Article(id=1322912343256085376, tenantId=1146029695717560320, journalId=1255847919539208197, issueId=1322912162913596032, articleNumber=null, orderNo=null, doi=10.13193/j.issn.1673-7717.2025.01.028, 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=null, acceptedDateStr=null, onlineDate=1793336481155, onlineDateStr=2026-10-30, pubDate=1736438400000, pubDateStr=2025-01-10, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1793336481155, onlineIssueDateStr=2026-10-30, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1793336481155, creator=13701087609, updateTime=1793336481155, updator=13701087609, issue=Issue{id=1322912162913596032, tenantId=1146029695717560320, journalId=1255847919539208197, year='2025', volume='43', issue='1', pageStart='1', pageEnd='258', issueExtLink='null', onlineDate='null', pubDate='1736438400000', pubDateStr='2025-01-10', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=0, createTime=1793336438157, creator='13701087609', updateTime=1793340633627, updator='13701087609', preIssue=null, nextIssue=null, articleTotal=null, ext={EN=IssueExt(id=1322929760048906989, tenantId=1146029695717560320, journalId=1255847919539208197, issueId=1322912162913596032, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1322929760048906990, tenantId=1146029695717560320, journalId=1255847919539208197, issueId=1322912162913596032, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null, downloadFileDto=null}, startPage=157, endPage=164, ext={EN=ArticleExt(id=1322912343444829057, articleId=1322912343256085376, tenantId=1146029695717560320, journalId=1255847919539208197, language=EN, title=Research Progress on Chemical and Pharmacological of Chuanxinlian(Andrographis paniculata)and Prediction Analysis on Quality Markers, columnId=1256183361521967297, journalTitle=Chinese Archives of Traditional Chinese Medicine, columnName=Target on National Project, runingTitle=null, highlight=null, articleAbstract=

Chuanxinlian(Andrographis paniculata)has become a commonly used medicinal plant in China,with the efficacy of clearing heatand removing toxins,cooling blood,eliminating swelling and drying dampness,playing a pivotal role in clinical application. Its chemical compositionmainly includes lactones,flavonoids,phenylpropanoids and other components,with antipyretic,antibacterial,antiviral,antitumor,regulating immunity,improving the cardiovascular system and other pharmacological effects,and is commonly used in the clinic for the treatment of a variety of infectious diseases,tumors as well as thrombotic occlusive vasculitis and so on. The article summarized the chemical composition and pharmacological effects of Chuanxinlian(Andrographis paniculata)in a systematic and comprehensive way,and based on this,it introduced the concept of “quality markers” in traditional Chinese medicine,and carried out the prediction and analysis of the quality markers of Chuanxinlian(Andrographis paniculata)from the aspects of phytopharmacology and chemical composition uniqueness,chemical composition and traditional medicinal properties,chemical composition and traditional efficacy,chemical composition measurability,different compounding environments,and transmission and traceability of chemical compositions. The results revealed that diterpene lactone,flavonoids and alkaloids can be used as candidate species of the quality markers of Chuanxinlian(Andrographis paniculata). It was initially hypothesized that andrographolide,deoxyandrographolide,dehydroandrographolide,neoandrographolide,panicoin,luteolin and apigenin can be used as candidate compounds of the quality markers of Chuanxinlian(Andrographis paniculata),which can lay the foundation of the establishment of the perfect quality evaluation system of Chuanxinlian(Andrographis paniculata)aswell as provide guidance to guarantee the quality of Chuanxinlian(Andrographis paniculata)in the hope of letting the chemical and pharmacological researches serve better to the clinic.

, authors=Hongyang DONG, Lianrui WANG, Yike AN, Huiyan YANG, Mingsan MIAO, authorsList=Hongyang DONG, Lianrui WANG, Yike AN, Huiyan YANG, Mingsan MIAO, authorCompany=null, correspAuthors=Mingsan MIAO, 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=1322912346624111498, articleId=1322912343256085376, tenantId=1146029695717560320, journalId=1255847919539208197, language=CN, title=穿心莲化学、药理研究进展及质量标志物(Q-Marker)预测分析, columnId=1256183362172142382, journalTitle=中华中医药学刊, columnName=国家项目点击, runingTitle=null, highlight=null, articleAbstract=

穿心莲现已成为我国常用药用植物,具有清热解毒、凉血消肿和燥湿的功效,在临床应用中发挥举足轻重的作用。其化学成分主要包括内酯类、黄酮类、苯丙素类及其他类成分,具有解热、抗菌、抗病毒、抗肿瘤、调节免疫、改善心血管系统等药理作用,临床常用来治疗各种感染性疾病、肿瘤以及血栓闭塞性脉管炎等。对穿心莲的化学成分和药理作用进行系统的总结,并以此为基础,引入中药“质量标志物(quality marker,Q-Marker)”的概念,从植物亲缘学及化学成分特有性、化学成分与传统药性相关、化学成分与传统功效相关、化学成分可测性、不同配伍环境、化学成分传递与溯源六个方面进行穿心莲质量标志物的预测分析。结果发现二萜内酯类、黄酮类和生物碱类可作为穿心莲质量标志物的候选物质种类,初步推测穿心莲内酯、脱氧穿心莲内酯、脱水穿心莲内酯、新穿心莲内酯、穿心莲黄酮、木犀草素、芹菜素等成分可作为穿心莲质量标志物的候选化合物,为建立完善的穿心莲质量评价体系奠定基础,也为保证穿心莲的药材质量提供指导,以期让化学和药理研究更好地服务于临床。

, authors=东红阳, 王连睿, 安一珂, 杨卉妍, 苗明三, authorsList=东红阳, 王连睿, 安一珂, 杨卉妍, 苗明三, authorCompany=null, correspAuthors=苗明三, authorNote=

东红阳(1998-),女,河南驻马店人,硕士在读,研究方向:中药药理学。

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苗明三(1965-),男,河南新乡人,教授,博士研究生导师,博士,研究方向:中药药理学。E-mail:。
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东红阳(1998-),女,河南驻马店人,硕士在读,研究方向:中药药理学。

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东红阳(1998-),女,河南驻马店人,硕士在读,研究方向:中药药理学。

