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quercetin, curcumin

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https://www.readbyqxmd.com/read/28484911/molecular-cloning-and-expression-of-a-glycosyltransferase-from-bacillus-subtilis-for-modification-of-morin-and-related-polyphenols
#1
Qianqian Wang, Yixiang Xu, Jiaqi Xu, Xudong Wang, Chen Shen, Yan Zhang, Xiufeng Liu, Boyang Yu, Jian Zhang
OBJECTIVES: To characterize glycosyltransferases from Bacillus subtilis ATCC 6633 and investigate their substrate specificity towards plant polyphenols. RESULTS: Among the cloned and expressed six UDP-glycosyltransferases (BsGT1-6), BsGT-1 showed activity with a wide range of polyphenols: morin, quercetin, alizarin, rehin, curcumin and aloe emodin. The gene of BsGT-1 has an ORF of 1206 bp encoding 402 amino acids. The recombinant enzyme was purified to homogeneity by Ni-NTA affinity chromatograph, and its biochemical characteristics were identified by HPLC-UV/MS, (1)H-NMR and (13)C-NMR...
May 8, 2017: Biotechnology Letters
https://www.readbyqxmd.com/read/28470323/differential-%C3%AE-amylase-%C3%AE-glucosidase-inhibitory-activities-of-plant-derived-phenolic-compounds-a-virtual-screening-perspective-for-the-treatment-of-obesity-and-diabetes
#2
Hassan Rasouli, Seyed Mohammad-Bagher Hosseini-Ghazvini, Hadi Adibi, Reza Khodarahmi
Recently, due to their biological properties, polyphenol-rich functional foods have been proposed to be unique supplementary and nutraceutical treatments for diabetes mellitus. Inhibition of α-amylase and α-glucosidase enzymes using natural products (especially polyphenols) is a novel oral policy to regulate carbohydrate metabolism and hyperglycemia. The present study aims to evaluate the α-amylase and α-glucosidase inhibitory activity of 26 polyphenols using molecular docking and virtual screening studies...
May 4, 2017: Food & Function
https://www.readbyqxmd.com/read/28435252/polyphenol-nanoformulations-for-cancer-therapy-experimental-evidence-and-clinical-perspective
#3
REVIEW
Yasamin Davatgaran-Taghipour, Salar Masoomzadeh, Mohammad Hosein Farzaei, Roodabeh Bahramsoltani, Zahra Karimi-Soureh, Roja Rahimi, Mohammad Abdollahi
Cancer is defined as the abnormal cell growth that can cause life-threatening malignancies with high financial costs for patients as well as the health care system. Natural polyphenols have long been used for the prevention and treatment of several disorders due to their antioxidant, anti-inflammatory, cytotoxic, antineoplastic, and immunomodulatory effects discussed in the literature; thus, these phytochemicals are potentially able to act as chemopreventive and chemotherapeutic agents in different types of cancer...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28420097/synthesis-of-curcuminoids-and-evaluation-of-their-cytotoxic-and-antioxidant-properties
#4
María Concepción Lozada-García, Raúl G Enríquez, Teresa O Ramírez-Apán, Antonio Nieto-Camacho, Juan Francisco Palacios-Espinosa, Zeltzin Custodio-Galván, Olivia Soria-Arteche, Jaime Pérez-Villanueva
Curcumin (1) and ten derivatives (2-11) were synthesized and evaluated as cytotoxic and antioxidant agents. The results of primary screening by Sulforhodamine B assay against five human cancer cell lines (U-251 MG, glioblastoma; PC-3, human prostatic; HCT-15, human colorectal; K562, human chronic myelogenous leukemia; and SKLU-1, non-small cell lung cancer) allowed us to calculate the half maximal inhibitory concentration (IC50) values for the more active compounds against HCT-15 and K562 cell lines. Compounds 2 and 10 were the most active against both cell lines and were more active than curcumin itself...
April 14, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28345531/polyphenols-in-preventing-endothelial-dysfunction
#5
Sylwia Biegańska-Hensoldt, Danuta Rosołowska-Huszcz
One of the main causes of mortality in developed countries is atherosclerosis. The pathogenesis of atherosclerosis is associated with endothelial dysfunction. Consumption of food rich in natural antioxidants including polyphenols significantly improves endothelial cells functions. Polyphenols have a beneficial effect on the human body and play an important part in protecting the cardiovascular system. Polyphenols present in food have antioxidant, anti-inflammatory, antihypertensive, antithrombotic and antiproliferative properties...
