Vitamin D3 / PKM2 Cancer Research Results

VitD3, Vitamin D3: Click to Expand ⟱
Features: Promote calcium and phosphorus absorption
Vitamin D3 (Cholecalciferol)
- Major VITAL study stated Vit D did not reduce invasive cancer, but Secondary Analysis stated reduces the incidence of metastatic cancer at diagnosis.
- Amount needed may depend on your BMI.
- Vitamin D deficiency, as determined by serum 25(OH)D concentrations of less than 30 ng/mL,
- Target achieving 80 ng/mL
- Vitamin D may modulate oxidative stress markers. (ROS)
- Nrf2 plays a key role in protecting cells against oxidative stress; this is modulated by vitamin D
- Vitamin D has antioxidant and anti-inflammatory regulatory effects; whether supplementation alters response to specific chemotherapy regimens remains context-dependent and not firmly established. - excess Vit D can raise calcium and cause harm
Vitamin D deficiency is generally defined as serum 25(OH)D <20 ng/mL (50 nmol/L), though some guidelines consider ≥30 ng/mL sufficient.
- One recommendation is to get your level up to around 125 ng/ml (however not supported by consensus clinical trial evidence).
- Chemo depletes Vitamin D levels so 10,000 IUs daily? – ask your doctor first. Typical maintenance dosing for most adults is 800–2000 IU/day; higher doses may be used short-term under medical supervision when correcting deficiency.

After correction of vitamin D deficiency through loading doses of oral vitamin D (or safe sun exposure), adequate maintenance doses of vitamin D3 are needed. This can be achieved in approximately 90% of the adult population with vitamin D supplementation between 1000 to 4000 IU/day, 10,000 IU twice a week, or 50,000 IU twice a month [10,125]. On a population basis, such doses would allow approximately 97% of people to maintain their serum 25(OH)D concentrations above 30 ng/mL [19,126]. Others, such as persons with obesity, those with gastrointestinal disorders, and during pregnancy and lactation, are likely to require doses of 6,000 IU/day.

Vitamin D, particularly its active form 1,25-dihydroxyvitamin D (calcitriol), exerts multiple biological effects that may influence cancer development and progression.
Calcitriol has been reported to induce cell cycle arrest (often at the G0/G1 phase) and promote pro-apoptotic mechanisms in various cancer cell types.

Inhibition of Angiogenesis:
Some studies indicate that vitamin D can reduce the expression of pro-angiogenic factors, thereby potentially limiting the blood supply to tumors, which is necessary for tumor growth and metastasis.

Effects on the Wnt/β-catenin Pathway:
The Wnt/β-catenin signaling pathway, often dysregulated in several cancers (for example, colorectal cancer), may be modulated by vitamin D.
Calcitriol has been shown in some models to inhibit β-catenin signaling, which is associated with decreased cell proliferation and tumor progression.
Vitamin D may interact with other signaling pathways, including the PI3K/AKT/mTOR pathway, which is involved in cell survival and proliferation.

Rank Pathway / Axis Cancer / Tumor Context Normal Tissue Context TSF Primary Effect Notes / Interpretation
1 VDR nuclear signaling (calcitriol → VDR/RXR → gene regulation) Differentiation ↑; proliferative drive ↓ (reported) Homeostatic gene regulation across many tissues R, G Transcriptional reprogramming Core biology is hormone-like gene regulation; many downstream “anti-cancer” effects are VDR-mediated and context-dependent.
2 Cell-cycle braking (p21/p27; Cyclin/CDK tone) Cell-cycle arrest ↑ (reported) ↔ / growth control support G Cytostasis Often described as downstream of VDR transcriptional programs; strength varies widely by tumor type and VDR expression.
3 Apoptosis / differentiation programs Apoptosis ↑ and/or differentiation ↑ (reported) G Phenotype shift Observed in many preclinical models; not a universal direct cytotoxin signature.
4 Immune modulation (innate/adaptive tone) Anti-inflammatory immune tone ↑ (context); microenvironment effects (reported) Immune regulation support R, G Immunomodulation Vitamin D signaling is active in both innate and adaptive immunity; effects depend on baseline status and context.
5 NF-κB / inflammatory transcription (downstream) Inflammatory programs ↓ (reported) Inflammation tone ↓ (context) R, G Anti-inflammatory signaling Commonly reported as a downstream correlate of VDR signaling and immune shifts; avoid presenting as a primary “direct inhibitor.”
6 Wnt/β-catenin & EMT/invasion programs (reported) EMT / invasion pressure ↓ (reported; model-dependent) G Anti-invasive phenotype Frequently discussed in colorectal and other models; keep “reported/model-dependent.”
7 Angiogenesis signaling (VEGF outputs; reported) Angiogenic outputs ↓ (reported) G Anti-angiogenic support Usually a later phenotype-level outcome tied to inflammatory and differentiation programs.
8 Systemic endocrine axis: calcium/phosphate homeostasis Hypercalcemia risk if excessive (therapy-limiting for analogs) Bone/mineral homeostasis (core physiologic role) R, G Endocrine regulation Key reason active vitamin D analogs in oncology are constrained: dose-limiting hypercalcemia.
9 Clinical oncology evidence (population-level) Incidence: generally no clear reduction; Mortality: some meta-analyses show modest reduction Translation constraint RCT meta-analyses often find reduced cancer mortality without clear reduction in total cancer incidence; results vary by trial design, baseline status, and dosing pattern.
10 Safety / monitoring constraints (hypercalcemia; interactions) Excess vitamin D can cause high calcium; risk increases with high-dose supplements and certain conditions/meds Clinical risk management Upper limits and avoiding unnecessary high-dose regimens matter; routine testing is not recommended for most healthy people without indications.

