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Bharat B Aggarwal - One of the best experts on this subject based on the ideXlab platform.
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chemical composition and product quality control of turmeric curcuma longa l
Pharmaceutical Crops, 2011Co-Authors: Shiyou Li, Wei Yuan, Guangrui Deng, Ping Wang, Peiying Yang, Bharat B AggarwalAbstract:Chemical constituents of various tissues of turmeric (Curcuma longa L.) have been extensively investigated. To date, at least 235 compounds, primarily phenolic compounds and terpenoids have been identified from the species, in- cluding 22 diarylheptanoids and diarylpentanoids, eight phenylpropene and other phenolic compounds, 68 monoterpenes, 109 sesquiterpenes, five diterpenes, three triterpenoids, four sterols, two alkaloids, and 14 other compounds. Curcumi- noids (diarylheptanoids) and essential oils are major bioactive ingredients showing various bioactivities in in vitro and in vivo bioassays. Curcuminoids in turmeric are primarily accumulated in rhizomes. The essential oils from leaves and flowers are usually dominated by monoterpenes while those from roots and rhizomes primarily contained sesquiterpenes. The contents of Curcuminoids in turmeric rhizomes vary often with varieties, locations, sources, and cultivation condi- tions, while there are significant variations in composition of essential oils of turmeric rhizomes with varieties and geo- graphical locations. Further, both Curcuminoids and essential oils vary in contents with different extraction methods and are unstable with extraction and storage processes. As a result, the quality of commercial turmeric products can be mark- edly varied. While Curcumin (1), demethoxyCurcumin (2), and bisdemethoxyCurcumin (5) have been used as marker com- pounds for the quality control of rhizomes, powders, and extract ("Curcumin") products, Ar-turmerone (99), � -turmerone (100), and � -turmerone (101) may be used to control the product quality of turmeric oil and oleoresin products. Authentication of turmeric products can be achieved by chromatographic and NMR techniques, DNA markers, with morphological and anatomic data as well as GAP and other information available.
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design of Curcumin loaded plga nanoparticles formulation with enhanced cellular uptake and increased bioactivity in vitro and superior bioavailability in vivo
Biochemical Pharmacology, 2010Co-Authors: Preetha Anand, Ajaikumar B. Kunnumakkara, Bokyung Sung, Hareesh B Nair, Vivek R Yadav, Rajeshwar Rao Tekmal, Bharat B AggarwalAbstract:Curcumin, a yellow pigment present in the spice turmeric (Curcuma longa), has been linked with antioxidant, anti-inflammatory, antiproliferative, anticancer, antidiabetic, antirheumatic, and antiviral effects, but its optimum potential is limited by its lack of solubility in aqueous solvents and poor oral bioavailability. We employed a polymer-based nanoparticle approach to improve bioavailability. Curcumin was encapsulated with 97.5% efficiency in biodegradable nanoparticulate formulation based on poly (lactide-co-glycolide) (PLGA) and a stabilizer polyethylene glycol (PEG)-5000. Dynamic laser light scattering and transmission electron microscopy indicated a particle diameter of 80.9 nm. This Curcumin, renamed from hereon "as Curcumin (NP)", was characterized for its biological activity. In vitro Curcumin (NP) exhibited very rapid and more efficient cellular uptake than Curcumin. Estrase staining revealed that Curcumin (NP) was at least as potent as or more potent than Curcumin in inducing apoptosis of leukemic cells and in suppressing proliferation of various tumor cell lines. When examined by electrophoretic gel shift mobility assay, Curcumin (NP) was more active than Curcumin in inhibiting TNF-induced NF-kappaB activation and in suppression of NF-kappaB-regulated proteins involved in cell proliferation (cyclin D1), invasion (MMP-9), and angiogenesis (VEGF). In mice, Curcumin (NP) was more bioavailable and had a longer half-life than Curcumin. Overall we demonstrate that Curcumin-loaded PLGA nanoparticles formulation has enhanced cellular uptake, and increased bioactivity in vitro and superior bioavailability in vivo over Curcumin.
