Inhibitory effects of curcumin and piperine on fluorescent advanced glycation end products formation in a bovine serum albumin–fructose model

This study investigated the inhibitory effects of curcumin and piperine on fluorescent advanced glycation end products (fAGEs) formation in a bovine serum albumin (BSA)–fructose model. Model systems of BSA and fructose were prepared, and curcumin or piperine was added. fAGEs and BSA oxidation product (dityrosine, kynurenine and N'-formylkynurenine) contents were determined. The results showed that fAGEs content decreased with increasing concentration of curcumin and piperine (P < 0.05). Addition of curcumin and piperine at 160 µg mL⁻¹ could inhibit fluorescent AGEs by 100% and 93% respectively. Dityrosine and N'-formylkynurenine contents decreased as curcumin and piperine concentration increased (P < 0.05). Furthermore, the result of principal component analysis indicated that curcumin and piperine markedly impeded BSA oxidation, resulting in a lower level of fAGEs in model systems. Therefore, adding curcumin and piperine may facilitate reduced fAGEs levels in BSA–fructose model.     

Curcumin loaded fish scale collagen-HPMC nanogel for wound healing application: Ex-vivo and In-vivo evaluation

The objective of the present investigation was to formulate curcumin loaded fish scale collagen (FSC)-hydroxypropyl methyl cellulose (HPMC K100) nanogel (CNG) for wound healing application. The curcumin nanoemulsion was prepared, characterized and loaded in FSC-HPMC nanogel. The nanogel was evaluated for ex-vivo permeation, in-vivo, skin irritation, and stability study. Ex-vivo permeation study demonstrated that CNG prolonged release and exhibited higher percent contraction value of wound compared to other formulations. In skin irritation study, formulation produced the score of less than 2 compared to control. It concluded that curcumin loaded FSC-HPMC nanogel could be prepared for wound healing applications.     

Curcumin antifungal and antioxidant activities are increased in the presence of ascorbic acid

The objective of this study was to evaluate the antifungal and antioxidant activities of curcumin, ascorbic acid and the mixture of these two compounds. For the antifungal assay, the minimum inhibitory concentrations (MIC) were determined using Candida strains (ATCC and clinical isolates). Curcumin alone inhibited growth of Candida albicans yeast cells, whereas ascorbic acid did not present effects. However, when the mixture of ascorbic acid and curcumin was assayed to determine the association of the two compounds, the curcumin MIC decreased 5- to 10-fold. In the antioxidant assays, the sum of the alone activities of curcumin and ascorbic acid were lower than the activity of the two-compound mixture. This study highlights the importance of the association between two common antioxidants in foods, to improve the antifungal and antioxidant activities of curcumin (in vitro), and can be applied to Candida spp. infection and diseases associated with oxidative stress.     

Curcumin based nanomedicines as efficient nanoplatform for treatment of cancer: New developments in reversing cancer drug resistance,rapid internalization,and improved anticancer efficacy

BackgroundCancer is a group of diseases involving an abnormal growth of cells which tend to proliferate in an uncontrolled fashion and in some cases metastasize to the surrounding tissues (malignancy). Resistance to chemotherapy is typically intrinsic (heterogeneity); however, acquired resistance has also become prevelant due to multiple factors including expression of energy-dependent transporters causing expulsion of internalized drug contents extracellular, insensitivity of tumor cells to drug-induced apoptosis, and induction of drug-detoxifying mechanisms. Curcumin (CUR) has gained widespread recognition due to remarkable anticancer, anti-mutagenic, and anti-metastasizing potentials via downregulation of proliferation of cancer cells and induction of apoptosis. Nevertheless, pharmaceutical significance and therapeutic feasibility of CUR is restricted due to intrinsic physicochemical characteristics including poor aqueous solubility, inadequate biological stability, low bioavailability, and short half-life.Scope and approachOwing to these pharmaceutical limitations of CUR, nanodelivery systems have attained remarkable fascination in the recent years. Therefore, this review was aimed to overview and critically ponders recent developments in improving anticancer viability of CUR.Key findings and conclusionCritical analysis of the literature revealed that nanodelivery systems showed promising efficiency in achieving tumor specific targetability, maximizing internalization of drugs into cancer cells, mitigating tumor metastasis, as well as improving anticancer efficacy of CUR. Moreover, nanocarrier-mediated improved pharmacokinetics, drug accumulation, induced promising cytotoxicity, and enhanced anticancer efficacy by suppressing Egr-1 induction, Mitogen-activated protein kinase (MAPK) pathway, and protein tyrosine kinase (PTK) cascades while mitigating the progression of tumor, have also been discussed.     

