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https://www.readbyqxmd.com/read/28513174/structure-and-activity-relationship-of-curcumin-role-of-methoxy-group-in-anti-inflammatory-and-anti-colitis-effects-of-curcumin
#1
Haixia Yang, Zheyuan Du, Weicang Wang, Mingyue Song, Katherine Z Sanidad, Elvira Sukamtoh, Jennifer Zheng, Li Tian, Hang Xiao, Zhenhua Liu, Guodong Zhang
Curcumin, a dietary compound from Turmeric, has beneficial effects on inflammatory diseases such as inflammatory bowel disease. While most previous studies have focused on structure-activity relationship of the thiol-reactive α, β-unsaturated carbonyl groups of curcumin, little is known about the roles of methoxy groups in biological activities of curcumin. Here we synthesized a series of curcumin analogs with different substitution groups (R = H-, Br-, Cl-, F-, NO2-, CH3-, and OH-) to replace the methoxy group, and evaluated their biological effects in vitro and in vivo...
May 17, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28485773/curcumin-alleviates-lumbar-radiculopathy-by-reducing-neuroinflammation-oxidative-stress-and-nociceptive-factors
#2
L Xiao, M Ding, A Fernandez, P Zhao, L Jin, X Li
Current non-surgical treatments for lumbar radiculopathy [e.g. epidural steroids and Tumour necrosis factor-α (TNF-α) antagonists] are neither effective nor safe. As a non-toxic natural product, curcumin possesses an exceptional anti-inflammatory profile. We hypothesised that curcumin alleviates lumbar radiculopathy by attenuating neuroinflammation, oxidative stress and nociceptive factors. In a dorsal root ganglion (DRG) culture, curcumin effectively inhibited TNF-α-induced neuroinflammation, in a dose-dependent manner, as shown by mRNA and protein expression of IL-6 and COX-2...
May 9, 2017: European Cells & Materials
https://www.readbyqxmd.com/read/28284806/diarylpentadienone-derivatives-curcumin-analogues-synthesis-and-anti-inflammatory-activity
#3
Zhi Sen Wang, Liu Zeng Chen, Hai Pin Zhou, Xin Hua Liu, Fei Hu Chen
A series of new (2E,4E)-1-(substitutedphenyl)-5-(substitutedphenyl)penta-2,4-dien-1-one derivatives were designed and synthesized. Compounds 3i, 3k were determined by X-ray. All of the compounds have been screened for their anti-inflammatory activity characterized by evaluating their inhibition against LPS-induced IL-6 and TNF-α release in cell RAW 264.7 stimulated with LPS. Compound 3i showed the highest anti-inflammatory activity on decreasing IL-6 and TNF-α. The further study showed that title compound 3i inhibited expression of proteins p-p65, iNOS, COX-2 LPS-induced...
February 24, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28222524/a-combination-of-resveratrol-and-curcumin-is-effective-against-aluminum-chloride-induced-neuroinflammation-in-rats
#4
Amira Zaky, Ahmad Bassiouny, Mahitab Farghaly, Bassma M El-Sabaa
BACKGROUND: Experimental studies have demonstrated that aluminum is an environmental toxin that induces neuroinflammation and the development of Alzheimer's disease. OBJECTIVE: In this report, we investigated the beneficial effect of a combination of resveratrol and curcumin to reduce aluminum-induced neuroinflammation. METHOD: We employed both an in vivo model of aluminum-induced neuroinflammation and an in vitro aluminum stimulated cultured PC-12 cells...
February 7, 2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28199187/combinatorial-effect-of-curcumin-with-docetaxel-modulates-apoptotic-and-cell-survival-molecules-in-prostate-cancer
#5
Saswati Banerjee, Santosh K Singh, Indrajit Chowdhury, James W Lillard, Rajesh Singh
Docetaxel is the most commonly used chemotherapeutic agent to target androgen signaling in metastatic prostate cancer (PCa); however, prolonged treatment with docetaxel results in drug-resistant cancer cells. Combination therapies have the potential of increasing the effectiveness of drug treatment as well as decreasing the side effects. Curcumin is a nontoxic organic compound with multifaceted chemopreventive potential. In this study, we evaluated whether curcumin can reinforce the effect of docetaxel on PCa cells...
