Journal of Natural Medicines最新文献

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Overwhelming glycyrrhizin production in Glycyrrhiza glabra induced by rihizobial symbiosis. 根瘤菌共生诱导光甘草产生压倒性甘草酸。
IF 2.5 4区 医学
Journal of Natural Medicines Pub Date : 2025-05-25 DOI: 10.1007/s11418-025-01918-2
Shion Yamamoto, Aya Shimomura, Satoshi Watanabe, Mareshige Kojoma, Akihiro Suzuki
{"title":"Overwhelming glycyrrhizin production in Glycyrrhiza glabra induced by rihizobial symbiosis.","authors":"Shion Yamamoto, Aya Shimomura, Satoshi Watanabe, Mareshige Kojoma, Akihiro Suzuki","doi":"10.1007/s11418-025-01918-2","DOIUrl":"https://doi.org/10.1007/s11418-025-01918-2","url":null,"abstract":"<p><p>We reported that Glycyrrhiza uralensis inoculated with rhizobium tended to increase biomass production and glycyrrhizic acid (GL) production, in this study we have also achieved drastically increase in biomass and GL production in Glycyrrhiza glabra. At thirty days after inoculation (DAI), a significant increase in SPAD values was observed, and the expression of GL synthesis marker genes was also significantly increased. At 150 DAI, a significant increase in biomass was observed. Characteristically, it was also found that thick roots were enlarged by rhizobial inoculation. In addition, the expression of GL synthesis marker genes was also significantly increased. Moreover, GL content per unit root dry weight reached 4%, and GL production per plant increased six times compared to uninoculated plants. Moreover, we tried to reveal the mechanism of induction of GL production by rhizobial inoculation. Since it has been reported that the expression of jasmonic acid (JA) synthesis marker genes is increased by rhizobium in soybean, we investigated the expression of those genes in G. glabra, and found that GgMYC2 and GgJAR1 were up-regulated at Thirty DAI. Furthermore, methyl jasmonate treatment increased the expression of GL synthesis marker genes, suggesting that JA signaling is involved in the increased GL production due to rhizobial inoculation. These results aid in understanding the mechanism of increased GL production through the introduction of rhizobial symbiosis, and show the potential for providing a technology to significantly shorten the cultivation period for the production of Glycyrrhiza that meets the criteria for herbal medicines.</p>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2025-05-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144141070","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A plasma metabolomic analysis revealed the metabolic regulatory mechanism of the water extract of Dendrobium huoshanense in improving streptozotocin-induced type 1 diabetes model rats. 血浆代谢组学分析揭示了霍山石斛水提物改善链脲佐菌素诱导的1型糖尿病模型大鼠代谢调节机制。
IF 2.5 4区 医学
Journal of Natural Medicines Pub Date : 2025-05-20 DOI: 10.1007/s11418-025-01909-3
Hai-Jun Xu, Zhen Zhang, Ya-Fei Zhang, Shu-Nan Cuan, Zhe Jia
{"title":"A plasma metabolomic analysis revealed the metabolic regulatory mechanism of the water extract of Dendrobium huoshanense in improving streptozotocin-induced type 1 diabetes model rats.","authors":"Hai-Jun Xu, Zhen Zhang, Ya-Fei Zhang, Shu-Nan Cuan, Zhe Jia","doi":"10.1007/s11418-025-01909-3","DOIUrl":"https://doi.org/10.1007/s11418-025-01909-3","url":null,"abstract":"<p><p>D. huoshanense is a traditional Chinese medicine with antidiabetes effects, but the underlying metabolic regulatory mechanism remains unknown. Plasma metabolomic analysis was applied to assess the metabolic regulatory mechanism underlying the alleviation of streptozotocin-induced type 1 diabetes (STZ-T1D) by D. huoshanense. The successfully STZ-T1D model rats were assigned to the model group, the model + water extract of D. huoshanense (DHWE) group, and the model + metformin (MET) group. They were administered the corresponding medication by gavage. After 28 days, the plasma levels of glucose, malondialdehyde (MDA), C-reactive protein (CRP), and total antioxidant capacity (T-AOC) were determined. Morphological changes in the pancreatic islet tissue were analyzed via hematoxylin and eosin (H&E) staining. The expression of occludin-1, zonula occludens protein 1 (ZO-1) and protein kinase RNA-like endoplasmic reticulum kinase (PERK) in the ileum tissue was determined via western blotting. Nontargeted metabolome analysis of the plasma