中草药

中药活性成分跨膜转运机制与其增效策略研究进展

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中草药 | 综述 2026,57(1): 364-374

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中草药 |综述 2026 , 57 (1) : 364 -374

中药活性成分跨膜转运机制与其增效策略研究进展

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姚嘉祎¹, 孙爽¹, 杨大宇¹, 郭玉岩¹, 吕邵娃¹

作者信息

通讯作者:

吕邵娃

作者简介:

姚嘉祎: 姚嘉祎,硕士研究生,研究方向为中药及复方的药效物质基础。E-mail:2926103540@qq.com

Research advances in transmembrane transport mechanisms and efficacy-enhancing strategies for active ingredients of traditional Chinese medicine

YAO Jiayi, SUN Shuang, YANG Dayu, GUO Yuyan, LYU Shaowa

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doi: 10.7501/j.issn.0253-2670.2026.01.033

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摘要

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跨膜转运作为药物吸收、分布与代谢的核心环节，直接决定中药活性成分的生物利用度及靶组织分布，是其体内暴露水平与药效发挥的关键制约因素。中药成分结构多样、机制复杂，其口服生物利用度普遍较低，严重限制了临床疗效的充分发挥，成为现代中药制剂研发的瓶颈。通过系统综述黄酮类、生物碱类、皂苷类、萜类、多糖及有机酸等主要中药活性成分的跨膜转运机制，重点揭示了其结构-转运关系及多种转运蛋白（如P-糖蛋白、多药耐药相关蛋白、有机阴离子转运多肽等）参与的复杂调控网络。鉴于传统研究长期聚焦于成分的定性定量分析，对跨膜转运机制的解析相对薄弱，制约了基于机制导向的制剂设计与优化。通过进一步深入梳理基于转运机制的新型增效策略，包括新型递送系统、结构修饰、外排蛋白抑制、菌群代谢增效及中药配伍协同，旨在为突破中药有效成分的体内递送屏障，提升中药制剂生物利用度以及实现临床精准用药提供启示。

关键词

跨膜转运 / 生物利用度 / 膜屏障突破 / 转运体调控 / 被动扩散 / 主动转运 / 增效策略

Abstract

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Transmembrane transport, as a core process in drug absorption, distribution, and metabolism, directly determines the bioavailability and target tissue distribution of active ingredients in traditional Chinese medicine (TCM). It is a key limiting factor for their systemic exposure and exertion of drug efficacy. The structural diversity and complex mechanisms of TCM components generally lead to low oral bioavailability, which severely restricts their full clinical therapeutic effects and has become a bottleneck in the development of modern TCM formulations. This article systematically reviews the transmembrane transport mechanisms of major active ingredients in TCM, such as flavonoids, alkaloids, saponins, terpenoids, polysaccharides, and organic acids, with a focus on elucidating their structure-transport relationships and the complex regulatory networks involving various transport proteins (e.g., P-glycoprotein, multidrug resistance-associated proteins, organic anion transporting polypeptides, etc.). Given that traditional research has long focused on qualitative and quantitative analysis of components while relatively neglecting the exploration of transmembrane transport mechanisms, hindering mechanism-guided formulation design and optimization. This review further delves into novel enhancement strategies based on transport mechanisms. These include advanced delivery systems, structural modification, efflux protein inhibition, gut microbiota-mediated metabolic enhancement, and synergistic compatibility of TCM ingredients. The aim is to overcome the in vivo delivery barriers of active TCM components, improve the bioavailability of TCM formulations, and ultimately provide insights for achieving precise clinical medication.

