Dong Huang, Yi-Ling Liao, Jia-Qian Chen, Fang-Yu Yuan, Shu-Qi Wu, Jia-Luo Huang, Tao Yuan, Xin Chen, Zhang-Hua Sun, Gui-Hua Tang, Lu Gan* and Sheng Yin*,
{"title":"具有抗肝纤维化活性的紫花葡萄烷二萜正酯A-I。","authors":"Dong Huang, Yi-Ling Liao, Jia-Qian Chen, Fang-Yu Yuan, Shu-Qi Wu, Jia-Luo Huang, Tao Yuan, Xin Chen, Zhang-Hua Sun, Gui-Hua Tang, Lu Gan* and Sheng Yin*, ","doi":"10.1021/acs.jnatprod.5c00536","DOIUrl":null,"url":null,"abstract":"<p >Bioassay─combined with molecular networking─guided chemical investigation of <i>Wikstroemia chamaedaphne</i> (Thymelaeaceae) led to the isolation of 15 daphnane diterpenoid orthoesters (DDOs), of which <b>1</b>–<b>9</b> were new. Compounds <b>1</b>–<b>5</b> and <b>8</b>–<b>9</b> are a rare group of 1-alkyl macrocyclic DDOs. These structures were determined by extensive spectroscopic and computational methods as well as single-crystal X-ray diffraction. All of DDOs were evaluated for anti-liver fibrosis activity in TGF-<i>β</i>1-stimulated LX-2 cells by high-throughput screening assays, and the results showed that six of isolates significantly inhibited the expression of fibronectin (FN) at 10 <i>μ</i>M, among which <b>1</b> and <b>11</b> exhibited the most potent activity that could dose-dependently inhibit protein levels of FN, <i>α</i>-smooth muscle actin (<i>α</i>-SMA), and collagen I in LX-2 and JS-1 cells. Our study indicated that macrocyclic DDOs could serve as a new type of structural motif in anti-liver fibrosis drug development.</p>","PeriodicalId":47,"journal":{"name":"Journal of Natural Products ","volume":"88 7","pages":"1781–1790"},"PeriodicalIF":3.6000,"publicationDate":"2025-07-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Wikstdaphnoids A–I, Daphnane Diterpenoid Orthoesters from Wikstroemia chamaedaphne with Anti-Liver Fibrosis Activity\",\"authors\":\"Dong Huang, Yi-Ling Liao, Jia-Qian Chen, Fang-Yu Yuan, Shu-Qi Wu, Jia-Luo Huang, Tao Yuan, Xin Chen, Zhang-Hua Sun, Gui-Hua Tang, Lu Gan* and Sheng Yin*, \",\"doi\":\"10.1021/acs.jnatprod.5c00536\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p >Bioassay─combined with molecular networking─guided chemical investigation of <i>Wikstroemia chamaedaphne</i> (Thymelaeaceae) led to the isolation of 15 daphnane diterpenoid orthoesters (DDOs), of which <b>1</b>–<b>9</b> were new. Compounds <b>1</b>–<b>5</b> and <b>8</b>–<b>9</b> are a rare group of 1-alkyl macrocyclic DDOs. These structures were determined by extensive spectroscopic and computational methods as well as single-crystal X-ray diffraction. All of DDOs were evaluated for anti-liver fibrosis activity in TGF-<i>β</i>1-stimulated LX-2 cells by high-throughput screening assays, and the results showed that six of isolates significantly inhibited the expression of fibronectin (FN) at 10 <i>μ</i>M, among which <b>1</b> and <b>11</b> exhibited the most potent activity that could dose-dependently inhibit protein levels of FN, <i>α</i>-smooth muscle actin (<i>α</i>-SMA), and collagen I in LX-2 and JS-1 cells. Our study indicated that macrocyclic DDOs could serve as a new type of structural motif in anti-liver fibrosis drug development.</p>\",\"PeriodicalId\":47,\"journal\":{\"name\":\"Journal of Natural Products \",\"volume\":\"88 7\",\"pages\":\"1781–1790\"},\"PeriodicalIF\":3.6000,\"publicationDate\":\"2025-07-15\",\"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://pubs.acs.org/doi/10.1021/acs.jnatprod.5c00536\",\"RegionNum\":2,\"RegionCategory\":\"生物学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Natural Products ","FirstCategoryId":"99","ListUrlMain":"https://pubs.acs.org/doi/10.1021/acs.jnatprod.5c00536","RegionNum":2,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Wikstdaphnoids A–I, Daphnane Diterpenoid Orthoesters from Wikstroemia chamaedaphne with Anti-Liver Fibrosis Activity
Bioassay─combined with molecular networking─guided chemical investigation of Wikstroemia chamaedaphne (Thymelaeaceae) led to the isolation of 15 daphnane diterpenoid orthoesters (DDOs), of which 1–9 were new. Compounds 1–5 and 8–9 are a rare group of 1-alkyl macrocyclic DDOs. These structures were determined by extensive spectroscopic and computational methods as well as single-crystal X-ray diffraction. All of DDOs were evaluated for anti-liver fibrosis activity in TGF-β1-stimulated LX-2 cells by high-throughput screening assays, and the results showed that six of isolates significantly inhibited the expression of fibronectin (FN) at 10 μM, among which 1 and 11 exhibited the most potent activity that could dose-dependently inhibit protein levels of FN, α-smooth muscle actin (α-SMA), and collagen I in LX-2 and JS-1 cells. Our study indicated that macrocyclic DDOs could serve as a new type of structural motif in anti-liver fibrosis drug development.
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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