was performed via ultrahigh-performance liquid chromatography. The results revealed that DHWE reduced blood glucose, C-reactive protein, and MDA levels; increased plasma T-AOC; improved intestinal mucous integrity and pancreatic islet morphological structure; and alleviated intestinal endoplasmic reticulum stress. Plasma metabolomics revealed that DHWE significantly increased the levels of ascorbic acid 2-sulfate, L-thyroxine, phosphatidylcholine (PC) (14:0e/5:0), and PC (16:1e/4:0); decreased the levels of D-(-)-fructose and indole-3-lactic acid; and significantly affected ascorbate and aldarate metabolism and glyoxylate and dicarboxylate metabolism in STZ-T1D rats (p < 0.05), and the effects on the citric acid cycle and pyruvate metabolism tended to be significant (p < 0.1). This study confirmed that DHWE alleviated STZ-T1D by reducing oxidative stress and the inflammatory response, enhancing intestinal mucosa integrity and affecting mainly the energy metabolism and vitamin C metabolism of STZ-T1D rats.</p>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2025-05-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144109375","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Safranal ameliorates atherosclerosis progression partly via repressing PI3K/Akt and NF-κB signaling pathways in ApoE (-/-) mice. Safranal部分通过抑制ApoE(-/-)小鼠的PI3K/Akt和NF-κ b信号通路来改善动脉粥样硬化进展。
IF 2.5 4区 医学
Journal of Natural Medicines Pub Date : 2025-05-14 DOI: 10.1007/s11418-025-01913-7
Yining Geng, Manping Song, Bing Huang, Ru Lin, Shiwen Wu, An Lin
{"title":"Safranal ameliorates atherosclerosis progression partly via repressing PI3K/Akt and NF-κB signaling pathways in ApoE (-/-) mice.","authors":"Yining Geng, Manping Song, Bing Huang, Ru Lin, Shiwen Wu, An Lin","doi":"10.1007/s11418-025-01913-7","DOIUrl":"https://doi.org/10.1007/s11418-025-01913-7","url":null,"abstract":"<p><p>Atherosclerosis (AS) remains the main cause of vascular diseases. This study reveals the effects of safranal and underlying mechanisms in RAW264.7 macrophages under AS context, which is hoped to facilitate its clinical application. Safranal reduced AS progression in ApoE (-/-) mice, and it also increased the serum level of HDL-C and decreased the levels of TG, TC, and LDL-C as well as ALT and AST. Besides, safranal repressed the pathophysiological processes of OS (downregulated levels of ROS and MDA and upregulated biosynthesis of GSH), ERS (decreased protein levels of activating transcription factor 6, X-Box Binding Protein 1, and glucose-regulated protein, 78 kDa), and inflammation (downregulated serum levels of TNF-α, IL-1β, and IL-6) in vivo. Mechanistically, safranal repressed PI3K/Akt and NF-κB signaling pathways in vivo. On the cellular level, safranal treatment relieved the uptake of ox-LDL, and decreased contents of TG, TC, and LDL-C while increasing HDL-C level in ox-LDL-treated RAW264.7 macrophages. It also reduced the molecular indexes of pathophysiological processes (OS, ESR, and release of inflammatory mediators) in ox-LDL-exposed RAW264.7 macrophages. Notably, safranal treatment also impaired PI3K/Akt and NF-κB signaling pathways in ox-LDL-exposed RAW264.7 macrophages. Additionally, the PI3K agonist 740Y-P notably reversed the in vitro inhibitory effects of safranal on lipid deposition, productions of TC and TNF-α, and protein levels of molecules of PI3K/Akt and NF-κB signaling pathways. Safranal exerts anti-AS effects via repressing OS, ERS, and inflammation in ApoE (-/-) mice, and it also negatively modulates PI3K/Akt and NF-κB signaling pathways in RAW264.7 macrophages.</p>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2025-05-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143957551","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Ginsenoside Rh3-induced neurotoxicity involving the IP3R-Ca2+/NOX2/NF-κB signaling pathways. 人参皂苷rh3诱导的神经毒性涉及IP3R-Ca2+/NOX2/NF-κB信号通路。
IF 2.5 4区 医学
Journal of Natural Medicines Pub Date : 2025-05-13 DOI: 10.1007/s11418-025-01912-8
Yuheng Wang, Jianwen Chen, Song Li, Zhengxu Cai