Key words

transmembrane transport / bioavailability / membrane barrier penetration / transporter regulation / passive diffusion / active transport / bioavailability-enhancing strategies

引用本文

姚嘉祎, 孙爽, 杨大宇, 郭玉岩, 吕邵娃. 中药活性成分跨膜转运机制与其增效策略研究进展. 中草药, 2026 , 57 (1) : 364 -374 . DOI: 10.7501/j.issn.0253-2670.2026.01.033

YAO Jiayi, SUN Shuang, YANG Dayu, GUO Yuyan, LYU Shaowa. Research advances in transmembrane transport mechanisms and efficacy-enhancing strategies for active ingredients of traditional Chinese medicine[J]. Chinese Traditional and Herbal Drugs, 2026 , 57 (1) : 364 -374 . DOI: 10.7501/j.issn.0253-2670.2026.01.033

基金

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国家自然科学基金资助项目 (82474098)

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Morales Castro D, Dresser L, Granton J, et al.Pharmacokinetic alterations associated with critical illness[J]. Clin Pharmacokinet, 2023, 62(2):209-220.
慈小燕,崔涛,武卫党,等.药物的跨膜转运机制研究进展[J]. 药物评价研究, 2018, 41(6):973-979.
Sugano K, Kansy M, Artursson P, et al. Coexistence of passive and carrier-mediated processes in drug transport[J]. Nat Rev Drug Discov, 2010, 9(8):597-614.
Wu K, Kwon S H, Zhou X H, et al. Overcoming challenges in small-molecule drug bioavailability:A review of key factors and approaches[J]. Int J Mol Sci, 2024, 25(23):13121.
Zhang H, Hassan Y I, Liu R H, et al. Molecular mechanisms underlying the absorption of aglycone and glycosidic flavonoids in a Caco-2 BBe1 cell model[J]. ACS Omega, 2020, 5(19):10782-10793.
胡军林,杨涛,何开勇.高良姜素在大鼠肠道的吸收机制[J]. 医药导报, 2015, 34(5):612-616.
张美玲,王新春,黄志巧,等.异甘草素在Caco-2细胞的摄取特性[J]. 中国实验方剂学杂志, 2011, 17(4):134-136.
张爱杰,李,刘羽康,等.甘草苷体内暴露特征及体外跨膜转运机制研究[J]. 中草药, 2021, 52(7):2053-2061.
徐倩,欧阳怡,吴鸿飞.黄芩苷及其固体脂质纳米粒在Caco-2细胞上的吸收机制研究[J]. 中国药学杂志,2019, 54(12):1000-1006.
Zhang X F, Song J H, Shi X P, et al. Absorption and metabolism characteristics of rutin in Caco-2 cells[J]. Sci World J, 2013, 2013:382350.
Chow J, Yang X L, Hu J R, et al. Gastrointestinal absorption and its regulation of hawthorn leaves flavonoids[J]. Sci Rep, 2025, 15(1):658.
Dai P M, Zhu L J, Luo F F, et al. Triple recycling processes impact systemic and local bioavailability of orally administered flavonoids[J]. AAPS J, 2015, 17(3):723-736.
Li P, Tian Y H, Wang H, et al. Effect of hepatic impairment on the pharmacokinetics of baicalin in rats:Critical roles of gut microbiota and hepatic transporters[J]. Pharmaceutics, 2025, 17(7):851.
Actis-Goretta L, Dew T P, Lévèques A, et al.Gastrointestinal absorption and metabolism of hesperetin-7-O-rutinoside and hesperetin-7-O-glucoside in healthy humans[J]. Mol Nutr Food Res, 2015, 59(9):1651-1662.
Zhang J M, Liao W, He Y X, et al. Study on intestinal absorption and pharmacokinetic characterization of diester diterpenoid alkaloids in precipitation derived from FuziGancao herb-pair decoction for its potential interaction mechanism investigation[J]. J Ethnopharmacol, 2013,147(1):128-135.
