Article(id=1304415028875125186, tenantId=1146029695717560320, journalId=1302319053441957962, issueId=1304414997581427653, articleNumber=null, orderNo=null, doi=10.7501/j.issn.0253-2670.2026.08.019, pmid=null, cstr=null, oa=null, hot=0, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=null, receivedDate=1764691200000, receivedDateStr=2025-12-03, revisedDate=null, revisedDateStr=null, acceptedDate=null, acceptedDateStr=null, onlineDate=1788926377742, onlineDateStr=2026-09-09, pubDate=null, pubDateStr=null, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1788926377742, onlineIssueDateStr=2026-09-09, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1788926377742, creator=13701087609, updateTime=1788926377742, updator=13701087609, issue=Issue{id=1304414997581427653, tenantId=1146029695717560320, journalId=1302319053441957962, year='2026', volume='57', issue='8', pageStart='2877', pageEnd='3260', issueExtLink='null', onlineDate='null', pubDate='1777305600000', pubDateStr='2026-04-28', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1788926370282, creator='13701087609', updateTime=1788926758667, updator='13701087609', preIssue=null, nextIssue=null, articleTotal=null, ext={EN=IssueExt(id=1304416626649096991, tenantId=1146029695717560320, journalId=1302319053441957962, issueId=1304414997581427653, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1304416626649096992, tenantId=1146029695717560320, journalId=1302319053441957962, issueId=1304414997581427653, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null, downloadFileDto=null}, startPage=3061, endPage=3071, ext={EN=ArticleExt(id=1304415030703841732, articleId=1304415028875125186, tenantId=1146029695717560320, journalId=1302319053441957962, language=EN, title=Preparation of ganoderic acid A liposomes and in vitro antitumor activity study, columnId=null, journalTitle=Chinese Traditional and Herbal Drugs, columnName=null, runingTitle=null, highlight=null, articleAbstract=Objective To develop formulation-optimized ganoderic acid A liposomes (GA-Lips) with improved stability and high encapsulation efficiency, and to evaluate their cellular uptake efficiency and in vitro antitumor activity. Methods GA-Lips were prepared using the thin-film hydration method, and formulation parameters were optimized by varying the ratios of GAA, phospholipids, and cholesterol. Particle size, ζ potential, and morphology were characterized. In vitro drug release and formulation stability were evaluated under different media, dilution, and storage conditions. Hemocompatibility was assessed by hemolysis assays. Cellular uptake efficiency was examined using confocal laser scanning microscopy and flow cytometry. Antiproliferative effects and apoptosis induction in HepG2 cells were analyzed using CCK-8 and Annexin V-FITC/PI assays, respectively. Results The optimized GA-Lips exhibited a uniform spherical morphology with a mean particle