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The mechanistic role of Poria cocos in cancer treatment: Antitumor activity and adjuvant potential in chemotherapy 茯苓在癌症治疗中的作用机制:抗肿瘤活性和化疗的辅助作用。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-01-01 Epub Date: 2025-12-04 DOI: 10.1016/j.fitote.2025.107016
Joanna Japhet Tibenda , Qian Gu , Shuai Duan , Chuang Song , Yuhua Du , Xiaofang Huang , Jianjun Zhao , Yi Nan , Ling Yuan
Poria cocos is a prominent traditional fungal medicine that has been utilized in China for over a millennium. Its major bioactive constituents include triterpenes and polysaccharides, along with other minor components such as steroids, histidine, choline, amino acids, and essential minerals, which exhibit diverse pharmacological mechanisms, including antitumor, antibacterial, immunomodulatory, anti-aging, antioxidant, anti-inflammatory, hepatoprotective, neuroprotective, and cardioprotective effects.
Globally, cancer remains a leading cause of mortality, accounting for approximately nine million deaths annually. Despite advances in current conventional therapies, complete tumor eradication remains elusive, and these treatments are often accompanied by severe adverse effects.
To comprehensively evaluate the therapeutic potential of poria cocos, publications from 2002 to 2025 were systematically reviewed from PubMed, Web of Science, ScienceDirect, and Google Scholar. This review elucidates the antitumor properties of poria cocos on various cancers, including lung, colorectal, breast, and gastric cancers. Furthermore, it highlights its adjuvant role in enhancing the efficacy of chemotherapeutic agents through multiple mechanisms, such as inhibition of cellular proliferation and metastasis, induction of apoptosis and cell cycle arrest, and modulation of immune, inflammatory, and oxidative signaling pathways.
Collectively, these findings demonstrate the promising antitumor and adjuvant potential of poria cocos in cancer therapy. Nevertheless, further investigations are required to determine optimal dosages, toxicity profiles, and clinical efficacy. Rigorous quality control, standardization, and well-designed clinical trials are essential to validate its safety and effective clinical application.
茯苓是一种著名的传统真菌药,在中国已有一千多年的历史。其主要生物活性成分包括三萜和多糖,以及其他次要成分,如类固醇、组氨酸、胆碱、氨基酸和必需矿物质,具有多种药理机制,包括抗肿瘤、抗菌、免疫调节、抗衰老、抗氧化、抗炎、肝保护、神经保护和心脏保护作用。在全球范围内,癌症仍然是导致死亡的主要原因,每年约有900万人死亡。尽管目前的常规治疗取得了进展,但完全根除肿瘤仍然是难以捉摸的,而且这些治疗往往伴随着严重的不良反应。为了全面评价茯苓的治疗潜力,系统地回顾了2002年至2025年PubMed、Web of Science、ScienceDirect和b谷歌Scholar上发表的文章。本文就茯苓对肺癌、结直肠癌、乳腺癌和胃癌等多种癌症的抗肿瘤作用作一综述。此外,它还通过多种机制,如抑制细胞增殖和转移、诱导细胞凋亡和细胞周期阻滞、调节免疫、炎症和氧化信号通路,在提高化疗药物疗效方面发挥辅助作用。总的来说,这些发现证明了茯苓在癌症治疗中的抗肿瘤和辅助治疗潜力。然而,需要进一步的研究来确定最佳剂量、毒性特征和临床疗效。严格的质量控制、标准化和精心设计的临床试验是验证其安全性和有效临床应用的必要条件。
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引用次数: 0
Phytochemical diversity, extraction techniques, and therapeutic potential of Erica species 埃里卡植物的化学多样性,提取技术和治疗潜力。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-01-01 Epub Date: 2025-12-04 DOI: 10.1016/j.fitote.2025.107011
Anfel Benmanseur , Abdelmalek Rezgui , Mustapha Tacherfiout , Widad Sobhi , Norbert M. Maier , Susanne K. Wiedmer
This review systematically examines the scientific literature on the genus Erica (heathers), with a focus on their phytochemical diversity and pharmacological potential. The objective is to critically analyze how extraction methods and species origin influence the profiles of bioactive compounds responsible for therapeutic effects. A comprehensive evaluation of phytochemical data is presented for widely studied species, including Erica arborea, Erica andevalensis, Erica australis, Erica manipuliflora, Erica cinerea, Erica verticillata, Erica carnea, Erica scoparia, Erica spiculifolia, Erica multiflora, and Erica mannii. Evidence indicates that extraction techniques and solvent polarity strongly affect the yield and diversity of secondary metabolites such as phenolic acids, flavonoids, and terpenoids, which are associated with antioxidant, anti-inflammatory, antimicrobial, diuretic, and anticancer activities. Importantly, this review highlights pronounced taxonomic and geographic sampling biases: most studies focus on European and Mediterranean Erica species, with very limited representation from Africa despite its exceptional species richness. These findings emphasize the need to optimize extraction protocols and expand research to underrepresented taxa. Overall, this synthesis underscores the therapeutic promise of Erica species and provides a foundation for future drug discovery efforts guided by phytochemical characterization and bioactivity screening.
