title: Pharmacokinetics of 23-epi-26-deoxyactein in women after oral administration of a standardized extract of black cohosh.
abstract: Dietary supplements containing black cohosh are alternatives to conventional hormone replacement therapy in menopause. This study investigates the maximum tolerated dose of a 75% ethanol extract of black cohosh and determines the pharmacokinetics of one of its most abundant triterpene glycosides, 23-epi-26-deoxyactein. Single doses of black cohosh extract containing 1.4, 2.8, or 5.6 mg of 23-epi-26-deoxyactein were administered to 15 healthy, menopausal women. Serial blood samples and 24-h urine samples were obtained; blood chemistry, hormonal levels, and 23-epi-26-deoxyactein levels were determined. No acute toxicity or estrogenic hormone effects were observed. Pharmacokinetic analyses of 23-epi-26-deoxyactein in sera indicated that the maximum concentration and area under the curve increased proportionately with dosage, and that the half-life was ~2 h for all dosages. Less than 0.01% of the 23-epi-26-deoxyactein was recovered in urine 24 h after administration. No phase I or phase II metabolites were observed either in clinical specimens or in vitro.
authors.affiliation: UIC/NIH Center for Botanical Dietary Supplements Research, University of Illinois College of Pharmacy, Department of Medicinal Chemistry and Pharmacognosy, Chicago, Illinois, USA. breemen@uic.edu
authors.forename: R B
authors.initials: RB
authors.lastname: van Breemen
authors.forename: W
authors.initials: W
authors.lastname: Liang
authors.forename: S
authors.initials: S
authors.lastname: Banuvar
authors.forename: L P
authors.initials: LP
authors.lastname: Shulman
authors.forename: Y
authors.initials: Y
authors.lastname: Pang
authors.forename: Y
authors.initials: Y
authors.lastname: Tao
authors.forename: D
authors.initials: D
authors.lastname: Nikolic
authors.forename: K M
authors.initials: KM
authors.lastname: Krock
authors.forename: D S
authors.initials: DS
authors.lastname: Fabricant
authors.forename: S-N
authors.initials: SN
authors.lastname: Chen
authors.forename: S
authors.initials: S
authors.lastname: Hedayat
authors.forename: J L
authors.initials: JL
authors.lastname: Bolton
authors.forename: G F
authors.initials: GF
authors.lastname: Pauli
authors.forename: C E
authors.initials: CE
authors.lastname: Piersen
authors.forename: E C
authors.initials: EC
authors.lastname: Krause
authors.forename: S E
authors.initials: SE
authors.lastname: Geller
authors.forename: N R
authors.initials: NR
authors.lastname: Farnsworth
mesh_terms: D000284:Administration, Oral; D019540:Area Under Curve; D031885:Cimicifuga / Q000737:chemistry*; D019587:Dietary Supplements; D004305:Dose-Response Relationship, Drug; D005260:Female; D006207:Half-Life; D006801:Humans; D020714:Maximum Tolerated Dose; D008593:Menopause; D008875:Middle Aged; D010936:Plant Extracts / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D012503:Saponins / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D014315:Triterpenes / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*
chemical_list: D010936:Plant Extracts; D012503:Saponins; D014315:Triterpenes; C457248:23-epi-26-deoxyactein