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https://www.readbyqxmd.com/read/28539719/ultrasound-assisted-extraction-of-ursolic-acid-from-the-flowers-of-ixora-coccinia-linn-rubiaceae-and-antiproliferative-activity-of-ursolic-acid-and-synthesized-derivatives
#1
Silvana Amadeu Ferreira Alves Monteath, Maria Aparecida M Maciel, Raquel Garcia Vega, Heloisa de Mello, Carollina de Araújo Martins, Andressa Esteves-Souza, Cerli Rocha Gattass, Aurea Echevarria
BACKGROUND: Ixora coccinea Linn (Rubiaceae) is an evergreen shrub with bright scarlet colored flowers found in several tropical and subtropical countries. It is used as an ornamental and medicinal plant. Phytochemical studies revealed that its major special metabolites are triterpene acids, such as ursolic and oleanolic acid. OBJECTIVE: To evaluate the isolation of ursolic acid (UA) (1) from methanol extracts of I. coccinea flowers through two methodologies, to prepare four derivatives, and to evaluate the cytotoxic effect against six cancer cell lines...
April 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28531996/poly-epsilon-caprolactone-nanoparticles-enhance-ursolic-acid-in-vivo-efficacy-against-trypanosoma-cruzi-infection
#2
Juliana Palma Abriata, Josimar O Eloy, Thalita Bachelli Riul, Patricia Mazureki Campos, Marcelo Dias Baruffi, Juliana Maldonado Marchetti
Despite affecting millions of people worldwide, Chagas disease is still neglected by the academia and industry and the therapeutic option available, benznidazole, presents limited efficacy and side effects. Within this context, ursolic acid may serve as an option for treatment, however has low bioavailability, which can be enhanced through the encapsulation in polymeric nanoparticles. Therefore, herein we developed ursolic acid-loaded nanoparticles with poly-ε-caprolactone by the nanoprecipitation method and characterized them for particle size, zeta potential, polydispersity, encapsulation efficiency, morphology by scanning electron microscopy and thermal behavior by differential scanning calorimetry...
August 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28531761/3%C3%AE-hydroxy-urs-12-en-28-oic-acid-confers-protection-against-znonps-induced-adversity-in-caenorhabditis-elegans
#3
Hema Negi, Shilpi Khare Saikia, Ranjana Kanaujia, Satish Jaiswal, Rakesh Pandey
Despite their well reported potent risk towards human health and environment Zinc oxide nanoparticles (ZnONPs) find an extensive commercial usage due to their antimicrobial properties. Here, we evaluated the efficacy of a natural triterpene ursolic acid (3β-hydroxy-urs-12-en-28-oic acid; UA) for overcoming the cytotoxic challenges of ZnONPs employing Ceanorhabditis elegans. The 24h LC50 of Zn-ONPs (<50nm TEM) was deduced as 4.75mgL(-1). UA (25μM) was observed to defend against this toxicity by attenuating Reactive Oxygen Species (ROS) resulting into better survival at 2mgL(-1) in a time dependent behavior...
May 8, 2017: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/28506699/cra-crosolic-acid-isolated-from-actinidia-valvata-dunn-radix-induces-apoptosis-of-human-gastric-cancer-cell-line-bgc823-in%C3%A2-vitro-via-down-regulation-of-the-nf-%C3%AE%C2%BAb-pathway
#4
Qi-Lai Cheng, Hong-Liang Li, Ying-Chen Li, Zhao-Wen Liu, Xiao-Hua Guo, Yi-Jian Cheng
A natural ursolic compound, 2α,3β-dihydroxy-urs-12-en-28-oic acid (corosolic acid, CRA) was isolated from the root of Actinidia valvata Dunn. (A. valvata Radix). Since a large number of triterpenoid compound has marked anticancer effects toward various types of cancer cell lines in vitro, this study was carried out to investigate the anticancer effect of CRA in human gastric cancer cell line BGC823 cells and the underlying apoptotic mechanism of CRA was examined in BGC823 cell lines. The results showed that CRA significantly suppressed the viability of BGC823 cells in a concentration- and time-dependent manner...
