Nelumal A, the Active Principle of Ligularia nelumbifolia, is a Novel Aromatase Inhibitor

被引:0
|
作者
Epifano, Francesco [1 ]
Genovese, Salvatore [1 ]
Fiorito, Serena [1 ]
Nde, Chantal Magne [2 ]
Clyne, Colin [2 ,3 ]
机构
[1] Univ G dAnnunzio, Dept Pharm, I-66100 Chieti, CH, Italy
[2] Prince Henrys Inst Med Res, Canc Drug Discovery Lab, Clayton, Vic 3168, Australia
[3] Monash Univ, Dept Biochem & Mol Biol, Clayton, Vic 3168, Australia
关键词
Aromatase inhibitors; Ligularia nelumbifolia; Nelumal A; Oxyprenylated secondary metabolites;
D O I
暂无
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Nelumal A, the active principle of Ligularia nelumbifolia was preliminarily tested as an aromatase inhibitors in HEK293 cells trartsfected with aromatase cDNA and using anastrazole as the reference drug. This screening revealed that it showed an appreciable level of inhibition. Subsequent experiments aimed to evaluate the aromatase activity and expression in KGN cells confirmed that the title natural product, after an incubation of 48 h, compared favourably with artastrazole (1 mu M) in the concentration range 10 - 30 mu M. Moreover, nelumal A (30 mu M) abolished the aromatase mRNA expression in the same cell line.
引用
收藏
页码:823 / 824
页数:2
相关论文
共 50 条
  • [31] NOVEL ANIMAL MODEL OF AROMATASE INHIBITOR-INDUCED ARTHRALGIA SUGGESTS AN ESTROGEN-INDEPENDENT INFLAMMATORY MECHANISM
    Young, N. A.
    Thomas, E.
    Snoad, B.
    Sharma, J.
    Mobeen, M.
    DeVries, A. C.
    Bratasz, A.
    Lustberg, M.
    Jarjour, W.
    Reinbolt, R.
    ANNALS OF THE RHEUMATIC DISEASES, 2017, 76 : 222 - 222
  • [32] A double-blind study of MPV-2213ad, a novel aromatase inhibitor, in healthy male subjects
    O. Ahokoski
    K. Irjala
    S. Huhtala
    E. Salminen
    H. Scheinin
    R. Huupponen
    European Journal of Clinical Pharmacology, 1999, 55 : 27 - 34
  • [33] Novel use of an aromatase inhibitor for fertility preservation via embryo cryopreservation in endometrial cancer: A case report.
    Oktay, KH
    Buyuk, E
    Rosenwaks, Z
    FERTILITY AND STERILITY, 2003, 80 : S144 - S144
  • [34] Approaches to the synthesis of a novel, anti-HIV active integrase inhibitor
    Okello, Maurice
    Nishonov, Malik
    Singh, Pankaj
    Mishra, Sanjay
    Mangu, Naveen
    Seo, Byung
    Gund, Machhindra
    Nair, Vasu
    ORGANIC & BIOMOLECULAR CHEMISTRY, 2013, 11 (45) : 7852 - 7858
  • [35] Efficacy of a novel, orally active cytokine inhibitor in a model of rheumatoid arthritis
    Morand, E
    Tapley, P
    Hall, P
    di Nezza, L
    Gilbert, T
    Yang, YH
    Danylec, B
    Iskander, M
    ARTHRITIS AND RHEUMATISM, 2005, 52 (09): : S351 - S351
  • [36] Synthesis and pharmacological evaluation of a novel orally active factor Xa inhibitor
    Nishida, H
    Ohkouchi, M
    Mukaihira, T
    Saitoh, F
    Nakamura, Y
    Miyazaki, Y
    Satoh, T
    Mizuno, M
    Kamino, T
    Hosaka, Y
    Shinozaki, M
    Oono, T
    Muramatsu, H
    Shiromizu, I
    Matsusue, T
    Kamiya, M
    Miyauchi, M
    Yokoyama, T
    Kakinuma, C
    Ogihara, T
    Yanagibashi, K
    Isomura, Y
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 230 : U2660 - U2661
  • [37] Vorozole (Rivizor™):: an active and well tolerated new aromatase inhibitor for the treatment of advanced breast cancer patients with prior tamoxifen exposure
    Paridaens, R
    Roy, JA
    Nooij, M
    Klijn, J
    Houston, SJ
    Beex, LVAM
    Vinholes, J
    Tomiak, E
    Van Vreckem, A
    Langenaeken, C
    Van Glabbeke, M
    Piccart, MJ
    ANTI-CANCER DRUGS, 1998, 9 (01) : 29 - 35
  • [38] The Aromatase Inhibitor Anastrozole: A Novel Treatment for Complex Atypical Endometrial Hyperplasia in Premenopausal Women Who Desire Fertility Preservation
    Rubal, Lauren
    Allen, Rene
    Stanczyk, Frank
    Patel, Sherfaraz
    Bendikson, Kristin
    Paulson, Richard
    Chung, Karine
    REPRODUCTIVE SCIENCES, 2011, 18 (03) : 258A - 258A
  • [39] Shear wave elastography detects novel imaging biomarkers of aromatase inhibitor-induced joint pain: a pilot study
    Martinez, Jessica A.
    Taljanovic, Mihra S.
    Witte, Russell S.
    Zuniga, Andres A. Nuncio
    Wertheim, Betsy C.
    Kwoh, C. Kent
    Goldstein, Brian A.
    Roe, Denise J.
    Chalasani, Pavani
    JOURNAL OF ULTRASONOGRAPHY, 2021, 21 (84) : E1 - E6
  • [40] The androgen metabolite dependent growth in hormone receptor positive breast cancer as a novel aromatase inhibitor-resistance mechanism
    Hanamura, T.
    Niwa, T.
    Nishikawa, S.
    Konno, H.
    Ghono, T.
    Kobayashi, Y.
    Kurosumi, M.
    Takei, H.
    Yamaguchi, Y.
    Ito, K-I
    Hayashi, S-, I
    CANCER RESEARCH, 2012, 72