Aromatase inhibition by synthetic lactones and flavonoids in human placental microsomes and breast fibroblasts — A comparative study
Interference of exogenous chemicals with the aromatase enzyme can be useful as a tool to identify chemicals that could act either chemopreventive for hormone-dependent cancer or adverse endocrine disruptive. Aromatase is the key enzyme in the biosynthesis of steroids, as it converts androgens to est...
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| Veröffentlicht in: | Toxicology and applied pharmacology 2008-05, Vol.228 (3), p.269-276 |
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| creator | van Meeuwen, J.A. Nijmeijer, S. Mutarapat, T. Ruchirawat, S. de Jong, P.C. Piersma, A.H. van den Berg, M. |
| description | Interference of exogenous chemicals with the aromatase enzyme can be useful as a tool to identify chemicals that could act either chemopreventive for hormone-dependent cancer or adverse endocrine disruptive. Aromatase is the key enzyme in the biosynthesis of steroids, as it converts androgens to estrogens. Certain flavonoids, plant derived chemicals, are known catalytic aromatase inhibitors. Various systems are in use to test aromatase inhibitory properties of compounds. Commonly used are microsomes derived from ovary or placental tissue characterized by high aromatase activity. To a lesser extent whole cell systems are used and specifically cell systems that are potential target tissue in breast cancer development. In this study aromatase inhibitory properties of fadrozole, 8-prenylnaringenin and a synthetic lactone (TM-7) were determined in human placental microsomes and in human primary breast fibroblasts. In addition, apigenin, chrysin, naringenin and two synthetic lactones (TM-8 and TM-9) were tested in human microsomes only. Comparison of the aromatase inhibitory potencies of these compounds between the two test systems showed that the measurement of aromatase inhibition in human placental microsomes is a good predictor of aromatase inhibition in human breast fibroblasts. |
| doi_str_mv | 10.1016/j.taap.2007.12.007 |
| format | Article |
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Aromatase is the key enzyme in the biosynthesis of steroids, as it converts androgens to estrogens. Certain flavonoids, plant derived chemicals, are known catalytic aromatase inhibitors. Various systems are in use to test aromatase inhibitory properties of compounds. Commonly used are microsomes derived from ovary or placental tissue characterized by high aromatase activity. To a lesser extent whole cell systems are used and specifically cell systems that are potential target tissue in breast cancer development. In this study aromatase inhibitory properties of fadrozole, 8-prenylnaringenin and a synthetic lactone (TM-7) were determined in human placental microsomes and in human primary breast fibroblasts. In addition, apigenin, chrysin, naringenin and two synthetic lactones (TM-8 and TM-9) were tested in human microsomes only. Comparison of the aromatase inhibitory potencies of these compounds between the two test systems showed that the measurement of aromatase inhibition in human placental microsomes is a good predictor of aromatase inhibition in human breast fibroblasts.</description><subject>60 APPLIED LIFE SCIENCES</subject><subject>ANDROGENS</subject><subject>Aromatase</subject><subject>Aromatase Inhibitors - pharmacology</subject><subject>Biological and medical sciences</subject><subject>BIOSYNTHESIS</subject><subject>Breast - enzymology</subject><subject>Catalysis</subject><subject>Cells, Cultured</subject><subject>ENZYMES</subject><subject>ESTROGENS</subject><subject>Female</subject><subject>FIBROBLASTS</subject><subject>Fibroblasts - enzymology</subject><subject>FLAVONOIDS</subject><subject>Flavonoids - pharmacology</subject><subject>Human breast fibroblasts</subject><subject>Human placental microsomes</subject><subject>Humans</subject><subject>INHIBITION</subject><subject>LACTONES</subject><subject>Lactones - pharmacology</subject><subject>MAMMARY