Kinisoquin (isoquercetin) / Quercis Pharma - LARVOL DELTA

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."

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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%."

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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

Fortification of non-dairy milk with date fruit, mustard seed, and turmeric: nutritional quality, probiotics viability, antimicrobial and antioxidant potentials. (PubMed, Sci Rep) - "Plant milk (97%TM + 3%MS) had the highest scavenging activity (89.10%) against 1,1-diphenyl-2-picrylhydrazyl (DPPH), while (97%SM+3%MS) showed the highest activity (305.10 µmol TE/mL) against ferric reducing antioxidant power (FRAP). Plant-based milk fortified with extracts from date fruit, mustard seed, and turmeric displayed nutraceutical potentials and could be considered as promising alternative source of functional foods."

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Moringa (Moringa oleifera) Leaf Attenuates the High-Cholesterol Diet-Induced Adverse Events in Zebrafish: A 12-Week Dietary Intervention Resulted in an Anti-Obese Effect and Blood Lipid-Lowering Properties. (PubMed, Pharmaceuticals (Basel)) - "The in silico findings underscore that the six phytoconstituents (chlorogenic acid, isoquercetin, kaempferol 3-O-rutinoside, astragalin, apigetrin, and myricetin) of MO exhibited a strong interaction with HMG-CoA reductase active and binding site residues via hydrogen and hydrophobic interactions. The findings demonstrated an antioxidant, anti-inflammatory, and hypoglycemic effect of MO, guiding the events to prevent HCD-induced metabolic stress and safeguard vital organs."

Adverse events • Journal • Dyslipidemia • Genetic Disorders • Metabolic Disorders • Obesity • IL6

Exploring the anti-obesity potential of Ailanthus excelsa Roxb in vitro enzymatic inhibition and computational pharmacology insights. (PubMed, Sci Rep) - "Moreover, metabolites showed stronger binding affinities to all four enzymes than reference molecules. By integrating in vitro assays with molecular modeling, this study highlights the promising potential of A. excelsa and its fractions in obesity management, offering valuable insights into its therapeutic applications."

Journal • Preclinical • Genetic Disorders • Obesity • ACACB • AKT1 • CD36 • FASN • IL6 • IR • PIK3CA • PPARA • PPARG • SCARB1 • SLC2A4

A comprehensive study on the color preservation mechanism of isoquercitrin in meat-based food systems. (PubMed, Food Chem X) - "Molecular dynamics and molecular docking experiments further confirmed the interaction between the two. This study confirmed that isoquercitrin can stabilize meat color through a variety of mechanisms, providing a theoretical basis for its application in meat processing."

Journal • MB

In Vivo, Ex Vivo, and In Vitro Antihyperglycemic Evaluation of Croton ehrenbergii. (PubMed, Planta Med) - "Acute oral toxicity studies indicated that the extract was safe at the tested dose. These results provide the first scientific evidence of the antihyperglycemic properties and preliminary safety of C. ehrenbergii."

Journal • Preclinical • Diabetes • Metabolic Disorders • PTPN1

Physiological, Biochemical, and Molecular Mechanisms of Resistance of Poacynum hendersonii to Melampsora apocyni. (PubMed, Plants (Basel)) - "Key enzyme genes (COMT, POD, CAD, F5H) and metabolites (chlorogenic acid, isoquercitrin, rutin) can be used as important targets for disease resistance breeding. Our research provides important reference for the prevention and control of M. apocyni in P. hendersonii."

Journal • Infectious Disease • Metabolic Disorders • COMT

Comprehensive phytochemical characterization, antioxidant potency, and toxicological evaluation of Paederia foetida in Wistar albino rats: Insights into therapeutic efficacy and safety profiles. (PubMed, J Ethnopharmacol) - "The therapeutic effects of P. foetida are closely linked to its high levels of polyphenols, especially chlorogenic acid, isoquercetin, rutin, scopoletin, quinic acid, and quercetin. These compounds are very important for its strong antioxidant and protective effects. PFME showed superior antioxidant and free radical scavenging activity than the PFEE and PFAE. PFME exhibited a favorable safety profile, with no adverse effects detected at doses up to 2000 mg/kg in acute toxicity studies and 1000 mg/kg/day in sub-acute toxicity studies, thereby establishing this dosage as the No-Observed-Adverse-Effect Level (NOAEL). These findings not only validate the traditional utilization of P. foetida but also establish a scientific foundation for its ongoing research and prospective advancement into safe and efficacious medicinal product formulations."

Journal • Preclinical • Hematological Disorders

The King Tuber Medicinal Mushroom Pleurotus tuberregium (Agaricomycetes): A Review on Nutritional Composition, Phytochemistry, Pharmacological Activities, and Toxicity Profile. (PubMed, Int J Med Mushrooms) - "The bioactive phytochemicals in P. tuberregium include kaempferol, quercetin, epicatechin, apigenin, quercitrin, naringin, rutin, isoquercetin, luteolin, caffeic acid, chlorogenic acid, p-coumaric acid, catechin and ellagic acid...This review revealed that P. tuberregium could be used for therapeutic purposes against diseases and as a new material to produce functional foods. However, further studies should be conducted to explore the effective and quality-controlled dosages for the use of this mushroom and to investigate the mechanism of action of the identified bioactive compounds for the treatment of various diseases."

