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Dominik Domanski, Oliwia Zegrocka-Stendel, Anna Perzanowska, Malgorzata Dutkiewicz, Magdalena Kowalewska, Iwona Grabowska, Dorota Maciejko, Anna Fogtman, Michal Dadlez, Katarzyna Koziak
β-escin is a mixture of triterpene saponins isolated from the horse chestnut seeds (Aesculus hippocastanum L.). The anti-edematous, anti-inflammatory and venotonic properties of β-escin have been the most extensively clinically investigated effects of this plant-based drug and randomized controlled trials have proved the efficacy of β-escin for the treatment of chronic venous insufficiency. However, despite the clinical recognition of the drug its pharmacological mechanism of action still remains largely elusive...
2016: PloS One
Elizabeth Harford-Wright, Nicolas Bidère, Julie Gavard
Glioblastoma multiforme (GBM) is a highly aggressive tumour of the central nervous system and is associated with an extremely poor prognosis. Within GBM exists a subpopulation of cells, glioblastoma-initiating cells (GIC), which possess the characteristics of progenitor cells, have the ability to initiate tumour growth and resist to current treatment strategies. We aimed at identifying novel specific inhibitors of GIC expansion through use of a large-scale chemical screen of approved small molecules. Here, we report the identification of the natural compound β-escin as a selective inhibitor of GIC viability...
September 1, 2016: Oncotarget
Venkateshwar Mutyam, Ming Du, Xiaojiao Xue, Kim M Keeling, E Lucile White, J Robert Bostwick, Lynn Rasmussen, Bo Liu, Marina Mazur, Jeong S Hong, Emily Falk Libby, Feng Liang, Haibo Shang, Martin Mense, Mark J Suto, David M Bedwell, Steven M Rowe
RATIONALE: Premature termination codons (PTCs) in the cystic fibrosis transmembrane conductance regulator (CFTR) gene cause cystic fibrosis. A number of agents are known to suppress PTCs, but are poorly efficacious or toxic. OBJECTIVES: To determine whether there are clinically available agents that elicit translational readthrough and improve CFTR function sufficient to confer therapeutic benefit to CF patients with PTCs. METHODS: Two independent screens, firefly luciferase and CFTR-mediated transepithelial chloride conductance assay (TECC), were performed on a library of 1600 clinically approved compounds using fisher rat thyroid (FRT) cells stably transfected with stop codons...
April 22, 2016: American Journal of Respiratory and Critical Care Medicine
Yuhui Wang, Xiaotian Xu, Peng Zhao, Bei Tong, Zhifeng Wei, Yue Dai
The saponin fraction of Aesculus chinensis Bunge fruits (SFAC) could inhibit the invasion and migration of MDA-MB-231 cells. Among which, escin Ia showed more potent inhibition of the invasion than other five main saponin constituents. It selectively reduced the expression of LOXL2 mRNA and promoted the expression of E-cadherin mRNA, and prevented the EMT process of MDA-MB-231 cells and TNF-α/TGF-β-stimulated MCF-7 cells. Moreover, it reduced the LOXL2 level in MDA-MB-231 cells but not in MCF-7 cells. When MCF-7 cells were stimulated with TNF-α/TGF-β, transfected with LOXL2 or treated with hypoxia, escin Ia down-regulated the level of LOXL2 in MCF-7 cells...
April 26, 2016: Oncotarget
Gabriela Mojžišová, Martin Kello, Martina Pilátová, Vladimíra Tomečková, Janka Vašková, Ladislav Vaško, Silvia Bernátová, Ladislav Mirossay, Ján Mojžiš
This study examined the antiproliferative effects of β-escin (E) in cancer cells. The study showed that E inhibited cancer cells growth in a dose-dependent manner. The flow cytometric analysis revealed an escin-induced increase in the sub-G1 DNA content, which is considered to be a marker of apoptosis. Apoptosis was also confirmed by annexin V staining and DNA fragmentation assay. These effects were associated with increased generation of reactive oxygen species (ROS), caspase-3 activation and decreased mitochondrial membrane potential (MMP)...
2016: Acta Biochimica Polonica
Zead Helmi Mahmoud Abudayeh, Khaldun Mohammad Al Azzam, Ahmad Naddaf, Uliana Vladimirovna Karpiuk, Viktoria Sergeevna Kislichenko
PURPOSE: To separate and quantify four major saponins in the extracts of the skin and the endosperm of seeds of horse chestnut (Aesculus hippocastanum L.) using ultrasonic solvent extraction followed by a high performance liquid chromatography-diode array detector (HPLC-DAD) with positive confirmation by thin layer chromatography (TLC). METHODS: The saponins: escin Ia, escin Ib, isoescin Ia and isoescin Ib were extracted using ultrasonic extraction method. The optimized extraction conditions were: 70% methanol as extraction solvent, 80 °C as extraction temperature, and the extraction time was achieved in 4 hours...