Epalle N H, Beitz E. Local attraction of substrates and cosubstrates enhances weak acid and base transmembrane transport[J]. Biomolecules, 2022, 12(12):1794.
Cui H M, Zhang Q Y, Wang J L, et al. Poor permeability and absorption affect the activity of four alkaloids from Coptis[J]. Mol Med Rep, 2015, 12(5):7160-7168.
马小花,魏玉辉,王丹,等.苦参碱大鼠肠吸收动力学研究[J]. 中成药, 2011, 33(10):1695-1699.
王丹,魏玉辉,张帆,等.拉马宁碱的大鼠在体肠吸收机制研究[J]. 中成药, 2012, 34(5):828-831.
葛修通,赵佳慧,任文静,等.黄柏不同炮制品中生物碱类成分在肾小管上皮细胞中的摄入差异考察[J]. 中草药, 2023, 54(18):5993-6000.
石琳,王泽,崔涛,等.肉碱/有机阳离子转运体对元胡止痛方中主要药性成分的转运机制研究[J]. 中草药, 2021, 52(8):2384-2391.
Cao Y H, Shi Y W, Cai Y, et al. The effects of traditional Chinese medicine on P-glycoprotein-mediated multidrug resistance and approaches for studying the herb-Pglycoprotein interactions[J]. Drug Metab Dispos, 2020,48(10):972-979.
Zhang Y T, Yu Y Q, Yan X X, et al. Different structures of berberine and five other protoberberine alkaloids that affect P-glycoprotein-mediated efflux capacity[J]. Acta Pharmacol Sin, 2019, 40(1):133-142.
陈健龙,张玉玲,董宇,等.小檗碱在Caco-2细胞单层模型中吸收和外排机制的研究[J]. 中成药, 2014,36(4):719-723.
高秀蓉,蒋学华,杜青青,等. P-糖蛋白抑制剂对蝙蝠葛碱跨膜转运的影响[J]. 华西药学杂志, 2013, 28(2):135-139.
Zhang Y, Hao R J, Chen J D, et al. Health benefits of saponins and its mechanisms:Perspectives from absorption, metabolism, and interaction with gut[J]. Crit Rev Food Sci Nutr, 2024, 64(25):9311-9332.
王筱懿,仇坤,陈明,等.三七皂苷R1、人参皂苷Rg1和人参皂苷Rb1的HPLC定量分析及其肠黏膜渗透性研究[J]. 上海中医药杂志, 2023, 57(9):78-84.
邢媛月,任偲琪,刘奇玮,等.柴胡皂苷d的体内外肠道吸收机制研究[J]. 中国药科大学学报, 2022, 53(4):473-480.
申文雯,仇守蓓,汤道权,等.蒸三七的肠吸收特性研究[J]. 中国新药杂志, 2017, 26(12):1461-1467.
章新晶,熊淑华,邹霞. Caco-2细胞对酸枣仁皂苷A的跨膜转运[J]. 江西医药, 2011, 46(1):8-10.
Zhang X, Cheng X, Wu Y L, et al. In vitro and in situ characterization of the intestinal absorption of capilliposide B and capilliposide C from Lysimachia capillipes Hemsl[J]. Molecules, 2019, 24(7):1227.
龚琴,何鹿玲,王木兰,等.白头翁皂苷B4在HEK293细胞中的跨膜转运研究[J]. 中国现代中药, 2024,26(12):2132-2140.
刘亚丽,徐贞权,李泽协,等.有机阴离子转运多肽对白头翁五环三萜皂苷在大鼠肠道吸收的影响[J]. 医药导报, 2021, 40(5):606-611.
Shan Z Y, Yang X M, Liu H H, et al. Cryo-EM structures of human organic anion transporting polypeptide OATP1B1[J]. Cell Res, 2023, 33(12):940-951.
张伟,朱全刚. P-糖蛋白抑制剂tariquidar对黄芪甲苷在bEND.3细胞上跨膜转运的影响及机制[J]. 中国药学杂志, 2021, 56(3):204-209.
柏希慧,刘诗雨,王晶,等.穿山龙提取物中薯蓣皂苷的大鼠在体肠吸收[J]. 医药导报, 2017, 36(6):610-613.
张孟繁.人参皂苷Rg3磷脂复合物自微乳的大鼠口服药动学和Caco-2细胞转运研究[D]. 长春:吉林大学,2024.
王爱娟.薄荷醇在Caco-2细胞模型中的促吸收机制研究[D]. 广州:广东药科大学, 2017.
彦培傲,彭成,张岚,等.马丁达比犬肾上皮细胞模型研究广藿香醇跨膜转运机制[J]. 中国新药与临床杂志, 2017, 36(1):24-29.
Desrosiers M R, Weathers P J. Artemisinin permeability via Caco-2 cells increases after simulated digestion of Artemisia annua leaves[J]. J Ethnopharmacol, 2018, 210:254-259.
