curcumin and cinnamaldehyde

The World Health Organization (WHO) for some years has been focusing on what is now commonly referred to as an "epidemic of obesity and diabetes" ("diabesity"): behind this outbreak, there are several risk factors grouped in what is called "metabolic syndrome" (MetS). The basis of this "epidemic" is either a diet too often characterized by excessive consumption of saturated and trans-esterified fatty acids, simple sugars and salt, either a sedentary lifestyle.. The aim of this review is to focus on the phytochemicals that have a more positive effect on the treatment and/or prevention of MetS.. Treatment strategies for MetS include pharmacologic and non-pharmacologic options, with varying degrees of success rate. The first is indicated for patients with high cardiovascular risk, while the second one is the most cost-effective preventive approach for subjects with borderline parameters and for patients intolerant to pharmacological therapy. MetS non-pharmacological treatments could involve the use of nutraceuticals, most of which has plant origins (phytochemicals), associated with lifestyle improvement. The chapter will discuss the available evidence on soluble fibres from psyllium and other sources, cinnamaldehyde, cinnamic acid and other cinnamon phytochemicals, berberine, corosolic acid from banaba, charantin from bitter gourd, catechins and flavonols from green tea and cocoa. Vegetable omega-3 polyunsaturated fatty acids, alliin from garlic, soy peptides, and curcumin from curcuma longa.. Some nutraceuticals, when adequately dosed, should improve a number of the MetS components.

Topics: Acrolein; Berberine; Catechin; Cinnamates; Curcumin; Diet; Dietary Fiber; Dietary Supplements; Fatty Acids, Omega-3; Flavonols; Humans; Metabolic Syndrome; Phytochemicals; Psyllium

Two phytonutrient mixtures, VAC (carvacrol, cinnamaldehyde, and Capsicum oleoresin), and MC (Capsicum oleoresin and turmeric oleoresin), were evaluated for their effects on chicken immune responses following immunization with an Eimeria profilin protein. Chickens were fed with a non-supplemented diet, or with VAC- or MC-supplemented diets, immunized with profilin, and orally challenged with virulent oocysts of Eimeria tenella. Immunity against infection was evaluated by body weight, fecal oocyst shedding, profilin antibody levels, lymphocyte recall responses, cytokine expression, and lymphocyte subpopulations. Following immunization and infection, chickens fed the VAC- or MC-supplemented diets showed increased body weights, greater profilin antibody levels, and/or greater lymphocyte proliferation compared with non-supplemented controls. Prior to Eimeria infection, immunized chickens on the MC-supplemented diet showed reduced IFN-γ and IL-6 levels, but increased expression of TNFSF15, compared with non-supplemented controls. Post-infection levels of IFN-γ and IL-6 were increased, while IL-17F transcripts were decreased, with MC-supplementation. For VAC-supplemented diets, decreased IL-17F and TNFSF15 levels were observed only in infected chickens. Finally, immunized chickens fed the MC-supplemented diet exhibited increased MHC class II(+), CD4(+), CD8(+), TCR1+, or TCR2(+) T cells compared with nonsupplemented controls. Animals on the VAC-containing diet only displayed an increase in K1(+) macrophages. In conclusion, dietary supplementation with VAC or MC alters immune parameters following recombinant protein vaccination against avian coccidiosis.

Topics: Acrolein; Animal Feed; Animal Nutritional Physiological Phenomena; Animals; Antibodies, Protozoan; Capsicum; Cell Proliferation; Chickens; Coccidiosis; Curcuma; Cymenes; Cytokines; Dietary Supplements; Eimeria tenella; Feces; Gene Expression Regulation; Lymphocytes; Monoterpenes; Plant Extracts; Poultry Diseases; Profilins; Protozoan Vaccines; RNA, Messenger; Spleen; Weight Gain

