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Chemical Diversity and Biological Activities of the Artemisia L. Genus Beyond Antimalarial Effects. 除抗疟作用外,青蒿属植物的化学多样性和生物活性。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-02-08 DOI: 10.1055/a-2805-3483
Olga Karoutzou, Leandros Alexios Skaltsounis

The genus Artemisia L. constitutes one of the largest and most widely distributed groups within the Asteraceae family, renowned for its pharmacological significance. Used in traditional medicine for over two millennia, Artemisia species have been employed to treat a broad spectrum of ailments, with modern pharmacological studies increasingly validating these traditional uses. Interest in the genus surged following the groundbreaking discovery of the antimalarial sesquiterpene lactone artemisinin from Artemisia annua L. Beyond antimalarial activity, Artemisia species exhibit diverse pharmacological effects including anti-inflammatory, antiproliferative, cytotoxic, antimicrobial and antiviral properties, largerly attributed to secondary metabolites such as sesquiterpene lactones, furofuran lignans, polyacetylenes and methylated flavonoids. This present study covers the bioactivities of extracts, essential oils and isolated compounds from Artemisia genus reported between 1998 and 2025. Representative compounds from the most characteristic classes of Artemisia secondary metabolites are linked to biological activities, incorporating in vitro and in vivo studies, pharmacokinetics, clinical data and toxicity profiles, while for each compound species-specific origin is reported.

青蒿属是菊科植物中最大和分布最广泛的一种,以其药理意义而闻名。在两千多年的传统医学中,青蒿被用来治疗各种各样的疾病,现代药理学研究越来越多地证实了这些传统用途。在从青蒿中突破性地发现抗疟倍半萜内酯青蒿素之后,人们对该属的兴趣激增。除了抗疟活性外,青蒿还表现出多种药理作用,包括抗炎、抗增殖、细胞毒性、抗菌和抗病毒特性,这主要归功于次级代谢产物,如倍半萜内酯、呋喃木脂素、聚乙炔和甲基化黄酮类化合物。本研究涵盖了1998年至2025年间报道的青蒿属植物提取物、精油和分离化合物的生物活性。青蒿次级代谢物最具特征的类别的代表性化合物与生物活性有关,包括体外和体内研究、药代动力学、临床数据和毒性概况,同时报告了每种化合物的物种特异性来源。
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引用次数: 0
Eupafolin in Nature and Science: Occurrence, Chemistry, Biosynthesis, Analytical Methods, and Potential Multifaceted Applications. 自然界和科学中的紫藻啉:存在、化学、生物合成、分析方法和潜在的多方面应用。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-02-05 DOI: 10.1055/a-2803-8122
Olusesan Ojo, Gerhard Prinsloo

Eupafolin (nepetin) is a bioactive flavonoid with a flavone backbone and hydroxyl groups contributing to its pharmacological properties. It is found in various medicinal plants and has garnered significant attention due to its biological activities, including anti-inflammatory, anticancer, antioxidant, antidiabetic, antimicrobial, and neuroprotective effects. This review explores eupafolin's natural occurrence, chemical structure, and biosynthetic pathway, highlighting its roles in different scientific domains, including pharmacology, pharmaceutical nanotechnology, and agriculture. Research data on eupafolin were sourced from databases, including Google Scholar, Science Direct, Scopus, and PubMed, up to April 2025, resulting in over 100 electronic references. Eupafolin shows promise in drug development and green nanoparticle synthesis, supporting eco-friendly nanomedicine and material science applications. Beyond the biomedical benefits of this flavone, its antimicrobial and anti-inflammatory properties also indicate potential use in plant protection and stress tolerance enhancement. Despite its pharmacological benefits, studies on eupafolin's direct toxicity and safety are lacking, with toxicity mainly observed in cultured cancer cells, suggesting chemotherapeutic potential. Thus, robust in vitro and in vivo studies are needed to determine its safety profile for drug development. Overall, this review presents a comprehensive analysis of eupafolin's occurrence, chemistry, derivatives, biosynthesis, and applications, emphasizing its potential in medicine, pharmaceutical nanotechnology, and agriculture.

