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https://www.readbyqxmd.com/read/27916903/combined-use-of-zoledronic-acid-augments-ursolic-acid-induced-apoptosis-in-human-osteosarcoma-cells-through-enhanced-oxidative-stress-and-autophagy
#1
Chia-Chieh Wu, Yi-Fu Huang, Chen-Pu Hsieh, Pin-Ju Chueh, Yao-Li Chen
Ursolic acid (UA), a naturally occurring pentacyclic triterpene acid found in many medicinal herbs and edible plants, triggers apoptosis in several tumor cell lines but not in human bone cancer cells. Most recently, we have demonstrated that UA exposure reduces the viability of human osteosarcoma MG-63 cells through enhanced oxidative stress and apoptosis. Interestingly, an inhibitor of osteoclast-mediated bone resorption, zoledronic acid (ZOL), also a third-generation nitrogen-containing bisphosphonate, is effective in the treatment of bone metastases in patients with various solid tumors...
November 30, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27897418/suppression-of-muscle-wasting-by-the-plant-derived-compound-ursolic-acid-in-a-model-of-chronic-kidney-disease
#2
Rizhen Yu, Ji-An Chen, Jing Xu, Jin Cao, Yanlin Wang, Sandhya S Thomas, Zhaoyong Hu
BACKGROUND: Muscle wasting in chronic kidney disease (CKD) and other catabolic disorders contributes to morbidity and mortality, and there are no therapeutic interventions that regularly and safely block losses of muscle mass. We have obtained evidence that impaired IGF-1/insulin signalling and increases in glucocorticoids, myostatin and/or inflammatory cytokines that contribute to the development of muscle wasting in catabolic disorders by activating protein degradation. METHODS: Using in vitro and in vivo models of muscle wasting associated with CKD or dexamethasone administration, we measured protein synthesis and degradation and examined mechanisms by which ursolic acid, derived from plants, could block the loss of muscle mass stimulated by CKD or excessive levels of dexamethasone...
November 17, 2016: Journal of Cachexia, Sarcopenia and Muscle
https://www.readbyqxmd.com/read/27867276/ursolic-acid-a-natural-pentacylcic-triterpene-from-ochrosia-elliptica-and-its-role-in-the-management-of-certain-neglected-tropical-diseases
#3
Rola M Labib, Sherif S Ebada, Fadia S Youssef, Mohamed L Ashour, Samir A Ross
BACKGROUND: Leishmaniasis and African trypanosomiasis are recognized as the leading causes of mortality and morbidity with the greatest prevalence in the developing countries. They affect more than one billion of the poorest people on the globe. OBJECTIVE: To find a cheap, affordable, safe, and efficacious antileshmanial and antitrypanosomal natural drug and to elucidate its probable mode of action. MATERIALS AND METHODS: Phytochemical investigation of the non-polar fraction of the methanol extract of leaves of Ochrosia elliptica Labill...
October 2016: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/27855928/ursolic-acid-from-apple-pomace-and-traditional-plants-a-valuable-triterpenoid-with-functional-properties
#4
REVIEW
Simone Tasca Cargnin, Simone Baggio Gnoatto
Apple juice production generates a large amount of residue comprising mainly peels, seeds, and pulp, known as apple pomace. In the global context, Brazil ranks 11th in apple production and thousands of tons of apple pomace are produced every year. This by-product is little explored, since it is a rich and heterogeneous mixture, containing interesting phytochemical groups. Among them, ursolic acid (UA) has attracted attention because of its therapeutic potential. UA is a pentacyclic triterpene found too in several traditional plants, and has shown several functional properties such as antibacterial, antiprotozoal, anti-inflammatory and antitumor...
April 1, 2017: Food Chemistry
https://www.readbyqxmd.com/read/27822011/ursolic-acid-sensitizes-cisplatin-resistant-hepg2-ddp-cells-to-cisplatin-via-inhibiting-nrf2-are-pathway
#5
Shouhai Wu, Tianpeng Zhang, Jingsheng Du
BACKGROUND: Combinations of adjuvant sensitizers with anticancer drugs is a promising new strategy to reverse chemoresistance. Ursolic acid (UA) is one of the natural pentacyclic triterpene compounds known to have many pharmacological characteristics such as anti-inflammatory and anticancer properties. This study investigates whether UA can sensitize hepatocellular carcinoma cells to cisplatin. MATERIALS AND METHODS: Cells were transfected with nuclear factor erythroid-2-related factor 2 (Nrf2) small interfering RNA and Nrf2 complementary DNA by using Lipofectin 2000...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27809705/potential-use-of-nanocarriers-with-pentacyclic-triterpenes-in-cancer-treatments
#6
Karina Valdés, Javier Morales, Lennin Rodríguez, Germán Günther
Ursolic, oleanolic and betulinic acids are representative pentacyclic triterpenoids found in various plants and fruits. Despite having marked antitumor potentials, the very poor water solubility of these triterpenes hinders treatment development. Nanotechnology can enhance solubility, stability, bioavailability and phytochemical delivery, improving the therapeutic efficiency of triterpenes. This review focuses on the formulation, characterization and in vitro/in vivo evaluation of several delivery nanosystems used to enhance the physicochemical properties of ursolic, oleanolic and betulinic acids...