May 12, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28493531/ternary-complex-of-human-ror%C3%AE-ligand-binding-domain-inverse-agonist-and-smrt-peptide-shows-a-unique-mechanism-of-corepressor-recruitment
#5
Masato Noguchi, Akihiro Nomura, Ken Murase, Satoki Doi, Keishi Yamaguchi, Kazuyuki Hirata, Makoto Shiozaki, Shintaro Hirashima, Masayuki Kotoku, Takayuki Yamaguchi, Yoshiaki Katsuda, Ruo Steensma, Xioalin Li, Haiyan Tao, Bruno Tse, Morgan Fenn, Robert Babine, Erin Bradley, Paul Crowe, Scott Thacher, Tsuyoshi Adachi, Masafumi Kamada
Retinoid-related orphan receptor gamma (RORγ) directly controls the differentiation of Th17 cell and the production of interleukin-17, which plays an integral role in autoimmune diseases. To obtain insight into RORγ, we have determined the first crystal structure of a ternary complex containing RORγ ligand-binding domain (LBD) bound with a novel synthetic inhibitor and a repressor peptide, 22-mer peptide from silencing mediator of retinoic acid and thyroid hormone receptor (SMRT). Comparison of a binary complex of nonliganded (apo) RORγ-LBD with a nuclear receptor co-activator (NCoA-1) peptide has shown that our inhibitor displays a unique mechanism different from those caused by natural inhibitor, ursolic acid (UA)...
May 11, 2017: Genes to Cells: Devoted to Molecular & Cellular Mechanisms
https://www.readbyqxmd.com/read/28492484/the-potential-of-triterpenoids-from-loquat-leaves-eriobotrya-japonica-for-prevention-and-treatment-of-skin-disorder
#6
Hui Tan, Tamrakar Sonam, Kuniyoshi Shimizu
The leaves of loquat (Eriobotrya japonica) possess high medicinal value and have been used as traditional medicines. However, there are no evidence-based studies on the skin-care effects of E. japonica leaves. To explore new biological activities of E. japonica leaves against skin disorder and to gain a better understanding of the chemical components associated with bioactivities, we evaluated 18 triterpenoids from E. japonica leaves on anti-melanogenesis, anti-acne, anti-allergy and anti-aging activities. Our results revealed that eight compounds showed anti-melanogenesis activity, of which ursolic acid (1) and maslinic acid (7) were the most potent with the similar selective index to that of arbutin...
May 11, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28474555/isolated-compounds-from-natural-products-with-potential-antidiabetic-activity-a-systematic-review
#7
Antonio C M Munhoz, Tânia S Fröde
BACKGROUND: Worldwide, Type 2 diabetes has become a growing health problem. While many research articles in the field of ethnopharmacology have focused on the antidiabetic properties of medicinal plant species, insufficient evidence remains regarding their therapeutic use. Studies using both in vitro and in vivo models are necessary to evaluate various medicinal plants species, used in folk medicine, by using scientific criteria. METHODS: This review focuses on isolated compounds from medicinal plant species that have reported antidiabetic activity in diabetes models...
May 5, 2017: Current Diabetes Reviews
https://www.readbyqxmd.com/read/28465178/oral-delivery-of-ursolic-acid-loaded-nanostructured-lipid-carrier-coated-with-chitosan-oligosaccharides-development-characterization-in-vitro-and-in-vivo-assessment-for-the-therapy-of-leishmaniasis
#8
Suman Das, Santanu Ghosh, Asit Kumar De, Tanmoy Bera
Visceral leishmaniasis (VL) is a life-threatening disease caused by Leishmania donovani due to uncontrolled parasitisation of liver, spleen, and bone marrow. Ursolic acid (UA), a promising anti-inflammatory, anti-bacterial and anti-diabetic drug used successfully for treatment of ailments. Development of new delivery system is extremely urgent for UA with better efficacy and fewer side effects. The aim of present research work was to formulate and evaluate the potential anti-leishmanial activity of UA loaded N-octyl-chitosan surface decorated nanostructured lipid carrier system (UA-NLC) for delivery to the macrophages for VL...
April 29, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28454670/structure-related-protein-tyrosine-phosphatase-1b-inhibition-by-naringenin-derivatives
#9
Hyun Ah Jung, Pradeep Paudel, Su Hui Seong, Byung-Sun Min, Jae Sue Choi
Naturally occurring flavonoids co-exist as glycoside conjugates, which dominate aglycones in their content. To unveil the structure-activity relationship of a naturally occurring flavonoid, we investigated the effects of the glycosylation of naringenin on the inhibition of enzyme systems related to diabetes (protein tyrosine phosphatase 1B (PTP1B) and α-glycosidase) and on glucose uptake in the insulin-resistant state. Among the tested naringenin derivatives, prunin, a single-glucose-containing flavanone glycoside, potently inhibited PTP1B with an IC50 value of 17...