槲皮素是一种具有生物活性的类黄酮,其黄酮骨架和羟基有助于其药理特性。它存在于多种药用植物中,因其生物活性,包括抗炎、抗癌、抗氧化、抗糖尿病、抗菌和神经保护作用而受到广泛关注。本文综述了尤帕弗林的天然存在、化学结构和生物合成途径,重点介绍了其在药理学、药物纳米技术和农业等不同科学领域的作用。eupafolin的研究数据来源于谷歌Scholar、Science Direct、Scopus和PubMed等数据库,截止到2025年4月,共有100多篇电子参考文献。Eupafolin在药物开发和绿色纳米颗粒合成方面显示出前景,支持环保纳米医学和材料科学应用。除了这种黄酮的生物医学益处外,它的抗菌和抗炎特性也表明它在植物保护和增强抗逆性方面的潜在用途。尽管具有药理作用,但对尤帕弗林的直接毒性和安全性研究较少,主要在培养的癌细胞中观察到毒性,提示其具有化疗潜力。因此,需要在体外和体内进行强有力的研究,以确定其在药物开发中的安全性。综上所述,本文综述了紫花酚的存在、化学、衍生物、生物合成和应用等方面的研究进展,重点介绍了紫花酚在医学、医药纳米技术和农业等方面的潜力。
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引用次数: 0
Phaeosphaeride A isolated from an endophytic Paraphoma sp. alleviates ABCG2-mediated resistance to mitoxantrone in breast cancer cells. 从内生Paraphoma sp中分离的Phaeosphaeride A可减轻abcg2介导的乳腺癌细胞对米托蒽醌的抗性。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-02-04 DOI: 10.1055/a-2805-4670
Alireza Tavakkoli, Hojjat Mortazavi, Mehrdad Iranshahi, Fatemeh Kalalinia, Khadijeh Jamialahmadi, Jon S Thorson, Khaled A Shaaban, Fatemeh Mosaffa

The efficacy of breast cancer chemotherapies is frequently limited by multidrug resistance (MDR), partly through efflux by ABC transporters, including ABCG2. This study evaluated whether phaeosphaeride A (PPA), a fungal metabolite isolated from a Paraphoma sp. endophyte of Ferula xylorhachis, can modulate ABCG2-mediated resistance to mitoxantrone (MTX). The endophyte was cultured, extracted with ethyl acetate, and purified by chromatography and HPLC to yield PPA, whose structure was confirmed by NMR and MS analyses. Cytotoxicity of MTX, PPA, and their combination was assessed in MCF-7 and ABCG2-overexpressing MCF-7/MX cells. MTX showed marked differential cytotoxicity (IC50 = 1.6 μM, 95% CI: 1.4-1.9 in MCF-7 vs. >25 μM in MCF-7/MX; p < 0.0001), whereas PPA exhibited comparable activity in both lines (23.2 μM, 95% CI: 18.0-30.1 vs. 36.1 μM, 95% CI: 28.7-46.0; p = 0.01). Co-treatment with PPA IC50 significantly reduced MTX IC50 to 0.4 μM (95% CI: 0.3-0.6) in MCF-7, and 1.9 μM (95% CI: 1.2-2.7) in MCF-7/MX, restoring MTX sensitivity in resistant cells to near MCF-7 levels. Flow cytometry showed that PPA (IC50) increased intracellular MTX accumulation with stronger effects in MCF-7/MX cells (p<0.0001) than in MCF-7 (p<0.05). In combination with MTX, PPA (IC50) increased Sub-G1 apoptotic populations in both lines. These findings demonstrate that PPA is unlikely to be a substrate of ABCG2 but functionally inhibits ABCG2-mediated efflux, contributing to the restoration of MTX sensitivity, although there may be additional mechanisms involved. PPA could be a promising MDR-reversal agent in ABCG2-driven chemotherapy resistance.

乳腺癌化疗的疗效经常受到多药耐药(MDR)的限制,部分原因是ABC转运体(包括ABCG2)的外排。本研究评估了一种真菌代谢物phaeosphaeride A (PPA)是否可以调节abcg2介导的对米托蒽醌(MTX)的抗性。PPA是从阿弗拉(Ferula xylorhachis)内生真菌Paraphoma sp.中分离出来的。对内生菌进行培养、乙酸乙酯提取、层析和高效液相色谱纯化得到PPA,经核磁共振和质谱分析证实其结构。在MCF-7和abcg2过表达的MCF-7/MX细胞中评估MTX、PPA及其联合使用的细胞毒性。MTX表现出明显的差异细胞毒性(MCF-7中IC50 = 1.6 μM, 95% CI: 1.4-1.9, MCF-7/MX中>25 μM, p < 0.0001),而PPA在两系中表现出相当的活性(23.2 μM, 95% CI: 18.0-30.1, 36.1 μM, 95% CI: 28.7-46.0, p = 0.01)。与PPA IC50共处理显著降低MCF-7的MTX IC50至0.4 μM (95% CI: 0.3-0.6), MCF-7/MX的MTX IC50至1.9 μM (95% CI: 1.2-2.7),使耐药细胞的MTX敏感性恢复到接近MCF-7的水平。流式细胞术显示,PPA (IC50)增加了细胞内MTX的积累,在MCF-7/MX细胞中作用更强(p
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引用次数: 0
Dioscorea bulbifera: Phytotherapeutic Potential and Toxicological Risks, A Critical Review. 黄薯蓣:植物治疗潜力和毒理学风险综述。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-02-03 DOI: 10.1055/a-2779-6570
Emi Mathew, Philip Litto Thomas, Linu Mathew

