Phytochemical Analysis最新文献

{"title":"Preclinical and Clinical Evidence on the Efficacy and Cytotoxicity of Curcumin and Curcumin Derivatives in Chronic Myeloid Leukemia: A Systematic Review.","authors":"Seyed Mohammad Hosseini, Fatemeh Peymaninezhad, Fatemeh Khademi, Alireza Khiabani, Alireza Khanahmad, Alireza Farsinejad, Ali Bazi","doi":"10.1002/pca.70074","DOIUrl":"10.1002/pca.70074","url":null,"abstract":"<p><strong>Background: </strong>Curcumin (CUR), an active secondary metabolite of Curcuma longa, is known for its therapeutic effects in diverse neoplastic and nonneoplastic conditions. Here, we systematically reviewed relevant literature to explore the efficacy and cytotoxicity of CUR and its derivatives in treating chronic myeloid leukemia (CML) in preclinical and clinical settings.</p><p><strong>Methods: </strong>We followed the PRISMA guideline to conduct a systematic literature search in PubMed, Web of Science, Scopus, and Embase on March 8, 2025, using relevant keywords, including chronic myeloid leukemia, CUR, and CUR derivatives. A manual search on Google Scholar was also performed to ensure comprehensive literature coverage. Duplicates were removed, and papers were evaluated for eligibility through a two-phase screening process. Data were then extracted and qualitatively analyzed.</p><p><strong>Results: </strong>A total of 728 publications were identified. After removing duplicates and irrelevant literature, the abstracts of 318 papers were assessed for eligibility. Finally, 64 studies (55 retrieved via database search and nine through manual search) were analyzed. Preclinical evidence demonstrated the antiproliferative and proapoptotic effects of CUR and its derivatives, alone or in combination with traditional therapies, against CML cells and models. Also, a single clinical study supported the adjunctive therapeutic effect of CUR in combination with imatinib.</p><p><strong>Conclusion: </strong>Preclinical evidence supports the potential role of CUR and its derivatives, adjuvant or stand-alone therapeutic agents, for CML management. More comprehensive clinical trials are warranted to validate these findings, optimize CUR formulations and dosing strategies, and maximize their clinical benefits.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"716-745"},"PeriodicalIF":2.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147819565","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Discovery of Active Compounds in Qigui Jiangzhi Formula for Metabolic Dysfunction-Associated Steatotic Liver Disease by a Multidimensional Phenotypic Analysis.","authors":"Xianghao Xu, Fanxing Zhou, Zhe Wu, Yi Zhou, Yanying Zhang, Miao Xu, Xudong Xing, Ping Li, Guangji Wang, Hua Yang","doi":"10.1002/pca.70075","DOIUrl":"10.1002/pca.70075","url":null,"abstract":"<p><strong>Background: </strong>The incidence of metabolic dysfunction-associated steatotic liver disease (MASLD) is rising steadily. Clinically, the Qigui Jiangzhi Formula (QGJZF) has been proven to be capable of effectively improving the conditions of patients with hyperlipidemia and those with metabolic-associated fatty liver disease by regulating the pathways of glucose and lipid metabolism.</p><p><strong>Purpose: </strong>This study aims to establish a strategy based on multidimensional phenotypic characteristics to screen for active compounds in QGJZF that can improve abnormal glucose and lipid metabolism.</p><p><strong>Methods: </strong>A multidimensional phenotypic method for liver cells based on high-content imaging has been developed. This method can correlate biological processes with morphological data, such as glucose metabolism, lipid metabolism, energy metabolism, and oxidative stress in MASLD. The chemical-phenotypic correlation analysis has identified the active compounds in QGJZF by activity score and cluster score. These scores were obtained by combining the mass spectrometry ion data of each fraction of QGJZF with the multidimensional phenotypic data. The data of active compounds were combined with network pharmacology for analysis, thereby elucidating the mechanism of QGJZF in improving MASLD.</p><p><strong>Results: </strong>Among the 199 cell phenotypic parameters obtained by multidimensional phenotypic method, 99, 51, 131, and 76 were respectively associated with glucose metabolism disorders, lipid metabolism disorders, energy metabolism disorders, and oxidative stress in MASLD. Subsequently, 23 active compounds were identified in QGJZF that improve glucose metabolism homeostasis, ameliorate lipid metabolism disorders, restore energy metabolism balance, and alleviate oxidative damage. The combined analysis of active compounds and network pharmacology results indicates that their mechanism of action may involve the AGE-RAGE, MASLD-related, AMPK, and HIF-1 signaling pathways.