Kinisoquin (isoquercetin) / Quercis Pharma - LARVOL DELTA

Targeting Ferroptosis, Pyroptosis, and NRF2 Signaling with Dietary Polyphenols in Diabetic Microvascular Complications: An Integrative Review. (PubMed, Nutrients) - "The proposed ferroptosis-pyroptosis-NRF2 network should therefore be viewed as a biologically plausible integrative framework rather than a clinically validated linear pathway. Future trials require chemically characterized interventions, exposure biomarkers, tissue-relevant pharmacokinetics, prespecified regulated-cell-death panels, and clinically meaningful microvascular endpoints."

Journal • Review • Cardiovascular • Diabetic Nephropathy • Diabetic Neuropathy • Diabetic Retinopathy • Inflammation • Metabolic Disorders • Nephrology • Pain • Peripheral Neuropathic Pain • Renal Disease • Retinal Disorders • GPX4 • NLRP3 • SLC7A11 • TXNIP

Isoquercetin targets histone methyltransferase G9a to promote BDNF expression and improve cerebral ischemia-reperfusion injury. (PubMed, Brain Res Bull) - "G9a overexpression reversed these protective effects. Isoquercetin alleviates cerebral I/R injury by inhibiting G9a-mediated histone methylation and promoting BDNF expression, highlighting a novel epigenetic mechanism for stroke therapy."

Journal • Cardiovascular • CNS Disorders • Reperfusion Injury • Vascular Neurology • BDNF

Structural and molecular insights into the binding mechanisms of β-glucosidase-ascorbic acid-rutin/isoquercetin ternary systems. (PubMed, Spectrochim Acta A Mol Biomol Spectrosc) - "AA enhanced the binding affinity between Rut/Iso and BGL, and a positive synergy in the co-binding of AA and Rut with BGL. These results provide a theoretical foundation for the potential application of BGL as a carrier for drugs or functional foods and offer new insights into natural enzyme activators and the valorisation of RRT resources."

Journal

Mutant-Selective Binding of Phyllanthus niruri Phytochemicals to EGFR T790M: A Quantum-Classical Mechanistic Study. (PubMed, Int J Mol Sci) - "Five phytochemicals exhibited computationally predicted binding affinities against EGFR T790M exceeding the non-covalent binding component of osimertinib (-25.74 kcal/mol): corilagin (-53.71 ± 5.05 kcal/mol), eriodictyol-7-rhamnopyranoside (-44.35 ± 4.51 kcal/mol), isoquercetin (-44.23 ± 2.92 kcal/mol), rutin (-42.15 ± 4.50 kcal/mol), and kaempferol-4-rhamnoside (-41.68 ± 3.69 kcal/mol)...Supervised PCA/LDA of 7416 MM-PBSA trajectory frames identified solvation energy (ΔGSOLV) as the primary pharmacological class discriminant, with the first discriminant function (LD1) capturing 93.1% of inter-class binding variance. Collectively, corilagin (hydrolyzable tannin), eriodictyol-7-rhamnopyranoside (flavonoid glycoside), and phyltetralin (lignan) constitute diverse computational leads from P. niruri warranting experimental validation as T790M-directed agents in HCC."

Journal • Hepatocellular Cancer • Oncology • Solid Tumor • EGFR

Evaluation of Secondary Metabolites in Various Stages of Okra Seed Development and Their Anti-Inflammatory Potential Against IL-1ß. (PubMed, Int J Mol Sci) - "The findings from this study showed that secondary metabolite accumulation in okra seeds varies at different stages of development. Thus, determining the bioactive compounds at different levels of seed development is considered essential for potential pharmacological advancements in biologically significant plants."

Journal • IL1B

Deciphering the bitterness contribution of Zanthoxylum bungeanum Maxim and its masking mechanism. (PubMed, J Sci Food Agric) - "These findings provide mechanistic insight into processing-induced protein-flavonol interactions and offer theoretical guidance for optimizing spice-assisted meat processing strategies and taste quality regulation."

Journal • TAS2R1

Anti-Infective Effect of Anacardium occidentale L. Flowers Against Eskape Group Bacteria In Vitro, In Vivo, and In Silico. (PubMed, Biomed Res Int) - "EHAo reduces bacterial virulence and improves survival in S. aureus-infected larvae, an activity probably related to the bactericidal activity, inhibition of adhesion and biofilm formation, and interaction with the sortase A active site."

Journal • Preclinical • Infectious Disease • Pneumonia • GDF15

Mechanism of seaweed polyphenols interacting with intestinal flora to regulate blood glucose. (PubMed, Food Chem) - "These bacteria feedback-regulated the production of hypoglycemic polyphenolic substances such as isovitexin and isoquercetin, which showed a strong positive correlation. Further mechanistic studies revealed that FPPE's digest could suppress cellular glucose transport by inhibiting the expression of Sodium Glucose Cotransporter 1 (SGLT1) and glucose transporter 2 (GLUT2), thereby reducing blood glucose levels."

