title: Inhibition of the DHT-induced PSA secretion by Verbascum xanthophoeniceum and Serenoa repens extracts in human LNCaP prostate epithelial cells.
abstract: BACKGROUND
  Verbascum xanthophoeniceum is a mullein plant, typical of Balkan region and some parts of Turkey, traditionally used as phytotherapeutic agent due to its anti-inflammatory properties. It is rich in phenylethanoid and iridoid metabolites whose anti-inflammatory properties are under characterization.
  
  
  METHODS
  The role of Verbascum xanthophoeniceum crude methanolic extract and its isolated phenylethanoid glycoside verbascoside have been evaluated, in comparison to a saw palmetto extract, on a human in vitro model of androgen-regulated prostate epithelium, the LNCaP cell line. Cytotoxicity and DHT-induced free and total PSA secretion have been thoroughly studied.
  
  
  RESULTS
  We have found that similar to saw palmetto, Verbascum xanthophoeniceum extract and its isolated phenylethanoid glycoside verbascoside have no cytotoxicity in human LNCaP prostate epithelial cells, whereas an inhibitory effect on the DHT-induced free and total PSA secretion, a recognized anti-androgen like activity, has been shown in case of both Verbascum xanthophoeniceum extract and pure verbascoside. Furthermore, in the absence of the endogenous androgen DHT, an androgen-like activity in Verbascum xanthophoeniceum is detectable as it is for saw palmetto, suggesting that a mixed androgen-antiandrogen activity is present.
  
  
  CONCLUSIONS
  For the first time, Serenoa repens and Verbascum xanthophoeniceum extracts have shown an absence of cytotoxicity and an inhibitory effect on DHT-induced PSA secretion in an in vitro model of human prostate epithelium, whereas the phenylethanoid glycoside verbascoside appeared to explain only part of the Verbascum xanthophoeniceum inhibitory activity on PSA secretion.
authors.affiliation: Istituto Superiore di Sanità - ISS, Department of Food Safety and Veterinary Public Health, Food and Veterinary Toxicology Unit, viale Regina Elena 299, 00161 Rome, Italy; University Roma Tre, Department of Biology, Viale Guglielmo Marconi 446, I-00146 Rome, Italy. Electronic address: daniele430@alice.it.
authors.forename: D
authors.initials: D
authors.lastname: Marcoccia
authors.affiliation: Bulgarian Academy of Sciences, The Stephan Angeloff Institute of Microbiology, Laboratory of Applied Biotechnologies, Ruski 139 Boulevard, 4000 Plovdiv, Bulgaria. Electronic address: milengeorgiev@gbg.bg.
authors.forename: M I
authors.initials: MI
authors.lastname: Georgiev
authors.affiliation: Bulgarian Academy of Sciences, Institute of Organic Chemistry with Center of Phytochemistry, Acad. G. Bonchev Street, Boulevard 9, 1113 Sofia, Bulgaria. Electronic address: alipieva@orgchm.bas.bg.
authors.forename: K I
authors.initials: KI
authors.lastname: Alipieva
authors.affiliation: Istituto Superiore di Sanità - ISS, Department of Food Safety and Veterinary Public Health, Food and Veterinary Toxicology Unit, viale Regina Elena 299, 00161 Rome, Italy. Electronic address: stefano.lorenzetti@iss.it.
authors.forename: S
authors.initials: S
authors.lastname: Lorenzetti
mesh_terms: D000726:Androgen Antagonists / Q000302:isolation & purification / Q000494:pharmacology; D000728:Androgens / Q000302:isolation & purification / Q000494:pharmacology; D000893:Anti-Inflammatory Agents / Q000302:isolation & purification / Q000494:pharmacology; D002460:Cell Line; D013196:Dihydrotestosterone / Q000494:pharmacology; D004847:Epithelial Cells / Q000187:drug effects / Q000378:metabolism; D005960:Glucosides / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D008297:Male; D010636:Phenols / Q000302:isolation & purification / Q000494:pharmacology; D010936:Plant Extracts / Q000494:pharmacology*; D011467:Prostate / Q000166:cytology / Q000187:drug effects*; D017430:Prostate-Specific Antigen / Q000187:drug effects / Q000378:metabolism; D028024:Serenoa / Q000737:chemistry*; D014421:Turkey; D032265:Verbascum / Q000737:chemistry*; D059808:Polyphenols
chemical_list: D000726:Androgen Antagonists; D000728:Androgens; D000893:Anti-Inflammatory Agents; D013196:Dihydrotestosterone; D005960:Glucosides; D010636:Phenols; D010936:Plant Extracts; D017430:Prostate-Specific Antigen; C058956:acteoside; D059808:Polyphenols
keywords: LNCaP; Prostate; Prostate-specific antigen; Saw palmetto; Verbascoside (PubChem CID: 5281800); Verbascoside (acteoside); Verbascum xanthophoeniceum