Isobavachalcone / AntiBio Cancer Research Results

IBC, Isobavachalcone: Click to Expand ⟱
Features:

Isobavachalcone - Prenylated Chalcone

Type: Natural prenylated chalcone / flavonoid-related phytochemical
-Chalcone → chemical class / parent scaffold, not a molecular target. -Example Chalones: Isobavachalcone, xanthohumol, licochalcone A, isoliquiritigenin

Sources: Found in several medicinal plants, particularly Psoralea corylifolia (Cullen corylifolium), as well as other plant species containing prenylated chalcones.

Function: Isobavachalcone is a bioactive prenylated chalcone with anticancer, anti-inflammatory, antioxidant, antimicrobial, and neuroprotective activities. Reported molecular effects include modulation of AKT, ERK/MAPK, ROS, apoptosis, inflammatory signaling, and cellular stress pathways.

Cancer: Experimental studies demonstrate inhibition of cancer-cell proliferation, migration, and invasion and induction of apoptosis and other forms of regulated cell death. IBC can suppress AKT and ERK signaling, increase tumor-cell oxidative stress, and modulate antitumor immune responses. Anticancer activity has been demonstrated in pancreatic, breast, oral, colorectal, thyroid, and other experimental cancer models.

Alzheimer's Disease: Preclinical studies indicate neuroprotective activity, including reduction of Aβ accumulation and plaque pathology, suppression of neuroinflammation, and improvement of memory and cognitive deficits in Alzheimer's disease models.

Isobavachalcone — Isobavachalcone (IBC; CAS 20784-50-3) is a naturally occurring prenylated chalcone and flavonoid-related phytochemical found particularly in Psoralea corylifolia L. (syn. Cullen corylifolium; Psoraleae Fructus/Bu Gu Zhi). It is an experimental small-molecule natural product with anticancer, anti-inflammatory, antimicrobial, and neuroprotective activities. Current anticancer evidence is preclinical and increasingly supports direct or proximal effects on SIRT2, DHODH, thioredoxin reductase 1, AKT signaling, mitochondrial function, and redox homeostasis. IBC has not been established as an approved anticancer or Alzheimer therapy.

Primary mechanisms (ranked):

  1. Mitochondrial and redox disruption with ↑ ROS, mitochondrial membrane depolarization, impaired respiration/ATP production, mitochondrial Ca²⁺ overload, and activation of mitochondrial permeability-transition-associated cell death.
  2. ↓ AKT signaling, including direct inhibition of AKT1 activity in early studies and suppression of AKT phosphorylation, reducing survival signaling and promoting mitochondrial apoptosis.
  3. Direct ↓ SIRT2 activity, disrupting SIRT2/α-tubulin signaling and downstream STAT3/c-Myc and Snail/MMP pathways in triple-negative breast cancer.
  4. ↓ DHODH with mitochondrial dysfunction, mtDNA release, ↑ ROS, and activation of cGAS-STING-associated antitumor immunity in gastric cancer models.
  5. ↓ thioredoxin reductase 1, weakening cellular thioredoxin antioxidant capacity and promoting ROS-dependent ER stress and apoptosis in prostate cancer.
  6. Induction of multiple regulated cell-death programs including mitochondrial apoptosis, non-canonical mitochondrial permeability-transition-driven necrosis, pyroptosis, necroptosis, and autophagy, depending on tumor model.
  7. Suppression of invasion and metastatic signaling through pathways including ↓ β-catenin, ↓ MMP-2/MMP-9, ↓ Snail, and other context-dependent AKT/GSK-3β/β-catenin and SIRT2-associated mechanisms.
  8. Antitumor immune modulation, including ↑ CD8+ T-cell infiltration, ↓ M2 macrophage polarization, and STING-associated innate immune activation in animal tumor models.
  9. ABCB1 modulation and membrane perturbation, potentially increasing drug accumulation in some multidrug-resistant cancer cells.
  10. Secondary NRF2/HO-1 activation has been reported primarily in anti-inflammatory/non-cancer contexts and should not be interpreted as the principal anticancer mechanism.