Journal

Chemical profile and in vitro antischistosomal activity of Crotalaria madurensis different extracts. (PubMed, Sci Rep) - "Identification of the isolated compounds relied on their chromatographic properties and spectral data (UV, ESI-MS, 1H NMR, 13C NMR, 1H-1H COSY, HSQC, and HMBC). The antischistosomal activity of the C. madurensis different extracts were assessed in vitro using schistosome worm killing, findings revealed that the aqueous methanol extract was the most effective extract, chromatographic fractionation of this extract revealed significant antischistosomal activity for fractions number V and VI rich in flavonoids and triterpene saponins, respectively."

Journal • Preclinical

In Vivo Anti-Nociceptive Activity of Isoquercetin in Rats Supported by ADMET and Molecular Docking Analysis. (PubMed, Chem Biodivers) - "The molecular docking identified a specific action on cyclooxygenases. Thus, IQN appears to be a promising candidate for the treatment of inflammatory pain, supported by its wide safety margin, potent antioxidant."

Journal • Preclinical • Pain

Associations of Bioactive Constituents of Aster yomena with Environmental Variables. (PubMed, Chem Pharm Bull (Tokyo)) - "HPLC and LC/MS analyses identified chlorogenic acid, rutin, isoquercetin, nicotiflorin, and triterpenoid saponins as the major bioactive constituents. Regression analyses demonstrated that available phosphorus, exchangeable magnesium, and certain climatic factors (e.g., temperature range) were positively correlated with metabolite levels and bioactivities. These findings are expected to provide essential foundational data for future applications of the bioactive constituents of A. yomena in functional foods and pharmaceuticals."

Journal • Gastric Cancer • Oncology • Solid Tumor

Polyphenol combinations improve quercetin absorption and inhibit carbohydrate digestion while reducing glucose transport. (PubMed, Food Funct) - "The mixture doubled quercetin absorption compared to quercetin alone at equal doses, which could be explained by kaempferol's inhibition of efflux transporters. These findings suggest that multi-component polyphenol formulations can enhance α-amylase inhibition and quercetin bioavailability while maintaining strong α-glucosidase inhibition."

Journal • Diabetes • Genetic Disorders • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus

Screening of Chemical Profile by Lc-Esi-Ms/Ms and Assessment of Biological Properties of Phoenix dactylifera From Algeria. (PubMed, Chem Biodivers) - "In addition, the Deglat nour spikelet (DNB) extract demonstrated selective BChE inhibition (IC50: 43.28 ± 0.83 µg/mL), showing greater potency than galantamine. These findings support the potential use of P. dactylifera as a valuable source of nutraceutical and pharmaceutical compounds."

Journal • Pain

Allosteric Interactions of Flavonoids with ACE2 and Potential Implications for COVID-19: Computational Insights, Metabolic and Mitochondrial Effects of Rutin in A549 Cells. (PubMed, Cell Biochem Biophys) - "These findings indicate that rutin formed stable interactions with ACE2, with the potential to influence cellular energy metabolism without inducing cytotoxicity and therapeutic benefits in conditions linked to mitochondrial dysfunction and metabolic stress. While direct ACE2 enzymatic modulation was not confirmed experimentally, these findings provide a mechanistic basis for further studies on ACE2-flavonoid interactions and their potential biological implications in ACE2-associated diseases."

Journal • Infectious Disease • Metabolic Disorders • Novel Coronavirus Disease • Respiratory Diseases • CYP3A4

Ethyl acetate extract from Dinizia excelsa Ducke wood: a potential phytotherapeutic agent with antioxidant, cytotoxic and hemolytic (in normal cells), immunomodulatory, antimicrobial, antiparasitic and antitumor activities. (PubMed, Mol Biochem Parasitol) - "(IC₅₀ 1.83-6.43µg/mL), with additional activity against Schistosoma mansoni (IC₅₀ 114.83-247.0µg/mL) and Plasmodium falciparum 3D7 (IC₅₀ 5438.27ng/mL). Antibacterial MICs ranged 16-512µg/mL and antifungal MICs 16-256µg/mL, consistent with bacteriostatic/fungistatic effects."

Journal • Hematological Disorders • Immunology • Oncology • IFNG • IL10 • IL12A • IL17A • IL2 • IL4 • TGFB1 • TNFA

Megastigmane sesquiterpenoids from the leaves of Gaultheria fragrantissima and their bioactivity evaluation. (PubMed, Phytochemistry) - "Six megastigmane sesquiterpenoids (1-3, 5, 8, and 10) exhibited weak PDI inhibitory activities by binding to the b domain of PDI, rather than the b' domain like isoquercetin. The preliminary structure-activity relationship analyses and AutoDock-based molecular docking analyses provide valuable hints for the rational design of PDI inhibitors based on megastigmane sesquiterpenoids."

Journal • NLRP3

Isoquercetin-ligustrazine co-polymorph attenuates hypoxia-accelerated Alzheimer's disease by suppressing PERK-CHOP-mediated ER stress. (PubMed, Exp Neurol) - "ILCP administration was associated with reduced PERK pathway activation, resulting in reduced oxidative stress, alleviated neuronal damage, and preserved synaptic plasticity. These findings support a role for PERK-CHOP signaling in hypoxia-driven AD pathology and suggest a potential link between ILCP treatment and modulation of this pathway."