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Curcumin as "Curecumin": From kitchen to clinic
Biochemical Pharmacology, 2008Co-Authors: Ajay Goel, Ajaikumar B. Kunnumakkara, Bharat B AggarwalAbstract:Although turmeric (Curcuma longa; an Indian spice) has been described in Ayurveda, as a treatment for inflammatory diseases and is referred by different names in different cultures, the active principle called Curcumin or diferuloylmethane, a yellow pigment present in turmeric (curry powder) has been shown to exhibit numerous activities. Extensive research over the last half century has revealed several important functions of Curcumin. It binds to a variety of proteins and inhibits the activity of various kinases. By modulating the activation of various transcription factors, Curcumin regulates the expression of inflammatory enzymes, cytokines, adhesion molecules, and cell survival proteins. Curcumin also downregulates cyclin D1, cyclin E and MDM2; and upregulates p21, p27, and p53. Various preclinical cell culture and animal studies suggest that Curcumin has potential as an antiproliferative, anti-invasive, and antiangiogenic agent; as a mediator of chemoresistance and radioresistance; as a chemopreventive agent; and as a therapeutic agent in wound healing, diabetes, Alzheimer disease, Parkinson disease, cardiovascular disease, pulmonary disease, and arthritis. Pilot phase I clinical trials have shown Curcumin to be safe even when consumed at a daily dose of 12 g for 3 months. Other clinical trials suggest a potential therapeutic role for Curcumin in diseases such as familial adenomatous polyposis, inflammatory bowel disease, ulcerative colitis, colon cancer, pancreatic cancer, hypercholesteremia, atherosclerosis, pancreatitis, psoriasis, chronic anterior uveitis and arthritis. Thus, Curcumin, a spice once relegated to the kitchen shelf, has moved into the clinic and may prove to be "Curecumin". © 2007.
Kjohn Cheung - One of the best experts on this subject based on the ideXlab platform.
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Curcumin induces apoptosis in human melanoma cells through a fas receptor caspase 8 pathway independent of p53
Experimental Cell Research, 2001Co-Authors: Jason A Bush, Kjohn CheungAbstract:Abstract In this study, we investigated the molecular pathways targeted by Curcumin during apoptosis of human melanoma cell lines. We found that Curcumin caused cell death in eight melanoma cell lines, four with wild-type and four with mutant p53. We demonstrate that Curcumin-induced apoptosis is both dose- and time-dependent. We found that Curcumin did not induce p53, suggesting that Curcumin activates other apoptosis pathways. Our data show that Curcumin activates caspases-3 and -8 but not caspase-9, supporting the rationale that apoptosis occurs via a membrane-mediated mechanism. Both a caspase-8 and broad-based caspase inhibitor, but not a caspase-9 specific inhibitor, suppressed Curcumin-induced cell death. To further support our hypothesis that Curcumin induces activation of a death receptor pathway, we show that Curcumin induces Fas receptor aggregation in a FasL-independent manner and that low-temperature incubation, previously shown to inhibit receptor aggregation, prevented Curcumin-induced cell death. Moreover, we demonstrate that expression of dominant negative FADD significantly inhibited Curcumin-induced cell death. In addition, our results indicate that Curcumin also blocks the NF-κB cell survival pathway and suppresses the apoptotic inhibitor, XIAP. Since melanoma cells with mutant p53 are strongly resistant to conventional chemotherapy, Curcumin may overcome the chemoresistance of these cells and provide potential new avenues for treatment.
Ajay Goel - One of the best experts on this subject based on the ideXlab platform.
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essential turmeric oils enhance anti inflammatory efficacy of Curcumin in dextran sulfate sodium induced colitis
Scientific Reports, 2017Co-Authors: Shusuke Toden, Arianne L Theiss, Xuan Wang, Ajay GoelAbstract:Turmeric has been used as a medicinal herb for thousands of years for treatment of various disorders. Although Curcumin is the most studied active constituents of turmeric, accumulating evidence suggests that other components of turmeric have additional anti-inflammatory and anti-tumorigenic properties. Herein, we investigated anti-inflammatory efficacy and associated gene expression alterations of a specific, Curcumin preparation containing essential turmeric oils (ETO-Curcumin) in comparison to standard Curcumin at three specific doses (0, 5, 25 or 50 mg/kg), in an animal model of dextran sodium sulfate (DSS)-induced colitis. The present study showed that both ETO and standard Curcumin treatments provided protection against DSS-induced inflammation. However, ETO-Curcumin improved disease activity index (DAI) dose-dependently, while the anti-inflammatory efficacy of standard Curcumin remained constant, suggesting that ETO-Curcumin may provide superior anti-inflammatory efficacy compared to standard Curcumin. Gene expression analysis revealed that anti-inflammatory cytokines including IL-10 and IL-11 as well as FOXP3 were upregulated in the colon by ETO-Curcumin. Collectively, these findings suggest that the combined treatment of Curcumin and essential turmeric oils provides superior protection from DSS-induced colitis than Curcumin alone, highlighting the anti-inflammatory potential of turmeric.
