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Cited by 52Ginseng Biological Effects and ApplicationsNatural product bioactivities and synthesisTraditional Chinese Medicine Analysis

The DOI matches its Crossref record; 130 of the 132 references it cites were found in a registry or an index.

Advancements and challenges in pharmacokinetic and pharmacodynamic research on the traditional Chinese medicine saponins: a comprehensive review

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Ma, Yuhan, Zhao, Yongxia, Luo, Mingxia, Jiang, Qin, Liu, Sha, Jia, Qi, Bai, Zhixun, Wu, Faming, Xie, Jian·2024·Frontiers in Pharmacology
DOI 10.3389/fphar.2024.1393409PMC PMC11106373
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Abstract

Recent research on traditional Chinese medicine (TCM) saponin pharmacokinetics has revealed transformative breakthroughs and challenges. The multicomponent nature of TCM makes it difficult to select representative indicators for pharmacokinetic studies. The clinical application of saponins is limited by their low bioavailability and short half-life, resulting in fluctuating plasma concentrations. Future directions should focus on novel saponin compounds utilizing colon-specific delivery and osmotic pump systems to enhance oral bioavailability. Optimizing drug combinations, such as ginsenosides with aspirin, shows therapeutic potential. Rigorous clinical validation is essential for practical applications. This review emphasizes a transformative era in saponin research, highlighting the need for clinical validation. TCM saponin pharmacokinetics, guided by traditional principles, are in development, utilizing multidisciplinary approaches for a comprehensive understanding. This research provides a theoretical basis for new clinical drugs and supports rational clinical medication.

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FIGURE 1 Pharmacological effects of saponins. (A) Anti-inflammatory effect: Saponins modulate immune cells to reduce inflammation by inhibiting the release of inflammatory mediators such as TNF-α and IL-1. (B) Antitumor effects: Saponins inhibit tumor cell proliferation and induce apoptosis through the activation of caspase-PARP pathways. (C) Antiviral effects: Saponins enhance immune response mediated by T-cells and B-cells, interfere with viral replication and propagation through the modulation of interferon p53 protein and PRb protein, and activate the immune system to augment antiviral efficacy. (D) Immunostimulation: Saponins boost the phagocytic activity of macrophages and promote the upregulation of cytokines and transcription factors associated with Th1 cells, including IFN-γ, TNF-α, and LPS. (E) Cholesterol reduction: Saponins regulate intracellular cholesterol levels through signaling pathways such as mTORC1 and AMPK. (F) Anti-Alzheimer’s: Saponins target the PPARA receptor, increasing acetylcholine concentrations in synaptic clefts to enhance neuronal signaling, influence the metabolism and aggregation of αβ-amyloid proteins, and reduce plaque formation, thereby slowing the progression of Alzheimer’s disease.
FIGURE 1 Pharmacological effects of saponins. (A) Anti-inflammatory effect: Saponins modulate immune cells to reduce inflammation by inhibiting the release of inflammatory mediators such as TNF-α and IL-1. (B) Antitumor effects: Saponins inhibit tumor cell proliferation and induce apoptosis through the activation of caspase-PARP pathways. (C) Antiviral effects: Saponins enhance immune response mediated by T-cells and B-cells, interfere with viral replication and propagation through the modulation of interferon p53 protein and PRb protein, and activate the immune system to augment antiviral efficacy. (D) Immunostimulation: Saponins boost the phagocytic activity of macrophages and promote the upregulation of cytokines and transcription factors associated with Th1 cells, including IFN-γ, TNF-α, and LPS. (E) Cholesterol reduction: Saponins regulate intracellular cholesterol levels through signaling pathways such as mTORC1 and AMPK. (F) Anti-Alzheimer’s: Saponins target the PPARA receptor, increasing acetylcholine concentrations in synaptic clefts to enhance neuronal signaling, influence the metabolism and aggregation of αβ-amyloid proteins, and reduce plaque formation, thereby slowing the progression of Alzheimer’s disease.CC BY · PubMed Central
FIGURE 2 Pharmacokinetics of Saponins. (A) Absorption: Saponins undergo acid hydrolysis in the stomach, with a fraction directly absorbed in the small intestine, while others are transformed by the intestinal microbiota for absorption. (B) Distribution: Saponins are distributed via the bloodstream to various tissues, predominantly accumulating in organs such as the liver, kidneys, intestines, and spleen. (C) Metabolism: Saponins undergo Phase I and Phase II metabolic reactions in the liver, some compounds enter the intestines where they are metabolized by intestinal microbiota into more absorbable forms. (D) Excretion: Saponins and their metabolic products are primarily excreted through urine and bile.
FIGURE 2 Pharmacokinetics of Saponins. (A) Absorption: Saponins undergo acid hydrolysis in the stomach, with a fraction directly absorbed in the small intestine, while others are transformed by the intestinal microbiota for absorption. (B) Distribution: Saponins are distributed via the bloodstream to various tissues, predominantly accumulating in organs such as the liver, kidneys, intestines, and spleen. (C) Metabolism: Saponins undergo Phase I and Phase II metabolic reactions in the liver, some compounds enter the intestines where they are metabolized by intestinal microbiota into more absorbable forms. (D) Excretion: Saponins and their metabolic products are primarily excreted through urine and bile.CC BY · PubMed Central

