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Benzylisoquinoline alkaloids from the embryo of Nelumbo nucifera and their antioxidant effects. 莲胚中苯基异喹啉类生物碱及其抗氧化作用。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-01-01 Epub Date: 2024-12-03 DOI: 10.1016/j.fitote.2024.106330
Zhanrong Zhou, Xin Wang, Hongqing Wang, Hongjie Shao, Junhua Sun, Ruoyun Chen, Jie Kang
{"title":"Benzylisoquinoline alkaloids from the embryo of Nelumbo nucifera and their antioxidant effects.","authors":"Zhanrong Zhou, Xin Wang, Hongqing Wang, Hongjie Shao, Junhua Sun, Ruoyun Chen, Jie Kang","doi":"10.1016/j.fitote.2024.106330","DOIUrl":"10.1016/j.fitote.2024.106330","url":null,"abstract":"<p><p>Seven benzylisoquinoline alkaloids, including three new (1-3) and four known compounds (4-7), were isolated from the embryo of Nelumbo nucifera (Plumula Nelumbinis). Their structures were elucidated by UV, IR, HRESIMS, 1D and 2D NMR, and ECD spectra, as well as optical rotations. All compounds were tested for the antioxidant activity. Compounds 1-7 prevented Fe<sup>2+</sup> induced lipid peroxidation in mouse liver microsomes, with the inhibitory rates of 76.1, 75.7, 60.0, 82.9, 75.5, 83.8 and 85.3 %, respectively.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106330"},"PeriodicalIF":2.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142784947","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}
引用次数: 0
Research on the anti-hepatic fibrosis effects and active components of the medicinal plant Tithonia diversifolia. 药用植物穿山甲抗肝纤维化作用及活性成分的研究。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-01-01 Epub Date: 2024-11-26 DOI: 10.1016/j.fitote.2024.106317
Jialin Wang, Haini Li, Ting Wang, Haifeng Xie, Yang Ruan, Chaofeng Zhang
{"title":"Research on the anti-hepatic fibrosis effects and active components of the medicinal plant Tithonia diversifolia.","authors":"Jialin Wang, Haini Li, Ting Wang, Haifeng Xie, Yang Ruan, Chaofeng Zhang","doi":"10.1016/j.fitote.2024.106317","DOIUrl":"10.1016/j.fitote.2024.106317","url":null,"abstract":"<p><strong>Background: </strong>The medicinal folk plant Tithonia diversifolia A. Gray has traditionally been used to treat hepatitis and liver cancer. However, the anti-fibrotic effect of this plant extract and its main active substances remain unclear.</p><p><strong>Objective: </strong>This study aims to elucidate the anti-fibrotic effect of T. diversifolia ethanol extract, identify the main active substances, and explore their possible molecular mechanisms.</p><p><strong>Methods: </strong>Firstly, carbon tetrachloride (CCl<sub>4</sub>) was injected intraperitoneally to induce liver fibrosis in mice to investigate the protective effect of T. diversifolia ethanol extract. Then, thirty compounds in this extract were identified through liquid chromatography-mass spectrometry (LC-MS/MS) analysis, column chromatography, and spectroscopic analysis. In addition, the anti-fibrotic effect of sesquiterpene lactone compounds were investigated on TGF-β-induced hepatic stellate cell activation.</p><p><strong>Results: </strong>The T. diversifolia ethanol extract significantly inhibits symptoms of carbon tetrachloride-induced liver fibrosis and the collagen deposition in pathological tissues by suppressing the protein expression of various pro-fibrotic factors. A comprehensive profile of thirty-one compounds was established, including nine sesquiterpenes, six phenolic acids, six fatty acids, five phenylpropanoids, and three flavonoids. Notably, one previously unreported sesquiterpene lactone, namely 1β-ethoxydiversifolin 3-O-methyl ether (1), together with twenty-nine known compounds were obatined. Sesquiterpene Tagitinin C shows significant anti-fibrotic effects on TGFβ1-induced HSC-T6 activation by inducing cell apoptosis and regulating the TGF-β1/Smad pathway.</p><p><strong>Conclusion: </strong>The above results indicate that the T. diversifolia extract can effectively alleviate liver fibrosis, with sesquiterpene lactones being a major component. In the future, the germacranolides-type of sesquiterpene lactone Tagitinin C can be developed as a precursor compound for anti-fibrotic therapy.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106317"},"PeriodicalIF":2.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142750076","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}