</p><p><strong>Conclusions: </strong>This study overcame the limitations of single-indicator screening methods for MASLD by proposing a multidimensional phenotypic method. Using this method, the active compounds in QGJZF and the key pathways through which they improve MASLD were identified.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"746-760"},"PeriodicalIF":2.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147778584","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Investigation of the Chemical Constituents and Hepatic-Exposed Components of the Bupleuri Radix-Rhei Radix et Rhizoma Herbal Pair Based on UPLC-Q-Orbitrap-MS Analysis.","authors":"Xinyu Dai, Jie Ma, Qian Lu, Zhiyuan Huang, Xinyu He, Tongyan Jiao, Ningning Cao, Shenshen Yang","doi":"10.1002/pca.70076","DOIUrl":"10.1002/pca.70076","url":null,"abstract":"<p><strong>Background: </strong>Bupleuri Radix (BR) and Rhei Radix et Rhizoma (RR) are commonly used in combination in traditional Chinese medicine, yet the chemical basis of their compatibility and the liver-exposed constituents after oral administration remain unclear.</p><p><strong>Objective: </strong>To systematically characterize the chemical constituents of the Bupleuri Radix-Rhei Radix et Rhizoma (BR-RR) aqueous extract and to investigate the exposed prototype components and metabolites in mouse liver after oral administration.</p><p><strong>Methods: </strong>UPLC-Q-Orbitrap-MS was employed to comprehensively analyze the chemical constituents of the BR-RR aqueous extract and the liver-exposed components in mice after gavage administration. Compound identification was performed by integrating retention times, accurate molecular weights, and multistage MS fragmentation data.</p><p><strong>Results: </strong>A total of 109 compounds were tentatively identified in the BR-RR aqueous extract, including anthraquinones, saponins, flavonoids, phenols, and organic acids. In mouse liver samples, 25 prototype components and 21 metabolites were tentatively characterized after oral administration, among which anthraquinones were the predominant chemical class. These findings revealed the major in vivo exposed constituents and metabolic characteristics of the BR-RR extract in the liver.</p><p><strong>Conclusions: </strong>This study systematically characterized the chemical constituents of the BR-RR aqueous extract and elucidated its liver exposure profile in mice. The findings provide an overall view of the in vivo exposure and metabolic characteristics of the extract and offer useful reference information for quality evaluation and further investigation of its material basis.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"761-791"},"PeriodicalIF":2.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147841369","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Nanoparticle-Based Delivery Systems for Traditional Chinese Medicine in Cardiovascular Diseases: Advances and Challenges.","authors":"Yanying Xiong, Hua Geng, Wenjing Jiang, Yuqing Meng","doi":"10.1002/pca.70073","DOIUrl":"10.1002/pca.70073","url":null,"abstract":"<p><strong>Background: </strong>Cardiovascular diseases (CVDs) remain a leading cause of global morbidity and mortality. Traditional Chinese Medicine (TCM) offers a rich source of bioactive compounds with demonstrated efficacy in CVD management through multi-target mechanisms, including modulation of oxidative stress, inflammation, apoptosis, and autophagy. However, the clinical application of TCM is often hampered by inherent pharmaceutical challenges such as poor solubility, low bioavailability, and non-specific targeting. The emergence of nanoparticle (NP)-based delivery systems presents a transformative strategy to overcome these limitations.</p><p><strong>Objective: </strong>This review comprehensively summarizes recent advances in various NP platforms, including lipid-based, polymeric, inorganic, and biomimetic nanocarriers, for the efficient and targeted delivery of TCM active ingredients in the treatment of CVDs.</p><p><strong>Methods: </strong>A systematic discussion is conducted on how these engineered nanocarriers enhance the stability, bioavailability, and targeted accumulation of TCM compounds at pathological sites, thereby amplifying their therapeutic effects while minimizing off-target toxicity.</p><p><strong>Results: </strong>Nanoparticle-based delivery systems significantly improve the pharmacokinetic and biodistribution profiles of TCM-derived compounds. These platforms enable enhanced therapeutic outcomes in CVD models through improved targeting and reduced systemic side effects.