Effect of essential oils, such as raspberry ketone and its derivatives, on antiandrogenic activity based on in vitro reporter gene assay

被引：25
|
作者：
Ogawa, Yoshihisa [1 ]
Akamatsu, Miki [2 ]
Hotta, Yudai [1 ]
Hosoda, Akifumi [1 ]
Tamura, Hiroto [1 ]
机构：
[1] Meijo Univ, Dept Environm Biosci, Nagoya, Aichi 4688502, Japan
[2] Kyoto Univ, Grad Sch Agr, Kyoto 6068502, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 07期
关键词：
Androgen; Antagonist; Essential oil; CoMFA; Drug design; RECEPTOR AGONISTS; ANDROGEN; ANTAGONISTS; BINDING; MDA-KB2; COMFA;
D O I：
10.1016/j.bmcl.2010.02.059
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The effect of essential oils, such as raspberry ketone, on androgen (AR) receptor was investigated using a MDA-kb2 human breast cancer cell line for predicting potential AR activity. Among them, eugenol had the highest AR antagonistic activity with its IC50 value of 19 mu M. Raspberry ketone, which has threefold higher anti-obese activity than that of capsaicin, also had AR antagonist activity with its IC50 value of 252 mu M. Based on these findings, a more precise CoMFA model was proposed as follows: pIC(50) [log (1/IC50)] = 3.77 + [CoMFA field terms] (n = 39, s = 0.249, r(2) = 0.834, s(cv) = 0.507, q(2) = 0.311 (three components). (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2111 / 2114
页数：4
相关论文
共 50 条
  • [31] Species Differences in Response to Binding Interactions of Bisphenol A and its Analogs with the Modeled Estrogen Receptor 1 and In Vitro Reporter Gene Assay in Human and Zebrafish
    Park, Chang Gyun
    Singh, Nancy
    Ryu, Chang Seon
    Yoon, Ju Yong
    Esterhuizen, Maranda
    Kim, Young Jun
    ENVIRONMENTAL TOXICOLOGY AND CHEMISTRY, 2022, 41 (10) : 2431 - 2443
  • [32] Reporter gene assay against lipophilic chemicals based on site-specific genomic recombination of a nuclear receptor gene, its response element, and a luciferase reporter gene within a stable HeLa cell line
    Mori, Tetsushi
    Saito, Fumiyo
    Yoshino, Tomoko
    Takeyama, Haruko
    Matsunaga, Tadashi
    BIOTECHNOLOGY AND BIOENGINEERING, 2008, 99 (06) : 1453 - 1461
  • [33] Incorporation of ifosfamide into various essential oils -based nanoemulsions ameliorates its apoptotic effect in the cancers cells
    Mayson H. Alkhatib
    Sahar M. AlMotwaa
    Huda M. Alkreathy
    Scientific Reports, 9
  • [34] Incorporation of ifosfamide into various essential oils -based nanoemulsions ameliorates its apoptotic effect in the cancers cells
    Alkhatib, Mayson H.
    AlMotwaa, Sahar M.
    Alkreathy, Huda M.
    SCIENTIFIC REPORTS, 2019, 9 (1)
  • [35] Effect of in vitro metabolism on the endocrine activity of testosterone in a yeast-based reportergene assay
    Kamp, H. G.
    Fabian, E.
    Damm, G.
    Huencr, H. -A.
    Verlohner, A.
    Landsiedel, R.
    van Ravenzwaay, B.
    NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 2007, 375 : 74 - 74
  • [36] A cellular reporter assay to monitor insulin receptor kinase activity based on STAT 5-dependent luciferase gene expression
    Storz, P
    Döppler, H
    Horn-Müller, J
    Groner, B
    Pfizenmaier, K
    Müller, G
    ANALYTICAL BIOCHEMISTRY, 1999, 276 (01) : 97 - 104
  • [37] In vitro antifungal activity and cytotoxic effect of essential oils and extracts of medicinal and aromatic plants against Candida krusei and Aspergillus fumigatus
    Correa-Royero, Julieth
    Tangarife, Veronica
    Duran, Camilo
    Stashenko, Elena
    Mesa-Arango, Ana
    REVISTA BRASILEIRA DE FARMACOGNOSIA-BRAZILIAN JOURNAL OF PHARMACOGNOSY, 2010, 20 (05): : 734 - 741
  • [38] Gastroprotective effect of alpha-pinene and its correlation with antiulcerogenic activity of essential oils obtained from Hyptis species
    Pinheiro, Marcelo de Almeida
    Magalhaes, Rafael Matos
    Torres, Danielle Mesquita
    Cavalcante, Rodrigo Cardoso
    Xavier Mota, Francisca Sheila
    Araujo Oliveira Coelho, Emanuela Maria
    Moreira, Henrique Pires
    Lima, Glauber Cruz
    da Costa Araujo, Pamella Cristina
    Leal Cardoso, Jose Henrique
    Coelho de Souza, Andrelina Noronha
    Leite Diniz, Lucio Ricardo
    PHARMACOGNOSY MAGAZINE, 2015, 11 (41) : 123 - 130
  • [39] Antimicrobial Activity of Essential Oils in Vapor Phase In Vitro and Its Application in Combination with Lactic Acid to Improve Chicken Breast Shelf Life
    de la Cruz, Jovany Fortino Rivera
    Schelegueda, Laura Ines
    Delcarlo, Sofia Belen
    Gliemmo, Maria Fernanda
    Campos, Carmen Adriana
    FOODS, 2023, 12 (22)
  • [40] A novel cell-based in vitro assay for antiviral activity of interferons α, β, and γ by qPCR of MxA gene expression
    Saber M.A.
    Okasha H.
    Khorshed F.
    Samir S.
    Recent Patents on Biotechnology, 2021, 15 (01) : 67 - 75
12345