Time-Scale Flag (TSF): P / R / G

  • P: 0–30 min (rapid signaling is limited; most effects are not truly “instant”)
  • R: 30 min–3 hr (early transcription/signaling shifts begin)
  • G: >3 hr (gene-regulatory adaptation and phenotype outcomes)


Clinical trial data suggest vitamin D supplementation effects may be attenuated in individuals with obesity, potentially due to pharmacokinetic and inflammatory differences.
Domain Normal BMI (<25) Overweight (25–29.9) Obesity (≥30) Interpretation / Notes
Baseline 25(OH)D Levels Higher on average Moderately lower Significantly lower (volume dilution + sequestration) Vitamin D is fat-soluble; adipose tissue can sequester vitamin D, lowering circulating 25(OH)D.
Response to Supplementation Greater increase per IU Blunted increase Markedly blunted increase Obese individuals often require higher doses to achieve the same serum 25(OH)D level.
VDR Expression / Signaling Baseline signaling intact Possible mild attenuation Evidence of altered vitamin D signaling (context-dependent) Obesity-associated inflammation and metabolic dysregulation may influence VDR activity.
Systemic Inflammation Lower baseline inflammatory tone Elevated Chronically elevated Obesity increases IL-6, TNF-α, CRP; this may blunt anti-inflammatory effects of vitamin D.
Cancer Incidence (VITAL Trial) No overall reduction in invasive cancer No significant reduction No significant reduction Primary endpoint showed no reduction across BMI groups.
Advanced / Metastatic Cancer Signal (Secondary Analyses) Stronger reduction signal in normal BMI Weaker effect No clear benefit observed Secondary analyses suggested benefit mainly in non-obese participants; interpretation remains debated.
Mortality Signal (Meta-analyses) Modest reduction reported Less consistent Attenuated or absent Some pooled analyses show reduced cancer mortality, with stronger signals in non-obese individuals.
Dose Considerations 800–2000 IU/day often sufficient May require higher maintenance dose Higher supervised dosing sometimes required Guidelines emphasize individualized dosing based on measured 25(OH)D and clinical context.
Hypercalcemia Risk Low at standard doses Low–moderate (dose dependent) Still present at high doses Risk relates to absolute dose and duration, not BMI alone.


PKM2, Pyruvate Kinase, Muscle 2: Click to Expand ⟱
Source:
Type: enzyme
PKM2 (Pyruvate Kinase, Muscle 2) is an enzyme that plays a crucial role in glycolysis, the process by which cells convert glucose into energy. PKM2 is a key regulatory enzyme in the glycolytic pathway, and it is primarily expressed in various tissues, including muscle, brain, and cancer cells.
-C-myc is a common oncogene that enhances aerobic glycolysis in the cancer cells by transcriptionally activating GLUT1, HK2, PKM2 and LDH-A
-PKM2 has been shown to be overexpressed in many types of tumors, including breast, lung, and colon cancer. This overexpression may contribute to the development and progression of cancer by promoting glycolysis and energy production in cancer cells.
-inhibition of PKM2 may cause ATP depletion and inhibiting glycolysis.
-PK exists in four isoforms: PKM1, PKM2, PKR, and PKL
-PKM2 plays a role in the regulation of glucose metabolism in diabetes.
-PKM2 is involved in the regulation of cell proliferation, apoptosis, and autophagy.
– Pyruvate kinase catalyzes the final, rate-limiting step of glycolysis, converting phosphoenolpyruvate (PEP) to pyruvate with the production of ATP.
– The PKM2 isoform is uniquely regulated and can exist in both highly active tetrameric and less active dimeric forms.
– Cancer cells often favor the dimeric form of PKM2 to slow pyruvate production, thereby accumulating upstream glycolytic intermediates that can be diverted into anabolic pathways to support cell growth and proliferation.
– Under low oxygen conditions, cancer cells rely on altered metabolic pathways in which PKM2 is a key player. – The shift to aerobic glycolysis (Warburg effect) orchestrated in part by PKM2 helps tumor cells survive and grow in hypoxic conditions.

