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https://www.readbyqxmd.com/read/28213701/ursolic-acid-mediated-changes-in-glycolytic-pathway-promote-cytotoxic-autophagy-and-apoptosis-in-phenotypically-different-breast-cancer-cells
#1
Anna Lewinska, Jagoda Adamczyk-Grochala, Ewa Kwasniewicz, Anna Deregowska, Maciej Wnuk
Plant-derived pentacyclic triterpenotids with multiple biological activities are considered as promising candidates for cancer therapy and prevention. However, their mechanisms of action are not fully understood. In the present study, we have analyzed the effects of low dose treatment (5-20 µM) of ursolic acid (UA) and betulinic acid (BA) on breast cancer cells of different receptor status, namely MCF-7 (ER(+), PR(+/-), HER2(-)), MDA-MB-231 (ER(-), PR(-), HER2(-)) and SK-BR-3 (ER(-), PR(-), HER2(+)). UA-mediated response was more potent than BA-mediated response...
February 17, 2017: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/28194155/functional-characterization-of-cyp716-family-p450-enzymes-in-triterpenoid-biosynthesis-in-tomato
#2
Shuhei Yasumoto, Hikaru Seki, Yuko Shimizu, Ery O Fukushima, Toshiya Muranaka
Triterpenoids are a group of structurally diverse specialized metabolites that frequently show useful bioactivities. These chemicals are biosynthesized from the common precursor 2,3-oxidosqualene in plants. The carbon skeletons produced by oxidosqualene cyclase (OSC) are usually modified by cytochrome P450 monooxygenases (P450s) and UDP-dependent glycosyltransferases. These biosynthetic enzymes contribute to the structural diversification of plant triterpenoids. Until now, many P450 enzymes have been characterized as triterpenoid oxidases...
2017: Frontiers in Plant Science
https://www.readbyqxmd.com/read/28177667/ursolic-acid-suppresses-leptin-induced-cell-proliferation-in-rat-vascular-smooth-muscle-cells
#3
Ya-Mei Yu, Chiang-Chin Tsai, Yu-Wen Tzeng, Weng-Cheng Chang, Su-Yin Chiang, Ming-Fen Lee
Accumulating lines of evidence indicate that high leptin levels are associated with adverse cardiovascular health in obese individuals. Proatherogenic effects of leptin include endothelial cell activation, vascular smooth muscle cell proliferation and migration. Ursolic acid (UA) has been reported to exhibit multiple biological effects including antioxidant and anti-inflammatory properties. In this study, we investigated the effect of UA on leptin-induced biological responses in rat vascular smooth muscle cells (VSMCs)...
January 29, 2017: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28166786/chemical-constituents-and-coagulation-activity-of-agastache-rugosa
#4
Pengran Cao, Pingyao Xie, Xuebiao Wang, Jinmei Wang, Jinfeng Wei, Wen-Yi Kang
BACKGROUND: In the Chinese traditional medicine, plant of Agastache rugosa (Fisch. & C.A. Mey.) Kuntze (A. rugosa) has been used to treat nausea, vomiting and dispel damp. However, currently, few reports about the chemical constituents, especially the non-volatile components of A. rugosa are available. METHODS: Through separation with various column chromatographies to elucidate the chemical constituents of A. rugosa, the biological activities of the major constituents were investigated...
February 6, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28155120/novel-glycoside-from-wedelia-calendulacea-inhibits-diethyl-nitrosamine-induced-renal-cancer-via-downregulating-the-cox-2-and-peg2-through-nuclear-factor-%C3%AE%C2%BAb-pathway
#5
Amita Verma, Bahar Ahmed, Firoz Anwar, Mahfoozur Rahman, Dinesh Kumar Patel, Gaurav Kaithwas, Ravi Rani, Prakash C Bhatt, Vikas Kumar
A new compound derivative of glycoside 19-α-hydroxy-ursolic acid glucoside (19-α-hydroxyurs-12(13)-ene-28-oic acid-3-O-β-D-glucopyranoside (HEG) was isolated from whole plant of Wedelia calendulacea (Compositae). The structure was elucidated and established by standard spectroscopy approaches. Diethylnitrosamine (DEN) (200 mg/kg) and ferric nitrilotriacetate (Fe-NTA) (9 mg/kg) were used for induction of renal cell carcinoma (RCC) in the rats. The rats were further divided into different groups and were treated with HEG doses for 22 weeks...
