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Tetrahydrocurcumin

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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
#1
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...
February 13, 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
#2
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
#3
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
#4
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 17-58×10 6 cells/ml (PBMC CLL,Grp 1 ) and >150×10 6 cells/ml (PBMC CLL,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
#5
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
#6
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...
November 1, 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
#7
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. THC shows multiple redistribution phases with corresponding increases in urinary excretion rate...
October 12, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28833102/tetrahydrocurcumin-ameliorates-homocysteine-mediated-mitochondrial-remodeling-in-brain-endothelial-cells
#8
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...
August 18, 2017: 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
#9
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
#10
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
#11
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
https://www.readbyqxmd.com/read/28386319/tetrahydrocurcumin-reduces-oxidative-stress-induced-apoptosis-via-the-mitochondrial-apoptotic-pathway-by-modulating-autophagy-in-rats-after-traumatic-brain-injury
#12
Yongyue Gao, Zong Zhuang, Shanting Gao, Xiang Li, Zihuan Zhang, Zhennan Ye, Liwen Li, Chao Tang, Mengliang Zhou, Xiao Han, Jie Li
Tetrahydrocurcumin (THC) has been identified as a multi-functional neuroprotective agent in numerous neurological disorders. Oxidative stress as a result of injury may induce neuronal apoptosis after traumatic brain injury (TBI). Treatment with THC may improve neurological function following TBI by attenuating oxidative stress and apoptosis and by enhancing autophagy. The purpose of this study was to investigate the mechanism of neuroprotection by THC against oxidative stress-induced neuronal apoptosis after TBI...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/28236190/protective-role-of-tetrahydrocurcumin-an-active-polyphenolic-curcuminoid-on-cadmium-inducedoxidative-damage-in-rats
#13
Ramalingam Ramakrishnan, Perumal Elangovan, Leelavinothan Pari
In the present work, protective effect of tetrahydrocurcumin (THC) against oxidative damages in cadmium (Cd)-induced toxicity in rats was evaluated. Cd is an important environmental and industrial toxicant that affects almost all the organs, especially liver. Liver is the major organ responsible for the metabolism and the primary target for many toxic chemicals and drugs. Effect of THC, the curcumin-derived polyphenolic compound on Cd-induced oxidative stress and hepatic damage was evaluated using male albino Wistar rats...
February 24, 2017: Applied Biochemistry and Biotechnology
https://www.readbyqxmd.com/read/28004737/investigating-the-neuroprotective-effects-of-turmeric-extract-structural-interactions-of-%C3%AE-amyloid-peptide-with-single-curcuminoids
#14
Rosario Randino, Manuela Grimaldi, Marco Persico, Augusta De Santis, Elena Cini, Walter Cabri, Antonella Riva, Gerardino D'Errico, Caterina Fattorusso, Anna Maria D'Ursi, Manuela Rodriquez
A broad biophysical analysis was performed to investigate the molecular basis of the neuroprotective action of Curcuma longa extracts in Alzheimer's disease. By combining circular dichroism and electron paramagnetic resonance experiments with molecular modeling calculations, the minor components of Curcuma longa extracts, such as demethoxycurcumin (2, DMC), bisdemethoxycurcumin (3, BDMC) and cyclocurcumin (4, CYC), were analyzed in a membrane environment mimicking the phospholipid bilayer. Our study provides the first evidence on the relative role of single curcuminoids interacting with Aβ-peptide...
December 22, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27996095/biological-and-pharmacological-evaluation-of-dimethoxycurcumin-a-metabolically-stable-curcumin-analogue-with-a-promising-therapeutic-potential
#15
REVIEW
Manouchehr Teymouri, Nastaran Barati, Matteo Pirro, Amirhosein Sahebkar
Dimethoxycurcumin (DiMC) is a synthetic analog of curcumin with superior inter-related pro-oxidant and anti-cancer activity, and metabolic stability. Numerous studies have shown that DiMC reserves the biologically beneficial features, including anti-inflammatory, anti-carcinogenic, and cytoprotective properties, almost to the same extent as curcumin exhibits. DiMC lacks the phenolic-OH groups as opposed to curcumin, dimethoxycurcumin, and bis-demethoxycurcumin that all vary in the number of methoxy groups per molecule, and has drawn the attentions of researchers who attempted to discover the structure-activity relationship (SAR) of curcumin...
