Pub Date : 2024-06-21DOI: 10.1080/10286020.2024.2349660
Modifications at different positions on the aloperine molecule were performed to improve its anticancer activity and develop anticancer drugs. The in vitro anticancer activities of 44 synthesized compounds were evaluated. The effect of modification positions on anticancer activity was discussed and a structure–activity relationship analysis was established. A novel series of compounds with modifications at the N12 position showed much higher cytotoxicity than aloperine. Among them, compound 22 displayed promising in vitro anticancer activity against PC9 cells with a median inhibitory concentration (IC50) of 1.43 μM. The mechanism studies indicated that compound 22 induced cell apoptosis and cell cycle arrest in PC9 cells. These results demonstrate the potential of aloperine thiourea derivatives in anticancer activity.
{"title":"Design, synthesis and biological evaluation of aloperine derivatives as potential anticancer agents","authors":"","doi":"10.1080/10286020.2024.2349660","DOIUrl":"10.1080/10286020.2024.2349660","url":null,"abstract":"<div><p>Modifications at different positions on the aloperine molecule were performed to improve its anticancer activity and develop anticancer drugs. The <em>in vitro</em> anticancer activities of 44 synthesized compounds were evaluated. The effect of modification positions on anticancer activity was discussed and a structure–activity relationship analysis was established. A novel series of compounds with modifications at the <em>N</em>12 position showed much higher cytotoxicity than aloperine. Among them, compound <strong>22</strong> displayed promising <em>in vitro</em> anticancer activity against PC9 cells with a median inhibitory concentration (IC<sub>50</sub>) of 1.43 μM. The mechanism studies indicated that compound <strong>22</strong> induced cell apoptosis and cell cycle arrest in PC9 cells. These results demonstrate the potential of aloperine thiourea derivatives in anticancer activity.</p></div>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2024-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141450595","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 : 2024-06-21DOI: 10.1080/10286020.2024.2368831
Natthaphitcha Khunsantiphong, May Thazin Thant, Chattarika Pengdee, Thanarat Salahong, Hnin Ei Ei Khine, Pithi Chanvorachote, Chatchai Chaotham, Boonchoo Sritularak
Dendroochreatene (1), a new phenanthrene derivative with a spirolactone ring, was isolated from the whole Dendrobium ochreatum plant together with 11 known compounds (2-12). The structure of the new compound was elucidated spectroscopically and phenolic compounds were firstly reported from D. ochreatum. Moscatilin (4), major compound isolated from D. ochreatum, was found to be cytotoxic toward H460 lung-cancer cells, with an IC50 value of 147.3 ± 0.9 µM, while loddigesiinol C (7), C-α-methoxy derivative was inactive.
{"title":"A new phenanthrene with a spirolactone ring from <i>Dendrobium ochreatum</i>.","authors":"Natthaphitcha Khunsantiphong, May Thazin Thant, Chattarika Pengdee, Thanarat Salahong, Hnin Ei Ei Khine, Pithi Chanvorachote, Chatchai Chaotham, Boonchoo Sritularak","doi":"10.1080/10286020.2024.2368831","DOIUrl":"https://doi.org/10.1080/10286020.2024.2368831","url":null,"abstract":"<p><p>Dendroochreatene (<b>1</b>), a new phenanthrene derivative with a spirolactone ring, was isolated from the whole <i>Dendrobium ochreatum</i> plant together with 11 known compounds (<b>2</b>-<b>12</b>). The structure of the new compound was elucidated spectroscopically and phenolic compounds were firstly reported from <i>D. ochreatum.</i> Moscatilin (<b>4</b>), major compound isolated from <i>D. ochreatum,</i> was found to be cytotoxic toward H460 lung-cancer cells, with an IC<sub>50</sub> value of 147.3 ± 0.9 µM, while loddigesiinol C (<b>7</b>), C-<i>α</i>-methoxy derivative was inactive.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2024-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141432046","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 : 2024-06-20DOI: 10.1080/10286020.2024.2363416
Shu-Lan Liu, Feng Wei, Jin Li, Ke-Jian Pang, Yerlan Bahetjan, Shi-Wen Kang, Xue-Ling Huang, Xin-Zhou Yang
A new coumarin (1) and a new flavonoid (2) were isolated from the air-dried flower buds of Ochrocarpus longifolius, together with ten known compounds (3-12). The structures of two new compounds were established by 1D and 2D NMR and MS data. In addition, the new compound 2 showed significant proliferation inhibitory activity on Eca-109 and MGC-803 cells. The results of this study may enrich the diversity of compounds from O. longifolius and provide a basis for further research on its natural products and pharmacological activities.