April 18, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28433520/corrigendum-to-therapeutic-effect-of-ursolic-acid-in-experimental-visceral-leishmaniasis-int-j-parasitol-drugs-drug-resist-7-2017-1-11
#10
Jessica A Jesus, Thais N Fragoso, Eduardo S Yamamoto, Marcia D Laurenti, Marcelo S Silva, Aurea F Ferreira, João Henrique G Lago, Gabriela Santos-Gomes, Luiz Felipe D Passero
No abstract text is available yet for this article.
April 4, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/28427811/new-derivatives-of-ursolic-acid-through-the-biotransformation-by-bacillus-megaterium-cgmcc-1-1741-as-inhibitors-on-nitric-oxide-production
#11
Chao Zhang, Shao-Hua Xu, Bai-Ling Ma, Wei-Wei Wang, Bo-Yang Yu, Jian Zhang
Microbial transformation of ursolic acid (1) by Bacillus megaterium CGMCC 1.1741 was investigated and yielded five metabolites identified as 3-oxo-urs-12-en-28-oic acid (2); 1β,11α-dihydroxy-3-oxo-urs-12-en-28-oic acid (3); 1β-hydroxy-3-oxo-urs-12-en-28, 13-lactoe (4); 1β,3β, 11α-trihydroxyurs-12-en-28-oic acid (5) and 1β,11α-dihydroxy-3-oxo-urs-12-en-28-O-β-d-glucopyranoside (6). Metabolites 3, 4, 5 and 6 were new natural products. Their nitric oxide (NO) production inhibitory activity was assessed in lipopolysaccharide (LPS) - stimulated RAW 264...
March 27, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28423086/evaluation-of-cytogenotoxicity-antioxidant-and-hypoglycemiant-activities-of-isolate-compounds-from-mansoa-hirsuta-d-c-bignoniaceae
#12
Joquebede R Pereira, Raphael F Queiroz, Erlânia A DE Siqueira, Ana Christina Brasileiro-Vidal, Antônio E G Sant'ana, Daniel M Silva, Paulo R A DE Mello Affonso
Mansoa hirsuta (Bignoniaceae) is a native plant from caatinga in Brazilian semiarid. This plant has been locally used as antimicrobial and hypoglycemiant agents, but their action mechanisms and toxicity remain largely unknown. Therefore, we evaluated the composition and antioxidant, cytoprotective and hypoglycemiant effects of raw extract, fractions and compounds from leaves of M. hirsuta. The cytogenotoxic effects of ursolic and oleanolic acids, the main phytotherapic components of this plant, were assessed...
January 2017: Anais da Academia Brasileira de Ciências
https://www.readbyqxmd.com/read/28420354/therapeutic-potentials-of-crataegus-azarolus-var-eu-azarolus-maire-leaves-and-its-isolated-compounds
#13
Eman Abu-Gharbieh, Naglaa Gamil Shehab
BACKGROUND: Hyperglycemia is a complicated condition accompanied with high incidence of infection and dyslipidemia. This study aimed to explore the phyto-constituents of Crataegus azarolus var. eu- azarolus Maire leaves, and to evaluate the therapeutic potentials particularly antimicrobial, antihyperglycemic and antihyperlipidemic of the extract and the isolated compound (3β-O-acetyl ursolic acid). METHODS: Total phenolics and flavonoidal contents were measured by RP-HPLC analysis...
April 18, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28412913/anti-carcinogenic-effects-of-carnosol-an-updated-review
#14
Saeed Samarghandian, Mohsen Azimi-Nezahad, Tahereh Farkhondeh
BACKGROUND: Despite the newly treatment procedures, cancer is considered as the main health threat nowadays and, therefore, new therapeutic options such as traditional medicine should be investigated. Rosemary (Rosmarinus officinalis L.) has been found to possess antitumor effects due to its major ingredients, including carnosic acid, carnosol, ursolic acid, and rosmarinic acid. OBJECTIVE: This study was designed to gather the recent literature findings from 2010 to 2016 on the cancer anti-tumor activities of carnosol and probably involved mechanisms...