Dioscorea bulbifera (air potato), a climbing perennial of the Dioscoreaceae family, is widely distributed in tropical regions and valued in Ayurveda, Traditional Chinese Medicine, and African ethnomedicine for managing inflammatory, infectious, metabolic, and neoplastic disorders. This systematic review critically evaluates its phytochemistry, pharmacology, and toxicology. Primary metabolites contribute to its nutritional value, whereas secondary metabolites-predominantly steroidal saponins, flavonoids, and diterpenoids from bulbils and tubers-underlie its wide range of reported bioactivities. African accessions are rich in clerodane diterpenoids, while Asian ones are rich in saponins and flavonoids, underscoring the need for comparative metabolomic and chemotaxonomic studies.Preclinical studies confirm antiproliferative, antioxidant, anti-inflammatory, antimicrobial, antidiabetic, and neuroprotective effects. However, furanoid diterpenoids, particularly diosbulbin B and 8-epidiosbulbin E acetate, have been shown to induce hepatotoxicity, with additional risks of nephrotoxicity, cardiotoxicity, gastrointestinal irritation, and thyroid dysfunction. Traditional processing methods, such as boiling and roasting, as well as co-administration with protective herbs, mitigate toxicity. Despite promising activity, clinical translation remains hindered by phytochemical variability, non-standardised preparations, and the complete absence of human trials. Future research should therefore focus on developing detoxified, standardised extracts supported by pharmacokinetic studies and well-designed randomised controlled trials to establish D. bulbifera as a safe and effective phytotherapeutic agent.

薯蓣属薯蓣科多年生攀缘植物,广泛分布于热带地区,在阿育吠陀、传统中医和非洲民族医学中具有治疗炎症、感染、代谢和肿瘤疾病的价值。本系统综述对其植物化学、药理学和毒理学进行了批判性评价。初级代谢物有助于其营养价值,而次生代谢物——主要是甾体皂苷、黄酮类化合物和来自球茎和块茎的二萜——是其广泛生物活性的基础。非洲植物富含氯烷二萜,而亚洲植物富含皂苷和类黄酮,这强调了进行比较代谢组学和化学分类学研究的必要性。临床前研究证实其具有抗增殖、抗氧化、抗炎、抗菌、抗糖尿病和神经保护作用。然而,呋烷类二萜,特别是黄黄素B和8-醋酸黄黄素E,已被证明可诱导肝毒性,并具有肾毒性、心脏毒性、胃肠道刺激和甲状腺功能障碍的额外风险。传统的加工方法,如煮沸和烘烤,以及与保护性草药共同施用,可以减轻毒性。尽管前景看好,但临床转化仍然受到植物化学变异性、非标准化制备和完全缺乏人体试验的阻碍。因此,未来的研究应侧重于开发解毒的、标准化的提取物,这些提取物应得到药代动力学研究和精心设计的随机对照试验的支持,以确定黄胶菊是一种安全有效的植物治疗药物。关键词:黄薯蓣,甾体皂苷,类呋喃二萜,肝毒性,民族药,植物疗法
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引用次数: 0
Synergistic Neuroprotection by Cannabis sativa and Tilia × viridis: Attenuation of Hippocampal Neurons Glutamate-Induced Oxidative Stress and LPS-Driven Microglial Inflammation. 大麻和紫椴的协同神经保护作用:海马神经元谷氨酸诱导的氧化应激和脂多糖驱动的小胶质细胞炎症的衰减。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-02-02 DOI: 10.1055/a-2751-0171
Elina Malen Saint Martin, María Laura Barreiro-Arcos, María Belén Gomez, Giuliana Colonna Soldavini, Carla Marrassini, Laura Cogoi, Ignacio Peralta, Analía Reinés, María Rosario Alonso, Claudia Anesini