{"title":"Ginsenoside Rh3-induced neurotoxicity involving the IP3R-Ca<sup>2+</sup>/NOX2/NF-κB signaling pathways.","authors":"Yuheng Wang, Jianwen Chen, Song Li, Zhengxu Cai","doi":"10.1007/s11418-025-01912-8","DOIUrl":"https://doi.org/10.1007/s11418-025-01912-8","url":null,"abstract":"<p><p>Ginsenoside Rh3, a bioactive component of ginsenosides, has gained attention for its potential therapeutic effects, especially in cancer treatment. However, its neurotoxic effects remain poorly characterized, raising concerns about its safety for clinical use. This study investigates the neurotoxic effects of ginsenoside Rh3 and explores the underlying mechanisms. We demonstrate that ginsenoside Rh3 induces significant cytotoxicity in Neuro-2a and C8-D1A cells, as confirmed by methyl thiazolyl tetrazolium (MTT) assays, live-dead staining, and lactate dehydrogenase (LDH) release assays. Neurotoxicity polymerase chain reaction (PCR) array analyses show that the cytotoxicity of ginsenoside Rh3 in Neuro-2a cells involves calcium ion transport, oxidative stress, inflammation, and programmed cell death (PCD). Specifically, ginsenoside Rh3 elevates intracellular Ca<sup>2+</sup> levels by activating the inositol 1,4,5-triphosphate receptor (IP3R), which in turn increases oxidative stress via nicotinamide adenine dinucleotide phosphate (NADPH) oxidase (NOX) 2. This cascade activates the phosphorylated nuclear factor-kappa B (NF-κB) signaling pathway, exacerbating apoptosis and leading to neuronal cell death. Molecular docking and dynamics simulations suggest direct interactions between ginsenoside Rh3 and both IP3R and NOX2. Notably, the neurotoxic effects of ginsenoside Rh3 were significantly attenuated by IP3R inhibitor 2-aminoethyl diphenylborinate (2-APB) and NOX2 inhibitor GSK2795039. These findings demonstrate that ginsenoside Rh3 induces neurotoxicity through IP3R-Ca<sup>2+</sup>/NOX2/NF-κB signaling pathways. This study provides critical insights into the safety concerns of ginsenoside Rh3, highlighting the need for caution in its clinical applications.</p>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2025-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143957604","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Loganin ameliorates left ventricular fibrosis and dysfunction induced by pressure overload via the Sirt1/AKT/TGF-β1 signaling pathway. 罗甘素通过Sirt1/AKT/TGF-β1信号通路改善压力过载诱导的左心室纤维化和功能障碍。
IF 2.5 4区 医学
Journal of Natural Medicines Pub Date : 2025-05-10 DOI: 10.1007/s11418-025-01911-9
Changbin Wang, Xiaoli Jiang, Shuhua Han, Huimei Zang, Xiaoyuan Gao
{"title":"Loganin ameliorates left ventricular fibrosis and dysfunction induced by pressure overload via the Sirt1/AKT/TGF-β1 signaling pathway.","authors":"Changbin Wang, Xiaoli Jiang, Shuhua Han, Huimei Zang, Xiaoyuan Gao","doi":"10.1007/s11418-025-01911-9","DOIUrl":"https://doi.org/10.1007/s11418-025-01911-9","url":null,"abstract":"<p><p>Loganin (LG), a natural compound derived from Cornus officinalis Sieb. et Zucc., possesses diverse pharmacological properties, such as anti-inflammatory, anti-hypertrophic, and antioxidant effects. However, the role of LG in the pathogenesis of Heart Failure (HF) remains unclear. The current work aimed to explore the underlying mechanism of LG in pressure overload-induced HF, both in vivo and in vitro, using transverse aortic constriction (TAC) surgery or isoproterenol (ISO) administration. Following eight weeks of TAC surgery, histological assessments, including hematoxylin and eosin staining, wheat germ agglutinin staining, TUNEL assay, and Masson's trichrome staining, were conducted to evaluate the extent of cardiomyocyte remodeling. Additionally, RT-PCR and WB analyses were performed to detect the levels of various targets. Furthermore, H9C2 cardiomyocytes were treated with ISO to induce hypertrophy, and the effects of LG on cell viability, α-smooth muscle actin (α-SMA) expression, and molecular targets were investigated. Our findings revealed that LG treatment at 40 mg/kg/day significantly attenuated cardiac dysfunction, decreased left ventricular collagen deposition in both interstitial and perivascular spaces. Mechanistically, LG mitigated ISO-induced toxicity in H9C2 cardiomyocytes, decreasing cellular hypertrophy and α-SMA expression. Moreover, we observed a downregulation of Sirtuin 1 (Sirt1) at the molecular level, accompanied by reduced phosphorylation of Akt and transforming growth factor-β1 (TGF-β1). Notably, the administration of the Sirt1 inhibitor, EX527, effectively abolished the protective effects of LG. Therefore, the cardio-protective effects of LG were mediated through the activation of the Sirt1/Akt/TGF-β1 signaling pathway, leading to reduced fibrosis and improved cardiac function.</p>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2025-05-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143959754","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Chlorinated illudalane sequiterpenoids from Saxiglossum angustissimum. 木参中氯代幻烷类四萜化合物。