本文系统地回顾了有关石南属植物的科学文献,重点介绍了石南属植物的化学多样性和药理潜力。目的是批判性地分析提取方法和物种来源如何影响负责治疗效果的生物活性化合物的概况。本文对研究较为广泛的植物种类,包括乔木埃里卡(Erica arborea)、美国埃里卡(Erica andevalensis)、南方埃里卡(Erica australis)、木兰花埃里卡(Erica manuliflora)、灰种埃里卡(Erica verticillata)、黄花埃里卡(Erica scoparia)、细花埃里卡(Erica spullifolia)、多花埃里卡(Erica multiflora)和曼尼埃里卡(Erica mannii)进行了植物化学数据的综合评价。有证据表明,提取技术和溶剂极性对次生代谢产物如酚酸、黄酮类化合物和萜类化合物的产量和多样性有很大影响,这些物质具有抗氧化、抗炎、抗菌、利尿和抗癌活性。重要的是,这篇综述强调了明显的分类学和地理抽样偏差:大多数研究集中在欧洲和地中海的Erica物种上,尽管非洲物种丰富,但来自非洲的代表性非常有限。这些发现强调了优化提取方案和将研究扩展到代表性不足的分类群的必要性。总的来说,该合成强调了Erica物种的治疗前景,并为未来通过植物化学表征和生物活性筛选指导的药物发现工作奠定了基础。
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引用次数: 0
Corrigendum to “Anti-diabetic compounds from the seeds of Psoralea corylifolia” [Fitoterapia 139 (2019) 104373] “补骨脂种子抗糖尿病化合物”的勘误表[Fitoterapia 139(2019) 104373]。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-01-01 Epub Date: 2025-12-15 DOI: 10.1016/j.fitote.2025.107036
Gaohui Zhu, Yanhong Luo, Xuejiao Xu, Huijiao Zhang, Min Zhu
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引用次数: 0
The Tetradium ruticarpum–Zingiber officinale Roscoe herb pair inhibits atherogenic events: A study of the synergistic effects and active ingredient combination of a two-herb formula 姜黄-金银花草本对抑制动脉粥样硬化事件:两种草本配方的协同作用和活性成分组合的研究。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-01-01 Epub Date: 2025-12-08 DOI: 10.1016/j.fitote.2025.107030
Chenglin Chi, Xiaoli Yang, Can Li, Zongchao Li, Shufang Yang, Yuan Du, Weizhen Huang, Rongxia Liu
The Tetradium ruticarpum (E)–Zingiber officinale Roscoe (Z) herb pair is a well-known herbal formulation with multiple beneficial cardiovascular pharmacological activities. Therefore, E and Z are potentially natural products for Atherosclerosis (AS). However, it is not clear whether E and Z work synergistically in the treatment of AS and which of their components is responsible. This study was to determine the synergistic effect of E and Z in the treatment of AS, to identify the active ingredient combination (AIC) that exerts the action of the original formula and to determine its molecular mechanism. First, the combined effects of E and Z were assessed in an ApoE−/− mouse model and then confirmed in vascular smooth muscle cells (VSMCs) by the combination index (CI). In addition, the AIC of E-Z was evaluated by cascade analysis and its efficacy was confirmed in vitro and in vivo. The results showed that both E, Z and E-Z had anti-AS effects in ApoE−/− mice, with E-Z having the most significant effect. Moreover, the CI method demonstrated that E, Z could synergistically inhibit the proliferation of VSMCs. In addition, the AICs obtained by the cascade analysis strategy effectively inhibited VSMCs proliferation in vitro and significantly reduced the formation of neoplastic endothelium in mice in vivo. This inhibitory effect was associated with the reduction of ROS levels and activation of the Nrf2/HO-1 signaling pathway in VSMCs. This study provides an effective method for characterizing herbal combinations, exploring their active ingredients, and promoting efficacy-based herbal quality control.