February 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/28152388/spectral-characterization-and-antibacterial-activity-of-an-isolated-compound-from-memecylon-edule-leaves
#6
R Srinivasan, D Natarajan, M S Shivakumar
Memecylon edule Roxb. (Melastamataceae family) is a small evergreen tree reported as having ethnobotanical and pharmacological properties. The present study was aimed to investigate the spectral characterization and antibacterial activity of isolated pure compound (3β-hydroxyurs-12-en-28-oic acid (ursolic acid)) from Memecylon edule leaves by performing bioassay guided isolation method. The structure derivation of isolated compound was done by different spectral studies like UV, FT-IR, LC-MS, CHNS analysis, 1D ((1)H, (13)C and DEPT-135) and 2D-NMR (HSQC and HMBC), respectively...
January 21, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28143855/-nutraceuticals-in-relation-to-human-skeletal-muscle-and-exercise
#7
Colleen Siobhan Deane, Daniel J Wilkinson, Bethan E Phillips, Kenneth Smith, Timothy Etheridge, Philip J Atherton
Skeletal muscles have a fundamental role in locomotion and whole body metabolism, with muscle mass and quality being linked to improved health and even lifespan. Optimising nutrition in combination with exercise is considered an established, effective ergogenic practice for athletic performance. Importantly, exercise and nutritional approaches also remain arguably the most effective countermeasure for muscle dysfunction associated with ageing and numerous clinical conditions e.g. cancer cachexia, COPD and organ failure, via engendering favourable adaptations such as increased muscle mass and oxidative capacity...
January 31, 2017: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28112016/the-anti-inflammatory-effect-of-sonchus-oleraceus-aqueous-extract-on-lipopolysaccharide-stimulated-raw-264-7-cells-and-mice
#8
Qi Li, Dan-Dan Dong, Qiu-Ping Huang, Jing Li, Yong-Yong Du, Bin Li, Huan-Qing Li, Ting Huyan
CONTEXT: Sonchus oleraceus L. (Asteraceae) (SO) is a dietary and traditional medicinal plant in China. However, its underlying mechanism of action as an anti-inflammatory agent is not known. OBJECTIVE: This study evaluates the anti-inflammatory activity of aqueous extract of SO. MATERIALS AND METHODS: The extract of SO was used to treat RAW 264.7 cells (in the working concentrations of 500, 250, 125, 62.5, 31.3 and 15.6 μg/mL) for 24 h...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28101738/synthesis-of-novel-oleanolic-acid-and-ursolic-acid-in-c-28-position-derivatives-as-potential-anticancer-agents
#9
Tian Tian, Xinyu Liu, Eung-Seok Lee, Jingyang Sun, Zhonghua Feng, Longxuan Zhao, Chunhui Zhao
A series of nitrogen-containing derivatives of oleanolic acid and ursolic acid were prepared by a modification at C-28 position via esterification with 2-hydroxyacetic acid followed by amidation with amines, such as piperazine, N-methylpiperazine, and alkane-1, 2-diamines, alkane-1, 4-diamines, alkane-1, 6-diamines. In vitro antiproliferative activities of the compounds prepared towards MCF-7, Hela and A549 cell lines were evaluated by a MTT method to show that OA-5a, OA-5b, OA-5c and UA-5a showed somewhat improved antiproliferative activities against MCF-7, Hela and A549 cells comparing to that of the positive control, gefitinib...
January 18, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28091396/anti-angiogenic-activity-and-antitumor-efficacy-of-amphiphilic-twin-drug-from-ursolic-acid-and-low-molecular-weight-heparin
#10
Wenming Cheng, Fatima Zohra Dahmani, Juan Zhang, Hui Xiong, Yuanyuan Wu, Lifang Yin, Jianping Zhou, Jing Yao
Heparin, a potential blood anti-coagulant, is also known for its binding ability to several angiogenic factors through electrostatic interactions due to its polyanionic character. However, the clinical application of heparin for cancer treatment is limited by several drawbacks, such as unsatisfactory therapeutic effects and severe anticoagulant activity that could induce hemorrhaging. Herein, low molecular weight heparin (LMWH) was conjugated to ursolic acid (UA), which is also an angiogenesis inhibitor, by binding the amine group of aminoethyl-UA (UA-NH2) with the carboxylic groups of LMWH...