引用次数: 0
One new polyketide and four new sesquiterpenes derivatives from the fungicolous fungi aspergillus nidulans LZ8 of Ganoderma lingzhi. 灵芝属真菌nidulaspergillus nidulans LZ8 1个新聚酮和4个新倍半萜衍生物。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-01-01 Epub Date: 2024-12-08 DOI: 10.1016/j.fitote.2024.106339
Hong Zhang, Zhuoda Zhou, Minghua Yang, Shengyu Li, Xia Liu, Lu Jin, Qiyang Shou, Huiying Fu
{"title":"One new polyketide and four new sesquiterpenes derivatives from the fungicolous fungi aspergillus nidulans LZ8 of Ganoderma lingzhi.","authors":"Hong Zhang, Zhuoda Zhou, Minghua Yang, Shengyu Li, Xia Liu, Lu Jin, Qiyang Shou, Huiying Fu","doi":"10.1016/j.fitote.2024.106339","DOIUrl":"10.1016/j.fitote.2024.106339","url":null,"abstract":"<p><p>One new polyketide asperfuranone D (1), four new sesquiterpenes derivatives aspergillone C-F (2-5) and three known compounds (6-8) were successfully isolated from Aspergillus nidulans LZ8, a fungicolous fungi from the macrofungal Ganoderma lingzhi. The structures of these compounds were elucidated by extensive spectroscopic analyses including ultraviolet-visible spectroscopy (UV), mass spectrometry (MS), nuclear magnetic resonance (NMR), and electronic circular dichroism (ECD) calculation. In addition, the anti-inflammatory activities of the new compounds were evaluated using LPS-induced RAW 264.7 cells. The results revealed that compound 5 showed moderate nitric oxide (NO) inhibitory activity with the IC<sub>50</sub> value of 13.19 ± 1.05 μM, while the IC<sub>50</sub> value of the positive control L-NMMA was 41.88 ± 0.91 μM.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106339"},"PeriodicalIF":2.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142806519","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}
引用次数: 0
Improved production of palitantin by design of experiments and semi-synthesis of palitantin derivatives for bioactivity assessment. 通过实验设计和巴立坦衍生物的半合成改进了巴立坦的生产,并进行了生物活性评价。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-01-01 Epub Date: 2024-11-29 DOI: 10.1016/j.fitote.2024.106310
Pedro M Santucci, Caroline R de Oliveira, Afif F Monteiro, Giovana R Mendes, Marcelo R de Amorim, Gabriel H S Rosa, Lara D Sette, Rafael C Marchi, Victor M Deflon, Pedro H T Dos Santos, Gabriela G Carvalho, Marcelo Brocchi, Rafael V C Guido, Antonio G Ferreira, Kleber T de Oliveira, Roberto G S Berlinck
{"title":"Improved production of palitantin by design of experiments and semi-synthesis of palitantin derivatives for bioactivity assessment.","authors":"Pedro M Santucci, Caroline R de Oliveira, Afif F Monteiro, Giovana R Mendes, Marcelo R de Amorim, Gabriel H S Rosa, Lara D Sette, Rafael C Marchi, Victor M Deflon, Pedro H T Dos Santos, Gabriela G Carvalho, Marcelo Brocchi, Rafael V C Guido, Antonio G Ferreira, Kleber T de Oliveira, Roberto G S Berlinck","doi":"10.1016/j.fitote.2024.106310","DOIUrl":"10.1016/j.fitote.2024.106310","url":null,"abstract":"<p><p>A new method for the production and isolation of (+)-palitantin (1) is herein reported, from cultures of the fungal strain Penicillium sp. AMF1a. (+)-Palitantin was isolated in 160 mg/L yield, as an alternative procedure to obtain 1 at a larger scale. The complete spectroscopic characterization, including conformational analysis, is presented for (+)-palitantin (1) and for its derivatives 3-α-palitantol (2), 3-β-palitantol (3), (Z)-palinitrorin (4), (Z)-paliphenin (5), (Z)-palifluorin (6) and (E)-palifluorin (7). The absolute configuration of the palitantin portion was confirmed by X-ray analysis of compound 4. The (4-(trifluoromethyl)benzyl)-hydrazone derivatives (6 and 7) displayed moderate biological activities. (Z)-Palifluorin (6) exhibited moderate antiplasmodial activity, while (E)-palifluorin (7) displayed weak antibacterial activity against E. faecalis and S. aureus, while palitantin itself was inactive in the same bioassays, indicating that the semi-synthesis of nitrogenated derivatives of 1 may be of potential interest to generate bioactive palitantin derivatives.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106310"},"PeriodicalIF":2.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142767618","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}