{"title":"A new coumarin and a new flavonoid from <i>Ochrocarpus longifolius</i>.","authors":"Shu-Lan Liu, Feng Wei, Jin Li, Ke-Jian Pang, Yerlan Bahetjan, Shi-Wen Kang, Xue-Ling Huang, Xin-Zhou Yang","doi":"10.1080/10286020.2024.2363416","DOIUrl":"https://doi.org/10.1080/10286020.2024.2363416","url":null,"abstract":"<p><p>A new coumarin (<b>1</b>) and a new flavonoid (<b>2</b>) were isolated from the air-dried flower buds of <i>Ochrocarpus longifolius</i>, together with ten known compounds (<b>3</b>-<b>12</b>). The structures of two new compounds were established by 1D and 2D NMR and MS data. In addition, the new compound <b>2</b> showed significant proliferation inhibitory activity on Eca-109 and MGC-803 cells. The results of this study may enrich the diversity of compounds from <i>O. longifolius</i> and provide a basis for further research on its natural products and pharmacological activities.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":null,"pages":null},"PeriodicalIF":1.7,"publicationDate":"2024-06-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141426941","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 : 2024-06-20DOI: 10.1080/10286020.2024.2362384
Lian Yang, Dong-Mei Lin, Xiu-Ming Cui, Lin-Jiao Shao, Xiao-Long Li, Fei-Xing Li, Xiao-Yan Yang
A new cladosporol derivative xylophilum A (1), together with 10 known compounds (2-11), were isolated from the rice fermentation of the fungus Cladosporium xylophilum. Their structures were established by extensive spectroscopic methods and comparison of their NMR data with literatures. The antimicrobial activity of compound 1 against 11 kinds of pathogenic microbial was evaluated, but no significant activity was found (MIC >100 μg/ml).
{"title":"Secondary metabolites from the fungus <i>Cladosporium xylophilum</i>.","authors":"Lian Yang, Dong-Mei Lin, Xiu-Ming Cui, Lin-Jiao Shao, Xiao-Long Li, Fei-Xing Li, Xiao-Yan Yang","doi":"10.1080/10286020.2024.2362384","DOIUrl":"https://doi.org/10.1080/10286020.2024.2362384","url":null,"abstract":"<p><p>A new cladosporol derivative xylophilum A (<b>1</b>), together with 10 known compounds (<b>2</b>-<b>11</b>), were isolated from the rice fermentation of the fungus <i>Cladosporium xylophilum</i>. Their structures were established by extensive spectroscopic methods and comparison of their NMR data with literatures. The antimicrobial activity of compound <b>1</b> against 11 kinds of pathogenic microbial was evaluated, but no significant activity was found (MIC >100 μg/ml).</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":null,"pages":null},"PeriodicalIF":1.7,"publicationDate":"2024-06-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141426942","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 new cucurbitane-type triterpenoid saponins, 2,20β,22β-trihydroxy-16α,23(R)-epoxycucurbita-1,5,24-triene-3,11-dione 2-O-β-D-glucopyranoside (1), 2,20β,22α-trihydroxy-16α,23(S)-epoxycucurbita-1,5...