November 2015: Advanced Pharmaceutical Bulletin
Yuan Du, Yanqin Song, Leiming Zhang, Menglin Zhang, Fenghua Fu
The present study was aimed at investigating whether low dose oral prednisone combined with escin could inhibit the progression of adjuvant-induced arthritis (AIA) in rats. Adjuvant arthritis was induced in SD rats began day 1 for 28 days. Prednisone at doses of 2, 10 mg/kg/day alone or escin at doses of 5, 10 mg/kg/day alone, or prednisone at dose of 2 mg/kg/day with escin at doses of 5 or 10 mg/kg/day were given to different groups of rats intragastrically from day 13 to 28 respectively. Paw swelling, arthritic index, histological and radiographic changes were assessed to evaluate the anti-arthritic effect...
February 2016: International Immunopharmacology
Kaijun Wang, Yiqian Jiang, Wei Wang, Jian Ma, Min Chen
Here we explored the anti-oxidative and cytoprotective potentials of escin, a natural triterpene-saponin, against hydrogen peroxide (H2O2) in retinal pigment epithelium (RPE) cells. We showed that escin remarkably attenuated H2O2-induced death and apoptosis of established (ARPE-19) and primary murine RPE cells. Meanwhile, ROS production and lipid peroxidation by H2O2 were remarkably inhibited by escin. Escin treatment in RPE cells resulted in NF-E2-related factor 2 (Nrf2) signaling activation, evidenced by transcription of anti-oxidant-responsive element (ARE)-regulated genes, including HO-1, NQO-1 and SRXN-1...
December 25, 2015: Biochemical and Biophysical Research Communications
Minmin Li, Chengwen Lu, Leiming Zhang, Jianqiao Zhang, Yuan Du, Sijin Duan, Tian Wang, Fenghua Fu
The present study aimed to investigate the effects of oral administration of escin on acute inflammation and intestinal mucosal injury in animal models. The effects of escin on carrageenan-induced paw edema in a rat model of acute inflammation, cecal ligation and puncture (CLP) induced intestinal mucosal injury in a mouse model, were observed. It was shown that oral administration of escin inhibits carrageenan-induced paw edema and decreases the production of prostaglandin E2 (PGE2) and cyclooxygenase- (COX-) 2...
2015: Evidence-based Complementary and Alternative Medicine: ECAM
Rayan Khaddaj-Mallat, Chantal Sirois, Marco Sirois, Edmond Rizcallah, Caroline Morin, Éric Rousseau
The aim of this study was to investigate the effects of resolvin D1 (RvD1), as well as the combined treatment of docosahexaenoic acid monoglyceride (MAG-DHA) and acetylsalicylic acid (ASA), on the resolution of inflammation markers and Ca(2+) sensitivity in IL-13-pretreated human bronchi (HB). Tension measurements performed with 300 nM RvD1 largely abolished (50%) the over-reactivity triggered by 10 ng/ml IL-13 pretreatment and reversed hyper Ca(2+) sensitivity. Addition of 300 nM 17(S)-HpDoHE, the metabolic intermediate between DHA and RvD1, displayed similar effects...
September 2015: Prostaglandins & Other Lipid Mediators
Yajun Cheng, Hongrui Wang, Min Mao, Chao Liang, Yu Zhang, Deijun Yang, Ziran Wei, Shunxiang Gao, Bo Hu, Lianghua Wang, Qingping Cai
BACKGROUND: Previous studies have described the effects of Escin on improving the survival rate of endotoxemic animals. The purpose of this study was to explore the molecular mechanisms of this potentially beneficial treatment. METHODS: First, the survival rate of endotoxemic mice was monitored for up to 2 weeks after Escin pretreatment, Escin post-treatment, or Escin post-treatment + rHMGB1. The effects of Escin on the release of pro-inflammatory cytokines such as TNF-α, IL-1β, IL-6 and HMGB1 in the serum of endotoxemic mice and LPS-induced macrophages were evaluated by ELISA...
2015: Cellular Physiology and Biochemistry
N Tugba Durlu-Kandilci, Merve Denizalti, Inci Sahin-Erdemli
Aging alters bladder functions where a decrease in filling, storage and emptying is observed. These changes cause urinary incontinence, especially in women. The aim of this study is to examine how aging affects the intracellular calcium movements due to agonist-induced contractions in permeabilized female rat bladder. Urinary bladder isolated from young and old female Sprague-Dawley rats were used. Small detrusor strips were permeabilized with β-escin. The contractile responses induced with agonists were compared between young and old groups...
August 2015: Age (2005-)
Roman Franiczek, Michał Gleńsk, Barbara Krzyżanowska, Maciej Włodarczyk
Aescin (escin) derived from the seeds of horse chestnut (Aesculus hippocastanum L.) is a natural mixture of triterpene saponins exhibiting a wide variety of pharmacological properties, including antiinflammatory, analgesic, and antipyretic activities. However, data concerning antifungal activities of these compounds are limited. This study aims to evaluate the in vitro antifungal susceptibility of Candida glabrata clinical isolates to α-aescin sodium, β-aescin crystalline and β-aescin sodium using the disk diffusion (DD) and broth microdilution (BMD) methods...
