An Update on the Pharmacological Usage of Curcumin: Has it Failed in the Drug Discovery Pipeline?

Olotu, Fisayo A.; Soremekun, Opeyemi; Agoni, Clement

doi:10.1007/s12013-020-00922-5

Cited by 28 publications

(24 citation statements)

References 213 publications

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“…The main bioactive constituents of turmeric are the structurally related curcuminoids curcumin (CUR), demethoxycurcumin (DMC) and bis(demethoxy)curcumin (BDMC), differing only in the presence or absence of one or two methoxy groups (Figure 1). The pharmacological benefits of curcumin, making up 75-80% of the curcuminoids, are the most extensively investigated [2][3][4][5][6][7][8][9][10]. It is reported to possess antioxidative, anti-inflammatory, neuroprotective, antibacterial, antifungal, antineoplastic, and proapopotic activity [3,4,[8][9][10], which render it a potential drug candidate for the treatment and prevention of cancer and Alzheimer's disease [5,7].…”

Section: Introductionmentioning

confidence: 99%

“…It is reported to possess antioxidative, anti-inflammatory, neuroprotective, antibacterial, antifungal, antineoplastic, and proapopotic activity [3,4,[8][9][10], which render it a potential drug candidate for the treatment and prevention of cancer and Alzheimer's disease [5,7]. Due to its poor bioavailability caused by low aqueous solubility, slow dissolution rate and rapid metabolism it has not yet been approved as a therapeutic [6].…”

Section: Introductionmentioning

confidence: 99%

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A Contribution to the Solid State Forms of Bis(demethoxy)curcumin: Co-Crystal Screening and Characterization

et al. 2021

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Bis(demethoxy)curcumin (BDMC) is one of the main active components found in turmeric. Major drawbacks for its usage are its low aqueous solubility, and the challenging separation from other curcuminoids present in turmeric. Co-crystallization can be applied to alter the physicochemical properties of BDMC in a desired manner. A co-crystal screening of BDMC with four hydroxybenzenes was carried out using four different methods of co-crystal production: crystallization from solution by slow solvent evaporation (SSE), and rapid solvent removal (RSR), liquid-assisted grinding (LAG), and crystallization from the melt phase. Two co-crystal phases of BDMC were obtained with pyrogallol (PYR), and hydroxyquinol (HYQ). PYR-BDMC co-crystals can be obtained only from the melt, while HYQ-BDMC co-crystals could also be produced by LAG. Both co-crystals possess an equimolar composition and reveal an incongruent melting behavior. Infrared spectroscopy demonstrated the presence of BDMC in the diketo form in the PYR co-crystals, while it is in a more stable keto-enol form in the HYQ co-crystals. Solubility measurements in ethanol and an ethanol-water mixture revealed an increase of solubility in the latter, but a slightly negative effect on ethanol solubility. These results are useful for a prospective development of crystallization-based separation processes of chemical similar substances through co-crystallization.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

A Contribution to the Solid State Forms of Bis(demethoxy)curcumin: Co-Crystal Screening and Characterization

et al. 2021

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“…The curcuminoids from C. longa have been extensively studied because of their antiinflammatory and antioxidant properties, and their potential activity as antitumoral, antibacterial, antioxidant, anti-inflammatory, antiviral, and antifungal agents (Abdel-Wahhab et al, 2016;Alavi et al, 2018;Pushpalatha et al, 2019;Zielińska et al, 2020a). However, the dietary and pharmacological application of native CUR is hindered due to poor water solubility and chemical instability, resulting in low bioavailability, fast metabolism, and predisposition to photochemical degradation (Alves et al, 2019;Altunbas et al, 2011;Olotu et al, 2020;Yallapu et al, 2012;Wang et al, 2016). One way to overcome these drawbacks can be the encapsulation of CUR to improve its water-solubility, stability, and consequently, the bioavailability of this phenolic compound.…”

Section: Introductionmentioning

confidence: 99%

Curcumin encapsulation in nanostructures for cancer therapy: A 10-year overview

D'Angelo

Noronha

Kurnik

et al. 2021

International Journal of Pharmaceutics

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This is a PDF file of an article that has undergone enhancements after acceptance, such as the addition of a cover page and metadata, and formatting for readability, but it is not yet the definitive version of record. This version will undergo additional copyediting, typesetting and review before it is published in its final form, but we are providing this version to give early visibility of the article. Please note that, during the production process, errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.