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tenantId=1146029695717560320, journalId=1255847919539208197, articleId=1322912343256085376, doi=null, pmid=null, pmcid=null, year=2013, volume=null, issue=null, pageStart=null, pageEnd=null, url=null, language=null, rfNumber=[88], rfOrder=87, authorNames=李文兰, journalName=基于体内过程的穿心莲化学分子群与生殖毒性相关性研究, refType=null, unstructuredReference=李文兰.基于体内过程的穿心莲化学分子群与生殖毒性相关性研究[J].哈尔滨:哈尔滨商业大学,2013., articleTitle=null, refAbstract=null), Reference(id=1322912543555072859, tenantId=1146029695717560320, journalId=1255847919539208197, articleId=1322912343256085376, doi=null, pmid=null, pmcid=null, year=2013, volume=25, issue=4, pageStart=511, pageEnd=513, 524, url=null, language=null, rfNumber=[89], rfOrder=88, authorNames=王学志, 李文兰, 白晶, journalName=天然产物研究与开发, refType=null, unstructuredReference=王学志,李文兰,白晶,等.穿心莲体内血清指纹图谱建立[J].天然产物研究与开发,2013,25(4):511-513, 524., articleTitle=穿心莲体内血清指纹图谱建立, refAbstract=null)], funds=[Fund(id=1322912532532441854, tenantId=1146029695717560320, journalId=1255847919539208197, 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编号化合物中文名称分子式参考文献
1穿心莲内酯C20H30O5[6]
2脱水穿心莲内酯C20H28O4[6]
3新穿心莲内酯C26H40O8[6]
4新穿心莲内酯苷元C20H30O3[7]
5脱水穿心莲内酯苷C26H39O9[8]
6穿心莲内酯苷C26H40O10[9]
73,14-二去氧穿心莲内酯C20H28O3[9]
8穿心莲新苷C26H40O8[8]
913-赖百当二烯-15,16-内酯C21H32O2[8]
103-O-β-D-葡萄糖-14-去氧穿心莲内酯苷C26H41O9[10]
11异穿心莲内酯C20H30O5[10]
12去氧穿心莲内酯苷C26H41O9[10]
13去氧穿心莲内酯C20H30O4[8]
148α-甲氧基-14-去氧-17β-羟基穿心莲内酯C21H34O6[11]
153-去氧穿心莲内酯苷C26H41O9[12]
1614-去氧-15-甲氧基穿心莲内酯C21H31O5[12]
173-脱氢脱氧穿心莲内酯C20H32O4[13]
1814-脱氧-11-氢穿心莲内酯C20H34O5[14]
197(R)-羟基-14-脱氧穿心莲内酯C20H34O4[8]
207(S)-羟基-14-脱氧穿心莲内酯C20H34O4[8]
2114-脱氧-12-甲氧基穿心莲内酯C21H36O5[10]
2212-表-14-脱氧-12-甲氧基穿心莲内酯C21H36O5[10]
2314-脱氧-12-羟基穿心莲内酯C20H34O5[15]
2418-羟基-14-脱氧穿心莲内酯C20H34O5[10]
253-氧代-14-脱氧-11,12-二脱氢穿心莲内酯C20H26O4[10]
266'-乙酰基新穿心莲苷C26H41O8[10]
278-甲基新穿心莲内酯苷元C20H30O3[13]
28(12R)-羟基穿心莲内酯C20H32O6[8]
29(12S)-羟基穿心莲内酯C20H32O6[8]
3019-羟基-8(17),13-ent-赖百当二烯-15,16-内酯C20H30O3[8]
31β-D-吡喃葡萄糖基-8(17),13-ent-赖百当二烯-16,15-内酯-19-酸酯C26H39O9[8]
323α,19-二羟基-15-甲氧基-8(17),11,13-ent-赖百当二烯-16,15-酸酯C21H30O5[8]
338(17),13-ent-赖百当二烯-15,16,19-三醇C20H34O3[8]
343α,15,19-三羟基-8(17),13-ent-赖百当二烯-16-酸C20H32O5[8]
35穿心莲酸C20H28O6[16]
363,13,14,19-四羟基-ent-labdadien-8(17),11-二烯-16,15-内酯C20H30O6[17]
37双穿心莲内酯AC40H56O8[10]
38双穿心莲内酯BC40H56O8[10]
39双穿心莲内酯CC40H56O8[10]
40双穿心莲内酯DC41H61O9[10]
41双穿心莲内酯EC42H60O8[8]
423α,19-二羟基-14,15,16-三-ent-赖百当二烯-8(17),11-二烯-13-酸C17H27O4[8]
433α,12,19-三羟基-13,14,15,16-四去氢-赖百当二烯-8(17)-烯C18H29O3[8]
443-脱氢-14-乙氧基-19-去甲穿心莲内酯C19H25O3[10]
452,4(18)-二烯-14-脱氧-19-去甲穿心莲内酯C19H27O3[10]
466β-羟基-2,4(18)-二烯-14-脱氧-19-去甲穿心莲内酯C19H27O4[10]
4714-脱氧-15-异亚丙基-11,12-二脱氢穿心莲内酯C23H30O4[18]
483,19-异丙亚基-14-脱氧-ent-赖百当二烯-8(17),13-二烯-16,15-内酯C23H34O4[17]
), ArticleFig(id=1322912532003959544, tenantId=1146029695717560320, journalId=1255847919539208197, articleId=1322912343256085376, language=CN, label=表1, caption=

