escin / Generic mfg. - LARVOL DELTA

β-escin mitigates neuroinflammation and apoptosis caused by ischemic stroke through the inhibition of the interleukin-6/Janus kinase 2/signal transducer and activator of transcription 3 signaling pathway. (PubMed, J Int Med Res) - "It significantly suppressed the release of proinflammatory cytokines and downregulated the expression of interleuin-6 and interleukin-6 receptor as well as the ratios of phosphorylated Janus Kinase 2/Janus Kinase 2 and phosphorylated signal transducer and activator of transcription 3/ signal transducer and activator of transcription 3. These protective effects were positively correlated with the dosage of β-escin.ConclusionThe findings suggested that β-escin exerted neuroprotective effects in ischemic stroke by modulating the interleukin-6/Janus kinase 2/signal transducer and activator of transcription 3 pathway, thereby reducing neuroinflammation and apoptosis."

Journal • Cardiovascular • CNS Disorders • Inflammation • Ischemic stroke • Oncology • IL1B • IL6 • IL6R • JAK2 • STAT3 • TNFA

Escin Preincubation Enhances the Therapeutic Effect of Umbilical Cord-Derived Mesenchymal Stem Cells in a Rat Model of Myocardial Infarction. (PubMed, Stem Cells Int) - "The current study demonstrates that escin upregulated ICAM1 and GATA4 gene expression in UCMSCs, thereby enhancing the therapeutic efficacy of UCMSCs in rats with MI. Therefore, pretreatment of UCMSCs with escin is a promising approach for the treatment of MI."

Journal • Preclinical • Cardiovascular • Fibrosis • Immunology • Myocardial Infarction • ICAM1 • TERC

Reparil: Evaluation of Aescin-Based Herbal Extracts for Managing Postoperative Sequelae Following Impacted Mandibular Third Molar Surgery: A Randomized, Single-Blind, Controlled Trial (clinicaltrials.gov) - P=N/A | N=100 | Not yet recruiting | Sponsor: Oman Medical Speciality Board

New trial • Pain

Escin displays neuroprotective effects in mice with intracerebral hemorrhage through ameliorating intestinal injury. (PubMed, Am J Transl Res) - "The ICH-induced brain injury caused intestinal barrier damage, resulting in LPS in the gut to enter blood circulation, which subsequently disrupted the BBB. Therefore, LPS plays an important role in ICH-induced secondary brain injury. Escin exerts its neuroprotective effect by attenuating gut injury following ICH."

Journal • Preclinical • Cerebral Hemorrhage • CNS Disorders • Hematological Disorders • Inflammation • Vascular Neurology

Efficacy and mechanism of escin in improving the tissue microenvironment of blood vessel walls via anti-inflammatory and anticoagulant effects: Implications for clinical practice. (PubMed, Open Life Sci) - "These mechanisms collectively enhance the tissue microenvironment of blood vessel walls and promote cardiovascular health, which provides a multi-target therapeutic strategy for cardiovascular diseases (CVD), integrating anti-inflammatory, antioxidant, endothelial repair, and microcirulation-enhancing mechanisms, consistent with current pathophysiological insights. The article also addresses the current research status, challenges, and future potential of escin in vascular protection, offering new perspectives and strategies for CVD treatment and prevention."

Journal • Review • Cardiovascular

Comparative analysis of solvent and advanced extraction techniques for optimizing phytochemical yield and bioactivity of Matthiola ovatifolia (Boiss.) Aerial parts. (PubMed, Sci Rep) - "The ethanolic extract prepared using the MAE contained the highest total phenolics (69.6 ± 0.3 mg gallic acid equivalent (GAE)/g dry weight), total flavonoids (44.5 ± 0.1 mg quercetin equivalent (QE)/g dry weight), total tannins (45.3 ± 0.5 mg catechin/g dry weight), total alkaloids (71.6 ± 0.2 mg atropine equivalent (AE)/g dry weight) and total saponins (285.6 ± 0.1 mg escin equivalent (EE)/g dry weight) as compared to the extracts obtained with the aid of other methods. The highest antioxidant, antibacterial, cytotoxic, antidiabetic, and anti-inflammatory activities were also found for the same extract. According to the obtained results, the MAE method was much more appropriate for the extraction of phytochemicals from the M. ovatifolia."