In transdermal drug delivery systems, the physicochemical properties of the drug affect its percutaneous permeability. However, whether the physicochemical properties of drugs change their transdermal permeability in the presence of pores in the presence of solid microneedles (MNs) has been less studied in this area. In this project, cinnamaldehyde, curcumin, ferulic acid and geniposide were selected as model drugs for the study of their transdermal permeability under the action of MNs, and a combination of classical experiments and visualization means such as scanning electron microscopy and laser confocal was used to investigate the permeation-promoting mechanism of MNs. The results showed that the MNs had significant permeation-promoting effects on different properties of drugs, with the permeation-promoting effects on cinnamaldehyde, curcumin, ferulic acid and geniposide being 6.36, 17.43, 29.54 and 8.91 times, respectively, and the permeation-promoting effects were more pronounced for lipid-soluble and amphiphilic drugs. Using scanning electron microscopy, transmission electron microscopy and other means to confirm that MNs can promote the penetration by acting on the skin to produce pores, and their effect on skin structure is greater than that of drugs. In addition, the existence of pores increases the amount of drug transdermal, which may enhance the diffusion of drug on the skin, and has no effect on lipid exchange and transdermal route. Through the research, it has been found that MNs is equivalent to direct peeling of the stratum corneum (SC), but it is simpler and safer for the patient.

Topics: Administration, Cutaneous; Curcumin; Drug Delivery Systems; Humans; Lipids; Needles; Permeability; Pharmaceutical Preparations; Skin

Topics: Animals; Anti-Bacterial Agents; Chitosan; Curcumin; Escherichia coli; Hydrogen-Ion Concentration; Pork Meat; Red Meat; Staphylococcus aureus; Swine; Zein

In this study, the effects of cinnamaldehyde and curcumin on Akt2, a serine/threonine protein kinase central to the insulin signaling pathway, were examined in preadipocytes. Cinnamaldehyde or curcumin treatment increased Akt2 phosphorylation at multiple sites including T450 and Y475, but had no effect on Akt2 phosphorylation at S474, which is critical for Akt2 activation. Surprisingly, insulin treatment with cinnamaldehyde or curcumin increased p-Akt2 (S474) by 3.5-fold versus insulin treatment alone. Furthermore, combined cinnamaldehyde, curcumin, and insulin treatment increased p-Akt2 (S474) by 7-fold versus insulin treatment alone. Interestingly, cinnamaldehyde and curcumin inhibited both serine/threonine phosphatase 2A (PP2A) and protein tyrosine phosphatase 1B (PTP1B). Akt2 activation is a multistep process that requires phosphorylation at T450 for proper folding and maturation, and phosphorylation of both Y475 and S474 for stabilization of the catalytic domain. It is plausible that by inhibiting PP2A and PTP1B, cinnamaldehyde and curcumin increase phosphorylation at T450 and Y475, and prime Akt2 for insulin-stimulated phosphorylation at S474. Notably, the combination of a PP2A inhibitor, okadaic acid, and a PTP1B inhibitor increased p-Akt2 (S474), even in the absence of insulin. Future combinations of PP2A and PTP1B inhibitors provide a rational platform to engineer new therapeutics for insulin resistance syndrome.

Topics: Acrolein; Curcumin; Enzyme Inhibitors; Insulin; Phosphorylation; Serine

Maintaining healthy body weight is an important component of any effective diabetes management plan. However, glycemic management using insulin generally leads to weight gain. In addition, weight loss medications prescribed for diabetes management are often associated with adverse side effects, which limit their long-term usage. Alternatively, nutrition intervention provides a safe, readily accessible, and inexpensive option for diabetes management. This study describes a composition of phytonutrients comprising berberine, cinnamaldehyde, and curcumin for glycemic and weight management. Functional complementarity between berberine, cinnamaldehyde, and curcumin provides an effective means to improve insulin sensitivity without increasing adiposity. In primary human omental preadipocytes, cinnamaldehyde and curcumin additively enhance insulin-stimulated activation of Akt2 and glucose uptake, whereas berberine inhibits de novo fatty acid biosynthesis and fat cell differentiation. In a diet-induced obesity murine model, a dietary supplement with berberine, cinnamaldehyde, and curcumin prevents weight gain, improves glucose tolerance, and reduces HbA1c, blood lipids, visceral adiposity, and liver steatosis. Collectively, the composition of phytonutrients comprising berberine, cinnamaldehyde, and curcumin protects against obesity and pre-diabetic conditions in a diet-induced obesity murine model. Safety and efficacy assessment of nutrition intervention using combined berberine, cinnamaldehyde, and curcumin for glycemic and weight management in future clinical trials are warranted.

