LDH Cancer Research Results

LDH, Lactate Dehydrogenase: Click to Expand ⟱
Source:
Type:
LDH is a general term that refers to the enzyme that catalyzes the interconversion of lactate and pyruvate. LDH is a tetrameric enzyme, meaning it is composed of four subunits.
LDH refers to the enzyme as a whole, while LDHA specifically refers to the M subunit. Elevated LDHA levels are often associated with poor prognosis and aggressive tumor behavior, similar to elevated LDH levels.
leakage of LDH is a well-known indicator of cell membrane integrity and cell viability [35]. LDH leakage results from the breakdown of the plasma membrane and alterations in membrane permeability, and is widely used as a cytotoxicity endpoint.

However, it's worth noting that some studies have shown that LDHA is a more specific and sensitive biomarker for cancer than total LDH, as it is more closely associated with the Warburg effect and cancer metabolism.

Dysregulated LDH activity contributes significantly to cancer development, promoting the Warburg effect (Chen et al., 2007), which involves increased glucose uptake and lactate production, even in the presence of oxygen, to meet the energy demands of rapidly proliferating cancer cells (Warburg and Minami, 1923; Dai et al., 2016b). LDHA overexpression favors pyruvate to lactate conversion, leading to tumor microenvironment acidification and aiding cancer progression and metastasis.

Inhibitors:
Flavonoids, a group of polyphenols abundant in fruit, vegetables, and medicinal plants, function as LDH inhibitors.
LDH is used as a clinical biomarker for Synthetic liver function, nutrition

Tier A — Direct LDH Enzyme Inhibitors (Validated Catalytic Inhibition)

Rank Compound Type LDH Target Potency Level Primary Effect Notes
1 NCI-006 Research drug LDHA / LDHB High (in vivo active) Potent glycolysis suppression Modern benchmark LDH inhibitor used in metabolic oncology models.
2 (R)-GNE-140 Research drug LDHA (±LDHB) High (nM range reported) Lactate production ↓ Widely used experimental LDH inhibitor.
3 FX11 Research drug LDHA High (μM range) Metabolic crisis in LDHA-dependent tumors Classic LDHA inhibitor; often increases ROS secondary to metabolic stress.
4 Oxamate Tool compound LDH (pyruvate-competitive) Moderate (mM cellular use) Reduces lactate flux Classical LDH inhibitor; requires high concentrations in cells.
5 Gossypol Natural product derivative LDHA Moderate–High Glycolysis inhibition Also has other targets; safety considerations apply.
6 Galloflavin Natural compound LDH isoforms Moderate Lactate production ↓ One of the better-supported “natural-like” LDH inhibitors.

Tier B — Indirect LDH-Axis Modulators (Glycolysis / Lactate Reduction Without Confirmed Direct Catalytic Inhibition)

Rank Compound Mechanism Type LDH Claim Type Primary Axis Notes / Caution
1 Lonidamine MCT/MPC modulation Lactate axis inhibition Metabolic transport blockade Better classified as lactate/pyruvate transport modulator.
2 Stiripentol Repurposed drug LDH pathway modulation Metabolic axis modulation Emerging oncology interest; primarily neurological drug.
3 Quercetin Flavonoid Reported LDH inhibition (mixed evidence) NF-κB / PI3K modulation Often LDH-release confusion; direct enzymatic proof limited.
4 Ursolic acid Triterpenoid Reported LDH interaction Warburg modulation More credible as metabolic signaling modulator.
5 Fisetin Flavonoid Docking / indirect reports Apoptosis / survival signaling Enzyme inhibition not well validated.
6 Resveratrol Polyphenol Indirect glycolysis suppression AMPK / HIF-1α modulation Reduces lactate via upstream signaling.
7 Curcumin Polyphenol Indirect LDH expression modulation Inflammation + metabolic signaling Bioavailability limits translational strength.
8 Berberine Alkaloid Indirect metabolic modulation AMPK activation Closer to metformin-like metabolic pressure.
9 Honokiol Lignan Indirect glycolysis effects Survival pathway suppression Not validated as catalytic LDH inhibitor.
10 Silibinin Flavonolignan Mixed / indirect reports Inflammation + metabolic axis Often misclassified as LDH inhibitor.
11 Kaempferol Flavonoid Often LDH-release marker confusion Glucose transport / signaling Do not list as direct LDH inhibitor without enzyme data.
12 Oleanolic acid / Limonin / Allicin / Taurine Natural compounds Weak / indirect evidence General metabolic modulation Should not be categorized as true LDH inhibitors.

