Polyphenol-based prebiotics and synbiotics: potential for cancer chemoprevention

Thilakarathna, W. P. D. Wass; Langille, Morgan G. I.; Rupasinghe, H.P. Vasantha

doi:10.1016/j.cofs.2018.02.011

Cited by 54 publications

(32 citation statements)

References 42 publications

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“…Structural modification, nanoencapsulation, and biotransformation are some of the strategies to combat the issue of low bioavailability of polyphenols [4]. Biotransformation of polyphenol-rich foods can be performed by incubating with microorganisms, especially probiotics which enable deglycosylation, ring fission, dehydroxylation, demethylation, lactonization, aromatic hydroxylation, reduction of carbon-carbon double bonds, or decarboxylation [5, 6], converting some polyphenols into more bioavailable and/or bioactive forms than their original forms [7].…”

Section: Introductionmentioning

confidence: 99%

Biotransformation of Cranberry Proanthocyanidins to Probiotic Metabolites byLactobacillus rhamnosusEnhances Their Anticancer Activity in HepG2 CellsIn Vitro

Rupasinghe

Parmar

Neir

2019

Oxidative Medicine and Cellular Longevity

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This study was designed to unravel the role of Lactobacillus rhamnosus in the bioconversion of cranberry proanthocyanidins and cytotoxicity of resulting metabolites to hepatocellular carcinoma HepG2 cells. Crude (CR) and flavonol+dihydrochalcone- (FL+DHC-), anthocyanin- (AN-), proanthocyanidin- (PR-), and phenolic acid+catechin- (PA+C-) rich fractions were subjected to fermentation with L. rhamnosus at 37°C for 12, 24, and 48 h under anaerobic conditions. The major metabolites produced by bioconversion of polyphenols were 4-hydroxyphenylacetic acid, 3-(4-hydroxyphenyl)propionic acid, hydrocinnamic acid, catechol, and pyrogallol. Furthermore, cytotoxicity of the biotransformed extracts was compared to their parent extracts using human hepatocellular carcinoma HepG2 cells. The results showed that PR-biotransformed extract completely inhibited HepG2 cell proliferation in a dose- and time-dependent manner with IC50 values of 47.8 and 20.1 μg/mL at 24 and 48 h, respectively. An insight into the molecular mechanisms involved revealed that the cytotoxic effects of PR at 24 h incubation were mitochondria-controlled and not by proapoptotic caspase-3/7 dependent. The present findings suggest that the application of a bioconversion process using probiotic bacteria can enhance the pharmacological activities of cranberry proanthocyanidins by generating additional biologically active metabolites.

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Section: Introductionmentioning

confidence: 99%

Biotransformation of Cranberry Proanthocyanidins to Probiotic Metabolites byLactobacillus rhamnosusEnhances Their Anticancer Activity in HepG2 CellsIn Vitro

Rupasinghe

Parmar

Neir

2019

Oxidative Medicine and Cellular Longevity

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“…Flavonoids showed antioxidant [ 28 ], anti-inflammatory [ 29 ], and sedative [ 30 ] effects in various studies. Moreover, flavonoid scaffolds present the outstanding potential of being chemoprotective agents toward cancer [ 31 ]. Consequently, flavonoids are often seen as quintessential nutraceuticals; e.g., the average intake of flavonoids in the United States is around 1 g/day [ 32 ].…”

Section: Introductionmentioning

confidence: 99%

Flavonoids as Putative Epi-Modulators: Insight into Their Binding Mode with BRD4 Bromodomains Using Molecular Docking and Dynamics