March 1, 2017: Frontiers in Bioscience (Elite Edition)
https://www.readbyqxmd.com/read/28198625/curcumin-attenuates-n-nitrosodiethylamine-induced-liver-injury-in-mice-by-utilizing-the-method-of-metabonomics
#6
Peiyu Qiu, Jiachen Sun, Shuli Man, He Yang, Long Ma, Peng Yu, Wenyuan Gao
N-Nitrosodiethylamine (DEN) exists as a food additive in cheddar cheese, processed meats, beer, water, and so forth. It is a potent hepatocarcinogen in animals and humans. Curcumin as a natural dietary compound decreased DEN-induced hepatocarcinogenesis in this research. According to the histopathological examination of liver tissues and biomarker detection in serum and livers, it was demonstrated that curcumin attenuated DEN-induced hepatocarcinogenesis through parts of regulating the oxidant stress enzymes (T-SOD and CAT), liver function (ALT and AST) and LDHA, AFP level, and COX-2/PGE2 pathway...
February 23, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28167853/curcumin-alters-neural-plasticity-and-viability-of-intact-hippocampal-circuits-and-attenuates-behavioral-despair-and-cox-2-expression-in-chronically-stressed-rats
#7
Ga-Young Choi, Hyun-Bum Kim, Eun-Sang Hwang, Seok Lee, Min-Ji Kim, Ji-Young Choi, Sung-Ok Lee, Sang-Seong Kim, Ji-Ho Park
Curcumin is a major diarylheptanoid component of Curcuma longa with traditional usage for anxiety and depression. It has been known for the anti-inflammatory, antistress, and neurotropic effects. Here we examined curcumin effect in neural plasticity and cell viability. 60-channel multielectrode array was applied on organotypic hippocampal slice cultures (OHSCs) to monitor the effect of 10 μM curcumin in long-term depression (LTD) through low-frequency stimulation (LFS) to the Schaffer collaterals and commissural pathways...
2017: Mediators of Inflammation
https://www.readbyqxmd.com/read/28053883/curcumin-reverses-neurochemical-histological-and-immuno-histochemical-alterations-in-the-model-of-global-brain-ischemia
#8
Glaura Fernandes Teixeira de Alcântara, Eudes Simões-Neto, Giovany Michely Pinto da Cruz, Maria Elizabeth Pereira Nobre, Kelly Rose Tavares Neves, Geanne Matos de Andrade, Gerly Anne de Castro Brito, Glauce Socorro de Barros Viana
Curcumin, a curcuminoid from Curcuma longa, presents antioxidant and anti-inflammatory actions and, among pathological changes of cerebral ischemic injury, inflammation is an important one. The objectives were to study the neuroprotective action of curcumin, in a model of global ischemia. Male Wistar rats (sham-operated, ischemic untreated and ischemic treated with curcumin, 25 or 50 mg/kg, p.o.) were anesthesized and their carotid arteries occluded, for 30 min. The SO group had the same procedure, except for carotid occlusion...
January 2017: Journal of Traditional and Complementary Medicine
https://www.readbyqxmd.com/read/28040561/development-and-characterization-of-anti-inflammatory-activity-of-curcumin-loaded-biodegradable-microspheres-with-potential-use-in-intestinal-inflammatory-disorders
#9
E Blanco-García, F J Otero-Espinar, J Blanco-Méndez, J M Leiro-Vidal, A Luzardo-Álvarez
This research addresses the development and in vitro evaluation of a microparticulate system intended for intestine-targeted delivery of curcumin (CRM), a natural polyphenol with anti-inflammatory properties. Microspheres (Ms) based on zein (ZN) and Gantrez(®) AN119 (PVMMA) were prepared by spray-drying and coated with a pH-sensitive polymer (Eudragit(®) FS30D). An experimental design was performed to optimize the microparticulate formulation. A detailed characterization of systems was carried out by SEM, DSC, FTIR, particle size, ζ potential measurements and in vitro CRM release...
