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ursolic acid

Robson Xavier Faria, André Luis Almeida Souza, Barbara Lima, Luis Armando Candido Tietbohl, Caio Pinho Fernandes, Raquel Rodrigues Amaral, Bettina Monika Ruppelt, Marcelo Guerra Santos, Leandro Rocha
Chagas disease is caused by the Trypanosoma cruzi affecting millions of people, and widespread throughout Latin America. This disease exhibits a problematic chemotherapy. Benznidazole, which is the drug currently used as standard treatment, lamentably evokes several adverse reactions. Among other options, natural products have been tested to discover a novel therapeutic drug for this disease. A lot of plants from the Brazilian flora did not contain studies about their biological effects. Restinga de Jurubatiba from Brazil is a sandbank ecosystem poorly studied in relation to plant biological activity...
November 17, 2017: Journal of Bioenergetics and Biomembranes
Maycow Marcos L de Azevedo, Márcia M Cascaes, Giselle Maria S P Guilhon, Eloisa Helena A Andrade, Maria das Graças B Zoghbi, Joyce Kelly R da Silva, Lourivaldo S Santos, Silvia Helena M da Silva
Chemical composition of the methanol extract of Myrciaria floribunda leaves was investigated. The nor-lupane triterpenoids platanic acid and messagenic I acid were identified, along with other known triterpenoids (betulinic aldehyde, ursolic acid acetate and betulinic acid), a new lupane triterpenoid (2α,6α,30-trihydroxybetulinic acid) and the flavonoids catechin, quercetrin and mirycitrin. The structures were determined by spectroscopic methods (NMR, LC-MS, GC-MS). The major isolated compound was betulinic acid...
November 13, 2017: Natural Product Research
Ana B Ramos-Hryb, Mauricio P Cunha, Francis L Pazini, Vicente Lieberknecht, Rui D S Prediger, Manuella P Kaster, Ana Lúcia S Rodrigues
BACKGROUND: Ursolic acid has been shown to display antidepressant-like effects in mice through the modulation of monoaminergic systems. In this study, we sought to investigate the involvement of signaling pathways on the antidepressant-like effects of ursolic acid. METHODS: Mice were treated orally with ursolic acid (0.1mg/kg) and, 45min later they received the followings inhibitors by intracerebroventricular route: H-89 (PKA inhibitor, 1μg/mouse), KN-62 (CAMK-II inhibitor, 1μg/mouse), chelerythrine (PKC inhibitor, 1μg/mouse), U0126 (MEK1/2 inhibitor, 5μg/mouse), PD98059 (MEK1/2 inhibitor, 5μg/mouse), wortmannin (PI3K irreversible inhibitor, 0...
May 24, 2017: Pharmacological Reports: PR
Zhichun Shen, Bowen Li, Yajun Liu, Guirong Zheng, Yan Guo, Ruirui Zhao, Kai Jiang, Lulu Fan, Jingwei Shao
Ursolic acid (UA), a natural triterpene acids, is a promising anti-cancer drug due to its inhibitory effect on tumor growth and metastasis. However, clinical translation of UA is limited by its poor water solubility and low bioavailability. To overcome these problems, herein an amphiphilic self-assembly nanodrug composed of UA, lactobionic acid (LA) and low-polyamidoamine (low-PAMAM) dendrimers is developed. This near-spherical nanodrug with a uniform size (~180nm) demonstrated to have an enhanced cytotoxicity against liver cancer SMMC7721 cells, and could attenuate the migration and adhesion of SMMC7721 cells at non-toxic concentrations by suppressing metastasis-related protein MMP-9 expression...
November 8, 2017: Nanomedicine: Nanotechnology, Biology, and Medicine
T S Frolova, A V Lipeeva, D S Baev, Y A Tsepilov, O I Sinitsyna
Pentacyclic triterpene acids are of great interest as compounds that exhibit selective cytotoxicity against malignant tumor cells. If earlier studies were carried out mainly in cancer cells of epithelial origin, in the present work the cytotoxic effect of ursolic and pomolic acids on the primary and permanent glioma cell lines was analyzed. Both compounds are toxic to oncotransformed cells and induce apoptosis in U-87 MG line. Using molecular docking, it has been shown that Akt1 and MDM2 may be potential targets of the studied triterpene acids...
September 2017: Molekuliarnaia Biologiia
Ana B Ramos-Hryb, Francis L Pazini, Manuella P Kaster, Ana Lúcia S Rodrigues
Ursolic acid is a pentacyclic triterpenoid found in several plants. Despite its initial use as a pharmacologically inactive emulsifier in pharmaceutical, cosmetic and food industries, several biological activities have been reported for this compound so far, including anti-tumoural, anti-diabetic, cardioprotective and hepatoprotective properties. The biological effects of ursolic acid have been evaluated in vitro, in different cell types and against several toxic insults (i.e. 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, amyloid-β peptides, kainic acid and others); in animal models of brain-related disorders (Alzheimer disease, Parkinson disease, depression, traumatic brain injury) and ageing; and in clinical studies with cancer patients and for muscle atrophy...