廖琼峰,姚媛,谢智勇,等.穿心莲内酯在Caco-2细胞单层模型中的吸收机制[J]. 中草药, 2011, 42(7):1363-1366.
华素,李园园,赵军利,等.穿心莲提取物中穿心莲内酯和脱水穿心莲内酯大鼠肠吸收特性研究[J]. 中草药, 2014, 45(21):3117-3123.
Zhang Y C, Li J, Lei X L, et al. Influence of verapamil on pharmacokinetics of triptolide in rats[J]. Eur J Drug Metab Pharmacokinet, 2016, 41(4):449-456.
Li X X, Li X, Michael A F, et al. Investigation of the attenuation effect of licorice on the toxicity of rhubarb using a P-gp lipid raft bioaffinity chromatography[J]. J Ethnopharmacol, 2025, 349:119929.
He Y F, Ci X Y, Xie Y, et al. Potential detoxification effect of active ingredients in liquorice by upregulating efflux transporter[J]. Phytomedicine, 2019, 56:175-182.
韩静文,李俊,黄成,等.栀子苷与栀子柏皮汤中栀子苷在MDCK细胞跨膜转运模型上的转运研究[J]. 中国药理学通报, 2014, 30(4):468-472.
张超,华悦,李喆,等.巴戟天中有效成分在Caco-2细胞模型中的吸收转运[J]. 中国现代中药, 2022, 24(5):837-844.
Wang B, Wang X F, Xiong Z W, et al. A review on the applications of traditional Chinese medicine polysaccharides in drug delivery systems[J]. Chin Med,2022, 17(1):12.
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.
Wubuli A, Chai J W, Liu H Q, et al. In vivo pharmacokinetics of Glycyrrhiza uralensis polysaccharides[J]. Front Pharmacol, 2024, 15:1431221.
Zhang B Y, Liu M M, Liu G, et al. Oral absorption mechanism of the polysaccharides from Gastrodia elata Blume base on fluorescence labeling[J]. Food Res Int,2021, 144:110342.
Zhang Y, Liu J X, Dou P F, et al. Oral absorption characteristics and mechanisms of a pectin-type polysaccharide from Smilax china L. across the intestinal epithelium[J]. Carbohydr Polym, 2021, 270:118383.
Zhang J H, He J X, Huang J M, et al. Pharmacokinetics,absorption and transport mechanism for ginseng polysaccharides[J]. Biomed Pharmacother, 2023, 162:114610.
胡杰,侯佳,李月婷,等.灯盏细辛提取物中3种活性成分在Caco-2细胞模型吸收机制的研究[J]. 中国药理学通报, 2016, 32(3):373-377.
程珍珍,周本宏,姜姗,等.没食子酸在Caco-2细胞模型中的吸收转运研究[J]. 中国药理学通报, 2020,36(8):1183-1184.
Chen R N, Shen C L, Xu Q Q, et al. The permeability characteristics and interaction of main components from Si-Ni-San in a MDCK epithelial cell monolayer model[J]. Xenobiotica, 2021, 51(2):239-248.
Zhao Q N, Yang J Y, Li J H, et al. Hypoglycemic effect and intestinal transport of phenolics-rich extract from digested mulberry leaves in Caco-2/insulin-resistant HepG2 coculture model[J]. Food Res Int, 2024, 175:113689.
Dong R H, Wang Y T, McClements D J, et al.Anthocyanin-sulfated polysaccharide-ovalbumin nano complex:Intestinal absorption mechanism and intracellular antioxidant activity in Caco-2 cells[J]. Food Chem, 2025, 492(Pt 2):145472.
Liu C Z, Ren L Y, Liu N, et al. Self-assembled mogroside V nanomicelle system improves oral bioavailability of the magnolol[J]. Food Chem, 2025, 487:144870.
Xia C J, Hu C H, Xu R, et al. An efficient brain delivery system co-loaded with multiple components of Salvia miltiorrhiza for synergistic treatment of ischemic stroke[J]. Mater Today Bio, 2025, 34:102102.
