Emadeldin M Kamel, Ahmed A Allam, Hassan A Rudayni, Faris F Aba Alkhayl, Noha A Ahmed, Al Mokhtar Lamsabhi
{"title":"Natural Product Modulators of Protein-Protein Interactions: A Comprehensive Review.","authors":"Emadeldin M Kamel, Ahmed A Allam, Hassan A Rudayni, Faris F Aba Alkhayl, Noha A Ahmed, Al Mokhtar Lamsabhi","doi":"10.1002/pca.70054","DOIUrl":"10.1002/pca.70054","url":null,"abstract":"<p><strong>Introduction: </strong>Natural products offer structurally diverse small molecules that modulate protein-protein interactions (PPIs) by disrupting pathogenic complexes or stabilizing beneficial ones, expanding therapeutic opportunities beyond classical enzyme inhibition.</p><p><strong>Objective: </strong>This review synthesizes natural product PPI modulators, emphasizing target coverage, mechanisms of action, reported potency/affinity, structural evidence, and functional outcomes in cellular or organismal models.</p><p><strong>Methods: </strong>We curated published examples of natural products acting as direct PPI inhibitors or indirect modulators and organized them by (i) functional PPI categories-oncogenic complexes (MDM2-p53, BCL-2 family, IAP-caspase), signaling assemblies (Wnt/β-catenin, 14-3-3/adaptor complexes), chaperone/co-chaperone systems (Hsp90 and partners), and immunophilin-mediated interactions (calcineurin-NFAT, mTOR complexes)-and (ii) mechanistic class, including competitive interface blockade, allosteric modulation, covalent modification of one partner, and stabilization via molecular glue or ternary-complex formation. For each class, we summarize representative scaffolds and report binding affinities or IC50/Ki values and structural data when available.</p><p><strong>Results: </strong>Natural products span multiple modes of PPI control and highlight tractable intervention points across diverse proteins. Representative examples include chlorofusin, a fungal metabolite that disrupts p53-MDM2 (IC<sub>50</sub> ~ 4.6 μM); (-)-gossypol, a plant polyphenol acting as a BH3 mimetic that binds BCL-xL (K<sub>i</sub> ~ 0.5 μM); celastrol, a covalent triterpenoid that impairs the Hsp90-Cdc37 complex; and cyclosporin A, FK506, and rapamycin, which form ternary complexes to reprogram immunophilin PPIs.</p><p><strong>Conclusion: </strong>Collectively, these modulators demonstrate PPI druggability and provide chemical probes and lead scaffolds for therapeutic development in cancer, neurodegeneration, infectious disease, and immune disorders.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"375-390"},"PeriodicalIF":2.6,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146166305","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":"Unveiling the Effects of Drying Techniques on Phytochemical Profiles and Quality Attributes of Eriobotryae Folium.","authors":"Ming-Jin Zhang, Ya-Ling An, Fei Huang, Bei-Bei Ding, Hao Wang, Jia-Wei Wang, Zhen-Wei Li, Xiao-Kang Liu, Dai-di Zhang, De-An Guo","doi":"10.1002/pca.70051","DOIUrl":"10.1002/pca.70051","url":null,"abstract":"<p><strong>Introduction: </strong>Drying is a thermodynamic process involving moisture phase transition and migration, crucial for extending the shelf life of traditional Chinese medicinal materials and reducing postharvest degradation. Eriobotryae folium (EF), the dried leaf of Eriobotrya japonica (Thunb.) Lindl. (Rosaceae), is valued for its medicinal and functional food applications. The retention of its bioactive compounds is strongly influenced by drying methods.</p><p><strong>Objectives: </strong>In this study, the effects of shade drying, hot air-drying (50°C, 75°C, 100°C), microwave drying, and vacuum freeze-drying on the chemical composition and antioxidant activity of EF were systematically evaluated.</p><p><strong>Materials and methods: </strong>Using fingerprint profiling and multivariate statistical analysis, chlorogenic acid, cryptochlorogenic acid, and neochlorogenic acid (CGAs) were identified as key differential components. Spectrum-effect relationship analysis, based on Pearson product-moment correlation analysis (PPMC) and gray relational analysis (GRA), confirmed these three compounds as not only distinguishing markers under different drying conditions but also major bioactive constituents contributing to EF's therapeutic effects. Thus, they are proposed as potential quality markers. A reliable quantitative method was developed for their determination, combined with final moisture content and visual assessment of appearance, to analyze which drying method yielded samples with the best overall quality.