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Curcumin as "Curecumin": From kitchen to clinic
Biochemical Pharmacology, 2008Co-Authors: Ajay Goel, Ajaikumar B. Kunnumakkara, Bharat B AggarwalAbstract:Although turmeric (Curcuma longa; an Indian spice) has been described in Ayurveda, as a treatment for inflammatory diseases and is referred by different names in different cultures, the active principle called Curcumin or diferuloylmethane, a yellow pigment present in turmeric (curry powder) has been shown to exhibit numerous activities. Extensive research over the last half century has revealed several important functions of Curcumin. It binds to a variety of proteins and inhibits the activity of various kinases. By modulating the activation of various transcription factors, Curcumin regulates the expression of inflammatory enzymes, cytokines, adhesion molecules, and cell survival proteins. Curcumin also downregulates cyclin D1, cyclin E and MDM2; and upregulates p21, p27, and p53. Various preclinical cell culture and animal studies suggest that Curcumin has potential as an antiproliferative, anti-invasive, and antiangiogenic agent; as a mediator of chemoresistance and radioresistance; as a chemopreventive agent; and as a therapeutic agent in wound healing, diabetes, Alzheimer disease, Parkinson disease, cardiovascular disease, pulmonary disease, and arthritis. Pilot phase I clinical trials have shown Curcumin to be safe even when consumed at a daily dose of 12 g for 3 months. Other clinical trials suggest a potential therapeutic role for Curcumin in diseases such as familial adenomatous polyposis, inflammatory bowel disease, ulcerative colitis, colon cancer, pancreatic cancer, hypercholesteremia, atherosclerosis, pancreatitis, psoriasis, chronic anterior uveitis and arthritis. Thus, Curcumin, a spice once relegated to the kitchen shelf, has moved into the clinic and may prove to be "Curecumin". © 2007.
Marion L Williams - One of the best experts on this subject based on the ideXlab platform.
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chemopreventive efficacy and pharmacokinetics of Curcumin in the min mouse a model of familial adenomatous polyposis
Cancer Epidemiology Biomarkers & Prevention, 2002Co-Authors: Sarah Perkins, Marion L Williams, William P Steward, Richard D Verschoyle, Kirsti A Hill, Ifat Parveen, Michael D Threadgill, Ricky A Sharma, Andreas J GescherAbstract:Curcumin, the major yellow pigment in turmeric, prevents the development of adenomas in the intestinal tract of the C57Bl/6J Min/+ mouse, a model of human familial APC. To aid the rational development of Curcumin as a colorectal cancer-preventive agent, we explored the link between its chemopreventive potency in the Min/+ mouse and levels of drug and metabolites in target tissue and plasma. Mice received dietary Curcumin for 15 weeks, after which adenomas were enumerated. Levels of Curcumin and metabolites were determined by high-performance liquid chromatography in plasma, tissues, and feces of mice after either long-term ingestion of dietary Curcumin or a single dose of [14C]Curcumin (100 mg/kg) via the i.p. route. Whereas Curcumin at 0.1% in the diet was without effect, at 0.2 and 0.5%, it reduced adenoma multiplicity by 39 and 40%, respectively, compared with untreated mice. Hematocrit values in untreated Min/+ mice were drastically reduced compared with those in wild-type C57Bl/6J mice. Dietary Curcumin partially restored the suppressed hematocrit. Traces of Curcumin were detected in the plasma. Its concentration in the small intestinal mucosa, between 39 and 240 nmol/g of tissue, reflects differences in dietary concentration. [14C]Curcumin disappeared rapidly from tissues and plasma within 2–8 h after dosing. Curcumin may be useful in the chemoprevention of human intestinal malignancies related to Apc mutations. The comparison of dose, resulting Curcumin levels in the intestinal tract, and chemopreventive potency suggests tentatively that a daily dose of 1.6 g of Curcumin is required for efficacy in humans. A clear advantage of Curcumin over nonsteroidal anti-inflammatory drugs is its ability to decrease intestinal bleeding linked to adenoma maturation.