Clinical • Journal • Breast Cancer • Hepatocellular Cancer • Liver Cancer • Oncology • Solid Tumor

Escin inhibits PD-L1 expression by suppressing the p38 MAPK/ERK signalling pathways and synergistically enhances PD-1 inhibitor efficacy in hepatocellular carcinoma. (PubMed, Phytomedicine) - "This study provides novel insights into the mechanism of action of escin in inhibiting HCC and confirms the potential of escin in conjunction with ICIs as a therapeutic approach to impede HCC progression."

IO biomarker • Journal • Hepatocellular Cancer • Liver Cancer • Oncology • Solid Tumor • CD8 • MRC1

Microcirculation-Promoting Effect of Escin on Cutaneous Tissue via Gsk3β Down-Regulation. (PubMed, Curr Issues Mol Biol) - "Escin-mediated Wnt signaling activation could enhance blood vessel networks via Gsk3β down-regulation. In conclusion, our data demonstrate that escin promotes angiogenic behavior and enhances adenosine-induced perfusion in humans, thereby supporting its potential role in modulating cutaneous microcirculation."

Journal • Inflammation • GSK3B • MAPK8

THE PROTECTIVE EFFECT AND MECHANISM OF ESCIN ON ETHANOL-INDUCED GASTRIC MUCOSAL INJURY IN RATS (UEGW 2025) - "For this purpose, a control, ethanol, ethanol+Escin , and ethanol+omeprazole groups were established in male SD rats to compare and analyze the ulcer index and histopathological scores of each group. Escin exerts a protective effect on ethanol-induced gastric mucosal damage by inhibiting the TNF-α/NF-κB pathway, reducing the expression of inflammatory factors and the level of cell apoptosis. Escin, as a novel therapeutic drug for ethanol-induced gastric ulcers, has certain clinical translational application value, but further clinical trials are needed to confirm the results."

IO biomarker • Preclinical • Inflammation • Peptic Ulcer • BCL2 • BCL3 • BIRC3 • CASP3 • CCL2 • CX3CL1 • IL1B • IL6 • MUC5AC • OSMR • PIM1 • SOCS1 • SOCS3 • TNFA

High-throughput screening methods to discover new ribosomal inhibitors that rescue multiple classes of CFTR variants (NACFC 2025) - "Studies included treatment comparisons to established inhibitors of translation (G418, PTC-124, ELX-02, Escin) and CFTR modulators (elexacaftor-tezacaftor-ivacaftor, vanzacaftor-tezacaftor-deutivacaftor). Partial depletion of RPL12 levels represents a feasible strategy for CFTR modulation, which may be applicable to CFTR genotypes refractory to available clinical interventions. Our work serves as a foundation from which future investigations may be pursued to examine efficacy and tolerability of anti-RPL12 compounds or ASOs delivered to CF animal models."

CFTR

The Effect of Escin on the Plasma Membrane of Human Red Blood Cells. (PubMed, Int J Mol Sci) - "Using two spin labels that covalently bonded with thiols, we demonstrated that treatment of RBCs with escin did not affect cytoskeletal proteins or plasma membrane surface proteins. Research indicates that the main target of escin's action is the lipid portion of the membrane, not membrane proteins."

Journal • Cardiovascular • Hematological Disorders

Escin alleviates DNCB-induced atopic dermatitis-like symptoms by promoting autophagy activation and tight junction barrier restoration. (PubMed, Int J Biochem Cell Biol) - "These protective effects were associated with the activation of the AMPK-mTORC1-TFEB signaling pathway. Collectively, our findings indicate that escin enhances autophagy and restores skin barrier function, highlighting its potential as a novel therapeutic agent for AD treatment."

Journal • Atopic Dermatitis • Dermatitis • Dermatology • Immunology • Inflammation • ATG7 • CLDN1 • IFNG • IL13 • IL4 • TFEB • TJP1

