Natural Products As Aromatase Inhibitors

Overview

Journal Anticancer Agents Med Chem

Publisher Bentham Science Publishers

Specialties Chemistry
Oncology

Date 2008 Aug 12

PMID 18690828

Citations 24

Authors

Marcy J Balunas

Bin Su

Robert W Brueggemeier

A Douglas Kinghorn

Affiliations

Soon will be listed here.

Abstract

With the clinical success of several synthetic aromatase inhibitors (AIs) in the treatment of postmenopausal estrogen receptor-positive breast cancer, researchers have also been investigating the potential of natural products as AIs. Natural products from terrestrial and marine organisms provide a chemically diverse array of compounds not always available through current synthetic chemistry techniques. Natural products that have been used traditionally for nutritional or medicinal purposes (e.g., botanical dietary supplements) may also afford AIs with reduced side effects. A thorough review of the literature regarding natural product extracts and secondary metabolites of plant, microbial, and marine origin that have been shown to exhibit aromatase inhibitory activity is presented herein.

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References

Safi R, Kovacic A, Gaillard S, Murata Y, Simpson E, McDonnell D . Coactivation of liver receptor homologue-1 by peroxisome proliferator-activated receptor gamma coactivator-1alpha on aromatase promoter II and its inhibition by activated retinoid X receptor suggest a novel target for breast-specific antiestrogen.... Cancer Res. 2005; 65(24):11762-70. DOI: 10.1158/0008-5472.CAN-05-2792. View

Satoh K, Sakamoto Y, Ogata A, Nagai F, Mikuriya H, Numazawa M . Inhibition of aromatase activity by green tea extract catechins and their endocrinological effects of oral administration in rats. Food Chem Toxicol. 2002; 40(7):925-33. DOI: 10.1016/s0278-6915(02)00066-2. View

Chin Y, Mdee L, Mbwambo Z, Mi Q, Chai H, Cragg G . Prenylated flavonoids from the root bark of Berchemia discolor, a Tanzanian medicinal plant. J Nat Prod. 2006; 69(11):1649-52. PMC: 2471879. DOI: 10.1021/np060418w. View

Piggott A, Karuso P . Quality, not quantity: the role of natural products and chemical proteomics in modern drug discovery. Comb Chem High Throughput Screen. 2004; 7(7):607-30. DOI: 10.2174/1386207043328409. View

Simpson E . Sources of estrogen and their importance. J Steroid Biochem Mol Biol. 2003; 86(3-5):225-30. DOI: 10.1016/s0960-0760(03)00360-1. View

Le Bail J, Laroche T, Habrioux G . Aromatase and 17beta-hydroxysteroid dehydrogenase inhibition by flavonoids. Cancer Lett. 1999; 133(1):101-6. DOI: 10.1016/s0304-3835(98)00211-0. View

Simpson E, Clyne C, Speed C, Rubin G, Bulun S . Tissue-specific estrogen biosynthesis and metabolism. Ann N Y Acad Sci. 2002; 949:58-67. DOI: 10.1111/j.1749-6632.2001.tb04002.x. View

Diaz-Cruz E, Brueggemeier R . Interrelationships between cyclooxygenases and aromatase: unraveling the relevance of cyclooxygenase inhibitors in breast cancer. Anticancer Agents Med Chem. 2006; 6(3):221-32. DOI: 10.2174/187152006776930873. View

Clyne C, Kovacic A, Speed C, Zhou J, Pezzi V, Simpson E . Regulation of aromatase expression by the nuclear receptor LRH-1 in adipose tissue. Mol Cell Endocrinol. 2004; 215(1-2):39-44. DOI: 10.1016/j.mce.2003.11.001. View

10.

. New developments in the realm of complementary medicine. J Support Oncol. 2005; 3(3):238-40, 245-6. View

11.

Gnoatto S, Dassonville-Klimpt A, Da Nascimento S, Galera P, Boumediene K, Gosmann G . Evaluation of ursolic acid isolated from Ilex paraguariensis and derivatives on aromatase inhibition. Eur J Med Chem. 2008; 43(9):1865-77. DOI: 10.1016/j.ejmech.2007.11.021. View

12.

Seralini G, Moslemi S . Aromatase inhibitors: past, present and future. Mol Cell Endocrinol. 2001; 178(1-2):117-31. DOI: 10.1016/s0303-7207(01)00433-6. View

13.

Monteiro R, Faria A, Azevedo I, Calhau C . Modulation of breast cancer cell survival by aromatase inhibiting hop (Humulus lupulus L.) flavonoids. J Steroid Biochem Mol Biol. 2007; 105(1-5):124-30. DOI: 10.1016/j.jsbmb.2006.11.026. View

14.

Tekmal R, Kirma N, Gill K, Fowler K . Aromatase overexpression and breast hyperplasia, an in vivo model--continued overexpression of aromatase is sufficient to maintain hyperplasia without circulating estrogens, and aromatase inhibitors abrogate these preneoplastic changes in mammary.... Endocr Relat Cancer. 2000; 6(2):307-14. DOI: 10.1677/erc.0.0060307. View

15.

Jeong H, Shin Y, Kim I, Pezzuto J . Inhibition of aromatase activity by flavonoids. Arch Pharm Res. 1999; 22(3):309-12. DOI: 10.1007/BF02976369. View

16.

Jones W, Chin Y, Kinghorn A . The role of pharmacognosy in modern medicine and pharmacy. Curr Drug Targets. 2006; 7(3):247-64. DOI: 10.2174/138945006776054915. View

17.

Jung H, Su B, Keller W, Mehta R, Kinghorn A . Antioxidant xanthones from the pericarp of Garcinia mangostana (Mangosteen). J Agric Food Chem. 2006; 54(6):2077-82. DOI: 10.1021/jf052649z. View

18.

White E, Ross L, Steele V, Kelloff G, Hill D . Screening of potential cancer preventing chemicals as aromatase inhibitors in an in vitro assay. Anticancer Res. 1999; 19(2A):1017-20. View

19.

Le Bail J, Pouget C, Fagnere C, Basly J, Chulia A, Habrioux G . Chalcones are potent inhibitors of aromatase and 17beta-hydroxysteroid dehydrogenase activities. Life Sci. 2001; 68(7):751-61. DOI: 10.1016/s0024-3205(00)00974-7. View

20.

Osawa Y, Tochigi B, Tochigi M, Ohnishi S, Watanabe Y, Bullion K . Aromatase inhibitors in cigarette smoke, tobacco leaves and other plants. J Enzyme Inhib. 1990; 4(2):187-200. DOI: 10.3109/14756369009040741. View