March 27, 2017: Postȩpy Higieny i Medycyny Doświadczalnej
https://www.readbyqxmd.com/read/28217823/novel-insight-from-computational-virtual-screening-depict-the-binding-potential-of-selected-phytotherapeutics-against-probable-drug-targets-of-clostridium-difficile
#6
Suman Kamath, Sinosh Skariyachan
This study explores computational screening and molecular docking approaches to screen novel herbal therapeutics against probable drug targets of Clostridium difficile. The essential genes were predicted by comparative genome analysis of C. difficile and best homologous organisms using BLAST search at database of essential genes (DEG). The functions of these genes in various metabolic pathways were predicted and some of these genes were considered as potential targets. Three major proteins were selected as putative targets, namely permease IIC component, ABC transporter and histidine kinase...
February 20, 2017: Interdisciplinary Sciences, Computational Life Sciences
https://www.readbyqxmd.com/read/28183265/some-important-dietary-polyphenolic-compounds-an-anti-inflammatory-and-immunoregulatory-perspective
#7
Mayank Kinger, Sushil Kumar, Vinod Kumar
Inflammation plays an important role in maintaining the body's homeostasis. It repairs the damaged tissues of the body resulting from injury or infection. In addition, a diverse array of diseases like hepatitis, arthritis and colitis has been reported and described to be associated with inflammatory processes. Some autoimmune diseases like inflammatory bowel disease (IBD) emerge by the influence of numerous genes in complex environmental situations belongs to inflammation. The currently available processes for curing inflammation and related disorders facilitate the use of non steroidal anti-inflammatory drugs (NSAIDs)...
February 8, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28178749/improving-on-nature-the-role-of-nanomedicine-in-the-development-of-clinical-natural-drugs
#8
REVIEW
Anna Rita Bilia, Vieri Piazzini, Clizia Guccione, Laura Risaliti, Martina Asprea, Giada Capecchi, Maria Camilla Bergonzi
Natural products have been used as a major source of drugs for millennia, and about half of the pharmaceuticals in use today are derived from natural products. However, their efficacy can be limited because of their low hydrophilicity and intrinsic dissolution rate(s), or physical/chemical instability. In addition, they can present scarce absorption, poor pharmacokinetics and bioavailability, scarce biodistribution, first-pass metabolism, trivial penetration and accumulation in the organs of the body, or low targeting efficacy...
March 2017: Planta Medica
https://www.readbyqxmd.com/read/28137215/targeting-cancer-stem-cells-for-chemoprevention-of-pancreatic-cancer
#9
Dharmalingam Subramaniam, Gaurav Kaushik, Prasad Dandawate, Shrikant Anant
Pancreatic ductal adenocarcinoma is one of the deadliest cancers worldwide and the fourth leading cause of cancer-related deaths in United States. Regardless of the advances in molecular pathogenesis and consequential efforts to suppress the disease, this cancer remains a major health problem in United States. By 2030, the projection is that pancreatic cancer will be climb up to be the second leading cause of cancer-related deaths in the United States. Pancreatic cancer is a rapidly invasive and highly metastatic cancer, and does not respond to standard therapies...
January 26, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28128562/combined-in-vitro-cell-based-in-silico-screening-of-naturally-occurring-flavonoids-and-phenolic-compounds-as-potential-anti-alzheimer-drugs
#10
Alba Espargaró, Tiziana Ginex, Maria Del Mar Vadell, Maria A Busquets, Joan Estelrich, Diego Muñoz-Torrero, F Javier Luque, Raimon Sabate
Alzheimer's disease (AD) is the main cause of dementia in people over 65 years. One of the major culprits in AD is the self-aggregation of amyloid-β peptide (Aβ), which has stimulated the search for small molecules able to inhibit Aβ aggregation. In this context, we recently reported a simple, but effective in vitro cell-based assay to evaluate the potential antiaggregation activity of putative Aβ aggregation inhibitors. In this work this assay was used together with docking and molecular dynamics simulations to analyze the anti-Aβ aggregation activity of several naturally occurring flavonoids and phenolic compounds...
