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Tetrahydrocurcumin

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https://www.readbyqxmd.com/read/29800660/lactose-crosslinked-fish-gelatin-based-porous-scaffolds-embedded-with-tetrahydrocurcumin-for-cartilage-regeneration
#1
A Etxabide, R D C Ribeiro, P Guerrero, A M Ferreira, G P Stafford, K Dalgarno, K de la Caba, P Gentile
Tetrahydrocurcumin (THC) is one of the major colourless metabolites of curcumin and shows even greater pharmacological and physiological benefits. The aim of this work was the manufacturing of porous scaffolds as a carrier of THC under physiological conditions. Fish-derived gelatin scaffolds were prepared by freeze-drying by two solutions concentrations (2.5% and 4% w/v), cross-linked via addition of lactose and heat-treated at 105 °C. This cross-linking reaction resulted in more water resistant scaffolds with a water uptake capacity higher than 800%...
May 22, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29719770/identification-of-curcumin-derivatives-as-human-lmtk3-inhibitors-for-breast-cancer-a-docking-dynamics-and-mm-pbsa-approach
#2
K Anbarasu, S Jayanthi
Human lemur tyrosine kinase-3 (LMTK3) is primarily involved in regulation of estrogen receptor-α (ERα) by phosphorylation activity. LMTK3 acts as key biomarker for ERα positive breast cancer and identified as novel drug target for breast cancer. Due to the absence of experimental reports, the computational approach has been followed to screen LMTK3 inhibitors from natural product curcumin derivatives based on rational inhibitor design. The initial virtual screening and re-docking resulted in identification of top three leads with favorable binding energy and strong interactions in critical residues of ATP-binding cavity...
May 2018: 3 Biotech
https://www.readbyqxmd.com/read/29689635/the-pharmacokinetics-and-tissue-distribution-of-curcumin-and-its-metabolites-in-mice
#3
Junjun Wang, Xuejin Yu, Ling Zhang, Ling Wang, Zhihong Peng, Yong Chen
Curcumin (CUR) is the major active component of turmeric and plays an important role in the prevention and treatment of many chronic diseases such as respiratory and neurodegenerative disease. In the present work, a rapid and simple LC-MS/MS method was developed to investigate the pharmacokinetics and tissue distribution of CUR and its metabolites in mice after intravenous administration of CUR (20 mg/kg). The results showed that the values of AUC0-∞ were 107.0 ± 18.3, 6.0 ± 1.2 and 12.0 ± 4...
April 24, 2018: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29686295/curcumin-interacts-directly-with-the-cysteine-259-residue-of-stat3-and-induces-apoptosis-in-h-ras-transformed-human-mammary-epithelial-cells
#4
Young-Il Hahn, Su-Jung Kim, Bu-Young Choi, Kyung-Cho Cho, Raju Bandu, Kwang Pyo Kim, Do-Hee Kim, Wonki Kim, Joon Sung Park, Byung Woo Han, Jeewoo Lee, Hye-Kyung Na, Young-Nam Cha, Young-Joon Surh
Signal transducer and activator of transcription 3 (STAT3) is a transcription factor that is latent but constitutively activated in many types of cancers. It is well known that STAT3 plays a key role in inflammation-associated tumorigenesis. Curcumin is an anti-inflammatory natural compound isolated from the turmeric (Curcuma longa L., Zingiberaceae) that has been extensively used in a traditional medicine over the centuries. In the present study, we have found that curcumin inhibits STAT3 signaling that is persistently overactivated in H-Ras transformed breast epithelial cells (H-Ras MCF10A)...
April 23, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29669346/tetrahydrocurcumin-provides-neuroprotection-in-experimental-traumatic-brain-injury-and-the-nrf2-signaling-pathway-as-a-potential-mechanism
#5
Guan Wei, Bingji Chen, Qingjiang Lin, Yasong Li, Liangqin Luo, Hefan He, Huangde Fu
The protective effect of tetrahydrocurcumin (THC) after experimental traumatic brain injury (TBI) has been demonstrated, as demonstrated by the inhibition of oxidative stress, mitochondrial dysfunction, and apoptosis. However, the mechanisms underlying this effect are still not well understood. This study was to investigate the neuroprotective effects of THC, and its potential mechanisms, in a rat model of TBI. To this end, rats were divided into 4 groups: the sham group, the TBI group, the TBI + vehicle (V) group, and the TBI + THC group...
