FitoterapiaPub Date : 2025-07-21DOI: 10.1016/j.fitote.2025.106749
Mahmoud Moustafa , Walaa S. Aboelmaaty , Weaam Ebrahim , Reham Hassan Mekky , Mohamed A. Tammam , Amr El-Demerdash , Ahmed M. Zaghloul
{"title":"Chemical profiling of Lycium shawii via RP-HPLC-QTOF-MS and MS/MS: unveiling its in-vivo wound-healing potential supported by molecular docking investigations","authors":"Mahmoud Moustafa , Walaa S. Aboelmaaty , Weaam Ebrahim , Reham Hassan Mekky , Mohamed A. Tammam , Amr El-Demerdash , Ahmed M. Zaghloul","doi":"10.1016/j.fitote.2025.106749","DOIUrl":"10.1016/j.fitote.2025.106749","url":null,"abstract":"<div><div><em>Lycium shawii</em> Roem. & Schult., traditionally used across arid regions for treating various ailments, was investigated for its wound-healing potential using integrated metabolomic, computational, and in- vivo approaches. Methanolic extract profiling via RP-HPLC-QTOF-MS/MS identified 62 metabolites, including terpenes, fatty acids, and phenolics. Six key compounds were selected for molecular docking and in silico pharmacokinetic/toxicity analysis, showing strong predicted activity and drug-likeness. In vivo evaluation using a rat excision wound model revealed that treatment with a 2 % extract cream significantly enhanced wound closure (88.63 % by day 14), re-epithelialization, collagen deposition, and VEGF expression compared to controls. The findings suggest that <em>L. shawii</em> promotes wound healing through angiogenesis and tissue regeneration mechanisms. This study supports its traditional use and highlights its pharmaceutical potential.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"185 ","pages":"Article 106749"},"PeriodicalIF":2.5,"publicationDate":"2025-07-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144694356","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}
{"title":"Baicalein, a major component of the root of Oroxylum indicum (L.) Kurz (Bignoniaceae), inhibits phosphodiesterase 5 and vasodilates isolated pulmonary arteries through endothelium-independent mechanisms","authors":"Nattiya Chaichamnong , Corine Girard , Céline Demougeot , Nitra Nuengchamnong , Samjhana Bhandari , Prapapan Temkitthawon , Kornkanok Ingkaninan , Perle Totoson","doi":"10.1016/j.fitote.2025.106753","DOIUrl":"10.1016/j.fitote.2025.106753","url":null,"abstract":"<div><div><em>Oroxylum indicum</em> (L.) Kurz root has been traditionally used as an aphrodisiac. This study aimed to elucidate the phosphodiesterase (PDE) 5 inhibition and vasodilatory effects of <em>O. indicum</em> root extract and its main constituent. LC-QTOF-MS/MS analysis identified twenty constituents within the extract, including baicalein, biochanin A, and chrysin, detected in both positive and negative modes. HPLC analysis confirmed baicalein as the major constituent of <em>O. indicum</em> root extract. The extract exhibited potential for PDE5 inhibition, with an IC<sub>50</sub> value of 1.96 μg/mL. Among the three compounds, biochanin A demonstrated the highest PDE5 inhibition, with an IC<sub>50</sub> value of 6.16 μM, followed by baicalein (IC<sub>50</sub> = 20.54 μM) and chrysin (IC<sub>50</sub> = 42.18 μM). The vascular effects and mechanisms of <em>O. indicum</em> extract (0.01–300 μg/mL) and compounds (10<sup>−11</sup>–10<sup>−6</sup> M) were evaluated in rat-isolated pulmonary artery (PA) and aorta. Both <em>O. indicum</em> extract and baicalein exhibited potent vasodilatory effects, with greater efficacy in the PA compared to the aorta. E<sub>max</sub> values for PA versus aorta were 84.8 % versus 24.8 % (<em>p</em> < 0.001) for <em>O. indicum</em> extract and 85.3 % versus 31.9 % (<em>p</em> < 0.001) for baicalein. <em>O. indicum</em>-induced PA relaxation was endothelium-dependent, involving eNOS activation, COX pathways, and EDHF production. Conversely, baicalein-induced PA relaxation was endothelium-independent, mediated by inhibition of K<sub>v</sub> channels, intracellular calcium release, and blockade of alpha-1 adrenergic receptors. Taken together, these findings expand the biological profile of <em>O. indicum</em> root and highlight baicalein as a promising candidate for cardiovascular disease treatment.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"185 ","pages":"Article 106753"},"PeriodicalIF":2.5,"publicationDate":"2025-07-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144697975","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}
FitoterapiaPub Date : 2025-07-21DOI: 10.1016/j.fitote.2025.106752
Shan Fan , Xiaoqun Shen , Qing Liu , Wenhui Jiang , Liuyin Wang , Yakun Hao , Jia Yan , Shengguo Ji