Journal • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Obstructive Sleep Apnea • Respiratory Diseases • Sleep Disorder

Isoquercetin Attenuates Myocardial Ischemia-Reperfusion Injury and Post-Infarct Ventricular Remodeling in Association with Inhibition of STING-TBK1-IRF3 Signaling. (PubMed, Tohoku J Exp Med) - No abstract available

Journal • Cardiovascular • Myocardial Ischemia • Reperfusion Injury • STING

Kratom (Mitragyna speciosa) as a Phytochemical-Based Natural Product Exhibiting Opioid-like Analgesic Effects with Reduced Tolerance and Dependence Liability via TLR4-Associated Neuroimmune Modulation. (PubMed, Molecules) - "Selected fractions suppressed pro-inflammatory cytokine expression, increased tail-pinch latency comparable to morphine, reduced withdrawal manifestations, and demonstrated nephroprotective and immunomodulatory effects, although mild reversible hepatic alterations were observed in specific fractions. Overall, kratom ethanol extract exhibited fraction-dependent analgesic and anti-neuroinflammatory activities associated with TLR4 modulation, supporting its potential as a botanical analgesic candidate while emphasizing the importance of safety optimization and standardized fraction development."

IO biomarker • Journal • Addiction (Opioid and Alcohol) • Immunology • Pain • IL1B • IL6 • TLR4

Isoquercetin treatment of mouse sickled red blood cells shows a discernible deformability and sickling phenotype. (PubMed, bioRxiv) - "Thiol isomerase antagonism increased sickled red cell elongation, cellular dehydration and the diamagnetic signature compared to control treatment. Thiol isomerases may be involved in regulating sickled red blood cells mechanical properties through mechanisms that require further investigation."

Journal • Preclinical • Genetic Disorders • Hematological Disorders • Sickle Cell Disease

Computational Screening of Phytocompounds Isolated from Clitoria ternatea Targeting the Inflammatory Pathway: Isoquercetin Identified as an IκB Kinase β Inhibitor for Accelerated Wound Healing. (PubMed, J Med Chem) - "Furthermore, commercial ISQ exhibits 83% DPPH free radical scavenging ability at 10 μg/mL, surpassing the standard and antibacterial activity against a range of bacterial strains and also exhibiting hemocompatibility and cytocompatibility in a dose-dependent manner. These vital bioactivities suggest that ISQ is a promising compound to reduce the inflammation phase by downregulating the IKK-β complex, thereby accelerating wound healing applications."

Journal • Inflammation

Biological Effects of an Isoquercetin-Containing Formulation in Preclinical Models of Skin Aging. (PubMed, Cureus) - "Conclusion In preclinical skin models, a compound containing isoquercetin significantly modulated oxidative stress, inflammatory response, collagen synthesis, and glycation pathways. Controlled clinical studies are required to determine whether these biological effects translate into measurable outcomes in human subjects."

Journal • Preclinical • Dermatology • Inflammation • CXCL8 • IL6 • NQO1

Isoquercetin Ameliorates Obesity-Associated Muscle Atrophy and Modulates the Gut Microbiota-Bile Acid Axis. (PubMed, J Agric Food Chem) - "Additionally, IQ (400 mg/kg) treatment effectively reduced colon inflammation (2.58-fold lower of IL-1β) and gut barrier permeability (1.66-fold lower of ZO-1), as well as reshaped gut microbial community and modulated bile acid composition in obese mice. Overall, these results provide novel evidence that IQ supplementation has the potential for mitigating obesity-related muscle atrophy."

Journal • Genetic Disorders • Inflammation • Muscular Atrophy • Obesity • IL1B • TJP1

Integrating the use of feijoa pulp and peel (Acca sellowiana) in kombucha fermentation: a sustainable approach to promote functionality and sensory acceptability. (PubMed, Food Res Int) - "In the sensory analysis, the GPFK sample stood out with an average overall acceptability score of 7.2 and was associated with positive attributes such as fruity and refreshing. The results reveal the market potential of feijoa-added products, especially those containing peel and pulp (GFK and GPFK), which can be used to produce beverages with functionality, high added value, and consumer acceptance."

Journal

Identification of anticancer compounds from Tapinanthus globiferus: integrating in vitro and in silico approaches. (PubMed, In Silico Pharmacol) - "Rutin, trifolin (a kaempferol glycoside), and epigallocatechin exhibited the strongest binding (e.g. rutin: - 8.85 kcal/mol to VEGF-A), surpassing the reference inhibitor Pazopanib (- 3.56 kcal/mol) with multiple stabilizing interactions with these proteins, suggesting potential to interfere with tumor angiogenesis and cell survival pathways. Collectively, these findings provide a scientific basis for the traditional use of T. globiferus and support its fraction as promising sources of multi-targeted anticancer agents. The identification of bioactive compounds further establishes a foundation for bioassay-guided isolation, mechanistic validation, and future drug development."

IO biomarker • Journal • Preclinical • Colon Cancer • Colorectal Cancer • Oncology • Solid Tumor • BCL2