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Ursolic acid AND diabetes

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https://www.readbyqxmd.com/read/29745030/synthesis-and-biological-evaluation-of-novel-n-aryl-%C3%AF-benzoazol-2-yl-sulfanylalkanamides-as-dual-inhibitors-of-%C3%AE-glucosidase-and-protein-tyrosine-phosphatase-1b
#1
Mei-Yan Wang, Xian-Chao Cheng, Xiu-Bo Chen, Yu Li, Lan-Lan Zang, Yu-Qing Duan, Ming-Zhu Chen, Peng Yu, Hua Sun, Run-Ling Wang
α-Glucosidase is known to catalyze the digestion of carbohydrates and release free glucose into the digestive tract. Protein tyrosine phosphatase 1B (PTP1B) is engaged in the dephosphorylation of the insulin receptor and regulation of insulin sensitivity. Therefore, dual antagonists by targeting both α-glucosidase and PTP1B may be potential candidates for type 2 diabetes therapy. In this work, three series of novel N-aryl-ω-(benzoazol-2-yl)-sulfanylalkanamides were synthesized and assayed for their α-glucosidase and PTP1B inhibitory activities, respectively...
May 9, 2018: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29719446/ursolic-acid-in-health-and-disease
#2
REVIEW
Dae Yun Seo, Sung Ryul Lee, Jun-Won Heo, Mi-Hyun No, Byoung Doo Rhee, Kyung Soo Ko, Hyo-Bum Kwak, Jin Han
Ursolic acid (UA) is a natural triterpene compound found in various fruits and vegetables. There is a growing interest in UA because of its beneficial effects, which include anti-inflammatory, anti-oxidant, anti-apoptotic, and anti-carcinogenic effects. It exerts these effects in various tissues and organs: by suppressing nuclear factor-kappa B signaling in cancer cells, improving insulin signaling in adipose tissues, reducing the expression of markers of cardiac damage in the heart, decreasing inflammation and increasing the level of anti-oxidants in the brain, reducing apoptotic signaling and the level of oxidants in the liver, and reducing atrophy and increasing the expression levels of adenosine monophosphate-activated protein kinase and irisin in skeletal muscles...
May 2018: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/29677678/%C3%AE-glucosidase-enzyme-inhibitory-effects-and-ursolic-and-oleanolic-acid-contents-of-fourteen-anatolian-salvia-species
#3
Zeynep Kalaycıoğlu, Sesil Uzaşçı, Tuncay Dirmenci, F Bedia Erim
During the last decade, ursolic and oleanolic acids have been of considerable interest because of their α-glucosidase inhibitory activities and potential effects for treatment of type 2 diabetes. A simple and sensitive reversed-phase HPLC method was developed for the simultaneous determination of ursolic acid and oleanolic acid. The optimal mobile phase was selected as 85% acetonitrile solution. The limit of detection of the method for ursolic acid and oleanolic acid were 14 ng mL-1 and 13 ng mL-1 , respectively...
April 11, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29380400/ursolic-acid-derivatives-as-potential-antidiabetic-agents-in-vitro-in-vivo-and-in-silico-studies
#4
Ricardo Guzmán-Ávila, Virginia Flores-Morales, Paolo Paoli, Guido Camici, Juan José Ramírez-Espinosa, Litzia Cerón-Romero, Gabriel Navarrete-Vázquez, Sergio Hidalgo-Figueroa, Maria Yolanda Rios, Rafael Villalobos-Molina, Samuel Estrada-Soto
Hit, Lead & Candidate Discovery Protein tyrosine phosphatase 1B (PTP-1B) has attracted interest as a novel target for the treatment of type 2 diabetes, this because its role in the insulin-signaling pathway as a negative regulator. Thus, the aim of current work was to obtain seven ursolic acid derivatives as potential antidiabetic agents with PTP-1B inhibition as main mechanism of action. Furthermore, derivatives 1-7 were submitted in vitro to enzymatic PTP-1B inhibition being 3, 5, and 7 the most active compounds (IC50  = 5...