Throughout history, Cannabis sativa has been linked to the therapeutic management of epilepsy and Tilia × viridis has a tradition of use as a sedative.This study aimed to evaluate the protective effect of an ethanolic extract of C. sativa (CSRD), an aqueous extract of T. × viridis (TE), and their combination against oxidative stress induced by glutamate in a murine hippocampal neuronal (HT-22) cell line, as well as their anti-inflammatory activity in male Wistar rats' microglial cells stimulated with LPS. A phytochemical analysis was also conducted. Glutamate-induced reactive oxygen species (ROS) were quantified using 2',7'-dichlorodihydrofluorescein diacetate via fluorescence microscopy. Cell viability was assessed using the MTT assay. Distinct microglial cell phenotypes were identified via immunofluorescence.Extracts partially reversed glutamate-induced loss of cell viability (52% to 200% for CSRD; 22% to 82% for TE). Their combination produced a greater effect, reversing glutamate-induced toxicity by 133% to 284% and fully restoring cell viability to control levels. Moreover, the combined treatment reduced intracellular ROS levels (52% to 58%). Notably, the combination also exhibited the most pronounced anti-inflammatory effects, significantly reducing the proportion of reactive phenotype 1 cells, while increasing the population of anti-inflammatory phenotype 2 cells and preserving the trophic phenotype 3 subpopulation. In conclusion, this study not only validates the ethnobotanical uses of C. sativa and T. × viridis but also reveals a potent synergy when combined. This provides a strong foundation for the development of phytomedicines with translational potential for managing complex pathologies like epilepsy or neuroinflammation associated with neurodegenerative diseases.

纵观历史,大麻一直与癫痫的治疗管理有关,而紫椴有作为镇静剂使用的传统。本研究旨在评价黄姜醇提物(CSRD)和黄姜水提物(TE)及其联合使用对谷氨酸诱导的小鼠海马神经元(HT-22)细胞氧化应激的保护作用,以及对LPS刺激的雄性Wistar大鼠小胶质细胞的抗炎作用。还进行了植物化学分析。用2',7'-二氯二氢荧光素对谷氨酸诱导的活性氧(ROS)进行荧光显微镜定量。采用MTT法测定细胞活力。不同的小胶质细胞表型通过免疫荧光鉴定。提取物部分逆转谷氨酸诱导的细胞活力丧失(CSRD为52%至200%;TE为22%至82%)。它们的组合产生了更大的效果,将谷氨酸诱导的毒性逆转了133%至284%,并将细胞活力完全恢复到控制水平。此外,联合治疗降低了细胞内ROS水平(52%至58%)。值得注意的是,该组合还表现出最显著的抗炎作用,显著降低了反应型1细胞的比例,同时增加了抗炎型2细胞的数量,并保留了营养型3亚群。综上所述,本研究不仅验证了芥蓝和绿皮草的民族植物学用途,而且揭示了两者联合使用时的强大协同效应。这为开发具有转化潜力的植物药物提供了坚实的基础,可用于治疗复杂的病理,如癫痫或与神经退行性疾病相关的神经炎症。
{"title":"Synergistic Neuroprotection by Cannabis sativa and Tilia × viridis: Attenuation of Hippocampal Neurons Glutamate-Induced Oxidative Stress and LPS-Driven Microglial Inflammation.","authors":"Elina Malen Saint Martin, María Laura Barreiro-Arcos, María Belén Gomez, Giuliana Colonna Soldavini, Carla Marrassini, Laura Cogoi, Ignacio Peralta, Analía Reinés, María Rosario Alonso, Claudia Anesini","doi":"10.1055/a-2751-0171","DOIUrl":"https://doi.org/10.1055/a-2751-0171","url":null,"abstract":"<p><p>Throughout history, <i>Cannabis sativa</i> has been linked to the therapeutic management of epilepsy and <i>Tilia</i> × <i>viridis</i> has a tradition of use as a sedative.This study aimed to evaluate the protective effect of an ethanolic extract of <i>C. sativa</i> (CSRD), an aqueous extract of <i>T.</i> × <i>viridis</i> (TE), and their combination against oxidative stress induced by glutamate in a murine hippocampal neuronal (HT-22) cell line, as well as their anti-inflammatory activity in male Wistar rats' microglial cells stimulated with LPS. A phytochemical analysis was also conducted. Glutamate-induced reactive oxygen species (ROS) were quantified using 2',7'-dichlorodihydrofluorescein diacetate via fluorescence microscopy. Cell viability was assessed using the MTT assay. Distinct microglial cell phenotypes were identified via immunofluorescence.Extracts partially reversed glutamate-induced loss of cell viability (52% to 200% for CSRD; 22% to 82% for TE). Their combination produced a greater effect, reversing glutamate-induced toxicity by 133% to 284% and fully restoring cell viability to control levels. Moreover, the combined treatment reduced intracellular ROS levels (52% to 58%). Notably, the combination also exhibited the most pronounced anti-inflammatory effects, significantly reducing the proportion of reactive phenotype 1 cells, while increasing the population of anti-inflammatory phenotype 2 cells and preserving the trophic phenotype 3 subpopulation. In conclusion, this study not only validates the ethnobotanical uses of <i>C. sativa</i> and <i>T.</i> × <i>viridis</i> but also reveals a potent synergy when combined. This provides a strong foundation for the development of phytomedicines with translational potential for managing complex pathologies like epilepsy or neuroinflammation associated with neurodegenerative diseases.</p>","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":""},"PeriodicalIF":2.0,"publicationDate":"2026-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146106789","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
Therapeutic Potential of Ugonins: Bioactive Flavonoids from Helminthostachys zeylanica with Multifaceted Biological Activities. 乌根素的治疗潜力:具有多方面生物活性的泽兰花黄酮。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-02-01 Epub Date: 2025-10-06 DOI: 10.1055/a-2717-2323
Abdul Bari Shah, Aizhamal Baiseitova, Young Jun Kim, Ki Yong Lee

