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Curcuminoids

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https://www.readbyqxmd.com/read/28604614/synthesis-and-evaluation-of-curcuminoid-analogues-as-antioxidant-and-antibacterial-agents
#1
Dalia R Emam, Ahmad M Alhajoj, Khaled M Elattar, Nabila A Kheder, Ahmed A Fadda
Diazocoupling reaction of curcumin with different diazonium salts of p-toluidine, 2-aminopyridine, and 4-aminoantipyrine in pyridine yielded the arylhydrazones 2a-c. Arylhydrazone of p-toluidine reacted with urea, thiourea, and guanidine nitrate to produce 5,6-dihydropyrimidines. Further reaction of 2a with 2,3-diaminopyrdine in sodium ethoxide solution yielded 1H-pyrido[2,3-b][1,4]diazepine derivative. Bis(2,5-dihydroisoxazole) is obtained from the reaction of 2a with hydroxylamine hydrochloride, while its reactions with hydrazines afforded the respective 4,5-dihydro-1H-pyrazoles...
June 11, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28601309/the-aryl-hydrocarbon-receptor-as-an-antitumor-target-of-synthetic-curcuminoids-in-colorectal-cancer
#2
Bryant W Megna, Patrick R Carney, Mitchell G Depke, Manabu Nukaya, James McNally, Lesley Larsen, Rhonda J Rosengren, Gregory D Kennedy
BACKGROUND: Curcumin has proven to be a potent antitumor agent in both preclinical and clinical models of colorectal cancer (CRC). It has also been identified as a ligand of the transcription factor known as the aryl hydrocarbon receptor (AHR). Our laboratory has identified the AHR as a mechanism which contributes to both tumorigenesis in a mouse model of inflammatory CRC as well an apoptotic target in vitro. Curcumin's role as an AHR ligand may modulate its effects to induce colon cancer cell death, and this role may be enhanced via structural modification of the curcumin backbone...
June 1, 2017: Journal of Surgical Research
https://www.readbyqxmd.com/read/28587282/curcumin-anti-apoptotic-action-in-a-model-of-intestinal-epithelial-inflammatory-damage
#3
Claudia Loganes, Sara Lega, Matteo Bramuzzo, Liza Vecchi Brumatti, Elisa Piscianz, Erica Valencic, Alberto Tommasini, Annalisa Marcuzzi
The purpose of this study is to determine if a preventive treatment with curcumin can protect intestinal epithelial cells from inflammatory damage induced by IFNγ. To achieve this goal we have used a human intestinal epithelial cell line (HT29) treated with IFNγ to undergo apoptotic changes that can reproduce the damage of intestinal epithelia exposed to inflammatory cytokines. In this model, we measured the effect of curcumin (curcuminoid from Curcuma Longa) added as a pre-treatment at different time intervals before stimulation with IFNγ...
June 6, 2017: Nutrients
https://www.readbyqxmd.com/read/28579928/single-cell-amperometry-reveals-curcuminoids-modulate-the-release-of-neurotransmitters-during-exocytosis-from-pc12-cells
#4
Xianchan Li, Amir Saeid Mohammadi, Andrew G Ewing
We used single cell amperometry to examine whether curcumin and bisdemethoxycurcumin (BDMC), substances that are suggested to affect learning and memory, can modulate monoamine release from PC12 cells. Our results indicate both curcumin and BDMC need long-term treatment (72 h in this study) to influence exocytosis effectively. By analyzing the parameters calculated from single exocytosis events, it can be concluded that curcumin and BDMC affect exocytosis through different mechanisms. Curcumin accelerates the event dynamics with no significant change of the monoamine amount released from single exocytotic events, whereas BDMC attenuates the amount from single exocytotic event with no significant change of the event dynamics...
November 15, 2016: Journal of Electroanalytical Chemistry
https://www.readbyqxmd.com/read/28571271/evaluation-of-efficacy-of-1-curcuminoids-as-local-application-in-management-of-oral-lichen-planus-interventional-study
#5
Anju Elizabeth Thomas, Beena Varma, Seema Kurup, Renju Jose, Marina Lazar Chandy, Sreeja P Kumar, M S Aravind, Athira Aruna Ramadas
INTRODUCTION: Oral Lichen Planus (OLP) is a chronic inflammatory mucocutaneous disease affecting the oral cavity which has been associated with severe burning sensation which in turn affects the quality of life of the patients. Currently, the effective treatment of choice remains the use of corticosteroids. The chronicity and recalcitrant nature of the disease demand the long term use of these drugs with ensuing adverse effects. Turmeric and its active ingredient, "curcumin", have been found to have anti-inflammatory, antioxidant and anticancer properties...