December 28, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27957686/curcumin-attenuates-colistin-induced-neurotoxicity-in-n2a-cells-via-anti-inflammatory-activity-suppression-of-oxidative-stress-and-apoptosis
#10
Chongshan Dai, Giuseppe D Ciccotosto, Roberto Cappai, Shusheng Tang, Daowen Li, Sanlei Xie, Xilong Xiao, Tony Velkov
Neurotoxicity is an unwanted side-effect seen in patients receiving therapy with the "last-line" polymyxin antibiotics. This is the first study to show that colistin-induced neurotoxicity in neuroblastoma-2a (N2a) cells gives rise to an inflammatory response involving the IL-1β/p-IκB-α/NF-κB pathway. Pretreatment with curcumin at 5, 10, and 20 μM for 2 h prior to colistin (200 μM) exposure for 24 h, produced an anti-inflammatory effect by significantly down-regulating the expression of the pro-inflammatory mediators cyclooxygenase-2 (COX-2), phosphorylation of the inhibitor of nuclear factor-kappa B (NF-κB) (p-IκB)-α, and concomitantly NF-κB levels...
December 12, 2016: Molecular Neurobiology
https://www.readbyqxmd.com/read/27765359/cardioprotective-actions-of-curcumin-on-the-pathogenic-nfat-cox-2-prostaglandin-e2-pathway-induced-during-trypanosoma-cruzi-infection
#11
Matías Hernández, Susana Wicz, Ricardo S Corral
BACKGROUND: Diverse cardiovascular signaling routes have been considered critical for Chagas cardiomyopathy caused by the protozoan parasite Trypanosoma cruzi. Along this line, T. cruzi infection and endothelin-1 (ET-1) have been shown to cooperatively activate the Ca(2+)/NFAT cascade in cardiomyocytes, leading to cyclooxygenase type 2 (COX-2) induction and increased release of prostanoids and prohypertrophic peptides. PURPOSE: To determine whether the well-known cardioprotective and anti-inflammatory effects of curcumin (Cur) could be helpful to interfere with this key machinery for pathogenesis of Chagas myocarditis...
November 15, 2016: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/27744738/resveratrol-and-curcumin-as-protective-agents-in-an-experimental-rat-model-of-intestinal-ischemia-and-reperfusion
#12
Cristina Cucolas, Alexandra Ioana Daneasa, Diana Olteanu, Nicoleta Decea, Remus Moldovan, Flaviu Tabaran, Gabriela Adriana Filip
The aim of this study was to evaluate the protective effects of resveratrol and curcumin in an experimental rat model of intestinal ischemia-reperfusion (I/R). Forty-eight adult Wistar rats were used: 12 animals undergoing the sham surgery and 36 animals undergoing laparotomy, with 15 min of mesentric artery clamping. The animals from the latter group (n = 12) were pretreated, for 1 week, with vehicle (CTR), resveratrol (RES), and curcumin (CUR). After 1 h and 6 h of reperfusion, respectively, cyclooxigenase (COX)-2, mucin-1, E-cadherin, nuclear factor (NK)-κB expressions, and tumor necrosis factor related apoptosis-inducing ligand (TRAIL) were assessed in the small intestine...