{"title":"Two new cucurbitane-type triterpenoid saponins from the fruit of Citrullus colocynthis","authors":"Si-Qi Liu, Zi-Ming Feng, Xiang Yuan, Xu Zhang, Ya-Nan Yang, Jiang He, Pei-Cheng Zhang, Jian-Shuang Jiang","doi":"10.1080/10286020.2024.2364908","DOIUrl":"https://doi.org/10.1080/10286020.2024.2364908","url":null,"abstract":"Two new cucurbitane-type triterpenoid saponins, 2,20β,22β-trihydroxy-16α,23(R)-epoxycucurbita-1,5,24-triene-3,11-dione 2-O-β-D-glucopyranoside (1), 2,20β,22α-trihydroxy-16α,23(S)-epoxycucurbita-1,5...","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":null,"pages":null},"PeriodicalIF":1.7,"publicationDate":"2024-06-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141503000","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 : 2024-06-17DOI: 10.1080/10286020.2024.2365437
Jing-Yu Zhang, Hui-Lin Yang, Wen-Rui Li, Rong-Mei Gao, Mi Li, Ru-Bing Wang, Jia Yang, Qian-Ru Wang, Yu-Huan Li, Li Li, Shuang-Gang Ma
Three new prenylated C6-C3 compounds (1-3), together with two known prenylated C6-C3 compounds (4-5) and one known C6-C3 derivative (6), were isolated from the roots of Illicium brevistylum A. C. Smith. The structures of 1-3 were elucidated by spectroscopic methods including 1D and 2D NMR, HRESIMS, CD experiments and ECD calculations. The structure of illibrefunone A (1) was confirmed by single-crystal X-ray diffraction analysis. All compounds were evaluated in terms of their anti-inflammatory potential on nitric oxide (NO) generation in lipopolysaccharide-stimulated murine RAW264.7 macrophages and murine BV2 microglial cells, antiviral activity against Coxsackievirus B3 (CVB3) and influenza virus A/Hanfang/359/95 (H3N2). Compounds 3 and 4 exhibited potent inhibitory effects on the production of NO in RAW 264.7 cells with IC50 values of 20.57 and 12.87 μM respectively, which were greater than those of dexamethasone (positive control). Compounds 1 and 4-6 exhibited weak activity against Coxsackievirus B3, with IC50 values ranging from 25.87 to 33.33 μM.
从 Illicium brevistylum A. C. Smith 的根中分离出了三种新的前烯化 C6-C3 化合物(1-3),以及两种已知的前烯化 C6-C3 化合物(4-5)和一种已知的 C6-C3 衍生物(6)。通过光谱方法,包括一维和二维核磁共振、HRESIMS、CD 实验和 ECD 计算,阐明了 1-3 的结构。通过单晶 X 射线衍射分析证实了伊利布酮 A (1) 的结构。评估了所有化合物在脂多糖刺激的小鼠 RAW264.7 巨噬细胞和小鼠 BV2 微神经胶质细胞中产生一氧化氮(NO)的抗炎潜力,以及对柯萨奇病毒 B3(CVB3)和流感病毒 A/HANfang/359/95 (H3N2)的抗病毒活性。化合物 3 和 4 对 RAW 264.7 细胞中 NO 的产生具有强效抑制作用,IC50 值分别为 20.57 和 12.87 μM,高于地塞米松(阳性对照)。化合物 1 和 4-6 对柯萨奇病毒 B3 的活性较弱,IC50 值在 25.87 至 33.33 μM 之间。
{"title":"Bioactive prenylated c<sub>6</sub>-c<sub>3</sub> derivatives from the roots of <i>Illicium brevistylum</i>.","authors":"Jing-Yu Zhang, Hui-Lin Yang, Wen-Rui Li, Rong-Mei Gao, Mi Li, Ru-Bing Wang, Jia Yang, Qian-Ru Wang, Yu-Huan Li, Li Li, Shuang-Gang Ma","doi":"10.1080/10286020.2024.2365437","DOIUrl":"10.1080/10286020.2024.2365437","url":null,"abstract":"<p><p>Three new prenylated C<sub>6</sub>-C<sub>3</sub> compounds (<b>1-3</b>), together with two known prenylated C<sub>6</sub>-C<sub>3</sub> compounds (<b>4-5</b>) and one known C<sub>6</sub>-C<sub>3</sub> derivative (<b>6</b>), were isolated from the roots of <i>Illicium brevistylum</i> A. C. Smith. The structures of <b>1-3</b> were elucidated by spectroscopic methods including 1D and 2D NMR, HRESIMS, CD experiments and ECD calculations. The structure of illibrefunone A (<b>1</b>) was confirmed by single-crystal X-ray diffraction analysis. All compounds were evaluated in terms of their anti-inflammatory potential on nitric oxide (NO) generation in lipopolysaccharide-stimulated murine RAW264.7 macrophages and murine BV2 microglial cells, antiviral activity against Coxsackievirus B3 (CVB3) and influenza virus A/Hanfang/359/95 (H3N2). Compounds <b>3</b> and <b>4</b> exhibited potent inhibitory effects on the production of NO in RAW 264.7 cells with IC<sub>50</sub> values of 20.57 and 12.87 μM respectively, which were greater than those of dexamethasone (positive control). Compounds <b>1</b> and <b>4-6</b> exhibited weak activity against Coxsackievirus B3, with IC<sub>50</sub> values ranging from 25.87 to 33.33 μM.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2024-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141419215","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 : 2024-06-14DOI: 10.1080/10286020.2024.2365442
