Article(id=1304388076562838187, tenantId=1146029695717560320, journalId=1302319053441957962, issueId=1304388049975137100, articleNumber=null, orderNo=null, doi=10.7501/j.issn.0253-2670.2026.11.004, pmid=null, cstr=null, oa=null, hot=0, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=null, receivedDate=1771171200000, receivedDateStr=2026-02-16, revisedDate=null, revisedDateStr=null, acceptedDate=null, acceptedDateStr=null, onlineDate=1788919951811, onlineDateStr=2026-09-09, pubDate=null, pubDateStr=null, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1788919951811, onlineIssueDateStr=2026-09-09, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1788919951811, creator=13701087609, updateTime=1788919951811, updator=13701087609, issue=Issue{id=1304388049975137100, tenantId=1146029695717560320, journalId=1302319053441957962, year='2026', volume='57', issue='11', pageStart='4089', pageEnd='4508', issueExtLink='null', onlineDate='null', pubDate='1781193600000', pubDateStr='2026-06-12', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1788919945471, creator='13701087609', updateTime=1788923432386, updator='13701087609', preIssue=null, nextIssue=null, articleTotal=null, ext={EN=IssueExt(id=1304402675202805770, tenantId=1146029695717560320, journalId=1302319053441957962, issueId=1304388049975137100, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1304402675207000075, tenantId=1146029695717560320, journalId=1302319053441957962, issueId=1304388049975137100, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null, downloadFileDto=null}, startPage=4112, endPage=4123, ext={EN=ArticleExt(id=1304388078395749037, articleId=1304388076562838187, tenantId=1146029695717560320, journalId=1302319053441957962, language=EN, title=Anti-inflammatory activity, structural characterization, and in vivo absorption and distribution profile of major polysaccharide-enriched fractions from Xiaoyao San, columnId=null, journalTitle=Chinese Traditional and Herbal Drugs, columnName=null, runingTitle=null, highlight=null, articleAbstract=Objective To prepare different polysaccharide fractions of Xiaoyao San (逍遥散, XYS) by graded ethanol precipitation and to clarify the anti-inflammatory activity, structural characteristics, and in vivo absorption and distribution behavior of the major enriched fraction. Methods Different polysaccharide fractions of XYS (40%, 60%, and 80% ethanol-precipitated fractions) were obtained using a water extraction-ethanol precipitation procedure, and the primary enriched fraction was screened based on yield comparison. Based on the inflammation-depression correlation, an LPS-induced microglial inflammation model was established, and anti-inflammatory activity was evaluated by measuring inflammatory markers including TNF-α, IL-1β, IL-6, and iNOS. The composition and structural features of the target polysaccharide were characterized using UV-Vis spectroscopy, FT-IR, and NMR analyses. Fluorescently labeled polysaccharides were further prepared for in vivo pharmacokinetic studies in mice to systematically assess exposure levels and tissue distribution characteristics. Results Significant differences in yield were observed among polysaccharide fractions obtained at different ethanol precipitation ratios. The 60% ethanol fraction (XYSP-60) was identified as the major enriched fraction, with an extraction recovery of 37.5%. In the LPS-induced