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ursolic acid

Yongzhi Chang, Shuxi Zhou, Enqin Li, Wenfeng Zhao, Yanpeng Ji, Xiaoan Wen, Hongbin Sun, Haoliang Yuan
Cholesteryl Ester Transfer Protein (CETP) is an important therapeutic target for the treatment of atherosclerotic cardiovascular disease. Our molecular modeling study revealed that pentacyclic triterpenoid compounds could mimic the protein-ligand interactions of the endogenous ligand cholesteryl ester (CE) by occupying its binding site. Alignment of the docking conformations of oleanolic acid (OA), ursolic acid (UA) and the crystal conformations of known CETP inhibitor Torcetrapib in the active site proposed the applicability of fragment-based drug design (FBDD) approaches in this study...
September 30, 2016: European Journal of Medicinal Chemistry
Dan Xu, Ying Lyu, Xiaowen Chen, Xiaoyu Zhu, Jinqiu Feng, Yajun Xu
Fructus ligustri Lucidi (FLL) is the fruit of Ligustrum lucidum Ait and a traditional Chinese medicine, primarily known for its role in osteoporosis prevention and treatment. The present study aimed to elucidate the effect and underlying mechanism of action of ethanol extract of FLL on osteoclast differentiation and bone resorption, and to identify the active compounds within it. RAW264.7 murine monocyte/macrophage cells were stimulated with the receptor activator of nuclear factor κB ligand (RANKL) to induce osteoclast differentiation in vitro...
October 13, 2016: Molecular Medicine Reports
Hui Ding, Handong Wang, Lin Zhu, Wuting Wei
Previous studies have indicated oxidative stress and inflammatory injury as significant contributors to the secondary damage associated with traumatic brain injury (TBI). Ursolic acid (UA) has been demonstrated to exert anti-oxidative and anti-inflammatory effects on cerebral ischemia by activating the nuclear factor-erythroid 2-related factor 2 (Nrf2) pathway. However, the effects of UA on TBI remain unclear. The aim of this study is to evaluate the potential roles of UA in the activation of the Nrf2 pathway using an experimental TBI model and the underlying mechanism...
October 12, 2016: Neurochemical Research
Jian-Li Gao, Yan-Mei Shui, Wei Jiang, En-Yi Huang, Qi-Yang Shou, Xin Ji, Bai-Cheng He, Gui-Yuan Lv, Tong-Chuan He
Hypoxic in the tumor mass is leading to the myeloproliferative-like disease (leukemoid reaction) and anemia of body, which characterized by strong extensive extramedullary hematopoiesis (EMH) in spleen. As the key transcription factor of hypoxia, hypoxia-inducible factor-1 (HIF-1) activates the expression of genes essential for EMH processes including enhanced blood cell production and angiogenesis. We found ursolic acid (UA), a natural pentacyclic triterpenoid carboxylic acid, inhibited growth of breast cancer both in vivo and in vitro...
September 30, 2016: Oncotarget
Hui Teng, Lei Chen, Hongbo Song
Agrimonia pilosa Ledeb (AP) has already been applied in practice for the treatment of different disorders and is available to access without the provision of a medical prescription. The present study aims at investigating the effect of bioactive compounds isolated from AP on the improvement of insulin resistance, figuring out the mechanism in insulin-responsive cell lines. Five compounds were isolated from AP using column chromatography, including agrimonolide (K1), desmethylagrimonolide (K2), tormentic acid (K3), ursolic acid (K4), and quercetin (K5)...
October 12, 2016: Food & Function
Wen-Tao Gai, Da-Peng Yu, Xin-Sheng Wang, Pei-Tao Wang
Ursolic acid is a type of pentacyclic triterpene compound with multiple pharmacological activities including cancer resistance, protection from liver injury, antisepsis, anti-inflammation and antiviral activity. The present study aimed to investigate the anticancer effect of ursolic acid. Ursolic acid activates cell apoptosis and its pro-apoptotic mechanism remains to be fully elucidated. Cell Counting kit-8 assays, flow cytometric analysis and analysis of caspase-3 and caspase-9 activity were used to estimate the anticancer effect of ursolic acid on DU145 prostate cancer cells...
October 2016: Oncology Letters
Giancarlo Verardo, Andrea Gorassini, Donata Ricci, Daniele Fraternale
INTRODUCTION: Very rarely fruit pulp has been used in in vitro culture to produce secondary metabolites useful in promoting health. OBJECTIVES: The aims of this work were the study of the best conditions to obtain the callus cultures from the pulp of two varieties of apples, Golden Delicious (GD) and "Mela Rosa Marchigiana" (MRM), and the quali-quantitative analysis of secondary metabolites produced by the two in vitro callus cultures. METHODOLOGY: Callus was induced on both Murashige and Skoog and Gamborg B5 media containing various combinations of supplements...