{"title":"Exploring the molecular mechanism of Chinese herbal extracts used to improve skin wound healing","authors":"Shan Fan , Xiaoqun Shen , Qing Liu , Wenhui Jiang , Liuyin Wang , Yakun Hao , Jia Yan , Shengguo Ji","doi":"10.1016/j.fitote.2025.106752","DOIUrl":"10.1016/j.fitote.2025.106752","url":null,"abstract":"<div><div>This study investigates the chemical composition and therapeutic mechanisms of Compound Pyocutaneous Liniments (CPL), a traditional Chinese medicine, in treating skin ulcers. Using UPLC-Q-Orbitrap-MS, 66 bioactive components were identified, including flavonoids, phenylpropanoids, and anthraquinones. Acute oral toxicity tests demonstrated that CPL has high safety within the tested dose range. Skin irritation tests revealed that CPL does not cause skin irritation. In a rat skin ulcer model, CPL significantly accelerated wound healing, enhanced collagen deposition, and upregulated CD34, VEGF, and EGF expression. Serum and skin metabolomics revealed CPL's regulation of glycerophospholipid and sphingolipid metabolism. Network pharmacology predicted TNF, AKT1, and EGFR as core targets, with pathways such as EGFR tyrosine kinase inhibitor resistance and VEGF signaling implicated. Molecular docking validated strong interactions between CPL components (e.g., luteolin) and these targets. These findings demonstrate CPL's multi-component, multi-target, and multi-pathway mechanisms, supporting its clinical application for skin ulcers.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"185 ","pages":"Article 106752"},"PeriodicalIF":2.5,"publicationDate":"2025-07-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144697976","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}
FitoterapiaPub Date : 2025-07-21DOI: 10.1016/j.fitote.2025.106755
Xiao-Hua Xu, Da-Jie Zou, Di-Jun Ji, Huan Wang, Yong-Chang Lu
{"title":"Study on the therapeutic effect of Fallopia aubertii (L.Henry) Holub against HUA combined with AGA and the separation of chemical components of ethyl acetate extract.","authors":"Xiao-Hua Xu, Da-Jie Zou, Di-Jun Ji, Huan Wang, Yong-Chang Lu","doi":"10.1016/j.fitote.2025.106755","DOIUrl":"https://doi.org/10.1016/j.fitote.2025.106755","url":null,"abstract":"<p><p>Fallopia aubertii (L.Henry) Holub, also known as Polygonum aubertii, is a traditional Tibetan medicinal plant widely used for its pharmacological effects, including clearing heat, dispelling wind and dampness, and promoting diuresis.Modern pharmacological studies have shown that Fallopia aubertii has better pharmacological effects on analgesic, anti-inflammatory and anti-hyperuricemia. However, its mechanism of action has not been elucidated.Therefore, in this study, the therapeutic effects of different extracts of Fallopia aubertii on HUA + AGA model rats were verified by in vivo experiments. Meanwhile, the main active parts of Fallopia aubertii were enriched and purified by on-line MCI column combined with two-dimensional preparative liquid chromatography to prepare high-purity single compounds, which initially explored the pharmacological constituents and mechanism of action of Fallopia aubertii. The pharmacological experiments showed that the ethyl acetate extracted part of Fallopia aubertii had significant efficacy in the treatment of acute gouty arthritis combined with hyperuricemia in rats. In addition, the main compounds isolated from the Fr6 fraction of the ethyl acetate fraction of Fallopia aubertii were flavonoids. It is speculated that the mechanism of action may be that the flavonoid compounds in Fallopia aubertii ethyl acetate inhibit the activity of XOD and reduce the level of inflammatory factors, thereby slowing down the synthesis of uric acid and alleviating inflammation. The online MCI column combined with two-dimensional liquid chromatography used in this study showed great potential in the separation of high-purity compounds from Fallopia aubertii, providing broad application prospects for the efficient separation of single compounds in natural plants.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106755"},"PeriodicalIF":2.5,"publicationDate":"2025-07-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144697977","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}
FitoterapiaPub Date : 2025-07-20DOI: 10.1016/j.fitote.2025.106748
Chao Liang, Oliver Gericke, Yong Zhao, Casper Steinmann, Parvathy Krishnan, Gerardo Flores-Iga, Karel Miettinen, Bekzod Khakimov, Aldo Almeida