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“…Curcumin (1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadien-3,5-dione) is an active ingredient extracted from turmeric ( Curcuma longa ), which is not only a traditional Chinese herb but also a dietary spice. Accumulating evidence has demonstrated that it could prevent and treat a wide range of diseases by its antioxidant and anti-inflammatory properties in preclinical trials, for instance, arthritis, cancer, neurodegenerative disorders, metabolic syndrome, cardiovascular diseases, diabetes and so on [8,9], and the same potential has been validated by many clinical trials [10]. Specifically, curcumin could regulate various molecular targets, such as nuclear factor κ B (NF- κ B), tumor necrosis factor-α (TNFα), and monocyte chemoattractant protein-1 (MCP-1), which might contribute to its therapeutic potential in obesity and diabetes [11].…”

Section: Introductionmentioning

confidence: 99%

Curcumin improves adipocytes browning and mitochondrial function in 3T3-L1 cells and obese rodent model

Zhao

Pan

et al. 2021

R. Soc. open sci.

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Accumulating evidence suggests that mitochondrial dysfunction and adipocyte differentiation promote lipid accumulation in the development of obesity and diabetes. Curcumin is an active ingredient extracted from Curcuma longa that has been shown to exhibit antioxidant and anti-inflammatory potency in metabolic disorders. However, the underlying mechanisms of curcumin in adipocytes remain largely unexplored. We studied the effects of curcumin on adipogenic differentiation and mitochondrial oxygen consumption and analysed the possible mechanisms. 3T3-L1 preadipocytes were used to assess the effect of curcumin on differentiation of adipocytes. The Mito Stress Test measured by Seahorse XF Analyzer was applied to investigate the effect of curcumin on mitochondrial oxygen consumption in 3T3-L1 adipocytes. The effect of curcumin on the morphology of both white and brown adipose tissue (WAT and BAT) was evaluated in a high-fat diet-induced obese mice model. We found that curcumin dose-dependently (10, 20 and 35 µM) induced adipogenic differentiation and the intracellular fat droplet accumulation. Additionally, 10 µM curcumin remarkably enhanced mature adipocyte mitochondrial respiratory function, specifically, accelerating basic mitochondrial respiration, ATP production and uncoupling capacity via the regulation of peroxisome proliferator-activated receptor γ (PPARγ) ( p < 0.01). Curcumin administration also attenuated the morphological changes in adipose tissues in high-fat diet-induced obese mice. Moreover, curcumin markedly increased the mRNA and protein expressions of mitochondrial uncoupling protein 1 (UCP1), PPARγ, peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α) and PR domain protein 16 (PRDM16) in vivo and in vitro . Collectively, the results demonstrate that curcumin promotes the adipogenic differentiation of preadipocytes and mitochondrial oxygen consumption in 3T3-L1 mature adipocytes by regulating UCP1, PRDM16, PPARγ and PGC-1α expression.

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An Update on the Pharmacological Usage of Curcumin: Has it Failed in the Drug Discovery Pipeline?

Cited by 28 publications

References 213 publications

A Contribution to the Solid State Forms of Bis(demethoxy)curcumin: Co-Crystal Screening and Characterization

A Contribution to the Solid State Forms of Bis(demethoxy)curcumin: Co-Crystal Screening and Characterization

Curcumin encapsulation in nanostructures for cancer therapy: A 10-year overview

Curcumin improves adipocytes browning and mitochondrial function in 3T3-L1 cells and obese rodent model

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