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https://www.readbyqxmd.com/read/29205802/a-two-center-assessor-blinded-prospective-trial-evaluating-the-efficacy-of-a-novel-hypertonic-draining-cream-for-cellulite-reduction-a-clinical-and-instrumental-antera-3d-cs-assessment
#1
Mario Puviani, Federica Tovecci, Massimo Milani
INTRODUCTION: Gynoid lipodystrophy, also known as cellulite, is a very common skin alteration representing mainly a cosmetic problem rather than a real disease. An effective treatment of cellulite has not been well established. The initial phase of cellulite is characterized by subdermal tissue edema with interstitial fluids retention. A new hypertonic topical product with draining action (HTC) containing NaCl 13%, escine, caffeine, and beta-sitosterol has been recently developed. A 28-day double-blind placebo-controlled study has shown that this cream is able to reduce thigh circumference and the thickness of adipose tissue...
December 4, 2017: Journal of Cosmetic Dermatology
https://www.readbyqxmd.com/read/29093683/the-amp-dependent-protein-kinase-ampk-activator-a-769662-causes-arterial-relaxation-by-reducing-cytosolic-free-calcium-independently-of-an-increase-in-ampk-phosphorylation
#2
Yi Huang, Corey A Smith, Grace Chen, Bharti Sharma, Amy S Miner, Robert W Barbee, Paul H Ratz
Although recent studies reveal that activation of the metabolic and Ca(2+) sensor AMPK strongly inhibits smooth muscle contraction, there is a paucity of information about the potential linkage between pharmacological AMPK activation and vascular smooth muscle (VSM) contraction regulation. Our aim was to test the general hypothesis that the allosteric AMPK activator A-769662 causes VSM relaxation via inhibition of contractile protein activation, and to specifically determine which activation mechanism(s) is(are) affected...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29022891/escin-induces-caspase-dependent-apoptosis-and-autophagy-through-the-ros-p38-mapk-signalling-pathway-in-human-osteosarcoma-cells-in-vitro-and-in-vivo
#3
Jian Zhu, Wei Yu, Bing Liu, Yitian Wang, Jianlin Shao, Junjie Wang, Kaishun Xia, Chengzhen Liang, Weijing Fang, Chenhe Zhou, Huimin Tao
Osteosarcoma is one of the most malignant neoplasms in adolescents, and it generally develops multidrug resistance. Escin, a natural mixture of triterpene saponins isolated from Aesculus hippocastanum (horse chestnut), has demonstrated potent anti-tumour potential in vitro and in vivo. In the present study, we found that escin inhibited osteosarcoma proliferation in a dose- and time-dependent manner. Additionally, escin-induced apoptosis was evidenced by the increased expression of caspase-related proteins and the formation of apoptotic bodies...
October 12, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28930257/physicochemical-properties-antioxidant-and-cytotoxic-activities-of-crude-extracts-and-fractions-from-phyllanthus-amarus
#4
Van Tang Nguyen, Jennette A Sakoff, Christopher J Scarlett
Background:Phyllanthus amarus (P. amarus) has been used as a medicinal plant for the prevention and treatment of chronic ailments such as diabetes, hepatitis, and cancer. Methods: The physicochemical properties, antioxidant and cytotoxic activities of crude extracts and fractions from P. amarus were determined using spectrophotometric method. Results: The P. amarus methanol (PAM) extract had lower levels of residual moisture (7.40%) and water activity (0.24) and higher contents of saponins, phenolics, flavonoids, and proanthocyanidins (1657...
June 18, 2017: Medicines (Basel, Switzerland)
https://www.readbyqxmd.com/read/28882559/enhancement-of-s1p-induced-contractile-response-in-detrusor-smooth-muscle-of-rats-having-cystitis
#5
Irfan Anjum, Merve Denizalti, Hilmi Burak Kandilci, Nezahat Tugba Durlu-Kandilci, Inci Sahin-Erdemli
Interstitial cystitis is a chronic disease characterized by lower abdominal pain and some nonspecific symptoms including an increase in urinary frequency and urgency. Sphingosine 1-phosphate (S1P) is a bioactive sphingolipid that controls smooth muscle tone via G-protein coupled receptors (S1P1-3 receptors). S1P production is known to take place both in physiological states and some pathological situations, such as in overactive bladder syndrome. The intracellular mechanism of S1P-induced contractile response was investigated in β-escin permeabilized detrusor smooth muscle of rats having cyclophosphamide-induced cystitis...
November 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28804235/management-of-varicose-veins-and-chronic-venous-insufficiency-in-a-comparative-registry-with-nine-venoactive-products-in-comparison-with-stockings
#6
G Belcaro, M Dugall, R Luzzi, M Corsi, A Ledda, A Ricci, L Pellegrini, M R Cesarone, M Hosoi, B M Errichi, U Cornelli, R Cotellese, G Agus, B Feragalli
The aim of this registry study was to compare products used to control symptoms of CVI. Endpoints of the study were microcirculation, effects on volume changes, and symptoms (analogue scale). Pycnogenol, venoruton, troxerutin, the complex diosmin-hesperidin, Antistax, Mirtoselect (bilberry), escin, and the combination Venoruton-Pycnogenol (VE-PY) were compared with compressions. No safety or tolerability problems were observed. At inclusion, measurements in the groups were comparable: 1,051 patients completed the registry...
September 2017: International Journal of Angiology: Official Publication of the International College of Angiology, Inc
https://www.readbyqxmd.com/read/28749143/self-assembly-of-escin-molecules-at-the-air-water-interface-as-studied-by-molecular-dynamics
#7
Sonya Tsibranska, Anela Ivanova, Slavka Tcholakova, Nikolai Denkov
Escin belongs to a large class of natural biosurfactants, called saponins, that are present in more than 500 plant species. Saponins are applied in the pharmaceutical, cosmetics, and food and beverage industries due to their variously expressed bioactivity and surface activity. In particular, escin adsorption layers at the air-water interface exhibit an unusually high surface elastic modulus (>1100 mN/m) and a high surface viscosity (ca. 130 N·s/m). The molecular origin of these unusual surface rheological properties is still unclear...
August 10, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28527823/antiviral-escin-derivatives-from-the-seeds-of-aesculus-turbinata-blume-japanese-horse-chestnut
#8
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...
July 1, 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
#9
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...
August 2017: Vascular Pharmacology
https://www.readbyqxmd.com/read/28378396/the-positive-clinical-therapeutically-effects-of-escin-on-advanced-thyroid-cancer
#10
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
#11
Van Tang Nguyen, Jennette A Sakoff, Christopher J Scarlett
Xao tam phan (Paramignya trimera) has been used for the treatment of cancer and cancer-like aliments. Among different parts of the P. trimera plant, leaf is considered as a residual part after harvesting of the root. This study aimed to determine the physiochemical properties and the antioxidant and anti-proliferative capacities of P. trimera leaf (PTL) using microwave drying for the preparation of dry sample; MeOH and microwave-assisted extraction for the preparation of crude extract; and freeze-drying for the preparation of powdered extract...
June 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28112272/endothelia-targeting-protection-by-escin-in-decompression-sickness-rats
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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