Ugonins are distinctive chemotaxonomic bioactive metabolites identified in Helminthostachys zeylanica. This uncommon fern species generates a diverse array of flavonoids, including ugonins, which facilitate various biological processes such as anti-inflammatory, neuroprotective, melanogenesis-inhibiting, antioxidant, anti-osteoporotic, and immunomodulatory functions. Our objective in this comprehensive literature review is to deliver a clear and visually engaging analysis of the therapeutic potential inherent in each of the compounds found in H. zeylanica. This review covers the isolation of ugonins A - Y and other metabolites from this plant. These compounds demonstrate a diverse range of biological properties, which are thoroughly discussed in this review. The binding scores of all ugonins A - Y against PTP1B were also presented, indicating their potential activities for future consideration. Ultimately, a thorough understanding of the diverse therapeutic properties inherent in this unique fern can be achieved through a meticulous examination of the existing literature.

乌贡素是一种独特的化学分类生物活性代谢物。这种罕见的蕨类植物产生多种黄酮类化合物,包括乌根素,促进各种生物过程,如抗炎、神经保护、抑制黑色素生成、抗氧化、抗骨质疏松和免疫调节功能。我们在这个全面的文献综述的目的是提供一个清晰的和视觉上引人入胜的分析,内在的治疗潜力的每一种化合物发现在泽兰花。本文综述了从该植物中分离出的ugonins A-Y及其代谢产物。这些化合物具有广泛的生物学特性,本文将对其进行详细的讨论。此外,还显示了所有肿瘤蛋白A-Y对PTP1B的结合评分,表明它们的潜在活性可供未来考虑。最终,通过对现有文献的细致检查,可以全面了解这种独特蕨类植物固有的多种治疗特性。
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引用次数: 0
Unveiling Rosmarinic Acid: Understanding Its Broad Spectrum of Bioactivities. 揭示迷迭香酸:了解其广谱生物活性。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-02-01 Epub Date: 2025-10-29 DOI: 10.1055/a-2727-3201
Ka Fai Leong, Zihan Chen, Paolo Coghi

Rosmarinic acid (RA) is a polyphenolic compound with various biological activities found in numerous traditional medicinal plants. Moreover, RA is already used as a food additive, demonstrating its safety. Current research has identified RA as having diverse effects, including sedative, hypnotic, antiepileptic, anti-Parkinson, neuroprotective, antidepressant, anti-inflammatory, antioxidant, cognitive-enhancing, metabolic-regulating, antimicrobial, and antitumor properties. Nevertheless, the mechanisms underlying these effects remain incompletely understood. This review attempts to define the mechanisms of its bioactivity by correlating RA's effect on different biomolecules. We performed an extensive search across major databases, using the core keyword "Rosmarinic acid" with relevant keywords to construct search queries. Our findings suggest that some mechanisms are shared among RA's various activities. For example, the chemical structure of RA itself makes it an antioxidant, and the antioxidant effect enables it to reduce inflammation caused by active substances such as ROS and free radicals. Its antioxidant and anti-inflammatory effects can relieve pain, provide neuroprotection, reduce chronic adipose inflammation, and improve insulin sensitivity. RA can also inhibit the aggregation of harmful proteins and promote their degradation, which plays a key role in neuroprotection and cognitive improvement. RA's modulation of neurotransmitters exerts both antidepressant effects and benefits on cognitive impairment. The regulation of key pathways by RA-such as ERK1/2, MAPK, STAT3, PI3K, Akt, NF-κB, and Nrf2-is central to its antioxidant, anti-inflammatory, lipid- and glucose-regulating, and antitumor effects.