Tier A = Direct catalytic LDH inhibition (enzyme-level validation).
Tier B = Indirect lactate reduction or glycolytic modulation without strong catalytic inhibition evidence.
Important: LDH release assays (cell damage marker) are not proof of LDH enzymatic inhibition.



Scientific Papers found: Click to Expand⟱
4427- AgNPs,    Silver nanoparticles induce apoptosis and G2/M arrest via PKCζ-dependent signaling in A549 lung cells
- in-vitro, Lung, A549
tumCV↓, LDH↑, TumCCA↑, BAX↑, BID↑, Bcl-2↓, PKCδ↓,
2836- AgNPs,  Gluc,    Glucose capped silver nanoparticles induce cell cycle arrest in HeLa cells
- in-vitro, Cerv, HeLa
eff↝, TumCCA↑, eff↑, eff↑, ROS↑, GSH↓, SOD↓, lipid-P↑, LDH↑,
2775- Bos,    The journey of boswellic acids from synthesis to pharmacological activities
- Review, Var, NA - Review, AD, NA - Review, PSA, NA
ROS↑, ER Stress↑, TumCG↓, Apoptosis↑, Inflam↓, ChemoSen↑, Casp↑, ERK↓, cl‑PARP↑, AR↓, cycD1/CCND1↓, VEGFR2↓, CXCR4↓, radioP↑, NF-kB↓, VEGF↓, P21↑, Wnt↓, β-catenin/ZEB1↓, Cyt‑c↑, MMP2↓, MMP1↓, MMP9↓, PI3K↓, MAPK↓, JNK↑, *5LO↓, *NRF2↑, *HO-1↑, *MDA↓, *SOD↑, *hepatoP↑, *ALAT↓, *AST↓, *LDH↑, *CRP↓, *COX2↓, *GSH↑, *ROS↓, *Imm↑, *Dose↝, *eff↑, *neuroP↑, *cognitive↑, *IL6↓, *TNF-α↓,
5702- BRU,  BJ,    Brusatol inhibits metastasis of triple-negative breast cancer through metabolic reprogramming
- in-vitro, BC, NA
AntiTum↑, PPP↓, Glycolysis↓, TCA↓, NADPH↓, ROS↑, chemoP↑, e-LDH↑, TumMeta↓, Glycolysis↓,
5880- CAR,    In vitro and in vivo antitumor potential of carvacrol nanoemulsion against human lung adenocarcinoma A549 cells via mitochondrial mediated apoptosis
- vitro+vivo, Lung, A549 - in-vitro, Nor, BEAS-2B - in-vitro, Lung, PC9
Dose↝, mt-ROS↑, p‑JNK↑, BAX↑, Cyt‑c↑, Casp↑, AntiTum↑, ER Stress↑, LDH↑, selectivity↑, Apoptosis↑, DNAdam↑, IRE1↑, XBP-1↑, CHOP↓, p‑eIF2α↓, GRP78/BiP↓, Ca+2↑, MMP↓, Bcl-2↓, Casp3↑, Casp9↑, eff↓, TumW↓, Weight↑, eff↑, eff↑,
1579- Citrate,    Effect of Food Additive Citric Acid on The Growth of Human Esophageal Carcinoma Cell Line EC109
- in-vitro, ESCC, Eca109
TumCP↓, e-LDH↑, MMP↓, Ca+2?, PFK↓, Glycolysis↓,
1869- DCA,    Dichloroacetate induces autophagy in colorectal cancer cells and tumours
- in-vitro, CRC, HT-29 - in-vitro, CRC, HCT116 - in-vitro, Pca, PC3 - in-vitro, CRC, HT-29
LC3II↑, ROS↑, mTOR↓, MCT1↓, NADH:NAD↓, NAD↑, TumAuto↑, lactateProd↓, LDH↑,
2841- FIS,    Fisetin, an Anti-Inflammatory Agent, Overcomes Radioresistance by Activating the PERK-ATF4-CHOP Axis in Liver Cancer
