Kinisoquin (isoquercetin) / Quercis Pharma - LARVOL DELTA

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

Pharmacological and Medicinal Properties of the South American Medicinal Plant Bowdichia virgilioides Kunth and Its Bioactive Products. (PubMed, Life (Basel)) - "Key products include ormosanine (alkaloid), vouacapane (diterpenoid), lupeol (terpenoid), isoquercetin (flavonoid), isocordoin (chalcone), and little-known specific products (bowdichine and bowdenol). The botanical and phytochemical analysis shed light on this valuable Fabaceae species with the objective to promote its preservation and cultivation, as well as further pharmacological investigations aimed at rationalizing its long-established ethnobotanical use."

Journal • Review • Diabetes • Immunology • Infectious Disease • Metabolic Disorders • Pulmonary Disease • Respiratory Diseases • Rheumatology

Isoquercitrin Attenuates Osteoarthritis Progression by Targeting P53-Mediated Ferroptosis: A Mechanistic Study Integrating Network Pharmacology and Experimental Validation. (PubMed, J Nutr Biochem) - "Notably, these protective effects were partially reversed upon co-treatment with nutlin-3, a pharmacological activator of P53. Collectively, these findings demonstrate that ISO alleviates OA pathology by inhibiting P53-dependent ferroptosis, highlighting its potential as a dietary supplement for the prevention and management of OA."

Journal • Immunology • Osteoarthritis • Pain • Rheumatology • ACAN • ADAMTS5 • COL2A1 • GPX4 • MMP13 • SLC7A11

Polygonum cognatum Extract: Multitarget Anti-inflammatory, Antidiabetic, and Epigenetic Modulation Properties. (PubMed, ChemistryOpen) - "Docking, IC50, and compositional data consistently indicate that quercetin, rutin, chlorogenic acid, and kaempferol are key contributors to the observed antioxidant, antidiabetic, anti-inflammatory, and HDAC inhibitory effects. These findings establish P. cognatum as a promising multitarget therapeutic agent with novel epigenetic regulatory mechanisms, supporting its potential development for inflammatory, metabolic, and epigenetic-related disorders."

Journal

Computational investigation of medicinal plants' active ingredient effects as a potential Zika virus treatment: molecular docking, molecular dynamics simulations, ADMET screening, and DFT. (PubMed, J Mol Model) - "As a result, they have excellent pharmacokinetic properties and appreciable bioavailability. The findings of this research strongly suggest that these five molecules could be potential inhibitors of anti-Zika action in the future."

Journal • Infectious Disease

Design Glycosyltransferases with High Glycosyl Transfer Efficiency to Efficiently Produce Isoquercetin from Quercetin. (PubMed, J Agric Food Chem) - "To enable cost-effective production, sucrose synthase GmSUS was coupled with PCAA to regenerate UDP-glucose during quercetin glycosylation, yielding 3.91 mM isoquercetin with a 78.1% conversion rate. This work overcomes a major bottleneck in isoquercetin biosynthesis and offers a practical strategy for its application in the food industry."

Journal

Metabolomics and Transcriptomics Analyses Explore the Genes Related to the Biosynthesis of Antioxidant Active Ingredient Isoquercetin. (PubMed, Foods) - "At the same time, based on the significant antioxidant activity of isoquercitrin, three genes that may be related to isoquercitrin biosynthesis were screened, namely IF7MAT, FG3, and UGT78D2. The results of this study provide insights into the biosynthesis and comprehensive development and utilization of flavonoids in A. membranaceus."

Journal

A Study of Isoquercetin in People With Ovarian Cancer (clinicaltrials.gov) - P2 | N=90 | Recruiting | Sponsor: Memorial Sloan Kettering Cancer Center | Not yet recruiting ➔ Recruiting

Enrollment open • Epithelial Ovarian Cancer • Oncology • Ovarian Cancer • Solid Tumor

Mapping the kidney distribution of Huangkui capsule-derived components in diabetic nephropathy treatment: a mass spectrometry imaging and metabolomics approach nominates quercetin and its conjugates as bioactive candidates. (PubMed, Anal Bioanal Chem) - "Crucially, matrix-assisted laser desorption/ionization mass spectrometry imaging (MALDI-TOF-MSI) directly visualized and identified these quercetin-derived conjugates, particularly quercetin glucuronide, within kidney tissues, suggesting their potential as primary in situ bioactive candidates. This study is the first to spatially resolve the kidney distribution of HKC's active constituents, providing a scientific basis for understanding its mechanism of action and advancing quality control protocols."