May 30, 2016: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/27677346/curcumin-synergistically-increases-effects-of-%C3%AE-interferon-and-retinoic-acid-on-breast-cancer-cells-in-vitro-and-in-vivo-by-up-regulation-of-grim-19-through-stat3-dependent-and-stat3-independent-pathways
#13
Min Ren, Ying Wang, Xiaodong Wu, Suxia Ge, Benzhong Wang
OBJECTIVE: The study aimed to investigate the effects of combination treatment of curcumin and β-interferon (IFN-β)/retinoic acid (RA) on breast cancer cells, including cell viability, apoptosis and migration, and to determine the mechanisms related to GRIM-19 through STAT3-dependent and STAT3-independent pathways. METHODS: The following groups were used for the in vitro experiment: control siRNA, GRIM-19 siRNA, IFN-β/RA and IFN-β/RA + curcumin. Cell viability is by the MTT method, cell apoptosis by flow cytometry and cell migration by wound healing experiment; GRIM-19, STAT3, survivin, Bcl-2, GADD153 and COX-2 expression was measured by Western blot...
October 16, 2016: Journal of Drug Targeting
https://www.readbyqxmd.com/read/27667581/plant-derived-anti-cancerous-secondary-metabolites-as-multipronged-inhibitor-of-cox-topo-and-aromatase-molecular-modeling-and-dynamics-simulation-analyses
#14
Swati Singh, Manika Awasthi, Veda P Pandey, Upendra N Dwivedi
In the present study, 300 plant derived secondary metabolites (100 each of alkaloid, flavonoid, and terpenoid), have been screened for their anti-cancerous activity through inhibition of selected key enzymatic targets, namely cyclooxygenases (COXs), topoisomerases (Topos), and aromatase by molecular docking approach. Furthermore, the stability of the complexes of top hits, from each class of secondary metabolites, with their respective enzymatic targets was analyzed using molecular dynamics (MD) simulation analyses and binding free energy calculations...
September 25, 2016: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/27267893/a-randomized-double-blind-placebo-controlled-phase-iib-trial-of-curcumin-in-oral-leukoplakia
#15
Moni Abraham Kuriakose, Kunnambath Ramdas, Bindu Dey, Subramanya Iyer, Gunaseelan Rajan, Kalavathy K Elango, Amritha Suresh, Divya Ravindran, Rajneesh R Kumar, Prathiba R, Surya Ramachandran, Nisha Asok Kumar, Gigi Thomas, Thara Somanathan, Hiran K Ravindran, Kannan Ranganathan, Sudhakar Babu Katakam, Shivashankar Parashuram, Vijayvel Jayaprakash, M Radhakrishna Pillai
Oral leukoplakia is a potentially malignant lesion of the oral cavity, for which no effective treatment is available. We investigated the effectiveness of curcumin, a potent inhibitor of NF-κB/COX-2, molecules perturbed in oral carcinogenesis, to treat leukoplakia. Subjects with oral leukoplakia (n = 223) were randomized (1:1 ratio) to receive orally, either 3.6 g/day of curcumin (n = 111) or placebo (n = 112), for 6 months. The primary endpoint was clinical response obtained by bi-dimensional measurement of leukoplakia size at recruitment and 6 months...
August 2016: Cancer Prevention Research
https://www.readbyqxmd.com/read/27258084/drug-targets-for-cardiovascular-safe-anti-inflammatory-in-silico-rational-drug-studies
#16
Sajad Shahbazi, Tammanna R Sahrawat, Monalisa Ray, Swagatika Dash, Dattatreya Kar, Shikha Singh
Cyclooxygenase-2 (COX-2) plays an important role in memory consolidation and synaptic activity, the most fundamental functions of the brain. It converts arachidonic acid to prostaglandin endoperoxide H2. In contrast, if over-expressed, it causes inflammation in response to cytokine, pro-inflammatory molecule, and growth factor. Anti-inflammatory agents, by allosteric or competitive inhibition of COX-2, alleviate the symptoms of inflammation. Coxib family drugs, particularly celecoxib, are the most famous anti-inflammatory agents available in the market showing significant inhibitory effect on COX-2 activity...
