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.
{"title":"Chemical Diversity and Biological Activities of the Artemisia L. Genus Beyond Antimalarial Effects.","authors":"Olga Karoutzou, Leandros Alexios Skaltsounis","doi":"10.1055/a-2805-3483","DOIUrl":"https://doi.org/10.1055/a-2805-3483","url":null,"abstract":"<p><p>The genus <i>Artemisia</i> 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, <i>Artemisia</i> 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 <i>Artemisia annua</i> L. Beyond antimalarial activity, <i>Artemisia</i> 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 <i>Artemisia</i> genus reported between 1998 and 2025. Representative compounds from the most characteristic classes of <i>Artemisia</i> secondary metabolites are linked to biological activities, incorporating <i>in vitro</i> and <i>in vivo</i> studies, pharmacokinetics, clinical data and toxicity profiles, while for each compound species-specific origin is reported.</p>","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":""},"PeriodicalIF":2.0,"publicationDate":"2026-02-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146143211","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}
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.
{"title":"Eupafolin in Nature and Science: Occurrence, Chemistry, Biosynthesis, Analytical Methods, and Potential Multifaceted Applications.","authors":"Olusesan Ojo, Gerhard Prinsloo","doi":"10.1055/a-2803-8122","DOIUrl":"https://doi.org/10.1055/a-2803-8122","url":null,"abstract":"<p><p>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.</p>","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":""},"PeriodicalIF":2.0,"publicationDate":"2026-02-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146125951","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}
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.
{"title":"Phaeosphaeride A isolated from an endophytic Paraphoma sp. alleviates ABCG2-mediated resistance to mitoxantrone in breast cancer cells.","authors":"Alireza Tavakkoli, Hojjat Mortazavi, Mehrdad Iranshahi, Fatemeh Kalalinia, Khadijeh Jamialahmadi, Jon S Thorson, Khaled A Shaaban, Fatemeh Mosaffa","doi":"10.1055/a-2805-4670","DOIUrl":"https://doi.org/10.1055/a-2805-4670","url":null,"abstract":"<p><p>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.</p>","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":""},"PeriodicalIF":2.0,"publicationDate":"2026-02-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146119907","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}
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.
{"title":"Dioscorea bulbifera: Phytotherapeutic Potential and Toxicological Risks, A Critical Review.","authors":"Emi Mathew, Philip Litto Thomas, Linu Mathew","doi":"10.1055/a-2779-6570","DOIUrl":"10.1055/a-2779-6570","url":null,"abstract":"<p><p>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.</p>","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":""},"PeriodicalIF":2.0,"publicationDate":"2026-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145857541","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}
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.
{"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}
Pub Date : 2026-02-01Epub Date: 2025-10-06DOI: 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.
{"title":"Therapeutic Potential of Ugonins: Bioactive Flavonoids from Helminthostachys zeylanica with Multifaceted Biological Activities.","authors":"Abdul Bari Shah, Aizhamal Baiseitova, Young Jun Kim, Ki Yong Lee","doi":"10.1055/a-2717-2323","DOIUrl":"10.1055/a-2717-2323","url":null,"abstract":"<p><p>Ugonins are distinctive chemotaxonomic bioactive metabolites identified in <i>Helminthostachys zeylanica</i>. 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 <i>H. zeylanica</i>. 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.</p>","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":"112-122"},"PeriodicalIF":2.0,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145239511","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}
Pub Date : 2026-02-01Epub Date: 2025-10-29DOI: 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.
{"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}
Pub Date : 2026-02-01Epub Date: 2025-11-04DOI: 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.
{"title":"Impact of Different Drying Methods on Magnolia officinalis Leaves.","authors":"Xue-Mei Lan, Xiao-Hong Yang, Jia-Qi Li, Zhen-Zhen Xue, Rong-Ping Yang, Hua Li, Bin Yang","doi":"10.1055/a-2720-9103","DOIUrl":"10.1055/a-2720-9103","url":null,"abstract":"<p><p>Different drying techniques can affect the quality characteristics of <i>Magnolia officinalis</i> 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.</p>","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":"139-147"},"PeriodicalIF":2.0,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145445528","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}
Pub Date : 2026-02-01Epub Date: 2025-10-20DOI: 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.
{"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}
Pub Date : 2026-02-01Epub Date: 2025-11-11DOI: 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。
{"title":"Caffeoylquinic Acids from Aster tataricus Leaves Inhibit Aldose Reductase and Attenuate Hyaloid-Retinal Vasodilation in a Zebrafish Model of Hyperglycemia.","authors":"Ik Soo Lee, Seung-Hyun Jung, Young Sook Kim","doi":"10.1055/a-2744-6263","DOIUrl":"10.1055/a-2744-6263","url":null,"abstract":"<p><p>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 <i>Aster tataricus</i>. Using UPLC-Q-Orbitrap-MS, we identified 11 major compounds, with caffeoylquinic acids (CQAs) being predominant. <i>In vitro</i> assays on rat lens aldose reductase (RLAR) revealed that di-caffeoylquinic acids (di-CQAs), particularly 3,5-di-O-caffeoylquinic acid (3,5-DCQA; IC<sub>50</sub> = 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 <i>in vivo</i> using a larval zebrafish model of hyperglycemia, where both the <i>A. tataricus</i> 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 <i>A. tataricus</i> leaves as promising natural product leads for developing therapeutics to manage early-stage diabetic retinopathy.</p>","PeriodicalId":20127,"journal":{"name":"Planta medica","volume":" ","pages":"148-159"},"PeriodicalIF":2.0,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145496017","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}