March 2018: Drug Development Research
https://www.readbyqxmd.com/read/29156537/ursolic-acid-ameliorates-oxidative-stress-inflammation-and-fibrosis-in-diabetic-cardiomyopathy-rats
#5
Xu-Tao Wang, Yan Gong, Bin Zhou, Jun-Jie Yang, Yin Cheng, Jin-Guo Zhao, Min-You Qi
Diabetic cardiomyopathy is a major and severe cardiovascular complication of diabetes mellitus. Ursolic acid, a pentacyclic triterpene compound widespread in fruits and plants, performs a variety of pharmacological activities including lowering blood glucose, anti-oxidation, anti-inflammation and anti-fibrosis. Our present study aimed to investigate the cardioprotective effects of ursolic acid on diabetic cardiomyopathy rats and uncover its underlying mechanism. Diabetes mellitus was induced by a single injection of STZ-only (40 mg/ kg, i...
January 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29098660/therapeutic-potential-of-ursolic-acid-to-manage-neurodegenerative-and-psychiatric-diseases
#6
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...
December 2017: CNS Drugs
https://www.readbyqxmd.com/read/29030193/inhibitory-mechanism-of-two-allosteric-inhibitors-oleanolic-acid-and-ursolic-acid-on-%C3%AE-glucosidase
#7
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...
February 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28964635/pentacyclic-triterpenes-as-%C3%AE-glucosidase-and-%C3%AE-amylase-inhibitors-structure-activity-relationships-and-the-synergism-with-acarbose
#8
Bo-Wei Zhang, Yan Xing, Chen Wen, Xiao-Xia Yu, Wen-Long Sun, Zhi-Long Xiu, Yue-Sheng Dong
In this paper, the inhibition of α-amylase and α-glucosidase by nine pentacyclic triterpenes was determined. For α-amylase inhibitory activity, the IC50 values of ursolic acid, corosolic acid, and oleanolic acid were 22.6±2.4μM, 31.2±3.4μM, and 94.1±6.7μM, respectively. For α-glucosidase inhibition, the IC50 values of ursolic acid, corosolic acid, betulinic acid, and oleanolic acid were 12.1±1.0μM, 17.2±0.9μM, 14.9±1.9μM, and 35.6±2.6μM, respectively. The combination of corosolic acid and oleanolic acid with acarbose showed synergistic inhibition against α-amylase...
November 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28872612/fructus-ligustri-lucidi-in-osteoporosis-a-review-of-its-pharmacology-phytochemistry-pharmacokinetics-and-safety
#9
REVIEW
Beibei Chen, Lili Wang, Lin Li, Ruyuan Zhu, Haixia Liu, Chenyue Liu, Rufeng Ma, Qiangqiang Jia, Dandan Zhao, Jianzhao Niu, Min Fu, Sihua Gao, Dongwei Zhang
Background: Fructus Ligustri Lucidi (FLL) has now attracted increasing attention as an alternative medicine in the prevention and treatment of osteoporosis. This study aimed to provide a general review of traditional interpretation of the actions of FLL in osteoporosis, main phytochemical constituents, pharmacokinetics, pharmacology in bone improving effect, and safety. Materials and Methods: Several databases, including PubMed, China National Knowledge Infrastructure, National Science and Technology Library, China Science and Technology Journal Database, and Web of Science were consulted to locate publications pertaining to FLL...
September 5, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28769799/allspice-and-clove-as-source-of-triterpene-acids-activating-the-g-protein-coupled-bile-acid-receptor-tgr5
#10
Angela Ladurner, Martin Zehl, Ulrike Grienke, Christoph Hofstadler, Nadina Faur, Fátima C Pereira, David Berry, Verena M Dirsch, Judith M Rollinger
Worldwide, metabolic diseases such as obesity and type 2 diabetes have reached epidemic proportions. A major regulator of metabolic processes that gained interest in recent years is the bile acid receptor TGR5 (Takeda G protein-coupled receptor 5). This G protein-coupled membrane receptor can be found predominantly in the intestine, where it is mainly responsible for the secretion of the incretins glucagon-like peptide 1 (GLP-1) and peptide YY (PYY). The aim of this study was (i) to identify plant extracts with TGR5-activating potential, (ii) to narrow down their activity to the responsible constituents, and (iii) to assess whether the intestinal microbiota produces transformed metabolites with a different activity profile...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28756460/ursolic-acid-activates-the-tgr5-receptor-to-enhance-glp-1-secretion-in-type-1-like-diabetic-rats
#11
Shih-Hsiang Lo, Yingxiao Li, Kai Chun Cheng, Chiang-Shan Niu, Juei-Tang Cheng, Ho-Shan Niu
Endogenous Takeda G-protein-coupled receptor 5 (TGR5), G-protein-coupled bile acid receptor 1 (GPBAR1), regulates glucose metabolism. In animals, TGR5 activation by a chemical agonist may increase incretin secretion and reduce the blood sugar level. Recently, betulinic acid has been suggested to activate TGR5. Ursolic acid is a well-known pentacyclic triterpenoid that is similar to betulinic acid. It is of special interest to determine the potential effect of ursolic acid on TGR5. Therefore, we transfected cultured Chinese hamster ovary (CHO-K1) cells with the TGR5 gene...