</p><p><strong>Results: </strong>CGAs were confirmed as key differential components. Spectrum-effect relationship analysis confirmed these three compounds as distinguishing markers and major bioactive constituents. Microwave-dried samples exhibited the best overall quality.</p><p><strong>Conclusion: </strong>This study established an integrated evaluation system-\"fingerprint profiling-spectrum-effect correlation-targeted component quantification\"-providing a practical and scientific approach for EF quality control and offering a reference for standardizing processing of leaf-derived herbal medicines.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"461-472"},"PeriodicalIF":2.6,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147356086","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}
Baihao Lao, Jingxian Zhang, Jian Sun, Heng Zhou, Hong Yu, Yingying Ran, Fan Huang, Yingying Shen, Xianxian Li, Xiuhong Mao, Shen Ji, Qing Hu
{"title":"Discovery and Absolute Quantification of Water-Soluble Signature Peptides via LC-MS/MS Based on Proteomics for Quality Evaluation of Goat Horn.","authors":"Baihao Lao, Jingxian Zhang, Jian Sun, Heng Zhou, Hong Yu, Yingying Ran, Fan Huang, Yingying Shen, Xianxian Li, Xiuhong Mao, Shen Ji, Qing Hu","doi":"10.1002/pca.70049","DOIUrl":"10.1002/pca.70049","url":null,"abstract":"<p><strong>Introduction: </strong>Goat horn is a primary substitute for the endangered Saiga antelope horn in traditional medicines. Current quality control (QC) methods lack specificity to effectively detect economically motivated adulteration with horns from other Bovidae species.</p><p><strong>Objective: </strong>This study is aimed at discovering the species-specific peptides and to develop a reliable mass spectrometry-based method for authenticating goat horn and quantifying its signature peptides.</p><p><strong>Methods: </strong>A label-free proteomics strategy was employed to characterize the tryptic digests across five Bovidae species: goat horn (originated from Capra hircus), sheep horn (Ovis aries), buffalo horn (Bubalus bubalis), cattle horn (Bos taurus), and yak horn (Bos grunniens) on a nanoLC-Orbitrap mass spectrometry and screen signature peptides. A novel ultrasound-assisted simultaneous extraction-enzymolysis (UASEE) method was developed for sample preparation. An absolute quantification for seven goat horn peptides was established on UHPLC-MS/MS. Twenty-two batches of goat horn samples were analyzed.</p><p><strong>Results: </strong>Thirteen signature peptides enabling unambiguous differentiation of five Bovidae species were identified. The UASEE method reduced the sample preparation time from over 24-6 h. The quantification method demonstrated satisfactory linearity (r ≥ 0.997), precision (RSD < 8.2%), repeatability (RSD < 5.8%), stability (RSD < 9.2%), and accuracy (recoveries 84.6%-114.2%, RSD < 13.9%). Based on the quantification results, GHpep 7 (mean 0.224 mg/g) and GHpep 11 (mean 0.137 mg/g) were proposed as the optimal QC markers due to high abundance and minimal batch variability (RSD < 15%).</p><p><strong>Conclusion: </strong>This work provides a platform for signature peptide discovery and absolute quantification using UASEE and LC-MS/MS for quality evaluation of goat horn. It effectively addresses adulteration challenges and establishes a foundation for QC standards of goat horn.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"432-441"},"PeriodicalIF":2.6,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145945665","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}
Ahad Nourmohammad, Niloofar Zonoubi, Nima Ghavamikia
{"title":"Therapeutic Potential and Mechanisms of Curcumin in Cardiovascular Diseases: A Comprehensive Review.","authors":"Ahad Nourmohammad, Niloofar Zonoubi, Nima Ghavamikia","doi":"10.1002/pca.70045","DOIUrl":"10.1002/pca.70045","url":null,"abstract":"<p><strong>Background: </strong>Curcumin is recognized for its therapeutic potential in cardiovascular diseases (CVDs), with effects on cardiomyocytes, vascular function, and hypertrophy.</p><p><strong>Objective: </strong>This review aims to evaluate curcumin's therapeutic effects, mechanisms of action, and safety in CVD management.</p><p><strong>Methods: </strong>A comprehensive review of existing literature was conducted, focusing on curcumin's impact on ischemia, hypoxia, myocardial hypertrophy, fibrosis, and endothelial function.