Pub Date : 2025-12-02DOI: 10.1080/10286020.2024.2325033
Jia-Yi Li , Xin-Yi Wang , Mei-Juan Han , Ming Bai , Xiao-Xiao Huang
Guiding by LC-MS/MS analysis and the Global Natural Products Social (GNPS) Molecular Networking, three undescribed sesquiterpenoids, stedapgens A–C, and two known analogues were discovered in the barks of Daphne genkwa Sieb. et Zucc. The structures were determined by analysis of their spectroscopic data and quantum-chemical calculations. All the isolated novel compounds were tested for their acetylcholinesterase inhibitory activities with IC50 = 0.754 ± 0.059, 0.696 ± 0.026, and 0.337 ± 0.023 μg/ml. Among them, stedapgen A displayed promising inhibitory activities against AChE, and the binding sites were predicted by molecular docking.
{"title":"Target isolation of diverse sesquiterpenoid from the stems of Daphne genkwa based on molecular networking","authors":"Jia-Yi Li , Xin-Yi Wang , Mei-Juan Han , Ming Bai , Xiao-Xiao Huang","doi":"10.1080/10286020.2024.2325033","DOIUrl":"10.1080/10286020.2024.2325033","url":null,"abstract":"<div><div>Guiding by LC-MS/MS analysis and the Global Natural Products Social (GNPS) Molecular Networking, three undescribed sesquiterpenoids, stedapgens A–C, and two known analogues were discovered in the barks of <em>Daphne genkwa</em> Sieb. et Zucc. The structures were determined by analysis of their spectroscopic data and quantum-chemical calculations. All the isolated novel compounds were tested for their acetylcholinesterase inhibitory activities with IC<sub>50</sub> = 0.754 ± 0.059, 0.696 ± 0.026, and 0.337 ± 0.023 <em>μ</em>g/ml. Among them, stedapgen A displayed promising inhibitory activities against AChE, and the binding sites were predicted by molecular docking.</div></div>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":"27 12","pages":"Pages 1807-1818"},"PeriodicalIF":1.3,"publicationDate":"2025-12-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140287496","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}
Pub Date : 2025-12-02DOI: 10.1080/10286020.2024.2360640
Yue-Lin Zhao , Yue Jin , Zi-Ying Han , Wen-Han Song , Hui-Lin Zhu , Jian Zhang , Qian Wang , Miao Wang , Xiao-Wen Jiang , Hui-Yuan Gao
In this study, a previously undescribed cassane diterpenoid, named caesalpinin JF (1), along with two known cassane diterpenoids caesanine C (2) and tomocinol B (3), was isolated from 95% EtOH extract of the seeds of Caesalpinia sappan Linn. Additionally, three known compounds including pulcherrin R (4), syringaresinol-4'-O-β-D-glucopyranoside (5) and kaempferol (6) were also identified. The structures of the isolated compounds were elucidated by comprehensive 1D and 2D NMR spectroscopic analyses. Additionally, electronic circular dichroism (ECD) calculation was used to identify the absolute structure of compound 1. Among the isolated compounds, compound 1 displayed a potent anti-neuroinflammation with an IC50 value of 9.87 ± 1.71 μM.