– Elevated expression of PKM2 is frequently observed in many cancer types, including lung, breast, colorectal, and pancreatic cancers.
– High levels of PKM2 are often correlated with enhanced tumor aggressiveness, poor differentiation, and advanced clinical stage.

PKM2 in carcinogenesis and oncotherapy

Inhibitors of PKM2:
-Shikonin, Resveratrol, Baicalein, EGCG, Apigenin, Curcumin, Ursolic Acid, Citrate (best known as an allosteric inhibitor of phosphofructokinase-1 (PFK-1), a key rate-limiting enzyme in glycolysis) potential to directly inhibit or modulate PKM2 is less well established

Full List of PKM2 inhibitors from Database
-key connected observations: Glycolysis↓, lactateProd↓, ROS↑ in cancer cell, while some result for opposite effect on normal cells.
Tumor pyruvate kinase M2 modulators

Flavonoids effect on PKM2
Compounds name IC50/AC50uM Effect
Flavonols
1. Fisetin 0.90uM Inhibition
2. Rutin 7.80uM Inhibition
3. Galangin 8.27uM Inhibition
4. Quercetin 9.24uM Inhibition
5. Kaempferol 9.88uM Inhibition
6. Morin hydrate 37.20uM Inhibition
7. Myricetin 0.51uM Activation
8. Quercetin 3-b- D-glucoside 1.34uM Activation
9. Quercetin 3-D -galactoside 27-107uM Ineffective
Flavanons
10. Neoeriocitrin 0.65uM Inhibition
11. Neohesperidin 14.20uM Inhibition
12. Naringin 16.60uM Inhibition
13. Hesperidin 17.30uM Inhibition
14. Hesperitin 29.10uM Inhibition
15. Naringenin 70.80uM Activation
Flavanonols
16. (-)-Catechin gallateuM 0.85 Inhibition
17. (±)-Taxifolin 1.16uM Inhibition
18. (-)-Epicatechin 1.33uM Inhibition
19. (+)-Gallocatechin 4-16uM Ineffective
Phenolic acids
20. Ferulic 11.4uM Inhibition
21. Syringic and 13.8uM Inhibition
22. Caffeic acid 36.3uM Inhibition
23. 3,4-Dihydroxybenzoic acid 78.7uM Inhibition
24. Gallic acid 332.6uM Inhibition
25. Shikimic acid 990uM Inhibition
26. p-Coumaric acid 22.2uM Activation
27. Sinapinic acids 26.2uM Activation
28. Vanillic 607.9uM Activation


Scientific Papers found: Click to Expand⟱
2369- VitD3,    Long Non-coding RNA MEG3 Activated by Vitamin D Suppresses Glycolysis in Colorectal Cancer via Promoting c-Myc Degradation
- in-vitro, CRC, DLD1 - in-vitro, CRC, RKO
MEG3↑, Glycolysis↓, lactateProd↓, LDHA↓, PKM2↓, HK2↓,
2365- VitD3,    Vitamin D Affects the Warburg Effect and Stemness Maintenance of Non- Small-Cell Lung Cancer Cells by Regulating the PI3K/AKT/mTOR Signaling Pathway
- in-vitro, Lung, A549 - in-vitro, Lung, H1975 - in-vivo, NA, NA
Glycolysis↓, Warburg↓, GLUT1↓, LDHA↓, HK2↓, PKM2↓, OCT4↓, SOX2↓, Nanog↓, PI3K↓, Akt↓, mTOR↓,

Showing Research Papers: 1 to 2 of 2

* indicates research on normal cells as opposed to diseased cells
Total Research Paper Matches: 2

Pathway results for Effect on Cancer / Diseased Cells:


Core Metabolism/Glycolysis

Glycolysis↓, 2,   HK2↓, 2,   lactateProd↓, 1,   LDHA↓, 2,   PKM2↓, 2,   Warburg↓, 1,  

Cell Death

Akt↓, 1,   MEG3↑, 1,  

Proliferation, Differentiation & Cell State

mTOR↓, 1,   Nanog↓, 1,   OCT4↓, 1,   PI3K↓, 1,   SOX2↓, 1,  

Barriers & Transport

GLUT1↓, 1,  
Total Targets: 14

Pathway results for Effect on Normal Cells:


Total Targets: 0

Scientific Paper Hit Count for: PKM2, Pyruvate Kinase, Muscle 2
Query results interpretion may depend on "conditions" listed in the research papers.
Such Conditions may include : 
  -low or high Dose
  -format for product, such as nano of lipid formations
  -different cell line effects
  -synergies with other products 
  -if effect was for normal or cancerous cells
Filter Conditions: Pro/AntiFlg:%  IllCat:%  CanType:%  Cells:%  prod#:167  Target#:772  State#:%  Dir#:1
wNotes=0 sortOrder:rid,rpid

 

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