{"title":"Adding value to botanical resources: Metabolic network analysis along with high-resolution bioassays screening and UHPLC-qToF-high-resolution MS/MS profiling detail the pharmacological potential of underexplored Latin-American plants.","authors":"Chao Liang, Oliver Gericke, Yong Zhao, Casper Steinmann, Parvathy Krishnan, Gerardo Flores-Iga, Karel Miettinen, Bekzod Khakimov, Aldo Almeida","doi":"10.1016/j.fitote.2025.106748","DOIUrl":"https://doi.org/10.1016/j.fitote.2025.106748","url":null,"abstract":"<p><p>Healthcare services are challenged by an increased incidence of diseases and a decline in new drugs being brought to market. Thus, there is renewed interest in drug discovery from plants. This paper focused on enhancing the value of a small but diverse botanical resource of 45 Latin-American plant species, mostly from Mexican origin, through untargeted metabolomics, metabolic network analysis and parallel-in-vitro-bioactivity screening. The plant-extract collection was tested for inhibitory activity of human neutrophil elastase (HNE), α-glucosidase and PTP-1B as well as reviewing in detail antifungal and CB<sub>2</sub>-agonist activities previously reported for this collection. Through these approaches it was found that only 30 % of plants mentioned in traditional medicine to treat diabetes, had greater than 60 % inhibitory activity against PTP-1B or α-glucosidase and this could be part of their modes of action, while six plant species previously undescribed for antidiabetic use could inhibit these enzymes, with three of these plant species being ornamentals (Cosmos bipinnatus, Cuphea ignea and Clarkia amoena). Biochromatograms from active extracts show that the bioactivity is due to specific fractions/compounds. The results, indicate that parallel-in-vitro-bioactivity screening of plants is a valuable approach that could lead to the expansion of the natural-product chemical space for new therapeutics, even if no previous evidence of their use in traditional medicine exists. Results for HNE, CB<sub>2</sub>-agonist and antifungal assays were similar. This study delivers a valuable UHPLC-qToF-HRMS/MS dataset along with bioactivity screens that can serve the natural-products community for future endeavors in exploring the valuable chemical space of Latin-American plants.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106748"},"PeriodicalIF":2.5,"publicationDate":"2025-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144689672","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}
FitoterapiaPub Date : 2025-07-20DOI: 10.1016/j.fitote.2025.106744
Haibo Tan , Shan Zhang , Ziyu Wang , Zhihao Zhang , Jianyong Zhang , Ertao Jia
{"title":"Combining transcriptomics and network pharmacology to reveal the mechanisms of QuZhuoHuaYu decoction ameliorating gouty arthritis","authors":"Haibo Tan , Shan Zhang , Ziyu Wang , Zhihao Zhang , Jianyong Zhang , Ertao Jia","doi":"10.1016/j.fitote.2025.106744","DOIUrl":"10.1016/j.fitote.2025.106744","url":null,"abstract":"<div><div>QuZhuoHuaYu decoction (QZHY), a traditional Chinese medicine, has demonstrated a potential effect in gouty arthritis (GA) treatment, but its underlying mechanisms have yet to be fully elucidated. In this study, a strategy of UHPLC-Q-Orbitrap-MS/MS, transcriptomics, and network pharmacology combined with experimental verification was conducted to explore the constituents and the potential mechanisms of QZHY. A total of 26 compounds were identified from QZHY. Furthermore, QZHY significantly reduced the swelling index and inflammatory cell infiltration, and restrained macrophage M1 polarization and NLRP3/IL-1β pathway in ankle joints of GA mice. According to network pharmacology and transcriptomic analysis, it found NF-κB, HIF-1, and neutrophil extracellular trap (NET) formation pathways are the potential pathways for QZHY against GA. Experimental verification revealed that QZHY treatment inhibited NF-κB, HIF-1, and NET formation pathways in GA mice. In conclusion, QZHY ameliorates inflammation in GA mice, which may be associated with the inhibition of NLRP3, NF-κB, HIF-1, and NET formation pathways. It highlights a multi-target pharmacological mechanism of QZHY and provides a scientific basis for further study of QZHY on GA treatment.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"185 ","pages":"Article 106744"},"PeriodicalIF":2.5,"publicationDate":"2025-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144679366","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}
FitoterapiaPub Date : 2025-07-20DOI: 10.1016/j.fitote.2025.106740
Milena Terzic , Abdullahi Ibrahim Uba , Mehmet Veysi Cetiz , Ismail Senkardes , Ismail Koyuncu , Ozgur Yuksekdag , Alina Kalyniukova , Halbay Turumtay , Gokhan Zengin