在这项研究中，从红豆杉种子 95% 的 EtOH 提取物中分离出了一种之前未曾描述过的决明子二萜，命名为 Caesalpinin JF (1)，以及两种已知的决明子二萜 caesanine C (2) 和 tomocinol B (3)。此外，还鉴定出三种已知化合物，包括 Pulcherrin R (4)、Syringaresinol-4'-O-β-D-吡喃葡萄糖苷 (5) 和山奈酚 (6)。通过全面的一维和二维核磁共振光谱分析，阐明了这些分离化合物的结构。在分离出的化合物中，化合物 1 具有很强的抗神经发炎作用，其 IC50 值为 9.87 ± 1.71 μM。
{"title":"A new cassane diterpenoid from the seed of Caesalpinia sappan","authors":"Yue-Lin Zhao , Yue Jin , Zi-Ying Han , Wen-Han Song , Hui-Lin Zhu , Jian Zhang , Qian Wang , Miao Wang , Xiao-Wen Jiang , Hui-Yuan Gao","doi":"10.1080/10286020.2024.2360640","DOIUrl":"10.1080/10286020.2024.2360640","url":null,"abstract":"<div><div>In this study, a previously undescribed cassane diterpenoid, named caesalpinin JF (<strong>1</strong>), along with two known cassane diterpenoids caesanine C (<strong>2</strong>) and tomocinol B (<strong>3</strong>), was isolated from 95% EtOH extract of the seeds of <em>Caesalpinia sappan</em> Linn. Additionally, three known compounds including pulcherrin R (<strong>4</strong>), syringaresinol-4'-<em>O</em>-<em>β</em>-D-glucopyranoside (<strong>5</strong>) and kaempferol (<strong>6</strong>) were also identified. The structures of the isolated compounds were elucidated by comprehensive 1D and 2D NMR spectroscopic analyses. Additionally, electronic circular dichroism (ECD) calculation was used to identify the absolute structure of compound <strong>1</strong>. Among the isolated compounds, compound <strong>1</strong> displayed a potent anti-neuroinflammation with an IC<sub>50</sub> value of 9.87 ± 1.71 <em>μ</em>M.</div></div>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":"27 12","pages":"Pages 1792-1798"},"PeriodicalIF":1.3,"publicationDate":"2025-12-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141468142","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}
Pub Date : 2025-12-02DOI: 10.1080/10286020.2024.2327524
Xiang Gao , Hao-Nan Li , Peng-Ju Liu , Xiao-Kang Long , Xue-Hai Guo , Hui-Ming Hua , Da-Hong Li
In recent years, with sinomenine hydrochloride as the main ingredient, Qingfengteng had been formulated as various dosage forms for clinical treatment. Subsequent findings confirmed a variety of biological roles for sinomenine. Here, 15 H2S-donating sinomenine derivatives were synthesized. Target hybrids a11 displayed substantial cytotoxic effects on cancer cell lines, particularly against K562 cells, with an IC50 value of 1.36 μM. In-depth studies demonstrated that a11 arrested cell cycle at G1 phase, induced apoptosis via both morphological changes in nucleus and membrane potential collapse in mitochondria. These results indicated a11 exerted an antiproliferative effect through apoptosis induction via mitochondrial pathway.
{"title":"Synthesis of sinomenine derivatives with potential anti-leukemia activity","authors":"Xiang Gao , Hao-Nan Li , Peng-Ju Liu , Xiao-Kang Long , Xue-Hai Guo , Hui-Ming Hua , Da-Hong Li","doi":"10.1080/10286020.2024.2327524","DOIUrl":"10.1080/10286020.2024.2327524","url":null,"abstract":"<div><div>In recent years, with sinomenine hydrochloride as the main ingredient, Qingfengteng had been formulated as various dosage forms for clinical treatment. Subsequent findings confirmed a variety of biological roles for sinomenine. Here, 15 H<sub>2</sub>S-donating sinomenine derivatives were synthesized. Target hybrids <strong>a11</strong> displayed substantial cytotoxic effects on cancer cell lines, particularly against K562 cells, with an IC<sub>50</sub> value of 1.36 μM. In-depth studies demonstrated that <strong>a11</strong> arrested cell cycle at G1 phase, induced apoptosis <em>via</em> both morphological changes in nucleus and membrane potential collapse in mitochondria. These results indicated <strong>a11</strong> exerted an antiproliferative effect through apoptosis induction <em>via</em> mitochondrial pathway.</div></div>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":"27 12","pages":"Pages 1819-1835"},"PeriodicalIF":1.3,"publicationDate":"2025-12-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140593511","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}
Pub Date : 2025-12-02DOI: 10.1080/10286020.2024.2317841
Lian Lian , Yue-Lin Zhao , Tian-Jian Zhang , Miao Wang , Hui-Yuan Gao
Two new cassane diterpenoids, sucupiranin MN (1) and sucupiranin ML (2), together with two known compounds sucutinirane C (3) and deacetylsucutinirane C (4) were isolated from the seed kernels of Caesalpinia sinensis. Their structures were elucidated by means of analysis of comprehensive spectroscopic data, especially HRESIMS and 1D/2D NMR spectroscopy. Compounds 1–4 are typical furan-type cassane derivatives with an aromatized C ring. Biological evaluation revealed that compounds 1–4 at the concentration of 10 μM could inhibit the overproduction of NO in LPS-stimulated RAW 264.7 macrophages.
