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ursolic acid

Edgar Isaac Rojas-Bedolla, Jorge Luis Gutiérrez-Pérez, Mario Iván Arenas-López, Marco Martin González-Chávez, Juan Ramón Zapata-Morales, Claudia Leticia Mendoza-Macías, Candy Carranza-Álvarez, Juan José Maldonado-Miranda, Martha Alicia Deveze-Álvarez, Angel Josabad Alonso-Castro
ETHNOPHARMACOLOGICAL RELEVANCE: Celtis pallida Torr (Cannabaceae) is employed as a folk medicine for the treatment of inflammation, pain, skin infections, and diarrhea, among other diseases. AIM OF THE STUDY: The purpose of this work was to assess the chemical composition, the in vitro and in vivo toxicity, the antimicrobial, anti-inflammatory, antidiarrheal, antinociceptive, locomotor, and sedative effects of an ethanolic extract obtained from Celtis pallida aerial parts (CPE)...
March 12, 2018: Journal of Ethnopharmacology
Dorota Nieoczym, Katarzyna Socała, Piotr Wlaź
Ursolic acid (UA) is a plant derived compound which is also a component of the standard human diet. It possesses a wide range of pharmacological properties, i.e., antioxidant, anti-inflammatory, antimicrobial and antitumor, which have been used in folk medicine for centuries. Moreover, influence of UA on central nervous system-related processes, i.e., pain, anxiety and depression, was proved in experimental studies. UA also revealed anticonvulsant properties in animal models of epilepsy and seizures. The aim of the present study was to investigate the influence of UA on seizure thresholds in three acute seizure models in mice, i...
March 14, 2018: Neurochemical Research
Yanxue Liu, Kefeng Liu, Xiaomin Li, Shangzhen Xiao, Dan Zheng, Pengbo Zhu, Chunxiao Li, Jing Liu, Jing He, Jiandu Lei, Luying Wang
The application of non-toxic carriers to increase drug loading, multi-drug delivery, and extremely small size of nano-drugs to construct a tremendous transmission system is the goal for all researchers to be pursued. The proposal of natural pectin nano-platform for delivery of multiple drugs is critical for biomedical research, especially a particle size of below 100nm with high yield. Here we design a new core-shell structure pectin-eight-arm polyethylene glycol-ursolic acid/hydrooxycampothecin nanoparticle (Pec-8PUH NPs) through a special self-assembly method for stabilizing and dispersing particles, improving water-solubility, and achieving drug controlled release...
May 1, 2018: Materials Science & Engineering. C, Materials for Biological Applications
Jesus Salinas-Casado, Santiago Méndez-Rubio, Manuel Esteban-Fuertes, Antonio Gómez-Rodríguez, Miguel Vírseda-Chamorro, Marcos Luján-Galán, Grupo Rituman
OBJECTIVE: To compare the efficacy and safety of dietary supplement "Manosar®" composed of D-mannose (2 g), 24 h prolonged release, associated with Proanthocyanidin (PAC) (140 mg), ursolic acid (7.98 mg), A, C, and D vitamins and the oligoelement zinc, versus 240 mg of PAC in recurrent urinary tract infections (UTI), for a designed follow-up of 24 weeks, in women. METHODS: A multicenter randomized experimental double-blind study was carried out. The study was approved by review board of "Complejo Hospitalario de Toledo" (Spain), and all patients gave informed consent...
March 2018: Archivos Españoles de Urología
Thomas Theis, Anmol Singh Johal, Maciej Kabat, Sayantani Basak, Melitta Schachner
Glycosylation fine-tunes signal transduction of adhesion molecules during neural development and supports synaptic plasticity and repair after injury in the adult nervous system. One abundantly expressed neural glycan is LewisX (LeX). Although it is known that its expression starts at the formation of the neural tube during the second embryonic week in the mouse and peaks during the first postnatal week, its functional relevance is only rudimentarily understood. To gain better insights into the functions of this glycan, we identified small organic compounds that mimic structurally and functionally this glycan glycosidically linked to several neural adhesion molecules...