穿心莲中的二萜内酯类化合物

, figureFileSmall=null, figureFileBig=null, tableContent=
编号化合物中文名称分子式参考文献
1穿心莲内酯C20H30O5[6]
2脱水穿心莲内酯C20H28O4[6]
3新穿心莲内酯C26H40O8[6]
4新穿心莲内酯苷元C20H30O3[7]
5脱水穿心莲内酯苷C26H39O9[8]
6穿心莲内酯苷C26H40O10[9]
73,14-二去氧穿心莲内酯C20H28O3[9]
8穿心莲新苷C26H40O8[8]
913-赖百当二烯-15,16-内酯C21H32O2[8]
103-O-β-D-葡萄糖-14-去氧穿心莲内酯苷C26H41O9[10]
11异穿心莲内酯C20H30O5[10]
12去氧穿心莲内酯苷C26H41O9[10]
13去氧穿心莲内酯C20H30O4[8]
148α-甲氧基-14-去氧-17β-羟基穿心莲内酯C21H34O6[11]
153-去氧穿心莲内酯苷C26H41O9[12]
1614-去氧-15-甲氧基穿心莲内酯C21H31O5[12]
173-脱氢脱氧穿心莲内酯C20H32O4[13]
1814-脱氧-11-氢穿心莲内酯C20H34O5[14]
197(R)-羟基-14-脱氧穿心莲内酯C20H34O4[8]
207(S)-羟基-14-脱氧穿心莲内酯C20H34O4[8]
2114-脱氧-12-甲氧基穿心莲内酯C21H36O5[10]
2212-表-14-脱氧-12-甲氧基穿心莲内酯C21H36O5[10]
2314-脱氧-12-羟基穿心莲内酯C20H34O5[15]
2418-羟基-14-脱氧穿心莲内酯C20H34O5[10]
253-氧代-14-脱氧-11,12-二脱氢穿心莲内酯C20H26O4[10]
266'-乙酰基新穿心莲苷C26H41O8[10]
278-甲基新穿心莲内酯苷元C20H30O3[13]
28(12R)-羟基穿心莲内酯C20H32O6[8]
29(12S)-羟基穿心莲内酯C20H32O6[8]
3019-羟基-8(17),13-ent-赖百当二烯-15,16-内酯C20H30O3[8]
31β-D-吡喃葡萄糖基-8(17),13-ent-赖百当二烯-16,15-内酯-19-酸酯C26H39O9[8]
323α,19-二羟基-15-甲氧基-8(17),11,13-ent-赖百当二烯-16,15-酸酯C21H30O5[8]
338(17),13-ent-赖百当二烯-15,16,19-三醇C20H34O3[8]
343α,15,19-三羟基-8(17),13-ent-赖百当二烯-16-酸C20H32O5[8]
35穿心莲酸C20H28O6[16]
363,13,14,19-四羟基-ent-labdadien-8(17),11-二烯-16,15-内酯C20H30O6[17]
37双穿心莲内酯AC40H56O8[10]
38双穿心莲内酯BC40H56O8[10]
39双穿心莲内酯CC40H56O8[10]
40双穿心莲内酯DC41H61O9[10]
41双穿心莲内酯EC42H60O8[8]
423α,19-二羟基-14,15,16-三-ent-赖百当二烯-8(17),11-二烯-13-酸C17H27O4[8]
433α,12,19-三羟基-13,14,15,16-四去氢-赖百当二烯-8(17)-烯C18H29O3[8]
443-脱氢-14-乙氧基-19-去甲穿心莲内酯C19H25O3[10]
452,4(18)-二烯-14-脱氧-19-去甲穿心莲内酯C19H27O3[10]
466β-羟基-2,4(18)-二烯-14-脱氧-19-去甲穿心莲内酯C19H27O4[10]
4714-脱氧-15-异亚丙基-11,12-二脱氢穿心莲内酯C23H30O4[18]
483,19-异丙亚基-14-脱氧-ent-赖百当二烯-8(17),13-二烯-16,15-内酯C23H34O4[17]
), ArticleFig(id=1322912532113011449, tenantId=1146029695717560320, journalId=1255847919539208197, articleId=1322912343256085376, language=EN, label=null, caption=null, figureFileSmall=null, figureFileBig=null, tableContent=
编号化合物中文名称分子式参考文献编号化合物中文名称分子式参考文献
1穿心莲黄酮C18H16O6[6]245,3'-二羟基-7,8,2'-三甲氧基黄酮C18H16O7[22]
2木犀草素C15H10O6[21]255,2',6'-三羟基-7-甲氧基-2'-O-β-D-葡萄糖黄酮苷C22H23O11[23]
3木犀草素-7-O-β-D葡萄糖醛酸苷C21H18O12[21]
4芹菜素C15H10O5[8]26汉黄芩素C16H12O5[23]
5芹菜素-7-O-β-D-葡萄糖苷C17H14O5[21]27黄芩新素C19H18O8[10]
6芹菜素-7-O-β-D-葡萄糖醛酸苷C21H18O11[21]28Didehydroskullcapflavone IC17H16O6[10]
7芹菜素-7-O-β-D-葡萄糖醛酸丁酯C25H26O11[21]297-O-甲基汉黄芩素C17H14O5[10]
8芹菜素-7-O-β-D-葡萄糖醛酸乙酯C24H26O11[21]30穿心莲黄酮苷AC23H26O10[16]
96-C-β-D-葡萄糖-8-C-β-D-半乳糖芹菜素C28H32O17[21]315,7,2',3'-四甲氧基黄酮C19H20O6[16]
10槲皮素C15H10O7[21]32异高山黄芩素C15H10O6[21]
11黄芩黄酮IC17H14O6[20]33异高山黄芩素-8-O-β-D-葡萄糖醛酸苷C21H18O12[21]
125-羟基-7,8-二甲氧基二氢黄酮C17H16O5[18]347-O-methylwogonin-5-O-glucosideC23H24O10[18]
135-羟基-7,2',3'-三甲氧基黄酮C18H16O6[14]355-羟基-7,8,2',5'-四甲氧基-5-O-β-D-葡萄糖黄酮苷C25H29O12[18]
145-羟基-7,8-二甲氧基黄酮C17H14O5[8]
155-羟基-7,8,2',5'-四甲氧基黄酮C19H18O7[8]36穿心莲黄酮苷GC23H24O11[24]
165-羟基-7,8,2',3'-四甲氧基黄酮C19H18O7[18]375,7,8,2'-四甲氧基黄酮C24H27O11[25]
175-羟基-7,2',6'-三甲氧基黄酮C18H16O6[18]382'-羟基-5,7,8-三甲氧基黄酮C23H25O11[22]
185,4'-二羟基-7-甲氧基-8-O-β-D-葡萄糖黄酮苷C22H23O11[21]39金合欢素-7-O-β-D-葡萄糖醛酸苷C22H20O11[21]
406,8-二-C-β-D-葡萄糖白杨素C27H30O16[21]
195,7,8-三甲氧基二氢黄酮C18H18O5[8]411,8-二羟基-3,7-二甲氧基黄酮C15H12O6[26]
205,4'-二羟基-7,8,2',3'-四甲氧基黄酮C19H18O8[22]424,8-二羟基-2,7-二甲氧基黄酮C15H12O6[26]
215,5'-二羟基-7,8,2'-三甲氧基黄酮C18H16O7[22]431,2-二羟基-6,8-二甲氧基黄酮C15H12O6[26]
225-羟基-7,8,2',6'-四甲氧基黄酮C19H18O7[22]443,7,8-三甲氧基-1-羟基黄酮C16H14O6[26]
235,3'-二羟基-7,8,4'-三甲氧基黄酮C18H16O7[22]
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穿心莲中的黄酮类化合物