size of (74.52 ± 1.00) nm, a PDI of 0.26 ± 0.01, and a ζ potential of (-46.75 ± 1.61) mV. The formulation showed sustained drug release, excellent stability under various test conditions, and negligible hemolytic activity. GA-Lips significantly enhanced cellular uptake efficiency in HepG2 cells compared with free GAA. Moreover, GA-Lips exhibited pronounced cytotoxic effects and markedly increased apoptosis induction. Conclusion The optimized GA-Lips demonstrated favorable stability and hemocompatibility, effectively enhancing the cellular uptake efficiency and in vitro antitumor efficacy of GAA. These results support the potential of GA-Lips as a promising nanocarrier system for ganoderic acid A and provide a foundation for further in vivo and mechanistic studies., authors=ZHOU Xinyu, XIA Fei, QIU Chong, WANG Jigang, authorsList=ZHOU Xinyu, XIA Fei, QIU Chong, WANG Jigang, 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=1304415029110006211, articleId=1304415028875125186, tenantId=1146029695717560320, journalId=1302319053441957962, language=CN, title=灵芝酸A脂质体的制备及其体外抗肿瘤活性研究, columnId=1304140189132149234, journalTitle=中草药, columnName=药剂与工艺, runingTitle=null, highlight=null, articleAbstract=目的 通过处方优化构建稳定性高、包封率优的灵芝酸A脂质体(ganoderic acid A liposomes,GA-Lips),并评价其细胞摄取效率及体外抗肿瘤效应。方法 采用薄膜分散法制备GA-Lips,通过调控药物、卵磷脂和胆固醇比例进行处方优化,并开展粒径、ζ电位及透射电子显微镜(transmission electron microscope,TEM)进行形貌表征。利用超滤离心法考察GA-Lips体外释放,结合介质稳定性、稀释稳定性和长期稳定性评估GA-Lips制剂稳定性。通过溶血实验评价血液相容性;采用共聚焦显微镜与流式细胞术分析细胞摄取行为;以CCK-8法测定体外抗增殖作用,并采用Annexin V-FITC/PI流式细胞术检测细胞凋亡。结果 优化后的GA-Lips粒径为(74.52±1.00)nm、PDI为0.26±0.01、ζ电位为(-46.75±1.61)mV,形貌均一。制剂呈缓释特性,在多种介质环境与稀释梯度下均保持良好稳定性,无显著溶血。GA-Lips显著提高HepG2肿瘤细胞的摄取水平,共聚焦显微镜及流式细胞术均得到验证。CCK-8结果显示,GA-Lips对HepG2细胞有显著的细胞毒性;流式分析表明,GA-Lips明显提高HepG2细胞凋亡比例。结论 处方优化构建的GA-Lips具有良好稳定性和安全性,可显著提升灵芝酸A的细胞摄取与体外抗肿瘤活性,为其进一步机制研究及纳米递药系统开发提供实验依据。, authors=周歆喻1,2 , 夏斐2 , 邱崇2 , 王继刚1,2 , authorsList=周歆喻, 夏斐, 邱崇, 王继刚, authorCompany=1 广西医科大学公共卫生学院, 广西 南宁 530021; 2 中国中医科学院 中药研究所青蒿素研究中心, 北京 100700, correspAuthors=邱崇, authorNote=周歆喻: 周歆喻,硕士研究生,研究方向为流行病与卫生统计学。E-mail:18776739339@163.com, correspAuthorsNote=null, copyrightStatement=null, copyrightOwner=null, extLink=null, 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detailUrlEn=https://castjournals.cast.org.cn/joweb/zcy/EN/10.7501/j.issn.0253-2670.2026.08.019, pdfUrlCn=https://castjournals.cast.org.cn/joweb/zcy/CN/PDF/10.7501/j.issn.0253-2670.2026.08.019, pdfUrlEn=https://castjournals.cast.org.cn/joweb/zcy/EN/PDF/10.7501/j.issn.0253-2670.2026.08.019, aliStartDate=null, aliEndDate=null, collectionFlag=false, citedCount=null, citedUrl=null, previewStatus=0, delFlag=0, hasFullText=0, orderTime=1788926377742, fullTextJson=null, articleText=null, reference=Yuan W, Jiang C J, Wang Q, et al. Biosynthesis of mushroom-derived type II ganoderic acids by engineered yeast[J]. Nat Commun, 2022, 13(1):7740. 吕俞娇, 周姝婷, 王丽娜, 等. 灵芝活性成分抗肿瘤机制研究进展[J]. 