紫金四合物(Tetradium ruticarpum, E)-黄姜(zingiber officinale Roscoe, Z)是一种众所周知的具有多种有益心血管药理活性的草药配方。因此,E和Z是动脉粥样硬化(AS)的潜在天然产物。然而,尚不清楚E和Z是否在治疗AS中协同作用,以及它们的哪个成分负责。本研究旨在确定E和Z在治疗AS中的协同作用,确定发挥原方作用的有效成分组合(AIC),并确定其分子机制。首先,在ApoE-/-小鼠模型中评估E和Z的联合作用,然后通过联合指数(CI)在血管平滑肌细胞(VSMCs)中证实。此外,通过级联分析评价了E-Z的AIC,并证实了其体外和体内的有效性。结果表明,E、Z和E-Z对ApoE-/-小鼠均有抗as作用,其中E-Z的作用最为显著。此外,CI法显示E、Z能协同抑制VSMCs的增殖。此外,通过级联分析策略获得的aic在体外有效抑制了VSMCs的增殖,并在体内显著减少了小鼠肿瘤内皮的形成。这种抑制作用与VSMCs中ROS水平的降低和Nrf2/HO-1信号通路的激活有关。本研究为中药复方的表征、有效成分的探索以及基于疗效的中药质量控制提供了一种有效的方法。
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引用次数: 0
Bioprospecting and exploration of the chemical profile of Lasiodiplodia sp. extracts: Evaluation of specialized metabolites by similarity calculations, and dereplication with differential 1H NMR Lasiodiplodia sp.提取物化学谱的生物勘探与探索:利用相似性计算评价特化代谢物,并用差异1HNMR进行重复。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-01-01 Epub Date: 2025-12-08 DOI: 10.1016/j.fitote.2025.107031
Lucas Silva Tironi , Johan Mateo Rios Marin , Omar Cabezas Gómez , Antonio Gilberto Ferreira , Jan Schripsema , Jaine Honorata Hortolan Luiz
Endophytic fungi are well known for producing a wide variety of specialized metabolites, often characterized by complex and diverse chemical structures. In this study, the differential 1H NMR technique was used as an innovative tool for dereplication and for supporting compound identification in complex mixtures, complemented by similarity calculations developed to evaluate the similarity of the chemical profiles of the extracts obtained over consecutive cultivation days of Lasiodiplodia sp. One-dimensional (1D) and two-dimensional (2D) NMR analyses of the POLd-14 extract and MLd-1 to MLd-3 subfractions led to the identification of known compounds: 3-carboxy-2-methylene-4-heptanolide (1) and decumbic acid (2) in POLd-14; indole-3-carboxylic acid (3) in MLd-1 and MLd-3; 4-hydroxybenzoic acid (4) and 4-hydroxymellein (5) in MLd-1; and 4-hydroxyphenylacetamide (6) in MLd-2. Differential 1H NMR enabled the unequivocal identification of compounds (1) and (2). These results contribute to bioprospecting and to a better understanding of the metabolite diversity of Lasiodiplodia sp. under varying culture conditions, including diferences in carbon and nitrogen sources, cultivation periods, and extraction methods. The study also underscore the potential of Lasiodiplodia sp. endophyte as an alternative source of bioactive metabolites with pharmacological relevance, which can be cultivated under different conditions guiding the production of different specialized metabolites.