迷迭香酸(RA)是一种多酚类化合物,具有多种生物活性,存在于许多传统药用植物中。此外,RA已被用作食品添加剂,证明其安全性。目前的研究已经确定RA具有多种作用,包括镇静、催眠、抗癫痫、抗帕金森、神经保护、抗抑郁、抗炎、抗氧化、增强认知、调节代谢、抗菌和抗肿瘤特性。然而,这些效应背后的机制仍然不完全清楚。本文试图通过比较RA对不同生物分子的作用来确定其生物活性的机制。我们在主要数据库中进行了广泛的搜索,使用核心关键字“迷迭香酸”和相关关键字构建搜索查询。我们的研究结果表明,RA的各种活动有一些共同的机制。例如,RA本身的化学结构使其具有抗氧化剂的特性,其抗氧化作用使其能够减少活性氧、自由基等活性物质引起的炎症。它的抗氧化和抗炎作用可以缓解疼痛,提供神经保护,减少慢性脂肪炎症,提高胰岛素敏感性。RA还可以抑制有害蛋白的聚集并促进其降解,在神经保护和认知改善中起关键作用。类风湿性关节炎对神经递质的调节具有抗抑郁作用和对认知障碍的益处。ra对ERK1/2、MAPK、STAT3、PI3K、Akt、NF-κ b和nrf2等关键通路的调控是其抗氧化、抗炎、调节脂质和葡萄糖以及抗肿瘤作用的核心。
{"title":"Unveiling Rosmarinic Acid: Understanding Its Broad Spectrum of Bioactivities.","authors":"Ka Fai Leong, Zihan Chen, Paolo Coghi","doi":"10.1055/a-2727-3201","DOIUrl":"10.1055/a-2727-3201","url":null,"abstract":"<p><p>Rosmarinic acid (RA) is a polyphenolic compound with various biological activities found in numerous traditional medicinal plants. Moreover, RA is already used as a food additive, demonstrating its safety. Current research has identified RA as having diverse effects, including sedative, hypnotic, antiepileptic, anti-Parkinson, neuroprotective, antidepressant, anti-inflammatory, antioxidant, cognitive-enhancing, metabolic-regulating, antimicrobial, and antitumor properties. Nevertheless, the mechanisms underlying these effects remain incompletely understood. This review attempts to define the mechanisms of its bioactivity by correlating RA's effect on different biomolecules. We performed an extensive search across major databases, using the core keyword \"Rosmarinic acid\" with relevant keywords to construct search queries. Our findings suggest that some mechanisms are shared among RA's various activities. For example, the chemical structure of RA itself makes it an antioxidant, and the antioxidant effect enables it to reduce inflammation caused by active substances such as ROS and free radicals. Its antioxidant and anti-inflammatory effects can relieve pain, provide neuroprotection, reduce chronic adipose inflammation, and improve insulin sensitivity. RA can also inhibit the aggregation of harmful proteins and promote their degradation, which plays a key role in neuroprotection and cognitive improvement. RA's modulation of neurotransmitters exerts both antidepressant effects and benefits on cognitive impairment. The regulation of key pathways by RA-such as ERK1/2, MAPK, STAT3, PI3K, Akt, NF-<i>κ</i>B, and Nrf2-is central to its antioxidant, anti-inflammatory, lipid- and glucose-regulating, and antitumor effects.</p>","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":"84-111"},"PeriodicalIF":2.0,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145401557","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
Impact of Different Drying Methods on Magnolia officinalis Leaves. 不同干燥方法对厚朴叶片的影响。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-02-01 Epub Date: 2025-11-04 DOI: 10.1055/a-2720-9103
Xue-Mei Lan, Xiao-Hong Yang, Jia-Qi Li, Zhen-Zhen Xue, Rong-Ping Yang, Hua Li, Bin Yang

Different drying techniques can affect the quality characteristics of Magnolia officinalis leaves (MOLs), including their chemical composition, color, and biological activity. This study comprehensively evaluated five drying methods: vacuum drying (VD), hot-air drying (HAD), freeze drying (FD), sun drying (SD), and shade drying (SHD). The non-volatile and volatile constituents of MOLs were analyzed by high-performance liquid chromatography (HPLC) and gas chromatography-mass spectrometry (GC-MS), respectively. Objective color parameters were measured using an electronic eye, and the antioxidant activity was evaluated by the DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging assay. Additionally, the moisture content and the alcohol-soluble extract content were determined. Results indicated that HAD had the least impact on the color, chemical composition, and antioxidant activity of MOLs, thereby demonstrating its superiority over the other four drying methods.