microglial inflammation model, XYSP-60 significantly downregulated the expression levels of TNF-α, IL-1β, IL-6, and iNOS, demonstrating clear anti-inflammatory activity. Structural characterization indicated that the polysaccharide mainly consisted of galacturonic acid, glucose, and fructose, with relatively stable structural features. Pharmacokinetic results showed that XYSP-60 exhibited high exposure in the intestine but limited entry into systemic circulation. Conclusion The 60% ethanol-precipitated fraction represents the principal enriched polysaccharide fraction of XYS, with stable structural characteristics and definite anti-inflammatory activity. Its in vivo behavior is characterized by high intestinal exposure and limited systemic absorption, suggesting that this fraction may serve as one of the key material bases underlying the anti-inflammatory effects of XYS., authors=HU Jing, GUAN Yongxia, ZENG Yu, LI Wenchao, YAO Zhihong, HE Liangliang, DI Xin, authorsList=HU Jing, GUAN Yongxia, ZENG Yu, LI Wenchao, YAO Zhihong, HE Liangliang, DI Xin, authorCompany=null, correspAuthors=null, authorNote=null, correspAuthorsNote=null, copyrightStatement=null, copyrightOwner=null, extLink=null, articleAbsUrl=null, sourceXml=null, magXml=null, pdfUrl=null, pdf=null, pdfFileSize=null, pdfExtLink=null, richHtmlUrl=null, mobilePdfUrl=null, reviewReport=null, pdfFirstPage=null, abstractGraph=null, abstractGraphContent=null, abstractVideo=null, citation=null, cebUrl=null, magXmlContent=null, mapNumber=null, fund=null), CN=ArticleExt(id=1304388078307668652, articleId=1304388076562838187, tenantId=1146029695717560320, journalId=1302319053441957962, language=CN, title=逍遥散多糖主要富集部位的抗炎活性、结构表征及体内吸收分布特征, columnId=1304140187169214944, journalTitle=中草药, columnName=化学成分, runingTitle=null, highlight=null, articleAbstract=目的 采用分级醇沉技术制备逍遥散多糖不同醇沉部位,明确其主要富集部位的抗炎活性、结构特征及体内吸收与分布行为。方法 基于水提醇沉工艺制备逍遥散多糖不同醇沉部位(40%、60%、80%),比较各部位得率以筛选多糖主要富集部位;基于“炎症-抑郁”相关性,建立脂多糖(lipopolysaccharide,LPS)诱导的小胶质细胞炎症模型,通过检测肿瘤坏死因子-α(tumor necrosis factor-alpha,TNF-α)、白细胞介素-1β(interleukin-1β,IL-1β)、白细胞介素-6(interleukin-6,IL-6)及诱导型一氧化氮合酶(inducible nitric oxide synthase,iNOS)等炎症相关指标评价其抗炎活性;采用紫外-可见吸收光谱、傅里叶变换红外光谱与核磁共振波谱等技术对目标多糖的组成与结构特征进行表征;通过荧光标记构建荧光示踪多糖,在小鼠体内开展药动学研究,系统评估其体内暴露水平与组织分布特征。结果 不同醇沉比例获得的多糖部位在得率上存在明显差异,其中60%醇沉部位(XYSP-60)为多糖主要富集部位,其提取率为37.50%;在LPS诱导的小胶质细胞炎症模型中,XYSP-60可显著下调TNF-α、IL-1β、IL-6及iNOS的表达水平,表现出明确的抗炎活性;结构表征结果显示,该多糖主要由半乳糖醛酸、葡萄糖和果糖构成,整体结构特征较为稳定;药动学结果表明,XYSP-60在肠道中暴露水平较高,而进入体循环的比例相对较低。结论 逍遥散多糖60%醇沉为主要富集部位,具有明确的抗炎作用和稳定的结构特征,其在体内过程以肠道高暴露、系统吸收有限为主要特征,可能构成逍遥散发挥抗炎作用的潜在物质基础之一。, authors=虎静1,2, 关永霞3, 曾宇2, 李文超2, 姚志红2, 何亮亮2, 邸欣1, authorsList=虎静, 关永霞, 曾宇, 李文超, 姚志红, 何亮亮, 邸欣, authorCompany=1 沈阳药科大学药学院, 辽宁 沈阳 110016; 2 暨南大学药学院中药与天然药物研究所, 广东 广州 510632; 3 经方与现代中药融合创新全国重点实验室, 山东 临沂 276000, correspAuthors=何亮亮, authorNote=虎静: 虎静,硕士研究生。E-mail:hujing20221225@163.com
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pdfUrlEn=https://castjournals.cast.org.cn/joweb/zcy/EN/PDF/10.7501/j.issn.0253-2670.2026.11.004, aliStartDate=null, aliEndDate=null, collectionFlag=false, citedCount=null, citedUrl=null, previewStatus=0, delFlag=0, hasFullText=0, orderTime=1788919951811, fullTextJson=null, articleText=null, reference=Zhou X, Ma Q Y, Yan Z Q, et al. 