Journal of pharmaceutical analysis最新文献

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Dual-mechanism driven adsorption on silica microspheres enables precision pharmacokinetic profiling of liposomal therapeutics. 双机制驱动吸附二氧化硅微球使脂质体治疗药物的精确药代动力学分析。
IF 8.9
Journal of pharmaceutical analysis Pub Date : 2026-09-01 Epub Date: 2026-07-08 DOI: 10.1016/j.jpha.2026.101714
Jinjing Che, Yixuan Zhang, Mei Yuan, Qianqian Bai
{"title":"Dual-mechanism driven adsorption on silica microspheres enables precision pharmacokinetic profiling of liposomal therapeutics.","authors":"Jinjing Che, Yixuan Zhang, Mei Yuan, Qianqian Bai","doi":"10.1016/j.jpha.2026.101714","DOIUrl":"10.1016/j.jpha.2026.101714","url":null,"abstract":"","PeriodicalId":94338,"journal":{"name":"Journal of pharmaceutical analysis","volume":"16 9","pages":"101714"},"PeriodicalIF":8.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13602245/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149043049","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
NAT10 aggravates psoriasis by promoting keratinocytes fatty acid synthesis via stable FASN transcription. NAT10通过稳定的FASN转录促进角化细胞脂肪酸合成,从而加重银屑病。
IF 8.9
Journal of pharmaceutical analysis Pub Date : 2026-09-01 Epub Date: 2026-02-17 DOI: 10.1016/j.jpha.2026.101590
Weibo Tang, Jingling Shen, Jiaxin Liu, Chunhui Jiang, Wenya Liu, Mengyao Xiao, Jindan Dai, Wenjie Gao, Junjie Lu, Chunyi Hu, Yonghuan Song, Ye Xu, Zhongxin Zhu, Weitao Cong
{"title":"NAT10 aggravates psoriasis by promoting keratinocytes fatty acid synthesis via stable FASN transcription.","authors":"Weibo Tang, Jingling Shen, Jiaxin Liu, Chunhui Jiang, Wenya Liu, Mengyao Xiao, Jindan Dai, Wenjie Gao, Junjie Lu, Chunyi Hu, Yonghuan Song, Ye Xu, Zhongxin Zhu, Weitao Cong","doi":"10.1016/j.jpha.2026.101590","DOIUrl":"10.1016/j.jpha.2026.101590","url":null,"abstract":"<p><p>RNA modifications have emerged as critical regulators of cellular function and disease pathogenesis; however, their contribution to psoriasis remains unclear. Here, we report that N-acetyltransferase 10 (NAT10) expression is markedly elevated in the epidermis of patients with psoriasis and in imiquimod (IMQ)-induced lesions. Single-cell RNA sequencing further identifies NAT10 upregulation in hyperproliferative and basal keratinocyte subsets. Keratinocyte-specific deletion of NAT10 attenuates IMQ-induced psoriatic phenotypes in mice. Integrative profiling of RNA sequencing and N4-acetylcytidine (ac4C) immunoprecipitation sequencing reveals fatty acid synthase (FASN) as a direct downstream target of NAT10. Mechanistically, NAT10 catalyzes ac4C RNA modification to enhance the stability of FASN mRNA, thereby driving fatty acid metabolic reprogramming and promoting keratinocyte proliferation. This metabolic shift contributes to epidermal hyperplasia and inflammation in psoriasis. Notably, pharmacological inhibition of NAT10 with remodelin alleviates disease severity <i>in vivo</i> and <i>in vitro</i>. Together, these findings identify a NAT10-dependent ac4C regulatory axis that links epitranscriptomic control to metabolic dysregulation in keratinocytes and highlight NAT10 as a promising therapeutic target for psoriasis.</p>","PeriodicalId":94338,"journal":{"name":"Journal of pharmaceutical analysis","volume":"16 9","pages":"101590"},"PeriodicalIF":8.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13499481/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148804390","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Fusion of tradition and modernity: Advances in Chinese materia medica self-assembly-driven study on compatibility and processing. 传统与现代的融合:中药自组装驱动的配伍与加工研究进展。
IF 8.9
Journal of pharmaceutical analysis Pub Date : 2026-09-01 Epub Date: 2026-01-16 DOI: 10.1016/j.jpha.2026.101554
Li Li, Jiawei Li, Xudong He, Yue Zhou, Juanhong Lei, Shibo Yu, Dan Li, Pingyan Ding, Oluwaniyi Isaiah Adejobi, Xia Chen, Mei Zhang, Jie Yu