- in-vitro, Nor, RAW264.7 - in-vitro, Liver, HepG2 - in-vitro, Liver, Hep3B - in-vitro, Liver, HUH7
*Inflam↓, *TNF-α↓, *IL1β↓, *IL6↓, Apoptosis↓, ER Stress↑, Ca+2↑, PERK↑, ATF4↑, CHOP↑, GRP78/BiP↑, tumCV↓, LDH↑, Casp3↑, cl‑Casp3↑, cl‑Casp8↑, cl‑Casp9↑, p‑eIF2α↑, RadioS↑,
2534- M-Blu,  doxoR,  PDT,    Methylene Blue-Mediated Photodynamic Therapy in Combination With Doxorubicin: A Novel Approach in the Treatment of HT-29 Colon Cancer Cells
- in-vitro, CRC, HT-29
LDH↑, ROS↑,
2430- PBG,    The cytotoxic effects of propolis on breast cancer cells involve PI3K/Akt and ERK1/2 pathways, mitochondrial membrane potential, and reactive oxygen species generation
- in-vitro, BC, MDA-MB-231
TumCP↓, TP53↓, Casp3↓, BAX↓, P21↓, ROS↑, eff↓, MMP↓, LDH↑, ATP↓, Ca+2↑,
3374- QC,    Therapeutic effects of quercetin in oral cancer therapy: a systematic review of preclinical evidence focused on oxidative damage, apoptosis and anti-metastasis
- Review, Oral, NA - Review, AD, NA
α-SMA↓, α-SMA↑, TumCP↓, tumCV↓, TumVol↓, TumCI↓, TumMeta↓, TumCMig↓, ROS↑, Apoptosis↑, BioAv↓, *neuroP↑, *antiOx↑, *Inflam↓, *Aβ↓, *cardioP↑, MMP↓, Cyt‑c↑, MMP2↓, MMP9↓, EMT↓, MMPs↓, Twist↓, Slug↓, Ca+2↑, AIF↑, Endon↑, P-gp↓, LDH↑, HK2↓, PKA↓, Glycolysis↓, GlucoseCon↓, lactateProd↓, GRP78/BiP↑, Casp12↑, CHOP↑,
3369- QC,    Pharmacological basis and new insights of quercetin action in respect to its anti-cancer effects
- Review, Pca, NA
FAK↓, TumCCA↑, p‑pRB↓, CDK2↑, CycB/CCNB1↓, CDK1↓, EMT↓, PI3K↓, MAPK↓, Wnt↓, ROS↑, miR-21↑, Akt↓, NF-kB↓, FasL↑, Bak↑, BAX↑, Bcl-2↓, Casp3↓, Casp9↑, P53↑, p38↑, MAPK↑, Cyt‑c↑, PARP↓, CHOP↑, ROS↓, LDH↑, GRP78/BiP↑, ERK↑, MDA↓, SOD↑, GSH↑, NRF2↑, VEGF↓, PDGF↓, EGF↓, FGF↓, TNF-α↓, TGF-β↓, VEGFR2↓, EGFR↓, FGFR1↓, mTOR↓, cMyc↓, MMPs↓, LC3B-II↑, Beclin-1↑, IL1β↓, CRP↓, IL10↓, COX2↓, IL6↓, TLR4↓, Shh↓, HER2/EBBR2↓, NOTCH↓, DR5↑, HSP70/HSPA5↓, CSCs↓, angioG↓, MMP2↓, MMP9↓, IGFBP3↑, uPA↓, uPAR↓, RAS↓, Raf↓, TSP-1↑,
4480- SeNPs,  Chit,    Biogenic synthesized selenium nanoparticles combined chitosan nanoparticles controlled lung cancer growth via ROS generation and mitochondrial damage pathway
- in-vitro, Lung, A549 - in-vitro, Nor, HK-2
selectivity↑, *toxicity↓, ROS↑, mtDam↑, Apoptosis↑, LDH↑,
2093- TQ,    Regulation of NF-κB Expression by Thymoquinone; A Role in Regulating Pro-Inflammatory Cytokines and Programmed Cell Death in Hepatic Cancer Cells
- in-vitro, Liver, HepG2 - in-vitro, Nor, NA
TumCD↑, selectivity↑, Casp3↑, DLC1↑, NF-kB↑, LDH↑, *toxicity↓,