Zhou X J, Zhang P, Yang Y Y, et al. Highly potent and intestine specific P-glycoprotein inhibitor to enable oral delivery of taxol[J]. Angew Chem Int Ed, 2024, 63(45):e202412649.
Liang J Y, Tang X D, Wan S H, et al. Structure modification of ginsenoside Rh2 and cytostatic activity on cancer cells[J]. ACS Omega, 2023, 8(19):17245-17253.
Qin B W, Yao Y J, Zhang J, et al. Bioavailability of Coix seed polyphenols in a MKN28/Caco-2 continuous transport model and their lipid-lowering effects via modulating adipocyte differentiation of 3T3-L1 cells[J]. J Agric Food Chem, 2023, 71(22):8425-8436.
郑蓉,张淇淞,胡雪黎,等.多药耐药相关蛋白2对汉黄芩素及其主要II相代谢产物药动学特征的影响[J]. 中草药, 2022, 53(21):6779-6784.
沈龙宇,朱昕昀,胡宇,等.异功散中人参皂苷类成分在脾虚大鼠模型肠吸收动力学变化及其陈皮的影响[J]. 世界科学技术-中医药现代化, 2024, 26(5):1298-1307.
Li Y Y, Yang K, Zhao L X, et al. Effects of Schisandra lignans on the absorption of protopanaxadiol-type ginsenosides mediated by P-glycoprotein and protopanaxatriol-type ginsenosides mediated by CYP3A4[J]. J Ethnopharmacol, 2024, 318(Pt B):117057.
Conrad J, Paras N A, Vaz R J. Model of P-glycoprotein ligand binding and validation with efflux substrate matched pairs[J]. J Med Chem, 2024, 67(7):5854-5865.
杨秀伟,周琪乐,杨雁芳,等.红参水提物中人参三萜在人源肠Caco-2细胞单层模型上的吸收转运研究[J]. 中草药, 2021, 52(12):3630-3641.
宋伏洋,孙宇宏,黄壮壮,等.肠道菌群介导肝爽颗粒活性成分代谢促进协同增效研究[J]. 中成药, 2025,47(4):1375-1381.
Shen H, Gao X J, Li T, et al. Ginseng polysaccharides enhanced ginsenoside Rb1 and microbial metabolites exposure through enhancing intestinal absorption and affecting gut microbial metabolism[J]. J Ethnopharmacol,2018, 216:47-56.
Zhang A N, Gao S Q, Shen C H, et al. Bupleuri Radix polysaccharides enhance the efficacy and intestinal absorption of baicalin via regulating intestinal β-glucuronidase activity in MASH mice[J]. Phytomedicine,2025, 145:157092.
高飞,周菲,甘帅,等.四逆汤全方与拆方主要药效成分肠吸收动力学对比研究[J]. 中国中药杂志, 2022,47(18):5064-5070.
刘金凤,王晓玫,李佳园,等.酸枣仁-五味子配伍对抗焦虑作用的影响及指标成分的肠吸收特性研究[J]. 中草药, 2022, 53(16):5093-5106.
Liang X L, Ji M M, Chen L, et al. Traditional Chinese herbal medicine Astragalus Radix and its effects on intestinal absorption of aconite alkaloids in rats[J]. Chin Herb Med, 2020, 13(2):235-242.
Zhang Y, Zhang J X, Xiao L X, et al. The synergistic effect of Huangqi Gegen Decoction on thrombosis relates to the Astragalus polysaccharide-improved oral delivery of puerarin[J]. J Ethnopharmacol, 2024, 335:118622.
叶泰玮,陶春晓,李敏,等.红花与桃仁配伍对羟基红花黄色素A理化性质的影响[J]. 中成药, 2022, 44(12):3896-3901.

2026年第57卷第1期

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doi: 10.7501/j.issn.0253-2670.2026.01.033

接收时间：2025-08-12
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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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