Soy isoflavone yeast fermented extract inhibits contraction of rat ileal smooth muscle via opening of K+ channels and activation of intracellular cyclic adenosine monophosphate- and cyclic guanosine monophosphate-related pathways. (PubMed, J Vet Med Sci) - "SoyF and soyN inhibited carbachol (CCh)- or KCl-induced contraction in a concentration-dependent manner; however, these effects were stronger for CCh-induced contraction than that for KCl, and the relaxation effect was stronger for soyF than for soyN. SoyF-induced relaxation was attenuated by 4-aminopyridine (4-AP), a Kv channel inhibitor, and iberiotoxin (IbTX), a calcium-activated potassium channel (BK channel) inhibitor...In β-escin-permeabilized muscle, CCh, guanosine 5'-O-(3-thiotriphosphate) (GTPγS), and phorbol-12,13-dibutyrate ( PDBu)-enhanced Ca2+-induced contraction, but soyF suppressed this Ca2+ sensitization...Cell membrane hyperpolarization is probably mediated by the activation of Kv and BK channels via cGMP-related signals. Furthermore, the inhibitory effect on the contractile protein is due to Ca2+ desensitization, probably through suppression of the Rho kinase/myosin phosphatase targeting subunit (MYPT) and/or the PKC/CPI-17 pathway."

Journal • Preclinical

Anti-Apoptotic Effects of Escin on Porphyromonas gingivalis-Derived Lipopolysaccharide-Induced Injury in SH-SY5Y Cells. (PubMed, Brain Behav) - "Pg-LPS leads to SH-SY5Y cells' mitochondria malfunction and programed cell death. Escin alleviated SH-SY5Y cell injury induced by Pg-LPS through its anti-apoptotic effects."

Journal • CNS Disorders • Movement Disorders • Parkinson's Disease • BAX • BCL2 • CASP3 • PARP1

Granzyme B as a potential biological target in toxic encephalopathy: A big data-based exploratory analysis. (PubMed, Medicine (Baltimore)) - "Furthermore, β-escin sodium and methylprednisolone may modulate GZMB expression, thereby alleviating neuronal damage and improving outcomes in delayed encephalopathy after carbon monoxide poisoning. Elevated GZMB expression likely contributes to the pathogenesis and progression of toxic encephalopathy through multiple pathways, making it a potential disease biomarker and therapeutic target."

Journal • CNS Disorders • GZMB • TGFB1

Protective effects of escin and dextromethorphan on Alzheimer disease in Caenorhabditis elegans models (PubMed, Beijing Da Xue Xue Bao Yi Xue Ban) - "ESC and DEX could improve the reductions of movement ability and cognitive function in the AD model worms and delay the aggravation of AD-related symptoms. ESC delays the progression of AD possibly by activating the SKN-1/Nrf2 pathway to protect against oxidative injury in the AD model."

Journal • Alzheimer's Disease • CNS Disorders

Enhancing Escin's Therapeutic Efficacy: A Nanoformulation Approach for Improved Stability and Anticancer Potential. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "Furthermore, the impact of the nanoformulation on cancer cell migration, mitochondrial membrane potential (MMP), ROS generation, and mitochondrial superoxide production was assessed, revealing a significant reduction in cancer cell proliferation and migration, accompanied by ROS-mediated apoptosis. These findings underscore the potential of escin-loaded cellulose nanofibers as a promising and favorable option for selectively targeting cancer."

Journal • Oncology

Nephronectin (NPNT) is a Crucial Determinant of Idiopathic Pulmonary Fibrosis: Modulating Cellular Senescence via the ITGA3/YAP1 Signaling Axis. (PubMed, Adv Sci (Weinh)) - "The study reveals that NPNT deficiency exacerbates bleomycin-induced senescence in alveolar epithelial cells, potentially intensifying fibrosis severity due to diminishes extracellular matrix turnover. Notably, pharmacological elevation of NPNT protein levels using Escin has been shown to alleviate pulmonary fibrosis and improve lung function in mice. The findings shed light on the key mechanism underlying stress-induced senescence and fibrosis, and offer a promising framework for interventions targeting aging-related diseases."

Journal • Fibrosis • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease • Respiratory Diseases • Targeted Protein Degradation • ITGA3 • LATS1 • YAP1

Chemopreventive and Anticancer Activity of Selected Triterpenoids in Melanoma. (PubMed, Cancers (Basel)) - "These plant-derived compounds exhibit diverse biological activities, e.g., cell viability and proliferation inhibition, apoptosis induction, cell cycle regulation, and immune system modulation. The review evaluates the current state of the art on the chemopreventive and anticancer activity of lupane- (betulinic acid), oleanane- (oleanolic acid, β-amyrin, escin, hederagenin, glycyrrhetinic acid), and ursane-type (ursolic acid, asiatic acid, madecassic acid, α-amyrin) triterpenoids in melanoma, highlighting their mechanisms of action, therapeutic potential, and challenges in clinical application."

