From bench to counter: Discovery and validation of a peony extract as tyrosinase inhibiting cosmeceutical

• Published in: European journal of medicinal chemistry 2019-12, Vol.184, p.111738-111738, Article 111738
• Main Authors: Rainer, Bettina, Revoltella, Silvia, Mayr, Fabian, Moesslacher, Julia, Scalfari, Valentina, Kohl, Roland, Waltenberger, Birgit, Pagitz, Konrad, Siewert, Bianka, Schwaiger, Stefan, Stuppner, Hermann
• Format: Article
• Language: English
• Subjects: Adult; Agaricales - enzymology; Aged; Animals; Anti-melanogenesis; Cell Line, Tumor; Cell Survival - drug effects; Cosmeceuticals; Cosmeceuticals - chemistry; Cosmeceuticals - isolation & purification; Cosmeceuticals - pharmacology; Dose-Response Relationship, Drug; Drug Discovery; Female; Humans; Light; Male; Mice; Middle Aged; Molecular Structure; Monophenol Monooxygenase - antagonists & inhibitors; Monophenol Monooxygenase - metabolism; Paeonia - chemistry; Paeonia officinalis subsp. officinalis; Plant Extracts - chemistry; Plant Extracts - isolation & purification; Plant Extracts - pharmacology; Resveratroloside; Seeds - chemistry; Skin - drug effects; Skin - pathology; Structure-Activity Relationship; Tyrosinase
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2019.111738

The anti-melanogenic principle of peony (Paeonia officinalis subsp. officinalis) seeds was elucidated via activity-guided isolation. Resveratroloside (trans-resveratrol-4′-O-beta-d-glucopyranoside) was found to be the main metabolite of P. officinalis subsp. officinalis seeds and its tyrosinase inhibiting activity was confirmed via an enzymatic assay. Furthermore, the in vitro activity and the therapeutic window were studied employing the murine melanoma cell line B16F10. The results from the conducted stability assay and the high content of resveratroloside in the seeds (i.e. 10.4% dw) motivated us to push the extract forward to an in vivo tolerance assay. A clinical study with forty Caucasian participants proofed a good skin-tolerance with high moisture effect and reduction of pores. [Display omitted] •Resveratroloside was isolated as main metabolite from Paeonia officinalis subsp. officinalis seeds.•Resveratroloside is a potent inhibitor – not a substrate – of mushroom and murine Tyrosinase.•The extract of P. officinalis subsp. officinalis seeds is a promising cosmeceutical candidate.•Anti-melanogenic activity was enzymatically and in vitro tested.•In vivo tolerance of the extract was proven in a small study with 40 participants.