02794nas a2200241 4500008004100000245014400041210006900185260001500254300001200269490000700281520199600288653002502284653001902309653001902328653001502347653001502362653003702377100001902414700001602433700002102449700001902470856006302489 2018 eng d00aDetection of Estrogenic, Antiestrogenic, and Drug Synergistic Activities of Seven Commercially Available Fruits by In Vitro Reporter Assays0 aDetection of Estrogenic Antiestrogenic and Drug Synergistic Acti cApril 2018 a137-1420 v103 a

Background: Fruits are known to possess antiosteoporotic and anticancer properties in part due to their estrogenic and antiestrogenic activities. Objective: In this study, estrogenic, antiestrogenic, and drug synergistic activities of seven commercially available fruits were evaluated. Materials and Methods: A steroid‑regulated transcription system in Saccharomyces cerevisiae containing a human estrogen receptor alpha expression plasmid, and a β‑galactosidase gene reporter plasmid was employed for the estrogenic, antiestrogenic, and drug agonistic studies. Results: California table grape extract showed the highest estrogenic activity. The estrogenic activities of other extracts ranked as follows: blackberry, red raspberry, strawberry > blueberry > jackfruit, black raspberry. The transcriptional activities of the combination estradiol‑fruit extracts (FEs) (400E equivalents) ranked as follows: blueberry (95.9%), blackberry (86.2%), black raspberry (88.9%), and California table grape (81.5%) > jackfruit (72.2%), and red raspberry (73.2%) > strawberry (60.7%). Black and red raspberry extracts showed the highest synergistic activities with 4‑hydroxytamoxifen (4‑OHT). Black and red raspberry extracts in combination with 4‑OHT lowered the estradiol activity by 74.9% and 73.9%, respectively. The highest synergistic activity with nafoxidine (NAF) was displayed by red raspberry extract. Together, NAF and red raspberry extract lowered estradiol activity by 77.9%. Fold changes were calculated for drug synergistic activities of FEs, and they ranged from 1.3 to 15.3 for 4‑OHT and 1.5–17.4 for NAF, respectively. Conclusions: The active compounds in the FEs studied may be useful in enhancing the antiestrogen activities of chemotherapy drugs and be used as chemopreventive agents for patients at high risk of estrogen‑induced cancers.

10a4‑hydroxytamoxifen10aAntiestrogenic10aDrug synergism10aEstrogenic10aNafoxidine10aSteroid‑regulated yeast system1 aBasu, Paramita1 aDixon, Dinu1 aVarghese, Sherin1 aMaier, Camelia uhttps://www.phcogres.com/article/2018/10/2/104103prpr11117