Bioavailability / PK relevance: Human pharmacokinetics have not been established. Rat oral pharmacokinetic studies demonstrate measurable systemic exposure after high oral dosing, but IBC undergoes extensive glucuronidation involving UGT1A1, UGT1A3 and additional UGT isoforms, with BCRP/MRP-mediated glucuronide efflux. These metabolic characteristics may limit free systemic exposure. IBC also inhibits multiple CYP and UGT enzymes in vitro at low-micromolar concentrations, creating a potential drug-interaction concern if therapeutically relevant human exposure can be achieved.

In-vitro vs systemic exposure relevance: Many anticancer experiments use approximately low- to several-tens-of-micromolar IBC concentrations; for example, MCF-7 growth inhibition has been reported at IC50 values around 28–38 µM, whereas direct SIRT2 inhibition occurs at substantially lower concentrations with an enzymatic IC50 of approximately 0.84 µM. Human plasma concentrations after oral dosing are unknown, so it cannot currently be assumed that the concentrations required for many cell-culture anticancer effects are clinically achievable. High-concentration mitochondrial ROS effects are particularly relevant to the hepatotoxicity signal and may narrow any therapeutic window.

Clinical evidence status: Preclinical. Anticancer activity has been demonstrated in numerous cancer cell systems and several mouse xenograft/allograft models, including breast, gastric, pancreatic, colorectal, prostate, AML, thyroid, and other cancers. No established human anticancer efficacy, therapeutic dose, validated exposure-response relationship, or regulatory approval has been demonstrated.

Safety: Hepatotoxicity is a significant translational constraint. IBC itself has produced mitochondrial dysfunction, ROS accumulation, loss of mitochondrial membrane potential, ATP depletion, apoptosis, and ferroptosis-associated injury in hepatic experimental systems. Psoralea corylifolia preparations are independently associated with clinically reported liver injury, although toxicity of the whole herb cannot be attributed exclusively to IBC. Potential CYP/UGT inhibition further raises concern for pharmacokinetic drug interactions.

Isobavachalcone Cancer-Relevant Mechanisms

Rank Pathway / Axis Cancer Cells Normal Cells Primary Effect Notes / Interpretation
1 Mitochondrial ROS and bioenergetic disruption ↑ ROS; ↓ mitochondrial membrane potential; ↓ respiration; ↓ ATP Similar mitochondrial toxicity can occur in hepatocytes Metabolic collapse and cell death Central recurring mechanism across multiple cancer models, but lack of strict tumor selectivity is an important safety limitation.
2 AKT survival signaling ↓ AKT activity; ↓ p-AKT ↓ p-AKT reported during hepatic toxicity ↓ survival signaling; ↑ apoptosis IBC has been reported to inhibit AKT1 kinase and repeatedly suppress cellular AKT phosphorylation.
3 Mitochondrial permeability transition and Ca²⁺ ↑ mitochondrial Ca²⁺; ↑ pore opening; ↓ membrane potential Not well characterized ↑ regulated necrosis ROS-dependent non-canonical mitochondrial permeability-transition-driven necrosis demonstrated in breast and lung cancer models.
4 SIRT2 signaling ↓ SIRT2; ↑ α-tubulin acetylation; ↓ STAT3/c-Myc; ↓ Snail/MMP signaling Limited comparative data ↓ proliferation and migration; ↑ apoptosis Direct SIRT2 inhibition reported with an enzymatic IC50 of approximately 0.84 µM in TNBC studies.
5 DHODH mitochondrial pyrimidine metabolism ↓ DHODH; ↑ ROS; ↑ mitochondrial damage; ↑ mtDNA release Limited comparative data Metabolic stress and antitumor immune activation Recent gastric-cancer evidence identifies DHODH as a functional target linking mitochondrial injury with STING signaling.
6 cGAS-STING innate immune signaling ↑ STING-associated signaling Context-dependent ↑ antitumor immune response Associated with mitochondrial damage and mtDNA release in gastric-cancer models.
7 Thioredoxin reductase 1 redox defense ↓ TrxR1; ↑ ROS; ↑ ER stress Potential oxidative toxicity ↑ apoptosis TrxR1 has been proposed as a direct redox-sensitive IBC target in prostate cancer cells.
8 Mitochondrial apoptosis ↑ Bax; ↓ Bcl-2/Bcl-xL/Mcl-1; ↑ cytochrome c; ↑ caspase-9/3; ↑ PARP cleavage Can also occur in hepatic cells ↑ apoptosis Highly reproducible downstream phenotype in several tumor types.
9 Pyroptosis ↑ caspase-dependent GSDME cleavage Insufficient comparative data ↑ inflammatory cell death Demonstrated particularly in anaplastic thyroid cancer models.
10 Necroptosis and autophagy ↑ RIP3/MLKL signaling; ↑ LC3-II/I (model-dependent) Context-dependent Multiple regulated cell-death responses Observed in selected breast-cancer models; not a universal IBC response.
11 AKT GSK-3β β-catenin signaling ↓ pathway activity Not well characterized ↓ proliferation and survival Reported prominently in colorectal cancer cells.
12 Migration and extracellular matrix remodeling ↓ MMP-2; ↓ MMP-9; ↓ Snail; ↓ migration/invasion Limited data ↓ invasive phenotype Supported in oral, breast, colorectal, and related cancer models.
13 Tumor immune microenvironment ↑ CD8+ T cells; ↓ M2 macrophages Immune modulation is context-dependent ↑ antitumor immunity Demonstrated in orthotopic pancreatic tumor models.
14 ABCB1 multidrug resistance ↓ ABCB1 transport function (context-dependent) May alter xenobiotic transport Potential chemosensitization IBC behaves as a membrane-active ABCB1 substrate and/or competitive inhibitor; clinical chemosensitization has not been established.
15 NRF2 HO-1 antioxidant signaling Context-dependent ↑ NRF2/HO-1 reported mainly in inflammatory models Anti-inflammatory and cytoprotective effects Secondary mechanism and potentially opposite to the desired pro-oxidant anticancer state.
16 Clinical Translation Constraint Effective concentrations frequently in low-to-tens-of-µM range Hepatic mitochondrial and ferroptotic toxicity documented experimentally Limits therapeutic translation Human PK, therapeutic exposure, tumor selectivity, maximum tolerated dose, and clinical efficacy remain undefined; extensive glucuronidation and CYP/UGT interactions are additional constraints.