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metabolism of the cancer chemopreventive agent Curcumin in human and rat intestine
Cancer Epidemiology Biomarkers & Prevention, 2002Co-Authors: Christopher R Ireson, Donald J L Jones, Samantha Orr, Michael W H Coughtrie, David J Boocock, Marion L Williams, Peter B Farmer, William P Steward, Andreas J GescherAbstract:Curcumin, the yellow pigment in turmeric, prevents malignancies in the intestinal tract of rodents. It is under clinical evaluation as a potential colon cancer chemopreventive agent. The systemic bioavailability of Curcumin is low, perhaps attributable, at least in part, to metabolism. Indirect evidence suggests that Curcumin is metabolized in the intestinal tract. To investigate this notion further, we explored Curcumin metabolism in subcellular fractions of human and rat intestinal tissue, compared it with metabolism in the corresponding hepatic fractions, and studied Curcumin metabolism in situ in intact rat intestinal sacs. Analysis by high-performance liquid chromatography, with detection at 420 or 280 nm, permitted characterization of Curcumin conjugates and reduction products. Chromatographic inferences were corroborated by mass spectrometry. Curcumin glucuronide was identified in intestinal and hepatic microsomes, and Curcumin sulfate, tetrahydroCurcumin, and hexahydroCurcumin were found as Curcumin metabolites in intestinal and hepatic cytosol from humans and rats. The extent of Curcumin conjugation was much greater in intestinal fractions from humans than in those from rats, whereas Curcumin conjugation was less extensive in hepatic fractions from humans than in those from rats. The Curcumin-reducing ability of cytosol from human intestinal and liver tissue exceeded that observed with the corresponding rat tissue by factors of 18 and 5, respectively. Curcumin sulfate was identified in incubations of Curcumin with intact rat gut sacs. Curcumin was sulfated by human phenol sulfotransferase isoenzymes SULT1A1 and SULT1A3. Equine alcohol dehydrogenase catalyzed the reduction of Curcumin to hexahydroCurcumin. The results show that Curcumin undergoes extensive metabolic conjugation and reduction in the gastrointestinal tract and that there is more metabolism in human than in rat intestinal tissue. The pharmacological implications of the intestinal metabolism of Curcumin should be taken into account in the design of future chemoprevention trials of this dietary constituent.
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characterization of metabolites of the chemopreventive agent Curcumin in human and rat hepatocytes and in the rat in vivo and evaluation of their ability to inhibit phorbol ester induced prostaglandin e2 production
Cancer Research, 2001Co-Authors: Christopher R Ireson, Donald J L Jones, Samantha Orr, Richard D Verschoyle, C K Lim, Jinli Luo, Lynne M Howells, Simon Plummer, Rebekah Jukes, Marion L WilliamsAbstract:Curcumin, the yellow pigment in turmeric, has been shown to prevent malignancies in a variety of tissues in rodents, especially in the intestinal tract. Pharmacological activities of Curcumin in cells in situ germane to chemoprevention, such as inhibition of expression of cyclooxygenase-2 (COX-2), require drug concentrations in the 10(-5) - 10(-4) M range. The systemic bioavailability of Curcumin is low, so that its pharmacological activity may be mediated, in part, by Curcumin metabolites. To investigate this possibility, we compared Curcumin metabolism in human and rat hepatocytes in suspension with that in rats in vivo. Analysis by high-performance liquid chromatography with detection at 420 and 280 nm permitted characterization of metabolites with both intact diferoylmethane structure and increased saturation of the heptatrienone chain. Chromatographic inferences were corroborated by mass spectrometry. The major metabolites in suspensions of human or rat hepatocytes were identified as hexahydroCurcumin and hexahydroCurcuminol. In rats, in vivo, Curcumin administered i.v. (40 mg/kg) disappeared from the plasma within 1 h of dosing. After p.o. administration (500 mg/kg), parent drug was present in plasma at levels near the detection