January 2018: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/27916377/tetrahydrocurcumin-provides-neuroprotection-in-rats-after-traumatic-brain-injury-autophagy-and-the-pi3k-akt-pathways-as-a-potential-mechanism
#16
Yongyue Gao, Jie Li, Lingyun Wu, Chenhui Zhou, Qiang Wang, Xiang Li, Mengliang Zhou, Handong Wang
BACKGROUND: Tetrahydrocurcumin provides neuroprotection in multiple neurologic disorders by modulating oxidative stress, inflammatory responses, and autophagy. However, in traumatic brain injury (TBI), it is unclear whether a beneficial effect of tetrahydrocurcumin exists. In this study, we hypothesized that administration of tetrahydrocurcumin provides neuroprotection in a rat model of TBI. MATERIAL AND METHODS: Behavioral studies were performed by recording and analyzing beam-walking scores...
November 2016: Journal of Surgical Research
https://www.readbyqxmd.com/read/27748926/suppression-of-grasp65-phosphorylation-by-tetrahydrocurcumin-protects-against-cerebral-ischemia-reperfusion-injury-via-erk-signaling
#17
Bin Lin, Heng Yu, Yuting Lin, Chao Cai, Huoquan Lu, Xinbo Zhu
The aim of the present study was to assess the neuroprotective effects of tetrahydrocurcumin (THC) in a mouse model of cerebral ischemia/reperfusion (I/R) injury, and to investigate the involvement of Golgi reassembly and stacking protein 65 (GRASP65) and the extracellular signal‑regulated kinase (ERK) signaling pathway. Cerebral I/R injury was induced using the Pulsinelli four‑vessel occlusion method. After 5 min of reperfusion, mice received THC (5, 10 or 25 mg/kg) or saline by intraperitoneal injection...
November 2016: Molecular Medicine Reports
https://www.readbyqxmd.com/read/27713040/tetrahydrocurcumin-in-combination-with-deferiprone-attenuates-hypertension-vascular-dysfunction-baroreflex-dysfunction-and-oxidative-stress-in-iron-overloaded-mice
#18
Weerapon Sangartit, Poungrat Pakdeechote, Veerapol Kukongviriyapan, Wanida Donpunha, Shigeki Shibahara, Upa Kukongviriyapan
Excessive iron can generate reactive oxygen species (ROS), leading to oxidative stress that is closely associated with cardiovascular dysfunction. Iron overload was induced in male ICR mice by injection of iron sucrose (10mg/kg/day) for eight weeks. Iron overload was evidenced by increased serum iron indices. The mice developed increased blood pressure, impaired vascular function and blunted response of the autonomic nervous system. These effects were accompanied by increased malondialdehyde levels in various tissues, increased nitric oxide metabolites in plasma and urine, and decreased blood glutathione...
December 2016: Vascular Pharmacology
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
#19
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
https://www.readbyqxmd.com/read/27327398/use-of-basic-mobile-phase-to-improve-chromatography-and-boost-sensitivity-for-quantifying-tetrahydrocurcumin-in-human-plasma-by-lc-ms-ms
#20
Aimin Tan, Yanxin Wu, Molly Wong, Albert Licollari, Gordon Bolger, John C Fanaras, George Shopp, Lawrence Helson
Tetrahydrocurcumin (THC), a major metabolite of curcumin, is often quantified by LC-MS or LC-MS/MS using acidic mobile phases due to the concern of its instability in a basic medium. However, acidic mobile phases often lead to poor chromatography (e.g. split or double peaks) and reduced detection sensitivity in the commonly used negative ionization mode. To overcome these shortcomings, a basic mobile phase was used for the first time in the LC-MS/MS quantification of THC. In comparison with the acidic mobile phases, a single symmetrical chromatographic peak was obtained and the sensitivity increased by 7-fold or more under the equivalent conditions...
August 15, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
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