</p><p><strong>Results: </strong>Curcumin protects cardiomyocytes, enhances vascular function, and exhibits inconsistent effects on cholesterol accumulation in macrophages.</p><p><strong>Conclusion: </strong>While curcumin shows promise as a complementary agent in CVD management, further research, particularly large-scale clinical trials, is essential to validate its efficacy and safety.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"348-361"},"PeriodicalIF":2.6,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146093697","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":"Integrating HPLC Fingerprinting, Gray Relational Analysis, and In Vitro-In Vivo Evaluation of Xiaochaihu Decoction and Its Nano-Phase.","authors":"Long Zhang, Yihong Qiu, Yanhong Wang, Lianzhi Wang, Yumeng Liu, Xiaoying Zhou, Jiayi Li, Qingxia Guan","doi":"10.1002/pca.70050","DOIUrl":"10.1002/pca.70050","url":null,"abstract":"<p><strong>Background: </strong>Self-assembled nano-systems (SANS) formed in traditional Chinese medicine (TCM) decoctions have recently emerged as promising carriers for enhancing the oral bioavailability of poorly soluble components. However, the pharmacokinetic characteristics of SANS in Xiaochaihu (XCH) decoction remain insufficiently investigated.</p><p><strong>Objective: </strong>This study aimed to clarify the component distribution and pharmacodynamic relevance of the nanoemulsion phase of XCH decoction (N-XCH) and to assess its potential to improve pharmacokinetics and tissue targeting.</p><p><strong>Methods: </strong>N-XCH was characterized by particle size analysis, zeta-potential measurement, TEM, UV-Vis, and FTIR spectroscopy. HPLC fingerprinting was used to compare the distribution of active components among the four phase states of XCH decoction. Gray relational analysis (GRA) was applied to relate index components to hepatoprotective and antipyretic endpoints. In vitro release, in vivo pharmacokinetic, and tissue distribution studies were performed to evaluate the release behavior and in vivo disposition of representative components.</p><p><strong>Results: </strong>Fingerprint and GRA analyses indicated that N-XCH is the optimal dissolution phase for co-loading active constituents, and identified saikosaponin A as a key component associated with both hepatoprotective and antipyretic effects. In vitro, N-XCH displayed sustained-release behavior obeying Weibull kinetics with Fickian diffusion. In rats, N-XCH significantly increased the AUC of baicalin, wogonoside, liquiritin, and glycyrrhetinic acid compared with the decoction, while maintaining similar or slightly reduced Cmax values and altered tissue exposure profiles with enhanced hepatic uptake (RUE > 1) for multiple analytes.</p><p><strong>Conclusion: </strong>N-XCH, as a self-assembled nanoemulsion phase in XCH decoction, markedly improves the systemic exposure and liver targeting of representative actives without excessive peak concentrations. These findings highlight the potential of SANS in TCM decoctions to optimize oral bioavailability and organ targeting, and provide an integrated analytical-pharmacokinetic framework for linking spectrum-effect relationships with nano-phase behavior.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"442-460"},"PeriodicalIF":2.6,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145990307","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}
Xi Mei, Yabo Shi, Bin Wang, Rong Xue, Qian Zhang, Chunqin Mao, Tulin Lu, Lin Li
{"title":"E-Eye, Flash GC E-Nose, and HS-GC-MS Combined With Chemometrics to Identify the Different Processed Products of Cyperus rotundus.","authors":"Xi Mei, Yabo Shi, Bin Wang, Rong Xue, Qian Zhang, Chunqin Mao, Tulin Lu, Lin Li","doi":"10.1002/pca.70044","DOIUrl":"10.1002/pca.70044","url":null,"abstract":"<p><strong>Introduction: </strong>Cyperus rotundus (CR) has been widely explored for the treatment and prevention of diseases. In traditional Chinese medicine (TCM), it is commonly used to treat liver diseases, abdominal pain, irregular menstruation, and dysmenorrhea. It has various processed products in clinical prescription; however, the quality distinctions among different processed products of CR remain unexplored.</p><p><strong>Objectives: </strong>To explore the quality distinctions in color, flavor, and volatile compounds among four processed products of CR.