不同的干燥工艺会影响厚朴叶片的化学成分、颜色和生物活性等品质特征。本研究综合评价了真空干燥(VD)、热风干燥(HAD)、冷冻干燥(FD)、日光干燥(SD)和荫蔽干燥(SHD)五种干燥方法。采用高效液相色谱法(HPLC)和气相色谱-质谱法(GC-MS)分别分析其非挥发性成分和挥发性成分。采用电子眼法测定其客观颜色参数,并采用DPPH(1,1-二苯基-2-苦味酰肼)自由基清除法评价其抗氧化活性。并测定了其水分含量和醇溶性浸出物含量。结果表明,HAD法对MOLs的颜色、化学成分和抗氧化活性的影响最小,显示了其相对于其他四种干燥方法的优越性。
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引用次数: 0
Active Components and Multi-target Mechanism of Tibetan Sinopodophyllum hexandrum Medicine Against Rheumatoid Arthritis Using a CFA-induced Arthritis Rat Model.
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-02-01 Epub Date: 2025-10-20 DOI: 10.1055/a-2706-8264
Bao-Lin Wang, Hui Qiu, Jian-Gen Ao, Wen-Peng Du, Chun Li, Hai-Ran Fan, Jian-Qiang Qian, Bin Zou, Jia-Ke He, Wei-Fang Zhang, Xiao-Long Hu

Sinopodophyllum hexandrum ("Taoerqi") is a traditional Tibetan medicine used for treating inflammation and arthralgia, but its therapeutic basis against rheumatoid arthritis (RA) remains unclear. This study aimed to identify its active anti-RA fraction, analyse its chemical composition, and explore its mechanisms of action. Using a CFA-induced arthritis rat model, the dichloromethane fraction of S. hexandrum (SHD) was evaluated for anti-RA activity. UHPLC-Q-TOF-MS/MS identified 57 compounds, mainly prenylated flavonoids and arylnaphthalene lignans. Network pharmacology predicted their targets, and in vitro assays on TNF-α-induced fibroblast-like synoviocytes confirmed the anti-RA effects of 15 isolates. Enzyme inhibition, molecular docking, surface plasmon resonance, and Western blot validated their interactions with TNF-α and JAK1. Oral administration of SHD significantly reduced paw swelling and neutrophil infiltration in RA rats. These findings suggest that prenylated flavonoids and arylnaphthalene lignans are key active components exerting anti-RA effects, respectively, via TNF-α and JAK1 inhibition, highlighting their potential for further drug development.