Showing Research Papers: 1 to 14 of 14

* indicates research on normal cells as opposed to diseased cells
Total Research Paper Matches: 14

Pathway results for Effect on Cancer / Diseased Cells:


Redox & Oxidative Stress ⓘ

GSH↓, 1,   GSH↑, 1,   lipid-P↑, 1,   MDA↓, 1,   NRF2↑, 1,   ROS↓, 1,   ROS↑, 9,   mt-ROS↑, 1,   SOD↓, 1,   SOD↑, 1,  

Mitochondria & Bioenergetics ⓘ

AIF↑, 1,   ATP↓, 1,   EGF↓, 1,   FGFR1↓, 1,   MMP↓, 4,   mtDam↑, 1,   Raf↓, 1,  

Core Metabolism/Glycolysis ⓘ

cMyc↓, 1,   GlucoseCon↓, 1,   Glycolysis↓, 4,   HK2↓, 1,   lactateProd↓, 2,   LDH↑, 11,   e-LDH↑, 2,   NAD↑, 1,   NADH:NAD↓, 1,   NADPH↓, 1,   PFK↓, 1,   PPP↓, 1,   TCA↓, 1,  

Cell Death ⓘ

Akt↓, 1,   Apoptosis↓, 1,   Apoptosis↑, 4,   Bak↑, 1,   BAX↓, 1,   BAX↑, 3,   Bcl-2↓, 3,   BID↑, 1,   Casp↑, 2,   Casp12↑, 1,   Casp3↓, 2,   Casp3↑, 3,   cl‑Casp3↑, 1,   cl‑Casp8↑, 1,   Casp9↑, 2,   cl‑Casp9↑, 1,   Cyt‑c↑, 4,   DR5↑, 1,   Endon↑, 1,   FasL↑, 1,   JNK↑, 1,   p‑JNK↑, 1,   MAPK↓, 2,   MAPK↑, 1,   MCT1↓, 1,   p38↑, 1,   TumCD↑, 1,  

Kinase & Signal Transduction ⓘ

HER2/EBBR2↓, 1,  

Transcription & Epigenetics ⓘ

miR-21↑, 1,   p‑pRB↓, 1,   tumCV↓, 3,  

Protein Folding & ER Stress ⓘ

CHOP↓, 1,   CHOP↑, 3,   p‑eIF2α↓, 1,   p‑eIF2α↑, 1,   ER Stress↑, 3,   GRP78/BiP↓, 1,   GRP78/BiP↑, 3,   HSP70/HSPA5↓, 1,   IRE1↑, 1,   PERK↑, 1,   XBP-1↑, 1,  

Autophagy & Lysosomes ⓘ

Beclin-1↑, 1,   LC3B-II↑, 1,   LC3II↑, 1,   TumAuto↑, 1,  

DNA Damage & Repair ⓘ

DNAdam↑, 1,   P53↑, 1,   PARP↓, 1,   cl‑PARP↑, 1,   TP53↓, 1,  

Cell Cycle & Senescence ⓘ

CDK1↓, 1,   CDK2↑, 1,   CycB/CCNB1↓, 1,   cycD1/CCND1↓, 1,   P21↓, 1,   P21↑, 1,   TumCCA↑, 3,  

Proliferation, Differentiation & Cell State ⓘ

CSCs↓, 1,   EMT↓, 2,   ERK↓, 1,   ERK↑, 1,   FGF↓, 1,   IGFBP3↑, 1,   mTOR↓, 2,   NOTCH↓, 1,   PI3K↓, 2,   RAS↓, 1,   Shh↓, 1,   TumCG↓, 1,   Wnt↓, 2,  