March 8, 2018: Molecular Neurobiology
C M de Almeida, W L O da Rosa, C T W Meereis, S M de Almeida, J S Ribeiro, A F da Silva, Rafael Guerra Lund
AIMS: The purpose of this study was to evaluate the efficacy of orthodontic bonding systems containing different antimicrobial agents, as well as the influence of antimicrobial agent incorporation in the bonding properties of these materials. METHODS: Eight databases were searched: PubMed (Medline), Web of Science, Scopus, Lilacs, Ibecs, BBO, Scielo and Google Scholar. Any study that evaluated antimicrobial activity in experimental or commercial orthodontic bonding systems was included...
March 5, 2018: Journal of Orthodontics
Maocai Zhai, Junyi Guo, Haiyan Ma, Wei Shi, David Jou, Dan Yan, Tianshu Liu, Jingwen Tao, Jialin Duan, Yina Wang, Sheng Li, Jiagao Lv, Chenglong Li, Jiayuh Lin, Cuntai Zhang, Li Lin
BACKGROUND AND AIMS: Abdominal aortic aneurysms (AAA) is a chronic inflammatory disease in which signal transducer and activator of transcription 3 (STAT3), and disintegrin and metalloproteinase 17 (ADAM17) play important roles. However, it remains unclear whether ursolic acid (UA), a natural pentacyclic triterpenoid carboxylic acid, can have an impact on STAT3 and ADAM17 and hence influence the formation of AAA. The objective of this study was to characterize the potential effect of UA on the pathogenesis of AAA and on STAT3 and ADAM17...
February 15, 2018: Atherosclerosis
Y Yoshimasu, T Ikeda, N Sakai, A Yagi, S Hirayama, Y Morinaga, S Furukawa, R Nakao
Propolis, a resinous substance produced by bees, is used as a folk medicine for treatment of periodontal diseases. However, its mode of the action and the compounds responsible for its activities remain obscure. In the present study, we comprehensively investigated the antibacterial activities of ethanol-extracted propolis (EEP) and EEP-derived compounds toward Porphyromonas gingivalis, a keystone pathogen for periodontal diseases. Broth microdilution and agar dilution assays were used to determine the minimum inhibitory concentrations of EEP against a range of oral bacterial species, of which P...
February 1, 2018: Journal of Dental Research
Víctor M Vergara Martínez, Samuel E Estrada-Soto, José de Jesús Arellano-García, Julio C Rivera-Leyva, Patricia Castillo-España, Angélica Flores Flores, Alexandre T Cardoso-Taketa, Irene Perea-Arango
Background: The production of triterpenes from plants for pharmacological purposes varies in concentration, due to genetic and environmental factors. In vitro culture enables the control and increase of these bioactive molecules. Objective: To evaluate the effect of plant growth regulators and elicitors in the induction of calli and the production of ursolic acid (UA) and oleanolic acid (OA) in Lepechinia caulescens . Materials and Methods: Leaf explants were exposed for the induction of calli at different concentrations and combinations of 2,4-dichlorophenoxyacetic acid (2,4-D) and 6-benzylaminopurine (BAP)...
January 2018: Pharmacognosy Magazine
Vijaya, Arun K Yadav, S Gogoi
Pinworm infections are one of the common problems in laboratory rodents and man. At present there are only few drugs against intestinal helminths, and new drugs are urgently needed to cope up any future risk of drug resistance. Interest in plant secondary metabolites (PSMs) has risen considerably in the recent years for the discovery and development of new drugs. In the present study, we explored the in vitro and in vivo anthelmintic potentials of two pentacyclic triterpenoids, ursolic acid (UA) and betulinic acid (BA), the important PSMs of many medicinal plants, against Syphacia obvelata (Nematoda: Oxyuridae), a common pinworm of mice...