Topics: Acrolein; Animals; Berberine; Blood Glucose; Curcumin; Diabetes Mellitus; Disease Models, Animal; Fatty Acids; Glycated Hemoglobin; Humans; Insulin; Insulin Resistance; Lipids; Mice; Obesity; Phytochemicals; Weight Gain

This study aimed to investigate the effectiveness of five natural plant extract compounds Curcumin (CUR); Eugenol (EUG), Cinnamaldehyde (CIN), Stigmasterol (ST) and Morin (MOR), on two species of Saprolegnia; Saprolegnia parasitica and S. australis. Selective compounds were screened for the minimum inhibitory concentration, first for anti-oomycetes activity and then mycelium growth inhibition, spore germination inhibition and colonisation test. Nitric oxide production and myeloperoxidase activity of the compounds were tested in head kidney leukocytes of rainbow trout, Oncorhynchus mykiss to assess the immunostimulatory potential. Molecular docking of effective compounds was carried out with effector proteins of S. parasitica to investigate the target binding sites. Among all, CUR could completely inhibit zoospore production and significantly (p ≤ .05) inhibit hyphal growth at 16 mg l

Topics: Acrolein; Animals; Cell Survival; Curcumin; Dose-Response Relationship, Drug; Eugenol; Head Kidney; Leukocytes; Microbial Sensitivity Tests; Molecular Docking Simulation; Oncorhynchus mykiss; Plant Extracts; Saprolegnia

The objective of the study was to evaluate the cytotoxicity and effect of curcumin-cinnamaldehyde hybrids (CCHs) on the biofilm of oral pathogens. Of the 18 hybrids tested, nine had an inhibitory effect on at least one of the bacterial species tested, with minimal inhibitory and bactericidal concentrations ranging from 9 to 625 μg ml

Topics: Acrolein; Anti-Bacterial Agents; Biofilms; Chlorhexidine; Curcumin; Microbial Sensitivity Tests

The objective of this study was to determine whether curcumin and a commercial microencapsulated phytogenic supplement containing thymol, cinnamaldehyde and carvacrol in broiler chicken feed would improve health and meat quality (fatty acid profile), as well as to determine the coccidiostatic and bactericidal potential of the additives. The broiler chickens were divided into five groups: NC - negative control feed; PC - positive control; CU - with 50 mg/kg of curcumin, PHY - 100 mg/kg phytogenic; and PHY + CU, a combination of both additives at 50 mg/kg (curcumin) and 100 mg/kg (phytogenic). We observed significantly higher levels of total proteins associated with increased circulating globulins, as well as lower levels of uric acid, cholesterol and triglycerides in the PHY + CU group than in the NC. There were significantly fewer oocysts in birds supplemented with additives in the NC group on day 21; on day 35, the NC, PHY and PHY + CU groups had significantly lower counts than the PC and CU groups; however, at 44 days, the lowest counts were in PC group. The bacterial counts were significantly lower on day 21 in all groups that received additives than those of the control group; however, at 44 days, the bacterial and Escherichia coli counts in these groups were significantly higher than those of the control. Curcumin with or without phytogenic agent improved meat quality, with increased antioxidant levels and reduction of lipid peroxidation. There were significantly lower total saturated fatty acid levels and significantly greater monounsaturated/polyunsaturated fatty acid levels in broilers that consumed additives individually and in combination. The combination of additives significantly increased the crypt/villus ratio, a marker of improved intestinal health and performance. Additives potentiated their individual effects, suggesting they can replace conventional growth promoters without compromising health, intestinal mucosa or meat quality.

Topics: Acrolein; Animal Feed; Animals; Bacteria; Bacterial Infections; Chickens; Coccidia; Coccidiosis; Curcumin; Cymenes; Dietary Supplements; Fatty Acids; Meat; Poultry Diseases; Thymol

Bacteriocins are small peptides that can inhibit the growth of a diverse range of microbes. There is a need to identify bacteriocins that are effective against biofilms of resistant clinical strains. The present study focussed on the efficacy of purified nisin like bacteriocin-GAM217 against extended spectrum β-lactamase (ESBL) and metallo-beta-lactamase (MBL) producing clinical strains. Bacteriocin-GAM217 when combined with curcumin and cinnamaldehyde, synergistically enhanced antibacterial activity against planktonic and biofilm cultures of