中国临床药理学与治疗学, 2024, 29(8):947-954. Wang M C, Han Q, Zhang X L, et al. Ganoderic acid a derivative induces apoptosis of cervical cancer cells by inhibiting JNK pathway[J]. Chin Herb Med, 2025, 17(4):756-767. 陈茵妮. 灵芝酸A对小鼠溃疡性结肠炎的改善作用及其作用机制的研究[D]. 南昌:南昌大学, 2025. 王磊, 梁峰, 赵宏伟, 等. 含灵芝多糖的复方制剂免疫调节功能及安全性评价[J]. 食品工业科技, 2024, 45(21):338-349. Jia Y, Li Y, Shang H, et al. Ganoderic acid a and its amide derivatives as potential anti-cancer agents by regulating the p53-MDM2 pathway:Synthesis and biological evaluation[J]. Molecules, 2023, 28(5):2374. Rahman M, Beg S, Alharbi K S, et al. Implications of solid lipid nanoparticles of ganoderic acid for the treatment and management of hepatocellular carcinoma[J]. J Pharm Innov, 2021, 16(2):359-370. Zhong C L, Li Y M, Li W L, et al. Ganoderma lucidum extract promotes tumor cell pyroptosis and inhibits metastasis in breast cancer[J]. Food Chem Toxicol, 2023, 174:113654. Fu Y F, Xia F, Sun L L, et al. Anti-lung cancer therapy using nano-assembly particles of traditional Chinese Medicine formula[J]. Mater Today Bio, 2025, 35:102502. 罗虹建, 鲁国东, 林占熺, 等. 灵芝主要活性成分药理作用及生物合成研究进展[J]. 中草药, 2025, 56(9):3366-3379. Rahman M, Al-Ghamdi S A, Alharbi K S, et al. Ganoderic acid loaded nano-lipidic carriers improvise treatment of hepatocellular carcinoma[J]. Drug Deliv, 2019, 26(1):782-793. 黄婷. 灵芝三萜载体材料纳米体的制备研究[D]. 合肥:合肥工业大学, 2015. 沈成英. 中药难溶性有效部位灵芝三萜纳米凝胶透皮给药系统的构建与评价[D]. 成都:成都中医药大学, 2015. Mu W W, Chu Q H, Liu Y J, et al. A review on nano-based drug delivery system for cancer chemoimmunotherapy[J]. Nanomicro Lett, 2020, 12(1):142. Large D E, Abdelmessih R G, Fink E A, et al. Liposome composition in drug delivery design, synthesis, characterization, and clinical application[J]. Adv Drug Deliv Rev, 2021, 176:113851. Qiu C, Xia F, Tu Q C, et al. Multimodal lung cancer theranostics via manganese phosphate/quercetin particle[J]. Mol Cancer, 2025, 24(1):43. 汪芳, 田莹莹, 曾慧婷, 等. 共载抗肿瘤中药活性成分纳米制剂研究进展[J]. 中成药, 2025, 47(9):2964-2970. Zhang L L, Shi J P, Zhu M H, et al. Liposomes-enabled cancer chemoimmunotherapy[J]. Biomaterials, 2025, 313:122801. Wu H Y, Yu M R, Miao Y Q, et al. Cholesterol-tuned liposomal membrane rigidity directs tumor penetration and anti-tumor effect[J]. Acta Pharm Sin B, 2019, 9(4):858-870. Rahman M M, Wang J, Wang G S, et al. Chimeric nanobody-decorated liposomes by self-assembly[J]. Nat Nanotechnol, 2024, 19(6):818-824. 王美丹, 胡扬, 宋辉, 等. 灵芝孢子粉化学成分和药理作用的研究进展及其质量标志物 (Q-Marker) 预测分析[J]. 中草药, 2023, 54(23):7918-7933. Weber M, Steinle H, Golombek S, et al. Blood-contacting biomaterials:In vitro evaluation of the hemocompatibility[J]. Front Bioeng Biotech, 2018, 6:99.)
中草药
|药剂与工艺
2026
, 57
(8) :
3061
-3071
灵芝酸A脂质体的制备及其体外抗肿瘤活性研究
全屏
周歆喻1,2 , 夏斐2 , 邱崇2 , 王继刚1,2
作者信息
1 广西医科大学公共卫生学院, 广西 南宁 530021; 2 中国中医科学院 中药研究所青蒿素研究中心, 北京 100700
通讯作者:
邱崇
作者简介:
周歆喻: 周歆喻,硕士研究生,研究方向为流行病与卫生统计学。E-mail:18776739339@163.com
Preparation of ganoderic acid A liposomes and in vitro antitumor activity study