内生真菌以产生各种各样的特殊代谢物而闻名,这些代谢物通常具有复杂多样的化学结构。在这项研究中,差异1HNMR技术被用作一种创新的工具,用于反复制和支持复杂混合物中的化合物鉴定。通过相似性计算来评估在连续培养几天内获得的Lasiodiplodia sp.提取物的化学特征的相似性。对POLd-14提取物和MLd-1与MLd-3亚组分进行一维(1D)和二维(2D) NMR分析,鉴定出POLd-14中的已知化合物:3-羧基-2-亚甲基-4-七烷内酯(1)和癸二酸(2);MLd-1和MLd-3中的吲哚-3-羧酸(3);MLd-1中的4-羟基苯甲酸(4)和4-羟基mellein (5);和4-羟基苯乙酰胺(6)。差异1HNMR能够明确地识别化合物(1)和(2)。这些结果有助于更好地了解不同培养条件下Lasiodiplodia sp.代谢物的多样性,包括碳氮源、培养周期和提取方法的差异。该研究还强调了Lasiodiplodia sp.内生菌作为具有药理意义的生物活性代谢物的替代来源的潜力,它可以在不同的条件下培养,指导不同专门代谢物的产生。
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引用次数: 0
The multifaceted properties of manna in skin wound healing include the enhancement of cell motility and differentiation, and antioxidant and anti-inflammatory actions 甘露在皮肤伤口愈合中的多方面特性包括增强细胞运动和分化,抗氧化和抗炎作用
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-01-01 Epub Date: 2025-11-14 DOI: 10.1016/j.fitote.2025.106994
Raffaella Belvedere , Nunzia Novizio , Mariangela Palazzo , Mussa Makran , Antonio Cilla , Alessandro Attanzio , Antonello Petrella
Manna is a natural substance exuded from the trunk and branches of certain Fraxinus species, primarily from Fraxinus ornus L. and Fraxinus angustifolia Vahl. The manna here used was predominantly obtained from F. angustifolia. It has gained attention for its potential pharmaceutical applications mainly for its antioxidant and anti-inflammatory effects. This in vitro study investigates the talented properties of manna in promoting skin regeneration. We used HaCaT, BJ, HUVEC and THP-1 cells to evaluate manna's effects on cell activation in terms of motility, differentiation with oxidative and inflammatory responses. In detail, we demonstrated that manna enhanced the migration and invasion of keratinocytes, fibroblasts, and endothelial cells, as key players in the wound healing process. Manna also exerted significant antioxidant activity on all these cells, by protecting them from hydrogen peroxide stress. Additionally, it induced angiogenesis by activating endothelial cells. The beneficial effects of manna are further promoted by favoring the differentiation of the analyzed cells through the regulation of levels of protein markers as cytokeratin 10 and involucrin on keratinocytes, vinculin and fibroblasts activated protein-1α on fibroblasts and CD31 on endothelial cells. It was also revealed that manna retained anti-inflammatory effects, by reducing the polarization of human macrophages in M1 pro-inflammatory phenotype and inhibiting the phosphorylation of NF-kB after stimulation with lipopolysaccharide/interferon-γ, thus further supporting the healing process. These findings provide valuable insights into the complex role of manna in the different stages intervening in the skin wound healing, highlighting its potential as a therapeutic agent in regenerative medicine.
甘露是一种天然物质,从某些曲霉属植物的树干和分支中渗出,主要来自于曲霉(Fraxinus ornus L.)和曲霉(Fraxinus angustifolia Vahl.)。这里使用的甘露主要是从鹅毛豆中获得的。由于其抗氧化和抗炎作用,其潜在的制药应用受到了人们的关注。本体外实验研究甘露促进皮肤再生的特性。我们使用HaCaT、BJ、HUVEC和THP-1细胞来评估甘薯在运动、氧化和炎症反应分化方面对细胞活化的影响。详细地说,我们证明甘露可以增强角化细胞、成纤维细胞和内皮细胞的迁移和侵袭,这些细胞是伤口愈合过程中的关键角色。甘露还通过保护这些细胞免受过氧化氢胁迫,对所有这些细胞发挥了显著的抗氧化活性。此外,它通过激活内皮细胞诱导血管生成。甘露通过调节角质形成细胞的细胞角蛋白10和天青蛋白、成纤维细胞的血管蛋白和成纤维细胞活化蛋白-1α以及内皮细胞的CD31等蛋白标记物水平,进一步促进了所分析细胞的分化。研究还发现,甘露通过降低人巨噬细胞M1促炎表型的极化,抑制脂多糖/干扰素-γ刺激后NF-kB的磷酸化,从而进一步支持愈合过程,从而保留抗炎作用。这些发现为甘露在不同阶段干预皮肤伤口愈合的复杂作用提供了有价值的见解,突出了其作为再生医学治疗剂的潜力。
{"title":"The multifaceted properties of manna in skin wound healing include the enhancement of cell motility and differentiation, and antioxidant and anti-inflammatory actions","authors":"Raffaella Belvedere ,&nbsp;Nunzia Novizio ,&nbsp;Mariangela Palazzo ,&nbsp;Mussa Makran ,&nbsp;Antonio Cilla ,&nbsp;Alessandro Attanzio ,&nbsp;Antonello Petrella","doi":"10.1016/j.fitote.2025.106994","DOIUrl":"10.1016/j.fitote.2025.106994","url":null,"abstract":"<div><div>Manna is a natural substance exuded from the trunk and branches of certain <em>Fraxinus</em> species, primarily from <em>Fraxinus ornus</em> L. and <em>Fraxinus angustifolia</em> Vahl. The