February 17, 2017: Nanotechnology
https://www.readbyqxmd.com/read/28089066/evaluation-and-prevention-of-the-negative-matrix-effect-of-terpenoids-on-pesticides-in-apples-quantification-by-gas-chromatography-tandem-mass-spectrometry
#11
Géraldine Giacinti, Christine Raynaud, Sophie Capblancq, Valérie Simon
The sample matrix can enhance the gas chromatography signal of pesticide residues relative to that obtained with the same concentration of pesticide in solvent. This paper is related to negative matrix effects observed in coupled gas chromatography-mass spectrometry ion trap (GC/MS(2)) quantification of pesticides in concentrated extracts of apple peel prepared by the Quick Easy Cheap Effective Rugged and Safe (QuEChERS) method. It is focused on the pesticides most frequently used on the apple varieties studied, throughout the crop cycle, right up to harvest, to combat pests and diseases and to improve fruit storage properties...
December 21, 2016: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28073673/discovery-of-fzu-03-010-as-a-self-assembling-anticancer-amphiphile-for-acute-myeloid-leukemia
#12
Yingyu Chen, Cailong Li, Yunquan Zheng, Yu Gao, Jianda Hu, Haijun Chen
Recently various drug candidates with excellent anticancer potency have been demonstrated, whereas their clinical application largely suffers from several limitations especially poor solubility. Ursolic acid (UA) as one of ubiquitous pentacyclic triterpenes in plantkingdom exhibited versatile antiproliferative effects in various cancer cell lines. However, the unfavorable pharmaceutical properties became the main obstacle for its clinical development. With the aim of development of novel derivatives with enhanced potency, a series of diversified UA amphiphiles have been designed, synthesized, and pharmacologically evaluated...
December 30, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28069166/evaluation-and-prevention-of-the-negative-matrix-effect-of-terpenoids-on-pesticides-in-apples-quantification-by-gas-chromatography-tandem-mass-spectrometry
#13
Géraldine Giacinti, Christine Raynaud, Sophie Capblancq, Valérie Simon
The sample matrix can enhance the gas chromatography signal of pesticide residues relative to that obtained with the same concentration of pesticide in solvent. This paper is related to negative matrix effects observed in coupled gas chromatography-mass spectrometry ion trap (GC/MS(2)) quantification of pesticides in concentrated extracts of apple peel prepared by the Quick Easy Cheap Effective Rugged and Safe (QuEChERS) method. It is focused on the pesticides most frequently used on the apple varieties studied, throughout the crop cycle, right up to harvest, to combat pests and diseases and to improve fruit storage properties...
February 3, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28066112/in-vitro-effectiveness-of-triterpenoids-and-their-synergistic-effect-with-antibiotics-against-staphylococcus-aureus-strains
#14
Muhammad Hamza, Maha Nadir, Nadir Mehmood, Adeel Farooq
OBJECTIVES: The aim of this study is to evaluate the effect of four triterpenoids such as oleanolic acid, ursolic acid, cycloastragenol, and beta-boswellic acid alone and in combination with antibiotics against Staphylococcus aureus strains. MATERIALS AND METHODS: Sixteen clinical strains of S. aureus from infected wounds were isolated. Eight were methicillin-sensitive S. aureus (MSSA), and the other eight were methicillin-resistant S. aureus (MRSA). The activity was also seen in reference S...
November 2016: Indian Journal of Pharmacology
https://www.readbyqxmd.com/read/28034283/in-silico-studies-revealed-multiple-neurological-targets-for-the-antidepressant-molecule-ursolic-acid
#15
Rajeev K Singla, Luciana Scotti, Ashok K Dubey
BACKGROUND: Ursolic acid, a bioactive pentacyclic triterpenoid had been evaluated for its interaction with the neurological targets associated with antidepressant drugs. Current study was to mechanistically analyze the probable site of action for ursolic acid on the target proteins. METHODS: Ursolic acid has been docked with monoamine oxidase isoforms: MAO-A and MAO-B, LeuT (homologue of SERT, NET, DAT) and Human C-terminal CAP1 using GRIP docking methodology. RESULTS: Results revealed its non-selective antidepressant action with strong binding affinity towards LeuT and MAO-A proteins, which was found to be comparable with the reference ligands like chlorgyline, clomipramine, sertraline and deprenyl / selegiline...
December 29, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/28025900/phytochemical-and-biological-evaluation-of-salvia-apiana
#16
Radhakrishnan Srivedavyasasri, Taylor Hayes, Samir A Ross
Salvia apiana (white sage, Lamiaceae family) plant is native to southern California and parts of Mexico. Some Native American tribes local to this region consider S. apiana to be sacred and burn the leaves as incense for purification ceremonies. The plant has been used to treat sore throats, coughs, chest colds, upper respiratory infections and poison oak rashes. The aqueous ethanolic extract of S. apiana showed moderate CB1 activity (58.3% displacement). Chromatographic purification of the ethanolic extract on silica gel column led to isolation of nine compounds: rosmadial (I), carnosol (II), 16-hydroxycarnosol (III), sageone (IV), cirsimaritin (V), salvigenin (VI), oleanolic acid (VII), 3β,28-dihydroxy-urs-12-ene (VIII), and ursolic acid (IX)...