2017: Neuroimmunomodulation
https://www.readbyqxmd.com/read/29629345/comparative-effects-of-curcumin-and-tetrahydrocurcumin-on-dextran-sulfate-sodium-induced-colitis-and-inflammatory-signaling-in-mice
#6
Joon-Yeop Yang, Xiancai Zhong, Su-Jung Kim, Do-Hee Kim, Hyun Soo Kim, Jeong-Sang Lee, Hye-Won Yum, Jeewoo Lee, Hye-Kyung Na, Young-Joon Surh
Background: Curcumin, a yellow ingredient of turmeric ( Curcuma longa Linn, Zingiberaceae), has long been used in traditional folk medicine in the management of inflammatory disorders. Although curcumin has been reported to inhibit experimentally-induced colitis and carcinogenesis, the underlying molecular mechanisms remain largely unresolved. Methods: Murine colitis was induced by dextran sulfate sodium (DSS) which mimics inflammatory bowel disease. Curcumin or tetrahydrocurcumin was given orally (0...
March 2018: Journal of Cancer Prevention
https://www.readbyqxmd.com/read/29546799/molecular-modelling-reveals-the-inhibition-mechanism-and-structure-activity-relationship-of-curcumin-and-its-analogues-to-staphylococcal-aureus-sortase-a
#7
Xiaodi Niu, Yawen Gao, Yiding Yu, Yanan Yang, Guizhen Wang, Lin Sun, Hongsu Wang
Previous studies found that the activity of Sortase A, a bacterial surface protein from Staphylococcus aureus, was inhibited by curcumin and its analogues. To explore this inhibitory mechanism, Sortase A and its inhibitors in complex systems were studied by molecular docking, molecular modelling, binding energy decomposition calculation and steered molecular dynamics simulations. Energy decomposition analysis indicated that PRO-163, LEU-169, GLN-172, ILE-182 and ILE-199 are key residues in Sortase A-inhibitor complexes...
April 2, 2018: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29492979/the-enhanced-effect-of-tetrahydrocurcumin-on-radiosensitivity-of-glioma-cells
#8
Xingzhen Zhang, Lei Peng, Anchang Liu, Jianbo Ji, Lixia Zhao, Guangxi Zhai
OBJECTIVES: To evaluate the effects of tetrahydrocurcumin (THC) on the radiosensitivity of glioma cells and the possible molecular mechanism. METHODS: MTT assay, colony forming and wound healing assays were performed to detect the proliferation, radiosensitivity and migration of cells with various treatments. Cell apoptosis, cell cycle and GHS level were determined for exploring potent sensitization mechanism of THC. Meanwhile, protein expressions of cyclin D1 and PCNA were also measured...
June 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29468071/dietary-tetrahydrocurcumin-reduces-renal-fibrosis-and-cardiac-hypertrophy-in-5-6-nephrectomized-rats
#9
Wei Ling Lau, Mahyar Khazaeli, Javad Savoj, Kasim Manekia, Maria Bangash, Roshni G Thakurta, Anhthu Dang, Nosratola D Vaziri, Bhupinder Singh
Tetrahydrocurcumin (THC) is the principal metabolite of curcumin and has antioxidant properties. In the present investigation, the effect of THC on renal and cardiovascular outcomes was studied in rats with chronic kidney disease (CKD). CKD rats were randomized following 5/6 nephrectomy to a special diet for 9 weeks which contained 1% THC (CKD+THC group). Low-dose polyenylphosphatidylcholine was used as a lipid carrier to increase bioavailability. Endpoints included tail blood pressure, normalized heart weight, plasma and urine biochemical data, and kidney tissue analyses...
April 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29436654/tetrahydrocurcumin%C3%A2-induced-autophagy-via-suppression-of-pi3k-akt-mtor-in-non%C3%A2-small-cell-lung-carcinoma-cells
#10
Guoqiang Song, Honghui Lu, Fei Chen, Youmei Wang, Weibin Fan, Weifang Shao, Huoquan Lu, Bin Lin
Lung carcinoma is the leading cause of mortality due to cancer worldwide. Autophagy has a significant role in the development and progression of non‑small cell lung carcinoma (NSCLC). A previous study has revealed that tetrahydrocurcumin (THC), a traditional Chinese medicine isolated from Curcuma wenyujin (Chen & Ling, 1981), induces autophagy in human A549 NSCLC cells. The present study evaluated THC‑induced autophagy in A549 cells using various assays, including the Cell Counting Kit‑8, acridine orange staining, flow cytometry, reverse transcription‑quantitative polymerase chain reaction (RT‑qPCR), and western blot analysis of the markers of autophagy...