Feng-Wu Li, Na Zhou, Jing-Jing Li, Ya-Jun Zhang, Xue Zhao
One promising approach to overcome drug resistance in asthma treatments involves dual-target therapy, specifically targeting the β2 adrenergic receptor (β2-AR) and muscarinic-3 acetylcholine receptor (M3R). This study investigated the anti-asthma effects and dual-target mechanisms of glycyrrhizic acid, hesperidin, and platycodin D (GHP) from Zhisou San. GHP administration effectively attenuated OVA-induced inflammatory infiltration and overproduction of mucus in asthmatic mice. Additionally, GHP treatment significantly suppressed M3R and promoted β2-AR activation, resulting in the relaxation of tracheal smooth muscle. These findings concluded that GHP mitigated asthma by targeting β2-AR and M3R to ameliorate airway inflammation and modulate airway smooth muscle relaxation.
克服哮喘治疗中耐药性的一种有希望的方法是双靶向治疗,特别是针对β2肾上腺素能受体(β2-AR)和毒蕈碱-3乙酰胆碱受体(M3R)。本研究探讨了知母散中的甘草酸、橙皮甙和桔梗甙 D(GHP)的抗哮喘作用和双靶机制。服用 GHP 能有效减轻 OVA 诱导的哮喘小鼠炎症浸润和粘液过度分泌。此外,GHP 还能明显抑制 M3R,促进 β2-AR活化,从而使气管平滑肌松弛。这些研究结果表明,GHP通过靶向β2-AR和M3R来改善气道炎症和调节气道平滑肌松弛,从而缓解哮喘。
{"title":"Protective effects of bioactive components targeting β2-adrenergic receptors and muscarinic-3 acetylcholine receptor in Zhisou San on ovalbumin-induced allergic asthma.","authors":"Feng-Wu Li, Na Zhou, Jing-Jing Li, Ya-Jun Zhang, Xue Zhao","doi":"10.1080/10286020.2024.2365442","DOIUrl":"https://doi.org/10.1080/10286020.2024.2365442","url":null,"abstract":"<p><p>One promising approach to overcome drug resistance in asthma treatments involves dual-target therapy, specifically targeting the β2 adrenergic receptor (β<sub>2</sub>-AR) and muscarinic-3 acetylcholine receptor (M<sub>3</sub>R). This study investigated the anti-asthma effects and dual-target mechanisms of glycyrrhizic acid, hesperidin, and platycodin D (GHP) from Zhisou San. GHP administration effectively attenuated OVA-induced inflammatory infiltration and overproduction of mucus in asthmatic mice. Additionally, GHP treatment significantly suppressed M<sub>3</sub>R and promoted β<sub>2</sub>-AR activation, resulting in the relaxation of tracheal smooth muscle. These findings concluded that GHP mitigated asthma by targeting β<sub>2</sub>-AR and M<sub>3</sub>R to ameliorate airway inflammation and modulate airway smooth muscle relaxation.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":null,"pages":null},"PeriodicalIF":1.7,"publicationDate":"2024-06-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141317447","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 : 2024-06-13DOI: 10.1080/10286020.2024.2366010
Zhao Zhai, Jie Fu, Meng-Liang Ye, Jing-Yue Wang, Hao-Jian Zhang, Hang Yu, Xin-Yu Yang, Hui Xu, Jia-Chun Hu, Jin-Yue Lu, Heng-Tong Zuo, Yi Zhao, Jian-Ye Song, Yong Zhang, Yan Wang, Nian-Zeng Xing
Liquiritigenin is a natural medicine. However, its inhibitory effect and its potential mechanism on bladder cancer (BCa) remain to be explored. It was found that it could be visualized that the transplanted tumours in the low-dose liquiritigenin -treated group and the high-dose liquiritigenin -treated group were smaller than those in the model group. Liquiritigenin treatment led to alterations in Lachnoclostridium, Escherichia-Shigella, Alistipes and Akkermansia. Non-targeted metabolomics analysis showed that a total of multiple differential metabolites were identified between the model group and the high-dose liquiritigenin-treated group. This provides a new direction and rationale for the antitumour effects of liquiritigenin.
