Physiologically relevant curcuminoids inhibit angiogenesis via VEGFR2 in human aortic endothelial cells

Giménez‐Bastida, Juan Antonio; Ávila‐Gálvez, María Ángeles; Carmena-Bargueño, Miguel; Pérez‐Sánchez, Horacio; Espı́n, Juan Carlos; González‐Sarrías, Antonio

doi:10.1016/j.fct.2022.113254

Cited by 8 publications

(13 citation statements)

References 60 publications

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“…Curcumin has pleiotropic activities; besides targeting pro-inflammatory cytokines, it can modulate adhesion molecules, antioxidant enzymes, and endothelial mediators which all are directly involved in endothelial function [ 18 , 26 , 48 , 49 ]. Apart from curcumin, other minor curcuminoids also have been shown to possess various biological activities in several in-vitro and in-vivo studies; and in some cases, demethoxycurcumin and bisdemethoxycurcumin have shown more potent effects than curcumin [ 20 , 50 ]. In a recent in-silico and in-vitro study, curcuminoids including curcumin, demethoxycurcumin and bisdemethoxycurcumin have shown to inhibit the tubulogenic and migration capacity of endothelial cells and reduced phosphorylation of the VEGFR2 in VEGF-165-stimulated cells suggesting an anti-angiogenic property [ 50 ].…”

Section: Discussionmentioning

confidence: 99%

“…Apart from curcumin, other minor curcuminoids also have been shown to possess various biological activities in several in-vitro and in-vivo studies; and in some cases, demethoxycurcumin and bisdemethoxycurcumin have shown more potent effects than curcumin [ 20 , 50 ]. In a recent in-silico and in-vitro study, curcuminoids including curcumin, demethoxycurcumin and bisdemethoxycurcumin have shown to inhibit the tubulogenic and migration capacity of endothelial cells and reduced phosphorylation of the VEGFR2 in VEGF-165-stimulated cells suggesting an anti-angiogenic property [ 50 ]. Moreover, bisdemethoxycurcumin has shown a novel anti-inflammatory pathway by inducing expression of heme oxygenase-1 and attenuating inducible NOS expression [ 51 ].…”

Section: Discussionmentioning

confidence: 99%

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Effect of nano-curcumin supplementation on angina status, and traditional and novel cardiovascular risk factors in overweight or obese patients with coronary slow flow phenomenon: a randomized double-blind placebo-controlled clinical trial

Rezaei,

Soltani,

Alipoor

et al. 2024

BMC Nutr

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Background Cardiovascular events and poor quality of life are frequently observed in patients with coronary slow flow phenomenon (CSFP). This trial evaluated the effect of nano-curcumin supplement containing curcuminoids, as multifunctional nutraceuticals, on angina status, and some traditional and novel cardiovascular risk factors in overweight or obese patients with CSFP. Methods In this double-blind, randomized, placebo-controlled clinical trial, 42 overweight or obese patients with CSFP received either 80 mg/day of nano-curcumin or placebo for 12 weeks. Seattle angina questionnaire (SAQ) as a clinical measure of angina status, circulating endocan, adropin, homocysteine, lipid profile, and the novel scores of visceral adiposity index (VAI) and waist-triglyceride index (WTI) were assessed before and after the intervention. The independent samples t-test, Mann-Whitney test, analysis of covariance, Chi-square, and Fisher’s exact tests were used where appropriate. Results All domains of SAQ including physical limitation, angina stability, angina frequency-severity, treatment satisfaction, and disease perception and quality of life improved significantly in the nano-curcumin compared with the placebo group. No significant changes were observed in serum endocan, adropin, and homocysteine following the intervention. Triglycerides, triglyceride/high-density lipoprotein cholesterol ratio, WTI and VAI values improved significantly only within the nano-curcumin group. Conclusions Supplementation with 80 mg/day nano-curcumin (containing curcuminoids) for 12 weeks significantly improved clinically important disease-specific aspects of health in patients with CSFP. Some traditional and novel cardiovascular risk factors improved significantly only compared with the baseline values, which need further investigation. Trial registration This study was approved by the Ethics Committee of Tehran University of Medical Sciences (IR.TUMS.VCR.REC.1398.794). The study protocol was registered at Iranian Registry of Clinical Trials by IRCT20131125015536N8 registration ID at 19.06.2019.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Effect of nano-curcumin supplementation on angina status, and traditional and novel cardiovascular risk factors in overweight or obese patients with coronary slow flow phenomenon: a randomized double-blind placebo-controlled clinical trial

Rezaei,

Soltani,

Alipoor

et al. 2024

BMC Nutr

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“…Curcumin, a bright yellow compound along with two of its analogs, namely demethoxycurcumin and bis demethoxycurcumin, are the major active constituents of turmeric powder and are collectively called curcuminoids ( Figure 1 ). Among the curcuminoids, curcumin is the most abundant fraction (~70%), followed by demethoxycurcumin (~17%) and bis demethoxycurcumin (~3%) [ 3 , 4 , 5 , 6 ].…”

Section: Curcumin and Its Limitations As A Drug Moleculementioning

confidence: 99%

“… Major curcuminoids present in turmeric powder. Reproduced with permission from [ 3 ] ( Food Chem. Toxicol.…”

Section: Figurementioning

confidence: 99%

Alginate and Chitosan-Based Delivery Systems for Improving the Bioavailability and Therapeutic Efficacy of Curcumin