Alzheimer's disease relevance: Isobavachalcone has meaningful but exclusively preclinical evidence in Alzheimer's disease. In transgenic AD mouse models, IBC has improved memory-related outcomes and reduced Aβ pathology, tau hyperphosphorylation, and neuroinflammation. More recent work links these effects to ↑ autophagic Aβ clearance and ↓ NLRP3 inflammasome activation in astrocytes. Earlier studies also identified inhibitory activity against several AD-associated targets, including Aβ42-related processes, BACE1, GSK-3β, and acetylcholinesterase. No human efficacy, dose, pharmacokinetic target, or clinical safety data support its use for AD.

Isobavachalcone Alzheimer-Relevant Mechanisms

Rank Pathway / Axis Modulation Primary Effect Notes / Interpretation
1 Amyloid beta clearance ↓ Aβ accumulation and plaque burden Reduced amyloid pathology Supported in transgenic mouse models.
2 Autophagy ↑ autophagic clearance ↑ Aβ removal Mechanistically supported in primary astrocytes and 5xFAD mice.
3 NLRP3 inflammasome ↓ NLRP3 activation ↓ neuroinflammation Astrocyte-associated anti-inflammatory mechanism demonstrated in recent preclinical work.
4 Tau pathology ↓ tau hyperphosphorylation and filament formation Reduced tau pathology Reported in 3×Tg-AD mice.
5 GSK-3β ↓ activity Potential reduction of tau phosphorylation Supported mainly by earlier multi-target biochemical studies.
6 BACE1 and amyloidogenic processing ↓ activity Potential ↓ Aβ generation Preclinical biochemical evidence; in-vivo contribution is less certain.
7 Acetylcholinesterase ↓ activity Potential cholinergic support Biochemical activity; clinical relevance has not been established.
8 Clinical Translation Constraint Human exposure and CNS penetration not established Uncertain therapeutic feasibility Potential hepatotoxicity, metabolism, drug interactions, and lack of human PK/efficacy are major constraints.