April 2018: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29341902/curcumin-potentiates-the-function-of-human-%C3%AE-7-nicotinic-acetylcholine-receptors-expressed-in-sh-ep1-cells
#11
Eslam El Nebrisi, Lina T Al Kury, Keun-Hang Susan Yang, Petrilla Jayaprakash, Frank C Howarth, Nadine Kabbani, Murat Oz
Effects of curcumin, a biologically active ingredient of turmeric, were tested on the Ca2+ transients induced by the activation of α7 subunit of the human nicotinic acetylcholine (α7 nACh) receptor expressed in SH-EP1 cells. Curcumin caused a significant potentiation of choline (1 mM)-induced Ca2+ transients with an EC50 value of 133 nM. The potentiating effect of curcumin was not observed in Ca2+ transients induced by high K+ (60 mM) containing solutions or activation of α4β2 nACh receptors and the extent of curcumin potentiation was not altered in the presence of Ca2+ channel antagonists nifedipine (1 μM), verapamil (1 μM), ω-conotoxin (1 μM), and bepridil (10 μM)...
January 13, 2018: Neurochemistry International
https://www.readbyqxmd.com/read/29333037/curcumin-and-natural-derivatives-inhibit-ebola-viral-proteins-an-in-silico-approach
#12
Shruti Baikerikar
Background: Ebola viral disease is a severe and mostly fatal disease in humans caused by Ebola virus. This virus belongs to family Filoviridae and is a single-stranded negative-sense virus. There is no single treatment for this disease which puts forth the need to identify new therapy to control and treat this fatal condition. Curcumin, one of the bioactives of turmeric, has proven antiviral property. Objective: The current study evaluates the inhibitory activity of curcumin, bisdemethoxycurcumin, demethoxycurcumin, and tetrahydrocurcumin against Zaire Ebola viral proteins (VPs)...
December 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/29277764/distribution-of-curcumin-and-thc-in-peripheral-blood-mononuclear-cells-isolated-from-healthy-individuals-and-patients-with-chronic-lymphocytic-leukemia
#13
Gordon T Bolger, Albert Licollari, Aimin Tan, Richard Greil, Lisa Pleyer, Brigitta Vcelar, Muhammad Majeed, Peter Sordillo
Background/Aim: Curcumin is being widely investigated for its anticancer properties and studies in the literature suggest that curcumin distributes to a higher degree in tumor versus non-tumor cells. In the current study, we report on investigation of the distribution of curcumin and metabolism to THC in PBMC from healthy individuals and chronic lymphocytic leukemia (CLL) patients following exposure to Lipocurc™ (liposomal curcumin). Materials and Methods: The time and temperature-dependent distribution of liposomal curcumin and metabolism to tetrahydrocurcumin (THC) were measured in vitro in human peripheral blood mononuclear cells (PBMC) obtained from healthy individuals, PBMC HI (cryopreserved and freshly isolated PBMC) and CLL patients (cryopreserved PBMC) with lymphocyte counts ranging from 17-58×106 cells/ml (PBMCCLL,Grp 1 ) and >150×106 cells/ml (PBMCCLL,Grp 2 )...
January 2018: Anticancer Research
https://www.readbyqxmd.com/read/29207631/tetrahydrocurcumin-induces-mesenchymal-epithelial-transition-and-suppresses-angiogenesis-by-targeting-hif-1%C3%AE-and-autophagy-in-human-osteosarcoma
#14
Yan Zhang, Ying Liu, Jilong Zou, Lixin Yan, Wei Du, Yafeng Zhang, Hanliang Sun, Peng Lu, Shuo Geng, Rui Gu, Hongyue Zhang, Zhenggang Bi
Human osteosarcoma is considered a malignant tumor with poor prognosis that readily metastasizes. Tetrahydrocurcumin (THC) has been reported to have anti-tumor activity in numerous tumors. In addition, hypoxia-inducible factor-1α (HIF-1α) has been demonstrated to be associated with tumor metastasis by regulating epithelial-mesenchymal transition (EMT). However, the role of THC in osteosarcoma remains uncertain. Therefore, this study aimed to elucidate the potential mechanisms. We found that THC significantly reduced the growth of osteosarcoma cells and suppressed migration and invasion, as tested in a nude mouse lung metastasis model...
October 31, 2017: Oncotarget
https://www.readbyqxmd.com/read/29094265/synthesis-and-cytotoxic-activity-of-novel-tetrahydrocurcumin-derivatives-bearing-pyrazole-moiety
#15
Ahmed Mahal, Ping Wu, Zi-Hua Jiang, Xiaoyi Wei
Tetrahydrocurcumin (THC) is a major metabolite of curcumin and plays an important role in curcumin-induced biological effects. THC is a promising preventive and chemotherapeutic agent for cancer. A series of new pyrazole derivatives of THC have been synthesized as potent anticancer agents. Direct condensation of THC with various substituted hydrazines leads to new pyrazole derivatives of THC (1-18). The prepared compounds have been evaluated via in vitro MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay for their cell proliferation-inhibitory activity against human lung adenocarcinoma (A549), human cervical carcinoma (HeLa) and human breast carcinoma (MCF-7) cells...