GLANDS</subject><subject>Medical sciences</subject><subject>MICROSOMES</subject><subject>Microsomes - enzymology</subject><subject>NEOPLASMS</subject><subject>OVARIES</subject><subject>Placenta - enzymology</subject><subject>Plant poisons toxicology</subject><subject>Structure-Activity Relationship</subject><subject>Synthetic lactones</subject><subject>Toxicology</subject><issn>0041-008X</issn><issn>1096-0333</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2008</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqF0c2KFDEQB_BGFHd29QU8SED01m0l_TEd8DIsugoLXhS8hcpHMxm6kzFJD8zN0z6BT-iTmGYavSk5VA6_FKn6F8ULChUF2r09VAnxWDGAbUVZlcujYkOBdyXUdf242AA0tATov10V1zEeAIA3DX1aXNGeAd02sCkedsFPmDAaYt3eSpusd0SeSTy7tDfJKjKiSt6ZSNBpMox48s5bHbMn-3lCR45ZGJdwJJNVwUc_rVgGgzGRwcrg5Zivkfz68ZPsiPLTEQMmezIkplmfnxVPBhyjeb7Wm-Lrh_dfbj-W95_vPt3u7kvVNHUqe911W9a2ugPNtkyylmMPukauGug7raA2Tc15L2EAzIdLRofatLJTbSdlfVO8uvT1MVkRlU1G7ZV3zqgkGKW5C6NZvbmoY_DfZxOTmGxUZhzRGT9H0XHKOG_-Dxlsad8wniG7wGU_MZhBHIOdMJwFBbGEKQ5iCVMsYQrKRC750cu1-ywno_8-WdPL4PUKMCoch4BO2fjHMaiB035x7y7O5NWerAnL5MYpo21YBtfe_usfvwGl4L94</recordid><startdate>20080501</startdate><enddate>20080501</enddate><creator>van Meeuwen, J.A.</creator><creator>Nijmeijer, S.</creator><creator>Mutarapat, T.</creator><creator>Ruchirawat, S.</creator><creator>de Jong, P.C.</creator><creator>Piersma, A.H.</creator><creator>van den Berg, M.</creator><general>Elsevier Inc</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7U7</scope><scope>C1K</scope><scope>7X8</scope><scope>OTOTI</scope></search><sort><creationdate>20080501</creationdate><title>Aromatase inhibition by synthetic lactones and flavonoids in human placental microsomes and breast fibroblasts — A comparative study</title><author>van Meeuwen, J.A. ; 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Aromatase is the key enzyme in the biosynthesis of steroids, as it converts androgens to estrogens. Certain flavonoids, plant derived chemicals, are known catalytic aromatase inhibitors. Various systems are in use to test aromatase inhibitory properties of compounds. Commonly used are microsomes derived from ovary or placental tissue characterized by high aromatase activity. To a lesser extent whole cell systems are used and specifically cell systems that are potential target tissue in breast cancer development. In this study aromatase inhibitory properties of fadrozole, 8-prenylnaringenin and a synthetic lactone (TM-7) were determined in human placental microsomes and in human primary breast fibroblasts. In addition, apigenin, chrysin, naringenin and two synthetic lactones (TM-8 and TM-9) were tested in human microsomes only. Comparison of the aromatase inhibitory potencies of these compounds between the two test systems showed that the measurement of aromatase inhibition in human placental microsomes is a good predictor of aromatase inhibition in human breast fibroblasts.</abstract><cop>San Diego, CA</cop><pub>Elsevier Inc</pub><pmid>18201740</pmid><doi>10.1016/j.taap.2007.12.007</doi><tpages>8</tpages></addata></record> |
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| ispartof | Toxicology and applied pharmacology, 2008-05, Vol.228 (3), p.269-276 |
| issn | 0041-008X 1096-0333 |
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| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | 60 APPLIED LIFE SCIENCES ANDROGENS Aromatase Aromatase Inhibitors - pharmacology Biological and medical sciences BIOSYNTHESIS Breast - enzymology Catalysis Cells, Cultured ENZYMES ESTROGENS Female FIBROBLASTS Fibroblasts - enzymology FLAVONOIDS Flavonoids - pharmacology Human breast fibroblasts Human placental microsomes Humans INHIBITION LACTONES Lactones - pharmacology MAMMARY GLANDS Medical sciences MICROSOMES Microsomes - enzymology NEOPLASMS OVARIES Placenta - enzymology Plant poisons toxicology Structure-Activity Relationship Synthetic lactones Toxicology |
| title | Aromatase inhibition by synthetic lactones and flavonoids in human placental microsomes and breast fibroblasts — A comparative study |
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