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https://www.readbyqxmd.com/read/28527823/antiviral-escin-derivatives-from-the-seeds-of-aesculus-turbinata-blume-japanese-horse-chestnut
#1
Ji Won Kim, Thi-Kim-Quy Ha, Hyomoon Cho, Eunhee Kim, Sang Hee Shim, Jun-Li Yang, Won Keun Oh
Porcine epidemic diarrhea virus (PEDV) causes severe diarrhea and high fatality of piglets, influencing the swine industry. Japanese horse chestnut (seed of Aesculus turbinata) contains many saponin mixtures, called escins, and has been used for a long time as a traditional medicinal plant. Structure-activity relationship (SAR) studies on escins have revealed that acylations at C-21 and C-22 with angeloyl or tigloyl groups were important for their cytotoxic effects. However, the strong cytotoxicity of escins makes them hard to utilize for other diseases and to develop as nutraceuticals...
May 8, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28526517/regulation-of-rhoa-rock-and-sustained-arterial-contraction-by-low-cytosolic-ca-2-levels-during-prolonged-depolarization-of-arterial-smooth-muscle
#2
Cristina Porras-González, Antonio Ordóñez, Antonio Castellano, Juan Ureña
The role of L-type Ca(2+) channels (LTCCs) and RhoA/Rho kinase (ROCK) on depolarization-induced sustained arterial contraction lasting several minutes is already known. However, in vivo, vascular smooth muscle cells can be depolarized for longer periods, inducing substantial inactivation of LTCCs and markedly reducing Ca(2+) influx into the myocytes. We have examined, in femoral arterial rings, the role of LTCCs and RhoA/ROCK during long-lasting depolarization. Our results reveal a new vasoreactive response after 20-30min of depolarization in 2...
May 16, 2017: Vascular Pharmacology
https://www.readbyqxmd.com/read/28378396/the-positive-clinical-therapeutically-effects-of-escin-on-advanced-thyroid-cancer
#3
Jin-Yu Mei, Ming-Jun Zhang, Yuan-Yuan Wang, Ye-Hai Liu
The incidences of thyroid cancer keep rising worldwide over the past few decades. Although most thyroid cancers are indolent and highly curable, the treatment for advanced thyroid cancer remains challengeable in clinical practice. We performed two separate cohorts to evaluate the safety and efficiency of Escin in patients with advanced thyroid cancer . In cohort 1, 120 patients were divided into four groups equally and were administrated with placebo or different dosages of Escin. The pharmacokinetics of Escin and the side effects were evaluated...
May 2017: Cancer Medicine
https://www.readbyqxmd.com/read/28122160/physicochemical-properties-antioxidant-and-anti-proliferative-capacities-of-dried-leaf-and-its-extract-from-xao-tam-phan-paramignya-trimera
#4
Van Tang Nguyen, Jennette A Sakoff, Christopher J Scarlett
Xao tam phan (P. trimera) has been used for the treatment of cancer and cancer-like aliments. Among different parts of P. trimera plant, leaf is considered as a residual part after harvesting of the root. This study aimed to determine the physiochemical properties, antioxidant and anti-proliferative capacities of P. trimera leaf (PTL) using microwave drying for the preparation of dry sample; methanol and microwave-assisted extraction for the preparation of crude extract; and freeze drying for the preparation of powdered extract...
January 25, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28112272/endothelia-targeting-protection-by-escin-in-decompression-sickness-rats
#5
Kun Zhang, Zhongxin Jiang, Xiaowei Ning, Xuhua Yu, Jiajun Xu, Peter Buzzacott, Weigang Xu
Endothelial dysfunction is involved in the pathogenesis of decompression sickness (DCS) and contributes substantively to subsequent inflammatory responses. Escin, the main active compound in horse chestnut seed extract, is well known for its endothelial protection and anti-inflammatory properties. This study aimed to investigate the potential protection of escin against DCS in rats. Escin was administered orally to adult male rats for 7 d (1.8 mg/kg/day) before a simulated air dive. After decompression, signs of DCS were monitored, and blood and pulmonary tissue were sampled for the detection of endothelia related indices...