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Gut microbiome and depression: What we know and what we need to know [J]. Rev Neurosci, 2018, 29(6): 629-643. Hao W Z, Ma Q Y, Wang L, et al. Gut dysbiosis induces the development of depression-like behavior through abnormal synapse pruning in microglia-mediated by complement C3[J]. Microbiome, 2024, 12(1): 34. Chen Y M, Zeng X X, Gong X R, et al. Ganoderma lucidum polysaccharides target the gut-brain axis: Unveiling a novel mechanism for ameliorating aging-induced cognitive impairment and oxidative stress [J]. Int J Biol Macromol, 2026, 337: 149519. 多水银, 张兴波, 吴玉辉, 等. 牛大力多糖的荧光标记、鉴定及其体内分布[J]. 饲料研究, 2024, 47(8): 88-91. Zhu L, Guan L J, Wang K L, et al. Recent trends in extraction, purification, structural characterization, and biological activities evaluation of Perilla frutescens (L.) Britton polysaccharide [J]. Front Nutr, 2024, 11: 1359813. Cortés-Ríos J, Zárate A M, Figueroa J D, et al. Protein quantification by bicinchoninic acid (BCA) assay follows complex kinetics and can be performed at short incubation times [J]. Anal Biochem, 2020, 608: 113904. 杨桐, 陈江, 张雪, 等. 分级醇沉玉竹多糖的结构表征及其抗糖尿病活性研究[J]. 中草药, 2025, 56(17): 6121-6136. Li Z W, Du Z M, Wang Y W, et al. Chemical modification, characterization, and activity changes of land plant polysaccharides: A review [J]. Polymers, 2022, 14(19): 4161. He X R, Wang X X, Fang J C, et al. Polysaccharides in Grifola frondosa mushroom and their health promoting properties: A review [J]. Int J Biol Macromol, 2017, 101: 910-921. 石云鑫, 杨家, 潘诗琴, 等. 不同方法提取的山茱萸多糖品质特征[J]. 南方农业学报, 2024, 55(7): 2031-2043. 杨德强, 魏名卓, 杨欣荣, 等. 多糖的高级结构鉴定分析的研究进展[J]. 化学工程师, 2023, 37(5): 68-71. Li L F, Yao H, Li X J, et al. Destiny of Dendrobium officinale polysaccharide after oral administration: Indigestible and nonabsorbing, ends in modulating gut microbiota [J]. J Agric Food Chem, 2019, 67(21): 5968-5977. Wang K P, Cheng F, Pan X L, et al. Investigation of the transport and absorption of Angelica sinensis polysaccharide through gastrointestinal tract both in vitro and in vivo [J]. Drug Deliv, 2017, 24(1): 1360-1371. Liu L X, Li H B, Wang Z Z, et al. Exploring the anti-migraine effects of Tianshu Capsule: Chemical profile, metabolic behavior, and therapeutic mechanisms [J]. Phytomedicine, 2024, 131: 155766. 禹恺, 帅哲玮, 黄洪军, 等. 小胶质细胞在中枢神经系统炎症性疾病中的作用和机制研究进展[J]. 上海交通大学学报: 医学版, 2025, 45(5): 630-638. 赵璐, 杨光路, 贾凯茹, 等. 小胶质细胞的双重作用在神经系统疾病中的研究进展[J]. 临床医学进展, 2023(10): 16401-16405. Vennapusa A R, Somayanda I M, Doherty C J, et al. A universal method for high-quality RNA extraction from plant tissues rich in starch, proteins and fiber [J]. Sci Rep, 2020, 10: 16887. Gurusaravanan P, Vinoth S, Vasanthkumar R, et al. In vitro regeneration of cotton (Gossypium hirsutum L.) cultivar KC3 with controlled phenolic secretion by using Kappaphycus alvarezii sulfated polysaccharide extract and plant growth regulators [J]. Vitro Cell Dev Biol Plant, 2024, 60(4): 561-574. Vedia G R, de Araújo Morandim-Giannetti A. Production of second-generation ethanol and carboxymethylcellulose from sugarcane bagasse pretreated with low-cost ionic liquids [J]. Cellulose, 2023, 30(17): 10767-10781. 李学玲, 白芩凡, 孙体杰, 等. 铁皮石斛多糖的结构表征与抗氧化活性研究[J]. 