本研究旨在鉴定其抗ra活性部位,分析其化学成分,探讨其作用机制。采用cfa诱导的关节炎大鼠模型,评价六己方二氯甲烷组分(SHD)的抗ra活性。UHPLC-Q-TOF-MS/MS鉴定出57个化合物,主要为烯丙基类黄酮和芳烷基萘木脂素。网络药理学预测了它们的靶点,TNF-α-诱导的成纤维细胞样滑膜细胞的体外实验证实了15株分离物的抗ra作用。酶抑制、分子对接、表面等离子体共振和Western blot验证了它们与TNF-α和JAK1的相互作用。口服SHD可显著减少类风湿关节炎大鼠足部肿胀和中性粒细胞浸润。这些发现表明,烯丙基黄酮和芳基萘木脂素是分别通过抑制TNF-α和JAK1发挥抗ra作用的关键活性成分,突出了它们进一步药物开发的潜力。
{"title":"Active Components and Multi-target Mechanism of Tibetan Sinopodophyllum hexandrum Medicine Against Rheumatoid Arthritis Using a CFA-induced Arthritis Rat Model.","authors":"Bao-Lin Wang, Hui Qiu, Jian-Gen Ao, Wen-Peng Du, Chun Li, Hai-Ran Fan, Jian-Qiang Qian, Bin Zou, Jia-Ke He, Wei-Fang Zhang, Xiao-Long Hu","doi":"10.1055/a-2706-8264","DOIUrl":"10.1055/a-2706-8264","url":null,"abstract":"<p><p><i>Sinopodophyllum hexandrum</i> (\"Taoerqi\") is a traditional Tibetan medicine used for treating inflammation and arthralgia, but its therapeutic basis against rheumatoid arthritis (RA) remains unclear. This study aimed to identify its active anti-RA fraction, analyse its chemical composition, and explore its mechanisms of action. Using a CFA-induced arthritis rat model, the dichloromethane fraction of <i>S. hexandrum</i> (SHD) was evaluated for anti-RA activity. UHPLC-Q-TOF-MS/MS identified 57 compounds, mainly prenylated flavonoids and arylnaphthalene lignans. Network pharmacology predicted their targets, and <i>in vitro</i> assays on TNF-<i>α</i>-induced fibroblast-like synoviocytes confirmed the anti-RA effects of 15 isolates. Enzyme inhibition, molecular docking, surface plasmon resonance, and Western blot validated their interactions with TNF-<i>α</i> and JAK1. Oral administration of SHD significantly reduced paw swelling and neutrophil infiltration in RA rats. These findings suggest that prenylated flavonoids and arylnaphthalene lignans are key active components exerting anti-RA effects, respectively, via TNF-<i>α</i> and JAK1 inhibition, highlighting their potential for further drug development.</p>","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":"123-138"},"PeriodicalIF":2.0,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145337524","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
Caffeoylquinic Acids from Aster tataricus Leaves Inhibit Aldose Reductase and Attenuate Hyaloid-Retinal Vasodilation in a Zebrafish Model of Hyperglycemia. 紫菀叶中的咖啡酰奎宁酸抑制高血糖斑马鱼醛糖还原酶并减弱透明质视网膜血管舒张。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-02-01 Epub Date: 2025-11-11 DOI: 10.1055/a-2744-6263
Ik Soo Lee, Seung-Hyun Jung, Young Sook Kim

Diabetic retinopathy (DR) is a leading cause of blindness, and its pathogenesis is strongly linked to the activation of aldose reductase (AR) under hyperglycemic conditions. Developing effective AR inhibitors (ARIs), particularly from natural sources, remains a critical therapeutic goal. This study investigated the AR inhibitory potential of an 80% ethanol extract from the leaves of Aster tataricus. Using UPLC-Q-Orbitrap-MS, we identified 11 major compounds, with caffeoylquinic acids (CQAs) being predominant. In vitro assays on rat lens aldose reductase (RLAR) revealed that di-caffeoylquinic acids (di-CQAs), particularly 3,5-di-O-caffeoylquinic acid (3,5-DCQA; IC50 = 0.31 µM), were potent noncompetitive inhibitors. Molecular docking simulations provided insights into their binding modes within the enzyme. The therapeutic relevance of these findings was confirmed in vivo using a larval zebrafish model of hyperglycemia, where both the A. tataricus extract and its constituent CQAs significantly suppressed hyaloid-retinal vessel dilation without inducing toxicity. Quantitative HPLC analysis confirmed that 3,5-DCQA was the most abundant di-CQA in the extract. These findings establish the CQA constituents of A. tataricus leaves as promising natural product leads for developing therapeutics to manage early-stage diabetic retinopathy.

糖尿病视网膜病变(DR)是致盲的主要原因,其发病机制与高血糖状态下醛糖还原酶(AR)的激活密切相关。开发有效的AR抑制剂(ARIs),特别是从天然来源,仍然是一个关键的治疗目标。本研究考察了紫菀叶80%乙醇提取物的AR抑制潜力。利用UPLC-Q-Orbitrap-MS鉴定了11个主要化合物,其中以咖啡酰奎宁酸(CQAs)为主。对大鼠晶态醛糖还原酶(RLAR)的体外实验显示,二咖啡基奎宁酸(di-CQAs),特别是3,5-二- o -咖啡基奎宁酸(3,5- dcqa; IC₅₀= 0.31µM)是有效的非竞争性抑制剂。分子对接模拟提供了它们在酶内结合模式的见解。这些发现的治疗相关性在体内用幼体斑马鱼高血糖模型得到了证实,其中,塔塔利乌提取物及其成分CQAs都能显著抑制透明体-视网膜血管扩张,而不会引起毒性。定量HPLC分析证实,3,5- dcqa是提取物中含量最多的二cqa。这些发现表明,塔塔利乌叶的CQA成分是开发治疗早期糖尿病视网膜病变的有希望的天然产物先导物。
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Planta medica
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