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编号化合物中文名称分子式参考文献编号化合物中文名称分子式参考文献
1穿心莲黄酮C18H16O6[6]245,3'-二羟基-7,8,2'-三甲氧基黄酮C18H16O7[22]
2木犀草素C15H10O6[21]255,2',6'-三羟基-7-甲氧基-2'-O-β-D-葡萄糖黄酮苷C22H23O11[23]
3木犀草素-7-O-β-D葡萄糖醛酸苷C21H18O12[21]
4芹菜素C15H10O5[8]26汉黄芩素C16H12O5[23]
5芹菜素-7-O-β-D-葡萄糖苷C17H14O5[21]27黄芩新素C19H18O8[10]
6芹菜素-7-O-β-D-葡萄糖醛酸苷C21H18O11[21]28Didehydroskullcapflavone IC17H16O6[10]
7芹菜素-7-O-β-D-葡萄糖醛酸丁酯C25H26O11[21]297-O-甲基汉黄芩素C17H14O5[10]
8芹菜素-7-O-β-D-葡萄糖醛酸乙酯C24H26O11[21]30穿心莲黄酮苷AC23H26O10[16]
96-C-β-D-葡萄糖-8-C-β-D-半乳糖芹菜素C28H32O17[21]315,7,2',3'-四甲氧基黄酮C19H20O6[16]
10槲皮素C15H10O7[21]32异高山黄芩素C15H10O6[21]
11黄芩黄酮IC17H14O6[20]33异高山黄芩素-8-O-β-D-葡萄糖醛酸苷C21H18O12[21]
125-羟基-7,8-二甲氧基二氢黄酮C17H16O5[18]347-O-methylwogonin-5-O-glucosideC23H24O10[18]
135-羟基-7,2',3'-三甲氧基黄酮C18H16O6[14]355-羟基-7,8,2',5'-四甲氧基-5-O-β-D-葡萄糖黄酮苷C25H29O12[18]
145-羟基-7,8-二甲氧基黄酮C17H14O5[8]
155-羟基-7,8,2',5'-四甲氧基黄酮C19H18O7[8]36穿心莲黄酮苷GC23H24O11[24]
165-羟基-7,8,2',3'-四甲氧基黄酮C19H18O7[18]375,7,8,2'-四甲氧基黄酮C24H27O11[25]
175-羟基-7,2',6'-三甲氧基黄酮C18H16O6[18]382'-羟基-5,7,8-三甲氧基黄酮C23H25O11[22]
185,4'-二羟基-7-甲氧基-8-O-β-D-葡萄糖黄酮苷C22H23O11[21]39金合欢素-7-O-β-D-葡萄糖醛酸苷C22H20O11[21]
406,8-二-C-β-D-葡萄糖白杨素C27H30O16[21]
195,7,8-三甲氧基二氢黄酮C18H18O5[8]411,8-二羟基-3,7-二甲氧基黄酮C15H12O6[26]
205,4'-二羟基-7,8,2',3'-四甲氧基黄酮C19H18O8[22]424,8-二羟基-2,7-二甲氧基黄酮C15H12O6[26]
215,5'-二羟基-7,8,2'-三甲氧基黄酮C18H16O7[22]431,2-二羟基-6,8-二甲氧基黄酮C15H12O6[26]
225-羟基-7,8,2',6'-四甲氧基黄酮C19H18O7[22]443,7,8-三甲氧基-1-羟基黄酮C16H14O6[26]
235,3'-二羟基-7,8,4'-三甲氧基黄酮C18H16O7[22]
), ArticleFig(id=1322912532280783612, tenantId=1146029695717560320, journalId=1255847919539208197, articleId=1322912343256085376, language=EN, label=null, caption=null, figureFileSmall=null, figureFileBig=null, tableContent=
编号化合物中文名称分子式参考文献
1咖啡酸C9H8O4[21]
2阿魏酸C10H10O4[21]
3绿原酸C16H18O9[21]
4对羟基桂皮酸C9H10O2[21]
5反式肉桂酸C9H8O2[22]
64-羟基-2-甲氧基肉桂醛C10H10O3[22]
7五加苷C28H35O13[24]
85-咖啡酰基奎宁酸C16H18O9[21]
93,4-二咖啡酰基奎宁酸C25H24O12[21]
103,4-二咖啡酰基奎宁酸甲酯C26H26O12[21]
113,4-二咖啡酰基奎宁酸丁酯C29H32O12[21]
124,5-二咖啡酰基奎宁酸甲酯C26H26O12[21]
), ArticleFig(id=1322912532356281085, tenantId=1146029695717560320, journalId=1255847919539208197, articleId=1322912343256085376, language=CN, label=表3, caption=

穿心莲中的苯丙素类化合物

, figureFileSmall=null, figureFileBig=null, tableContent=
编号化合物中文名称分子式参考文献
1咖啡酸C9H8O4[21]
2阿魏酸C10H10O4[21]
3绿原酸C16H18O9[21]
4对羟基桂皮酸C9H10O2[21]
5反式肉桂酸C9H8O2[22]
64-羟基-2-甲氧基肉桂醛C10H10O3[22]
7五加苷C28H35O13[24]
85-咖啡酰基奎宁酸C16H18O9[21]
93,4-二咖啡酰基奎宁酸C25H24O12[21]
103,4-二咖啡酰基奎宁酸甲酯C26H26O12[21]
113,4-二咖啡酰基奎宁酸丁酯C29H32O12[21]
124,5-二咖啡酰基奎宁酸甲酯C26H26O12[21]
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穿心莲化学、药理研究进展及质量标志物(Q-Marker)预测分析
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东红阳 , 王连睿 , 安一珂 , 杨卉妍 , 苗明三
中华中医药学刊 | 国家项目点击 2025,43(1): 157-164
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中华中医药学刊 |国家项目点击 2025 , 43 (1) : 157 -164
穿心莲化学、药理研究进展及质量标志物(Q-Marker)预测分析
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东红阳, 王连睿, 安一珂, 杨卉妍, 苗明三
作者信息
  • 河南中医药大学,河南 郑州 450046
通讯作者:
苗明三(1965-),男,河南新乡人,教授,博士研究生导师,博士,研究方向:中药药理学。E-mail:。
作者简介:

东红阳(1998-),女,河南驻马店人,硕士在读,研究方向:中药药理学。

Research Progress on Chemical and Pharmacological of Chuanxinlian(Andrographis paniculata)and Prediction Analysis on Quality Markers
Hongyang DONG, Lianrui WANG, Yike AN, Huiyan YANG, Mingsan MIAO
Affiliations
  • Henan University of Chinese Medicine, Zhengzhou 450046, Henan, China
出版时间: 2025-01-10 doi: 10.13193/j.issn.1673-7717.2025.01.028
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穿心莲现已成为我国常用药用植物,具有清热解毒、凉血消肿和燥湿的功效,在临床应用中发挥举足轻重的作用。其化学成分主要包括内酯类、黄酮类、苯丙素类及其他类成分,具有解热、抗菌、抗病毒、抗肿瘤、调节免疫、改善心血管系统等药理作用,临床常用来治疗各种感染性疾病、肿瘤以及血栓闭塞性脉管炎等。对穿心莲的化学成分和药理作用进行系统的总结,并以此为基础,引入中药“质量标志物(quality marker,Q-Marker)”的概念,从植物亲缘学及化学成分特有性、化学成分与传统药性相关、化学成分与传统功效相关、化学成分可测性、不同配伍环境、化学成分传递与溯源六个方面进行穿心莲质量标志物的预测分析。结果发现二萜内酯类、黄酮类和生物碱类可作为穿心莲质量标志物的候选物质种类,初步推测穿心莲内酯、脱氧穿心莲内酯、脱水穿心莲内酯、新穿心莲内酯、穿心莲黄酮、木犀草素、芹菜素等成分可作为穿心莲质量标志物的候选化合物,为建立完善的穿心莲质量评价体系奠定基础,也为保证穿心莲的药材质量提供指导,以期让化学和药理研究更好地服务于临床。

穿心莲  /  质量标志物  /  化学成分  /  药理作用

Chuanxinlian(Andrographis paniculata)has become a commonly used medicinal plant in China,with the efficacy of clearing heatand removing toxins,cooling blood,eliminating swelling and drying dampness,playing a pivotal role in clinical application. Its chemical compositionmainly includes lactones,flavonoids,phenylpropanoids and other components,with antipyretic,antibacterial,antiviral,antitumor,regulating immunity,improving the cardiovascular system and other pharmacological effects,and is commonly used in the clinic for the treatment of a variety of infectious diseases,tumors as well as thrombotic occlusive vasculitis and so on. The article summarized the chemical composition and pharmacological effects of Chuanxinlian(Andrographis paniculata)in a systematic and comprehensive way,and based on this,it introduced the concept of “quality markers” in traditional Chinese medicine,and carried out the prediction and analysis of the quality markers of Chuanxinlian(Andrographis paniculata)from the aspects of phytopharmacology and chemical composition uniqueness,chemical composition and traditional medicinal properties,chemical composition and traditional efficacy,chemical composition measurability,different compounding environments,and transmission and traceability of chemical compositions. The results revealed that diterpene lactone,flavonoids and alkaloids can be used as candidate species of the quality markers of Chuanxinlian(Andrographis paniculata). It was initially hypothesized that andrographolide,deoxyandrographolide,dehydroandrographolide,neoandrographolide,panicoin,luteolin and apigenin can be used as candidate compounds of the quality markers of Chuanxinlian(Andrographis paniculata),which can lay the foundation of the establishment of the perfect quality evaluation system of Chuanxinlian(Andrographis paniculata)aswell as provide guidance to guarantee the quality of Chuanxinlian(Andrographis paniculata)in the hope of letting the chemical and pharmacological researches serve better to the clinic.