manna here used was predominantly obtained from <em>F. angustifolia</em>. It has gained attention for its potential pharmaceutical applications mainly for its antioxidant and anti-inflammatory effects. This in vitro study investigates the talented properties of manna in promoting skin regeneration. We used HaCaT, BJ, HUVEC and THP-1 cells to evaluate manna's effects on cell activation in terms of motility, differentiation with oxidative and inflammatory responses. In detail, we demonstrated that manna enhanced the migration and invasion of keratinocytes, fibroblasts, and endothelial cells, as key players in the wound healing process. Manna also exerted significant antioxidant activity on all these cells, by protecting them from hydrogen peroxide stress. Additionally, it induced angiogenesis by activating endothelial cells. The beneficial effects of manna are further promoted by favoring the differentiation of the analyzed cells through the regulation of levels of protein markers as cytokeratin 10 and involucrin on keratinocytes, vinculin and fibroblasts activated protein-1α on fibroblasts and CD31 on endothelial cells. It was also revealed that manna retained anti-inflammatory effects, by reducing the polarization of human macrophages in M1 pro-inflammatory phenotype and inhibiting the phosphorylation of NF-kB after stimulation with lipopolysaccharide/interferon-γ, thus further supporting the healing process. These findings provide valuable insights into the complex role of manna in the different stages intervening in the skin wound healing, highlighting its potential as a therapeutic agent in regenerative medicine.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"188 ","pages":"Article 106994"},"PeriodicalIF":2.6,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145527096","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
Antifungal activity of Eugenia dysenterica (Mart.) DC. (Myrtaceae) alone or in combination with antifungal agents against Candida (Candidozyma) auris 赤霉素的抗真菌活性研究直流。(桃金娘科)单独或与抗真菌剂联合抗念珠菌(念珠菌)耳。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-01-01 Epub Date: 2025-11-27 DOI: 10.1016/j.fitote.2025.107004
Gabriel Henrique Rodrigues da Cruz , Fabíola Lucini , Gabriel Vichoski Santos , Rafael Cardoso Rial , Claudia Andrea Lima Cardoso , Simone Simionatto , Luana Rossato
Candida (Candidozyma) auris is a multidrug-resistant fungal pathogen associated with high mortality and limited treatment options. Eugenia dysenterica, a medicinal plant from the Brazilian Cerrado traditionally used for gastrointestinal ailments, is rich in bioactive phenolics with potential therapeutic applications. To evaluate the chemical composition, antifungal activity, mechanisms of action, and in vivo effects of ethanolic leaf extract of E. dysenterica (Ed-EE) against C. auris. Ed-EE was analyzed for phenolic and flavonoid content. Its antifungal activity and interactions with amphotericin B (AmB) and fluconazole (FLC) were tested using microdilution and checkerboard assays. Mechanisms of action were explored through membrane integrity and efflux pump inhibition assays. Hemolysis assay was performed to assess hemocompatibility. In vivo toxicity and efficacy were evaluated using Tenebrio molitor larvae. Ed-EE exhibited fungistatic activity against C. auris, with a MIC of 32 μg/mL. When combined with AmB, a synergistic effect was observed (FICI = 0.5), reducing the MICs to 8 μg/mL for Ed-EE and 0.5 μg/mL for AmB. Mechanistic assays indicated moderate membrane disruption and efflux pump inhibition. Hemolysis and in vivo assays using T. molitor larvae showed survival rates above 80 %, confirming low toxicity. However, Ed-EE did not significantly inhibit biofilm formation at tested concentrations. Ed-EE exhibits promising antifungal activity against C. auris, particularly in synergy with AmB, and demonstrates a favorable safety profile as potential adjuvant therapy for resistant fungal infections.