Inhibitory effects of curcumin on activity of cytochrome P450 2C9 enzyme in human and 2C11 in rat liver microsomes

Cytochrome P450 2C9 (CYP2C9), one of the most important phase I drug metabolizing enzymes, could catalyze the reactions that convert diclofenanc into diclofenac 4′-hydroxylation. Evaluation of the inhibitory effects of compounds on CYP2C9 is clinically important because inhibition of CYP2C9 could result in serious drug–drug interactions. The objective of this work was to investigate the effects of curcumin on CYP2C9 in human and cytochrome P450 2C11 (CYP2C11) in rat liver microsomes. The results showed that curcumin inhibited CYP2C9 activity (10?µmol?L^–1 diclofenac) with half-maximal inhibition or a half-maximal inhibitory concentration (IC50) of 15.25?µmol?L^–1 and Ki?=?4.473?µmol?L^–1 in human liver microsomes. Curcumin’s mode of action on CYP2C9 activity was noncompetitive for the substrate diclofenanc and uncompetitive for the cofactor NADPH. In contrast to its potent inhibition of CYP2C9 in human, diclofenanc had lesser effects on CYP2C11 in rat, with an IC50 ≥100?µmol L^–1. The observations imply that curcumin has the inhibitory effects on CYP2C9 activity in human. These in vitro findings suggest that more attention should be paid to special clinical caution when intake of curcumin combined with other drugs in treatment.     

荧光光谱法研究姜黄素与牛血清白蛋白的相互作用

考察了姜黄素与牛血清白蛋白(BSA)的相互作用机制。利用荧光光谱考察了两者之间的荧光淬灭类型,计算结合数(n)和结合常数,结果显示姜黄素与BSA作用可导致BSA发生静态淬灭,采用Stern-Volmer拟合方程测得结合常数Ka=4.52×108L/mol,结合位点数n=1.62。姜黄素可与牛血清白蛋白发生结合,导致牛血清蛋白发生静态荧光淬灭。     

Formation of zein nanoparticles by electrohydrodynamic atomization: Effect of the main processing variables and suitability for encapsulating the food coloring and active ingredient curcumin

Nanoparticles with a compact spherical structure and a narrow size distribution were prepared from a zein protein polymer by electrohydrodynamic atomization. The effects of key parameters of the process (polymer concentration, flow rate and applied voltage) on the size and morphology of the particles was studied. Zein nanoparticles could be obtained from zein concentrations ranging from 2.5% to 15% (w/w). The sizes of these particles, ranging from 175 to 900 nm, increased with increasing polymer concentration. Compact nanostructures were obtained for 2.5% and 5% zein solutions whereas 10% and 15% solutions yielded collapsed and shrunken particles. Flow rate also exerted an effect, the lower the flow rate the smaller the nanoparticles. The morphology of the nanoparticles did not change after incorporating curcumin in proportions ranging from 1:500 to 1:10 (curcumin:zein), and the encapsulation efficiency was around 85–90%. Fluorescence microscopy images showed that the nanostuctures obtained took the form of matrix systems with the curcumin homogeneously distributed in the zein matrix. The curcumin remained in the amorphous state in the nanoparticle, as revealed by X-Ray diffractometry, evidencing intimate contact with the polymer. After three months of storage at 23 °C and 43% relative humidity in the dark, neither the size or the morphology of the nanoparticles had undergone significant changes, nor had the curcumin content altered. Thanks to encapsulation, the curcumin presented good dispersion in an aqueous food matrix: semi-skimmed milk.     

Tetrahydrocurcumin, a major metabolite of curcumin, induced autophagic cell death through coordinative modulation of PI3K/Akt-mTOR and MAPK signaling pathways in human leukemia HL-60 cells

Scope: Autophagy (type II programmed cell death) is crucial for maintaining cellular homeostasis. Several autophagy‐deficient or knockout studies indicate that autophagy is a tumor suppressor. Tetrahydrocurcumin (THC), a major metabolite of curcumin, has been demonstrated with anti‐colon carcinogenesis and antioxidation in vivo. Methods and results: In the present study, we found that treatment with THC induced autophagic cell death in human HL‐60 promyelocytic leukemia cells by increasing autophage marker acidic vascular organelle (AVO) formation. Flow cytometry also confirmed that THC treatment did not increase sub‐G1 cell population whereas curcumin did with strong apoptosis‐inducing activity. At the molecular levels, the results from Western blot analysis showed that THC significantly down‐regulated phosphatidylinositol 3‐kinase/protein kinase B and mitogen‐activated protein kinase signalings including decreasing the phosphorylation of mammalian target of rapamycin, glycogen synthase kinase 3β and p70 ribosomal protein S6 kinase. Further molecular analysis exhibited that the pretreatment of 3‐methyladenine (an autophagy inhibitor) also significantly reduced acidic vascular organelle production in THC‐treated cells. Conclusion: Taken together, these results demonstrated the anticancer efficacy of THC by inducing autophagy as well as provided a potential application for the prevention of human leukemia.