March 2018: Journal of Parasitic Diseases: Official Organ of the Indian Society for Parasitology
Matteo Dal Prà, Davide Carta, Gyorgy Szabadkai, Matteo Suman, Yahima Frión-Herrera, Nicola Paccagnella, Giulia Castellani, Sara De Martin, Maria Grazia Ferlin
Designing novel inverse agonists of NR RORγt still represents a challenge for the pharmaceutical community to develop therapeutics for treating immune diseases. By exploring the structure of NRs natural ligands, the representative arotenoid ligands and RORs specific ligands share some chemical homologies which can be exploited to design a novel molecular structure characterized by a polycyclic core bearing a polar head and a hydrophobic tail. Compound MG 2778 (8), a cyclopenta[a]phenantrene derivative, was identified as lead compound which was chemically modified at position 2 in order to obtain a small library for preliminary SARs...
February 15, 2018: Bioorganic & Medicinal Chemistry
Trong Nghia Ngo, Cong Thin Vo, Nguyen Kim Tuyen Pham, Nhat Minh Phan, Trong Dat Bui, Quoc Luan Ngo, Van Son Dang, Cong Luan Tran, Dinh Tri Mai, Tan Phat Nguyen
One new cycloartane triterpenoid, named markhacanasin C (1), together with three known triterpenoids, oleanolic acid (2), ursolic acid (3) and 6β,19α-dihydroxyursolic acid (4) were isolated by various chromatographic methods from the most cytotoxic fraction of the ethyl acetate extract of Markhamia stipulata var. canaense V.S. Dang leaves. Among them, 4 was reported for the first time from the genus Markhamia, while 2 and 3 were found for the first time from this species. Their structures were elucidated by IR, UV, HR-ESI-MS and NMR experiments...
February 22, 2018: Natural Product Research
Dawei Mu, Gaobiao Zhou, Jianye Li, Bin Su, Heqing Guo
Ursolic acid has various pharmacological activities, and can reduce blood fat as well as having antihepatic, antitumoral, anti-inflammatory and antiviral properties. However, the pro-apoptotic mechanism by which ursolic acid influences human prostate cancer requires additional study. The aim of the present study was to assess whether ursolic acid activates the apoptosis of prostate cancer and to investigate the mechanism by which the Rho-associated protein kinase 1 (ROCK1)/phosphatase and tensin homolog (PTEN) signaling pathway performs a role in ursolic acid-mediated cofilin-1 to induce apoptosis in human prostate cancer...
March 2018: Oncology Letters
Wei Li, Hongxiu Zhang, Mingxiu Nie, Wei Wang, Zongtao Liu, Ceshi Chen, Haijun Chen, Rong Liu, Zulqarnain Baloch, Ke Ma
The present study investigated the anticancer functions of ursolic acid (UA) and its novel derivatives, with a nitrogen-containing heterocyclic scaffold and the privileged fragment at the C-28 position on apoptosis induction, cell proliferation and cell cycle in human BC lines. UA was chemically modified in the present study to increase its antitumor activity and bioavailability. A novel UA derivative, FZU3010, was synthesized using a nitrogen-containing heterocyclic scaffold and a privileged fragment at the C-28 position...
February 2018: Oncology Letters
Er-Min Wang, Qiu-Ling Fan, Yuan Yue, Li Xu
BACKGROUND To investigate the protective effect of ursolic acid (UA) on high glucose (HG)-induced human glomerular mesangial cell injury and to determine whether UA inhibits cell proliferation and reactive oxygen species (ROS) production by suppressing PI3K/Akt/mTOR pathway activation. MATERIAL AND METHODS Human mesangial cells were cultured with normal glucose (NG group), high glucose (HG group), mannitol (mannitol hypertonic control group), or high glucose with different concentrations (0.5, 1.0, and 2.0 mmol/L) of UA (HG+UA groups)...