Topics: Acrolein; Animals; Anti-Bacterial Agents; Bacteriocins; beta-Lactamases; Biofilms; Chlorocebus aethiops; Curcumin; Microbial Sensitivity Tests; Nisin; Vero Cells

Protein tyrosine phosphatase (PTP1B) is a potential target for the treatment of type 2 diabetes and cancer. Curcumin and cinnamaldehyde have been previously reported to have antidiabetic and anticancer potentials. The aim of this study was to investigate the effect of curcumin in comparison to cinnamaldehyde on the enzymatic activity of PTP1B and the viability of MCF-7 cancer cells.. Enzymatic activity and cell viability assays were utilized. Experiments were performed using the breast cancer MCF-7 cell line.. Curcumin and cinnamaldehyde decreased the activity of PTP1B, and had inhibitory effects on the viability of MCF-7 cancer cells. Curcumin had a significantly higher inhibitory effect than cinnamaldehyde.. Curcumin can be considered a potential agent for the treatment of type-2 diabetes or cancer.

Topics: Acrolein; Antineoplastic Agents; Breast Neoplasms; Cell Survival; Curcumin; Diabetes Mellitus, Type 2; Drug Screening Assays, Antitumor; Female; Humans; Hypoglycemic Agents; MCF-7 Cells; Protein Tyrosine Phosphatase, Non-Receptor Type 1

Staphylococcus epidermidis is reported to be the main causative agent of nosocomial infections. It has become increasingly difficult to treat this micro-organism because of the emergence of new antibiotic-resistant strains and its ability to form biofilm on medical associated devices. Phytochemicals acting in synergy are effective in killing the micro-organisms by lowering the doses, and synergistic compounds evade the development of resistance due to different mechanism of action. This study aims to determine the synergistic antimicrobial potential of curcumin with cinnamaldehyde, eugenol, and ellagic acid against S. epidermidis. Curcumin with ellagic acid as well as eugenol were found to have additive antimicrobial effect, whereas, in combination, curcumin and cinnamaldehyde were found to have synergistic effect against S. epidermidis (fractional inhibitory concentration index (FICI) = 0.5). Synergy between curcumin and cinnamaldehyde was established by time-kill kinetics and was further evaluated for antibiofilm activity. The dose required to inhibit biofilm formation was reduced to half than that needed to inhibit its planktonic culture (minimal inhibitory concentration (MIC) of curcumin = 3.12 μg/ml; MIC of cinnamaldehyde = 15.62 μg/ml; FICI = 0.248). Both curcumin and cinnamaldehyde disrupted the bacterial membrane for killing the bacteria as determined by permeability studies on Escherichia coli ML-35p.

Topics: Acrolein; Algorithms; Anti-Bacterial Agents; Anti-Infective Agents; Curcumin; Drug Synergism; Ellagic Acid; Eugenol; Molecular Structure; Staphylococcus epidermidis

Cinnamaldehyde, its derivatives and curcumin are reported to have strong antifungal activity. In this work we report and compare anticandidal activity of curcumin (CUR) and α-methyl cinnamaldehyde (MCD) against 38 strains of Candida (3; standard, fluconazole sensitive, 24; clinical, fluconazole sensitive, 11; clinical, fluconazole resistant). The minimum inhibitory concentrations (MIC₉₀) of CUR ranged from 250 to 650 μg/ml for sensitive strains and from 250 to 500 μg/ml for resistant strains. MIC₉₀ of MCD varied between 100 and 250 μg/ml and 100-200 μg/ml for sensitive and resistant strains, respectively. Higher activity of MCD as compared to CUR was further reinforced by spot assays and growth curve studies. At their respective MIC₉₀ values, in the presence of glucose, average inhibition of H+-efflux caused by CUR and MCD against standard, clinical and resistant isolates was 24%, 31%, 32% and 54%, 52%, 54%, respectively. Inhibition of H+-extrusion leads to intracellular acidification and cell death, average pHi for control, CUR and MCD exposed cells was 6.68, 6.39 and 6.20, respectively. Scanning electron micrographs of treated cells show more extensive damage in case of MCD. Haemolytic activity of CUR and MCD at their highest MIC was 11.45% and 13.00%, respectively as against 20% shown by fluconazole at typical MIC of 30 μg/ml. In conclusion, this study shows significant anticandidal activity of CUR and MCD against both azole-resistant and sensitive clinical isolates, MCD is found to be more effective.