从中华皂荚的种仁中分离出了两种新的皂荚烷二萜类化合物：琥珀烷宁 MN (1) 和琥珀烷宁 ML (2)，以及两种已知化合物琥珀烷宁 C (3) 和脱乙酰基琥珀烷宁 C (4)。通过分析全面的光谱数据，特别是 HRESIMS 和 1D/2D NMR 光谱，阐明了它们的结构。化合物 1-4 是具有芳香化 C 环的典型呋喃型卡桑烷衍生物。生物学评价显示，浓度为 10 μM 的化合物 1-4 可抑制 LPS 刺激的 RAW 264.7 巨噬细胞中 NO 的过度产生。
{"title":"Two new cassane diterpenoids from the seed kernels of Caesalpinia sinensis","authors":"Lian Lian , Yue-Lin Zhao , Tian-Jian Zhang , Miao Wang , Hui-Yuan Gao","doi":"10.1080/10286020.2024.2317841","DOIUrl":"10.1080/10286020.2024.2317841","url":null,"abstract":"<div><div>Two new cassane diterpenoids, sucupiranin MN (<strong>1</strong>) and sucupiranin ML (<strong>2</strong>), together with two known compounds sucutinirane C (<strong>3</strong>) and deacetylsucutinirane C (<strong>4</strong>) were isolated from the seed kernels of <em>Caesalpinia sinensis</em>. Their structures were elucidated by means of analysis of comprehensive spectroscopic data, especially HRESIMS and 1D/2D NMR spectroscopy. Compounds <strong>1–4</strong> are typical furan-type cassane derivatives with an aromatized C ring. Biological evaluation revealed that compounds <strong>1–4</strong> at the concentration of 10 μM could inhibit the overproduction of NO in LPS-stimulated RAW 264.7 macrophages.</div></div>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":"27 12","pages":"Pages 1786-1791"},"PeriodicalIF":1.3,"publicationDate":"2025-12-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139996275","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}
Pub Date : 2025-12-01Epub Date: 2025-11-17DOI: 10.1080/10286020.2025.2588076
Shao-Jiang Song
{"title":"Special issue commemorating the 40th anniversary of the College of Traditional Chinese Medicine, Shenyang Pharmaceutical University.","authors":"Shao-Jiang Song","doi":"10.1080/10286020.2025.2588076","DOIUrl":"10.1080/10286020.2025.2588076","url":null,"abstract":"","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1737-1738"},"PeriodicalIF":1.3,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145534295","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}
Pub Date : 2025-11-26DOI: 10.1080/10286020.2025.2587634
De-Wu Zhang, Xi-Dian Yue, Yue Wang, Jia-Huan Liu, Sheng-Jun Dai
Three new neo-clerodane diterpenoids, named scuregeliolides A-C (1-3), were isolated from the whole plant of Scutellaria regeliana. Their chemical structures, including absolute stereochemical configurations, were fully elucidated by means of integrated spectroscopic techniques and Electronic Circular Dichroism (ECD) calculations. In vitro, three undescribed neo-clerodane diterpenoids showed significant anti-inflammatory activities due to inhibiting the release of TNF-α, IL-6 and IL-1β in the LPS-induced RAW264.7 cells, as well as preventing the release of β-glucuronidase from the PAF-stimulated PMNs.
{"title":"Scuregeliolides a-C: new <i>neo</i>-clerodane diterpenoids from <i>Scutellaria regeliana</i> and their anti-inflammatory activities.","authors":"De-Wu Zhang, Xi-Dian Yue, Yue Wang, Jia-Huan Liu, Sheng-Jun Dai","doi":"10.1080/10286020.2025.2587634","DOIUrl":"https://doi.org/10.1080/10286020.2025.2587634","url":null,"abstract":"<p><p>Three new <i>neo</i>-clerodane diterpenoids, named scuregeliolides A<b>-</b>C (<b>1</b>-<b>3</b>), were isolated from the whole plant of <i>Scutellaria regeliana</i>. Their chemical structures, including absolute stereochemical configurations, were fully elucidated by means of integrated spectroscopic techniques and Electronic Circular Dichroism (ECD) calculations. <i>In vitro</i>, three undescribed <i>neo</i>-clerodane diterpenoids showed significant anti-inflammatory activities due to inhibiting the release of TNF-<i>α</i>, IL-6 and IL-1<i>β</i> in the LPS-induced RAW264.7 cells, as well as preventing the release of <i>β</i>-glucuronidase from the PAF-stimulated PMNs.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-11"},"PeriodicalIF":1.3,"publicationDate":"2025-11-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145604219","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}
Pub Date : 2025-11-16DOI: 10.1080/10286020.2025.2582733
Chaeeun Bang, Eun Hyang Jang, Da-Eun Lee, Gye Lim Kim, Yunjae Jung, Hanbo Shin, Jin Hee Na, Sangmin Lee, Jong-Ho Kim
Glutinol (GT), a major triterpenoid component of Orostachys japonica, suppresses TGF-β-induced epithelial-mesenchymal transition (EMT) in human cancer cells. GT treatment restored epithelial characteristics by upregulating E-cadherin and downregulating Snail, thereby reducing cancer cell migration and invasion in A549 and MCF-7 cells. In vivo, GT significantly inhibited lung metastasis of TGF-β-treated A549-luc cells in mice. These findings demonstrate that GT exerts potent anti-metastatic effects through modulation of the TGF-β/Snail/E-cadherin signaling axis, highlighting its potential as a natural therapeutic agent against cancer metastasis.
