Abstract
The hyperforin content of Hypericum perforatum herb was repeatedly reported to be responsible for a multitude of pharmacological
activities. Our recent report about the hyperforin accumulation in in vitro root cultures of H. perforatum provides an alternative perspective to achieve constant product quality and to serve
the rapidly growing market. In this study, the antiproliferative effect of a petroleum
ether extract from the in vitro root cultures was investigated. When normalized to 1 µM hyperforin content, the extract
reduced the viability of human keratinocytes (HaCaT) and human dermal fibroblast monolayers
to 33 and 36%, respectively, after 72 h of incubation. A cytotoxicity assay and live-dead
cell staining confirmed that the extract lacked a cytotoxic effect and that the reduction
in cell viability was mainly due to the antiproliferative activity. Application of
the 1 µM hyperforin-normalized extract to a 3D artificial skin construct significantly
reduced the proliferation of HaCaT in the presence of fibroblasts. This effect was
proved by the reduction in thickness of the epidermal construct from 100 µm (control)
to 17 µm (treated). Notably, 1 µM pure hyperforin lacked effectiveness in both monolayer
cultures and 3D artificial skin constructs. Nor were fractions of the extract containing
colupulone and xanthones active. The combination of these constituents also failed
to reassemble the antiproliferative activity, which indicates a synergistic role of
yet unidentified components present in the extract. Our findings may introduce H. perforatum root cultures as a novel lead system for the treatment of hypertrophic scars.
Key words
Hypericum perforatum
- Hypericaceae - keratinocytes - fibroblasts - root culture - root extract
