Vitexin activates the Vitamin D Receptor to fight Colon Cancer

Created January 2025

Harnessing the Power of Vitexin as a Vitamin D Receptor Agonist in Colorectal Cancer: A New Frontier - behind paywall - Jan 2025

Balkan Med J. 2025 Jan 15. doi: 10.4274/balkanmedj.galenos.2024.2024-10-105

Manahil Mubeen 1, Hafsa Ali 2, Syeda Sabika Zehra 1, Aman Khan 1

What is Vitexin - Perplexity AI Jan 2025

Vitexin is an apigenin flavone glycoside, a natural compound found in various food and medicinal plants  1  3

. This important flavonoid can be found in several sources including:

  • Passion flower

  • Bamboo leaves

  • Pearl millet

  • Hawthorn berries

  • Mung beans

  • Buckwheat

  • Chaste tree (Vitex agnus-castus)

  • Fenugreek seeds

    Pharmacological Properties

    Antioxidant Effects

Vitexin acts as a powerful antioxidant by neutralizing reactive oxygen species (ROS) and reducing lipid peroxidation  1  2

. It enhances antioxidant enzyme activities and protects against oxidative stress-induced cellular damage  4

. Neuroprotective Effects

The compound demonstrates significant neuroprotective properties by reducing brain edema, neuronal cell death, and blood-brain barrier breakdown  1

. It improves neurogenesis and memory function while helping alleviate neurodegenerative disorders  2

. Anti-inflammatory Properties

Vitexin exhibits strong anti-inflammatory effects by inhibiting inflammatory cytokines and promoting anti-inflammatory molecules  2

. It helps reduce inflammation-associated pain and supports healthy inflammatory responses  1

. Cardiovascular Benefits

The compound provides cardioprotective effects by:

  • Decreasing myocardial infarct size

  • Reducing cardiac enzyme activities

  • Protecting vascular endothelial cells

  • Supporting healthy blood circulation  2 4

    Additional Benefits

  • Supports healthy blood sugar levels

  • Demonstrates anti-cancer properties

  • Shows antimicrobial effects

  • Helps maintain pancreatic health

  • Exhibits antiviral properties   2 4  5

Is it an activator of the Vitamin D Receptor (spoiler: Yes) - Perplexity AI Jan 2025

Recent research has revealed that vitexin is indeed a novel VDR (Vitamin D Receptor) agonist.

Here are the key findings about its interaction with VDR:

Mechanism of Action

Direct VDR Targeting

Vitexin specifically targets the VDR protein and facilitates its translocation into the cell nucleus

where it can exert transcriptional activity  2  4

. Transcriptional Regulation

The compound functions through the VDR/PBLD (phenazine biosynthesis-like domain protein) signaling pathway, regulating transcriptional activation  2

Therapeutic Effects

Anti-Cancer Properties

Vitexin's activation of VDR shows particular promise in treating colitis-associated colorectal cancer (CAC). It helps mitigate the progression from chronic colitis to colorectal cancer through:

  • Promoting macrophage polarization toward the M1 phenotype

  • Modulating the tumor microenvironment

  • Activating the VDR/PBLD pathway  2  4

    Validation Studies

The role of vitexin as a VDR agonist has been confirmed through multiple experimental approaches:

  • Co-culture models of macrophages and cancer cells

  • ChIP-seq analysis

  • Dual luciferase reporter assays

  • Mouse models with VDR gene knockout  2

These findings establish vitexin as a legitimate VDR agonist with therapeutic potential, particularly in inflammatory and cancer-related conditions.

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VitaminDWiki - Vitamin D Receptor activation can be increased in many ways

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VitaminDWiki - studies in both categories Colon Cancer and Vitamin D Receptor

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Please compare Vitexin with Butyrate in fighting colon cancer - Perplexity AI Jan 2025

Mechanism of Action

Vitexin

  • Induces apoptosis by suppressing autophagy in cancer cells  2

  • Inhibits COX-2 expression and NF-κB activity  8

  • Shows particular effectiveness against multi-drug resistant cancer cells  2

  • Works synergistically with aspirin to enhance anti-cancer effects  8

    Butyrate

  • Functions as an HDAC inhibitor in cancer cells due to the Warburg effect  14

  • Suppresses glucose metabolism in cancer cells  3

  • Reduces GLUT1 membrane content and glucose uptake  3

  • Enhances the effectiveness of chemotherapy drugs like 5-fluorouracil  1

    Effectiveness

Aspect Vitexin Butyrate
Dose Range 5-100 µM effective in vitro 2 2.5-20 mM effective in vitro 1
Cell Death Mechanism Induces apoptosis through caspase activation 2 Promotes apoptosis through HDAC inhibition 14
Drug Resistance Overcomes multi-drug resistance 2 Can develop resistance with prolonged exposure 5
Combination Therapy Works well with aspirin 8 Enhances effects of irinotecan and 5-fluorouracil 1

Unique Properties

Vitexin Advantages

  • Effectively kills drug-resistant cancer cells  2

  • Shows consistent dose-dependent effects  2

  • Demonstrates both in vitro and in vivo efficacy  2

    Butyrate Advantages

  • Serves as energy source for healthy colonocytes while killing cancer cells  14

  • Shows selective toxicity between normal and cancer cells  14

  • Improves intestinal barrier function while fighting cancer  17

Both compounds show promising anti-cancer properties but work through different mechanisms,

suggesting potential complementary use in cancer treatment.

Tags: Colon Cancer Vit D Receptor