食品工业科技, 2024, 45(19): 32-39. Wang S Q, Li G, Zhang X F, et al. Structural characterization and antioxidant activity of Polygonatum sibiricum polysaccharides [J]. Carbohydr Polym, 2022, 291: 119524. Song Q Q, Jiang L, Yang X Q, et al. Physicochemical and functional properties of a water-soluble polysaccharide extracted from Mung bean (Vigna radiate L.) and its antioxidant activity [J]. Int J Biol Macromol, 2019, 138: 874-880. Xu Y Y, He F, Jin C, et al. Stachyose with effect on anti-angiogenic activity from Salvia yunnanensis [J]. J Funct Foods, 2024, 112: 105971. Speciale I, Notaro A, Garcia-Vello P, et al. Liquid-state NMR spectroscopy for complex carbohydrate structural analysis: A hitchhiker’s guide [J]. Carbohydr Polym, 2022, 277: 118885. Zhou W T, Kan X H, Dong W, et al. In vivo absorption and fecal excretion of polysaccharides from the fruits of Lycium barbarum L. in rats through fluorescence labeling [J]. Int J Biol Macromol, 2024, 278: 134613. Mohan T, Kleinschek K S, Kargl R. Polysaccharide peptide conjugates: Chemistry, properties and applications [J]. Carbohydr Polym, 2022, 280: 118875. Bai J, Ge J, Zhang W, et al. Physicochemical, morpho-structural, and biological characterization of polysaccharides from three Polygonatum spp [J]. RSC Advances, 2021, 11(60): 37952-37965.)
Anti-inflammatory activity, structural characterization, and in vivo absorption and distribution profile of major polysaccharide-enriched fractions from Xiaoyao San
HU Jing, GUAN Yongxia, ZENG Yu, LI Wenchao, YAO Zhihong, HE Liangliang, DI Xin
Objective To prepare different polysaccharide fractions of Xiaoyao San (逍遥散, XYS) by graded ethanol precipitation and to clarify the anti-inflammatory activity, structural characteristics, and in vivo absorption and distribution behavior of the major enriched fraction. Methods Different polysaccharide fractions of XYS (40%, 60%, and 80% ethanol-precipitated fractions) were obtained using a water extraction-ethanol precipitation procedure, and the primary enriched fraction was screened based on yield comparison. Based on the inflammation-depression correlation, an LPS-induced microglial inflammation model was established, and anti-inflammatory activity was evaluated by measuring inflammatory markers including TNF-α, IL-1β, IL-6, and iNOS. The composition and structural features of the target polysaccharide were characterized using UV-Vis spectroscopy, FT-IR, and NMR analyses. Fluorescently labeled polysaccharides were further prepared for in vivo pharmacokinetic studies in mice to systematically assess exposure levels and tissue distribution characteristics. Results Significant differences in yield were observed among polysaccharide fractions obtained at different ethanol precipitation ratios. The 60% ethanol fraction (XYSP-60) was identified as the major enriched fraction, with an extraction recovery of 37.5%. In the LPS-induced microglial inflammation model, XYSP-60 significantly downregulated the expression levels of TNF-α, IL-1β, IL-6, and iNOS, demonstrating clear anti-inflammatory activity. Structural characterization indicated that the polysaccharide mainly consisted of galacturonic acid, glucose, and fructose, with relatively stable structural features. Pharmacokinetic results showed that XYSP-60 exhibited high exposure in the intestine but limited entry into systemic circulation. Conclusion The 60% ethanol-precipitated fraction represents the principal enriched polysaccharide fraction of XYS, with stable structural characteristics and definite anti-inflammatory activity. Its in vivo behavior is characterized by high intestinal exposure and limited systemic absorption, suggesting that this fraction may serve as one of the key material bases underlying the anti-inflammatory effects of XYS.