{"title":"LC-MS-qTOF analysis and biological evaluation of Chrozophora tinctoria extracts: A novel attempt at integrating in vitro and in silico approaches","authors":"Milena Terzic , Abdullahi Ibrahim Uba , Mehmet Veysi Cetiz , Ismail Senkardes , Ismail Koyuncu , Ozgur Yuksekdag , Alina Kalyniukova , Halbay Turumtay , Gokhan Zengin","doi":"10.1016/j.fitote.2025.106740","DOIUrl":"10.1016/j.fitote.2025.106740","url":null,"abstract":"<div><div>This manuscript investigates the phytochemical composition and biological potential of <em>Chrozophora tinctoria</em> extracts obtained with solvents of different polarities (ethyl acetate, ethanol, 70 % ethanol, and water). Comprehensive in vitro analyses revealed that ethanol and ethyl acetate extracts had the highest levels of phenolic and flavonoid compounds, which corresponded with strong antioxidant activity and significant inhibitory effects on key enzymes such as acetylcholinesterase, butyrylcholinesterase, α-amylase, α-glucosidase, and tyrosinase. Cytotoxicity tests on several human cell lines showed that the plant species tested did not exhibit cytotoxic activity. LC-MS-qTOF analysis identified bioactive components, with apigenin emerging as one of the most interesting compounds. An integrated in silico approach involving network pharmacology, molecular docking, and molecular dynamics simulations revealed strong and stable interactions between apigenin and therapeutic targets involved in neurodegenerative and metabolic processes. These findings could serve as an outline for future studies on the medicinal plant's potential.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"185 ","pages":"Article 106740"},"PeriodicalIF":2.5,"publicationDate":"2025-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144685577","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}
FitoterapiaPub Date : 2025-07-20DOI: 10.1016/j.fitote.2025.106746
Shehroz Abbas , Muhammad Shahbaz , Amjad Ali , Saqlain Irshad , Salman Ahmad , Jaya Seelan Sathiya Seelan , Christophe Wiart , Praneetha Palasuberniam , Nazirah Mustaffa
{"title":"Casticin: A natural flavonoid with promising pharmacological and biological activities","authors":"Shehroz Abbas , Muhammad Shahbaz , Amjad Ali , Saqlain Irshad , Salman Ahmad , Jaya Seelan Sathiya Seelan , Christophe Wiart , Praneetha Palasuberniam , Nazirah Mustaffa","doi":"10.1016/j.fitote.2025.106746","DOIUrl":"10.1016/j.fitote.2025.106746","url":null,"abstract":"<div><div>Casticin, a flavonoid extracted from diverse botanical sources, has garnered substantial scientific interest due to its remarkable pharmacological properties and significant therapeutic potential. This review provides an extensive evaluation of casticin's biological activities, emphasizing its broad-spectrum antimicrobial effects, including antibacterial, antiviral and antifungal. Its anticancer potential is demonstrated by its ability to suppress tumour proliferation, induce apoptosis, and regulate oncogenic pathways. Casticin also exhibits significant antidiabetic properties through enhanced glucose metabolism and insulin sensitivity, along immunomodulatory capacities that modulate cytokine expression and immune cell function. Additional properties include its antioxidant activity, anti-inflammatory effects, and wound-healing potential, characterized by enhanced tissue regeneration and angiogenic. Moreover, the review highlights casticins organ-protective potential, <em>i.e.</em>, neuroprotective, cardioprotective, hepatoprotective, nephroprotective, pulmonary, and testicular cytoprotection. The molecular mechanisms underlying these pleiotropic effects have been discussed, particularly its ability to modulate critical signaling pathways and gene expression dynamics. Casticin's bioavailability, pharmacokinetics, and synergistic potential with other therapeutics further support its promise as a multi-targeted natural compound. This review underscores casticins broad pharmacological spectrum and encourages future research into its clinical applications.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"185 ","pages":"Article 106746"},"PeriodicalIF":2.5,"publicationDate":"2025-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144689673","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}
FitoterapiaPub Date : 2025-07-20DOI: 10.1016/j.fitote.2025.106754
Ashis Kumar Goswami , Anupam Sarma , Sahabuddin Ahmed , Bhrigu Kumar Das
