Screening for Compounds with Aromatase Inhibiting Activities from Atractylodes macrocephala Koidz 英文参考文献.docVIP

Molecules 2011, 16, 3146-3151; doi:10.3390/moleculeOPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Communication Screening for Compounds with Aromatase Inhibiting Activities from Atractylodes macrocephala Koidz Hai Jiang 1, Jing Shi 2,* and Yuanyuan Li 2 1 Department of Urology, First Affiliated Hospital, School of Medicine, Zhejiang University, No.79 Qingchun Rd., Hangzhou 310003, China; E-Mail: jhai123@ 2 Department of Pharmacy, Zhejiang Medical College, No.481 Binwen Rd., Hangzhou 310053, China * Author to whom correspondence should be addressed; E-Mail: shij136@; Tel.: +86-571 Fax: +86-571 Received: 31 March 2011; in revised form: 11 April 2011 / Accepted: 12 April 2011 / Published: 14 April 2011 Abstract: Ten compounds were isolated from the dichloromethane extract of Atractylodes macrocephala and their aromatase inhibiting activities were tested using an in vitro fluorescent-based aromatase assay. The results indicated that atractylenolide I (1), atractylenolide II (2) and atractylenolide III (3) had inhibition ratios of 94.56 ± 0.70%, 90.93 ± 1.41% and 86.31 ± 8.46%, respectively, at a concentration of 10 μM. We conclude from our results that atractylenolide and its derivates may serve as potential aromatase inhibitors (AIs) and thus merit continued study in the future. Keywords: aromatase; Atractylodes macrocephala; atractylenolide 1. Introduction Breast cancer is one of the most commonly diagnosed types of cancer in women. In the United States, breast cancer is the second leading cause of death from cancer in women. About two-thirds premenopausal and three-quarters of postmenopausal breast cancer patients have estrogen-dependent cancer, which means estrogens play a critical role in stimulating breast cancer cell proliferation [1]. Therefore, antagonizing the action of estrogen can depress the development of breast cancer.