{"title":"基于多靶点的五环三萜熊果酸衍生物和齐墩果酸衍生物的设计、合成及其抗肿瘤活性。","authors":"Jun-Jiao Ma, Liang-Feng Zhang, Dong-Ping Xu, Zan Wang, Yan-Qiu Meng","doi":"10.1080/10286020.2025.2473635","DOIUrl":null,"url":null,"abstract":"<p><p>Totally twelve inhibitors of Survivin and Sp1 based on ursolic acid (<b>UA</b>) derivatives and oleanolic acid (<b>OA</b>) derivatives were designed and synthesized with modification at C-2, C-3 and C-28 of <b>UA</b> and <b>OA</b>. Their structures were confirmed by HRMS,<sup>1</sup>H NMR and <sup>13</sup>C NMR. <i>In vitro</i> activity assay showed that these compounds can inhibit cell proliferation of HeLa, SKOV3, BGC-823 and HT1080 cells, especially compounds <b>IV</b> and <b>X</b> showed better inhibitory activity on these tumor cells than that of the positive control drug Gefitinib and similar to Vp-16. Mechanistically, selected compound may inhibit the proliferation of <b>SKOV3</b> cells and trigger apoptosis by activating Sp1 to inhibit Survivin protein expression, which may be promising leading compounds for cancer therapy.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-18"},"PeriodicalIF":1.3000,"publicationDate":"2025-03-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design, synthesis and antitumor activity of pentacyclic triterpenoid ursolic acid derivatives and oleanolic acid derivatives based on multi-target.\",\"authors\":\"Jun-Jiao Ma, Liang-Feng Zhang, Dong-Ping Xu, Zan Wang, Yan-Qiu Meng\",\"doi\":\"10.1080/10286020.2025.2473635\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Totally twelve inhibitors of Survivin and Sp1 based on ursolic acid (<b>UA</b>) derivatives and oleanolic acid (<b>OA</b>) derivatives were designed and synthesized with modification at C-2, C-3 and C-28 of <b>UA</b> and <b>OA</b>. Their structures were confirmed by HRMS,<sup>1</sup>H NMR and <sup>13</sup>C NMR. <i>In vitro</i> activity assay showed that these compounds can inhibit cell proliferation of HeLa, SKOV3, BGC-823 and HT1080 cells, especially compounds <b>IV</b> and <b>X</b> showed better inhibitory activity on these tumor cells than that of the positive control drug Gefitinib and similar to Vp-16. Mechanistically, selected compound may inhibit the proliferation of <b>SKOV3</b> cells and trigger apoptosis by activating Sp1 to inhibit Survivin protein expression, which may be promising leading compounds for cancer therapy.</p>\",\"PeriodicalId\":15180,\"journal\":{\"name\":\"Journal of Asian Natural Products Research\",\"volume\":\" \",\"pages\":\"1-18\"},\"PeriodicalIF\":1.3000,\"publicationDate\":\"2025-03-21\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Asian Natural Products Research\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/10286020.2025.2473635\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, APPLIED\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Asian Natural Products Research","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/10286020.2025.2473635","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, APPLIED","Score":null,"Total":0}
Design, synthesis and antitumor activity of pentacyclic triterpenoid ursolic acid derivatives and oleanolic acid derivatives based on multi-target.
Totally twelve inhibitors of Survivin and Sp1 based on ursolic acid (UA) derivatives and oleanolic acid (OA) derivatives were designed and synthesized with modification at C-2, C-3 and C-28 of UA and OA. Their structures were confirmed by HRMS,1H NMR and 13C NMR. In vitro activity assay showed that these compounds can inhibit cell proliferation of HeLa, SKOV3, BGC-823 and HT1080 cells, especially compounds IV and X showed better inhibitory activity on these tumor cells than that of the positive control drug Gefitinib and similar to Vp-16. Mechanistically, selected compound may inhibit the proliferation of SKOV3 cells and trigger apoptosis by activating Sp1 to inhibit Survivin protein expression, which may be promising leading compounds for cancer therapy.
期刊介绍：
The Journal of Asian Natural Products Research (JANPR) publishes chemical and pharmaceutical studies in the English language in the field of natural product research on Asian ethnic medicine. The journal publishes work from scientists in Asian countries, e.g. China, Japan, Korea and India, including contributions from other countries concerning natural products of Asia. The journal is chemistry-orientated. Major fields covered are: isolation and structural elucidation of natural constituents (including those for non-medical uses), synthesis and transformation (including biosynthesis and biotransformation) of natural products, pharmacognosy, and allied topics. Biological evaluation of crude extracts are acceptable only as supporting data for pure isolates with well-characterized structures.
All published research articles in this journal have undergone rigorous peer review, based on initial editor screening and anonymized refereeing by at least two expert referees.
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