{"title":"Linalool in chronic diseases: A comprehensive review of its pharmacological potential and delivery aspects","authors":"Ashis Kumar Goswami , Anupam Sarma , Sahabuddin Ahmed , Bhrigu Kumar Das","doi":"10.1016/j.fitote.2025.106754","DOIUrl":"10.1016/j.fitote.2025.106754","url":null,"abstract":"<div><div>Chronic diseases rank among the leading causes of death worldwide. Plant-derived phytochemicals are known to exert a wide range of health benefits, and linalool, a noncyclic monoterpenoid found in commonly used culinary herbs and spices, has demonstrated diverse pharmacological activities, including anti-inflammatory, cardioprotective, hepatoprotective, and anti-cancer effects. Plants synthesize linalool <em>via</em> the mevalonate pathway and the 2-<em>C</em>-methyl-D-erythritol 4-phosphate pathway. It undergoes a metabolic transformation in the mammalian system upon ingestion, resulting in bioactive metabolites. Therefore, this review aims to comprehensively explore the biosynthesis of linalool, its metabolism, pharmacological mechanisms, and drug delivery approaches related to linalool in the context of chronic disease management. A detailed literature search was conducted using the PubMed, ScienceDirect, Scopus, and Web of Science databases up to March 2025. A total of 259 articles relevant to linalool's biosynthesis, therapeutic effects, molecular mechanisms, and pharmacokinetics were included. The review summarizes current knowledge on linalool's biosynthesis, its biological activities across a spectrum of chronic diseases, and the molecular mechanisms involved, such as modulation of dopamine levels, tyrosine hydroxylase activity, oxidative stress pathways, and expression of inflammatory enzymes like cyclooxygenase (COX). Furthermore, the review highlights innovative delivery systems, including nanocarriers, that have been developed to enhance the bioavailability and therapeutic efficacy of linalool. Given its multitargeted pharmacological profile, linalool is a promising candidate for managing chronic diseases. However, further preclinical and clinical investigations are necessary to validate its therapeutic potential and optimize delivery strategies.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"185 ","pages":"Article 106754"},"PeriodicalIF":2.5,"publicationDate":"2025-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144685576","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}
FitoterapiaPub Date : 2025-07-20DOI: 10.1016/j.fitote.2025.106750
Tomasz Tuzimski , Anna Petruczynik , Tomasz Plech , Mateusz Sugajski , Adrianna Frydrysiak-Brzozowska , Małgorzata Szultka-Młyńska , Daria Janiszewska , Barbara Wasilewska , Bogusław Buszewski
{"title":"Determination of selected isoquinoline alkaloids from Corydalis species extracts by liquid chromatography and their in vitro and in silico cholinesterases inhibition and in vitro and in vivo cytotoxic activity against human melanoma cells","authors":"Tomasz Tuzimski , Anna Petruczynik , Tomasz Plech , Mateusz Sugajski , Adrianna Frydrysiak-Brzozowska , Małgorzata Szultka-Młyńska , Daria Janiszewska , Barbara Wasilewska , Bogusław Buszewski","doi":"10.1016/j.fitote.2025.106750","DOIUrl":"10.1016/j.fitote.2025.106750","url":null,"abstract":"<div><div>Neurodegenerative diseases and cancers represent a significant global health burden, and should be effectively addressed with better therapeutic strategies. Therefore, new therapeutic agents are needed for the management of these diseases. The aim of the present study is to determine the <em>in vitro</em> cholinesterase inhibitory effects of extracts obtained from selected <em>Corydali</em>s species. Investigated alkaloid standards and most of the investigated plant extracts exhibited significant anti-cholinesterases activity. The kinetic results indicated that canadine competitively inhibited acetylcholinesterase, while butyrylcholinesterase was inhibited <em>via</em> a mixed mode. Protopine also exhibited mixed-type inhibition of acetylcholinesterase. The aim of the study was also to determine the cytotoxic activity of the tested extracts towards human melanoma cells lines (A375 and SK-MEL-3). All investigated extracts exhibited higher activity against SK-MEL-3 cells than the anticancer drug etoposide. The most cytotoxic extract was obtained from the rhizome of <em>Corydalis solida</em> with IC<sub>50</sub> = 11.3 μg/mL. The cytotoxic properties of the extract were also investigated in <em>in vivo</em> experiments using the <em>Danio rerio</em> larvae xenograft model. The obtained results confirmed a significant effect of the <em>Corydalis solida</em> rhizome extract on the number of cancer cells in a living organism. The activity of the extract in <em>in vivo</em> investigations was significantly higher than that of etoposide. Our results demonstrate that extracts obtained from <em>Corydalis</em> species, especially the <em>Corydalis solida</em> rhizome extract, can be recommended for further experiments in order to confirm the possibility of their application in the treatment of neurodegenerative diseases and, especially, human melanoma.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"185 ","pages":"Article 106750"},"PeriodicalIF":2.6,"publicationDate":"2025-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144689674","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}