AntiBio, Antibiotic/Antimicrobial activity: Click to Expand ⟱
Source:
Type:

Antibiotic / antimicrobial activity: The ability of a substance to suppress or kill microorganisms, especially bacteria, by disrupting microbial survival, growth, biofilm formation, cell-wall integrity, membrane function, protein synthesis, nucleic-acid synthesis, quorum sensing, or virulence.

Natural Products that might have antimicrobial properties

Natural supplement or product Principal constituents Potential antimicrobial activity Evidence assessment Reference
Garlic
Allium sativum		 Allicin, ajoene and diallyl sulfides Antibacterial and antifungal activity, with some antiviral and antiparasitic effects reported in laboratory studies. Extensive laboratory evidence, but insufficient clinical evidence to use garlic as a treatment for established infections. Tesfaye A. Revealing the therapeutic uses of garlic and its potential for drug discovery. Scientific review.
Berberine Berberine isoquinoline alkaloid May damage bacterial membranes, inhibit efflux pumps, interfere with nucleic-acid and protein synthesis, and inhibit biofilm formation. Strong preclinical evidence and limited indication-specific clinical evidence. Poor oral bioavailability and drug interactions limit its use as a general antimicrobial. Berberine as a therapeutic alkaloid against ESKAPE and multidrug-resistant bacteria: a comprehensive review.
Cranberry extract
Vaccinium macrocarpon		 A-type proanthocyanidins Primarily reduces adhesion of uropathogenic bacteria, particularly Escherichia coli, to urinary epithelial cells. May reduce recurrent urinary tract infections in selected populations. It is preventive rather than a reliable treatment for an active UTI. National Center for Complementary and Integrative Health: Cranberry—Usefulness and Safety.
Probiotics
Lactobacillus, Bifidobacterium and Saccharomyces boulardii 		Live microorganisms; effects are strain-specific Competitive exclusion of pathogens, production of bacteriocins, inhibition of pathogen adhesion and restoration of microbiome function. Some human evidence for antibiotic-associated diarrhea and selected gastrointestinal or vaginal indications. Results cannot be generalized from one strain to another. NIH Office of Dietary Supplements: Probiotics—Health Professional Fact Sheet.
Medical-grade honey / Manuka honey Methylglyoxal, hydrogen peroxide, defensin-1, organic acids and high osmolarity Broad topical antibacterial and antibiofilm activity; also supports autolytic debridement and wound healing. Clinically relevant primarily as a standardized, medical-grade topical wound product. Ordinary food honey is not equivalent. Jull AB et al. Honey as a topical treatment for wounds. Cochrane systematic review.
Oregano oil
Origanum vulgare		 Carvacrol and thymol Antibacterial, antifungal and antibiofilm activity, largely through disruption of microbial membranes. Strong laboratory activity, but inadequate human evidence for oral treatment of infections. Concentrated oil can cause irritation. Chemical composition, biological activity and potential uses of oregano and oregano essential oil: a review.
Thyme
Thymus vulgaris		 Thymol and carvacrol Antibacterial, antifungal and antibiofilm activity through membrane damage and altered microbial permeability. Better established as a constituent of topical antiseptic and oral-care formulations than as an oral treatment for systemic infection. PubMed literature: thyme, thymol and antimicrobial activity.
Tea tree oil
Melaleuca alternifolia		 Terpinen-4-ol and related monoterpenes Topical antibacterial and antifungal activity with some antiviral laboratory activity. Some clinical evidence for topical acne and fungal skin conditions. Tea tree oil is toxic when swallowed and may cause contact dermatitis. Carson CF et al. Melaleuca alternifolia oil: a review of antimicrobial and other medicinal properties.
Echinacea
Echinacea species		 Alkamides, caffeic-acid derivatives, polysaccharides and glycoproteins Primarily immunomodulatory; relatively weak and inconsistent direct antimicrobial activity. Evidence for preventing or shortening respiratory infections is inconsistent and preparation-dependent. National Center for Complementary and Integrative Health: Echinacea—Usefulness and Safety.
Elderberry
Sambucus nigra		 Anthocyanins, flavonols and phenolic acids Antiviral effects have been reported in cell-culture and preclinical studies, including interference with viral entry or replication. Small human trials have examined respiratory symptoms, but evidence remains insufficient to establish treatment of influenza or other viral infections. National Center for Complementary and Integrative Health: Elderberry.
Curcumin / turmeric
Curcuma longa		 Curcumin and related curcuminoids Antibacterial, antifungal, antiviral and antibiofilm activity through multiple membrane, enzyme and signalling effects. Predominantly laboratory evidence. Poor aqueous solubility and low systemic bioavailability are major clinical limitations. Moghadamtousi SZ et al. A review on antibacterial, antiviral and antifungal activity of curcumin.
Ginger
Zingiber officinale		 Gingerols, shogaols and zingerone Antibacterial and antifungal activity, including possible inhibition of microbial adhesion and biofilm formation. Primarily laboratory evidence; there is little direct clinical evidence that ginger supplements treat infections. PubMed literature: ginger, gingerols and antimicrobial activity.