Chuanxinlian(Andrographis paniculata)  /  quality markers  /  chemical composition  /  pharmacological effects
东红阳, 王连睿, 安一珂, 杨卉妍, 苗明三. 穿心莲化学、药理研究进展及质量标志物(Q-Marker)预测分析. 中华中医药学刊, 2025 , 43 (1) : 157 -164 . DOI: 10.13193/j.issn.1673-7717.2025.01.028
Hongyang DONG, Lianrui WANG, Yike AN, Huiyan YANG, Mingsan MIAO. Research Progress on Chemical and Pharmacological of Chuanxinlian(Andrographis paniculata)and Prediction Analysis on Quality Markers[J]. Chinese Archives of Traditional Chinese Medicine, 2025 , 43 (1) : 157 -164 . DOI: 10.13193/j.issn.1673-7717.2025.01.028
穿心莲为爵床科植物穿心莲Andrographis paniculata(Burm. f.)Nees的干燥地上部分,原产于印度和东南亚等热带地区[1],现广东、福建等长江南北各地均引种栽培。穿心莲首载于《岭南采药录》[2],味苦,性寒,具有清热解毒,消炎退肿的药效,常用于治疗咽喉炎症,痢疾,还可以解蛇毒,具有很高的药用价值。穿心莲栽培容易,见效快,产量高,效益大,具有非常好的经济效益,但穿心莲的主要化学成分却因栽培、贮藏、加工的方法不同而产生较大不同,进而导致穿心莲的药效存在较大差异。为保证穿心莲药效的稳定性,更好地控制穿心莲的质量,本文总结阐释穿心莲的化学成分和药理作用,并以此为基础,基于中药质量标志物理论(Quality marker,Q-Marker),预测穿心莲的质量标志物,为建立穿心莲完整的质量控制体系提供依据,以促进穿心莲的应用及发展。
内酯类化合物是穿心莲的主要药效成分,包括二萜内酯类化合物、双二萜内酯类及倍半萜内酯类化合物。其中以穿心莲内酯为代表的二萜内酯类化合物对穿心莲药效的发挥起主导作用[3],穿心莲内酯具有抗炎、抑菌、抗病毒等多种药理活性[4]。现代化学对二萜内酯类的研究也较为深入,除穿心莲内酯外还发现脱水穿心莲内酯、新穿心莲内酯及14-脱氧穿心莲内酯等在内的50余种二萜内酯类成分[5]。具体成分见表1,穿心莲二萜内酯类常见母核结构见图1。
黄酮类化合物在穿心莲中的成分占比仅次于内酯类化合物,现代药理学研究表明,黄酮类化合物具有抗氧化、抗菌、抗病毒、抗肿瘤以及维持免疫系统稳态的作用[19]。随着研究的深入,已从穿心莲中分离鉴定出70余种黄酮类化合物,主要有黄酮类、黄酮醇类、二氢黄酮类及查尔酮类等,大多以游离的黄酮苷元形式存在,包括穿心莲黄酮、木犀草素、芹菜素、槲皮素等,仅有少部分以结合成苷的形式存在[20]。具体成分见表2,常见母核结构见图2。
穿心莲还含有多种苯丙素类成分,迄今共分离出近20种,多为简单苯丙素及其衍生物,如咖啡酸、阿魏酸、反式肉桂酸等[21]。具体成分见表3,常见母核结构见图3。
穿心莲含量丰富,除以上成分外,还含有环烯醚萜类、甾醇类、生物碱类及部分有机酸和三萜类成分[27]。张慧等研究发现,穿心莲中还含有维生素和矿物质等营养成分,以及包含人体所必需的7种氨基酸在内的至少17种氨基酸[28]。穿心莲中的化学成分还有待进一步地挖掘和开发。
穿心莲作为常用中药,具有清热凉血的功效。郑晨等[29]研究发现,喜炎平注射液(主要成分为:水溶性穿心莲内酯总酯磺化物)可通过抑制发热家兔下丘脑和脑脊液中中枢致热介质前列腺素E2(Prostaglandin E2,PGE2)、环磷酸腺苷(Cyclic adenosine monophosphate,cAMP)的合成,促进脑脊液中中枢解热介质精氨酸加压素(Arginine vasopressin,AVP)的释放发挥解热作用。徐志勇等[30]研究证实,穿心莲软胶囊可通过下调下丘脑和脑脊液中中枢发热介质cAMP、上调下丘脑中抑制性神经递质5-羟色胺(5-hydroxytryptamine,5-HT)含量对脂多糖发热模型家兔发挥良好的解热作用,同时提出,穿心莲软胶囊对生理状态下的家兔体温也有一定的下调作用。李春英等[31]用酵母菌感染诱导大鼠发热模型,证实了穿心莲提取物对细菌感染引起的高热也具有明显的退热作用,作用时长达6 h。
现代药理学研究表明穿心莲具有抗菌消炎的药理作用,其中的二萜内酯类提取物穿心莲内酯是发挥抗菌作用的主要成分之一[32]。铜绿假单胞菌感染生物体后,分泌的多糖蛋白复合物聚集成膜,称为生物被膜[33],生物被膜的产生会降低抗生素的治疗效果。程惠娟等[34]观察到穿心莲内酯可以在早期抑制生物被膜的形成,并在一定程度上破坏成熟的生物被膜,从而对铜绿假单胞菌感染产生抑制作用。国外学者对大肠杆菌的耐药模式进行研究发现,穿心莲内酯可以通过下调头孢菌素酶(Ampicillin,AmpC)基因的表达,减少胞外多糖的产生从而抑制大肠杆菌的生长和生物膜的形成,对大肠杆菌发挥抗菌作用[35]。金典等[36]在体外观察金黄色葡萄球菌的生长,证实了穿心莲内酯的干预可大大提高细菌中组氨酸、亮氨酸和苯丙氨酸的浓度,从而增加葡萄糖的代谢,间接地降低细菌的致病性和毒性,从而对金黄色葡萄球菌的感染产生抗菌作用。穿心莲内酯抗菌谱广,除此以外还对凝固酶阴性葡萄球菌、链球菌、白色念珠菌、表皮葡萄球菌、肺炎克雷伯氏菌、鼠沙门伤寒杆菌、甲型溶血性链球菌、乙型溶血性链球菌、鲍曼不动杆菌等发挥抑制作用[37]。