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Cites

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Research works printed but not linked: 5

  1. Chen, 2023, Research progress on the antitumor effect of traditional Chinese medicine saponins, Res. Zhuang Yao Ethn. Med., 50
  2. Jing, 2023, Research on extraction and separation technology of traditional Chinese medicine, Mod. Chem. Res., 175, 10.20087/j.cnki.1672-8114.2023.15.058 · DOI
  3. Wang, Application of physiological pharmacokinetic model in clinical rational drug use, Chin. J. Clin. Pharmacol., 39, 127, 10.13699/j.cnki.1001-6821.2023.01.027 · DOI
  4. Wang, 2022, Research progress on the pharmacological mechanism of traditional Chinese medicine saponins in the treatment of Parkinson's disease, Jiangsu J. Traditional Chin. Med., 54, 79, 10.19844/j.cnki.1672-397X.2022.12.025 · DOI
  5. Xu, 2023, Effect and mechanism of astragaloside saponins on different types of breast cancer cells, World Chin. Med., 18, 783, 10.3969/j.issn.1673-7202.2023.06.008 · DOI

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Metadata

Authors
Ma, Y., Zhao, Y., Luo, M., Jiang, Q., Liu, S., Jia, Q., Bai, Z., Wu, F., & Xie, J.
Affiliations
Zunyi Medical University (CN)
Corresponding author
  • Wu, Faming
  • Xie, Jian
ORCID
Venue
Frontiers in Pharmacology
Publisher
Frontiers Media SA
Published
2024-05-07
Volume
15
Pages
1393409-1393409
ISSN
1663-9812 (ISSN-L)
DOI
10.3389/fphar.2024.1393409
PMC
PMC11106373
OpenAlex
W4396700405
Cited by
44
References
132
Citations by year
2026: 22 · 2025: 19 · 2024: 3
FWCI
1.79
Type
journal article
Language
en
Open access
Licence
Locations
  • Frontiers in Pharmacology (publishedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion)
Funders
National Natural Science Foundation of China (82060687)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Ginseng Biological Effects and Applications
  • Physical Sciences › Chemistry › Organic Chemistry › Natural product bioactivities and synthesis
  • Health Sciences › Medicine › Complementary and alternative medicine › Traditional Chinese Medicine Analysis
Keywords
pharmacokinetics, pharmacodynamics, bioavailability, ginsenosides, colon-targeted drug delivery, osmotic pump, plasma concentration fluctuation, combination therapy, clinical validation

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CoChat. (2026). Citation check: Advancements and challenges in pharmacokinetic and pharmacodynamic research on the traditional Chinese medicine saponins: a comprehensive review. https://app.cochat.ai/papers/10.3389/fphar.2024.1393409
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Ma, Y., Zhao, Y., Luo, M., Jiang, Q., Liu, S., Jia, Q., Bai, Z., Wu, F., & Xie, J. (2024). Advancements and challenges in pharmacokinetic and pharmacodynamic research on the traditional Chinese medicine saponins: a comprehensive review. Frontiers in Pharmacology. https://doi.org/10.3389/fphar.2024.1393409

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