Clove
Syzygium aromaticum		 Eugenol and eugenyl acetate Antibacterial, antifungal and local antiseptic activity, principally through membrane and protein disruption. Relevant mainly to topical, food-preservation and dental applications. Evidence for systemic infection treatment is insufficient. PubMed literature: clove, eugenol and antimicrobial activity.
Cinnamon
Cinnamomum species		 Cinnamaldehyde, eugenol and cinnamic acid derivatives Antibacterial, antifungal and antibiofilm activity; may alter microbial membranes and quorum-sensing pathways. Predominantly laboratory evidence. Cassia cinnamon can contribute substantial coumarin exposure when consumed in concentrated amounts. PubMed literature: cinnamon, cinnamaldehyde and antimicrobial activity.
Neem
Azadirachta indica		 Nimbidin, nimbin, nimbolide, azadirachtin and other limonoids Antibacterial, antifungal, antiparasitic and antibiofilm effects have been reported. Some topical and dental research exists, but systemic clinical evidence is inadequate. Oral neem preparations have important safety concerns. PubMed literature: Azadirachta indica and antimicrobial activity.
Black seed
Nigella sativa		 Thymoquinone, thymohydroquinone and related volatile compounds Antibacterial, antifungal, antiparasitic and possible antiviral activity. Considerable laboratory research but limited, heterogeneous clinical evidence for infectious diseases. PubMed literature: Nigella sativa, thymoquinone and antimicrobial activity.
Green tea extract
Camellia sinensis		 Epigallocatechin gallate (EGCG) and other catechins Antibacterial, antiviral and antibiofilm activity; may damage membranes, inhibit microbial enzymes and enhance some antibiotics. Some localized oral-health evidence, but limited evidence for treating systemic infections. Concentrated extracts may cause liver injury in susceptible individuals. PubMed literature: EGCG, green tea and antimicrobial activity.
Licorice root
Glycyrrhiza species		 Glycyrrhizin, glycyrrhetinic acid, liquiritigenin and other flavonoids Antiviral, antibacterial and antifungal effects have been reported in laboratory and preclinical studies. Limited clinical antimicrobial evidence. Glycyrrhizin can cause hypertension, hypokalemia, fluid retention and clinically important drug interactions. National Center for Complementary and Integrative Health: Licorice Root.
Andrographis
Andrographis paniculata		 Andrographolide and related diterpenoid lactones Immunomodulatory, anti-inflammatory and possible antiviral or antibacterial activity. Some evidence for modest symptom reduction in uncomplicated respiratory infections, but this does not establish direct pathogen eradication. PubMed literature: Andrographis and respiratory infections.
Pelargonium sidoides Proanthocyanidins, phenolic acids and oxygenated coumarin derivatives Possible antiviral, antibacterial anti-adhesive and immunomodulatory activity. Some human evidence for modest symptom improvement in acute bronchitis and selected respiratory infections. It is not a substitute for antibiotics when bacterial treatment is indicated. Timmer A et al. Pelargonium sidoides extract for acute respiratory tract infections. Cochrane systematic review.
Monolaurin
Glycerol monolaurate		 Monolaurin, a monoester derived from lauric acid May disrupt lipid membranes and interfere with signalling or virulence in certain bacteria and enveloped viruses. Predominantly laboratory and animal evidence. There is insufficient clinical evidence to recommend oral monolaurin for infections. PubMed literature: glycerol monolaurate and antimicrobial activity.
Caprylic acid Octanoic acid, an eight-carbon medium-chain fatty acid Antifungal and membrane-disrupting activity, particularly against Candida species, has been reported in vitro. Insufficient human evidence for treating candidiasis or systemic fungal infection. Marketing claims commonly exceed the evidence. PubMed literature: caprylic acid and Candida.
Olive leaf extract
Olea europaea		 Oleuropein, hydroxytyrosol and elenolic-acid derivatives Antibacterial, antiviral and antifungal activity has been observed in laboratory studies. Preliminary evidence only; clinical trials have not established it as a treatment for infectious disease. PubMed literature: olive leaf, oleuropein and antimicrobial activity.
Goldenseal
Hydrastis canadensis		 Hydrastine, canadine and berberine Extracts and individual alkaloids show antibacterial activity in laboratory studies. There is no good clinical evidence that goldenseal treats human infections. Product composition, absorption and drug interactions are important limitations. National Center for Complementary and Integrative Health: Goldenseal.
Sweet wormwood / artemisinin
Artemisia annua 		Artemisinin and related sesquiterpene lactones Artemisinin derivatives are potent antimalarial agents. Additional antibacterial, antiviral and antiparasitic effects are being studied. Artemisinin-based combination therapies are established medicines, not ordinary supplements. Herbal preparations should not replace standardized malaria treatment because dose variability can promote treatment failure and resistance. World Health Organization: Guidelines for malaria.