Journal • Diabetic Nephropathy • Nephrology • Renal Disease

Discovering the Anti-Inflammatory Potential of Compounds Isolated from the Aerial Parts of Gelasia tomentosa (L.) Zaika, Sukhor. & N.Kilian (Syn. Scorzonera tomentosa), Through In Vitro Techniques and Advanced In Silico Modeling Approaches. (PubMed, Molecules) - "Cichoriin (8) and staphylinioside E (14) are in accordance with Lipinski's, Pfizer's, GSK's, and Golden Triangle rules, indicating a favorable ADME profile as a drug candidate. Further studies are needed to test this potential in specific inflammation models."

Journal • Preclinical • Inflammation • Rheumatology • TP53

Isoquercetin and Zafirlukast Cooperatively Suppress Tumor Growth and Thromboinflammatory Signaling in a Xenograft Model of Ovarian Cancer. (PubMed, FASEB J) - "ISOQ also potentiated standard cisplatin/gemcitabine chemotherapy. Notably, the combination of low-dose ISOQ plus ZAF achieved ≥ 80% inhibition of key tumor-associated markers at one-third the monotherapy dose and outperformed either agent alone. These findings support ISOQ and ZAF as promising agents for the treatment of cancer and CAT and establish thiol isomerase inhibition as a strategy to simultaneously target thrombosis, tumor progression, and immune escape."

IO biomarker • Journal • Preclinical • Cardiovascular • Hematological Disorders • Oncology • Ovarian Cancer • Solid Tumor • Venous Thromboembolism • PDIA3 • PD-L1

Molecular Docking and Inhibition of Phosphatidylinositol 3-kinase by Quercetin and Isoquercetin from Streptomyces griseoaurantiacus HNF214. (PubMed, Anticancer Res) - "The microbial-derived quercetins effectively induce apoptosis and inhibit HepG2 proliferation by inactivating the PI3K/Akt/mTOR signaling pathway. Quercetin is specifically predicted to directly inhibit PI3K and AKT proteins, underscoring the potential of these compounds as targeted anticancer candidates."

Journal • Oncology • ANXA5 • CASP3 • CASP9

Processing-Induced Changes in Phenolic Composition and Dough Properties of Grape Pomace-Enriched Wheat Buns. (PubMed, Foods) - "FTIR confirmed spectral shifts likely due to fPHE-protein/starch interactions. In summary, incorporation of just 5% GP enhanced the nutritional profile of wheat buns."

Journal

A Study of Isoquercetin in People With Ovarian Cancer (clinicaltrials.gov) - P2 | N=90 | Not yet recruiting | Sponsor: Memorial Sloan Kettering Cancer Center

New P2 trial • Epithelial Ovarian Cancer • Oncology • Ovarian Cancer • Solid Tumor

Discovery of Potent Antibacterial and Anticancer Flavonoids from Beehive-Associated Streptomyces griseoaurantiacus HNF214. (PubMed, Pak J Biol Sci) - "<b></b> <i>Streptomyces griseoaurantiacus</i> HNF214 from beehives produces quercetin and isoquercetin, exhibiting both antibacterial and anticancer activities, likely via MAPK/ERK pathway inhibition. While promising, further safety and <i>in vivo</i> studies are crucial before therapeutic development."

Journal • Cervical Cancer • Infectious Disease • Liver Cancer • Oncology • Solid Tumor • MAP2K1 • MAP2K2

Therapeutic Perspectives of SIRT6 Regulation: Computational Analysis of Activation and Inhibition by Bioactive Molecules. (PubMed, J Mol Recognit) - "Therefore, we investigated the interactions between the ligands quercetin (QUE), isoquercetin (ISO), catechin gallate (CG), and trichostatin A (TSA) with SIRT6, using computational methods from the perspective of molecular modeling through the Molecular Fractionation with Caps Conjugates (MFCC) technique and according to the calculation parameters of Density Functional Theory (DFT)...In addition, residues such as PRO62, MET136, MET157, and VAL115 stand out as key components of the protein active site. These findings offer strategic insights into the molecular mechanisms underlying the binding of the studied ligands to SIRT6, providing a deep understanding of their affinity and pharmacological potential."