穿心莲提取物对多种病毒的繁殖和复制发挥抑制作用,具有良好的抗病毒疗效。体外实验表明,穿心莲内酯可下调半胱氨酸天冬氨酸蛋白水解酶(Cysteinyl aspartate specific proteinase,Caspase)-1、Caspase-3和多聚二磷酸腺苷核糖聚合酶(Poly ADP-ribosepolymerase,PARP)蛋白的表达,从而抑制基孔肯雅病毒(Chikungunyavirus,CHIKV)诱导的内质网应激和细胞凋亡,从而对孔肯雅病毒的感染发挥抑制作用[38]。WANG D Y等[39]研究发现,穿心莲内酯处理可以显著抑制肠道病毒D68(Enterovirus D-68,EV-D68)RNA复制和蛋白质合成,从而发挥抗病毒的疗效,并且在杀毒浓度下不产生显著的细胞毒性。CHURIYA H等[40]研究显示,穿心莲干燥叶子的90%乙醇提取物能够抑制转染于肺癌人类肺泡基底上皮细胞(A549细胞)上的猴逆转录病毒(Simian Retrovirus,SRV),其效果与阳性药拉米夫定相似,且对A549细胞系的毒性相对较小,对SRV发挥抗病毒的疗效。除此以外,研究显示穿心莲内酯还对甲型流感病毒、乙肝病毒、丙肝病毒、1-型单纯疱疹病毒、人类疱疹病毒、人乳头瘤病毒、基孔肯亚病毒等病毒有抑制作用[41]。
穿心莲的抗癌作用已在各种癌症实验中得到了验证,对于穿心莲抗结肠癌、乳腺癌的研究最多[42]。PARAMASIVAM V等研究表明,用穿心莲叶提取物处理MCF7人乳腺癌细胞,可大大降低该癌细胞的活力,穿心莲叶提取物对MCF7人乳腺癌细胞发挥抑制增殖的作用[43]。KHAN I等[44]研究发现,穿心莲的主要药用成分穿心莲内酯可以负调控Notch信号通路,从而抑制结肠癌相关细胞的增殖。除此以外,研究表明穿心莲内酯的衍生物也具有优秀的抗肿瘤活性,QUAH S Y等[45]研究发现,穿心莲内酯衍生物SRJ09和SRJ23可以通过和致癌蛋白(Kirsten rats arcomaviral oncogene homolog,K-Ras)蛋白结合,使致癌蛋白失去活性,发挥抗肿瘤作用。穿心莲内酯及其衍生物均表现出很强的抗癌活性,抗癌机制较为复杂,但穿心莲内酯已成为潜在的抗肿瘤中药制剂成分。
现有研究表明穿心莲对细胞免疫有一定的调节作用,主要通过影响巨噬细胞以及细胞因子的分泌而发挥免疫调节作用[46]。WANG W等[47]研究发现,穿心莲可以通过下调白细胞介素4(Interleukin 4,IL-4)诱导的巨噬细胞甘露糖受体(CD206)和脂多糖(Lipopolysaccharide,LPS)诱导的巨噬细胞主要组织相容性复合体(Major histocompatibility complex class I,MHC I)、CD40、CD80、CD86的表达来抑制巨噬细胞的活化,从而抑制M1型巨噬细胞和M2型巨噬细胞因子的表达,抑制机体的免疫过程。JING M等[48]通过体外研究证实,穿心莲内酯的衍生物14-硫辛酰-3,19-二羟基-穿心莲内酯可以通过减少巨噬细胞生长中活性氧和一氧化氮的产生抑制巨噬细胞的生长,还能通过逆转炎性细胞因子的表达从而抑制炎症反应的发生以调节免疫系统。NIE X等[49]通过对不同穿心莲内酯衍生物对细胞因子的影响实验中证实,穿心莲内酯衍生物3b、5a和5b通过抑制肿瘤坏死因子-α(Tumor necrosis factor-α,TNF-α)/核转录因子κB(Nuclear transcription factor κB,NF-κB)和Toll样受体4(Toll-like receptor 4,TLR4)/NF-κB信号通路抑制免疫反应,化合物3b、3a,5b和6b通过减弱p65和核因子κB抑制因子α(IkappaB-alpha,IκBα)的磷酸化抑制免疫反应,化合物6b通过抑制NF-κB、p65亚基的表达抑制免疫反应,化合物3b还能通过抑制p65磷酸化和血清促炎细胞因子和趋化因子的减少抑制免疫反应,首次提出并确定了化合物3b是一种有效的免疫抑制剂,具有保护急性肺部感染的潜力。
现代研究表明,穿心莲对心血管系统具有良好的治疗和保护作用。陈思[50]研究制作了富含穿心莲内酯的水凝胶制剂,并将该制剂导入心肌梗死的大鼠心脏中,发现该制剂能促进心脏血管的生成,大大改善了心肌梗死的微环境,治疗后大鼠心肌梗死面积和纤维化面积分别减少了17.9%和33.5%,心脏功能显著恢复。HAMIDY M Y等[51]研究发现,泡沫细胞的形成存在于动脉粥样硬化发生的早期阶段,用穿心莲内酯干预动脉粥样硬化大鼠模型,发现给予穿心莲内酯的大鼠泡沫细胞数量相比未干预模型大鼠显著降低,证实了穿心莲内酯在动脉粥样硬化的起始阶段可抑制泡沫细胞的形成,延缓病情的发展,具有良好的抗动脉粥样硬化作用。XIE S Y等[52]利用动物实验,首次发现穿心莲的醇提物可以通过显著增强核因子红细胞系2相关因子2(Nuclear Factor erythroid 2-Related Factor 2,Nrf2)信号通路的活性,下调心肌梗死小鼠的心脏肥大,心脏纤维化,炎症反应和心脏氧化应激来缓解不良心脏重塑,证明穿心莲可在心肌梗死后发挥心脏保护作用。
除以上药理作用外,穿心莲还具有对中枢神经系统、消化系统以及抗生育等药理作用。大量实验研究表明,穿心莲的提取物可以穿过血脑屏障并进入大脑的不同区域,这一发现促进了穿心莲提取物对中枢神经系统影响的研究[42],丁永波等[53]通过实验证实,穿心莲的提取物可抑制帕金森小鼠模型中小胶质细胞的活化功能,以减少致炎因子的释放,减轻神经系统炎症,进而起到神经保护作用。董晓雪探究了发酵穿心莲对仔猪生产性能和肠道功能的影响,结果显示发酵穿心莲可以降低腹泻率,提高猪仔的肠道功能[54]。李荣等[55]研究报道了穿心莲可通过抗孕激素作用和直接损伤绒毛细胞发挥抗生育的作用。
中药化学成分复杂多样,易受到种植、采收、贮藏、加工等过程中的各种条件影响,而导致中药材之间成分、药效差异显著。为保证中药材的质量可控、药效可控,能更好地服务于临床,2016年刘昌孝院士提出Q-Marker即中药“质量标志物”的新概念[56]。“中药质量标志物”概念以传递性与溯源性、特有性、有效性、可测性和处方配伍为核心内容,总结归纳可用于控制中药安全性和有效性的标志性物质[57]。本文基于此概念,对穿心莲的Q-Marker进行预测分析,为穿心莲药材的质量控制、疗效保证提供系统的规范和总结。