November 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28637397/ursolic-acid-derivatives-for-pharmaceutical-use-a-patent-review-2012-2016
#12
REVIEW
Hidayat Hussain, Ivan R Green, Iftikhar Ali, Ikhlas A Khan, Zulfiqar Ali, Abdullah M Al-Sadi, Ishtiaq Ahmed
Ursolic acid (UA), belongs to a group of pentacyclic triterpenoids and is known to possess some very interesting biological properties. Protocols have been developed in order to synthesize bioactive UA analogs which have resulted in numerous ursolic acid analogs being synthesized during the period 2012-2016. Ursolic acid and its analogues can be employed to treat various cancers, inflammatory diseases, diabetes, Parkinson's disease, Alzheimer's disease, hepatitis B, hepatitis C and AIDS to mention but a few...
September 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28474555/isolated-compounds-from-natural-products-with-potential-antidiabetic-activity-a-systematic-review
#13
Antonio C M Munhoz, Tania S Frode
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...
2018: 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
#14
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...
September 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28454670/structure-related-protein-tyrosine-phosphatase-1b-inhibition-by-naringenin-derivatives
#15
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...
June 1, 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
#16
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/28372473/selection-of-chemical-markers-for-the-quality-control-of-medicinal-plants-of-the-genus-cecropia
#17
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
#18
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/28318895/competitive-protein-tyrosine-phosphatase-1b-ptp1b-inhibitors-prenylated-caged-xanthones-from-garcinia-hanburyi-and-their-inhibitory-mechanism
#19
Xue Fei Tan, Zia Uddin, Chanin Park, Yeong Hun Song, Minky Son, Keun Woo Lee, Ki Hun Park
Protein tyrosine phosphatase 1B (PTP1B) plays important role in diabetes, obesity and cancer. The methanol extract of the gum resin of Garcinia hanburyi (G. hanburyi) showed potent PTP1B inhibition at 10µg/ml. The active compounds were identified as prenylated caged xanthones (1-9) which inhibited PTP1B in dose-dependent manner. Carboxybutenyl group within caged motif (A ring) was found to play a critical role in enzyme inhibition such as 1-6 (IC50 s=0.47-4.69µM), whereas compounds having hydroxymethylbutenyl 7 (IC50 =70...
April 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27927056/bioassay-guided-fractionation-and-identification-of-%C3%AE-amylase-inhibitors-from-syzygium-cumini-leaves
#20
Jeyakumaran Poongunran, Handunge Kumudu Irani Perera, Lalith Jayasinghe, Irushika Thushari Fernando, Ramaiah Sivakanesan, Hiroshi Araya, Yoshinori Fujimoto
CONTEXT: Pancreatic α-amylase and α-glucosidase inhibitors serve as important strategies in the management of blood glucose. Even though Syzygium cumini (L.) Skeels (Myrtaceae) (SC) is used extensively to treat diabetes; scientific evidence on antidiabetic effects of SC leaves is scarce. OBJECTIVE: SC leaf extract was investigated for α-amylase inhibitory effect and continued with isolation and identification of α-amylase inhibitors. MATERIALS AND METHODS: Bioassay-guided fractionation was conducted using in vitro α-amylase inhibitory assay (with 20-1000 μg/mL test material) to isolate the inhibitory compounds from ethyl acetate extract of SC leaves...
December 2017: Pharmaceutical Biology
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