ZHOU Xinyu, XIA Fei, QIU Chong, WANG Jigang
Affiliations
doi: 10.7501/j.issn.0253-2670.2026.08.019
文章导航
目的 通过处方优化构建稳定性高、包封率优的灵芝酸A脂质体(ganoderic acid A liposomes,GA-Lips),并评价其细胞摄取效率及体外抗肿瘤效应。方法 采用薄膜分散法制备GA-Lips,通过调控药物、卵磷脂和胆固醇比例进行处方优化,并开展粒径、ζ电位及透射电子显微镜(transmission electron microscope,TEM)进行形貌表征。利用超滤离心法考察GA-Lips体外释放,结合介质稳定性、稀释稳定性和长期稳定性评估GA-Lips制剂稳定性。通过溶血实验评价血液相容性;采用共聚焦显微镜与流式细胞术分析细胞摄取行为;以CCK-8法测定体外抗增殖作用,并采用Annexin V-FITC/PI流式细胞术检测细胞凋亡。结果 优化后的GA-Lips粒径为(74.52±1.00)nm、PDI为0.26±0.01、ζ电位为(-46.75±1.61)mV,形貌均一。制剂呈缓释特性,在多种介质环境与稀释梯度下均保持良好稳定性,无显著溶血。GA-Lips显著提高HepG2肿瘤细胞的摄取水平,共聚焦显微镜及流式细胞术均得到验证。CCK-8结果显示,GA-Lips对HepG2细胞有显著的细胞毒性;流式分析表明,GA-Lips明显提高HepG2细胞凋亡比例。结论 处方优化构建的GA-Lips具有良好稳定性和安全性,可显著提升灵芝酸A的细胞摄取与体外抗肿瘤活性,为其进一步机制研究及纳米递药系统开发提供实验依据。
灵芝酸A
/
脂质体
/
薄膜分散法
/
处方优化
/
抗肿瘤活性
/
纳米递药系统
Objective To develop formulation-optimized ganoderic acid A liposomes (GA-Lips) with improved stability and high encapsulation efficiency, and to evaluate their cellular uptake efficiency and in vitro antitumor activity. Methods GA-Lips were prepared using the thin-film hydration method, and formulation parameters were optimized by varying the ratios of GAA, phospholipids, and cholesterol. Particle size, ζ potential, and morphology were characterized. In vitro drug release and formulation stability were evaluated under different media, dilution, and storage conditions. Hemocompatibility was assessed by hemolysis assays. Cellular uptake efficiency was examined using confocal laser scanning microscopy and flow cytometry. Antiproliferative effects and apoptosis induction in HepG2 cells were analyzed using CCK-8 and Annexin V-FITC/PI assays, respectively. Results The optimized GA-Lips exhibited a uniform spherical morphology with a mean particle size of (74.52 ± 1.00) nm, a PDI of 0.26 ± 0.01, and a ζ potential of (-46.75 ± 1.61) mV. The formulation showed sustained drug release, excellent stability under various test conditions, and negligible hemolytic activity. GA-Lips significantly enhanced cellular uptake efficiency in HepG2 cells compared with free GAA. Moreover, GA-Lips exhibited pronounced cytotoxic effects and markedly increased apoptosis induction. Conclusion The optimized GA-Lips demonstrated favorable stability and hemocompatibility, effectively enhancing the cellular uptake efficiency and in vitro antitumor efficacy of GAA. These results support the potential of GA-Lips as a promising nanocarrier system for ganoderic acid A and provide a foundation for further in vivo and mechanistic studies.
ganoderic acid A
/
liposomes
/
thin-film dispersion
/
formulation optimization
/
antitumor activity
/
nanocarrier system
周歆喻, 夏斐, 邱崇, 王继刚.
灵芝酸A脂质体的制备及其体外抗肿瘤活性研究.
中草药,
2026
, 57
(8)
: 3061
-3071
.
DOI: 10.7501/j.issn.0253-2670.2026.08.019
ZHOU Xinyu, XIA Fei, QIU Chong, WANG Jigang.
Preparation of ganoderic acid A liposomes and in vitro antitumor activity study[J].
Chinese Traditional and Herbal Drugs ,
2026
, 57
(8)
: 3061
-3071
.