Journal • Review • Oncology

Identification of Dendrobium devonianum Samples With Different Growth Years Based on Active Ingredients and Deduction of the Chemical Structural Transformation. (PubMed, Biomed Chromatogr) - "The results of the volcano plot analysis showed that the up-regulated components among samples with different growth years were mainly naringin, apigenin, and 4-hydroxy benzaldehyde; the content of 4-hydroxy benzaldehyde varied the most among the D. devonianum samples with different growth years. Through a literature review and analysis of the changes in the active compounds in D. devonianum samples with different growth years, the chemical structural transformation of the active compounds in D. devonianum was deduced, and the optimal harvesting period of D. devonianum in Yunnan was determined to be the fourth year of growth."

Journal

Cochlospermum angolense Welw ex Oliv: Phytochemical Profile, Antioxidant Activity, and Therapeutic Prospects. (PubMed, Molecules) - "For the first time, the present study identified new compounds never reported in this species, such as (+)-abscisic acid, angustine B, pinobanksin, dihydrogenistein, (-)-8-prenylnaringenin, isoquercetin, samandarine, dihydromyricetin, and eupatoriocromene, in the leaves, bark, and roots, marking a significant advance in the chemical characterization of C. angolense. These findings enhance our understanding of the bioactive phytochemicals and antioxidant properties of C. angolense and open new avenues for future therapeutic and pharmacological research, further supporting its traditional use in Angolan medicine."

Journal • CA6

Green extraction of polyphenol compound from walnut green husk by microwave-assisted choline chloride-based deep eutectic solvents: identification, kinetic, comparison and bioactivity. (PubMed, Food Chem) - "Besides, DES provided better stability of phenolic compounds during the storage period. This study demonstrates that MAE-DES is a potential extraction technique for the recovery of highly bioactive phenolic compounds from food by-products."

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Isolation and Characterization of Microorganisms from Buckwheat Farmland for the Bioconversion of Quercetin. (PubMed, Microorganisms) - "Among the four potential candidates identified, isoquercetin was determined to be the most likely agent for flavonoid bioconversion based on its biosynthetic pathway and substrate specificity, as well as known characteristics of strain 3P-1. These findings suggest that the isolated strain 3P-1 has substantial potential as a bioconversion agent for transforming quercetin to isoquercetin, which enhances its bioavailability."

Journal

Enhancing bioactive profiles of elderberry juice through yeast fermentation: a pathway to low-sugar functional beverages. (PubMed, Curr Res Food Sci) - "The same cultures significantly released phenolics (including chlorogenic acid, quercetin, hyperoside, and isoquercetin) with biological activity...In conclusion, binary yeast cultures offer an effective way to enrich low-sugar elderberry beverage with bioactive metabolites and appealing flavor. Future research should focus on in vivo validation of bioactivities, product stability, and consumer acceptability to support industrial application."

Journal • Metabolic Disorders

Identification of Novel Leishmania donovani Nucleoside Hydrolase Inhibitors from Banisteriopsis laevifolia Using Affinity Selection-Mass Spectrometry. (PubMed, ACS Omega) - "Among these, isoquercetin and astragalin demonstrated potent LdNH inhibition with IC50 values of 40.2 ± 16.6 and 41.6 ± 8.9 μmol/L, respectively. These findings highlight B. laevifolia as a promising source of bioactive compounds and demonstrate the utility of AS-MS for efficiently identifying enzyme inhibitors in natural libraries."

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Plant-Based Potential in Diabetes Management: In Vitro Antioxidant, Wound-Healing, and Enzyme Inhibitory Activities of Southern Algarve Species. (PubMed, Molecules) - "viscosa showed the highest antioxidant activity (FRAP: 1132.99 ± 19.54 mg TE/g dw; DPPH IC50 = 25.85 ± 0.75 μg/mL) and total phenolic/flavonoid content, with a diverse profile including caffeic and chlorogenic acids, isoquercetin, and quercetin. It also exhibited potent α-glucosidase inhibition (IC50 = 0.61 ± 0.06 mg/mL), outperforming acarbose...A strong correlation was observed between phenolic content and antioxidant/antidiabetic activity. These findings support further in vivo studies on D. viscosa and A. baetica for potential use in T2DM management and diabetic wound healing."

Journal • Preclinical • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus • ELANE

Rosa multiflora fructus and its active compound ellagic acid improve depressive-like behaviors in mice via monoamine oxidase inhibition. (PubMed, Biomed Pharmacother) - "They were then treated with RMFE (100 or 300 mg/kg/day, p.o.) or selegiline (10 mg/kg/day, p.o.) as a positive control...Consistently, EA administration effectively alleviated depressive-like behaviors and increased monoamine neurotransmitter levels in CORT-treated mice. These results suggest that RMFE exerts antidepressant effects by inhibiting MAO, restoring monoamine levels, and modulating hippocampal astrocytic hypertrophy, with EA identified as the primary bioactive compound driving its efficacy."

Journal • Preclinical • CNS Disorders • Depression • Psychiatry