2016: PloS One
https://www.readbyqxmd.com/read/27226186/role-of-curcumin-in-protection-of-gastric-mucosa-against-stress-induced-gastric-mucosal-damage-involvement-of-hypoacidity-vasoactive-mediators-and-sensory-neuropeptides
#17
R Czekaj, J Majka, A Ptak-Belowska, A Szlachcic, A Targosz, K Magierowska, M Strzalka, M Magierowski, T Brzozowski
The antioxidizing properties of curcumin, a highly pleiotropic substance used for centuries in traditional medicine has been confirmed by numerous experimental and clinical studies. Curcumin exhibits anti-inflammatory, antiproliferative and anti-angiogenic actions inhibiting the development and progression of tumors but the efficacy of this compound to influence gastric acid secretion n in the stomach and to affect the gastric mucosal damage induced by non-topical ulcerogenes such as stress has been little studied...
April 2016: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/27133426/small-molecule-tolfenamic-acid-and-dietary-spice-curcumin-treatment-enhances-antiproliferative-effect-in-pancreatic-cancer-cells-via-suppressing-sp1-disrupting-nf-kb-translocation-to-nucleus-and-cell-cycle-phase-distribution
#18
Riyaz Basha, Sarah F Connelly, Umesh T Sankpal, Ganji Purnachandra Nagaraju, Hassaan Patel, Jamboor K Vishwanatha, Sagar Shelake, Leslie Tabor-Simecka, Mamoru Shoji, Jerry W Simecka, Bassel El-Rayes
Combination of dietary/herbal spice curcumin (Cur) and COX inhibitors has been tested for improving therapeutic efficacy in pancreatic cancer (PC). The objective of this study was to identify agent with low toxicity and COX-independent mechanism to induce PC cell growth inhibition when used along with Cur. Anticancer NSAID, tolfenamic acid (TA) and Cur combination were evaluated using PC cell lines. L3.6pl and MIA PaCa-2 cells were treated with Cur (5-25μM) or TA (25-100μM) or combination of Cur (7.5μM) and TA (50μM)...
May 2016: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/27128654/novel-synthetic-curcumin-analogs-as-potent-antiangiogenic-agents-in-colorectal-cancer
#19
Balney Rajitha, Ganji Purnachandra Nagaraju, Walid L Shaib, Olatunji B Alese, James P Snyder, Mamoru Shoji, Subasini Pattnaik, Afroz Alam, Bassel F El-Rayes
The transcription factor NF-κB plays a central role in angiogenesis in colorectal cancer (CRC). Curcumin is a natural dietary product that inhibits NF-κB. The objective of this study is to evaluate the antiangiogenic effects of curcumin and two potent synthetic analogues (EF31 and UBS109) in CRC. IC50 values for curcumin, EF31, and UBS109 were determined in the HCT116 and HT-29 cell lines. HUVEC tube formation, egg CAM assay, and matrigel plug assays revealed decreased angiogenesis in cell lines treated with curcumin, EF31, or UBS109...
January 2017: Molecular Carcinogenesis
https://www.readbyqxmd.com/read/27109049/emu-oil-based-nano-emulgel-for-topical-delivery-of-curcumin
#20
COMPARATIVE STUDY
Manish Kumar Jeengar, Sri Vishnu Kiran Rompicharla, Shweta Shrivastava, Naveen Chella, Nalini R Shastri, V G M Naidu, Ramakrishna Sistla
Curcumin and emu oil derived from emu bird (Dromaius novaehollandiae) has shown promising results against inflammation. However, the delivery of curcumin is hindered due to low solubility and poor permeation. In addition, till date the role of emu oil in drug delivery has not been explored systemically. Hence, the current investigation was designed to evaluate the anti-inflammatory potential of curcumin in combination with emu oil from a nanoemulgel formulation in experimental inflammation and arthritic in vivo models...
June 15, 2016: International Journal of Pharmaceutics
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