November 2015: Medical Mycology: Official Publication of the International Society for Human and Animal Mycology
Gülşen Akalin Çiftçi, Arzu Işcan, Mehtap Kutlu
Aesculus hippocastanum (the horse chestnut) seed extract has a wide variety of biochemical and pharmacological effects including anti-inflammatory, antianalgesic, and antipyretic activities. The main active compound of this plant is escin. It is known that several medicinal herbs with anti-inflammatory properties have been found to have a role in the prevention and treatment of cancer. In the present study, the cytotoxic effects of escin in the C6 glioma and A549 cell lines were analyzed by MTT. Apoptotic effects of escin on both cell lines were evaluated by Annexin V binding capacity with flow cytometric analysis...
October 2015: Cytotechnology
J Vašková, A Fejerčáková, G Mojžišová, L Vaško, P Patlevič
OBJECTIVE: Antioxidant, anti-inflammatory and venoconstrictor properties have been attributed to extracts from Aesculus hippocastanum. These unusual and diverse properties may be possibly basically linked with ability to scavenge free radicals. MATERIALS AND METHODS: The scavenging capacity of dry horse chestnut extract of and escin have been investigated in vitro against superoxide anion radicals, hydroxyl radicals, nitrites and peroxynitrite. RESULTS: In general, the activity of the whole extract against superoxide radicals did not exceed 15% at pH 7...
2015: European Review for Medical and Pharmacological Sciences
Katarzyna Filip, Grzegorz Grynkiewicz, Mariusz Gruza, Kamil Jatczak, Bogdan Zagrodzki
Escin, a complex mixture of pentacyclic triterpene saponins obtained from horse chestnut seeds extract (HCSE; Aesculus hippocastanum L.), constitutes a traditional herbal active substance of preparations (drugs) used for a treatment of chronic venous insufficiency and capillary blood vessel leakage. A new approach to exploitation of pharmacological potential of this saponin complex has been recently proposed, in which the β-escin mixture is perceived as a source of a hitherto unavailable raw material, pentacyclic triterpene aglycone-protoescigenin...
November 2014: Acta Poloniae Pharmaceutica
Gui-Li Huang, Dong-Yan Shen, Cheng-Fu Cai, Qiu-Yan Zhang, Hong-Yue Ren, Qing-Xi Chen
AIM: To develop a safe and effective agent for cholangiocarcinoma (CCA) chemotherapy. METHODS: A drug combination experiment was conducted to determine the effects of β-escin in combination with chemotherapy on CCA cells. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay was performed to determine the effects of β-escin and common chemotherapeutics on the proliferation of human CCA cells (QBC939, Sk-ChA-1, and MZ-ChA-1). Immunocytochemistry was used to detect the expression of P-glycoprotein (P-gp) protein...
January 28, 2015: World Journal of Gastroenterology: WJG
Fenglan Zhang, Xuejing Man, Huajun Yu, Limei Liu, Yuanbin Li
Previous studies have shown that escin possesses glucocorticoid (GC)‑like anti‑edematous and anti‑inflammatory effects. The present study was designed to investigate whether escin exhibits synergistic protective effects against blood‑retinal barrier (BRB) breakdown when combined with GC in an in vitro monolayer BRB model, based on retinal pigment epithelial (RPE) cells and human umbilical vein endothelial cells (HUVECs). The results showed that low concentrations of escin and triamcinolone acetonide (TA) administered separately did not affect BRB trans‑endothelial (epithelium) resistance (TEER)...
February 2015: Molecular Medicine Reports
Xiu-Jun Wu, Xiang-Yong Cui, Lian-tian Tian, Feng Gao, Xin Guan, Jing-Kai Gu
ETHNOPHARMACOLOGICAL RELEVANCE: Escin, a natural mixture of triterpene saponins, is commonly utilized for the treatment of chronic venous insufficiency, hemorrhoids, inflammation and edema. Escin Ia is the chief active ingredient in escin and plays key role in mediating its pharmacological effects. Adequate pharmacokinetic data are essential for proper application of escin agent in clinical practice. However, pharmacokinetic properties of escin Ia are still poorly understood and this conflicts with the growing use of escin agent over the years...
October 28, 2014: Journal of Ethnopharmacology
Tian Wang, Shanshan Zhao, Yucun Wang, Yujiao Yang, Le Yao, Liuxiang Chu, Hanhan Du, Fenghua Fu
Escin, a natural mixture of triterpenoid saponin isolated from the seed of the horse chestnut, is reported to have a potent antiulcer activity against ethanol-induced gastric mucosal lesions. This study investigated the possible mechanisms underlying the gastroprotective effect of escin against indomethacin-induced gastric ulcer in mice. Gastric ulceration was induced by a single intragastric administration of indomethacin (18 mg/kg). The mice underwent intragastric treatment with escin at doses of 0.45, 0...
December 2014: Toxicology Mechanisms and Methods
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