{"title":"Fusion of tradition and modernity: Advances in Chinese materia medica self-assembly-driven study on compatibility and processing.","authors":"Li Li, Jiawei Li, Xudong He, Yue Zhou, Juanhong Lei, Shibo Yu, Dan Li, Pingyan Ding, Oluwaniyi Isaiah Adejobi, Xia Chen, Mei Zhang, Jie Yu","doi":"10.1016/j.jpha.2026.101554","DOIUrl":"10.1016/j.jpha.2026.101554","url":null,"abstract":"<p><p>Rooted in Chinese medicine theory, the compatibility and processing of Chinese materia medica (CMM) have played a vital role in clinical practice for millennia. These practices employ multifaceted approaches such as the Monarch-Minister-Assistant-Guide, the four properties, Qiqing (seven effects), and various processing techniques to enhance therapeutic efficacy, reduce toxicity, improve palatability, and generate novel pharmacological effects. Despite their longstanding history, the global application of CMM remains limited, largely due to an incomplete understanding of the mechanisms underlying compatibility and processing. Recent studies have demonstrated that bioactive components in CMM often undergo spontaneous self-assembly, forming nanoscale aggregates through noncovalent interactions. These self-assembled aggregates offer a novel material basis for pharmacological activities, addressing the limitations of traditional decoctions and offering new perspectives for the development and application of CMM formulations. This review compiles and analyzes 121 academic publications published from 1995 to 2025 that explore the intersection of nanotechnology with CMM compatibility or processing. It outlines the bioactive constituents and mechanisms involved in the formation of CMM self-assembled aggregates. Furthermore, it examines methods for separation and preparation, advanced characterization techniques, and the pharmacokinetics/pharmacodynamics (PK/PD) of CMM self-assembled aggregates. Focal attention is given to the role of self-assembly in enhancing the compatibility and processing of CMM. In addition, the environmental impact and sustainability of using CMM self-assembled aggregates are also discussed. Finally, the review identifies five unresolved challenges and proposes six future research directions, with the aim of advancing the study of CMM compatibility and processing, and promoting the internationalization, modernization, and precision application of CMM.</p>","PeriodicalId":94338,"journal":{"name":"Journal of pharmaceutical analysis","volume":"16 9","pages":"101554"},"PeriodicalIF":8.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13546910/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148908492","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
In situ construction of an SPR biosensor using cell-free protein synthesis technology and its application in drug screening for CXCR4. 无细胞蛋白合成技术原位构建SPR生物传感器及其在CXCR4药物筛选中的应用
IF 8.9
Journal of pharmaceutical analysis Pub Date : 2026-09-01 Epub Date: 2026-03-24 DOI: 10.1016/j.jpha.2026.101613
Xiaofei Wang, Yanting Wang, Hao Chen, Ningqi Xia, Jiayu Gu, Linfeng Zhang, Dongyao Wang, Bin Lu, Diya Lv, Xiaofei Chen, Yan Cao, Yifeng Chai
{"title":"<i>In situ</i> construction of an SPR biosensor using cell-free protein synthesis technology and its application in drug screening for CXCR4.","authors":"Xiaofei Wang, Yanting Wang, Hao Chen, Ningqi Xia, Jiayu Gu, Linfeng Zhang, Dongyao Wang, Bin Lu, Diya Lv, Xiaofei Chen, Yan Cao, Yifeng Chai","doi":"10.1016/j.jpha.2026.101613","DOIUrl":"10.1016/j.jpha.2026.101613","url":null,"abstract":"<p><p>Surface plasmon resonance (SPR) biosensor has emerged as a transformative tool in high-throughput drug screening and label-free analysis of biomolecular interactions. However, a critical limitation of SPR lies in its stringent requirement for highly purified proteins to ensure reliable quantification of binding affinities and kinetic parameters. In order to address the limitations, the lentiviral particle (LVP) and styrene-maleic acid (SMA) polymer have been previously developed to extract and stabilize transmembrane proteins (TMs) indirectly and thus to detect ligands interaction with TMs by SPR biosensor. The present study proposes a high-throughput SPR-based drug screening system that utilizes cell-free protein synthesis (CFPS) to achieve <i>in situ</i> purification and immobilization of TMs on SPR biosensors. First, C-X-C chemokine receptor 4 (CXCR4) protein with histidine (His)-tag was prepared by CFPS. Then, two types of nickel-nitrilotriacetic acid (Ni-NTA) biosensors, modified with carboxymethylated dextran (CMD) and coated with polycarboxylate hydrogel coating (HC) matrix, were compared with classical carboxymethylated dextran 5 (CM5) biosensor in order to determine the optimal strategy for coupling the CXCR4-CFPS protein. The CMD-NTA/SPR biosensor was next applied to screen for CXCR4 ligands from 96 natural products. Finally, glycyrrhizic acid and ginsenoside Re were proved to be function as CXCR4 inhibitors by affinity test, molecular docking, and cell migration assay. The combination of CFPS with SPR technologies facilitates <i>in-situ</i> purification and immobilization of target proteins in a single step, thereby significantly enhancing the efficiency of SPR assay procedures. The system has broad applicability for targeting various challenging TMs and provides potential candidates for subsequent drug development.