引用次数: 0
C17-Labdane diterpenoid alkaloids bearing a rare skeleton with anti-inflammatory and anti-oxidant activities from Forsythia suspensa. 连翘中具有抗炎和抗氧化活性的稀有骨架的C17-Labdane二萜生物碱。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-01-01 Epub Date: 2024-12-10 DOI: 10.1016/j.fitote.2024.106345
Jia-Huan Liu, Yue Wang, Sheng-Jun Dai, De-Wu Zhang, Xi-Dian Yue
{"title":"C<sub>17</sub>-Labdane diterpenoid alkaloids bearing a rare skeleton with anti-inflammatory and anti-oxidant activities from Forsythia suspensa.","authors":"Jia-Huan Liu, Yue Wang, Sheng-Jun Dai, De-Wu Zhang, Xi-Dian Yue","doi":"10.1016/j.fitote.2024.106345","DOIUrl":"10.1016/j.fitote.2024.106345","url":null,"abstract":"<p><p>Two undescribed C<sub>17</sub>-Labdane diterpenoid alkaloids, named forsylinfenines A and B (1-2), attributable to a rare 4,4,10,13-tetramethyl-1(2),3(4),5(10),6(7)-octahydrobenzo[f]quinolin skeleton, along with three known β-carboline-type alkaloids (3-5), were isolated. The chemical structures including absolute configurations of two undescribed compounds were established by means of integrated spectroscopic techniques and electronic circular dichroism (ECD) calculations. In addition, a plausible biosynthetic pathway for the formation of compounds 1 and 2 was proposed. In vitro, five alkaloids (1-5), especially two undescribed alkaloids with rare skeleton (1-2), exhibited significant anti-inflammatory activities due to inhibiting the release of TNF-α, IL-6, and IL-1β, as well as effective anti-oxidant activities owing to preventing the production of ROS in the LPS-induced RAW264.7 cells.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106345"},"PeriodicalIF":2.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142817523","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}
引用次数: 0
Multi-platform comparison and phytochemical insights of Tripleurospermum taxa from Greece. 希腊三种植物分类群的多平台比较及其植物化学意义。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-01-01 Epub Date: 2024-12-10 DOI: 10.1016/j.fitote.2024.106340
Eleftherios Kalpoutzakis, Christodoulos Anagnostou, Sofia Mitakou, Eleni V Mikropoulou, Maria Halabalaki
{"title":"Multi-platform comparison and phytochemical insights of Tripleurospermum taxa from Greece.","authors":"Eleftherios Kalpoutzakis, Christodoulos Anagnostou, Sofia Mitakou, Eleni V Mikropoulou, Maria Halabalaki","doi":"10.1016/j.fitote.2024.106340","DOIUrl":"10.1016/j.fitote.2024.106340","url":null,"abstract":"<p><p>The Tripleurospermum (L.) Sch.Bip, (Asteraceae) genus, comprises 30 to 40 species widely spread in the northern hemisphere, and across the Mediterranean region. Out of the seven taxa encountered in Greece, four can only be found in specific areas, with limited spread throughout the country. The current work describes the phytochemical investigation, using modern analytical techniques, of the differences between the aerial parts of T. tempskyanum and T. rosellum collected from two floristic regions of Greece (Lesvos isl. and Mt. Parnon) and the common chamomile (Matricaria recutita). GC-MS was first applied for the analysis of the essential oils and dichloromethane extracts, significantly differentiating M. recutita from the Tripleurospermum taxa. Afterwards, a fractionation of T. tempskyanum 's non-polar and polar extracts afforded their major compounds, thus assisting to the unambiguous distinction of different isomers of matricaria lactone, as well as the first-time isolation of demethyl brevisnosideyne. Finally, the polar extracts were analyzed by means of UPLC-Orbitrap-HRMS/MS, revealing similarities among the species, with profiles dominated by cinnamic and flavonoid derivatives and fatty acids, with quantitative differences being observed for specific groups of compounds. Overall, the current study provides novel insight on the phytochemical differentiation between the studied genera and species.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106340"},"PeriodicalIF":2.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142817633","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}