December 27, 2016: Natural Product Research
https://www.readbyqxmd.com/read/28025124/major-triterpenoids-in-chinese-hawthorn-crataegus-pinnatifida-and-their-effects-on-cell-proliferation-and-apoptosis-induction-in-mda-mb-231-cancer-cells
#17
Lingrong Wen, Ruixue Guo, Lijun You, Arshad Mehmood Abbasi, Tong Li, Xiong Fu, Rui Hai Liu
The cytotoxicity and antiproliferative effect of phytochemicals presenting in the fruits of Chinese hawthorn (Crataegus pinnatifida) were evaluated. Shanlihong (Crataegus pinnatifida Bge. var. major N.E.Br.) variety possessed significant levels of flavonoids and triterpenoids, and showed potent antiproliferative effect against HepG2, MCF-7 and MDA-MB- 231 human cancer cells lines. Triterpenoids-enriched fraction (S9) prepared by Semi-preparative HPLC, and its predominant ingredient ursolic acid (UA) demonstrated remarkably antiproliferative activities for all the tested cancer cell lines...
February 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28008473/cyp716a179-functions-as-a-triterpene-c-28-oxidase-in-tissue-cultured-stolons-of-glycyrrhiza-uralensis
#18
Keita Tamura, Hikaru Seki, Hideyuki Suzuki, Mareshige Kojoma, Kazuki Saito, Toshiya Muranaka
CYP716A179, a cytochrome P450 monooxygenase expressed predominantly in tissue-cultured stolons of licorice ( Glycyrrhiza uralensis ), functions as a triterpene C-28 oxidase in the biosynthesis of oleanolic acid and betulinic acid. Cytochrome P450 monooxygenases (P450s) play key roles in the structural diversification of plant triterpenoids. Among these, the CYP716A subfamily, which functions mainly as a triterpene C-28 oxidase, is common in plants. Licorice (Glycyrrhiza uralensis) produces bioactive triterpenoids, such as glycyrrhizin and soyasaponins, and relevant P450s (CYP88D6, CYP72A154, and CYP93E3) have been identified; however, no CYP716A subfamily P450 has been isolated...
March 2017: Plant Cell Reports
https://www.readbyqxmd.com/read/28003581/triterpenes-suppress-octanoylated-ghrelin-production-in-ghrelin-expressing-human-gastric-carcinoma-cells
#19
Kensuke Nakajima, Shigeru Oiso, Takuhiro Uto, Osamu Morinaga, Yukihiro Shoyama, Hiroko Kariyazono
Ghrelin is an appetite-stimulating peptide hormone with an octanoyl modification at serine 3 that is essential for its orexigenic effect. Ghrelin O-acyltransferase (GOAT) is the enzyme that catalyzes ghrelin acylation using fatty acyl-coenzyme A as a substrate. We previously developed an assay system based on the AGS-GHRL8 cell line that produces octanoylated ghrelin in the presence of octanoic acid, and demonstrated that some fatty acids suppressed octanoylated ghrelin production. Recent studies have reported that triterpenes have anti-obesity effect...
2016: Biomedical Research
https://www.readbyqxmd.com/read/27999607/effect-of-loquat-leaf-extract-on-muscle-strength-muscle-mass-and-muscle-function-in-healthy-adults-a-randomized-double-blinded-and-placebo-controlled-trial
#20
Young Hye Cho, Sang Yeoup Lee, Cheol Min Kim, Nam Deuk Kim, Sangmin Choe, Chang-Hyung Lee, Jin-Hong Shin
Ursolic acid (UA) is the major active component of the loquat leaf extract (LLE) and several previous studies have indicated that UA may have the ability to prevent skeletal muscle atrophy. Therefore, we conducted a randomized, double-blind, and placebo-controlled study to investigate the effects of the LLE on muscle strength, muscle mass, muscle function, and metabolic markers in healthy adults; the safety of the compound was also evaluated. We examined the peak torque/body weight at 60°/s knee extension, handgrip strength, skeletal muscle mass, physical performance, and metabolic parameters at baseline, as well as after 4 and 12 weeks of intervention...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
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