January 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28075477/escin-induces-apoptosis-in-human-renal-cancer-cells-through-g2-m-arrest-and-reactive-oxygen-species-modulated-mitochondrial-pathways
#6
Sheau-Yun Yuan, Chen-Li Cheng, Shian-Shiang Wang, Hao-Chung Ho, Kun-Yuan Chiu, Chuan-Shu Chen, Cheng-Che Chen, Ming-Yuh Shiau, Yen-Chuan Ou
Escin, a natural pentacyclic triterpenoid compound, exhibits antitumor effects on various types of human cancer cells, but its effect on human renal cancer cells has not been fully elucidated. In the present study, we demonstrated that escin elicits cytotoxic effects on human renal cancer cells (786-O and Caki-1) in a dose-dependent manner, as determined by MTT assay. Escin induced G2/M arrest, and then increased the sub-G1 population, Annexin V binding, activation of caspase-9/-3, cleavage of poly(ADP-ribose) polymerase (PARP) and Bax protein...
February 2017: Oncology Reports
https://www.readbyqxmd.com/read/28029227/physicochemical-antioxidant-and-cytotoxic-properties-of-xao-tam-phan-paramignya-trimera-root-extract-and-its-fractions
#7
Van Tang Nguyen, Jennette A Sakoff, Christopher J Scarlett
Xao tam phan (Paramignya trimera (Oliv.) Guillaum) has been used as a medicinal plant for cancer prevention and treatment in recent years. The objective of this study was to determine the physicochemical, antioxidant, and cytotoxic properties of crude P. trimera root (PTR) extract and its fractions using MeOH as a solvent and microwave-assisted extraction as an advanced technique for preparation of the PTR extract. The results showed that the PTR extract had high contents of saponins, phenolics, flavonoids, and proanthocyanidins (7731...
April 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/27727329/molecular-mechanism-for-cellular-response-to-%C3%AE-escin-and-its-therapeutic-implications
#8
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
https://www.readbyqxmd.com/read/27589691/%C3%AE-escin-selectively-targets-the-glioblastoma-initiating-cell-population-and-reduces-cell-viability
#9
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...
October 11, 2016: Oncotarget
https://www.readbyqxmd.com/read/27104944/discovery-of-clinically-approved-agents-that-promote-suppression-of-cystic-fibrosis-transmembrane-conductance-regulator-nonsense-mutations
#10
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 (CF). Several 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 patients with CF with PTCs. METHODS: Two independent screens, firefly luciferase and CFTR-mediated transepithelial chloride conductance assay, were performed on a library of 1,600 clinically approved compounds using fisher rat thyroid cells stably transfected with stop codons...
November 1, 2016: American Journal of Respiratory and Critical Care Medicine
https://www.readbyqxmd.com/read/27008697/escin-ia-suppresses-the-metastasis-of-triple-negative-breast-cancer-by-inhibiting-epithelial-mesenchymal-transition-via-down-regulating-loxl2-expression
#11
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
https://www.readbyqxmd.com/read/26824290/antiproliferative-effect-of-%C3%AE-escin-an-in-vitro-study
#12
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
https://www.readbyqxmd.com/read/26819933/determination-of-four-major-saponins-in-skin-and-endosperm-of-seeds-of-horse-chestnut-aesculus-hippocastanum-l-using-high-performance-liquid-chromatography-with-positive-confirmation-by-thin-layer-chromatography
#13
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
https://www.readbyqxmd.com/read/26773773/combined-treatment-with-low-dose-prednisone-and-escin-improves-the-anti-arthritic-effect-in-experimental-arthritis
#14
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
https://www.readbyqxmd.com/read/26505797/escin-activates-akt-nrf2-signaling-to-protect-retinal-pigment-epithelium-cells-from-oxidative-stress
#15
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
https://www.readbyqxmd.com/read/26199634/oral-administration-of-escin-inhibits-acute-inflammation-and-reduces-intestinal-mucosal-injury-in-animal-models
#16
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
https://www.readbyqxmd.com/read/26159746/reversal-of-il-13-induced-inflammation-and-ca-2-sensitivity-by-resolvin-and-mag-dha-in-association-with-asa-in-human-bronchi
#17
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
https://www.readbyqxmd.com/read/26159678/escin-increases-the-survival-rate-of-lps-induced-septic-mice-through-inhibition-of-hmgb1-release-from-macrophages
#18
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
https://www.readbyqxmd.com/read/26153091/aging-changes-agonist-induced-contractile-responses-in-permeabilized-rat-bladder
#19
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-)
https://www.readbyqxmd.com/read/26092104/%C3%AE-aescin-at-subinhibitory-concentration-sub-mic-enhances-susceptibility-of-candida-glabrata-clinical-isolates-to-nystatin
#20
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
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