Article(id=1236344967174615990, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1236344966058931117, articleNumber=null, orderNo=null, doi=null, pmid=null, cstr=null, oa=null, hot=null, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=null, receivedDate=null, receivedDateStr=null, revisedDate=null, revisedDateStr=null, acceptedDate=1652803200000, acceptedDateStr=2022-05-18, onlineDate=1772697210353, onlineDateStr=2026-03-05, pubDate=1678809600000, pubDateStr=2023-03-15, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1772697210353, onlineIssueDateStr=2026-03-05, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1772697210353, creator=13701087609, updateTime=1772697210353, updator=13701087609, issue=Issue{id=1236344966058931117, tenantId=1146029695717560320, journalId=1235980733773295621, year='2023', volume='32', issue='5', pageStart='441', pageEnd='552', issueExtLink='null', onlineDate='null', pubDate='null', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1772697210087, creator=13701087609, updateTime=1772697640190, updator=13701087609, preIssue=null, nextIssue=null, ext={EN=IssueExt(id=1236346770087793082, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1236344966058931117, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1236346770087793083, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1236344966058931117, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null}, startPage=531, endPage=539, ext={EN=ArticleExt(id=1236344967375942590, articleId=1236344967174615990, tenantId=1146029695717560320, journalId=1235980733773295621, language=EN, title=Analysis of serum metabolomics characteristics of new ginsenoside derivatives in tumor-bearing mice based on UPLC-Q-TOF-MS technology, columnId=null, journalTitle=Chinese Journal of New Drugs, columnName=null, runingTitle=null, highlight=null, articleAbstract=
Objective: A new type of ginsenoside was semi-synthesized by D-ribose and ginsenoside DQ using glycosyl trichloroacetimide ester method. Its in vivo and in vitro anti-tumor activity and its mechanism of action were studied, and the metabolic pathways and products were analyzed by serum metabolomics.
Methods: Using D-ribose and ginsenoside DQ as raw materials, new ginsenoside derivatives were synthesized by chemical methods, and their structures were identified. The effects on S180 cells, human lung adenocarcinoma SPC-A-1 cells, anti-tumor activity in A549 cells and inhibition to mouse S180 tumor cells were determined by MTT method. Its anti-tumor mechanism was explored based on cell metabolomics analysis.
Results: For the first time, a new ocotillol-type ginsenoside, 12-riboside-pseudoginsengenin DQ (RPDQ), was semi-synthesized by chemical methods, and was identified as (20S, 24S)-12-O-α-D-ribofuranosyl-Dama-20,24-epoxy-3β,12β, 25-triol, the yield is 38.6%, and the purity is 99.1%. MTT detection of RPDQ can significantly inhibit the proliferation of three kinds of tumor cells. In vivo experiments demonstrated that RPDQ inhibited solid tumors in tumor-bearing mice, improved the histomorphology of tumor cells, reduced the spleen and thymus indices in tumor-bearing mice and prolonged the survival days of mice. Metabolomics results showed that RPDQ exerted its anti-tumor effects by regulating seven metabolic pathways, including arachidonic acid metabolism, glycerophospholipid metabolism and tryptophan metabolism. Sixteen biomarkers were identified through principal component analysis (PCA) and orthogonal partial least squares discriminant analysis (OPLS-DA) screening, and a network of signaling pathways related to the anti-tumor effects of RPDQ in mice was investigated.
Conclusion: The synthesis of RPDQ provides a reference for the synthesis and activity research of such ginsenoside derivatives. RPDQ shows good anti-tumor activity, which provides a theoretical basis and data support for the further research and development of pseudoginsengenin.
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目的： 采用糖基三氯乙酰亚胺酯法将D-核糖与拟人参皂苷元DQ半合成得到新型人参皂苷，对其体内外抗肿瘤活性以及作用机制进行研究，通过血清代谢组学分析其代谢途径及产物。
方法： 以D-核糖和拟人参皂苷元DQ为原料，通过化学方法合成得到新型人参皂苷衍生物，并对其进行结构鉴定；采用MTT比色法测定其对S180细胞、人肺腺癌SPC-A-1细胞、A549细胞的抗肿瘤活性以及对小鼠S180肿瘤细胞的抑制作用，基于细胞代谢组学分析探究其抗肿瘤作用机制。
结果： 首次通过化学方法半合成得到了新的奥克梯隆（Ocotillol）型人参皂苷，12-核糖基-拟人参皂苷DQ（12-riboside-pseudoginsengenin DQ, RPDQ），鉴定为（20S，24S）-12-O-α-D-呋喃核糖基-达玛-20，24-环氧-3β，12β，25-三醇，产率为38.6%，纯度为99.1%。MTT法检测RPDQ能够明显抑制3种肿瘤细胞的增殖；体内实验证明RPDQ对荷瘤小鼠的实体瘤有抑制作用，能够改善肿瘤细胞组织形态、降低荷瘤小鼠的脏脾和胸腺指数，延长小鼠的生存天数；代谢组学表明RPDQ通过调控花生四烯酸代谢、甘油磷脂代谢、色氨酸代谢等7个代谢途径达到抗肿瘤的作用，通过主成分分析（PCA）和正交偏最小方差判别分析（OPLS-DA）筛选鉴定出16个生物标记物，并研究出RPDQ在小鼠体内发挥抗肿瘤作用相关信号途径网络。
结论： RPDQ的合成为此类人参皂苷衍生物的合成与活性研究提供了参考，RPDQ表现出较好的抗肿瘤活性，为拟人参皂苷的进一步研究与开发提供了理论和数据上的支撑。
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, authorsList=刘芮, 徐伟, 王彩虹, 赵莹, 王振洲)}, authors=[Author(id=1236344967849898972, tenantId=1146029695717560320, journalId=1235980733773295621, articleId=1236344967174615990, orderNo=0, firstName=null, middleName=null, lastName=null, nameCn=null, orcid=null, stid=null, country=null, authorPic=null, dead=0, email=1063904814@qq.com, emailSecond=null, emailThird=null, correspondingAuthor=0, authorType=1, ext={EN=AuthorExt(id=1236344967929590754, tenantId=1146029695717560320, journalId=1235980733773295621, articleId=1236344967174615990, authorId=1236344967849898972, language=EN, stringName=Rui LIU, firstName=Rui, middleName=null, lastName=LIU, prefix=null, suffix=null, authorComment=null, nameInitials=null, affiliation=null, department=null, xref=null, address=Changchun University of Chinese Medicine, Changchun 130117, China, bio=null, bioImg=null, bioContent=null, aboutCorrespAuthor=null), CN=AuthorExt(id=1236344968021865446, tenantId=1146029695717560320, journalId=1235980733773295621, articleId=1236344967174615990, authorId=1236344967849898972, language=CN, stringName=刘芮, firstName=null, middleName=null, lastName=null, prefix=null, suffix=null, authorComment=null, nameInitials=null, affiliation=null, department=null, xref=null, address=长春中医药大学，长春 130117, bio={"content":"
刘芮，女，硕士研究生，研究方向：天然产物活性研究。联系电话：(0431)86763972，E-mail: 1063904814@qq.com。
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刘芮，女，硕士研究生，研究方向：天然产物活性研究。联系电话：(0431)86763972，E-mail: 1063904814@qq.com。
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