</p><p><strong>Conclusion: </strong>Despite these promising advances, significant challenges remain that hinder clinical translation, including the inherent complexity of multi-component TCM formulations, unresolved nanosafety concerns, lack of standardization in both herbal extracts and nano-formulations, and substantial hurdles in industrial scalability and regulatory approval. By integrating the holistic principles of TCM with the precision of nanotechnology, this evolving field holds immense promise for developing next-generation, targeted therapeutics for cardiovascular diseases, bridging the gap between traditional medicine and modern drug delivery paradigms.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"692-715"},"PeriodicalIF":2.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147691440","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"From Ethnopharmacology to Drug Discovery: The Therapeutic Potential of Anisomeles indica.","authors":"Yihao Long, Yuxian Wang, Yanxia Liu, Xiaoyang He, Huizhen Wang, Congwei Luo, Sijia Chen, Xiaohong Zheng, Jinzhu Yang, Fenfen Peng, Xiaowen Chen, Haibo Long","doi":"10.1002/pca.70071","DOIUrl":"10.1002/pca.70071","url":null,"abstract":"<p><strong>Background: </strong>Anisomeles indica (Lamiaceae) is a traditional medicinal plant widely used in the treatment of inflammatory and systemic disorders. Increasing evidence suggests that it represents a rich source of bioactive natural products with broad pharmacological potential.</p><p><strong>Aims: </strong>This review aims to systematically summarize the phytochemistry, pharmacological activities, safety profiles, and recent advances in drug discovery of Anisomeles indica, with a particular focus on its major diterpenoid constituent, ovatodiolide (OVA).</p><p><strong>Materials and methods: </strong>A comprehensive literature search was conducted across multiple databases, including PubMed, Web of Science, Scopus, and CNKI, covering studies related to ethnopharmacology, phytochemistry, pharmacology, toxicology, and pharmacokinetics of Anisomeles indica and its constituents.</p><p><strong>Results: </strong>Phytochemical studies have identified diverse constituents, particularly macrocyclic diterpenoids such as OVA, which exhibit extensive biological activities including anti-inflammatory, anti-cancer, antiviral, antibacterial, antioxidant, and immunomodulatory effects. Mechanistically, these effects involve key signaling pathways such as NF-κB, STAT3, PI3K/Akt/mTOR, β-catenin, and TGF-β signaling. Despite promising bioactivities, OVA is limited by rapid clearance and poor oral bioavailability. To overcome these limitations, medicinal chemistry efforts have led to the development of optimized derivatives, such as NMP-diepoxyovatodiolide and ACT004, which demonstrate improved pharmacokinetics, enhanced safety, and robust efficacy in preclinical models.</p><p><strong>Discussion: </strong>The pharmacological diversity of Anisomeles indica arises from its complex chemical composition and multi-target mechanisms. However, challenges remain, including variability in extract composition, insufficient clinical validation, and suboptimal pharmacokinetic properties of key compounds.</p><p><strong>Conclusion: </strong>Anisomeles indica represents a promising source of multifunctional therapeutic agents. Continued efforts in standardization, mechanistic validation, and clinical translation, together with the development of pharmacokinetically optimized derivatives, are essential to fully realize its potential as a platform for next-generation drug discovery.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"659-691"},"PeriodicalIF":2.9,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147778635","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Baicalein Alleviates Cardiomyocyte Hypoxia Injury via ESR1-Dependent Modulation of BAX/BCL-XL Balance.","authors":"Yu Xia, Xinyi Zhong, Chenggang Zhang","doi":"10.1002/pca.70069","DOIUrl":"10.1002/pca.70069","url":null,"abstract":"<p><strong>Background: </strong>Hypoxia is a core pathological factor in myocardial injury and is involved in the development of various cardiovascular diseases. Although baicalein shows cardiovascular protective potential, its mechanism against hypoxic injury remains unclear.</p><p><strong>Methods: </strong>H9c2 cardiomyocytes were exposed to sodium sulfite to establish a chemical hypoxia model. Network pharmacology, molecular docking, molecular dynamics simulation, and molecular biology assays were employed to predict the core target and investigate the underlying mechanism.</p><p><strong>Results: </strong>Network pharmacology identified ESR1 as a core target, with stable binding to baicalein confirmed by molecular docking and dynamics simulations. Baicalein alleviated hypoxia-induced oxidative stress by elevating key antioxidant markers and reducing malondialdehyde levels. It also ameliorated energy metabolism disorders, reduced lactate dehydrogenase release, suppressed reactive oxygen species production, and decreased cell apoptosis. Furthermore, baicalein upregulated hypoxia-suppressed ESR1 protein expression and enhanced its co‑localization with the antiapoptotic protein BCL-XL. The cytoprotective effects were abolished by the ESR1 inhibitor fulvestrant.