April 2017: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/28547897/mannich-curcuminoids-as-potent-anticancer-agents
#6
Márió Gyuris, László Hackler, Lajos I Nagy, Róbert Alföldi, Eszter Rédei, Annamária Marton, Tibor Vellai, Nóra Faragó, Béla Ózsvári, Anasztázia Hetényi, Gábor K Tóth, Péter Sipos, Iván Kanizsai, László G Puskás
A series of novel curcuminoids were synthesised for the first time via a Mannich-3CR/organocatalysed Claisen-Schmidt condensation sequence. Structure-activity relationship (SAR) studies were performed by applying viability assays and holographic microscopic imaging to these curcumin analogues for anti-proliferative activity against A549 and H1975 lung adenocarcinoma cells. The TNFα-induced NF-κB inhibition and autophagy induction effects correlated strongly with the cytotoxic potential of the analogues. Significant inhibition of tumour growth was observed when the most potent analogue 44 was added in liposomes at one-sixth of the maximally tolerated dose in the A549 xenograft model...
May 26, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28538196/self-assembly-of-gd-3-sds-hepes-complex-and-curcumin-entrapment-for-enhanced-stability-fluorescence-image-in-cellular-system
#7
Chonticha Sahub, Gamolwan Tumcharern, Prae Chirawatkul, Vithaya Ruangpornvisuti, Sanong Ekgasit, Supasorn Wanichweacharungruang, Thawatchai Tuntulani, Tanapat Palaga, Boosayarat Tomapatanaget
At present, strategies to disperse hydrophobic molecules in water without altering their chemical structures include conventional surfactant-based micellar and vesicular systems, encapsulation into water dispersible polymeric nanoparticles, and loading onto the surface of various metal nanoparticles. Here, we report a simple and low cost platform to incorporate hydrophobic molecules into a stable water dispersible nanostructure that can significantly increase the stability of the encapsulated materials. The platform is based on the incorporation of hydrophobic molecules into the self-assembled complex of gadolinium ion (Gd(3+)), sodium dodecyl sulfate (SDS), and 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES) called GdSH...
May 13, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28534138/a-chemically-modified-curcumin-cmc-2-24-inhibits-nuclear-factor-%C3%AE%C2%BAb-activation-and-inflammatory-bone-loss-in-murine-models-of-lps-induced-experimental-periodontitis-and-diabetes-associated-natural-periodontitis
#8
Muna S Elburki, Carlos Rossa, Morgana R Guimarães-Stabili, Hsi-Ming Lee, Fabiana A Curylofo-Zotti, Francis Johnson, Lorne M Golub
The purpose of this study was to assess the effect of a novel chemically modified curcumin (CMC 2.24) on NF-κB and MAPK signaling and inflammatory cytokine production in two experimental models of periodontal disease in rats. Experimental model I: Periodontitis was induced by repeated injections of LPS into the gingiva (3×/week, 3 weeks); control rats received vehicle injections. CMC 2.24, or the vehicle, was administered by daily oral gavage for 4 weeks. Experimental model II: Diabetes was induced in adult male rats by streptozotocin injection; periodontal breakdown then results as a complication of uncontrolled hyperglycemia...
May 22, 2017: Inflammation
https://www.readbyqxmd.com/read/28532009/exploring-recent-developments-to-improve-antioxidant-anti-inflammatory-and-antimicrobial-efficacy-of-curcumin-a-review-of-new-trends-and-future-perspectives
#9
REVIEW
Zahid Hussain, Hnin Ei Thu, Muhammad Wahab Amjad, Fahad Hussain, Tarek A Ahmed, Shahzeb Khan
Curcumin derivatives have been well-documented due to their natural antioxidant, antimicrobial and anti-inflammatory activities. Curcuminoids have also gained widespread recognition due to their wide range of other activities which include anti-infective, anti-mutagenic, anticancer, anti-coagulant, antiarthrititc, and wound healing potential. Despite of having a wide range of activities, the inherent physicochemical characteristics (poor water solubility, low bioavailability, chemical instability, photodegradation, rapid metabolism and short half-life) of curcumin derivatives limit their pharmaceutical significance...
