Yan-Qiu Meng, Chao-Hui Zhang, Dong-Ping Xu, Lei Gao, Yan Li
{"title":"New modified silybin derivatives: design, synthesis, and preliminary evaluation of antitumor activity.","authors":"Yan-Qiu Meng, Chao-Hui Zhang, Dong-Ping Xu, Lei Gao, Yan Li","doi":"10.1080/10286020.2025.2515257","DOIUrl":"https://doi.org/10.1080/10286020.2025.2515257","url":null,"abstract":"<p><p>Based on the molecular docking of Epidermal Growth Factor Receptor inhibitors and known small molecules, key amino acid fragments and active groups were analyzed through computer-aided drug design techniques. Subsequently, these active functional groups were introduced at positions C-23 and C-7 of silybin to design and synthesize 12 novel silybin derivatives. The structures of these innovative silybin analogues were confirmed by nuclear magnetic resonance and mass spectrometry. Moreover, the antitumor activities of these novel analogues were evaluated by MTT assay. As a result, compounds <b>I<sub>2</sub></b> and <b>I<sub>8</sub></b> exhibited greater cytotoxicity against tumor cells compared to silybin and positive control drugs such as gefitinib. In conclusion, our study synthesized 12 novel silybin derivatives and identified compounds <b>I<sub>2</sub></b> and <b>I<sub>8</sub></b> as potential candidates or cancer therapy.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-12"},"PeriodicalIF":1.3,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144325843","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Ying Yue, Jia-Rong Liu, Nan Wang, Xing-Rong Wang, Jun-Yi Ma, Jun-Li Yang
{"title":"Design, synthesis, and biological evaluation of bergapten derivatives as potent anti-pancreatic cancer agents.","authors":"Ying Yue, Jia-Rong Liu, Nan Wang, Xing-Rong Wang, Jun-Yi Ma, Jun-Li Yang","doi":"10.1080/10286020.2025.2514692","DOIUrl":"https://doi.org/10.1080/10286020.2025.2514692","url":null,"abstract":"<p><p>Bergapten, a natural product from <i>Zanthoxylum bungeanum</i> Maxim., exhibits anticancer, antibacterial, anti-inflammatory, and hypolipidemic effects. A derivative, FSG-Y5 showed potent activity against pancreatic cancer cells PANC-1 (IC<sub>50</sub> = 2.31 ± 0.25 µM) and CFPAC-1 (IC<sub>50</sub> = 4.41 ± 0.47 µM), inhibiting their survival, migration, and invasion while inducing apoptosis <i>via</i> Bax and Cleaved caspase-3 regulation. FSG-Y5 also suppressed pancreatic cancer organoids and zebrafish tumor growth in a concentration and time-dependent manner. These findings highlight bergapten derivatives as promising anticancer candidates, with FSG-Y5 as a potential anti-pancreatic cancer agent for further study.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-17"},"PeriodicalIF":1.3,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144325842","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Design, synthesis and anti-tumor activity of oleanolic acid derivatives targeting EGFR.","authors":"Yan-Qiu Meng, Li-Ming Liu, Dong-Ping Xu, Guo Chen, Tong-Tong Gu","doi":"10.1080/10286020.2025.2515260","DOIUrl":"https://doi.org/10.1080/10286020.2025.2515260","url":null,"abstract":"<p><p>With computer-aided drug design (CADD) technology, a total of 12 inhibitors of EGFR based on oleanolic acid (<b>OA</b>) derivatives were designed and synthesized with modification at C-3 and C-28 positions of <b>OA</b>. Their structures were confirmed by <sup>1</sup>H-NMR,<sup>13</sup>C-NMR and ESI-MS. The anti-tumor activities of these novel analogues were evaluated by MTT assay, and the results showed that the derivatives <b>I<sub>6</sub></b> and <b>II<sub>2</sub></b> had stronger cytotoxicity on A549 and MCF-7 cancer cells, which may be potential candidate compounds for tumor therapy.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-12"},"PeriodicalIF":1.3,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144325841","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Apoptotic effect of carvacrol on different cancer cells and its potential as an active medicine ingredient.","authors":"Müge Musmula, Senem Akkoc","doi":"10.1080/10286020.2025.2517669","DOIUrl":"https://doi.org/10.1080/10286020.2025.2517669","url":null,"abstract":"<p><p>Apoptosis is the programmed death of cells that have lost their function, have been damaged, or are no longer needed in the organism. Genes that control this process are overexpressed in some tumors. Carvacrol, a terpenoid, has been shown to inhibit tumor growth and induce apoptosis in cancerous cells, increasing caspase activity, DNA fragmentation, and the expression of the Bax protein, while decreasing Bcl-2 expression. In this review, the effects of carvacrol on various cancers and its potential as a drug are summarized.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-18"},"PeriodicalIF":1.3,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144325840","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Lei Gao, Liang-Feng Zhang, Yan Li, Chao-Hui Zhang, Yan-Qiu Meng