DOI: 10.7501/j.issn.0253-2670.2026.08.019
参考文献
引证文献
Yuan W, Jiang C J, Wang Q, et al. Biosynthesis of mushroom-derived type II ganoderic acids by engineered yeast[J]. Nat Commun, 2022, 13(1):7740. 吕俞娇, 周姝婷, 王丽娜, 等. 灵芝活性成分抗肿瘤机制研究进展[J]. 中国临床药理学与治疗学, 2024, 29(8):947-954. Wang M C, Han Q, Zhang X L, et al. Ganoderic acid a derivative induces apoptosis of cervical cancer cells by inhibiting JNK pathway[J]. Chin Herb Med, 2025, 17(4):756-767. 陈茵妮. 灵芝酸A对小鼠溃疡性结肠炎的改善作用及其作用机制的研究[D]. 南昌:南昌大学, 2025. 王磊, 梁峰, 赵宏伟, 等. 含灵芝多糖的复方制剂免疫调节功能及安全性评价[J]. 食品工业科技, 2024, 45(21):338-349. Jia Y, Li Y, Shang H, et al. Ganoderic acid a and its amide derivatives as potential anti-cancer agents by regulating the p53-MDM2 pathway:Synthesis and biological evaluation[J]. Molecules, 2023, 28(5):2374. Rahman M, Beg S, Alharbi K S, et al. Implications of solid lipid nanoparticles of ganoderic acid for the treatment and management of hepatocellular carcinoma[J]. J Pharm Innov, 2021, 16(2):359-370. Zhong C L, Li Y M, Li W L, et al. Ganoderma lucidum extract promotes tumor cell pyroptosis and inhibits metastasis in breast cancer[J]. Food Chem Toxicol, 2023, 174:113654. Fu Y F, Xia F, Sun L L, et al. Anti-lung cancer therapy using nano-assembly particles of traditional Chinese Medicine formula[J]. Mater Today Bio, 2025, 35:102502. 罗虹建, 鲁国东, 林占熺, 等. 灵芝主要活性成分药理作用及生物合成研究进展[J]. 中草药, 2025, 56(9):3366-3379. Rahman M, Al-Ghamdi S A, Alharbi K S, et al. Ganoderic acid loaded nano-lipidic carriers improvise treatment of hepatocellular carcinoma[J]. Drug Deliv, 2019, 26(1):782-793. 黄婷. 灵芝三萜载体材料纳米体的制备研究[D]. 合肥:合肥工业大学, 2015. 沈成英. 中药难溶性有效部位灵芝三萜纳米凝胶透皮给药系统的构建与评价[D]. 成都:成都中医药大学, 2015. Mu W W, Chu Q H, Liu Y J, et al. A review on nano-based drug delivery system for cancer chemoimmunotherapy[J]. Nanomicro Lett, 2020, 12(1):142. Large D E, Abdelmessih R G, Fink E A, et al. Liposome composition in drug delivery design, synthesis, characterization, and clinical application[J]. Adv Drug Deliv Rev, 2021, 176:113851. Qiu C, Xia F, Tu Q C, et al. Multimodal lung cancer theranostics via manganese phosphate/quercetin particle[J]. Mol Cancer, 2025, 24(1):43. 汪芳, 田莹莹, 曾慧婷, 等. 共载抗肿瘤中药活性成分纳米制剂研究进展[J]. 中成药, 2025, 47(9):2964-2970. Zhang L L, Shi J P, Zhu M H, et al. Liposomes-enabled cancer chemoimmunotherapy[J]. Biomaterials, 2025, 313:122801. Wu H Y, Yu M R, Miao Y Q, et al. Cholesterol-tuned liposomal membrane rigidity directs tumor penetration and anti-tumor effect[J]. Acta Pharm Sin B, 2019, 9(4):858-870. Rahman M M, Wang J, Wang G S, et al. Chimeric nanobody-decorated liposomes by self-assembly[J]. Nat Nanotechnol, 2024, 19(6):818-824. 王美丹, 胡扬, 宋辉, 等. 灵芝孢子粉化学成分和药理作用的研究进展及其质量标志物 (Q-Marker) 预测分析[J]. 中草药, 2023, 54(23):7918-7933. Weber M, Steinle H, Golombek S, et al. Blood-contacting biomaterials:In vitro evaluation of the hemocompatibility[J]. Front Bioeng Biotech, 2018, 6:99.
2026年第57卷第8期
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doi: 10.7501/j.issn.0253-2670.2026.08.019
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2种不同金属材料的力学参数
科 Family 属数 Number of genus 种数 Number of species 占总种数比例 Percentage of total species (%) 属 Genus 种数 Number of species 占总种数比例 Percentage of total species (%) 鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78 小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39 多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39 红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87 小菇属 Mycena 11 5.26 光柄菇属 Pluteus 5 2.39 红菇属 Russula 17 8.13 栓菌属 Trametes 5 2.39
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