</p><p><strong>Conclusion: </strong>These findings demonstrate that baicalein protects cardiomyocytes against hypoxic injury through an ESR1‑dependent mechanism by modulating the BCL‑XL/BAX apoptotic balance, mitigating oxidative stress, and improving energy metabolism.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"618-635"},"PeriodicalIF":2.6,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147593878","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Harnessing Phytochemicals for Brain Cancer Therapy: Insights Into Medulloblastoma and Glioblastoma Treatment.","authors":"Ilkay Irem Ozbek, Mesra Aktas, Hale Saybasili, Kutlu O Ulgen","doi":"10.1002/pca.70067","DOIUrl":"10.1002/pca.70067","url":null,"abstract":"<p><p>Primary brain tumors are life-threatening diseases. Glioblastoma is the most aggressive type with a poor prognosis. Medulloblastoma is the most common pediatric brain tumor. While surgical treatments often result in recurrences owing to the complex nature of the tumor microenvironment, conventional treatments lower the quality of life of patients by causing serious side effects. Therefore, cutting-edge therapies are required to alleviate patients' burden. Phytochemicals such as curcumin, quercetin, berberine, and resveratrol have been shown as potential therapeutic agents by demonstrating anticancer activity, including the inhibition of cell migration and proliferation, and the induction of apoptosis. This review summarizes the pharmacokinetic and cellular effects of phytochemicals that can be utilized in the treatment of medulloblastoma and glioblastoma by targeting cellular pathways associated with the progression of these diseases. Additionally, the synergistic relationships of these phytochemicals with traditional drugs and the emerging studies that utilize nanotechnology to ensure effective delivery of phytochemicals are covered in this review.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"507-535"},"PeriodicalIF":2.6,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147691481","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Optimal Compatibility of Main Effective Parts of Astragali Radix-Safflower for the Treatment of Cerebral Ischemia/Reperfusion by Pharmacokinetics-Pharmacodynamics Analysis Based on Microdialysis and Liquid Chromatography-Tandem Mass Spectrometry.","authors":"Xinyu Dong, Peng Zhou, Qiaomei Lou, Chang Li, Yu Du, Yu He","doi":"10.1002/pca.70055","DOIUrl":"10.1002/pca.70055","url":null,"abstract":"<p><strong>Purpose: </strong>To research the therapeutic effect and compatibility mechanism of Astragali Radix-Safflower (ARSA) main effective parts in cerebral ischemia/reperfusion injury (CI/RI), especially pharmacokinetics and pharmacodynamics study.</p><p><strong>Method: </strong>Nine formulas of three main effective parts (total flavonoids of Astragali Radix, total saponins of Astragali Radix and safflower yellow pigment) of ARSA were formulated according to L₉ (3⁴) orthogonal design. The sample collection was performed via blood-brain dual-channel microdialysis, combined with LC-MS/MS to quantify six components (hydroxysafflor yellow A, astragaloside IV, calycosin-7-O-β-D-glucopyranoside, ononin, calycosin, and formononetin) of ARSA and five neurotransmitters (aspartic acid, 5-hydroxytryptamine, γ-aminobutyric acid, dopamine, and glutamate) associated with CI/RI. The entropy weight method and the partial least square method were applied to analyze data.</p><p><strong>Results: </strong>The best compatibility prescription of the main effective parts of ARSA was total flavonoids of Astragali Radix 600 mg/kg, total saponins of Astragali Radix 140 mg/kg, and safflower yellow pigment 840 mg/kg, which had a better therapeutic effect and the largest total area under the curve than other formulas. Undergoing CI/RI, glutamate was primarily regulated among the five neurotransmitters, and the components with the greater impact on neurotransmitter modulation were hydroxysafflor yellow A and astragaloside IV.</p><p><strong>Conclusion: </strong>The different compatibility of effective parts of traditional Chinese medicine would influence the pharmacokinetics parameters of each active component in CI/RI rats. Orthogonal compatibility and total statistical moment method provided a way to find the best compatibility. This study provided a pattern for the exploration of traditional Chinese medicine compatibility.