Prieto‐Martínez

Medina-Franco

2018

Biomolecules

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Flavonoids are widely recognized as natural polydrugs, given their anti-inflammatory, antioxidant, sedative, and antineoplastic activities. Recently, different studies showed that flavonoids have the potential to inhibit bromodomain and extraterminal (BET) bromodomains. Previous reports suggested that flavonoids bind between the Z and A loops of the bromodomain (ZA channel) due to their orientation and interactions with P86, V87, L92, L94, and N140. Herein, a comprehensive characterization of the binding modes of fisetin and the biflavonoid, amentoflavone, is discussed. To this end, both compounds were docked with BET bromodomain 4 (BRD4) using four docking programs. The results were post-processed with protein–ligand interaction fingerprints. To gain further insight into the binding mode of the two natural products, the docking results were further analyzed with molecular dynamics simulations. The results showed that amentoflavone makes numerous contacts in the ZA channel, as previously described for flavonoids and kinase inhibitors. It was also found that amentoflavone can potentially make contacts with non-canonical residues for BET inhibition. Most of these contacts were not observed with fisetin. Based on these results, amentoflavone was experimentally tested for BRD4 inhibition, showing activity in the micromolar range. This work may serve as the basis for scaffold optimization and the further characterization of flavonoids as BET inhibitors.

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“…Thilakarathna et al . [54] illustrated the potential use of probiotics and prebiotics in cancer prevention. Thilakarathna et al .…”

Section: Classification Of Nutraceuticalsmentioning

confidence: 99%

“…Thilakarathna et al . explained how gut microbes can prevent cancer progression by demonstrating many mechanisms [54]. For instance, it was reported that probiotics have significant efficiency on reduction of toxins and carcinogens.…”

Section: Classification Of Nutraceuticalsmentioning

confidence: 99%

Nutraceuticals’ Novel Formulations: The Good, the Bad, the Unknown and Patents Involved

Helal

Eassa

Amer³

et al. 2019

DDF

104

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: Traditional nutraceuticals and cosmeceuticals hold pragmatic nature with respect to their definitions, claims, purposes and marketing strategies. Their definitions are not well established worldwide. They also have different regulatory definitions and registration regulatory processes in different parts of the world. Global prevalence of nutraceuticals and cosmeceuticals is noticeably high with large market share with minimal regulation compared to traditional drugs. The global market is flooded with nutraceuticals and cosmeceuticals claiming to be of natural origin and sold with a therapeutic claim by major online retail stores such as Amazon and eBay. Apart from the traditional formulations, many manufacturers and researchers use novel formulation technologies in nutraceutical and cosmeceutical formulations for different reasons and objectives. Manufacturers tend to differentiate their products with novel formulations to increase market appeal and sales. On the other hand, researchers use novel strategies to enhance nutraceuticals and cosmeceuticals activity and safety. : The objective of this review is to assess the current patents and research adopting novel formulation strategies in nutraceuticals and cosmeceuticals. Patents and research papers investigating nutraceutical and cosmeceutical novel formulations were surveyed for the past 15 years. Various nanosystems and advanced biotechnology systems have been introduced to improve the therapeutic efficacy, safety and market appeal of nutraceuticals and cosmeceuticals, including liposomes, polymeric micelles, quantum dots, nanoparticles, and dendrimers. This review provides an overview of nutraceuticals and cosmeceuticals current technologies, highlighting their pros, cons, misconceptions, regulatory definitions and market. This review also aims in separating the science from fiction in the nutraceuticals and cosmeceuticals development, research and marketing.

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Polyphenol-based prebiotics and synbiotics: potential for cancer chemoprevention

Cited by 54 publications

References 42 publications

Biotransformation of Cranberry Proanthocyanidins to Probiotic Metabolites byLactobacillus rhamnosusEnhances Their Anticancer Activity in HepG2 CellsIn Vitro

Biotransformation of Cranberry Proanthocyanidins to Probiotic Metabolites byLactobacillus rhamnosusEnhances Their Anticancer Activity in HepG2 CellsIn Vitro

Flavonoids as Putative Epi-Modulators: Insight into Their Binding Mode with BRD4 Bromodomains Using Molecular Docking and Dynamics

Nutraceuticals’ Novel Formulations: The Good, the Bad, the Unknown and Patents Involved

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