December 2017: Natural Products and Bioprospecting
https://www.readbyqxmd.com/read/29023392/disposition-metabolism-and-histone-deacetylase-and-acetyltransferase-inhibition-activity-of-tetrahydrocurcumin-and-other-curcuminoids
#16
Júlia T Novaes, Ryan Lillico, Casey L Sayre, Kalyanam Nagabushnam, Muhammed Majeed, Yufei Chen, Emmanuel A Ho, Ana Luísa de P Oliveira, Stephanie E Martinez, Samaa Alrushaid, Neal M Davies, Ted M Lakowski
Tetrahydrocurcumin (THC), curcumin and calebin-A are curcuminoids found in turmeric ( Curcuma longa ). Curcuminoids have been established to have a variety of pharmacological activities and are used as natural health supplements. The purpose of this study was to identify the metabolism, excretion, antioxidant, anti-inflammatory and anticancer properties of these curcuminoids and to determine disposition of THC in rats after oral administration. We developed a UHPLC-MS/MS assay for THC in rat serum and urine...
October 12, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28833102/tetrahydrocurcumin-ameliorates-homocysteine-mediated-mitochondrial-remodeling-in-brain-endothelial-cells
#17
Jonathan C Vacek, Jyotirmaya Behera, Akash K George, Pradip K Kamat, Anuradha Kalani, Neetu Tyagi
Homocysteine (Hcy) causes endothelial dysfunction by inducing oxidative stress in most neurodegenerative disorders. This dysfunction is highly correlated with mitochondrial dynamics such as fusion and fission. However, there are no strategies to prevent Hcy-induced mitochondrial remodeling. Tetrahydrocurcumin (THC) is an anti-inflammatory and anti-oxidant compound. We hypothesized that THC may ameliorates Hcy-induced mitochondria remodeling in mouse brain endothelial cells (bEnd3) cells. bEnd3 cells were exposed to Hcy treatment in the presence or absence of THC...
April 2018: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/28766664/tetrahydrocurcumin-is-more-effective-than-curcumin-in-inducing-the-apoptosis-of-h22-cells-via-regulation-of-a-mitochondrial-apoptosis-pathway-in-ascites-tumor-bearing-mice
#18
Weihai Liu, Zhenbiao Zhang, Guosheng Lin, Dandan Luo, Hanbin Chen, Hongmei Yang, Jiali Liang, Yuhong Liu, Jianhui Xie, Ziren Su, Hongying Cao
Curcumin (CUR), a widely used food additive, is derived mainly from Curcuma species that has been applied traditionally for the treatment of various diseases, including hepatocellular carcinoma (HCC). However, its poor systemic bioavailability hampers its clinical application, which may be related to its wide metabolism. Tetrahydrocurcumin (THC) is a major metabolite of CUR and has been reported to have multiple biologic activities. We investigated, for the first time, the efficacy and associated mechanism of action of THC and CUR in a H22 ascites tumor-bearing model in mice...
September 20, 2017: Food & Function
https://www.readbyqxmd.com/read/28668837/distribution-and-metabolism-of-lipocurc%C3%A2-liposomal-curcumin-in-dog-and-human-blood-cells-species-selectivity-and-pharmacokinetic-relevance
#19
Gordon T Bolger, Albert Licollari, Aimin Tan, Richard Greil, Brigitta Vcelar, Muhammad Majeed, Lawrence Helson
BACKGROUND/AIM: The aim of this study was to investigate the distribution of curcumin (in the form of Lipocurc™) and its major metabolite tetrahydrocurcumin (THC) in Beagle dog and human red blood cells, peripheral blood mononuclear cells (PBMC) and hepatocytes. MATERIALS AND METHODS: Lipocurc™ was used as the source of curcumin for the cell distribution assays. In vitro findings with red blood cells were also compared to in vivo pharmacokinetic data available from preclinical studies in dogs and phase I clinical studies in humans...
July 2017: Anticancer Research
https://www.readbyqxmd.com/read/28416863/protective-effects-of-tetrahydrocurcumin-thc-on-fibroblast-and-melanoma-cell-lines-in-vitro-it-s-implication-for-wound-healing
#20
Mahendra Kumar Trivedi, Mayank Gangwar, Sambhu Charan Mondal, Snehasis Jana
The aim of this study was to investigate the role of tetrahydrocurcumin (THC) against various skin health parameters using in vitro human foreskin fibroblast and melanoma cell lines (i.e. HFF-1 and B16-F10). The study was assessed using cell viability by MTT assay, identification of extracellular matrix component in HFF-1 cell line (i.e. collagen, elastin and hyaluronic acid), melanin synthesis in B16-F10 cells, cell viability against UVB-induced stress in HFF-1 cells, and in vitro wound healing by the scratch assay...
April 2017: Journal of Food Science and Technology
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