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"536-554"},"PeriodicalIF":2.6,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146220770","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An Integrated Identification Strategy for Closely Related Plants Mahonia bealei, Mahonia fortunei, and Berberis soulieana Using Microscopic Characterization, HPLC-QTOF-MS/MS, and DNA Barcoding: A Controversial Case on the Taxonomy of Mahonia and Berberis.","authors":"Fang-Tong Liu, Rui-Bo Sun, Xin-Ru Zhang, Zi-Xuan Ding, Tian-Qi Zhang, Hong-Juan Hou, Yi-Fan Wang, Hui Zhang, Si-Yu Li, Wen-Bo Yang, Mu Zhang, Cheng Qian, Yue-Hua Chen, Hui-Peng Song","doi":"10.1002/pca.70066","DOIUrl":"10.1002/pca.70066","url":null,"abstract":"<p><strong>Introduction: </strong>The taxonomic boundary between Mahonia and Berberis has long been controversial. Mahonia bealei (Fort.) Carr. (MB) and Mahonia fortunei (Lindl.) Fedde (MF) are representative species of Mahonia, while Berberis soulieana Schneid. (BS) represents Berberis. These three plants are often confused in practical medicinal use.</p><p><strong>Objective: </strong>This study aims to elucidate the diagnostic characteristics and taxonomic relationships among MB, MF, and BS. It seeks to provide a potential basis for generic realignment.</p><p><strong>Methodology: </strong>Their structural differences were compared based on macro-morphological features of leaves and microscopic characteristics of roots. Qualitative and quantitative analyses of the chemical components in the three samples were carried out using HPLC-QTOF-MS/MS, followed by a comparison of their chemical fingerprints and the content of major components. Based on multiple DNA barcoding, interspecific genetic distances were calculated and RNA secondary structures were predicted.</p><p><strong>Results: </strong>The differences in the root transverse sections provided a basis for distinguishing the three samples. A total of 67 compounds were identified using HPLC-QTOF-MS/MS, with 24 of these being common to all three samples. While their chemical fingerprints were highly similar, berberine content served as a key differentiating marker. Among DNA barcodes, PsbA3 exhibited the highest sequence variation and largest inter-species genetic distance. These properties made it the optimal barcode for discrimination. Notably, its secondary structure was relatively conserved, exhibiting a unique phenomenon of highly variable sequences with conserved structures.</p><p><strong>Conclusion: </strong>Although several diagnostic features were identified, the marked chemical similarities, conserved DNA barcodes, and shared microscopic characteristics provided novel insights into the taxonomic relationship between the genera Mahonia and Berberis.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"586-603"},"PeriodicalIF":2.6,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147474939","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"TLC-Bioautography-Guided Natural Product Discovery: An Integrated Platform for Rapid Profiling of Plant-Derived Phosphodiesterase Inhibitors.","authors":"Yu-Xin Yuan, Jian-Guo Chen, Zhong-Duo Yang, Cui-Juan Xu, Ling-Bo Liu, Lei-Lei Chen, Yong-Jiao Niu, Qian-Qian Wang, Bing Sun, Tian-Kun Zhao, Ai-Hong Zhao, Sahyun Kim","doi":"10.1002/pca.70068","DOIUrl":"10.1002/pca.70068","url":null,"abstract":"<p><strong>Introduction: </strong>Phosphodiesterase (PDE) inhibitors are important therapeutic targets. There is a need for rapid and efficient screening methods to identify novel PDE inhibitors from complex natural product extracts.</p><p><strong>Objective: </strong>This study aimed to develop an integrated thin-layer chromatography-bioautography (TLC-B) platform for the rapid screening and visual localization of PDE inhibitors in plant-derived samples.</p><p><strong>Material and methods: </strong>Eighteen candidate substrates were synthesized and evaluated. Thymidine 5'-monophosphate-α-naphthyl ester was selected as the optimal enzymatic substrate via HPLC-UV analysis, with Solid Violet B as the chromogenic agent. A four-step TLC-B protocol was established involving separation, sequential spraying of enzyme/substrate solutions, incubation (45°C, 40 min), and visualization. The method was validated using vincristine as a control.</p><p><strong>Results: </strong>The validated method showed high sensitivity, detecting vincristine at 6.25 μg/spot as distinct white inhibition zones against a pink background. Application to an ethyl acetate extract of Lilium pumilum endophyte Z-SDBHTR-4 successfully localized the following three bioactive compounds: curvulinic acid (T1), O-methylcurvulinic acid (T2), and methyl curvulinate (T3).</p><p><strong>Conclusion: </strong>The developed TLC-B platform effectively combines chromatographic separation with bioactivity mapping, creating a streamlined workflow for the discovery of natural product-based enzyme inhibitors. It demonstrates significant potential for accelerating pharmaceutical development.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"604-617"},"PeriodicalIF":2.6,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147491442","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}