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

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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.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.CC BY · PubMed Central

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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: Jia, Qi
Bai, Zhixun
Wu, Faming
Xie, Jian
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: gold
doi.org
Licence: cc-by
creativecommons.org/licenses/by/4.0/ (vor)
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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Advancements and challenges in pharmacokinetic and pharmacodynamic research on the traditional Chinese medicine saponins: a comprehensive review

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