February 24, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28124813/synthesis-of-quercetin-imprinted-polymer-spherical-particles-with-improved-ability-to-capture-quercetin-analogues
#11
Antonelle Pardo, Thomas Josse, Laetitia Mespouille, Bertrand Blankert, Philippe Dubois, Pierre Duez
INTRODUCTION: Molecularly imprinted polymers (MIPs) are composed of specific cavities able to selectively recognise a template molecule. Used as chromatographic sorbents, MIPs may not trap related structures due to the high rigidity of their cross-linking. OBJECTIVE: To improve the capture of quercetin analogues by modulating the synthesis strategy for a quercetin-imprinted polymer (Qu MIP). METHODOLOGY: An additional comonomer bearing a short oligoethylene glycol (OEG) unit was used to prepare a Qu MIP that was compared to a traditional one formulated in a similar fashion, but without the OEG-comonomer...
January 26, 2017: Phytochemical Analysis: PCA
https://www.readbyqxmd.com/read/28101199/ultrastructural-changes-during-lung-carcinogenesis-modulation-by-curcumin-and-quercetin
#12
Xin Wang, Lei Wang, Hao Zhang, Ke Li, Jiqin You
The aim of the present study was to examine the effectiveness of curcumin and quercetin in modulating ultrastructural changes during lung carcinogenesis. A total of 24 male laka mice were divided into the normal control, benzo[a]pyrene (BP)-treated, BP+curcumin-treated, BP+quercetin- treated, and BP+curcumin+quercetin-treated groups (n=6 per group). Lung carcinogenesis was induced by a single intraperitoneal injection of BP [100 mg/kg of body weight (b.wt.)]. Curcumin was supplemented to mice at a dose level of 60 mg/kg of b...
December 2016: Oncology Letters
https://www.readbyqxmd.com/read/28063518/role-of-nutraceutical-sirt1-modulators-in-ampk-and-mtor-pathway-evidence-of-a-synergistic-effect
#13
Luca Giovannini, Sara Bianchi
OBJECTIVE: The aim of this study was to evaluate the effect of different natural substances on SIRT1 expression and on AMPK and mTOR phosphorylation. Moreover, we investigated the presence of a synergistic effect between the substances. METHODS: Human cervical carcinoma cells were seeded in 12-well plates, then incubated with the nine tested substances (resveratrol, quercetin, berberine, catechin, tyrosol, ferulic acid, niclosamide, curcumin, and malvidin) at different concentrations and left in incubation for 3, 6, and 24 h...
February 2017: Nutrition
https://www.readbyqxmd.com/read/28025942/nano-medicine-improving-the-bioavailability-of-small-molecules-for-the-prevention-of-neurodegenerative-diseases
#14
Piera Di Martino, Roberta Censi, Maria Rosa Gigliobianco, Luana Zerrillo, Federico Magnoni, Dimitrios Agas, Wilma Quaglia, Giulio Lupidi
Neurodegenerative diseases, including Parkinson's and Alzheimer's, are a heterogeneous group of brain disorders characterized by the progressive degeneration of the structure and function of the central or peripheral nervous system. It is thought that the number of people affected by these pathologies will increase in future decades, particularly in the more economically developed countries, where the populations are experiencing a demographic shift towards older ages. For many of these pathologies, and in particular for Alzheimer's disease, no effective treatments are available, and the consequent economic and social costs are very high...
December 27, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27956075/natural-product-htp-screening-for-attenuation-of-cytokine-induced-neutrophil-chemo-attractants-cincs-and-no2-in-lps-ifn%C3%AE-activated-glioma-cells
#15
Elizabeth A Mazzio, David Bauer, Patricia Mendonca, Equar Taka, Karam F A Soliman
Chronic and acute central nervous system (CNS) inflammation are contributors toward neurological injury associated with head trauma, stroke, infection, Parkinsons or Alzheimers disease. CNS inflammatory illnesses can also contribute toward risk of developing glioblastoma multiforme (GBM). With growing public interest in complementary and alternative medicines (CAMs), we conduct a high throughput (HTP) screening of >1400 natural herbs, plants and over the counter (OTC) products for anti-inflammatory effects on lipopolysaccharide (LPS)/interferon gamma (IFNγ) activated C6 glioma cells...