February 11, 2018: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
Christina N Ramirez, Wenji Li, Chengyue Zhang, Renyi Wu, Shan Su, Chao Wang, Linbo Gao, Ran Yin, Ah-Ng Tony Kong
The citation of the author name "Ah-Ng Tony Kong" in PubMed is not the author's preference. Instead of "Kong AT", the author prefers "Kong AN".
February 6, 2018: AAPS Journal
Ruirui Zhao, Guirong Zheng, Lulu Fan, Zhichun Shen, Kai Jiang, Yan Guo, Jing-Wei Shao
Nanosized drug delivery systems (NDDS) with photothermal therapy (PTT) and photodynamic therapy (PDT) have been extensively exploited to improve the therapeutic performance and bio-safety of chemotherapeutic drugs in cancer. In this work, a carrier-free nanodrug was developed by co-assembly of the anti-cancer agent ursolic acid (UA), an asialoglycoprotein receptor (ASGPR), which can recognize the target molecule lactobionic acid (LA), and the near-infrared (NIR) probe dye indocyanine green (ICG) to form UA-LA-ICG NPs by a simple and green self-assembly approach...
February 5, 2018: Acta Biomaterialia
Lucía López-Hortas, Patricia Pérez-Larrán, María Jesús González-Muñoz, Elena Falqué, Herminia Domínguez
Ursolic acid (UA) is a pentacyclic triterpenoid widely found in herbs, leaves, flowers and fruits; update information on the major natural sources or agro-industrial wastes is presented. Traditional (maceration, Soxhlet and heat reflux) and modern (microwave-, ultrasound-, accelerated solvent- and supercritical fluid) extraction and purification technologies of UA, as well as some patented process, are summarized. The great interest in this bioactive compound is related to the beneficial effects in human health due to antioxidant, antimicrobial, anti-inflammatory, hepatoprotective, immunomodulatory, anti-tumor, chemopreventive, cardioprotective, antihyperlipidemic and hypoglycemic activities, and others...
January 2018: Food Research International
Chao Wang, Limin Shu, Chengyue Zhang, Wenji Li, Renyi Wu, Yue Guo, Yuqing Yang, Ah-Ng Kong
SCOPE: This study aimed to investigate the role of the epigenetic regulator SET domain-containing lysine methyltransferase 7 (Setd7) in regulating the antioxidant Nrf2 pathway in prostate cancer (PCa) cells and examined the effects of two phytochemicals, phenethyl isothiocyanate (PEITC) and ursolic acid (UA). METHODS AND RESULTS: Lentivirus-mediated shRNA knockdown of Setd7 in LNCaP and PC-3 cells decreased the expression of downstream Nrf2 targets, such as NAD(P)H: quinone oxidoreductase 1 (Nqo1) and glutathione S-transferase theta 2 (Gstt2)...
January 30, 2018: Molecular Nutrition & Food Research
Ricardo Guzmán-Ávila, Virginia Flores-Morales, Paolo Paoli, Guido Camici, Juan José Ramírez-Espinosa, Litzia Cerón-Romero, Gabriel Navarrete-Vázquez, Sergio Hidalgo-Figueroa, Maria Yolanda Rios, Rafael Villalobos-Molina, Samuel Estrada-Soto
Hit, Lead & Candidate Discovery Protein tyrosine phosphatase 1B (PTP-1B) has attracted interest as a novel target for the treatment of type 2 diabetes, this because its role in the insulin-signaling pathway as a negative regulator. Thus, the aim of current work was to obtain seven ursolic acid derivatives as potential antidiabetic agents with PTP-1B inhibition as main mechanism of action. Furthermore, derivatives 1-7 were submitted in vitro to enzymatic PTP-1B inhibition being 3, 5, and 7 the most active compounds (IC50  = 5...
January 29, 2018: Drug Development Research
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