August 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28516478/determination-of-oral-bioavailability-of-curcuminoid-dispersions-and-nanoemulsions-prepared-from-curcuma-longa-linnaeus
#10
P S Lu, B S Inbaraj, B H Chen
BACKGROUND: Curcuminoid from Curcuma longa Linnaeus has been demonstrated to be effective in anti-cancer and anti-inflammation. The objectives of this study were to prepare curcuminoid dispersion and nanoemulsion from C. longa and determine their oral bioavailability in rats. RESULTS: After curcuminoid extraction using 99.5% ethanol, bisdemethoxycurcumin (BDMC), demethoxycurcumin (DMC) and curcumin were separated within 10 min by HPLC with an Eclipse XDB-C18 column and a gradient mobile phase of 0...
May 18, 2017: Journal of the Science of Food and Agriculture
https://www.readbyqxmd.com/read/28511061/uptake-of-ga-curcumin-derivatives-in-different-cancer-cell-lines-toward-the-development-of-new-potential-68-ga-labelled-curcuminoids-based-radiotracers-for-tumour-imaging
#11
Sara Rubagotti, Stefania Croci, Erika Ferrari, Giulia Orteca, Michele Iori, Pier C Capponi, Annibale Versari, Mattia Asti
Thanks to the ability to suppress the proliferation and to kill tumour cells, several studies have shown the anti-cancer effects of curcumin (CUR) and its derivatives, i.e. diacetylcurcumin (DAC) and bis-dehydroxycurcumin (bDHC). This study is focused onto the development of curcuminoid complexes with gallium-68 employed as potential new radio-labelled probes to detect neoplastic tissues through imaging techniques such as positron emission tomography. To this purpose, the uptake of three Ga-curcuminoid complexes, namely Ga(CUR)2(+), Ga(DAC)2(+), Ga(bDHC)2(+), by various tumour cell lines was compared with the uptake of the same compounds by normal human lymphocytes by flow cytometry using the intrinsic fluorescence of the curcuminoids...
May 10, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/28503046/reflections-about-osteoarthritis-and-curcuma-longa
#12
REVIEW
Marina Cristina Akuri, Sandra Maria Barbalho, Raíssa Meira Val, Elen Landgraf Guiguer
Osteoarthritis (OA) is a chronic inflammatory degenerative process that affects joints such as the hands, hips, shoulders, feet, spine, and especially knees in millions of people worldwide. Some authors have shown that Curcuma longa components may exhibit benefic effects in the treatment of degenerative diseases as OA. This plant belongs to the family Zingiberaceae and it is popularly known as turmeric or saffron. This review intended to perform a retrospective search to identify studies involving humans and animal models...
January 2017: Pharmacognosy Reviews
https://www.readbyqxmd.com/read/28470851/effectiveness-of-curcuminoids-in-the-treatment-of-knee-osteoarthritis-a-systematic-review-and-meta-analysis-of-randomized-clinical-trials
#13
Igho J Onakpoya, Elizabeth A Spencer, Rafael Perera, Carl J Heneghan
AIM: To critically appraise and evaluate the evidence for effectiveness of curcuminoids in the treatment of osteoarthritis (OA) in adults. METHODS: We conducted electronic searches in Medline, Embase, AMED, Cinahl and the Cochrane library. We included randomized controlled trials (RCTs) that investigated the effectiveness of orally-administered curcuminoids in OA in adults, and assessed risk of bias using the Cochrane risk of bias criteria. We used a random-effect model for meta-analysis...
May 4, 2017: International Journal of Rheumatic Diseases
https://www.readbyqxmd.com/read/28448635/excited-state-dynamics-of-bis-dehydroxycurcumin-tert-butyl-ester-a-diketo-shifted-derivative-of-the-photosensitizer-curcumin
#14
Luca Nardo, Angelo Maspero, Andrea Penoni, Giovanni Palmisano, Erika Ferrari, Monica Saladini
Bis-dehydroxycurcumin tert-butyl ester (K2T23) is a derivative of the natural spice curcumin. Curcumin is widely studied for its multiple therapeutic properties, including photosensitized cytotoxicity. However, the full exploitation of curcumin phototoxic potential is hindered by the extreme instability of its excited state, caused by very efficient non radiative decay by means of transfer of the enolic proton to the nearby keto oxygen. K2T23 is designed to exhibit a tautomeric equilibrium shifted toward the diketo conformers with respect to natural curcumin...