September 30, 2016: Phytochemical Analysis: PCA
Qiao Tang, Yajun Liu, Tao Li, Xiang Yang, Guirong Zheng, Hongning Chen, Lee Jia, Jingwei Shao
Metastasis currently remains the predominant cause of breast carcinoma treatment failure. The effective targeting of metastasis-related-pathways in cancer holds promise for a new generation of therapeutics. In this study, we developed an novel Asp-UA conjugate, which was composed of classical "old drug" aspirin and low toxicity natural product ursolic acid for targeting breast cancer metastasis. Our results showed that Asp-UA could attenuate the adhesion, migration and invasion of breast cancer MCF-7 and MDA-MB-231 cells in a more safe and effective manner in vitro...
September 24, 2016: Oncotarget
Emma Maldonado, Leonel Galicia, Ma Isabel Chávez, Simón Hernández-Ortega
A series of neo-clerodane-type diterpenoids were isolated from the aerial parts of Salvia filipes, including the new compounds 4-epi-polystachyne A (1), salvifilines A (3), C (7), and D (8), and salvifiline B, which was isolated as the 15-O-methyl derivatives 4/5. In addition, the five known diterpenoids (2, 9-12), together with ursolic, oleanolic, and betulinic acids, and the flavone eupatorin were also isolated. The structures were determined by analysis of their spectroscopic data, mainly 1D and 2D NMR. The structure of salvifiline D was confirmed by X-ray analysis...
September 28, 2016: Journal of Natural Products
Anna M Mancha-Ramirez, Thomas J Slaga
Chronic diseases pose a worldwide problem and are only continuing to increase in incidence. Two major factors contributing to the increased incidence in chronic disease are a lack of physical activity and poor diet. As the link between diet and lifestyle and the increased incidence of chronic disease has been well established in the literature, novel preventive, and therapeutic methods should be aimed at naturally derived compounds such as ursolic acid (UA), the focus of this chapter. As chronic diseases, obesity and cancer share the common thread of inflammation and dysregulation of many related pathways, the focus here will be on these two chronic diseases...
2016: Advances in Experimental Medicine and Biology
Ran-Xi Zhang, Yang Li, Dong-Dong Tian, Yang Liu, Wu Nian, Xiang Zou, Qian-Zhao Chen, Lin-Yun Zhou, Zhong-Liang Deng, Bai-Cheng He
Although multiple chemotherapeutic agents have been used for osteosarcoma (OS) treatment, their mechanisms need further study. Ursolic acid (UA), a pentacyclic triterpenoid, can reduce cell proliferation and induce apoptosis in various cancer cells, such as OS. However, the exact mechanism underlying this function remains unclear. In this study, we investigated the anti‑proliferative effect of UA in human OS 143B cells and dissected the possible molecular mechanism underlying this effect. We demonstrated that UA can reduce cell proliferation, induce apoptosis and arrest cell cycle in 143B cells, as well as inhibit OS tumor growth in a mouse xenograft model...
September 21, 2016: International Journal of Oncology
Ze Lin, Jikai Jiang, Xiao-Shan Liu
Ursolic acid (UA) is a promising natural compound for cancer prevention and therapy. We previously reported that UA induced apoptosis in CML-derived K562 cells. Here we show that the apoptotic process is accompanied by down-regulation of Bcl-xL and Mcl-1 expression and dephosphorylation of Bad. These events are associated with Stat5 inhibition, which is partially mediated through elevated expression of transcriptional repressor Gfi-1. Gfi-1 knockdown using siRNA abrogates the ability of UA to decrease Stat5b expression and attenuates apoptosis induction by UA...
2016: Scientific Reports
Vijaya, Arun K Yadav
A large number of medicinal plants are used as herbal remedy for the treatment of helminthic diseases in the developing countries, however, far too little attention has been paid to assess the anthelmintic potentials of chemical compounds that are present in these plants. This study was carried out to assess the in vitro anthelmintic effects of biochanin A, ursolic acid, betulinic acid and beta-sitosterol which are the major phytochemicals of Trifolium repens, Houttuynia cordata and Lasia spinosa, the traditionally used anthelmintic plants of Northeast India...
September 2016: Journal of Parasitic Diseases: Official Organ of the Indian Society for Parasitology
Jian-Zhen Shan, Yan-Yan Xuan, Qi Zhang, Jian-Jin Huang
OBJECTIVE: To explore the efficacy of ursolic acid in sensitizing colon cancer cells to chemotherapy under hypoxia and its underlying mechanisms. METHODS: Three colon cancer cell lines (RKO, LoVo, and SW480) were used as in vitro models. 5-Fluorouracil (5-FU) and oxaliplatin were used as chemotherapeutic drugs. Cell viability and apoptosis were tested to evaluate the sensitivity of colon cancer cells to chemotherapy. The transcription and expression levels of hypoxia-inducible factor-1α (HIF-1α), multidrug resistance gene 1 (MDR1), and vascular endothelial growth factors (VEGF) were assessed by quantitative real-time polymerase chain reaction (qRT-PCR) and immunoblotting...