November 4, 2016: Nanomedicine
https://www.readbyqxmd.com/read/27798869/ursolic-acid-suppresses-hepatitis-b-virus-x-protein-mediated-autophagy-and-chemotherapeutic-drug-resistance
#7
Ching-Dong Chang, Ping-Yuan Lin, Jue-Liang Hsu, Wen-Ling Shih
Hepatitis B virus X (HBx) protein is a multifunctional oncoprotein that affects diverse cell activities via regulation of various host cell signaling pathways. The current investigation demonstrated that ursolic acid (UA), a pentacyclic triterpenoid, protected hepatoma cells and reduced HBx-mediated autophagy through modulation of Ras homolog gene family member A (RhoA). Low-level ectopic HBx expression in Huh7 cells induced more significant autophagosome formation than high-level HBx expression. HBx activated beclin-1 promoter and enhanced the beclin-1 protein expression under low HBx expression...
October 2016: Anticancer Research
https://www.readbyqxmd.com/read/27783971/corrigendum-to-synthesis-and-cytotoxic-activity-of-novel-a-ring-cleaved-ursolic-acid-derivatives-in-human-non-small-cell-lung-cancer-cells-eur-j-med-chem-123-2016-317-331
#8
Vanessa I S Mendes, Geoffrey A Bartholomeusz, Mary Ayres, Varsha Gandhi, Jorge A R Salvador
No abstract text is available yet for this article.
October 23, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27776775/microcrystalline-cellulose-based-matrix-solid-phase-dispersion-microextration-for-isomeric-triterpenoid-acids-in-loquat-leaves-by-ultrahigh-performance-liquid-chromatography-and-quadrupole-time-of-flight-mass-spectrometry
#9
Jun Cao, Li-Qing Peng, Jing-Jing Xu
An analytical procedure based on matrix solid phase dispersion (MSPD) microextration and ultrahigh-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry was developed for the determination of isomeric triterpenoid acids (maslinic acid, corosolic acid, oleanolic acid and ursolic acid) in loquat leaves. Microcrystalline cellulose was used for the first time as a solid sorbent in MSPD microextration. Compared with the traditional extraction methods, the proposed method possessed the advantages of shorter extraction time, and lower consumption of sample, sorbent and organic solvent...
October 13, 2016: Journal of Chromatography. A
https://www.readbyqxmd.com/read/27776314/comparison-of-the-interaction-between-lactoferrin-and-isomeric-drugs
#10
Ming Guo, Xiaowang Lu, Yan Wang, Peter E Brodelius
The binding properties of pentacyclic triterpenoid isomeric drugs, i.e. ursolic acid (UA) and oleanolic acid (OA), to bovine lactoferrin (BLF) have been studied by molecule modeling, fluorescence spectroscopy, UV-visible absorbance spectroscopy and infrared spectroscopy (IR). Molecular docking, performed to reveal the possible binding mode or mechanism, suggested that hydrophobic interaction and hydrogen bonding play important roles to stabilize the complex. The results of spectroscopic measurements showed that the two isomeric drugs both strongly quenched the intrinsic fluorescence of BLF through a static quenching procedure although some differences between UA and OA binding strength and non-radiation energy transfer occurred within the molecules...
October 18, 2016: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/27773812/3%C3%AE-hydroxy-urs-12-en-28-oic-acid-prolongs-lifespan-in-c-elegans-by-modulating-jnk-1
#11
Hema Negi, Aparna Shukla, Feroz Khan, Rakesh Pandey
Remarkably the c-Jun-NH2-terminal kinase (JNK) pathway is all evolutionarily conserved across species. In view of the hypothesis that increased stress resistance subdue aging, we investigated the role of ursolic acid (3β-Hydroxy-urs-12-en-28-oic acid; UA) in the pioneering aging model Caenorhabditis elegans with an increase in mean and maximum lifespan by up to 30%. Our genetic study unravelled the underlying pathway where JNK-1 is acting independently of insulin-IGF-1 signalling (IIS) pathway to modulate longevity...