{"title":"Glutinol, main component of <i>orostachys japonica</i>, inhibits <i>in vitro and in vivo</i> TGF-β-induced epithelial mesenchymal transition of human cancer cells.","authors":"Chaeeun Bang, Eun Hyang Jang, Da-Eun Lee, Gye Lim Kim, Yunjae Jung, Hanbo Shin, Jin Hee Na, Sangmin Lee, Jong-Ho Kim","doi":"10.1080/10286020.2025.2582733","DOIUrl":"https://doi.org/10.1080/10286020.2025.2582733","url":null,"abstract":"<p><p>Glutinol (GT), a major triterpenoid component of <i>Orostachys japonica</i>, suppresses TGF-β-induced epithelial-mesenchymal transition (EMT) in human cancer cells. GT treatment restored epithelial characteristics by upregulating E-cadherin and downregulating Snail, thereby reducing cancer cell migration and invasion in A549 and MCF-7 cells. <i>In vivo</i>, GT significantly inhibited lung metastasis of TGF-β-treated A549-luc cells in mice. These findings demonstrate that GT exerts potent anti-metastatic effects through modulation of the TGF-β/Snail/E-cadherin signaling axis, highlighting its potential as a natural therapeutic agent against cancer metastasis.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-13"},"PeriodicalIF":1.3,"publicationDate":"2025-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145530592","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}
Pub Date : 2025-11-16DOI: 10.1080/10286020.2025.2577900
Qiu-Hong Li, Ming-Xing Lu, Yu-Han Feng, Mao Zhao, Ting-Dan Mo, Wen-Wen Jiang, Xia Zhang, Lu Wang
Rutin, a dietary flavonoid, can relieve insulin resistance to improve hyperglycemia, while the precise mechanism remains unclear. In this study, we found that rutin bound well to the insulin receptor, alleviated glucosamine-induced insulin resistance in HepG2 cells and observably increased glucose consumption and glucose uptake in vitro. Furthermore, rutin increased the levels of IRS-1, IRS-2, PI3K, p-AKT, p-GSK3β and p-FOXO1 and decreased the expression of p-IRS-1, p-GS, PEPCK and G6Pase, indicating that rutin could promote glycogen synthesis and inhibit gluconeogenesis via the IRS/PI3K/Akt signaling pathway. Overall, the findings confirmed that rutin potentially mitigates glucosamine-induced insulin resistance in hepatocytes via activation of IRS/PI3K/Akt pathways.
