. Electronic address: s.scholl@tu-bs.de.
authors.forename: Stephan
authors.initials: S
authors.lastname: Scholl
authors.affiliation: Institute of Pharmaceutical Biology, Technische Universität Braunschweig, Braunschweig, Germany; Center of Pharmaceutical Engineering, Technische Universität Braunschweig, Braunschweig, Germany. Electronic address: l.beerhues@tu-bs.de.
authors.forename: Ludger
authors.initials: L
authors.lastname: Beerhues
mesh_terms: D019149:Bioreactors; D020902:Hypericum / Q000737:chemistry / Q000378:metabolism*; D010696:Phloroglucinol / Q000031:analogs & derivatives* / Q000032:analysis / Q000737:chemistry / Q000378:metabolism; D010936:Plant Extracts; D018517:Plant Roots / Q000737:chemistry / Q000378:metabolism*; D013729:Terpenes / Q000032:analysis / Q000737:chemistry / Q000378:metabolism*
chemical_list: D010936:Plant Extracts; D013729:Terpenes; C008299:lupulon; D010696:Phloroglucinol; C001654:hyperforin
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)