November 2, 2017: CNS Drugs
Yosuke Matsubara, Takashi Matsumoto, Junichi Koseki, Atsushi Kaneko, Setsuya Aiba, Kenshi Yamasaki
Stratum corneum tryptic enzyme kallikrein 5 (KLK5) is a serine protease that is involved in the cell renewal and maintenance of the skin barrier function. The excessive activation of KLK5 causes an exacerbation of dermatoses, such as rosacea and atopic dermatitis. Some triterpenoids are reported to suppress the serine proteases. We aimed to investigate whether bioactive triterpenoids modulate the KLK5 protease. Nineteen triterpenoids occurring in medicinal crude drugs were evaluated using an enzymatic assay to measure the anti-KLK5 activity...
October 27, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Hye Eun Lee, Gabsik Yang, Jae Sue Choi, Joo Young Lee
The host immune system is the first line of host defense, consisting mainly of innate and adaptive immunity. Immunity must be maintained, orchestrated, and harmonized, since overactivation of immune responses can lead to inflammation and autoimmune diseases, while immune deficiency can lead to infectious diseases. We investigated the regulation of innate and adaptive immune cell activation by Artemisia capillaris and its components (ursolic acid, hyperoside, scopoletin, and scopolin). Macrophage phagocytic activity was determined using fluorescently labeled Escherichia coli, as an indicator of innate immune activation...
October 2017: Toxicological Research
Kunihiro Sakuma, Akihiko Yamaguchi
Sarcopenia, the age-related loss of skeletal muscle mass, is characterized by a deterioration of muscle quantity and quality leading to a gradual slowing of movement, a decline in strength and power, increased risk of fall-related injury, and often frailty. This review focuses on the recent advances of pharmacological, hormonal, and nutritional approaches for attenuating sarcopenia. The article is composed of the data reported in many basic and some clinical studies for mammalian muscles. Resistance training combined with amino acid-containing supplements is the gold standard to prevent sarcopenia...
October 18, 2017: Pflügers Archiv: European Journal of Physiology
Juan Luo, Yan-Ling Hu, Hong Wang
Breast cancer, which is the second leading cause of cancer-associated mortality in women worldwide, develops from breast tissue. Chemotherapy is the most commonly used therapy to treat breast cancer. However, a number of natural plant-derived products have been suggested as alternative therapies to treat different types of cancer, such as breast cancer. The aim of the present study was to determine the anti-tumor effects of ursolic acid and its effect on apoptosis and inflammation in breast cancer cells. The anti-cancer effects of ursolic acid were evaluated in vitro using flow cytometry, western blotting and reverse transcription-quantitative polymerase chain reaction...
October 2017: Experimental and Therapeutic Medicine
Shan-Shan Yu, Biao Chen, Chen-Kai Huang, Juan-Juan Zhou, Xin Huang, An-Jiang Wang, Bi-Min Li, Wen-Hua He, Xuan Zhu
Activation of quiescent hepatic stellate cells (q-HSCs) and their transformation to myofibroblasts (MFBs) is a key event in liver fibrosis. Hedgehog (Hh) signaling stimulates q-HSCs to differentiate into MFBs, and NADPH oxidase (NOX) may be involved in regulating Hh signaling. The author's preliminary study demonstrated that ursolic acid (UA) selectively induces apoptosis in activated HSCs and inhibits their proliferation in vitro via negative regulation of NOX activity and expression. However, the effect of UA on q-HSCs remains to be elucidated...
October 2017: Experimental and Therapeutic Medicine
Andressa Maria Pironi, Patricia Rocha de Araújo, Mariza Aires Fernandes, Hérida Regina Nunes Salgado, Marlus Chorilli
Ursolic acid (UA) is a naturally occurring triterpenoid which is a promising candidate for the development of new therapeutic approaches and for the prevention and treatment of several diseases owing to its pharmacological importance. However, its low solubility in aqueous medium affects its therapeutic application. Several strategies have been used to overcome this obstacle. In this study, the incorporation of UA in to different drug delivery systems was found to be highly efficient. In addition, important investigations were performed about methods for qualitative and quantitative analyses of UA in various raw materials, including plants, biological fluids, and drug delivery systems, were investigated...
October 17, 2017: Critical Reviews in Analytical Chemistry
Angela Caunii, Camelia Oprean, Mirabela Cristea, Alexandra Ivan, Corina Danciu, Calin Tatu, Virgil Paunescu, Daniela Marti, George Tzanakakis, Demetrios A Spandidos, Aristides Tsatsakis, Razvan Susan, Codruta Soica, Stefana Avram, Cristina Dehelean
Among the triterpenoids, oleanolic acid (OA) and its isomer, ursolic acid (UA) are promising therapeutic candidates, with potential benefits in the management of melanoma. In this study, we aimed to examine the in vitro and in vivo anti‑invasive and anti‑metastatic activity of OA and UA to determine their possible usefulness as chemopreventive or chemotherapeutic agents in melanoma. For the in vitro experiments, the anti‑proliferative activity of the triterpenic compounds on SK‑MEL‑2 melanoma cells was examined...