耳念珠菌是一种多重耐药真菌病原体,具有高死亡率和有限的治疗选择。Eugenia dysenterica是巴西塞拉多地区的一种药用植物,传统上用于治疗胃肠道疾病,富含生物活性酚类物质,具有潜在的治疗应用。目的:探讨E. dysenterica乙醇叶提取物(Ed-EE)的化学成分、抗真菌活性、作用机制及对金黄色葡萄球菌的体内抑制作用。分析Ed-EE的酚类和类黄酮含量。采用微量稀释法和棋盘法检测其抗真菌活性及与两性霉素B (AmB)和氟康唑(FLC)的相互作用。通过膜完整性和外排泵抑制实验探讨其作用机制。采用溶血试验评价血液相容性。采用黄粉甲幼虫进行体内毒性和药效评价。Ed-EE对金黄色葡萄球菌具有抑菌活性,MIC为32 μg/mL。当与AmB联用时,观察到协同效应(FICI = 0.5),Ed-EE的mic降至8 μg/mL, AmB的mic降至0.5 μg/mL。机制分析表明中度膜破坏和外排泵抑制。溶血和体内实验表明,其存活率在80% %以上,毒性较低。然而,Ed-EE在测试浓度下并没有显著抑制生物膜的形成。Ed-EE对金黄色葡萄球菌具有良好的抗真菌活性,特别是与AmB协同作用,并且作为耐药真菌感染的潜在辅助治疗具有良好的安全性。
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引用次数: 0
Unraveling the active ingredients and molecular mechanisms of Qinghua Changyan granule against irritable bowel syndrome with diarrhea: Effects on gut microbiota and glutamine transport via an integrative approach combining UHPLC-MS/MS and experimental verification 清肠炎颗粒抗肠易激综合征伴腹泻的有效成分及分子机制研究:UHPLC-MS/MS结合实验验证对肠道菌群及谷氨酰胺转运的影响
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-01-01 Epub Date: 2025-10-30 DOI: 10.1016/j.fitote.2025.106960
Jiayu Yang , Yuchen Wang , Shirong Wang , Zikun Liu , Xiao Chen , Rong Jia , Jie Wang , Feixia Wang , Qin Yang , Li Tang , Weifeng Miao
Irritable bowel syndrome with diarrhea (IBS-D) is a prevalent functional gut disorder, with conventional treatments limited by incomplete symptom relief and side effects. Qinghua Changyan Granules (QHCYG), a traditional Chinese medicine, has clinical efficacy in treating IBS-D, though its molecular mechanisms are unclear. This study aimed to elucidate these mechanisms. Key components of QHCYG were identified via UHPLC-MS/MS and network pharmacology, with quercetin, kaempferol, luteolin, naringenin, and nobiletin confirmed as major active components. Pharmacodynamic results showed QHCYG significantly ameliorated IBS-D-related symptoms, including reduced fecal water content, diarrhea frequency, Bristol stool scale scores, and visceral hypersensitivity. Furthermore, QHCYG restored gut microbial diversity, increased the abundance of beneficial taxa (Akkermansia, Bifidobacterium) and decreased Allobaculum proportion; it also upregulated the expression of key intestinal barrier proteins, including zonula occludens-1 (ZO-1), epithelial cadherin (E-cadherin), catenin beta-1 (β-catenin), Claudin-1. Molecular docking indicated QHCYG's active components could bind to alanine-serine-cysteine-preferring transporter 2 (ASCT2), and QHCYG further elevated intestinal glutamine concentrations and ASCT2 expression. Notably, depletion of gut microbiota by antibiotics abolished all these therapeutic effects, confirming a microbiota-dependent mechanism. In conclusion, QHCYG alleviates IBS-D through restoring gut microbiota, enhancing intestinal barrier function, and promoting ASCT2-mediated glutamine transport, revealing a “Microbiota-Glutamine axis-Intestinal barrier” multi-target regulatory mechanism.