Journal • Review • Genetic Disorders • Melanoma • Oncology • Skin Cancer • Solid Tumor

Chitosan/xanthan gum polyelectrolyte complex microparticles for enhanced oral delivery of ibuprofen and escin: pharmacokinetic and safety assessment in Wistar rats. (PubMed, Int J Biol Macromol) - "The safety of escin was also maintained both in solution and in microparticle form. These findings emphasize the potential of chitosan/xanthan gum polyelectrolyte complex-based microparticles to overcome the respective challenges of oral administration of ibuprofen and escin."

Journal • PK/PD data • Preclinical

ESCIN ATTENUATED DSS-INDUCED COLITIS BY REMODELING MACROGHAPFE POLARIZATION THROUGH NF-KAPPA B SIGNALING (DDW 2025) - "We discovered that escin effectively attenuates colitis, preserves mucosal barrier integrity, and induces a phenotypic transition of macrophages from immature pro-inflammatory states to mature pro-resolving forms. This transition is associated with the inhibition of NF-κB signaling activation. Our findings underscore the potential therapeutic value of escin in the treatment of inflammatory bowel disease (IBD)."

Gastroenterology • Gastrointestinal Disorder • Immunology • Infectious Disease • Inflammation • Inflammatory Bowel Disease • IL1B • IL6 • OCLN • TJP1 • TNFA

Mechanical adaptivity of red blood cell flickering to extrinsic membrane stiffening by the solid-like biosurfactant β-Aescin. (PubMed, Biophys J) - "Experiments show that active RBC flickers adapt mechanically to β-escin, unlike the passive thermal fluctuations observed in lipid bilayers without an active skeleton...From the unveiled diffusive mechanics, we model an adaptive RBC homeostasis that recapitulates the active flickering phenomenon as an optimal membrane softness upon a regulated friction as observed under aescin-induced membrane hardening. From a physiological perspective, RBC flicker adaptiveness to rigidization is discussed according to regulatory principles of energy conservation and minimal dissipation."

Journal

Escin Rescues Blood-brain Barrier and Inhibits NLRP3 Inflammasome-mediated Pyroptosis in Rats with Superior Sagital Sinus Thrombosis. (PubMed, Int J Med Sci) - " Treatment with escin improved motor function not by recanalizing the SSS. Treatment with escin protected the blood-brain barrier, inhibited the microglia activation and suppressed the NLRP3 inflammasome-mediated pyroptosis in the parasagittal cortex of SSST rats, thereby playing an anti-pyroptosis and neuroprotective effect."

Journal • Preclinical • Cardiovascular • Hematological Disorders • Thrombosis • CASP1 • CD68 • IL18 • IL1B • MMP9 • NLRP3 • OCLN • TJP1

Escin Ia Ameliorates DSS-Induced Chronic Colitis in Mice by Inhibiting Inflammation and Oxidative Stress via the LOXL2/MMP-9 Pathway. (PubMed, J Ethnopharmacol) - "Escin Ia inhibits inflammation and oxidative stress through the LOXL2/MMP-9 pathway, thereby restoring intestinal mucosal barrier function. Improved recurrent symptoms in mice with enteritis."

Journal • Preclinical • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Stress Ulcer • Ulcerative Colitis • LOXL2 • MMP9

Ameliorative Effects of Escin on Inflammation via Glucocorticoid Receptor (GR) in Atopic Dermatitis (AD) Mouse Model. (PubMed, J Microbiol Biotechnol) - "Interestingly, pre-treatment with RU486, a glucocorticoid receptor (GR) antagonist, attenuated the therapeutic effects of escin. Furthermore, escin inhibited the lipopolysaccharide (LPS)-induced overproduction of nitric oxide (NO), protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), and mRNA expression of IL-6 and IL-1β in RAW 264.7 cells. These results indicate that escin may offer therapeutic potential in treating AD through the GR."

Journal • Preclinical • Atopic Dermatitis • Dermatitis • Dermatology • Immunology • Inflammation • Oncology • FLG • IFNG • IL13 • IL1B • IL6 • PTGS2 • TNFA • TSLP