</p><p><strong>Methods: </strong>Eleven batches for each of the four processed products of CR were prepared. The color of the powders was determined utilizing the electronic eye (E-eye). The flavor information of each sample was analyzed with flash gas chromatography electronic nose (Flash GC e-nose). The volatile components were characterized using headspace gas chromatography-mass spectrometry (HS-GC-MS), and the data were analyzed employing chemometric methods.</p><p><strong>Results: </strong>The color parameters L*, a*, and b* were consistently obtained by E-eye, and four discriminant functions were established to distinguish different CR products rapidly. Using the Flash GC e-nose, 20 odor compounds were identified, among which 2-methylpropanal, 2-methylbutanal, methyl 2-methylbutyrate, and ethyl 2-methylcrotonate were generated after vinegar-processing, wine-processing, and stir-frying. A total of 36 volatile compounds were identified by HS-GC-MS with acetic acid and furfural being newly generated. Four potential differential chemical markers were selected.</p><p><strong>Conclusion: </strong>Overall, this study provides novel ideas and methods for the identification and quality evaluation of four processed products of CR. Furthermore, it also provides a reference for standardizing the processing technology of TCM.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"391-401"},"PeriodicalIF":2.6,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145912759","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":"Danqi Pill (DQP) Attenuates OGD-Induced Injury in HUVECs via SHP2-ROS-NLRP3 Axis.","authors":"Xinyi Zhong, Hui Wang, Nan Li, Mijia Zhou, Hanyan Xie, Binghua Tang, Tian Tian, Tianhua Liu, Dongqing Guo","doi":"10.1002/pca.70047","DOIUrl":"10.1002/pca.70047","url":null,"abstract":"<p><strong>Background: </strong>The NLRP3 inflammasome-mediated inflammatory response plays a critical role in endothelial dysfunction. Danqi pill (DQP), a Chinese patent medicine composed of Salvia miltiorrhiza and Panax notoginseng, has demonstrated protective effects on endothelial cells, though its underlying mechanisms remain incompletely understood.</p><p><strong>Methods: </strong>Human umbilical vein endothelial cells (HUVECs) were subjected to oxygen-glucose deprivation (OGD) to simulate ischemic injury. Cell viability, migration, reactive oxygen species (ROS) production, mitochondrial membrane potential, and protein expression related to the NLRP3 inflammasome and Src homology 2-containing protein tyrosine phosphatase 2 (SHP2) were assessed.</p><p><strong>Results: </strong>DQP (600 μg/mL) protected HUVECs against OGD-induced injury by enhancing cell viability and migration, reducing ROS production and cell death, and preserving mitochondrial membrane potential. Mechanistically, DQP promoted the translocation of SHP2 to mitochondria, which subsequently suppressed ROS generation and NLRP3 inflammasome activation.</p><p><strong>Conclusion: </strong>These findings reveal that DQP attenuates OGD-induced injury in HUVECs via SHP2-ROS-NLRP3 axis.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"402-413"},"PeriodicalIF":2.6,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146011430","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}
Mohammed Burhan Uddin, Md Nasimul Haque Shipon, Rituparna Biswas Suma, Md Anisur Rahman, Ali G Alkhathami, Emon Mia, Abul Bashar Ripon Khalipha, Khadija Akter, Md Sakib Al Hasan
{"title":"Anticancer Activity of Corosolic Acid With Botanical Sources, Biopharmaceutical Profile, Mechanistic Insight, Toxicity, and Clinical Evidence.","authors":"Mohammed Burhan Uddin, Md Nasimul Haque Shipon, Rituparna Biswas Suma, Md Anisur Rahman, Ali G Alkhathami, Emon Mia, Abul Bashar Ripon Khalipha, Khadija Akter, Md Sakib Al Hasan","doi":"10.1002/pca.70052","DOIUrl":"10.1002/pca.70052","url":null,"abstract":"<p><strong>Introduction: </strong>Corosolic acid (CRS) is a naturally occurring pentacyclic triterpenoid primarily isolated from Lagerstroemia speciosa and other medicinal plants and has attracted growing interest because of its promising anticancer properties.</p><p><strong>Objectives: </strong>This review provides a comprehensive synthesis of the botanical sources, biopharmaceutical characteristics, molecular mechanisms of action, toxicological profile, and clinical evidence associated with CRS.</p><p><strong>Materials and methods: </strong>A comprehensive literature search was conducted across major scientific databases, including PubMed, Google Scholar, Web of Science, ScienceDirect, SpringerLink, and Wiley Online, covering studies published up to April 2025. Peer-reviewed articles investigating the anticancer activity, pharmacology, toxicity, pharmacokinetics, and clinical relevance of CRS were included.