Evidence interpretation

  • Clinical evidence: Effects have been studied in human participants, but usually for a specific preparation, route, dose and indication.
  • Preclinical evidence: Activity has mainly been demonstrated in cell culture, microbial cultures or animal models.
  • Anti-adhesive or probiotic activity: The product may reduce colonization or pathogen attachment without directly killing the microorganism.
  • Topical evidence: Results from topical use cannot be assumed to apply to an orally administered supplement.


Scientific Papers found: Click to Expand⟱
7385- IBC,    Fighting cancer by triggering non-canonical mitochondrial permeability transition-driven necrosis through reactive oxygen species induction
- vitro+vivo, Lung, A549 - in-vitro, BC, 4T1
Apoptosis↑, necrosis↑, ROS↑, mtDam↑, Ca+2↑, MPT↑, MMP↓, AntiCan↑, *AntiBio↑, *Inflam↓, *antiOx↓, *neuroP↑, p‑Akt↓, DHODH↓, Diff↑, MAPK↑,

Showing Research Papers: 1 to 1 of 1

* indicates research on normal cells as opposed to diseased cells
Total Research Paper Matches: 1

Pathway results for Effect on Cancer / Diseased Cells:


NA, unassigned(tgid=0) ⓘ

DHODH↓, 1,  

Redox & Oxidative Stress(tgid=1) ⓘ

ROS↑, 1,  

Mitochondria & Bioenergetics(tgid=3) ⓘ

MMP↓, 1,   MPT↑, 1,   mtDam↑, 1,  

Cell Death(tgid=5) ⓘ

p‑Akt↓, 1,   Apoptosis↑, 1,   MAPK↑, 1,   necrosis↑, 1,  

Proliferation, Differentiation & Cell State(tgid=12) ⓘ

Diff↑, 1,  

Migration(tgid=13) ⓘ

Ca+2↑, 1,  

Functional Outcomes(tgid=23) ⓘ

AntiCan↑, 1,  
Total Targets: 12

Pathway results for Effect on Normal Cells:


NA, unassigned(tgid=0) ⓘ

AntiBio↑, 1,  

Redox & Oxidative Stress(tgid=1) ⓘ

antiOx↓, 1,  

Immune & Inflammatory Signaling(tgid=16) ⓘ

Inflam↓, 1,  

Functional Outcomes(tgid=23) ⓘ

neuroP↑, 1,  
Total Targets: 4

Scientific Paper Hit Count for: AntiBio, Antibiotic/Antimicrobial activity
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#:446  Target#:1483  State#:%  Dir#:%
  wNotes=0  sortOrder:rid,rpid

 

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