Sable,

Kunwar,

Barik

2024

Pharmaceutics

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One of the major challenges in harnessing the therapeutic benefits of curcumin (an active ingredient from turmeric) is its poor bioavailability due to its short biological half-life. In this regard, nanoformulations have shown tremendous hope for improving the pharmacokinetic and therapeutic behavior of curcumin by altering its biological stability and bioavailability. Biopolymers, especially alginate and chitosan, have received special attention as excipients to prepare nanoformulations of curcumin due to their abundant availability, biocompatibility, and amicability to form different types of self-assembled structures and ease of undergoing chemical modifications. However, there are certain challenges, such as poor water solubility under physiological conditions and heterogeneity with regard to molecular weight and large-scale production of well-preserved nanostructures. Substantial advancement has been achieved towards overcoming these challenges by developing newer derivatives through a chemical modifications approach, and this has ascertained the suitability of alginate and chitosan as excipients for drug delivery systems (DDS). The present minireview briefly discusses curcumin and its limitation as a drug molecule, carbohydrates as DDS, and the recent developments related to the alginate and chitosan-based nanoformulations of curcumin. Special emphasis has been given to highlighting the impact of alginate and chitosan-based nanoformulations in improving the therapeutic efficacy and bioavailability of curcumin.

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“…It is known for its vibrant yellow color and numerous health benefits . In past research, curcumin was known for good antibacterial, anti-inflammatory, anticancer, and hypolipidemic effects and was recommended for treating numerous health conditions . The National Cancer Institute (NCI) considered curcumin as a third-generation cancer preventive agent. , The most important reason for the widespread use of curcumin in pharmaceuticals, supplements, and functional foods is its significant antioxidant activity.…”

Section: Introductionmentioning

confidence: 99%

Curcumin Encapsulation in Geranium Oil Microemulsion Elevates Its Antibacterial, Antioxidant, Anti-Inflammatory, and Anticancer Activities

Hassan,

Asghar,

Ullah Khan

et al. 2024

ACS Omega

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One of the major challenges with curcumin is its poor solubility in water, which limits its absorption and bioavailability in the body. This study aimed to develop and characterize stable microemulsions (MEs) as MEs increase the dispersibility of curcumin in water and aid its absorption in the body. Curcumin-loaded MEs were developed with the goal of enhancing topical delivery and its pharmacological activity (antioxidant, antibacterial, anticancer activity, and anti-inflammatory). The pseudoternary phase diagram was constructed to find out the desired microemulsion region. The prepared MEs (ME1− ME5) were evaluated for pH, viscosity, size of the particle, electrical conductivity, zeta potential, and ex vivo permeation of the drug. The optimized ME formulation was selected based on particle size and was further evaluated for biological activity (in vitro/vivo). In vitro cytotoxic effects of formulations were checked on the human liver cancer cell line, HEPG2 (a cell line exhibiting epithelial-like morphology that was isolated from a hepatocellular carcinoma). Geranium oil, Tween 80 (as a surfactant), and propylene glycol (as a cosurfactant) were screened out based on solubility to formulate MEs. The optimized ME formulation (ME5), with a composition of 20:50:30 (geranium oil:Tween 80:propylene glycol), exhibited pH 4.36 ± 0.057, conductivity of 40.06 ± 0.05 μS/cm, viscosity of 165 ± 0.37 mPa•s, and droplet diameter of 199.39 ± 0.017 nm. The ex vivo permeation study demonstrated a significant cumulative amount of curcumin permeated in 24 h and had a flux of 130.91 ± 0.02 μg/cm 2 /h. Antioxidant activity demonstrated that curcuminloaded microemulsion (ME5) exhibited higher scavenging activity (99.27 ± 0.021%) than blank microemulsion (94.67 ± 0.001%). Optimized curcumin-loaded microemulsion (ME5) exhibited zones of inhibition of 25.18 and 28.37 mm against Escherichia coli and Staphylococcus aureus, respectively. Among the cell lines tested, a higher concentration of ME5 showed the greatest cytotoxicity with a % viability of 8.22 ± 1.09%. Evidently, it also revealed significant in vivo anti-inflammatory effects with 93.29 ± 0.030% inhibition by the carrageenan-induced paw edema model (6 h study) and 88.39 ± 0.002% inhibition by the formalin-induced paw edema model (14 day study). In conclusion, microemulsion was safe and effective for effective delivery of curcumin with the potential for antioxidant, antibacterial, cytotoxic, and in vivo anti-inflammatory activities.

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Physiologically relevant curcuminoids inhibit angiogenesis via VEGFR2 in human aortic endothelial cells

Cited by 8 publications

References 60 publications

Effect of nano-curcumin supplementation on angina status, and traditional and novel cardiovascular risk factors in overweight or obese patients with coronary slow flow phenomenon: a randomized double-blind placebo-controlled clinical trial

Effect of nano-curcumin supplementation on angina status, and traditional and novel cardiovascular risk factors in overweight or obese patients with coronary slow flow phenomenon: a randomized double-blind placebo-controlled clinical trial

Alginate and Chitosan-Based Delivery Systems for Improving the Bioavailability and Therapeutic Efficacy of Curcumin

Curcumin Encapsulation in Geranium Oil Microemulsion Elevates Its Antibacterial, Antioxidant, Anti-Inflammatory, and Anticancer Activities

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