| 引用本文: | 许文庆,张丽珍,孙梦超,葛浩冉,盛华刚,朱立俏.桔梗多糖不同组分对桔梗皂苷D在体肠吸收特性的影响及其微观结构表征[J].中国现代应用药学,2026,43(14):109-119. |
| xuwenqing,zhanglizhen,sunmengchao,gehaoran,shenghuagang,zhuliqiao.Study on the Effects of Different Fractions of Platycodon grandiflorum Polysaccharides on the In Vivo Intestinal Absorption Characteristics of Platycodin D and Their Microstructural Characterization[J].Chin J Mod Appl Pharm(中国现代应用药学),2026,43(14):109-119. |
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| 摘要: |
| 摘要 目的 明确桔梗多糖（Platycodon grandiflorum polysaccharides，PGPs）促进桔梗皂苷D（Platycodin D，PD）肠吸收的有效组分，并比较不同组分微观结构的差异。方法 采用大鼠在体单向肠灌流模型，以PD的表观吸收系数（Papp）、吸收速率常数（Ka）和单位面积每小时累计吸收量（Q）为指标，比较PGPs在十二指肠、空肠、回肠、结肠中对PD肠吸收的影响；采用DEAE纤维素柱色谱，以不同浓度NaCl溶液洗脱，将PGPs分为PGPs-1、PGPs-2和PGPs-3三个组分，采用高效液相凝胶渗透色谱（HPGPC）测定其分子量，比较三个多糖组分对PD在回肠中肠吸收的差异；采用P-糖蛋白（P-glycoprotein，P-gp）抑制剂考察P-gp对PGPs-2促进PD肠吸收的作用；通过激光粒度仪、扫描电镜（SEM）表征桔梗水提液灌流液、桔梗皂苷提取物（platycosides extract，PE）灌流液、PE+PGPs混合灌流液、PGPs-2灌流液、PE+PGPs-2灌流液的粒径和形貌等微观结构；采用原子力显微镜观察PGPs-2+PE灌流液的空间结构和形态。结果 PGPs在空肠、回肠可显著增加PD的Papp、Ka和Q（P<0.05，P<0.01），与桔梗水提液组相当。在结肠中PGPs也可促进PD吸收，但促进效果没有空肠、回肠显著。在十二指肠中则无明显促进作用（P＞0.05）。PGPs-1、PGPs-2和PGPs-3三个组分的分子量分别为3 638.72、15 826.11和22 475.36 Da；在三个多糖组分中，仅PGPs-2可显著提高PD在回肠中的Papp、Ka和Q （P<0.01），而PGPs-1和PGPs-3无显著作用（P>0.05）。PGPs-2促进PD肠吸收的作用与PGPs无显著性差异（P>0.05），但PGPs-2促进PD的吸收与P-gp无关。微观结构结果表明，PGPs-2能与PD自组装形成平均粒径约305.24 ± 0.57 nm、分散均匀（PDI=0.2723 ± 0.0108）的纳米粒，表明PGPs-2与PD形成的纳米体系更为稳定。结论 PGPs-2是促进PD肠吸收的有效组分，其机制可能与PGPs-2与PD可自组装形成稳定的纳米颗粒有关。本研究明确了PGPs中促进PD吸收的有效组分，从纳米微观结构阐释了PGPs-2促进PD吸收的潜在机制，为深入理解中药多成分间相互作用研究提供参考。 |
| 关键词: 桔梗多糖 桔梗皂苷D 肠吸收 在体单向肠灌流 微观结构 |
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| 基金项目:山东省自然科学基金面上项目(ZR2022MH173)；山东省中医药科技项目(M20241702)； |
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| Study on the Effects of Different Fractions of Platycodon grandiflorum Polysaccharides on the In Vivo Intestinal Absorption Characteristics of Platycodin D and Their Microstructural Characterization |
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xuwenqing, zhanglizhen, sunmengchao, gehaoran, shenghuagang, zhuliqiao
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Shandong University of Traditional Chinese Medicine
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| Abstract: |
| ABSTRACT: OBJECTIVE This study aims to identify the effective fraction of Platycodon grandiflorum polysaccharides (PGPs) that promotes the intestinal absorption of Platycodin D (PD).It also seeks to compare the microstructure differences among diffferent perfusates. METHODS An in vivo single-pass intestinal perfusion model in rats was employed.The apparent permeability coefficient (Papp), absorption rate constant (Ka), and cumulative absorption per unit area per hour (Q) of PD were used as indicators. These indicators helped compare the effects of PGPs on PD’s intestinal absorption in the duodenum, jejunum, ileum, and colon. PGPs were fractionated into three sub-fractions (PGPs-1, PGPs-2, and PGPs-3) via DEAE-cellulose column chromatography. Elution was carried out with NaCl solutions of different concentrations. High-performance liquid gel permeation chromatography (HPGPC) was used to determine the molecular weights of the three sub-fractions. Their effects on PD absorption in the ileum were further compared. P-glycoprotein (P-gp) inhibitors were utilized to investigate P-gp’s role in the promotion of PD intestinal absorption by PGPs-2. A laser particle size analyzer and scanning electron microscopy (SEM) were employed to characterize the microstructure (including particle size and morphology) of five perfusates.These perfusates included the Platycodon grandiflorum aqueous extract perfusate, platycosides extract (PE) perfusate, PE-PGPs mixed perfusate, PGPs-2 perfusate, and PE-PGPs-2 perfusate.The spatial structure and morphology of the PGPS-2+PE perfusate were observed using an atomic force microscope (AFM). RESULTS In the jejunum and ileum, PGPs significantly increased PD’s Papp, Ka, and Q (P<0.05, P<0.01). This effect was comparable to that observed in the Platycodon grandiflorum aqueous extract group. In the colon, PGPs also promoted PD absorption. However, the promoting effect was less significant than that in the jejunum and ileum. In the duodenum, PGPs exerted no obvious promoting effect on PD absorption (P>0.05).The molecular weights of PGPs-1, PGPs-2, and PGPs-3 were 3638.72 Da, 15826.11 Da, and 22475.36 Da, respectively. Among the three sub-fractions, PGPs-2 significantly increased PD’s Papp, Ka, and Q compared with the PD group (P<0.01). PGPs-1 and PGPs-3 had no significant effect (P>0.05). No significant difference was found in the promoting effect on PD intestinal absorption between PGPs-2 and the original PGPs (P>0.05). However, the promotion of PD absorption by PGPs-2 was independent of P-glycoprotein (P-gp). PGPs-2 can self-assemble with PD form nanoparticles. These nanoparticles had an average particle size of approximately 305.24±0.57 nm and uniform dispersion (polydispersity index, PDI = 0.2723±0.0108). This indicates that the nano-system formed by PGPs-2 and PD is more stable. CONCLUSION PGPs-2 is the effective fraction for promoting the intestinal absorption of PD. Its mechanism may be related to its ability to self-assemble with PD into stable nanoparticles. This study identified the effective fraction within PGPs that enhances PD absorption. It elucidated the potential mechanism of PGPs-2 in promoting PD absorption from the perspective of nano-microstructure. Additionally, it provides a reference for in-depth research on the interactions between multiple components in traditional Chinese medicines (TCMs). |
| Key words: Platycodon grandiflorum polysaccharides Platycodin D intestinal absorption in situ single-pass intestinal perfusion microstructure |
