ArticlePharmacology research & perspectives2015
Maackiain is a novel antiallergic compound that suppresses transcriptional upregulation of the histamine H1 receptor and interleukin-4 genes.
Article in Pharmacology research & perspectives, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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14 citing papers in PubMed, 40 citations in OpenAlex.
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- Bioassay-guided isolation of two antiproliferative metabolites fromFrontiers in pharmacology · 2024Article
- Bioprospecting microbes and enzymes for the production of pterocarpans and coumestans.Frontiers in bioengineering and biotechnology · 2023Review
- A Novel Splice Variant ofCancers · 2022Article
- Maackiain Modulates miR-374a/GADD45A Axis to Inhibit Triple-Negative Breast Cancer Initiation and Progression.Frontiers in pharmacology · 2022Article
- Molecular Signaling and Transcriptional Regulation of Histamine HCurrent topics in behavioral neurosciences · 2022Review
- Patho-Pharmacological Research of Anti-allergic Natural Products Targeting Antihistamine-Sensitive and -Insensitive Allergic Mechanisms.Current topics in behavioral neurosciences · 2022Review
- Signaling Pathway of Histamine HCurrent issues in molecular biology · 2021Article
- Phytochemical studies on traditional herbal medicines based on the ethnopharmacological information obtained by field studies.Journal of natural medicines · 2021Review
- Maackiain Protects the Kidneys of Type 2 Diabetic Rats via Modulating the Nrf2/HO-1 and TLR4/NF-κB/Caspase-3 Pathways.Drug design, development and therapy · 2021Article
- Elucidation of Inverse Agonist Activity of Bilastine.Pharmaceutics · 2020Article
- Synthesis of anti-allergic drugs.RSC advances · 2020Review
- Cytisine-Pterocarpan-Derived Compounds: Biomimetic Synthesis and Apoptosis-Inducing Activity in Human Breast Cancer Cells.Molecules (Basel, Switzerland) · 2018Article
- Disruption of Heat Shock Protein 90 (Hsp90)-Protein Kinase Cδ (PKCδ) Interaction by (-)-Maackiain Suppresses Histamine H1 Receptor Gene Transcription in HeLa Cells.The Journal of biological chemistry · 2015Article
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12 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Kujin contains antiallergic compounds that inhibit upregulation of histamine H1 receptor (H1R) and interleukin (IL)-4 gene expression. However, the underlying mechanism remains unknown. We sought to identify a Kujin-derived antiallergic compound and investigate its mechanism of action. The H1R and IL-4 mRNA levels were determined by real-time quantitative RT-PCR. To investigate the effects of maackiain in vivo, toluene-2,4-diisocyanate (TDI)-sensitized rats were used as a nasal hypersensitivity animal model. We identified (-)-maackiain as the responsible component. Synthetic maackiain showed stereoselectivity for the suppression of IL-4 gene expression but not for H1R gene expression, suggesting distinct target proteins for transcriptional signaling. (-)-Maackiain inhibited of PKCδ translocation to the Golgi and phosphorylation of Tyr(311) on PKCδ, which led to the suppression of H1R gene transcription. However, (-)-maackiain did not show any antioxidant activity or inhibition of PKCδ enzymatic activity per se. Pretreatment with maackiain alleviated nasal symptoms and suppressed TDI-induced upregulations of H1R and IL-4 gene expressions in TDI-sensitized rats. These data suggest that (-)-maackiain is a novel antiallergic compound that alleviates nasal symptoms in TDI-sensitized allergy model rats through the inhibition of H1R and IL-4 gene expression. The molecular mechanism underlying its suppressive effect for H1R gene expression is mediated by the inhibition of PKCδ activation.
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