January 15, 2017: Journal of Neuroimmunology
https://www.readbyqxmd.com/read/27925249/inhibition-of-glucuronidation-and-oxidative-metabolism-of-buprenorphine-using-gras-compounds-or-dietary-constituents-supplements-in-vitro-proof-of-concept
#16
Neha V Maharao, Anand A Joshi, Phillip M Gerk
The present study investigated the potential of generally recognized as safe (GRAS) compounds or dietary substances to inhibit the presystemic metabolism of buprenorphine and to increase its oral bioavailability. Using IVIVE, buprenorphine extraction ratios in intestine and liver were predicted as 96% and 71%, respectively. In addition, the relative fraction of buprenorphine metabolized by oxidation and glucuronidation in these two organs was estimated using pooled human intestinal and liver microsomes. In both organs, oxidation appeared to be the major metabolic pathway with a 6 and 4 fold higher intrinsic clearance than glucuronidation in intestine and liver, respectively...
March 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/27774900/phytochemicals-against-advanced-glycation-end-products-ages-and-the-receptor-system
#17
Sho-Ichi Yamagishi, Takanori Matsui, Yuji Ishibashi, Fumiyuki Isami, Yumi Abe, Tatsuya Sakaguchi, Yuichiro Higashimoto
Reducing sugars can react non-enzymatically with amino groups of proteins and lipids to form irreversibly cross-linked macroprotein derivatives called as advanced glycation end products (AGEs). Cross-linking modification of extracellular matrix proteins by AGEs deteriorate their tertiary structural integrity and function, contributing to aging-related organ damage and diabetes-associated complications, such as cardiovascular disease (CVD). Moreover, engagement of receptor for AGEs, RAGE with the ligands evoke oxidative stress generation and inflammatory, thrombotic and fibrotic reactions in various kinds of tissues, further exacerbating the deleterious effects of AGEs on multiple organ systems...
October 21, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27771282/phytochemical-mediated-modulation-of-the-expression-and-transporter-function-of-breast-cancer-resistance-protein-at-the-blood-brain-barrier-an-in-vitro-study
#18
Manjit Kaur, Raj K S Badhan
Clinical translation of BCRP inhibitors have failed due to neurotoxicity and novel approaches are required to identify suitable modulators of BCRP to enhance CNS drug delivery. In this study we examine 18 compounds, primarily phytochemicals, as potential novel modulators of AhR-mediated regulation of BCRP expression and function in immortalised and primary porcine brain microvascular endothelial cells as a mechanism to enhance CNS drug delivery. The majority of modulators possessed a cellular viability IC50 > 100µM in both cell systems...
October 19, 2016: Brain Research
https://www.readbyqxmd.com/read/27681738/the-role-of-bioactive-dietary-components-in-modulating-mirna-expression-in-colorectal-cancer
#19
REVIEW
Laura I Gavrilas, Corina Ionescu, Oana Tudoran, Cosmin Lisencu, Ovidiu Balacescu, Doina Miere
Colorectal cancer is the third most common cancer in the world and considered to be one of the most diet-related types of cancer. Extensive research has been conducted but still the link between diet and colorectal cancer is complex. Recent studies have highlight microRNAs (miRNAs) as key players in cancer-related pathways in the context of dietary modulation. MicroRNAs are involved in most biological processes related to tumor development and progression; therefore, it is of great interest to understand the underlying mechanisms by which dietary patterns and components influence the expression of these powerful molecules in colorectal cancer...
September 26, 2016: Nutrients
https://www.readbyqxmd.com/read/27659301/anti-ageing-active-ingredients-from-herbs-and-nutraceuticals-used-in-traditional-chinese-medicine-pharmacological-mechanisms-and-implications-for-drug-discovery
#20
REVIEW
Chun-Yan Shen, Jian-Guo Jiang, Li Yang, Da-Wei Wang, Wei Zhu
Ageing, an unanswered question in the medical field, is a multifactorial process that results in a progressive functional decline in cells, tissues and organisms. Although it is impossible to prevent ageing, slowing down the rate of ageing is entirely possible to achieve. Traditional Chinese medicine (TCM) is characterized by the nourishing of life and its role in anti-ageing is getting more and more attention. This article summarizes the work done on the natural products from TCM that are reported to have anti-ageing effects, in the past two decades...
June 2017: British Journal of Pharmacology
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