穿心莲为爵床科植物穿心莲Andrographis paniculata(Burm. f.)Nees的干燥地上部分,爵床科植物种类繁多,大约包括250属4000多种。该科植物性喜温暖、湿润气候,大部分生长在热带、亚热带地区,只有少数种类可生长在温带地区。中国约有50属400余种,多分布于长江以南阴湿的山谷或石灰岩地区,以云南省最多[58]。该科植物含有不少种药用植物[59],如板蓝[60]、穿心莲、尖药花、枪刀药[61]、九头狮子草[62]等。爵床科植物常具有抗癌[63]、抗菌[64]、抗炎[65]、抗糖尿病[66]的功效,多含有生物碱[67]、黄酮[68]、丹宁[69]、萜类[70]化合物,其中生物碱类和黄酮类化合物含量较高。穿心莲为爵床科常用的药用植物,其化学成分的组成和含量与其他爵床科植物具有差异性,主要化学成分为二萜内酯类、黄酮类和苯丙素类化合物,而二萜内酯类和黄酮类是其主要的活性成分。《中华人民共和国药典》为保证穿心莲药材的质量,以“穿心莲内酯、脱水穿心莲内酯”等二萜内酯类成分为指标,对药材质量进行控制[71]。当前穿心莲的化学成分研究也多以二萜内酯类成分为主导[72],研究显示穿心莲内酯、脱水穿心莲内酯、异穿心莲内酯、新穿心莲内酯和14去氧穿心莲内酯为穿心莲的特有性化学成分[73],常作为该植物鉴定和质量控制的指标性成分,因此基于植物亲缘学及化学成分特有性推测穿心莲内酯、脱水穿心莲内酯、异穿心莲内酯、新穿心莲内酯和14去氧穿心莲内酯可作为穿心莲的质量标志物。
中药的性味归经是中医药理论的重要组成部分,中药的药性是对药物性质和作用的高度概括,对临床用药和配伍也具有重要意义。刘昌孝院士提出“性-效-物”的三元关系,并阐释了其相互作用的机制,指出药性的分析在质量标志物的预测方面也具有重要意义[74]。穿心莲性寒,味苦,归心、肺经[75],中医认为,寒性药物多具有清热泻火、凉血解毒的功效;苦味药物能泄、能燥、能坚,首先苦能通泄;其次苦能降泄;再次苦能清泄,能燥指苦燥显能坚:首先苦能坚阴,即泻火存阴,再指苦能坚厚肠胃。穿心莲具有清热燥湿,凉血解毒的功效,与寒性药和苦味药的药性相符合。现代化学研究显示,苦味药的苦多来源于生物碱类、苷类、挥发油、黄酮类、苦味素及木脂素等;近期魏子路等利用电子舌技术、紫外-可见分光光度法(Ultravioletvisible spectroscopy,UV-Vis)以及高效液相色谱(High performance liquid chromatography,HPLC)法测定白术的苦味值与其成分之间的关系并进行双变量“谱味”相关性分析,指出内酯类成分也是苦味的物质基础。“寒性”主要与挥发油、生物碱、卤素及其盐类、重金属元素、蒽醌类成分相关[76]。因此,基于化学成分和传统药性之间的关系,推测二萜内酯类及生物碱类成分可作为穿心莲的质量标志物。
中药的传统功效是现代药理学的研究基础,也是中药应用于临床的根本遵循。将中药的传统功效与其化学成分之间的关系进行挖掘和阐述,有助于明确中药的药效物质基础,建立与药物临床效能直接关联的中药评价体系。《泉州本草》[77]记载:“穿心莲,一名一见喜、百病草、苦草。味苦,性寒,无毒。入心、肺二经。清热解毒,消炎退肿。治咽喉炎症,痢疾,高热”。清热解毒,消炎退肿对应上文所述解热作用、抗菌作用、抗病毒作用、调节免疫系统等多种药理作用。穿心莲内酯是穿心莲发挥解热作用的活性成分,对于伤寒、副伤寒菌苗所引起发热或者由2,4-二硝基苯酚所致的发热均有一定的解热效果,对同时感染肺炎双球菌和溶血性链球菌培养物所致的发热有延缓体温上升时间、降低体温上升程度作用[78]。二萜内酯类化合物是穿心莲发挥抗菌作用的主要活性成分[32],黄嘉玲等[20]研究发现穿心莲中黄酮类成分也具有明显的抑制真菌感染的作用。穿心莲内酯是穿心莲发挥抗病毒作用的有效成分,蔡文涛提出[79],脱水穿心莲内酯同穿心莲内酯一样发挥抗病毒的功效,并指出脱水穿心莲内酯是通过激活磷脂酰肌醇3激酶(Phosphatidylinositol 3-kinase,PI3K)/蛋白激酶B(Protein kinase B,Akt)通路来抑制流感诱导的细胞凋亡,提高了宿主细胞的存活率,从而发挥抗流感感染的作用。穿心莲的免疫系统调节作用与穿心莲内酯密切相关,IRURETAGOYENA M I等[80]发现,穿心莲内酯能有效阻断体内外T淋巴细胞的刺激作用,下调体液和细胞适应性免疫反应,此外,穿心莲内酯能干扰T细胞繁殖,下调变态原刺激的细胞因子释放,对体液免疫和细胞免疫发挥调节作用,增强机体的免疫力。上述现代药理学研究的药理作用与传统古籍记载的“清热解毒,消炎退肿”的药效相一致,因此基于穿心莲化学成分与传统功效之间的关系,推测二萜内酯类和黄酮类可作为穿心莲的质量标志物。
化学成分的可测性是作为中药质量标志物的基础,是中药质量标志物选取的根本原则。方朝缵[6]采用UPLC法建立穿心莲不同部位(主茎、侧茎、叶)的指纹图谱,结果在穿心莲主茎、侧茎、叶均确定了13个共有峰,并指认出木犀草素-7-O-β-D葡萄糖醛酸苷、穿心莲内酯、新穿心莲内酯、14-去氧穿心莲内酯和脱水穿心莲内酯5个特征峰,相似度评价结果显示,同一部位的质量较为稳定,在不同部位三者的化学成分差异也较大。赵晴等[81]采用气相色谱仪-质谱联用仪(Gaschromatography-mass spectrometry,GC-MS)、HPLC、UV对穿心莲提取物进行成分分析和含量测定,结果显示穿心莲内酯的含量为2.67%,黄酮的含量为4.85%,含量较高。张峻淞等[82]建立穿心莲饮片的HPLC指纹图谱,测定了穿心莲内酯的含量达0.16%~0.51%,新穿心莲内酯的含量达0.13%~0.34%,脱水穿心莲内酯的含量达0.11%~0.55%,去氧穿心莲内酯的含量达0.12%~0.49%,上述4个内酯成分总含量达0.75%~1.52%。综上,穿心莲中二萜内酯类、黄酮类成分可通过现代分析检测手段准确测定其化学含量,可作为基于穿心莲化学成分可测性得到的质量标志物。
中药方剂多以复方的形式运用于临床治疗,配伍复方的药效通常大于单味中药[83]。单味中药在不同的配伍环境中可发挥不同的作用,临床常用于治疗不同的疾病。“四味穿心莲散”由穿心莲、辣蓼、大青叶和葫芦茶配伍组成,具有清热解毒、除湿化滞的功效,常用来治疗泻痢和积滞。方中穿心莲具有广谱抗菌和抗病毒的功效,发挥抗菌消炎的功效,发挥抑菌作用的主要效用成分为二萜内酯类和黄酮类成分[84]。“清火栀麦片”由穿心莲、麦冬和栀子等中药组成,为清热剂,具有清热解毒,凉血消肿之功效,主治肺胃热盛所致的咽喉肿痛,发热,牙痛,目赤,方中穿心莲苦寒降泄,清热解毒,消炎退肿,而发挥清热作用的主要效用成分为二萜内酯类成分,发挥抗炎作用的效用成分为二萜内酯类和黄酮类成分[85]。“消炎利胆片”由穿心莲、苦木、溪黄草3味药配伍组成,三药合用发挥清热解毒、利湿通淋、利胆的效果,配伍中穿心莲味苦寒,清热解毒、燥湿泻火为臣药,其主要效用成分为二萜内酯类、黄酮类成分[86]。综上,在复方配伍环境中,穿心莲主要发挥抗菌消炎、清热解毒的功效,主要的效用成分为二萜内酯类和黄酮类,因此,基于不同的复方配伍环境中,可将二萜内酯类和黄酮类成分确定为穿心莲的质量标志物。
