{"title":"通过同时调节成骨细胞和破骨细胞治疗骨质疏松症的甲莫西汀衍生物","authors":"Xiao-Jun Yan, Zhao-Jie Wang, Huan Wang, Mei-Zhen Wei, Yi-Chi Chen, Yun-Li Zhao, Xiao-Dong Luo","doi":"10.1021/acs.jnatprod.4c00437","DOIUrl":null,"url":null,"abstract":"<p><p>Seven new formononetin derivatives (<b>1</b>-<b>7</b>) were designed and prepared from formononetin (phase II phytoestrogen). The derivatives 9-butyl-3-(4-methoxyphenyl)-9,10-dihydro-4<i>H</i>,8<i>H</i>-chromeno[8,7-<i>e</i>][1,3]oxazin-4-one (<b>2</b>) and 9-(furan-3-ylmethyl)-3-(4-methoxyphenyl)-9,10-dihydro-4<i>H</i>,8<i>H</i>-chromeno[8,7-<i>e</i>][1,3]oxazin-4-one (<b>7</b>) promoted significant osteoblast formation by modulating the BMP/Smad pathway. Compound <b>7</b> exhibited potent antiosteoclastogenesis activity in RANKL-induced RAW264.7 cells and ovariectomy (OVX)-induced osteoporosis in mice by regulation of the RANK/RANKL/OPG pathway. Compound <b>7</b> regulated osteoblast and osteoclast simultaneously and showed better effect than the well-known drug ipriflavone <i>in vivo</i>, suggesting <b>7</b> as a patented antiosteoporosis candidate.</p>","PeriodicalId":47,"journal":{"name":"Journal of Natural Products ","volume":" ","pages":"2004-2013"},"PeriodicalIF":3.3000,"publicationDate":"2024-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Formononetin Derivative for Osteoporosis by Simultaneous Regulating Osteoblast and Osteoclast.\",\"authors\":\"Xiao-Jun Yan, Zhao-Jie Wang, Huan Wang, Mei-Zhen Wei, Yi-Chi Chen, Yun-Li Zhao, Xiao-Dong Luo\",\"doi\":\"10.1021/acs.jnatprod.4c00437\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Seven new formononetin derivatives (<b>1</b>-<b>7</b>) were designed and prepared from formononetin (phase II phytoestrogen). The derivatives 9-butyl-3-(4-methoxyphenyl)-9,10-dihydro-4<i>H</i>,8<i>H</i>-chromeno[8,7-<i>e</i>][1,3]oxazin-4-one (<b>2</b>) and 9-(furan-3-ylmethyl)-3-(4-methoxyphenyl)-9,10-dihydro-4<i>H</i>,8<i>H</i>-chromeno[8,7-<i>e</i>][1,3]oxazin-4-one (<b>7</b>) promoted significant osteoblast formation by modulating the BMP/Smad pathway. Compound <b>7</b> exhibited potent antiosteoclastogenesis activity in RANKL-induced RAW264.7 cells and ovariectomy (OVX)-induced osteoporosis in mice by regulation of the RANK/RANKL/OPG pathway. Compound <b>7</b> regulated osteoblast and osteoclast simultaneously and showed better effect than the well-known drug ipriflavone <i>in vivo</i>, suggesting <b>7</b> as a patented antiosteoporosis candidate.</p>\",\"PeriodicalId\":47,\"journal\":{\"name\":\"Journal of Natural Products \",\"volume\":\" \",\"pages\":\"2004-2013\"},\"PeriodicalIF\":3.3000,\"publicationDate\":\"2024-08-23\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Natural Products \",\"FirstCategoryId\":\"99\",\"ListUrlMain\":\"https://doi.org/10.1021/acs.jnatprod.4c00437\",\"RegionNum\":2,\"RegionCategory\":\"生物学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/7/21 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Natural Products ","FirstCategoryId":"99","ListUrlMain":"https://doi.org/10.1021/acs.jnatprod.4c00437","RegionNum":2,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/7/21 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Formononetin Derivative for Osteoporosis by Simultaneous Regulating Osteoblast and Osteoclast.
Seven new formononetin derivatives (1-7) were designed and prepared from formononetin (phase II phytoestrogen). The derivatives 9-butyl-3-(4-methoxyphenyl)-9,10-dihydro-4H,8H-chromeno[8,7-e][1,3]oxazin-4-one (2) and 9-(furan-3-ylmethyl)-3-(4-methoxyphenyl)-9,10-dihydro-4H,8H-chromeno[8,7-e][1,3]oxazin-4-one (7) promoted significant osteoblast formation by modulating the BMP/Smad pathway. Compound 7 exhibited potent antiosteoclastogenesis activity in RANKL-induced RAW264.7 cells and ovariectomy (OVX)-induced osteoporosis in mice by regulation of the RANK/RANKL/OPG pathway. Compound 7 regulated osteoblast and osteoclast simultaneously and showed better effect than the well-known drug ipriflavone in vivo, suggesting 7 as a patented antiosteoporosis candidate.
期刊介绍：
The Journal of Natural Products invites and publishes papers that make substantial and scholarly contributions to the area of natural products research. Contributions may relate to the chemistry and/or biochemistry of naturally occurring compounds or the biology of living systems from which they are obtained.
Specifically, there may be articles that describe secondary metabolites of microorganisms, including antibiotics and mycotoxins; physiologically active compounds from terrestrial and marine plants and animals; biochemical studies, including biosynthesis and microbiological transformations; fermentation and plant tissue culture; the isolation, structure elucidation, and chemical synthesis of novel compounds from nature; and the pharmacology of compounds of natural origin.
When new compounds are reported, manuscripts describing their biological activity are much preferred.
Specifically, there may be articles that describe secondary metabolites of microorganisms, including antibiotics and mycotoxins; physiologically active compounds from terrestrial and marine plants and animals; biochemical studies, including biosynthesis and microbiological transformations; fermentation and plant tissue culture; the isolation, structure elucidation, and chemical synthesis of novel compounds from nature; and the pharmacology of compounds of natural origin.
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