October 20, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27771513/ph-sensitive-mesoporous-silica-nanoparticles-anticancer-prodrugs-for-sustained-release-of-ursolic-acid-and-the-enhanced-anti-cancer-efficacy-for-hepatocellular-carcinoma-cancer
#12
Tao Li, Xiufen Chen, Yajun Liu, Lulu Fan, Liqing Lin, Yu Xu, Sijia Chen, Jingwei Shao
Ursolic acid (UA) as a nature product exhibits good anti-cancer activity, low toxicity, and good liver protection features. However, the low-solubility and poor bioavailability restrict its further clinical application. To overcome this problem, a pH-sensitive prodrug delivery system (UA@MSN-UA) that incorporated acid-sensitive linkage between drug and silica-based mesoporous nanosphere (MSN) was successfully designed and synthesized. The physicochemical properties of the UA@MSN-UA nanoparticles were investigated for shape, particle size, zeta potential, nitrogen adsorption-desorption and infrared (IR) spectroscopy...
October 19, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27769622/discovery-of-ursolic-acid-prodrug-nx-201-pharmacokinetics-and-in-vivo-antitumor-effects-in-panc-1-pancreatic-cancer
#13
Yeohong Yoon, Jee Woong Lim, Jiyoung Kim, Younggi Kim, Keun Ho Chun
The aim of our study was to develop ursolic acid (UA) prodrugs in order to overcome UA's weakness, which has an extremely low bioavailability. UA-medoxomil (NX-201), one of our UA prodrugs, showed an improved bioavailability about 200times better than UA in rodent model. According to in vivo test performed with PANC-1 xenograft SCID mouse model, tumor growth rate decreased dose-dependently and 100mg/kg dose of NX-201 had an anticancer effect comparable to gemcitabine. Most of all the combination of NX-201 (50mg/kg, po, daily) and gemcitabine (40mg/kg, iv, 2timesperweek) even reduced tumor size after three weeks...
October 6, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27765249/composition-and-morphology-of-cuticular-wax-in-blueberry-vaccinium-spp-fruits
#14
Wenjing Chu, Haiyan Gao, Shifeng Cao, Xiangjun Fang, Hangjun Chen, Shangyue Xiao
The chemical composition and morphology of cuticular wax in mature fruit of nine blueberry cultivars were investigated using gas chromatography-mass spectrometry (GC-MS) and scanning electron microscope (SEM). Triterpenoids and β-diketones were the most prominent compounds, accounting for on average 64.2% and 16.4% of the total wax, respectively. Ursolic or oleanolic acid was identified as the most abundant triterpenoids differing in cultivars. Two β-diketones, hentriacontan-10,12-dione and tritriacontan-12,14-dione, were detected in cuticular wax of blueberry fruits for the first time...
March 15, 2017: Food Chemistry
https://www.readbyqxmd.com/read/27762142/synthesis-structural-studies-and-cytotoxic-evaluation-of-novel-ursolic-acid-hybrids-with-capabilities-to-arrest-breast-cancer-cells-in-mitosis
#15
Banita Pattnaik, Jerripothula K Lakshmi, Rachineni Kavitha, Bharatam Jagadeesh, Debanjan Bhattacharjee, Nishant Jain, Uppuluri V Mallavadhani
Some novel chemically modified frameworks of ursolic acid have been designed and synthesized. The key step was the cycloaddition of azidopropyl-3β-hydroxy-urs-12-en-28-oate with the appropriate C28 propargyl esters of ursolic, corosolic, asiatic, oleanolic, and betulinic acid under Click reaction conditions, and the products were obtained in 74-84% yields. In view of their intriguing structural diversity, they have been subjected to detailed 1D and 2D NMR studies and their structures are thoroughly assigned...
October 20, 2016: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/27750148/fragment-based-discovery-of-novel-pentacyclic-triterpenoid-derivatives-as-cholesteryl-ester-transfer-protein-inhibitors
#16
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
https://www.readbyqxmd.com/read/27748884/fructus-ligustri-lucidi-ethanol-extract-inhibits-osteoclastogenesis-in-raw264-7-cells-via-the-rankl-signaling-pathway
#17
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
https://www.readbyqxmd.com/read/27734181/ursolic-acid-ameliorates-early-brain-injury-after-experimental-traumatic-brain-injury-in-mice-by-activating-the-nrf2-pathway
#18
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
https://www.readbyqxmd.com/read/27708244/hypoxia-pathway-and-hypoxia-mediated-extensive-extramedullary-hematopoiesis-are-involved-in-ursolic-acid-s-anti-metastatic-effect-in-4t1-tumor-bearing-mice
#19
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
https://www.readbyqxmd.com/read/27704066/the-potential-beneficial-effects-of-phenolic-compounds-isolated-from-a-pilosa-ledeb-on-insulin-resistant-hepatic-hepg2-cells
#20
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
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