Journal • Metabolic Disorders • Oncology • SIRT6

Computational profiling of flavonoids against key breast cancer targets: an in-silico exploration. (PubMed, In Silico Pharmacol) - "Comparative docking with five reference drugs (Alpelisib, Buparlisib, Lapatinib, Gefitinib, and Afatinib) identified nine flavonoids; Sphaerobioside, Avicularin, Nicotiflorin, Myricetin, Quercitrin, Rutin, Isoquercetin, Didymin, and Robinin as promising candidates with favorable binding affinities and stable receptor interactions...Collectively, these findings highlight the multitarget inhibitory potential of selected flavonoids and demonstrate how integrated computational profiling can accelerate the discovery and optimization of natural product-based anticancer agents. The online version contains supplementary material available at 10.1007/s40203-025-00489-0."

Journal • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • EGFR • HER-2

Nanonine, a Synthetic Nanobody Targeting Protein Disulfide Isomerase, Is a New Weapon in Our Antithrombotic Arsenal (ASH 2024) - "Conclusions : NanoNine, a synthetic nanobody targeting PDI, shows promise as a new candidate for preclinical development. The cryo-EM structure of the PDI-NanoNine complex will facilitate further drug discovery and structure-based optimization of PDI-targeted antithrombotics."

Cardiovascular • Thrombosis

CATIQ P3: The Effect of Kinisoquin on Thromboembolic Events in Patients With Metastatic Pancreatic Cancer (clinicaltrials.gov) - P3 | N=480 | Recruiting | Sponsor: Quercis Pharma AG | Not yet recruiting ➔ Recruiting | N=340 ➔ 480 | Trial completion date: Dec 2026 ➔ Oct 2029 | Initiation date: Jun 2025 ➔ Oct 2025 | Trial primary completion date: Jul 2026 ➔ Oct 2027

Enrollment change • Enrollment open • Trial completion date • Trial initiation date • Trial primary completion date • Cardiovascular • Oncology • Pancreatic Cancer • Solid Tumor • Venous Thromboembolism

Isoquercetin mitigates neuroinflammation and oxidative stress by targeting the NF-κB pathway. (PubMed, Brain Res) - "According to an IHC study, ISO decreased the expression of NF-κB, which results in a decrease in neuroinflammation. The neuroprotective effect of ISO in MPTP-induced PD in zebrafish is attributed by modulating by NF-κB pathway."

Journal • CNS Disorders • Inflammation • Mood Disorders • Movement Disorders • Parkinson's Disease • Psychiatry • CAT • IL1B • IL6 • TNFA

Antihyperlipidemic Effect of Flavonoids and Saponins from Pyracantha fortuneana Fruits on L02 Cells and Caenorhabditis elegans. (PubMed, Foods) - "Meanwhile, both PFF and PFS significantly reduced lipid deposition, reactive oxygen species (ROS) levels, malondialdehyde (MDA) content, and catalase activity in C. elegans. In summary, our results indicated that the flavonoids and saponins of P. fortuneana are potential natural products in antihyperlipidemic effect."

Journal • Dyspepsia • Metabolic Disorders • CAT

Chemical composition and antioxidant activity of Amazonian Myrciaria dubia seed. (PubMed, Nat Prod Res) - "In the antioxidant analysis, the hydroalcoholic extract showed superior capacity when compared to the aqueous extract in all methods. The compounds scopolin, 2',4-dihydroxychalcone and dihydroxymandelic acid were identified for the first time in the camu-camu seed, and further studies are needed on the relationship between the activity of these compounds and how the structural position affects the antioxidant activity of the camu-camu."

Journal

Physicochemical Properties and Quality of Bread Enriched with Haskap Berry (Lonicera caerulea L.) Pomace. (PubMed, Molecules) - "Enrichment resulted in elevated concentrations of chlorogenic acid, neochlorogenic acid, cryptochlorogenic acid, protocatechuic acid, and p-coumaric acid. Furthermore, the contents of flavonoid aglycones, particularly quercetin and luteolin, as well as flavonoid glycosides, especially rutin and isoquercetin, were increased. Considering the quality attributes of bread enriched with Lonicera caerulea pomace, together with the associated increase in bioactive compounds, its proportion in wheat flour should not exceed 2%."

Journal

Inducing a synergistic anti-obesity effect by increasing the bioavailability of the flavonoid rutin with a L. plantarum strain. (PubMed, Food Chem) - "At 30 min post-administration, isoquercetin-more bioavailable and effective than its precursor, rutin-peaked (∼9 μM) in mouse portal vein blood, while remaining minimal or undetectable in controls. This pairing of functional flavonoid and tailored probiotic synergistically combats obesity via ileal isoquercetin conversion, offering a promising single-flavonoid, single-probiotic obesity-management strategy."

Journal • Genetic Disorders • Obesity