2017: PloS One
https://www.readbyqxmd.com/read/28440093/turmeric-curcuma-longa-l-extract-may-prevent-the-deterioration-of-spatial-memory-and-the-deficit-of-estimated-total-number-of-hippocampal-pyramidal-cells-of-trimethyltin-exposed-rats
#15
Sapto Yuliani, Mustofa, Ginus Partadiredja
CONTEXT: Protection of neurons from degeneration is an important preventive strategy for dementia. Much of the dementia pathology implicates oxidative stress pathways. Turmeric (Curcuma longa L.) contains curcuminoids which has anti-oxidative and neuro-protective effects. These effects are considered to be similar to those of citicoline which has been regularly used as one of standard medications for dementia. OBJECTIVE: This study aimed at investigating the effects of turmeric rhizome extract on the hippocampus of trimethyltin (TMT)-treated Sprague-Dawley rats...
April 25, 2017: Drug and Chemical Toxicology
https://www.readbyqxmd.com/read/28430129/curcumin-inhibits-apoptosis-of-chondrocytes-through-activation-erk1-2-signaling-pathways-induced-autophagy
#16
Xiaodong Li, Kai Feng, Jiang Li, Degang Yu, Qiming Fan, Tingting Tang, Xiao Yao, Xiaoqing Wang
Osteoarthritis (OA) is an inflammatory disease of load-bearing synovial joints that is currently treated with drugs that exhibit numerous side effects and are only temporarily effective in treating pain, the main symptom of the disease. Consequently, there is an acute need for novel, safe, and more effective chemotherapeutic agents for the treatment of osteoarthritis and related arthritic diseases. Curcumin, the principal curcuminoid and the most active component in turmeric, is a biologically active phytochemical...
April 21, 2017: Nutrients
https://www.readbyqxmd.com/read/28420097/synthesis-of-curcuminoids-and-evaluation-of-their-cytotoxic-and-antioxidant-properties
#17
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/28417091/biological-activities-of-curcuminoids-other-biomolecules-from-turmeric-and-their-derivatives-a-review
#18
REVIEW
Augustine Amalraj, Anitha Pius, Sreerag Gopi, Sreeraj Gopi
In recent years, several drugs have been developed deriving from traditional products and current drug research is actively investigating the possible therapeutic roles of many Ayruvedic and Traditional Indian medicinal therapies. Among those being investigated is Turmeric. Its most important active ingredient is curcuminoids. Curcuminoids are phenolic compounds commonly used as a spice, pigment and additive also utilized as a therapeutic agent used in several foods. Comprehensive research over the last century has revealed several important functions of curcuminoids...
April 2017: Journal of Traditional and Complementary Medicine
https://www.readbyqxmd.com/read/28417083/effects-of-turmeric-curcuminoids-and-metformin-against-central-sensitivity-to-pain-in-mice
#19
Suruchi Verma, Deepak Mundkinajeddu, Amit Agarwal, Shyam Sunder Chatterjee, Vikas Kumar
The reported experimental study was conducted to compare the effects of repeated daily oral doses of curcuminoids (CLE) with metformin as potential antidepressants and analgesics. Effects of a single and ten daily oral doses of CLE (5, 20, 80 mg/kg/day) and of 50 mg/kg/day metformin (MET) were compared in mice hot plate test (HPT) for analgesics. On the 11th treatment day, all animals were subjected to foot shock stress triggered hyperthermia test, and on the 12th treatment day to tail suspension test (TST) for antidepressants...
April 2017: Journal of Traditional and Complementary Medicine
https://www.readbyqxmd.com/read/28415473/preparation-of-a-novel-bioavailable-curcuminoid-formulation-cureit%C3%A2-using-polar-nonpolar-sandwich-pns-technology-and-its-characterization-and-applications
#20
Augustine Amalraj, Shintu Jude, Karthik Varma, Joby Jacob, Sreeraj Gopi, Oluwatobi S Oluwafemi, Sabu Thomas
Health benefits of curcuminoid are highly limited due to their poor aqueous solubility, very low systemic bioavailability, fast metabolic alterations and rapid elimination. In this study, a novel bioavailable curcuminoid formulation Cureit™ was prepared by using Polar-Nonpolar-Sandwich (PNS) technology with complete natural turmeric matrix (CNTM). The synthesized bioavailable curcuminoid formulation Cureit™ was characterizations by Nuclear magnetic resonance spectroscopy (NMR), scanning electron microscopy (SEM), X-ray diffraction (XRD), Fourier transform infra-red (IR), current-voltage (I-V) study, Quadrupole Time-of-Flight Mass Spectrometry (Q-TOF), differential scanning calorimeter (DSC) and thermogravimetric analysis (TGA)...
June 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
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