Topics: Acrolein; Antifungal Agents; Candida; Curcumin; Drug Resistance; Erythrocytes; Fluconazole; Hemolysis; Humans; Plant Extracts

Spice active principles are reported to have anti-diabetic, anti-hypercholesterolemic, antilithogenic, anti-inflammatory, anti-microbial and anti-cancer properties. In our previous report we have shown that spices and their active principles inhibit 5-lipoxygenase and also formation of leukotriene C4. In this study, we report the modulatory effect of spice active principles viz., eugenol, capsaicin, piperine, quercetin, curcumin, cinnamaldehyde and allyl sulphide on in vitro human platelet aggregation. We have demonstrated that spice active principles inhibit platelet aggregation induced by different agonists, namely ADP (50microM), collagen (500microg/ml), arachidonic acid (AA) (1.0mM) and calcium ionophore A-23187 (20microM). Spice active principles showed preferential inhibition of arachidonic acid-induced platelet aggregation compared to other agonists. Among the spice active principles tested, eugenol and capsaicin are found to be most potent inhibitors of AA-induced platelet aggregation with IC50 values of 0.5 and 14.6microM, respectively. The order of potency of spice principles in inhibiting AA-induced platelet aggregation is eugenol>capsaicin>curcumin>cinnamaldehyde>piperine>allyl sulphide>quercetin. Eugenol is found to be 29-fold more potent than aspirin in inhibiting AA-induced human platelet aggregation. Eugenol and capsaicin inhibited thromboxane B2 (TXB2) formation in platelets in a dose-dependent manner challenged with AA apparently by the inhibition of the cyclooxygenase (COX-1). Eugenol-mediated inhibition of platelet aggregation is further confirmed by dose-dependent decrease in malondialdehyde (MDA) in platelets. Further, eugenol and capsaicin inhibited platelet aggregation induced by agonists-collagen, ADP and calcium ionophore but to a lesser degree compared to AA. These results clearly suggest that spice principles have beneficial effects in modulating human platelet aggregation.

Topics: Acrolein; Adenosine Diphosphate; Alkaloids; Allyl Compounds; Arachidonic Acid; Benzodioxoles; Calcimycin; Capsaicin; Collagen Type III; Curcumin; Eugenol; Humans; Malondialdehyde; Piperidines; Platelet Aggregation; Platelet Aggregation Inhibitors; Polyunsaturated Alkamides; Quercetin; Spices; Sulfides; Thromboxanes

In this study, chemical compositions of hydrodistilled essential oil and anti-inflammatory activities from the twigs of Cinnamomum osmophloeum Kaneh. were investigated for the first time. The chemical constituents of the twig essential oil were further analyzed by GC-MS and they were found to be L-bornyl acetate (15.89%), caryophyllene oxide (12.98%), gamma-eudesmol (8.03%), beta-caryophyllene (6.60%), T-cadinol (5.49%), delta-cadinene (4.79%), trans-beta-elemenone (4.25%), cadalene (4.19%), and trans-cinnamaldehyde (4.07%). The effects of essential oil on nitric oxide (NO) and prostaglandin E2 (PGE2) production in lipopolysaccharide (LPS)-activated RAW 264.7 macrophages were also examined. Results of nitric oxide tests indicated that twig essential oil and its major constituents such as trans-cinnamaldehyde, caryophyllene oxide, L-borneol, L-bornyl acetate, eugenol, beta-caryophyllene, E-nerolidol, and cinnamyl acetate have excellent activities. These findings demonstrated that essential oil of C. osmophloeum twigs have excellent anti-inflammatory activities and thus have great potential to be used as a source for natural health products.