Key words
Xiaoyao San
/
polysaccharides
/
material basis
/
fluorescent labeling
/
BV-2 cells
HU Jing, GUAN Yongxia, ZENG Yu, LI Wenchao, YAO Zhihong, HE Liangliang, DI Xin.
Anti-inflammatory activity, structural characterization, and in vivo absorption and distribution profile of major polysaccharide-enriched fractions from Xiaoyao San[J].
Chinese Traditional and Herbal Drugs,
2026
, 57
(11)
: 4112
-4123
.
DOI: 10.7501/j.issn.0253-2670.2026.11.004
Zhou X, Ma Q Y, Yan Z Q, et al. Efficacy and safety of Chinese patent medicine Xiao Yao San in polycystic ovary syndrome: A systematic review and Meta-analysis [J]. J Ethnopharmacol, 2023, 313: 116517. Wang Y T, Wang X L, Wang Z Z, et al. Antidepressant effects of the traditional Chinese herbal formula Xiao-Yao-San and its bioactive ingredients [J]. Phytomedicine, 2023, 109: 154558. Zhang Y, Li X J, Wang X R, et al. Integrating metabolomics and network pharmacology to explore the mechanism of Xiao-Yao-San in the treatment of inflammatory response in CUMS mice [J]. Pharmaceuticals, 2023, 16(11): 1607. 张娜, 刘扬, 陈小强, 等. 化学修饰植物多糖的生物活性及其在食品领域中的应用研究进展[J]. 食品工业科技, 2025, 46(7): 375-384. El-Saadony M T, Saad A M, Alkafaas S S, et al. Chitosan, derivatives, and its nanoparticles: Preparation, physicochemical properties, biological activities, and biomedical applications–A comprehensive review [J]. Int J Biol Macromol, 2025, 313: 142832. Winter G, Hart R A, Charlesworth R P G, et al. Gut microbiome and depression: What we know and what we need to know [J]. Rev Neurosci, 2018, 29(6): 629-643. Hao W Z, Ma Q Y, Wang L, et al. Gut dysbiosis induces the development of depression-like behavior through abnormal synapse pruning in microglia-mediated by complement C3[J]. Microbiome, 2024, 12(1): 34. Chen Y M, Zeng X X, Gong X R, et al. Ganoderma lucidum polysaccharides target the gut-brain axis: Unveiling a novel mechanism for ameliorating aging-induced cognitive impairment and oxidative stress [J]. Int J Biol Macromol, 2026, 337: 149519. 多水银, 张兴波, 吴玉辉, 等. 牛大力多糖的荧光标记、鉴定及其体内分布[J]. 饲料研究, 2024, 47(8): 88-91. Zhu L, Guan L J, Wang K L, et al. Recent trends in extraction, purification, structural characterization, and biological activities evaluation of Perilla frutescens (L.) Britton polysaccharide [J]. Front Nutr, 2024, 11: 1359813. Cortés-Ríos J, Zárate A M, Figueroa J D, et al. Protein quantification by bicinchoninic acid (BCA) assay follows complex kinetics and can be performed at short incubation times [J]. Anal Biochem, 2020, 608: 113904. 杨桐, 陈江, 张雪, 等. 分级醇沉玉竹多糖的结构表征及其抗糖尿病活性研究[J]. 中草药, 2025, 56(17): 6121-6136. Li Z W, Du Z M, Wang Y W, et al. Chemical modification, characterization, and activity changes of land plant polysaccharides: A review [J]. Polymers, 2022, 14(19): 4161. He X R, Wang X X, Fang J C, et al. Polysaccharides in Grifola frondosa mushroom and their health promoting properties: A review [J]. Int J Biol Macromol, 2017, 101: 910-921. 石云鑫, 杨家, 潘诗琴, 等. 