Petasiphenone, a Phenol Isolated from Cimicifuga Racemosa , in vitro Inhibits Proliferation of the Human Prostate Cancer Cell Line LNCaP

Division of Clinical and Experimental Endocrinology, University of Göttingen, Göttingen, Germany.
Planta Medica (Impact Factor: 2.15). 02/2007; 73(2):184-7. DOI: 10.1055/s-2006-957081
Source: PubMed


Extracts of Cimicifuga racemosa (L.) Nutt. (syn.: Actaea racemosa L.) (CR) inhibit the proliferation of the human prostate cancer cell line LNCaP. Recently, the phenylpropanoid ester 3,4-dihydroxyphenacyl caffeate (petasiphenone, 1) was isolated from CR. This substance is a structural homologue to petasiphenol ([3-(3,4-dihydroxyphenyl)-2-oxopropyl caffeate]), a compound produced by Petasites japonicus Sieb. & Zucc. which inhibits the growth of various human leukemia cell lines. Because of the structural similarity, we examined whether 1 affects the proliferation of LNCaP cells and the secretion of prostate-specific antigen (PSA). Under basal conditions as well as under co-incubation with 10 nM estradiol [E2 or 1 nM dihydrotestosterone (DHT)], 1 dose-dependently inhibited proliferation of LNCaP cells while PSA release per cell was not altered. We report for the first time that a defined compound isolated from CR inhibits the growth of the human prostate cancer cells LNCaP.

Download full-text


Available from: Adolf Nahrstedt
  • Source
    • "Petasiphenol, a phenolic compound from PJ was reported to be a potent antiangiogenic agent [23]. Petasiphenone, a phenol isolated from Climicuifuga racemosa also demonstrated inhibitory effects on the proliferation of a human prostate cancer line cell [14]. However, petasitenine, a pyrrolizidine alkaloid from the young flower stalk of PJ was associated with liver cell adenoma and hemangioendothelial sarcoma in rats [9,10]. "
    [Show abstract] [Hide abstract]
    ABSTRACT: The methanol extract from the leaves of Petasites japonicus Maxim (PJ) was studied for its (anti-)mutagenic effect with the SOS chromotest and reverse mutation assay. The (anti-)carcinogenic effects were evaluated by the cytotoxicity on human cancer line cells and by the function and the expression of gap junctions in rat liver epithelial cell. PJ extracts significantly decreased spontaneous beta-galactosidase activity and beta-galactosidase activity induced by a mutagen, ICR, in Salmonella (S.) typhimurium TA 1535/pSK 1002. All doses of the extract (0.08-100 mg/plate) decreased the reversion frequency induced by benzo (alpha)pyrene (BaP) in S. typhimurium TA 98. It decreased not only the spontaneous reversion frequency but also that induced by BaP in S. typhimurium TA 100. PJ extract showed greater cytotoxic effects on human stomach, colon and uterus cancer cells than on other cancer cell types and normal rat liver epithelial cells. Dye transfers though gap junctions were significantly increased by PJ extracts at concentrations greater than 200 microg/mL and the inhibition of dye transfer by 12-O-tetradecanoylphorobol-13-acetate (TPA) was obstructed in all concentrations of PJ. PJ significantly increased the numbers of gap junction protein connexin 43, and increased the protein expression decreased by TPA in a dose-dependent manner. Based on these findings, PJ is suggested to contain antimutagenic and anticarcionogenic compounds.
    Full-text · Article · Mar 2010 · Journal of veterinary science (Suwŏn-si, Korea)
  • Source
    [Show abstract] [Hide abstract]
    ABSTRACT: Black cohosh is commonly used to treat hot flashes and other symptoms associated with menopause. It is thought to have multiple mechanisms of action, including potential phytoestrogenic properties. This has caused some concern about its use by patients with hormone-sensitive cancer. This paper will present the results of a systematic review of the safety and efficacy of black cohosh (Cimicifuga racemosa [L.] Nutt.) in patients with cancer. A critical assessment of clinical (n = 5) and preclinical (n = 21) studies of black cohosh and cancer (breast and prostate) to treat hot flashes and other related symptoms is presented. In addition, clinical studies, case reports, animal studies, and in vitro assessments of the safety of black cohosh for patients with hormonally sensitive cancers is summarized and interpreted. In general, the research assessing efficacy of black cohosh for the treatment of hot flashes in women with breast cancer is inconclusive. There is laboratory evidence of antiproliferative properties but no confirmation from clinical studies for a protective role in cancer prevention. Black cohosh seems to have a relatively good safety profile. Concerns about liver toxicity are inconclusive. With relevance to cancer patients, black cohosh also seems not to exhibit phytoestrogenic activity and is in fact possibly an inhibitor of tumor growth. The use of black cohosh appears to be safe in breast cancer patients without risk for liver disease, although further research is needed in this and other populations.
    Full-text · Article · Sep 2007 · Supportive Care Cancer
  • [Show abstract] [Hide abstract]
    ABSTRACT: Aceaea racemosa (formerly Cimicifuga racemosa, black cohosh, AR) extracts have been widely used as an alternative to hormonal replacement therapy for menopausal symptoms. Recent evidences suggest AR extracts are also effective in protecting against postmenopausal bone loss. To determine whether AR has any direct anabolic effect on osteoblasts, we investigated the ethanolic extract of AR on bone nodule formation in mouse MC3T3-E1 preosteoblast cells. AR did not stimulate osteoblast proliferation. Rather, at high doses of 1000 ng/mL for 48 h, AR suppressed (7.2+/-0.9% vs. control) osteoblast proliferation. At 500 ng/mL, a significant increase in bone nodule formation was seen with Von Kossa staining. Using quantitative PCR analysis, AR was shown to enhance the gene expression of runx2 and osteocalcin. Co-treatment with ICI 182,780, the selective estrogen receptor antagonist, abolished the stimulatory effect of AR on runx2 and osteocalcin gene induction, as well as on bone nodule formation in MC3T3-E1 cells. This is a first report of the direct effect of AR on enhancement of bone nodule formation in osteoblasts, and this action was mediated via an estrogen receptor-dependent mechanism. The results provide a scientific rationale at the molecular level for the claim that AR can offer effective prevention of postmenopausal bone loss.
    No preview · Article · Jun 2008 · Bone
Show more