</p><p><strong>Results: </strong>Preclinical evidence demonstrates that CRS exerts broad-spectrum anticancer activity by inducing apoptosis, autophagy, ferroptosis, and cytotoxicity, while inhibiting tumor cell proliferation, metastasis, and survival signaling pathways, including PI3K/Akt/mTOR, NF-κB, STAT3, and YAP/TAZ. Emerging data also highlight its immunomodulatory role, particularly through suppression of Th17-mediated inflammatory responses, which may further contribute to its antitumor effects. Toxicological evaluations indicate that CRS possesses a favorable safety profile at therapeutic doses; however, its clinical translation is hindered by poor aqueous solubility and limited oral bioavailability. Recent advances in formulation strategies and structural modification approaches show potential for overcoming these limitations.</p><p><strong>Conclusion: </strong>Overall, this review integrates current knowledge, identifies critical research gaps, and emphasizes the need for well-designed clinical trials to establish CRS as a viable multitarget anticancer agent.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"362-374"},"PeriodicalIF":2.6,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146086764","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":"Ameliorating Effects of Murraya paniculata (L.) Jack Extract on Arthritis via Suppressing Multi-Target-Mediated Synovial Hyperplasia, Inflammation, and Oxidative Stress.","authors":"Guoping Wu, Yuxin Fan, Junming Chen, Qiushuo Ma, Yawen Yao, Wenbo Xie, Hua Yu","doi":"10.1002/pca.70048","DOIUrl":"10.1002/pca.70048","url":null,"abstract":"<p><strong>Introduction: </strong>Rheumatoid arthritis (RA) is a chronic autoimmune disorder characterized by persistent inflammation, synovial hyperplasia, and osteochondral damage. Murraya paniculata (L.) Jack (MP), a botanical source of Murrayae Folium et Cacumen (MFC), has not previously been investigated for its potential arthritis-protective effects and underlying mechanisms, prompting our study of MP in this context.</p><p><strong>Objectives: </strong>This study is aimed at evaluating the ameliorating effects of MP and elucidating its underlying mechanisms in RA.</p><p><strong>Methods: </strong>The chemical composition of MP extract was analyzed using ultra-performance liquid chromatography (UPLC). The anti-arthritic effects of MP extract were assessed in collagen-induced arthritis (CIA) rats and interleukin (IL)-1β-stimulated SW982 cells.</p><p><strong>Results: </strong>UPLC quantification identified four major constituents: luteolin tetramethylether (0.547 ± 0.012%), 5,7,3',4',5'-pentamethoxyflavone (1.558 ± 0.030%), 3',4',5,5',6,7-hexamethoxyflavone (0.273 ± 0.006%), and 5-demethylnobiletin (0.848 ± 0.023%). In vivo, MP alleviated arthritis in CIA rats by reducing clinical symptoms (including arthritis index, hind paw volume/swelling, and histopathological joint damage), suppressing inflammatory responses, and attenuating oxidative stress. In vitro, MP mitigated pathological changes in IL-1β-stimulated SW982 cells by inhibiting cell proliferation and migration, dampening inflammation, and reducing oxidative stress. Furthermore, network pharmacology and transcriptomic analyses guided the investigation of MP's regulatory effects on key RA-related targets. Specifically, MP downregulated IL-1β-induced overexpression of iNOS, COX-2, and MMP2/9 in SW982 cells and inhibited AP-1/NF-κB activation. These effects were confirmed in vivo, where MP suppressed MMP2/9 expression and blocked AP-1/NF-κB activation in CIA rats.</p><p><strong>Conclusions: </strong>Integrating phytochemical profiling, in vivo and in vitro models, network pharmacology-transcriptomics, and target validation, this study demonstrates that MP exerts anti-arthritic effects via modulating proliferation-inflammation-oxidation crosstalk.</p>","PeriodicalId":20095,"journal":{"name":"Phytochemical Analysis","volume":" ","pages":"414-431"},"PeriodicalIF":2.6,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145990304","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":"https://doi.org/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":""},"PeriodicalIF":2.6,"publicationDate":"2026-03-20","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}