{"title":"Synthesis and antitumor activity of silibinin derivatives targeting VEGFR.","authors":"Lei Gao, Liang-Feng Zhang, Yan Li, Chao-Hui Zhang, Yan-Qiu Meng","doi":"10.1080/10286020.2025.2515250","DOIUrl":"https://doi.org/10.1080/10286020.2025.2515250","url":null,"abstract":"<p><p>Totally 10 inhibitors of VEGFR based on silibinin derivatives were designed and synthesized with the modification on the hydroxyl group at C-3 and C-7 positions of silibinin through acylation, selective aminolysis, alkylation, oxidation, and dehydrogenation reactions. Their structures were confirmed by MS, <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 A549 and SGC7901 cells, especially compounds <b>I<sub>3</sub></b> and <b>I<sub>8</sub></b> showed better inhibitory activity on these tumor cells, and similar to the positive control drug lapatinib, which may be potential candidate compounds for tumor therapy.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-11"},"PeriodicalIF":1.3,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144325844","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Ling-Feng Tian, Mei-Zhen Ye, Ting-Ting Li, Qiao Long, Shu Wang, Min Zhang, Lin Chen, Shuai Huang, Xian-Li Zhou
{"title":"C<sub>19</sub>-Diterpenoid alkaloids from two plants of <i>Aconitum sinoaxillare</i> and <i>Aconitum chasmanthum</i>.","authors":"Ling-Feng Tian, Mei-Zhen Ye, Ting-Ting Li, Qiao Long, Shu Wang, Min Zhang, Lin Chen, Shuai Huang, Xian-Li Zhou","doi":"10.1080/10286020.2025.2513492","DOIUrl":"https://doi.org/10.1080/10286020.2025.2513492","url":null,"abstract":"<p><p>Five new compounds (<b>1</b>-<b>5</b>) were isolated from the whole plants of two species of <i>Aconitum</i>, including two aconitine-type C<sub>19</sub>-diterpenoid alkaloids, sinoaxidines A (<b>1</b>) and B (<b>2</b>) and a franchetine-type C<sub>19</sub>-diterpenoid alkaloid, sinoaxidine C (<b>3</b>) from <i>Aconitum sinoaxillare</i> W. T. Wang. Two aconitine-type C<sub>19</sub>-diterpenoid alkaloids, chasmanthumines A (<b>4</b>) and B (<b>5</b>) from <i>Aconitum chasmanthum</i> Stapf, and forty known diterpenoid alkaloids were also isolated. The structures of all compounds were identified based on extensive IR, 1D, 2D NMR and HR-ESI-MS data analysis. Compound <b>6</b> exhibited potent inhibitory effects on the production of NO in RAW 264.7 cells with IC<sub>50</sub> of 29.60 <i>μ</i>M respectively.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-14"},"PeriodicalIF":1.3,"publicationDate":"2025-06-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144266324","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Jin-Qiu Ren, Xiao-Qiang Lei, Qing-Lan Guo, Jian-Gong Shi
{"title":"Minor indoloquinolizidine monoterpene alkaloids from an aqueous extract of the hook-bearing stem of <i>Uncaria rhynchophylla</i>.","authors":"Jin-Qiu Ren, Xiao-Qiang Lei, Qing-Lan Guo, Jian-Gong Shi","doi":"10.1080/10286020.2025.2509764","DOIUrl":"https://doi.org/10.1080/10286020.2025.2509764","url":null,"abstract":"<p><p>Six minor undescribed indoloquinolizidine monoterpene alkaloids, uncarrhynchophyllines F - K (<b>1 </b>-<b> 6</b>), were isolated from an aqueous decoction of the hook-bearing stems of <i>Uncaria rhynchophylla</i> (gou-teng). Their structures were determined by spectroscopic data analysis in combination with electron circular dichroism (ECD) and NMR calculations. Compounds <b>1 </b>-<b> 4</b> are rare indoloquinolizidine iminium zwitterions, while <b>5</b> exhibited protective effects against APAP induced liver cell injury.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-12"},"PeriodicalIF":1.3,"publicationDate":"2025-06-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144248011","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Chen-Lu Du, Xue-Yao Zhao, Xiao Xiao, Chuan Zhang, Yue-Wei Guo, Liang Chen, Yan-Wei Wu, Song-Wei Li