不同方法提取的山茱萸多糖品质特征[J]. 南方农业学报, 2024, 55(7): 2031-2043. 杨德强, 魏名卓, 杨欣荣, 等. 多糖的高级结构鉴定分析的研究进展[J]. 化学工程师, 2023, 37(5): 68-71. Li L F, Yao H, Li X J, et al. Destiny of Dendrobium officinale polysaccharide after oral administration: Indigestible and nonabsorbing, ends in modulating gut microbiota [J]. J Agric Food Chem, 2019, 67(21): 5968-5977. Wang K P, Cheng F, Pan X L, et al. Investigation of the transport and absorption of Angelica sinensis polysaccharide through gastrointestinal tract both in vitro and in vivo [J]. Drug Deliv, 2017, 24(1): 1360-1371. Liu L X, Li H B, Wang Z Z, et al. Exploring the anti-migraine effects of Tianshu Capsule: Chemical profile, metabolic behavior, and therapeutic mechanisms [J]. Phytomedicine, 2024, 131: 155766. 禹恺, 帅哲玮, 黄洪军, 等. 小胶质细胞在中枢神经系统炎症性疾病中的作用和机制研究进展[J]. 上海交通大学学报: 医学版, 2025, 45(5): 630-638. 赵璐, 杨光路, 贾凯茹, 等. 小胶质细胞的双重作用在神经系统疾病中的研究进展[J]. 临床医学进展, 2023(10): 16401-16405. Vennapusa A R, Somayanda I M, Doherty C J, et al. A universal method for high-quality RNA extraction from plant tissues rich in starch, proteins and fiber [J]. Sci Rep, 2020, 10: 16887. Gurusaravanan P, Vinoth S, Vasanthkumar R, et al. In vitro regeneration of cotton (Gossypium hirsutum L.) cultivar KC3 with controlled phenolic secretion by using Kappaphycus alvarezii sulfated polysaccharide extract and plant growth regulators [J]. Vitro Cell Dev Biol Plant, 2024, 60(4): 561-574. Vedia G R, de Araújo Morandim-Giannetti A. Production of second-generation ethanol and carboxymethylcellulose from sugarcane bagasse pretreated with low-cost ionic liquids [J]. Cellulose, 2023, 30(17): 10767-10781. 李学玲, 白芩凡, 孙体杰, 等. 铁皮石斛多糖的结构表征与抗氧化活性研究[J]. 食品工业科技, 2024, 45(19): 32-39. Wang S Q, Li G, Zhang X F, et al. Structural characterization and antioxidant activity of Polygonatum sibiricum polysaccharides [J]. Carbohydr Polym, 2022, 291: 119524. Song Q Q, Jiang L, Yang X Q, et al. Physicochemical and functional properties of a water-soluble polysaccharide extracted from Mung bean (Vigna radiate L.) and its antioxidant activity [J]. Int J Biol Macromol, 2019, 138: 874-880. Xu Y Y, He F, Jin C, et al. Stachyose with effect on anti-angiogenic activity from Salvia yunnanensis [J]. J Funct Foods, 2024, 112: 105971. Speciale I, Notaro A, Garcia-Vello P, et al. Liquid-state NMR spectroscopy for complex carbohydrate structural analysis: A hitchhiker’s guide [J]. Carbohydr Polym, 2022, 277: 118885. Zhou W T, Kan X H, Dong W, et al. In vivo absorption and fecal excretion of polysaccharides from the fruits of Lycium barbarum L. in rats through fluorescence labeling [J]. Int J Biol Macromol, 2024, 278: 134613. Mohan T, Kleinschek K S, Kargl R. Polysaccharide peptide conjugates: Chemistry, properties and applications [J]. Carbohydr Polym, 2022, 280: 118875. Bai J, Ge J, Zhang W, et al. Physicochemical, morpho-structural, and biological characterization of polysaccharides from three Polygonatum spp [J]. RSC Advances, 2021, 11(60): 37952-37965.