</p>","PeriodicalId":94338,"journal":{"name":"Journal of pharmaceutical analysis","volume":"16 9","pages":"101613"},"PeriodicalIF":8.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13587802/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149009691","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Genipin induces liver injury by disrupting the CPS1-regulated urea cycle and redox homeostasis. Genipin通过破坏cps1调控的尿素循环和氧化还原稳态诱导肝损伤。
IF 8.9
Journal of pharmaceutical analysis Pub Date : 2026-09-01 Epub Date: 2026-05-07 DOI: 10.1016/j.jpha.2026.101647
Hongzhan Xu, Xinhui Huang, Yujia Zhang, Shilin Gong, Yusha Luo, Yichao Fang, Xiaolan Hu, Miaomiao Luo, Yujia Zhai, Fangyuan Gao, Xinglong Chen, Rongping Zhang, Longshan Zhao, Yong Wang, Jian-Lin Wu, Xin Zhang, Huiqing Liang, Jun Wen, Tingting Zhou
{"title":"Genipin induces liver injury by disrupting the CPS1-regulated urea cycle and redox homeostasis.","authors":"Hongzhan Xu, Xinhui Huang, Yujia Zhang, Shilin Gong, Yusha Luo, Yichao Fang, Xiaolan Hu, Miaomiao Luo, Yujia Zhai, Fangyuan Gao, Xinglong Chen, Rongping Zhang, Longshan Zhao, Yong Wang, Jian-Lin Wu, Xin Zhang, Huiqing Liang, Jun Wen, Tingting Zhou","doi":"10.1016/j.jpha.2026.101647","DOIUrl":"10.1016/j.jpha.2026.101647","url":null,"abstract":"<p><p>Genipin (GP) is the key metabolite of geniposide (GE), the primary active component of the traditional Chinese medicine Gardeniae Fructus. Its hepatotoxicity poses a potential risk to safe clinical administration, while its core pathophysiological mechanism remains unclear. This study systematically elucidated the molecular mechanisms of GP-induced hepatotoxicity through integrated multi-omics and functional validation. GP treatment induced significant liver damage and oxidative stress in rats, characterized by elevated serum transaminases (alanine aminotransferase (ALT) increased by approximately 63.5-fold; aspartate aminotransferase (AST) by 18.6-fold), an approximately 1.8-fold decrease in superoxide dismutase (SOD) activity, and an approximately 10-fold accumulation of malondialdehyde (MDA) (all <i>P</i> < 0.001). Metabolomic and proteomic analyses revealed that GP binds to carbamoyl phosphate synthetase 1 (CPS1), triggering urea cycle dysfunction marked by citrulline depletion and significant downregulation of its downstream product fumarate. <i>In vitro</i> experiments confirmed that disrupting CPS1 impairs the urea cycle and induces oxidative stress, while CPS1 overexpression or exogenous fumarate supplementation significantly reversed oxidative stress. Clinical sample analysis revealed similar urea cycle metabolic disturbances, characterized by citrulline depletion and reduced fumarate levels, in plasma from patients with liver injury due to inappropriate use of Gardeniae Fructus-containing formulas, confirming clinical relevance. This study reveals a novel hepatotoxic mechanism whereby GP targets CPS1 to disrupt the urea cycle, reducing fumarate production and impairing nuclear factor erythroid 2-related factor 2 (Nrf2)-mediated antioxidant defense, thereby inducing oxidative stress. These findings provide a scientific basis for improving the safety evaluation and rational clinical use of Gardeniae Fructus-containing preparations.</p>","PeriodicalId":94338,"journal":{"name":"Journal of pharmaceutical analysis","volume":"16 9","pages":"101647"},"PeriodicalIF":8.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13601060/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149043025","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Therapeutic potential of traditional Chinese medicine-derived formulations and extracts in Candida infections: Current trends and future directions. 中药衍生制剂和提取物治疗念珠菌感染的潜力:当前趋势和未来方向。
IF 8.9
Journal of pharmaceutical analysis Pub Date : 2026-09-01 Epub Date: 2026-01-06 DOI: 10.1016/j.jpha.2026.101549
Maozhu Liu, Cuilin He, Xiwen Wang, Jiao Ye, Enqiang Chen, Tao Tao