{"title":"Diterpenoids from the soft coral <i>Pachyclavularia violacea</i> and their anti-inflammatory activities.","authors":"Chen-Lu Du, Xue-Yao Zhao, Xiao Xiao, Chuan Zhang, Yue-Wei Guo, Liang Chen, Yan-Wei Wu, Song-Wei Li","doi":"10.1080/10286020.2025.2511896","DOIUrl":"https://doi.org/10.1080/10286020.2025.2511896","url":null,"abstract":"<p><p>The detailed chemical investigation of the South China Sea soft coral <i>Pachyclavularia violacea</i>, led to the isolation and characterization of a new casbane-type diterpenoid, 7,8-epoxy-casbene (<b>1</b>), along with seven known compounds (<b>2</b>-<b>8</b>). Their structures were determined by extensive spectroscopic analysis, quantum mechanical nuclear magnetic resonance (QM-NMR) method, time-dependent density functional theory electronic circular dichroism (TDDFT-ECD) calculation, and comparison with the spectral data previously reported in the literature. In <i>in vitro</i> bioassays, the anti-inflammatory activities of the isolated compounds were evaluated in the lipopolysaccharide (LPS)-induced RAW 264.7 cells, and compounds <b>6</b>-<b>8</b> displayed interesting inhibitory effects on LPS-induced tumor necrosis factor (TNF)-<i>α</i> protein release with half-maximal inhibitory concentration (IC<sub>50</sub>) values of 201.1, 231.7, and 66.21 µM, respectively.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-9"},"PeriodicalIF":1.3,"publicationDate":"2025-06-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144225537","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Chemical constituents of <i>Erythrina speciosa</i>.","authors":"Xi Yang, Yong-Chun Gao, Ya-Ping Chen, Li-Qin Wang","doi":"10.1080/10286020.2025.2513489","DOIUrl":"https://doi.org/10.1080/10286020.2025.2513489","url":null,"abstract":"<p><p>Three unreported pterocarpans, erystrictin D (<b>1</b>) and a pair of diastereoisomers, erystrictins E/F (<b>2a/2b</b>), along with fifteen known compounds (<b>3</b>-<b>17</b>) were isolated from <i>Erythrina speciosa.</i> Their structures were established by extensive spectroscopic analyses, including HRESIMS, 1D and 2D NMR, and electronic circular dichroism (ECD) spectra. All the compounds were isolated from this plant for the first time. Compounds <b>1</b>-<b>3</b>, <b>5</b> and <b>6</b> were evaluated for their inhibitory activities against a panel of cancer cell lines by MTS method. Compound <b>1</b> showed inhibitory activities against HepG2 and SW480 cells, with IC<sub>50</sub> values of 3.160 ± 0.069 and 6.575 ± 0.525 <i>μ</i>M, respectively; compound <b>5</b> against HepG2 cells, with IC<sub>50</sub> value of 22.05 ± 0.83 <i>μ</i>M.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-8"},"PeriodicalIF":1.3,"publicationDate":"2025-06-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144215911","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
He-Lin Wei, Jing-Jing Sun, Jia-Qi Chen, Tao Wang, Jun Li, Peng-Fei Tu
{"title":"Leptols A and B, one meroterpenoid and one coumarin hybrid from the leaves of Melicope pteleifolia and its anti-inflammation in BV2 cells.","authors":"He-Lin Wei, Jing-Jing Sun, Jia-Qi Chen, Tao Wang, Jun Li, Peng-Fei Tu","doi":"10.1080/10286020.2025.2509767","DOIUrl":"https://doi.org/10.1080/10286020.2025.2509767","url":null,"abstract":"<p><p>One meroterpenoid and one coumarin hybrid, namely leptols A (<b>1</b>) and B (<b>2</b>), respectively, and seven known chromone analogues have been isolated from the leaves of <i>Melicope pteleifolia</i>. The structures were elucidated on the basis of spectroscopic methods (UV, IR, HRMS, and NMR), and the absolute configuration was determined by comparing its experimental and calculated OR values. These isolates were evaluated for anti-inflammatory activities on the lipopolysaccharide (LPS) induced nitric oxide (NO) production in BV2 microglial cells, and compound <b>1</b> exhibited potential nitric oxide inhibitory activities with IC<sub>50</sub> value of 12.0 µM.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-8"},"PeriodicalIF":1.3,"publicationDate":"2025-06-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144215912","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}