{"title":"The changes of intestinal microbiota and metabolomics during the inhibition of bladder cancer by liquiritigenin.","authors":"Zhao Zhai, Jie Fu, Meng-Liang Ye, Jing-Yue Wang, Hao-Jian Zhang, Hang Yu, Xin-Yu Yang, Hui Xu, Jia-Chun Hu, Jin-Yue Lu, Heng-Tong Zuo, Yi Zhao, Jian-Ye Song, Yong Zhang, Yan Wang, Nian-Zeng Xing","doi":"10.1080/10286020.2024.2366010","DOIUrl":"https://doi.org/10.1080/10286020.2024.2366010","url":null,"abstract":"<p><p>Liquiritigenin is a natural medicine. However, its inhibitory effect and its potential mechanism on bladder cancer (BCa) remain to be explored. It was found that it could be visualized that the transplanted tumours in the low-dose liquiritigenin -treated group and the high-dose liquiritigenin -treated group were smaller than those in the model group. Liquiritigenin treatment led to alterations in Lachnoclostridium, <i>Escherichia-Shigella, Alistipes</i> and <i>Akkermansia</i>. Non-targeted metabolomics analysis showed that a total of multiple differential metabolites were identified between the model group and the high-dose liquiritigenin-treated group. This provides a new direction and rationale for the antitumour effects of liquiritigenin.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":null,"pages":null},"PeriodicalIF":1.7,"publicationDate":"2024-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141310757","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 : 2024-06-13DOI: 10.1080/10286020.2024.2366007
Hong-Ping Wang, Zhao-Zhou Lin, Chen Zhao, Qiong Yin, Jun Jia
Astragalus membranaceus is a traditional Chinese medicine with multiple pharmacological activities. Modern pharmacological research has found that Astragalus membranaceus extract has an inhibitory effect on α-glucosidase, however, which component can inhibit the activity of α-glucosidase and its degree of inhibition are unknown. To address this issue, this study used affinity ultrafiltration screening combined with UPLC-ESI-Orbitrap-MS technology to screen α-glucosidase inhibitors in Astragalus membranaceus. Using affinity ultrafiltration technology, we obtained the active components, and using UPLC-ESI-Orbitrap-MS technology, we quickly analyzed and identified them. As a result, a total of 8 ingredients were selected as α-glucosidase inhibitors.