Topics: Acrolein; Animals; Anti-Inflammatory Agents; Cell Death; Cell Line; Cinnamomum; Curcumin; Dinoprostone; Humans; Lipopolysaccharides; Mice; Nitric Oxide; Oils, Volatile

In the present study the irreversible inhibition of human glutathione S-transferase P1-1 (GSTP1-1) by alpha, beta-unsaturated aldehydes and ketones was studied. When GSTP1-1 was incubated with a 50-fold molar excess of the aldehydes acrolein (ACR) and 4-hydroxy-2-nonenal (HNE) and the ketones curcumin (CUR) and ethacrynic acid (EA) at 22 degrees C, all of them inactivated GSTP1-1. The remaining activity after 4 h of incubation in all cases was lower than 10%. The aldehydes crotonaldehyde (CRA), cinnamaldehyde (CA) and trans-2-hexenal were found to inhibit GSTP1-1 only at a 5000-fold molar excess and even then, for example, for CA a higher remaining activity of 17% was observed. The same inhibition experiments were conducted with 3 mutants of GSTP1-1: the C47S and C101S mutants and the double mutant C47S/C101S. Remaining activity for C47S varied between +/- 40% for CRA, CA, CUR and HEX and +/- 80% for ACR, EA and HNE. For C101S it varied between 0 and 9% and for the double mutant C47S/C101S, activity after 4 h of incubation was variable. Again it varied between +/- 40% for CRA, CA, CUR and HEX and +/- 80% for ACR, EA and HNE. EA is known to react almost exclusively with cysteine 47. When [14C]EA was incubated with the GSTP1-1, modified by the alpha, beta-unsaturated carbonyl compounds, no [14C]EA was incorporated in the enzyme, indicating that in all cases this cysteine residue was one of the major targets. Since Michael addition with these reagents is known to be reversible, the results of incubation of the inactivated enzymes with an excess of glutathione (GSH) were determined. For all compounds, a restoration of the catalytic activity was observed. The results indicate that alpha, beta-unsaturated carbonyl derivatives inhibit GSTP1-1 irreversibly mainly by binding to cysteine residues of GSTP1-1, especially Cys-47, This means that some of these compounds (e.g. CUR) might modify GST activity in vivo when GSH concentrations are low by covalent binding to the enzyme.

Topics: Acrolein; Aldehydes; Curcumin; Cysteine Proteinase Inhibitors; Enzyme Inhibitors; Ethacrynic Acid; Glutathione S-Transferase pi; Glutathione Transferase; Humans; Isoenzymes; Ketones; Mutagenesis, Site-Directed

The glutathione S-transferase (GST) activity towards 1-chloro-2,4-dinitrobenzene in intact human IGR-39 melanoma cells was determined by the quantification by HPLC-analysis of the excreted glutathione (GSH) conjugate (S-(2,4-dinitrophenyl)glutathione; DNPSG). The major GST subunit expressed in these melanoma cells is the pi-class GST subunit P1. Using this system, the effect of exposure for 1 h to a series of alpha, beta-unsaturated carbonyl compounds at non-toxic concentrations was studied. Curcumin was the most potent inhibitor (96% inhibition at 25 microM), while 67 and 61% inhibition at 25 microM was observed for ethacrynic acid and trans-2-hexenal, respectively. Moderate inhibition was observed for cinnamaldehyde and crotonaldehyde, while no inhibition was found for citral. The reactive acrolein did not inhibit the DNPSG-excretion at 2.5 microM, the highest non-toxic concentration. Up to about 50% GSH-depletion was found after treatment with crotonaldehyde, curcumin and ethacrynic acid, however the consequences for GST conjugation are presumably small. Reversible inhibition of GST was the major mechanism of inhibition of DNPSG-excretion in melanoma cells, except in the cases of curcumin and ethacrynic acid, which compounds also inactivated GSTP1-1 by covalent modification. This was clear from the fact that depending on the dose between 30 and 80% inhibition was still observed after lysis of the cells, under which conditions reversible inhibition was is absent. Intracellular levels of DNPSG remained relatively high in the case of ethacrynic acid. It is possible that ethacrynic acid also inhibits the transport of DNPSG by inhibition of the multidrug resistance-associated protein gene encoding glutathione conjugate export pump (MRP/GS-X pump) in some way.

Topics: Acrolein; Acyclic Monoterpenes; Aldehydes; Chromatography, High Pressure Liquid; Curcumin; Enzyme Inhibitors; Ethacrynic Acid; Glutathione; Glutathione Transferase; Humans; Melanoma; Monoterpenes; Skin Neoplasms; Terpenes; Tumor Cells, Cultured