引用次数: 0
Highly modified lanostane triterpenoids from natural fruiting bodies of Ganoderma cf. hochiminhense. 来自天然灵芝子实体的高修饰羊角甾烷三萜类化合物。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-01-01 Epub Date: 2024-12-12 DOI: 10.1016/j.fitote.2024.106336
Somporn Palasarn, Wilunda Choowong, Natthawut Wiriyathanawudhiwong, Rattaket Choeyklin, Masahiko Isaka
{"title":"Highly modified lanostane triterpenoids from natural fruiting bodies of Ganoderma cf. hochiminhense.","authors":"Somporn Palasarn, Wilunda Choowong, Natthawut Wiriyathanawudhiwong, Rattaket Choeyklin, Masahiko Isaka","doi":"10.1016/j.fitote.2024.106336","DOIUrl":"10.1016/j.fitote.2024.106336","url":null,"abstract":"<p><p>Eight previously undescribed highly modified lanostane triterpenoids, ganoboninketals G-K (1-5), ganoboninone I (6), ganoderlactone G (7), and (24E)-3,11-dioxolanosta-8,24-dien-26-oic acid (8), were isolated from natural fruiting bodies of Ganoderma cf. hochiminhense. The structures were elucidated on the basis of NMR spectroscopic and mass spectrometry data. Ganoboninketals G (1), H (2), and J (4) exhibited antimalarial activity against Plasmodium falciparum K1 (multidrug-resistant strain) with IC<sub>50</sub> values of 17, 16, and 5.1 μM, respectively.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106336"},"PeriodicalIF":2.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142823970","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}
引用次数: 0
Terpenoids mediated cell apoptotsis in cervical cancer: Mechanisms, advances and prospects. 萜类介导的宫颈癌细胞凋亡:机制、进展与展望。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-01-01 Epub Date: 2024-12-02 DOI: 10.1016/j.fitote.2024.106323
Peng Zhang, Hong Liu, Yuan Yu, Shiyang Peng, Anqi Zeng, Linjiang Song
{"title":"Terpenoids mediated cell apoptotsis in cervical cancer: Mechanisms, advances and prospects.","authors":"Peng Zhang, Hong Liu, Yuan Yu, Shiyang Peng, Anqi Zeng, Linjiang Song","doi":"10.1016/j.fitote.2024.106323","DOIUrl":"10.1016/j.fitote.2024.106323","url":null,"abstract":"<p><strong>Background: </strong>Cervical cancer remains one of the most common malignancies among women globally, causing hundreds of thousands of deaths annually. Despite widespread vaccination and screening programs, the incidence of cervical cancer remains high in developing countries.</p><p><strong>Objective: </strong>This review aims to systematically summarize the existing terpenoids effective in preventing cervical cancer, elucidate their potential mechanisms in the prophylaxis and treatment of cervical cancer, and assess the limitations of current studies.</p><p><strong>Results: </strong>Studies have shown that terpenoids can decrease the incidence of cervical cancer and promote apoptosis of cancer cells through various signaling pathways, including the PI3K/AKT pathway, the endoplasmic reticulum stress (ERS) pathway, and the mitochondria- and caspase-dependent cell death pathways. Furthermore, some terpenoids have been found to enhance the sensitivity to chemotherapy drugs, thus improving patients' quality of life.</p><p><strong>Conclusion: </strong>Terpenoids play a significant role in inhibiting the progression of cervical cancer. However, due to their diversity and complex mechanisms of action, further research is necessary to investigate their specific targets and bioactivities to advance their clinical trials and applications.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106323"},"PeriodicalIF":2.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142779573","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}
引用次数: 0