IF 2.5 4区 医学
Journal of Natural Medicines Pub Date : 2025-05-09 DOI: 10.1007/s11418-025-01910-w
Yu-Ting Chen, Jian-Hua Hong, Cai-Ying Peng, Jian-Qun Liu, Yu-Ye Zhu, Ji-Cheng Shu
{"title":"Chlorinated illudalane sequiterpenoids from Saxiglossum angustissimum.","authors":"Yu-Ting Chen, Jian-Hua Hong, Cai-Ying Peng, Jian-Qun Liu, Yu-Ye Zhu, Ji-Cheng Shu","doi":"10.1007/s11418-025-01910-w","DOIUrl":"https://doi.org/10.1007/s11418-025-01910-w","url":null,"abstract":"<p><p>Eight chlorinated illudalane sesquiterpenoids were isolated from the aerial parts of Saxiglossum angustissimum, including a pair of new pterosin enantiomers, (2R)-angupterosin (1) and (2S)-angupterosin (2), as well as a new pteroside, angupteroside (3). The structures of these compounds were determined through comprehensive analysis of HRESI-MS, NMR spectral data, ECD, and comparisons with previously reported literature. Remarkably, these chlorine-containing compounds (1-8) are rare and represent the first discovery of such metabolites within the family Pyrrosioideae. The chlorinated illudalane sesquiterpenoids from S. angustissimum may serve as valuable chemotaxonomic markers for this species. Furthermore, compounds 1-8 demonstrated inhibitory effects on LPS-induced NO release in BV2 cells, highlighting their potential anti-inflammatory properties.</p>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2025-05-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143957574","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Amyloid-β aggregation inhibitory activity of triterpene saponins from the cactus Stenocereus gummosus. 仙人掌三萜皂苷抑制淀粉样蛋白-β聚集活性的研究。
IF 2.5 4区 医学
Journal of Natural Medicines Pub Date : 2025-05-08 DOI: 10.1007/s11418-025-01905-7
Tatsumi Matsumoto, Koji Fujihara, Tomomi Inayama, Hiroaki Sasaki, Kaoru Kinoshita
{"title":"Amyloid-β aggregation inhibitory activity of triterpene saponins from the cactus Stenocereus gummosus.","authors":"Tatsumi Matsumoto, Koji Fujihara, Tomomi Inayama, Hiroaki Sasaki, Kaoru Kinoshita","doi":"10.1007/s11418-025-01905-7","DOIUrl":"https://doi.org/10.1007/s11418-025-01905-7","url":null,"abstract":"<p><p>Seven new triterpene saponins (1-7) and two known saponins (8, 9) were isolated from MeOH extracts of Stenocereus gummosus (Engelm.) A.C.Gibson & K.E.Horak. The structures of the isolated saponins were elucidated using MS, IR and comprehensive NMR measurements. To develop drugs for treating Alzheimer's disease (AD) based on the amyloid cascade hypothesis, the isolated saponins were evaluated for inhibition of amyloid beta (Aβ) aggregation using the thioflavin-T (Th-T) assay. Among the isolated saponins, weak activity was observed for compounds 1, 2, 8 and 9 (IC<sub>50</sub> = 39.0, 36.7, 39.5, and 35.7 µM, respectively). The aglycons of the isolated saponins, gummosogenin and alamosenogenin, also showed inhibitory activity related to Aβ aggregation (IC<sub>50</sub> = 14.9 and 15.5 µM, respectively).</p>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2025-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143959406","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Oleanane-type triterpene saponins promote extracellular vesicle secretion of human adipose-derived mesenchymal stem cells. 齐墩烷型三萜皂苷促进人脂肪源性间充质干细胞胞外囊泡分泌。
IF 2.5 4区 医学
Journal of Natural Medicines Pub Date : 2025-05-07 DOI: 10.1007/s11418-025-01908-4
Jianyu Lin, Hongqiang Lin, Kohei Sato, Atsushi Kimishima, Satoru Tamura, Kazuki Ujiie, Chitose Oneyama, Jinping Liu, Masayoshi Arai