September 2016: Journal of Zhejiang University. Science. B
Hongbo Xie, Jie Wu, Dan Liu, Mingyi Liu, Hong Zhang, Shibo Huang, Yuqing Xiong, Chunhua Xia
1. Ursolic acid (UA) and oleanolic acid (OA) may have important activity relevant to health and disease prevention. Thus, we studied the activity of UA and OA on UDP-glucuronosyltransferases (UGTs) and used trifluoperazine as a probe substrate to test UGT1A4 activity. Recombinant UGT-catalyzed 4-methylumbelliferone (4-MU) glucuronidation was used as a probe reaction for other UGT isoforms. 2. UA and OA inhibited UGT1A3 and UGT1A4 activity but did not inhibit other tested UGT isoforms. 3. UA-mediated inhibition of UGT1A3 catalyzed 4-MU-β-D-glucuronidation was via competitive inhibition (IC50 0...
September 7, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Shin-Hye Chung, Soha Cho, Kyungsun Kim, Bum-Soon Lim, Sug-Joon Ahn
OBJECTIVE: To compare the antimicrobial and physical properties of experimental primers containing chlorhexidine (CHX) or ursolic acid (UA) with a commercial primer. MATERIALS AND METHODS: Two antibacterial agents, 3 mg each of CHX and UA were incorporated respectively into 1 ml of Transbond XT primer (TX) to form antibacterial primers, TX-CHX and TX-UA. The antimicrobial activity of the three primers (TX, TX-CHX, and TX-UA) against Streptococcus mutans in both planktonic and biofilm phases was analyzed by determining minimum inhibitory and bactericidal concentrations and by performing growth and biofilm assays...
September 6, 2016: Angle Orthodontist
Prasant Nahak, Gourab Karmakar, Priyam Chettri, Biplab Roy, Pritam Guha, Shila Elizabeth Besra, Anjana Soren, Alexey G Bykov, Alexander V Akentiev, Boris A Noskov, Amiya Kumar Panda
The impact of saturation and unsaturation in the fatty acyl hydrocarbon chain on the physicochemical properties of nanostructured lipid carriers (NLCs) was investigated to develop novel delivery systems loaded with an anticancer drug, ursolic acid (UA). Aqueous NLC dispersions were prepared by a high-pressure homogenization-ultrasonication technique with Tween 80 as a stabilizer. Mutual miscibility of the components at the air-water interface was assessed by surface pressure-area measurements, where attractive interactions were recorded between the lipid mixtures and UA, irrespective of the extent of saturation or unsaturation in fatty acyl chains...
September 27, 2016: Langmuir: the ACS Journal of Surfaces and Colloids
Jun Peng, Xingfeng Ren, Tianbiao Lan, Yan Chen, Ziyun Shao, Cheng Yang
Ursolic acid, a pentacyclic triterpene compound with low toxicity and easy availability, has a variety of biological activities, including antitumor, antioxidant, antihepatitis, anti‑inflammatory and antibacterial effects. The present study aimed to investigate the renoprotective effects of ursolic acid on ischemia/reperfusion‑induced acute kidney injury (I/R‑IAKI) in rats associated with its antioxidant and anti‑inflammatory effects, as well as interference with the signal transducer and activator of transcription (STAT)3/nuclear factor (NF)‑κB signaling pathway...
October 2016: Molecular Medicine Reports
Emmanuel Fajardo-Sánchez, Vicente Galiano, José Villalaín
Ursolic acid (URS), an ursane-representative bioactive pentacyclic triterpene, is a plant secondary metabolite presenting a great number of pharmacological beneficial properties. Due to the prominent hydrophobic character of URS and its high phospholipid/water partition coefficient, some of its possible effects on biological systems might be related to its capacity to interact with and locate into the membrane as well as interact specifically with its components. In this work, we have studied the location and orientation of URS in the membrane by molecular dynamics simulations...
August 28, 2016: Journal of Biomolecular Structure & Dynamics
Dongyu Li, Daoyuan Ren, Yiyang Luo, Xingbin Yang
This study was designed to investigate the preventive effect of ursolic acid (UA), a plant-based pentacyclic triterpenoid carboxyl acid, against vascular endothelial damage and liver oxidative injury in the mice fed with 3% dietary high choline (HC) water. Mice fed 3% HC water for 8 weeks significantly displayed liver oxidative stress and vascular endothelial dysfunction (p < 0.01). Furthermore, continuous administration of UA at 400 and 800 mg/kg bw in HC-fed mice could significantly inhibit the HC-induced elevation of serum total cholesterol, total triglyceride, low density lipoprotein-cholesterol, endothelin 1 and thromboxane A2 levels as well as alanine aminotransferase and aspartate aminotransferase activities, while the HC-induced decline of serum high density lipoprotein-cholesterol, endothelial nitric oxide synthase, nitric oxide and prostaglandin I2 levels could be markedly elevated following the treatment (p < 0...
October 25, 2016: Chemico-biological Interactions
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