{"title":"Screening of potential α-glucosidase inhibitors from <i>astragalus membranaceus</i> by affinity ultrafiltration screening coupled with UPLC-ESI-Orbitrap-MS method.","authors":"Hong-Ping Wang, Zhao-Zhou Lin, Chen Zhao, Qiong Yin, Jun Jia","doi":"10.1080/10286020.2024.2366007","DOIUrl":"https://doi.org/10.1080/10286020.2024.2366007","url":null,"abstract":"<p><p><i>Astragalus membranaceus</i> is a traditional Chinese medicine with multiple pharmacological activities. Modern pharmacological research has found that <i>Astragalus membranaceus</i> extract has an inhibitory effect on α-glucosidase, however, which component can inhibit the activity of α-glucosidase and its degree of inhibition are unknown. To address this issue, this study used affinity ultrafiltration screening combined with UPLC-ESI-Orbitrap-MS technology to screen α-glucosidase inhibitors in <i>Astragalus membranaceus</i>. Using affinity ultrafiltration technology, we obtained the active components, and using UPLC-ESI-Orbitrap-MS technology, we quickly analyzed and identified them. As a result, a total of 8 ingredients were selected as α-glucosidase inhibitors.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":null,"pages":null},"PeriodicalIF":1.7,"publicationDate":"2024-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141310756","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 : 2024-06-13DOI: 10.1080/10286020.2024.2364912
Le Thi Giang, SeonJu Park, Nguyen Thi Cuc, Bui Huu Tai, Phan Van Kiem, Nguyen Thi Minh Hang, Ninh Khac Ban, Pham Van Cuong, Nguyen Xuan Nhiem
One new bithiophene derivative, 5-(but-3-en-1-yn-1-yl)-5'-(methoxymethyl)-2,2'-bithiophene (1), along with twelve known compounds, senecioester (2), tiglinsaureester (3), 5-acetoxymethyl-2'-(but-3-en-1-yn-1-yl)-2,5'-bithiophene (4), 5-(4-isovaleroyloxybut-1-ynyl)-2,2'-bithiophene (5), 5-hydroxymethyl-(2,5':2',5'')-terthienyl tiglate (6), 5-hydroxymethyl-(2,5':2',5'')-terthienyl agelate (7), 5- hydroxymethyl-2,5':2',5''-terthiophene dimethylacrylate (8), 5-methoxymethyl-2,2':5',2''-terthiophene (9), α-terthiophene (10), 1,3,8,9-tetrahydroxycoumestan 3-sulfate (11), demethylwedelolactone (12), and wedelolactone (13) were isolated from the methanol extract of aerial parts of Eclipta prostrata (L.) L. All isolated compounds were evaluated for the protective ability on the HepG2 cells. At the concentration of 100 μM, compounds 11-13 showed the highest hepatoprotective effects, with HepG2 cell viability ranging from 38.68% to 48.54%. Bithiophenes showed higher hepatoprotective cell viability than terthiophenes.
{"title":"Bithiophene and coumestan derivatives from <i>Eclipta prostrata</i> (L.) L. and their hepatoprotective activity.","authors":"Le Thi Giang, SeonJu Park, Nguyen Thi Cuc, Bui Huu Tai, Phan Van Kiem, Nguyen Thi Minh Hang, Ninh Khac Ban, Pham Van Cuong, Nguyen Xuan Nhiem","doi":"10.1080/10286020.2024.2364912","DOIUrl":"https://doi.org/10.1080/10286020.2024.2364912","url":null,"abstract":"<p><p>One new bithiophene derivative, 5-(but-3-en-1-yn-1-yl)-5'-(methoxymethyl)-2,2'-bithiophene (1), along with twelve known compounds, senecioester (2), tiglinsaureester (3), 5-acetoxymethyl-2'-(but-3-en-1-yn-1-yl)-2,5'-bithiophene <b>(</b>4), 5-(4-isovaleroyloxybut-1-ynyl)-2,2'-bithiophene (5), 5-hydroxymethyl-(2,5':2',5'')-terthienyl tiglate (6), 5-hydroxymethyl-(2,5':2',5'')-terthienyl agelate (7), 5- hydroxymethyl-2,5':2',5''-terthiophene dimethylacrylate (8), 5-methoxymethyl-2,2':5',2''-terthiophene (9), α-terthiophene (10), 1,3,8,9-tetrahydroxycoumestan 3-sulfate (11), demethylwedelolactone (12), and wedelolactone (13) were isolated from the methanol extract of aerial parts of <i>Eclipta prostrata</i> (L.) L. All isolated compounds were evaluated for the protective ability on the HepG2 cells. At the concentration of 100 μM, compounds <b>11</b>-<b>13</b> showed the highest hepatoprotective effects, with HepG2 cell viability ranging from 38.68% to 48.54%. Bithiophenes showed higher hepatoprotective cell viability than terthiophenes.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":null,"pages":null},"PeriodicalIF":1.7,"publicationDate":"2024-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141310754","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}