中药化学成分复杂,且中药材从种植、采收、加工、炮制、制剂到临床应用被机体代谢,其化学成分受到其中环节的各个因素影响,任何一个环节中药的化学成分都会发生显著的变化。要保证中药材临床应用的疗效,应当对中药材采收加工过程中的任何一个环节进行质量控制。穿心莲的炮制过程主要为除去杂质,洗净,切段,干燥,炮制加工后使药材洁净,便于调配和煎煮。《中华人民共和国药典》2020年版[71]对穿心莲的质量评价标准即为干燥茎叶中脱水穿心莲内酯和穿心莲内酯的总含量要求。药物进入体内后,吸收入血,发挥特定的生理功效,入血成分及代谢产物的体内过程是中药发挥临床疗效的基础。因此,对穿心莲的入血成分和代谢产物进行测定和规范是控制穿心莲药材质量的重要手段。刘开永等[87]运用血清药物化学的理论,利用液质连用技术对比分析穿心莲超微粉在鸡体内外的成分,发现9个入血成分,其中有4个成分来源于原药,它们分别是穿心莲内酯、新穿心莲内酯、脱氧穿心莲内酯、脱水穿心莲内酯,其余可能为代谢产物。李文兰等[88]建立穿心莲在血,尿,粪及肝匀浆中成分的高效液相色谱-质谱联用技术(High performance liquid chromatography-mass spectrometry,HPLC-MS)图谱,鉴定出穿心莲在血液中12个化学成分。王学志等[89]采用高效液相色谱-二级线性阵列检测器法(High Performance Liquid Chromatography with Diode Array Detector,HPLC-DAD)技术,建立穿心莲血清指纹图谱,得到穿心莲入血10个成分中,其中有4个为原型成分,推测其为穿心莲内酯、脱氧穿心莲内酯、新穿心莲内酯和脱水穿心莲内酯,6个推测其为体内代谢产物。综上,根据穿心莲的炮制要求和最终入血成分可将穿心莲内酯、脱氧穿心莲内酯、新穿心莲内酯和脱水穿心莲内酯作为穿心莲的质量标志物。
基于前文对穿心莲所含化学成分的总结,从植物亲缘学及化学成分特有性方面预测可将穿心莲内酯、脱水穿心莲内酯、异穿心莲内酯、新穿心莲内酯和14去氧穿心莲内酯作为穿心莲的质量标志物,从化学成分与传统药性相关方面考虑可将二萜内酯类及生物碱类成分作为穿心莲的质量标志物,从化学成分与传统功效相关方面预测可将二萜内酯类及黄酮类成分作为穿心莲的质量标志物,从化学成分可测性方面进行预测可将二萜内酯类和黄酮类作为穿心莲的质量标志物、从不同配伍环境方面进行预测可将二萜内酯类和黄酮类作为穿心莲的质量标志物,从化学成分传递与溯源方面进行预测可将穿心莲内酯、脱氧穿心莲内酯、新穿心莲内酯和脱水穿心莲内酯作为穿心莲的质量标志物,如图4所示。因此初步推测二萜内酯类、黄酮类和生物碱类可作为穿心莲质量标志物的物质种类;穿心莲内酯、脱氧穿心莲内酯、脱水穿心莲内酯、新穿心莲内酯、穿心莲黄酮、木犀草素、芹菜素等成分可作为穿心莲质量标志物的候选化合物。
穿心莲作为外来引进中药材,因其突出的清热解毒、凉血消肿功效,已经成为临床常用的一味清热药。现穿心莲已在国内进行大量的栽培种植,主产于广东、广西。穿心莲从种植到临床应用经历多个环节,任何一个环节的变化都会对穿心莲药材的质量和药效产生巨大的影响,建立科学、全面的质量控制体系是保证穿心莲临床疗效的基础。
本文全面列举了穿心莲药材所含的二萜内酯类、黄酮类、苯丙素类以及其他类化学成分,总结阐释了穿心莲解热、抗菌、抗病毒、抗肿瘤、调节免疫系统、改善心血管系统等药理作用。并以这两部分内容为基础引入中药“质量标志物”的概念,基于上文总结的穿心莲的化学成分,从植物亲缘学及化学成分特有性、传统药性、传统功效、化学成分可测性、不同配伍环境以及化学成分传递与溯源六个方面明确可以控制穿心莲药材质量的标志物。为全面建立穿心莲的质量评价体系,保证穿心莲的临床药效提供了基础。未来研究还需进一步明确穿心莲的药效物质基础,借助网络药理学、分子对接等手段探寻穿心莲发挥药理作用的活性成分,并将其作为穿心莲药材评价的质量标志物,建立逐步完善的穿心莲的质量评价体系。
  • 国家自然科学基金项目(82274119)
  • 国家中医药管理局岐黄学者项目(国中医药人教函2022-6)
  • 河南省重大专项(221100310400)
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2025年第43卷第1期
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doi: 10.13193/j.issn.1673-7717.2025.01.028
  • 首发时间:2026-10-30
  • 出版时间:2025-01-10
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国家自然科学基金项目(82274119)
国家中医药管理局岐黄学者项目(国中医药人教函2022-6)
河南省重大专项(221100310400)
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    河南中医药大学,河南 郑州 450046

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苗明三(1965-),男,河南新乡人,教授,博士研究生导师,博士,研究方向:中药药理学。E-mail:。
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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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