December 2017: International Journal of Oncology
Chengyue Zhang, Chao Wang, Wenji Li, Renyi Wu, Yue Guo, David Cheng, Yuqing Yang, Ioannis P Androulakis, Ah-Ng Kong
The triterpenoid ursolic acid (UA) has been proposed as a potential cancer chemopreventive agent in many preclinical and clinical studies. In the present work, we aimed to characterize the pharmacokinetics (PK) of UA and to quantitatively assess the antioxidative and anti-inflammatory effects of UA, which are potentially linked to its chemopreventive efficacy. UA was administered intravenously (i.v., 20 mg/kg) or by oral gavage (100 mg/kg) to male Sprague-Dawley rats, and blood samples were collected at a series of designated time points...
November 6, 2017: Molecular Pharmaceutics
Ye Zhang, Longchang Huang, Haoze Shi, Hang Chen, Jianxin Tao, Renhui Shen, Tong Wang
It has been reported that ursolic acid has anti-tumor activity and it enhances the therapeutic effect of oxaliplatin in colorectal cancer (CRC). However, the underlying mechanisms remain unknown. In the present study, the mechanisms of the enhancement of therapeutic effects through use of ursolic acid were investigated. We treated CRC cell lines HCT8 and SW480 with ursolic acid and oxaliplatin and monitored the effects on cell proliferation, apoptosis, reactive oxygen species (ROS) production and drug resistance gene production...
October 16, 2017: Cancer Science
Huafang Ding, Xing Hu, Ximing Xu, Guowen Zhang, Deming Gong
Glycemic control which can be efficaciously regulated by inhibiting α-glucosidase activity is an effective therapy for diabetes mellitus. This work is to investigate the kinetics and inhibition mechanism of oleanolic acid and ursolic acid on α-glucosidase. Oleanolic acid and ursolic acid exhibited potent inhibitory activities with IC50 values of (6.35±0.02)×10(-6) and (1.69±0.03)×10(-5)molL(-1) respectively in a reversible and non-competitive manner. Both of them binding to α-glucosidase induced the conformational change and intrinsic fluorescence quenching of α-glucosidase...
October 10, 2017: International Journal of Biological Macromolecules
Dongyin Chen, Fengguo Xu, Pu Zhang, Jie Deng, Hongbin Sun, Xiaoan Wen, Jun Liu
A practical synthesis of α-amyrin (1), β-amyrin (2), and lupeol (3) was accomplished in total yields of 32, 42, and 40% starting from easily available ursolic acid (4), oleanolic acid (5), and betulin (6), respectively. Remarkably, these three natural pentacyclic triterpenes exhibited potential inhibitory activity against human oxidosqualene cyclase.
October 13, 2017: Archiv der Pharmazie
Sylvain Legay, Emmanuelle Cocco, Christelle M André, Cédric Guignard, Jean-Francois Hausman, Gea Guerriero
Russeting is characterized by a particular rough and brown phenotype, which is mainly due to the accumulation of suberin in the inner part of the epidermal cell walls. In our previous bulk transcriptomic analysis, comparing fully russeted, and waxy apple varieties, showed, in apple fruit skin, a massive decreased expression of cutin, wax and some pentacyclic triterpene biosynthesis genes in the russeted varieties, with an expected concomitant enhanced expression of the suberin biosynthetic genes. In the present work, we performed a deep investigation of the aliphatic composition of the cutin, suberin, waxes, and triterpenes in the waxy and russeted patches of the semi-russeted apple variety "Cox Orange Pippin...
2017: Frontiers in Plant Science
Claire Beaufay, Marie-France Hérent, Joëlle Quetin-Leclercq, Joanne Bero
BACKGROUND: Considering the need for new anti-malarial drugs, further investigations on Keetia leucantha (Rubiaceae), an in vitro antiplasmodial plant traditionally used to treat malaria, were carried out. This paper aimed to assess the in vivo anti-malarial efficacy of K. leucantha triterpenic esters previously identified as the most in vitro active components against Plasmodium falciparum and their potential toxicity as well as those of anti-malarial extracts. RESULTS: These eight triterpenic esters and the major antiplasmodial triterpenic acids, ursolic and oleanolic acids, were quantified in the twigs dichloromethane extract by validated HPLC-UV methods...
October 10, 2017: Malaria Journal
Babban Jee, Sanjay Kumar, Renu Yadav, Yogesh Singh, Anuj Kumar, Naveen Sharma
Small heat shock protein16.3 (sHSP16.3) is a crucial protein for survival of Mycobacterium tuberculosis (MTB) in its host. Besides, this protein acts as a molecular chaperone during stress and is indispensable for MTB's growth, virulence and cell wall thickening. sHSP16.3 is also a promising candidate for vaccine, serodiagnosis and drug design as well. In the present study, we have targeted sHSP16.3 with two phytochemicals namely ursolic acid and carvacrol using in silico approach. Molecular docking analysis showed that both phytochemicals (ursolic acid and carvacrol) has docked with sHSP16...
October 6, 2017: Journal of Biomolecular Structure & Dynamics
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