{"title":"Rutin inhibits hepatic gluconeogenesis and increases glycogen synthesis through the IRS/PI3K/akt signaling pathway in insulin resistant hepatocytes.","authors":"Qiu-Hong Li, Ming-Xing Lu, Yu-Han Feng, Mao Zhao, Ting-Dan Mo, Wen-Wen Jiang, Xia Zhang, Lu Wang","doi":"10.1080/10286020.2025.2577900","DOIUrl":"https://doi.org/10.1080/10286020.2025.2577900","url":null,"abstract":"<p><p>Rutin, a dietary flavonoid, can relieve insulin resistance to improve hyperglycemia, while the precise mechanism remains unclear. In this study, we found that rutin bound well to the insulin receptor, alleviated glucosamine-induced insulin resistance in HepG2 cells and observably increased glucose consumption and glucose uptake <i>in vitro</i>. Furthermore, rutin increased the levels of IRS-1, IRS-2, PI3K, p-AKT, p-GSK3β and p-FOXO1 and decreased the expression of p-IRS-1, p-GS, PEPCK and G6Pase, indicating that rutin could promote glycogen synthesis and inhibit gluconeogenesis via the IRS/PI3K/Akt signaling pathway. Overall, the findings confirmed that rutin potentially mitigates glucosamine-induced insulin resistance in hepatocytes via activation of IRS/PI3K/Akt pathways.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-15"},"PeriodicalIF":1.3,"publicationDate":"2025-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145534344","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}
Two previously undescribed macrocyclic diterpenoids, cycloserratol (1) and isopapyrifuranol A (2) were isolated from the gum resin of Boswellia seratta. Compound 1 was confirmed as trihydroxy substituted 12-membered macrocyclic cembrane-type diterpenoid skeleton and 2 was a new 1,12-oxygen fused trihydroxy cembrane skeleton. The structures of these new metabolites were characterized by HRESIMS, 1D NMR and 2D NMR analysis.
{"title":"Two new macrocyclic cembrane diterpenoids from <i>Boswellia seratta</i> gum resin.","authors":"Durgaprasad Metta, Raveendra Babu Kothapalli, Ramarao Paidi, Ramakrishna Singuru","doi":"10.1080/10286020.2025.2583447","DOIUrl":"https://doi.org/10.1080/10286020.2025.2583447","url":null,"abstract":"<p><p>Two previously undescribed macrocyclic diterpenoids, cycloserratol (<b>1</b>) and isopapyrifuranol A (<b>2</b>) were isolated from the gum resin of <i>Boswellia seratta.</i> Compound <b>1</b> was confirmed as trihydroxy substituted 12-membered macrocyclic cembrane-type diterpenoid skeleton and <b>2</b> was a new 1,12-oxygen fused trihydroxy cembrane skeleton. The structures of these new metabolites were characterized by HRESIMS, 1D NMR and 2D NMR analysis.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-8"},"PeriodicalIF":1.3,"publicationDate":"2025-11-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145504492","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}
Pub Date : 2025-11-13DOI: 10.1080/10286020.2025.2581721
Ning Li, Xing-Long Dai, Gui-Xin Xiong, Wan-Li Meng, Jie Hao, Jie-Jie Hao
N-(4-Guanidinobutyl)-2-(4-hydroxyphenyl)-2-oxoacetamide (C1), a marine-derived leonurine analogue, was synthesized via a six-step route with 38% total yield. Biological evaluation demonstrated potent anticoagulant activity through significant prolongation of APTT (20 mM) and PT (5 mM). C1 dose-dependently (100-200 μM) suppressed LPS-induced NO production in RAW 264.7 macrophages without cytotoxicity and modulated phagocytosis. In LPS-induced acute lung injury rats, C1 reduced proinflammatory cytokines in BALF. These findings highlight C1's dual anticoagulant and anti-inflammatory properties as a promising lead compound.
{"title":"Synthesis and biological activity of the marine-derived leonurine analogue N-(4-guanidinobutyl)-2-(4-hydroxyphenyl)-2-oxoacetamide.","authors":"Ning Li, Xing-Long Dai, Gui-Xin Xiong, Wan-Li Meng, Jie Hao, Jie-Jie Hao","doi":"10.1080/10286020.2025.2581721","DOIUrl":"https://doi.org/10.1080/10286020.2025.2581721","url":null,"abstract":"<p><p>N-(4-Guanidinobutyl)-2-(4-hydroxyphenyl)-2-oxoacetamide (<b>C1</b>), a marine-derived leonurine analogue, was synthesized via a six-step route with 38% total yield. Biological evaluation demonstrated potent anticoagulant activity through significant prolongation of APTT (20 mM) and PT (5 mM). <b>C1</b> dose-dependently (100-200 μM) suppressed LPS-induced NO production in RAW 264.7 macrophages without cytotoxicity and modulated phagocytosis. In LPS-induced acute lung injury rats, <b>C1</b> reduced proinflammatory cytokines in BALF. These findings highlight <b>C1</b>'s dual anticoagulant and anti-inflammatory properties as a promising lead compound.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-17"},"PeriodicalIF":1.3,"publicationDate":"2025-11-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145504563","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}
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