April 13, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28372473/selection-of-chemical-markers-for-the-quality-control-of-medicinal-plants-of-the-genus-cecropia
#15
Andrés Rivera-Mondragón, Orlando O Ortíz, Sebastiaan Bijttebier, Arnold Vlietinck, Sandra Apers, Luc Pieters, Catherina Caballero-George
CONTEXT: Several Cecropia (Cecropiaceae) species are traditionally used in Latin America for the treatment of a variety of diseases including diabetes, arterial hypertension, asthma, bronchitis, anxiety, and inflammation. At present, a number of commercial products based on these plants have been introduced into the market with very little information on methods for guaranteeing their quality and safety. OBJECTIVE: This work proposes potential chemical markers for the quality control of the raw materials of Cecropia obtusifolia Bertol...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28358057/synthesis-and-biological-evaluation-of-novel-ursolic-acid-analogues-as-potential-%C3%AE-glucosidase-inhibitors
#16
Pan-Pan Wu, Bing-Jie Zhang, Xi-Ping Cui, Yang Yang, Zheng-Yun Jiang, Zhi-Hong Zhou, Ying-Ying Zhong, Yu-Ying Mai, Zhong Ouyang, Hui-Sheng Chen, Jie Zheng, Su-Qing Zhao, Kun Zhang
Ursolic acid (UA) is a major pentacyclic triterpenoid in plants, vegetables and fruits, which has been reported to have a potential anti-diabetic activity. Despite various semi-synthetic ursolic acid derivatives already described, new derivatives still need to be designed and synthesized to further improve the anti-diabetic activity. In the present study, two series of novel UA derivatives, were synthesized and their structures were confirmed. The enzyme inhibition activities of semi-synthesized analogues against α-glucosidase were screened in vitro...
March 30, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28356955/ursolic-acid-sensitizes-radioresistant-nsclc-cells-expressing-hif-1%C3%AE-through-reducing-endogenous-gsh-and-inhibiting-hif-1%C3%AE
#17
Bing Song, Qian Zhang, Maohu Yu, Xinrong Qi, Gang Wang, Linlin Xiao, Qiyi Yi, Wensen Jin
In previous studies, the present authors demonstrated that effective sensitization of ionizing radiation-induced death of tumor cells, including non-small cell lung cancer (NSCLC) cells, could be produced by oleanolic acid (OA), a pentacyclic triterpenoid present in plants. In the present study, it was investigated whether ursolic acid (UA), an isomer of OA, had also the capacity of sensitizing radioresistant NSCLC cells. The radioresistant cell line H1299/M-hypoxia inducible factor-1α (HIF-1α) was established by transfection with a recombinant plasmid expressing mutant HIF-1α (M-HIF-1α)...
February 2017: Oncology Letters
https://www.readbyqxmd.com/read/28356113/killing-of-serratia-marcescens-biofilms-with-chloramphenicol
#18
Christopher Ray, Anukul T Shenoy, Carlos J Orihuela, Norberto González-Juarbe
Serratia marcescens is a Gram-negative bacterium with proven resistance to multiple antibiotics and causative of catheter-associated infections. Bacterial colonization of catheters mainly involves the formation of biofilm. The objectives of this study were to explore the susceptibility of S. marcescens biofilms to high doses of common antibiotics and non-antimicrobial agents. Biofilms formed by a clinical isolate of S. marcescens were treated with ceftriaxone, kanamycin, gentamicin, and chloramphenicol at doses corresponding to 10, 100 and 1000 times their planktonic minimum inhibitory concentration...
March 29, 2017: Annals of Clinical Microbiology and Antimicrobials
https://www.readbyqxmd.com/read/28347799/ursolic-acid-attenuates-cigarette-smoke-induced-emphysema-in-rats-by-regulating-perk-and-nrf2-pathways
#19
Lin Li, Yan Yin, Gang Hou, Dan Han, Jian Kang, Qiuyue Wang
OBJECTIVE: Ursolic acid (UA) is widely distributed in natural plants to against oxidation, virus, inflammation, tumor, and has been widely used in the pharmaceutical and cosmetics. However, its effect on emphysema of chronic obstructive pulmonary disease (COPD) is unknown. Unfolded protein response is involved in pathogenesis of COPD through PERK pathway. Nuclear erythroid-related factor 2 (Nrf2) regulates antioxidant defensive mechanism in COPD. This study was to explore effect and mechanism of UA on cigarette smoke (CS)-induced rat emphysema...
March 24, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28347227/comparative-proteomics-network-analysis-of-proteins-responsible-for-ursolic-acid-induced-cytotoxicity-in-colorectal-cancer-cells
#20
Qiaoyan Cai, Jing Lin, Ling Zhang, Jiumao Lin, Lili Wang, Daxin Chen, Jun Peng
Ursolic acid is a key active compound present in many medicinal herbs that have been widely used in traditional Chinese medicine for the clinical treatment of various cancers. However, the precise mechanisms of its antitumor activity have been poorly understood. To identify the cellular targets of ursolic acid, two-dimensional gel electrophoresis combined with mass spectrometry was performed in this study, which identified 15 proteins with significantly altered levels in protein expression. This demonstrated that ursolic acid-induced cytotoxicity in colorectal cancer cells involves dysregulation in protein folding, signal transduction, cell proliferation, cell cycle, and apoptosis...
March 2017: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
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