limit. The major products of Curcumin biotransformation identified in rat plasma were Curcumin glucuronide and Curcumin sulfate whereas hexahydroCurcumin, hexahydroCurcuminol, and hexahydroCurcumin glucuronide were present in small amounts. To test the hypothesis that Curcumin metabolites resemble their progenitor in that they can inhibit COX-2 expression, Curcumin and four of its metabolites at a concentration of 20 microM were compared in terms of their ability to inhibit phorbol ester-induced prostaglandin E2 (PGE2) production in human colonic epithelial cells. Curcumin reduced PGE2 levels to preinduction levels, whereas tetrahydroCurcumin, previously shown to be a murine metabolite of Curcumin, hexahydroCurcumin, and Curcumin sulfate, had only weak PGE2 inhibitory activity, and hexahydroCurcuminol was inactive. The results suggest that (a) the major products of Curcumin biotransformation by hepatocytes occur only at low abundance in rat plasma after Curcumin administration; and (b) metabolism of Curcumin by reduction or conjugation generates species with reduced ability to inhibit COX-2 expression. Because the gastrointestinal tract seems to be exposed more prominently to unmetabolized Curcumin than any other tissue, the results support the clinical evaluation of Curcumin as a colorectal cancer chemopreventive agent.
Xiaoyong Wang - One of the best experts on this subject based on the ideXlab platform.
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shift of acid base equilibrium of Curcumin in its complexes with gemini surfactant hexamethylene 1 6 bis dodecyldimethyl ammonium bromide
Colloids and Surfaces A: Physicochemical and Engineering Aspects, 2014Co-Authors: Xiaoyong WangAbstract:Abstract Surfactant micelles are suitable carriers for solubilizing and stabilizing Curcumin that is a natural polyphenolic compound with many biological and pharmacological activities but suffers poor bioavailability. In this paper, the acid–base equilibrium of Curcumin (Cur 0 = Cur − + H + ) has been studied in surfactant concentration dependent complexes of Curcumin with gemini surfactant hexamethylene-1,6-bis-(dodecyldimethyl ammonium bromide) (12-6-12). The absorption and fluorescence spectra of Curcumin show that Cur − electrostatically binds with cationic 12-6-12 monomer to form Curcumin/monomer complexes, whereas Cur 0 and Cur − are located in the palisade layer of 12-6-12 aggregates with different positions in Curcumin/premicelle and Curcumin/micelle complexes. The increase of surfactant concentration often leads to the right-shift of acid–base equilibrium of Curcumin and higher amount of anionic Cur − , as shown in the fluorescence spectra, p K a1 and [Cur − ]/[Cur 0 ] of Curcumin. By contrast, the added salt is found to be beneficial for Curcumin to shift the acid–base equilibrium to the left side and keep in neutral Cur 0 .
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binding of Curcumin with bovine serum albumin in the presence of ι carrageenan and implications on the stability and antioxidant activity of Curcumin
Journal of Agricultural and Food Chemistry, 2013Co-Authors: Mingling Yang, Haibo Zhou, Xiaoyong WangAbstract:This work studied the influences of formation of BSA/ι-carrageenan complexes on the binding, stability, and antioxidant activity of Curcumin. In the presence of BSA and ι-carrageenan, Curcumin gives higher intensities of absorption and fluorescence than free Curcumin and Curcumin only combined with BSA. The added ι-carrageenan is observed to promote Curcumin for quenching the instrinsic fluorescence of BSA. These results are explained in terms of the formation of BSA/ι-carrageenan complexes, which help to stabilize the folded structure of BSA for providing Curcumin with a more hydrophobic microenvironment. The small difference in anisotropy values of Curcumin with BSA alone and of BSA/ι-carrageenan complexes suggests that ι-carrageenan acts as outer stretch conformation in BSA/ι-carrageenan complexes but does not directly disturb the hydrophobic pockets inside BSA, where Curcumin is hydrophobically located. The determined values of the binding constant are higher for Curcumin with BSA/ι-carrageenan comple...