New flavonoid glycosides from the stems and leaves of Astragalus membranaceus. 从黄芪茎叶中提取新的黄酮类苷。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-01-01 Epub Date: 2024-12-03 DOI: 10.1016/j.fitote.2024.106321
Jin-Yan Tan, Jia-Xin Zhao, Yun Zang, Pei Li, Si-Qi Yang, Xiao-Mao Li, Ying-Li Wang, Yan-Gang Cheng
{"title":"New flavonoid glycosides from the stems and leaves of Astragalus membranaceus.","authors":"Jin-Yan Tan, Jia-Xin Zhao, Yun Zang, Pei Li, Si-Qi Yang, Xiao-Mao Li, Ying-Li Wang, Yan-Gang Cheng","doi":"10.1016/j.fitote.2024.106321","DOIUrl":"10.1016/j.fitote.2024.106321","url":null,"abstract":"<p><p>Astragalus membranaceus, a well-known traditional medicine and food, has been extensively studied for its roots. However, comparatively little attention has been paid to its stems and leaves. In this study, we successfully isolated and identified three new flavonoid glycosides (1-3), and eight known analogues (4-11) from the stems and leaves of A. membranaceus. Notably, compound 10 exhibited significant anti-inflammatory activities in LPS-induced BV2 cells, with IC<sub>50</sub> value of 1.11 ± 0.04 μM. These findings highlight flavonoids as the key bioactive components present in the stems and leaves of A. membranaceus.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106321"},"PeriodicalIF":2.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142784924","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}
引用次数: 0
Identification of bioactive compounds in Brassica oleracea var. capitata L. with enzyme-inhibitory activity against postprandial hyperglycemia. 鉴定 Brassica oleracea var. capitata L. 中对餐后高血糖具有酶抑制活性的生物活性化合物。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-01-01 Epub Date: 2024-12-10 DOI: 10.1016/j.fitote.2024.106343
Jonatan Jafet Uuh Narvaez, Guillermo Emilio Moguel Ojeda, José A Guerrero-Analco, Juan L Monribot-Villanueva, Abraham Vidal-Limon, Guiomar Melgar Lalanne, Rafael Rojas Herrera, Maira Rubi Segura Campos
{"title":"Identification of bioactive compounds in Brassica oleracea var. capitata L. with enzyme-inhibitory activity against postprandial hyperglycemia.","authors":"Jonatan Jafet Uuh Narvaez, Guillermo Emilio Moguel Ojeda, José A Guerrero-Analco, Juan L Monribot-Villanueva, Abraham Vidal-Limon, Guiomar Melgar Lalanne, Rafael Rojas Herrera, Maira Rubi Segura Campos","doi":"10.1016/j.fitote.2024.106343","DOIUrl":"10.1016/j.fitote.2024.106343","url":null,"abstract":"<p><p>Postprandial hyperglycemia is a hallmark of diabetes, and inhibition of key carbohydrate digestion enzymes such as α-amylase (α-AMY) and α-glucosidase (α-GLU) is an effective therapeutic target. A potential unexplored source of inhibitory compounds of these enzymes is Brassica oleracea var. capitata L (BOCE). This study explored the in vitro inhibition mechanism of BOCE and studied in silico the interaction of its compounds identified and quantified by UPLC-QTOF-MS on α-AMY and α-GLU. BOCE demonstrated IC<sub>50</sub> values of 3.08 mg/mL for α-AMY and 22.63 mg/mL for α-GLU, indicating competitive and mixed-type inhibitions, respectively. Untargeted metabolomics identified 21 compounds, primarily phenolic acids such as t-cinnamic, sinapic, and caffeoylquinic acid. In the targeted analysis, 11 compounds were quantified, mainly phenolic acids. The most impactful biosynthetic pathways identified were phenylpropanoids and brassinosteroids. In silico analysis revealed that for α-AMY and α-GLU, castasterone and 26-hydroxybrassinolide displayed the lowest binding free energies with specific hydrogen bond patterns to catalytic residues in the binding site, respectively. B. oleracea is a promising source of compounds with the ability to modulate key enzymes related to hyperglycemia. Specifically, compounds such as castasterone and 26-hydroxybrassinolide show potential against α-AMY and α-GLU inhibition, offering a novel approach to diabetes.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106343"},"PeriodicalIF":2.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142817628","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}
引用次数: 0
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