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Pharmacokinetics and tissue distribution of dual PPARα/γ agonist gigantol in mice

ABSTRACT: Gigantol is a bioactive compound in Dendrobium officinale with a wide range of pharmacological properties. This study developed an ultrahigh-performance liquid chromatography coupled with quadrupole-time-of-flight mass spectrometry (UHPLC-Q-TOF/MS) method for quantifying gigantol, which was subsequently applied to assess its pharmacokinetics and tissue distribution in Kunming mice. Additionally, the effects of gigantol on peroxisome proliferator-activated receptors (PPARs) were investigated. The UHPLC-Q-TOF/MS method was validated following the guidelines provided by the FDA and EMA for bioanalytical methods. Pharmacokinetic analysis revealed that gigantol exhibits a non-linear kinetic profile. Tissue distribution studies demonstrated high concentrations of gigantol in the liver and lungs. RNA sequencing (RNA-seq) indicated significant enrichment of PPAR signaling pathways in the KEGG database during gigantol-induced gene expression changes in the liver of Kunming mice. Molecular fingerprinting, docking studies and dual luciferase reporter assays confirmed that gigantol is a dual PPARα/γ agonist. These findings provide valuable insights for preclinical research on gigantol.

ORGANISM(S): Mus musculus

PROVIDER: GSE312718 | GEO | 2025/12/06

REPOSITORIES: GEO

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Project description:Background: Dendrobium officinale, an endangered Chinese herb, has extensive therapeutic effects and contains bioactive ingredients including a large number of polysaccharides and alkaloids, and minimal flavonoids. Firstly, this study attempts to obtain the protocorm-like bodies of this plant through tissue culture to produce the main secondary metabolites whose distribution in each organelle and protocorm like bodies is analyzed. Then, analysis of the correlation between comparative transcriptome sequence and the metabolite content in different organs enables the discovery of putative genes encoding enzymes involved in the biosynthesis of polysaccharides and alkaloids, and flavonoids. Results: The optimum condition for protocorm-like bodies (PLBs) induction and propagation of D. officinale is established. For protocorm induction, we use the seed as the explant, and the optimum medium formula for PLBs propagation is 1/2 MS + α-NAA 0.5 mg·L-1 +6-BA 1.0 mg·L-1 + 2, 4-D 1.5-2.0 mg·L-1 + potato juice 100 g·L-1. The distribution of polysaccharides, alkaloids and flavonoids in D. officinale organs was clarified. Stems, PLBs and leaves have the highest content of polysaccharides, alkaloids and flavonoids, respectively. PLBs replace organs to produce alkaloids in D. officinale, and naringenin was only produced in stem. Hot water extraction (HWE) method was found outperforming the ultrasound-assisted extraction (UAE) method for polysaccharides from D. officinale. A comparative transcriptome analysis of the protocorm-like bodies and leaves of D. officinale showed genes encoding enzymes involved in polysaccharides, alkaloids and flavonoids biosynthetic pathway were differentially expressed. Putative genes encoding enzymes involved in polysaccharides, alkaloids and flavonoids synthetic pathway were identified. Notably, genes encoding enzymes of strictosidine beta-glucosidase, geissoschizine synthase and vinorine synthase in alkaloids biosynthesis of D. officinale are first reported. Conclusions: Our works, especially the identification of candidate genes encoding enzymes involved in metabolites biosynthesis will help to explore and protect the endangered genetic resources and will also facilitate further analysis of the molecular mechanism of secondary metabolites’ biosynthesis in D. officinale.

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Pharmacokinetics and tissue distribution of dual PPARα/γ agonist gigantol in mice

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