{"title":"新型雄烯二酮衍生物14α-羟基-4-雄烯-3,6,17-三酮(14α-OHAT)对人子宫肿瘤芳香酶活性的抑制作用","authors":"Takara Yamamoto , Masaaki Fukuoka , Yasuko Fujimoto , Jo Kitawaki , Masamichi Nakakoshi , Makoto Yoshihama , Hiroji Okada","doi":"10.1016/0022-4731(90)90167-Q","DOIUrl":null,"url":null,"abstract":"<div><p>The development of human uterine estrogen-dependent tumors is considered to be closely related to estrogen biosynthesis. This study examined whether or not 14α-hydroxy-4-androstene-3,6,17-trione (14α-OHAT), a new 4-androstene-3,17-dione derivative synthesized microbiologically, inhibits estrogen biosynthetase (aromatase) activities of human uterine tumors (i.e. uterine endometrial cancer, uterine leiomyoma and uterine adenomyosis tissues).</p><p>14α-OHAT inhibited aromatase activity in all uterine tumors, dose-dependently (0.1–10 μM).</p><p>Moreover, 14α-OHAT did not show the binding affinity to rabbit uterine cytosol-sex steroids, and it was not converted to estrogen in human placental preparations. p]Thus, 14α-OHAT, an aromatase inhibitor, may be useful clinically as an endocrine chemotherapy for peri- or post-menopausal women with uterine estrogen-dependent tumors.</p></div>","PeriodicalId":17138,"journal":{"name":"Journal of steroid biochemistry","volume":"36 6","pages":"Pages 517-521"},"PeriodicalIF":0.0000,"publicationDate":"1990-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0022-4731(90)90167-Q","citationCount":"20","resultStr":"{\"title\":\"Inhibitory effect of a new androstenedione derivative, 14α-hydroxy-4-androstene-3,6,17-trione (14α-OHAT) on aromatase activity of human uterine tumors\",\"authors\":\"Takara Yamamoto , Masaaki Fukuoka , Yasuko Fujimoto , Jo Kitawaki , Masamichi Nakakoshi , Makoto Yoshihama , Hiroji Okada\",\"doi\":\"10.1016/0022-4731(90)90167-Q\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>The development of human uterine estrogen-dependent tumors is considered to be closely related to estrogen biosynthesis. This study examined whether or not 14α-hydroxy-4-androstene-3,6,17-trione (14α-OHAT), a new 4-androstene-3,17-dione derivative synthesized microbiologically, inhibits estrogen biosynthetase (aromatase) activities of human uterine tumors (i.e. uterine endometrial cancer, uterine leiomyoma and uterine adenomyosis tissues).</p><p>14α-OHAT inhibited aromatase activity in all uterine tumors, dose-dependently (0.1–10 μM).</p><p>Moreover, 14α-OHAT did not show the binding affinity to rabbit uterine cytosol-sex steroids, and it was not converted to estrogen in human placental preparations. p]Thus, 14α-OHAT, an aromatase inhibitor, may be useful clinically as an endocrine chemotherapy for peri- or post-menopausal women with uterine estrogen-dependent tumors.</p></div>\",\"PeriodicalId\":17138,\"journal\":{\"name\":\"Journal of steroid biochemistry\",\"volume\":\"36 6\",\"pages\":\"Pages 517-521\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1990-08-28\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/0022-4731(90)90167-Q\",\"citationCount\":\"20\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of steroid biochemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/002247319090167Q\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of steroid biochemistry","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/002247319090167Q","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Inhibitory effect of a new androstenedione derivative, 14α-hydroxy-4-androstene-3,6,17-trione (14α-OHAT) on aromatase activity of human uterine tumors
The development of human uterine estrogen-dependent tumors is considered to be closely related to estrogen biosynthesis. This study examined whether or not 14α-hydroxy-4-androstene-3,6,17-trione (14α-OHAT), a new 4-androstene-3,17-dione derivative synthesized microbiologically, inhibits estrogen biosynthetase (aromatase) activities of human uterine tumors (i.e. uterine endometrial cancer, uterine leiomyoma and uterine adenomyosis tissues).
14α-OHAT inhibited aromatase activity in all uterine tumors, dose-dependently (0.1–10 μM).
Moreover, 14α-OHAT did not show the binding affinity to rabbit uterine cytosol-sex steroids, and it was not converted to estrogen in human placental preparations. p]Thus, 14α-OHAT, an aromatase inhibitor, may be useful clinically as an endocrine chemotherapy for peri- or post-menopausal women with uterine estrogen-dependent tumors.
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