{"title":"Oleanane-type triterpene saponins promote extracellular vesicle secretion of human adipose-derived mesenchymal stem cells.","authors":"Jianyu Lin, Hongqiang Lin, Kohei Sato, Atsushi Kimishima, Satoru Tamura, Kazuki Ujiie, Chitose Oneyama, Jinping Liu, Masayoshi Arai","doi":"10.1007/s11418-025-01908-4","DOIUrl":"https://doi.org/10.1007/s11418-025-01908-4","url":null,"abstract":"<p><p>The application of mesenchymal stem cell (MSC)-derived extracellular vesicles (EVs) holds significant promise in anti-aging cosmetics, regenerative medicine, and drug delivery systems. However, their limited production efficiency remains a critical barrier to advancing related therapies and pharmaceutical applications. In this study, a library of triterpene saponins was screened, leading to the re-discovery of an oleanane-type triterpene saponin Lucyoside H (1), along with its structural analogs, Chikusetsusaponins IVa (2), IV (3), and V (4), which were found to increase the production of EV from human adipose-derived mesenchymal stem cells (ADMSCs) at a concentration ranging from 10 to 100 µM. A comparative analysis of the chemical structures and activities of all evaluated compounds, along with oleanolic acid (5), revealed that (i) disubstitution of glycosyl on C-3 and C-28 of oleanane aglycone was crucial to the promoting effect; (ii) 3-O-β-D-glucuronopyranosyl substitution achieved the highest efficiency in the promoting effect and alteration of this group attenuated the activity. These results highlight the potential for developing a natural product-based approach to increase EV production by MSCs.</p>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2025-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143951344","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Identification of specialized metabolites from Artocarpus lacucha as potent α-glucosidase and acetylcholinesterase inhibitors: enzyme kinetic, in vitro and in silico study. 石竹特化代谢物α-葡萄糖苷酶和乙酰胆碱酯酶抑制剂的鉴定:酶动力学、体外和室内研究。
IF 2.5 4区 医学
Journal of Natural Medicines Pub Date : 2025-05-06 DOI: 10.1007/s11418-025-01904-8
Weerasak Songoen, Witthawat Phanchai, Johann Schinnerl, Lothar Brecker, Morakot Thabpho, Sorachat Tharamak, Wanchai Pluempanupat, Siriphan Sukkhaeng, Sasiwimol Chansuthep
{"title":"Identification of specialized metabolites from Artocarpus lacucha as potent α-glucosidase and acetylcholinesterase inhibitors: enzyme kinetic, in vitro and in silico study.","authors":"Weerasak Songoen, Witthawat Phanchai, Johann Schinnerl, Lothar Brecker, Morakot Thabpho, Sorachat Tharamak, Wanchai Pluempanupat, Siriphan Sukkhaeng, Sasiwimol Chansuthep","doi":"10.1007/s11418-025-01904-8","DOIUrl":"https://doi.org/10.1007/s11418-025-01904-8","url":null,"abstract":"<p><p>Artocarpus species play an important role in the folk medicine of various ethnic groups in Africa, South Asia, and Southeast Asia. In the present study, we investigated the potential of Artocarpus lacucha in the treatment of diabetes mellitus and Alzheimer's disease. During this work, one previously undescribed compound (1), along with 10 known compounds (2-11), were isolated from the leaves of Artocarpus lacucha. Their molecular structures were established using NMR and HRMS experiments. Among the tested compounds, flavan-benzofuran artocarpinol B, displayed significant α-glucosidase inhibitory activity with an IC<sub>50</sub> value of 4.01 ± 0.04 µM (positive control acarbose: 475.14 ± 4.65 µM). The conducted enzyme kinetic study revealed their inhibition mode through competitive type. This is also supported by the molecular docking and dynamics simulations which gave insight into the interactions and stability between α-glucosidase and artocarpinol B in the active site. In addition, 4-geranyl-2',3,4',5-tetrahydroxy-trans-stilbene (5) further shows potent acetylcholinesterase inhibition, with IC<sub>50</sub> = 8.57 ± 0.39 µM. Compounds 5 and 6 displayed moderate activity against Staphylococcus aureus and Streptococcus agalactiae, with MIC and MBC values ranging from 26.9 to 69.9 μM. This study explored the potential of constituents from A. lacucha as α-glucosidase and acetylcholinesterase inhibitors, which are crucial in the treatment of Diabetes mellitus and Alzheimer's disease.</p>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2025-05-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143951881","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Mechanism study of the effects of astragaloside IV and quercetin on idiopathic pulmonary fibrosis. 黄芪甲苷、槲皮素治疗特发性肺纤维化的机制研究。
IF 2.5 4区 医学
Journal of Natural Medicines Pub Date : 2025-04-30 DOI: 10.1007/s11418-025-01896-5
Ye Luo, Chang-Jun Xu, Xing-Hui Ai, Yu-Ping Li, Xing Zhu, Chang-Fu Yang
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