{"title":"Therapeutic potential of traditional Chinese medicine-derived formulations and extracts in <i>Candida</i> infections: Current trends and future directions.","authors":"Maozhu Liu, Cuilin He, Xiwen Wang, Jiao Ye, Enqiang Chen, Tao Tao","doi":"10.1016/j.jpha.2026.101549","DOIUrl":"10.1016/j.jpha.2026.101549","url":null,"abstract":"<p><p><i>Candida</i> infections have emerged as a global public health crisis with elevating morbidity and mortality. Currently, the major obstacles to managing <i>Candida</i> infections are limited antifungal options, increasing fungal resistance, and serious adverse drug reactions, all of which significantly compromise patient prognosis. Consequently, developing innovative and effective therapeutic agents to address these challenges is exceedingly demanded. Accumulating evidence highlights that traditional Chinese medicines (TCMs) possess favorable antifungal properties, offering advantages such as improved efficacy, reduced resistance, and fewer side effects. As a result, TCMs are increasingly recognized as promising sources for discovering novel antifungals. In light of this, this review summarizes the relevant literature published over the last decade (2014-2024), providing an exhaustive overview of the anti-<i>Candida</i> effects of TCM-derived formulations and bioactive extracts, along with their underlying mechanisms. Collectively, we emphasize that future research trends in this field should focus on continuously identifying novel anti-<i>Candida</i> drugs derived from TCMs and elucidating their exact mechanisms of action. In addition, clinical trials should be conducted to validate the antifungal efficacy of TCMs in humans, ultimately advancing their future medical applications.</p>","PeriodicalId":94338,"journal":{"name":"Journal of pharmaceutical analysis","volume":"16 9","pages":"101549"},"PeriodicalIF":8.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13560540/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148946433","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Advancements in pharmaceutical research on traditional Chinese medicine-metal complexes. 中药-金属配合物的药学研究进展。
IF 8.9
Journal of pharmaceutical analysis Pub Date : 2026-09-01 Epub Date: 2026-01-05 DOI: 10.1016/j.jpha.2026.101548
Minyu Han, Jinning Mao, Guodong Liu, Peng Xue
{"title":"Advancements in pharmaceutical research on traditional Chinese medicine-metal complexes.","authors":"Minyu Han, Jinning Mao, Guodong Liu, Peng Xue","doi":"10.1016/j.jpha.2026.101548","DOIUrl":"10.1016/j.jpha.2026.101548","url":null,"abstract":"<p><p>Traditional Chinese medicine (TCM) has gained significant recognition as an adjuvant treatment modality for cancer, infections, and inflammatory diseases, owing to its outstanding antitumor, antimicrobial, and anti-inflammatory properties. With the advancement of TCM-based coordination chemistry, TCM-metal complexes have attracted growing interest in recent years. These novel compounds, formed by integrating traditional TCM components with metal ions, not only enhance the therapeutic efficacy of TCM but also exhibit unique biological activities. This review highlights the design strategies and pharmaceutical applications of various categories of TCM-metal complexes, including those based on polyphenols, alkaloids, and other drug-metal conjugates. By applying modern nanobiotechnology alongside TCM principles, TCM-metal complexes demonstrate considerable potential for the diagnosis and treatment of major diseases. Finally, this review discusses the challenges and future prospects of TCM-metal complexes in clinical applications, providing valuable insights to guide further research and development in this emerging field.</p>","PeriodicalId":94338,"journal":{"name":"Journal of pharmaceutical analysis","volume":"16 9","pages":"101548"},"PeriodicalIF":8.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13545372/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148898841","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovery of organelle-targeted active ingredients combination from Qifu decoction to treat heart failure via modulating cardiac mitochondria-lysosome dysfunction and contacts. 通过调节心脏线粒体-溶酶体功能障碍及接触,发现七腑汤细胞器靶向活性成分组合治疗心衰。
IF 8.9
Journal of pharmaceutical analysis Pub Date : 2026-09-01 Epub Date: 2026-05-07 DOI: 10.1016/j.jpha.2026.101648
Xin Ding, Qian Zhou, Ya Zhang, Junli Liang, Xuemei Su, Hongrui Ma, Ping Li, Jing Ma, Guangguo Tan