肠易激综合征伴腹泻(IBS-D)是一种常见的功能性肠道疾病,常规治疗受症状不完全缓解和副作用的限制。中药清花肠炎颗粒(QHCYG)治疗IBS-D具有临床疗效,但其分子机制尚不清楚。本研究旨在阐明这些机制。通过UHPLC-MS/MS和网络药理学对其关键成分进行鉴定,确定槲皮素、山奈酚、木犀草素、柚皮素、白皮草素为主要有效成分。药理学结果显示,QHCYG显著改善ibs - d相关症状,包括减少粪便含水量、腹泻频率、布里斯托大便评分和内脏过敏。QHCYG恢复了肠道微生物多样性,增加了有益类群(Akkermansia、Bifidobacterium)的丰度,降低了异源菌(Allobaculum)的比例;它还上调了关键肠屏障蛋白的表达,包括闭塞带-1 (ZO-1)、上皮钙粘蛋白(E-cadherin)、连环蛋白β- 1 (β-catenin)、Claudin-1。分子对接表明,QHCYG活性成分可结合丙氨酸-丝氨酸-半胱氨酸偏好转运蛋白2 (ASCT2), QHCYG进一步提高肠道谷氨酰胺浓度和ASCT2表达。值得注意的是,抗生素消耗肠道微生物群消除了所有这些治疗效果,证实了微生物群依赖机制。综上所述,QHCYG通过恢复肠道菌群、增强肠道屏障功能、促进asct2介导的谷氨酰胺转运来缓解IBS-D,揭示了“微生物-谷氨酰胺轴-肠道屏障”的多靶点调控机制。
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引用次数: 0
Toonasonoids A-K, limonoids from Toona ciliata M. Roem, attenuate inflammatory response through mediating the PI3K/AKT/NF-κB pathway 香椿类A-K,香椿纤毛中的柠檬素,通过介导PI3K/AKT/NF-κB通路减轻炎症反应。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-01-01 Epub Date: 2025-11-01 DOI: 10.1016/j.fitote.2025.106962
Kang-Hong Zhao , Xu-Tong Fang , Jia-Le Deng , Hui-Lan Yue , Qiang-Qiang Shi
Eleven previously undescribed limonoids, toonasonoids A-K (1−11), and a known semi-synthetic analogue (12) with three basic carbon skeletons, were isolated from the twigs of Toona ciliata M. Roem. Among them, compounds 1–3 possessed a six-membered α,β-unsaturated ketone moiety in ring A, 4–9 characterized with a seven-membered α,β-unsaturated lactone A-ring, and 10–11 featured ring B-seco and formed a B tetrahydrofuran ring. The relative structures of the undescribed compounds were established via comprehensive spectroscopic analyses and NMR calculation united with DP4+ probability analysis, and their absolute configurations were assigned by ECD calculations. The cytotoxicity, anti-inflammatory, and the action mechanisms of these isolates on the PI3K/AKT/NF-κB signaling pathway were also evaluated. The results demonstrated that compounds 1, 3, 8, and 9 effectively reduced nitric oxide (NO) release with IC50 values ranging from 4.41 to 9.84 μM. Notably, compounds 1 and 9 could inhibit the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase 2 (COX-2), and block NF-κB (p65) nuclear translocation by triggering the PI3K/AKT pathway, indicating their considerable anti-inflammatory effects.