Migration ⓘ

Ca+2?, 1,   Ca+2↑, 4,   DLC1↑, 1,   FAK↓, 1,   MMP1↓, 1,   MMP2↓, 3,   MMP9↓, 3,   MMPs↓, 2,   PDGF↓, 1,   PKA↓, 1,   PKCδ↓, 1,   Slug↓, 1,   TGF-β↓, 1,   TSP-1↑, 1,   TumCI↓, 1,   TumCMig↓, 1,   TumCP↓, 3,   TumMeta↓, 2,   Twist↓, 1,   uPA↓, 1,   uPAR↓, 1,   α-SMA↓, 1,   α-SMA↑, 1,   β-catenin/ZEB1↓, 1,  

Angiogenesis & Vasculature ⓘ

angioG↓, 1,   ATF4↑, 1,   EGFR↓, 1,   VEGF↓, 2,   VEGFR2↓, 2,  

Barriers & Transport ⓘ

P-gp↓, 1,  

Immune & Inflammatory Signaling ⓘ

COX2↓, 1,   CRP↓, 1,   CXCR4↓, 1,   IL10↓, 1,   IL1β↓, 1,   IL6↓, 1,   Inflam↓, 1,   NF-kB↓, 2,   NF-kB↑, 1,   TLR4↓, 1,   TNF-α↓, 1,  

Hormonal & Nuclear Receptors ⓘ

AR↓, 1,  

Drug Metabolism & Resistance ⓘ

BioAv↓, 1,   ChemoSen↑, 1,   Dose↝, 1,   eff↓, 2,   eff↑, 4,   eff↝, 1,   RadioS↑, 1,   selectivity↑, 3,  

Clinical Biomarkers ⓘ

AR↓, 1,   CRP↓, 1,   EGFR↓, 1,   HER2/EBBR2↓, 1,   IL6↓, 1,   LDH↑, 11,   e-LDH↑, 2,   TP53↓, 1,  

Functional Outcomes ⓘ

AntiTum↑, 2,   chemoP↑, 1,   radioP↑, 1,   TumVol↓, 1,   TumW↓, 1,   Weight↑, 1,  
Total Targets: 165

Pathway results for Effect on Normal Cells:


Redox & Oxidative Stress ⓘ

antiOx↑, 1,   GSH↑, 1,   HO-1↑, 1,   MDA↓, 1,   NRF2↑, 1,   ROS↓, 1,   SOD↑, 1,  

Core Metabolism/Glycolysis ⓘ

ALAT↓, 1,   LDH↑, 1,  

Migration ⓘ

5LO↓, 1,  

Immune & Inflammatory Signaling ⓘ

COX2↓, 1,   CRP↓, 1,   IL1β↓, 1,   IL6↓, 2,   Imm↑, 1,   Inflam↓, 2,   TNF-α↓, 2,  

Protein Aggregation ⓘ

Aβ↓, 1,  

Drug Metabolism & Resistance ⓘ

Dose↝, 1,   eff↑, 1,  

Clinical Biomarkers ⓘ

ALAT↓, 1,   AST↓, 1,   CRP↓, 1,   IL6↓, 2,   LDH↑, 1,  

Functional Outcomes ⓘ

cardioP↑, 1,   cognitive↑, 1,   hepatoP↑, 1,   neuroP↑, 2,   toxicity↓, 2,  
Total Targets: 30

Scientific Paper Hit Count for: LDH, Lactate Dehydrogenase
2 Silver-NanoParticles
2 Quercetin
1 Glucose
1 Boswellia (frankincense)
1 brusatol
1 Brucea javanica
1 Carvacrol
1 Citric Acid
1 Dichloroacetate
1 Fisetin
1 Methylene blue
1 doxorubicin
1 Photodynamic Therapy
1 Propolis -bee glue
1 Selenium NanoParticles
1 chitosan
1 Thymoquinone
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#:%  Target#:906  State#:%  Dir#:2
  wNotes=0  sortOrder:rid,rpid

 

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