{"title":"Discovery of organelle-targeted active ingredients combination from Qifu decoction to treat heart failure via modulating cardiac mitochondria-lysosome dysfunction and contacts.","authors":"Xin Ding, Qian Zhou, Ya Zhang, Junli Liang, Xuemei Su, Hongrui Ma, Ping Li, Jing Ma, Guangguo Tan","doi":"10.1016/j.jpha.2026.101648","DOIUrl":"10.1016/j.jpha.2026.101648","url":null,"abstract":"","PeriodicalId":94338,"journal":{"name":"Journal of pharmaceutical analysis","volume":"16 9","pages":"101648"},"PeriodicalIF":8.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13494894/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148804356","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Preparation and collaborative study of a recombinant adeno-associated virus (rAAV) genome copy number reference material. 重组腺相关病毒(rAAV)基因组拷贝数参考物质的制备与合作研究。
IF 8.9
Journal of pharmaceutical analysis Pub Date : 2026-09-01 Epub Date: 2026-05-15 DOI: 10.1016/j.jpha.2026.101660
Hua Bi, Wenxiu Hou, Youxue Ding, Haohang Sun, Zhihao Fu, Xinchang Shi, Wei Jiang, Zengmin Du, Dening Pei, Xiang Li, Xi Qin, Chenggang Liang
{"title":"Preparation and collaborative study of a recombinant adeno-associated virus (rAAV) genome copy number reference material.","authors":"Hua Bi, Wenxiu Hou, Youxue Ding, Haohang Sun, Zhihao Fu, Xinchang Shi, Wei Jiang, Zengmin Du, Dening Pei, Xiang Li, Xi Qin, Chenggang Liang","doi":"10.1016/j.jpha.2026.101660","DOIUrl":"https://doi.org/10.1016/j.jpha.2026.101660","url":null,"abstract":"","PeriodicalId":94338,"journal":{"name":"Journal of pharmaceutical analysis","volume":"16 9","pages":"101660"},"PeriodicalIF":8.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13578975/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148993412","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A quantitative screening strategy based on activity-content ratio for prioritizing bioactive compounds in medicinal plants. 基于活性-含量比的药用植物活性成分定量筛选策略研究。
IF 8.9
Journal of pharmaceutical analysis Pub Date : 2026-09-01 Epub Date: 2026-05-21 DOI: 10.1016/j.jpha.2026.101665
Lin Chen, Xinxin Chen, Shengnan Pi, Ditong Huang, Manhuayun Zhai, Jincai Wang, Zhengjin Jiang, Tingting Zhang
{"title":"A quantitative screening strategy based on activity-content ratio for prioritizing bioactive compounds in medicinal plants.","authors":"Lin Chen, Xinxin Chen, Shengnan Pi, Ditong Huang, Manhuayun Zhai, Jincai Wang, Zhengjin Jiang, Tingting Zhang","doi":"10.1016/j.jpha.2026.101665","DOIUrl":"https://doi.org/10.1016/j.jpha.2026.101665","url":null,"abstract":"<p><p>Accurately evaluating the intrinsic bioactivity of individual constituents, independent of their abundance, remains a major challenge in natural product screening. To address this, we proposed the activity-content ratio (ACR) as a novel index for direct intrinsic inhibitory potency characterization of constituents. Utilizing an at-line nanofractionation platform, an ACR-based screening method for acetylcholinesterase inhibitors was established. The method was validated using both mixed standards and a complex extract of <i>Corydalis rhizoma</i> alkaloids. Results demonstrated a strong linear correlation (<i>R</i> <sup>2</sup> > 0.93) between ACR% and IC<sub>50</sub> for 16 active constituents. High-ACR% compounds, such as berberine, palmatine, and dehydrocorydalin, exhibited significant inhibitory activities at nanomolar concentrations. The model's broad applicability was further confirmed by screening <i>Citri reticulatae pericarpium</i> flavonoids for α-glucosidase inhibitors, showing excellent linearity (<i>R</i> <sup>2</sup> = 0.96) for the five identified active constituents. Notably, rutin displayed the highest ACR% and an IC<sub>50</sub> of 15.21 ± 1.23 μM. The consistent performance of the ACR model across two distinct enzymatic targets and chemical families (alkaloids and flavonoids) demonstrates its reliability and broad applicability. This study provides a reliable and efficient quantitative tool for bioactivity evaluation, which is expected to greatly accelerate the discovery and quality control of bioactive medicinal plants.</p>","PeriodicalId":94338,"journal":{"name":"Journal of pharmaceutical analysis","volume":"16 9","pages":"101665"},"PeriodicalIF":8.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13627906/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149121571","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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