从香椿的细枝中分离出了11种先前未被描述过的柠檬素,香椿类a - k(1-11)和一种已知的半合成类似物(12),它们具有三个基本的碳骨架。其中化合物1-3在a环上具有6元α β-不饱和酮,4-9在a环上具有7元α β-不饱和内酯,10-11在B-二环上具有B'四氢呋喃环。通过综合波谱分析和核磁共振结合DP4+概率分析确定了化合物的相对结构,并通过ECD计算确定了化合物的绝对构型。我们还评估了这些分离株的细胞毒性、抗炎作用以及对PI3K/AKT/NF-κB信号通路的作用机制。结果表明,化合物1、3、8和9能有效降低NO的释放,IC50值在4.41 ~ 9.84 μM之间。值得注意的是,化合物1和9可以抑制诱导型一氧化氮合酶(iNOS)和环氧合酶2 (COX-2)的表达,并通过触发PI3K/AKT通路阻断NF-κB (p65)核易位,表明其具有相当的抗炎作用。
{"title":"Toonasonoids A-K, limonoids from Toona ciliata M. Roem, attenuate inflammatory response through mediating the PI3K/AKT/NF-κB pathway","authors":"Kang-Hong Zhao ,&nbsp;Xu-Tong Fang ,&nbsp;Jia-Le Deng ,&nbsp;Hui-Lan Yue ,&nbsp;Qiang-Qiang Shi","doi":"10.1016/j.fitote.2025.106962","DOIUrl":"10.1016/j.fitote.2025.106962","url":null,"abstract":"<div><div>Eleven previously undescribed limonoids, toonasonoids A-K (<strong>1−11</strong>), and a known semi-synthetic analogue (<strong>12</strong>) with three basic carbon skeletons, were isolated from the twigs of <em>Toona ciliata</em> M. Roem. Among them, compounds <strong>1–3</strong> possessed a six-membered <em>α,β</em>-unsaturated ketone moiety in ring A, <strong>4–9</strong> characterized with a seven-membered <em>α,β</em>-unsaturated lactone A-ring, and <strong>10–11</strong> featured ring B-<em>seco</em> and formed a B<em>′</em> tetrahydrofuran ring. The relative structures of the undescribed compounds were established via comprehensive spectroscopic analyses and NMR calculation united with DP4+ probability analysis, and their absolute configurations were assigned by ECD calculations. The cytotoxicity, anti-inflammatory, and the action mechanisms of these isolates on the PI3K/AKT/NF-κB signaling pathway were also evaluated. The results demonstrated that compounds <strong>1</strong>, <strong>3</strong>, <strong>8</strong>, and <strong>9</strong> effectively reduced nitric oxide (NO) release with IC<sub>50</sub> values ranging from 4.41 to 9.84 μM. Notably, compounds <strong>1</strong> and <strong>9</strong> could inhibit the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase 2 (COX-2), and block NF-κB (p65) nuclear translocation by triggering the PI3K/AKT pathway, indicating their considerable anti-inflammatory effects.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"188 ","pages":"Article 106962"},"PeriodicalIF":2.6,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145437871","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
In vitro anti-diabetic activities of phytochemicals isolated from Cornus officinalis fruits 山茱萸果实植物化学物质体外抗糖尿病活性研究。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-01-01 Epub Date: 2025-11-10 DOI: 10.1016/j.fitote.2025.106984
Zhi-you Hao , Xiao-lan Wang , Meng Yang , Shi-qi Zhou , Chao-yuan Xiao , Jun-yang Zhang , Shuang-shuang Xie , Meng Li , Yan-gang Cao , Yan-jun Sun , Xiao-ke Zheng , Wei-sheng Feng
Four previously undescribed compounds, including two dihydroisocoumarin glycosides (1 and 2), a truxillic acid derivative (4), and a cadinane-type sesquiterpene (5), were isolated from the fruits of Cornus officinalis Sieb. et Zucc., along with seven known ones (3, 611). Their chemical structures were determined by extensive spectroscopic methods and computational analyses. All isolated compounds were evaluated for the effects on glucose consumption in insulin-resistant (IR) HepG2 cells. The compounds exhibited no significant cytotoxicity at 10.0 μM in the CCK-8 assay. Compounds 2, 3, and 8 significantly increased glucose consumption (P < 0.05) at 5.0 and 10.0 μM. The 2-NBDG labeling indicated that compounds 2 and 8 significantly increased glucose uptake at 10 μM. Moreover, compounds 2 and 8 also significantly increased insulin receptor (INSR) expression, indicating their potential to upregulate the INSR in the cytomembrane and enhance glucose uptake.
从山茱萸(Cornus officinalis Sieb)的果实中分离出四种先前未描述的化合物,包括两种二氢异香豆素苷(1和2),一种松木酸衍生物(4)和一种cadinine型倍半萜(5)。调查。,以及七个已知的(3,6 -11)。通过广泛的光谱方法和计算分析确定了它们的化学结构。所有分离的化合物都被评估对胰岛素抵抗(IR) HepG2细胞葡萄糖消耗的影响。CCK-8实验显示,在10.0 μM下,化合物没有明显的细胞毒性。化合物2、3和8显著增加葡萄糖消耗(P
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Fitoterapia
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