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1.
Expert Opin Drug Metab Toxicol ; 20(5): 333-345, 2024 May.
Article in English | MEDLINE | ID: mdl-38721667

ABSTRACT

INTRODUCTION: There is a large body of preclinical data implicating that grapefruit juice (GJ) inhibits many CYP 450 isoforms. The potential of GJ-to-drug is of high relevance to clinical psychiatry, because a wide range of psychotropic medicines undergo CYP 450 metabolism and P-gp transport. AREAS COVERED: Relevant data were identified by searching the electronic databases up to February 2024. This work constitutes a summary of preclinical and clinical data on GJ impact on CYP 450 metabolism, P-glycoprotein, and organic anion-transporting polypeptides (OATPs), with focus on studies that assessed GJ-to-psychotropic drug interactions. Additionally, an unpublished case series of nine patients is provided. EXPERT OPINION: The impact of GJ on CYP 3A4 appears to be the critical mechanism for the majority of GJ-to-psychopharmacotherapy interactions described in human studies or case reports. However, there are studies and cases of patients clearly showing that this is not the only route explaining the GJ effect, and at times, this particular is of no relevance and that other CYP 450 isoforms as well as drug transporting proteins might be involved. The risk of GJ-to-psychotropic drugs needs to be further evaluated in a 'real-world' setting and apply not only measures of pharmacokinetics but also treatment effectiveness and safety.


Subject(s)
Citrus paradisi , Food-Drug Interactions , Fruit and Vegetable Juices , Psychotropic Drugs , Humans , Psychotropic Drugs/administration & dosage , Psychotropic Drugs/pharmacokinetics , Psychotropic Drugs/adverse effects , Psychotropic Drugs/pharmacology , Animals , Cytochrome P-450 CYP3A/metabolism , Cytochrome P-450 Enzyme System/metabolism , Organic Anion Transporters/metabolism , ATP Binding Cassette Transporter, Subfamily B, Member 1/metabolism
2.
Molecules ; 29(9)2024 May 01.
Article in English | MEDLINE | ID: mdl-38731581

ABSTRACT

In this study, TiO2/P, K-containing grapefruit peel biochar (TiO2/P, K-PC) composites were synthesized in situ biomimetically using grapefruit peel as the bio-template and carbon source and tetrabutyl titanate as the titanium source. This was achieved using the two-step rotary impregnation-calcination method. Adjusting the calcination temperature of the sample in an air atmosphere could regulate the mass ratio of TiO2 to carbon. The prepared samples were subjected to an analysis of their compositions, structures, morphologies, and properties. It demonstrated that the prepared samples were complexes of anatase TiO2 and P, K-containing carbon, with the presence of graphitic carbon. They possessed a unique morphological structure with abundant pores and a large surface area. The grapefruit peel powder played a crucial role in the induction and assembly of TiO2/P, K-PC composites. The sample PCT-400-550 had the best photocatalytic activity, with the degradation rate of RhB, MO, and MB dye solutions reaching more than 99% within 30 min, with satisfactory cyclic stability. The outstanding photocatalytic activity can be credited to its unique morphology and the efficient collaboration between TiO2 and P, K-containing biochar.


Subject(s)
Charcoal , Citrus paradisi , Titanium , Titanium/chemistry , Citrus paradisi/chemistry , Charcoal/chemistry , Catalysis , Biomass
3.
Int J Biol Macromol ; 267(Pt 1): 131397, 2024 May.
Article in English | MEDLINE | ID: mdl-38582479

ABSTRACT

This study aimed to develop a multifunctional active composite film to extend the shelf life of minced pork. The composite film was prepared by incorporating zinc-doped grapefruit peel-derived carbon quantum dots (Zn-GFP-CD) into a cellulose nanofiber (CNF) matrix. The resulting film significantly improved UV-blocking properties from 39.0 % to 85.7 % while maintaining the film transparency. Additionally, the CNF/Zn-GFP-CD5% composite film exhibits strong antioxidant activity with ABTS and DPPH radical scavenging activities of 99.8 % and 77.4 %, respectively. The composite film also showed excellent antibacterial activity against both Gram-negative and Gram-positive bacteria. When used in minced pork packaging, the composite films effectively inhibit bacterial growth, maintaining bacterial levels below 7 Log CFU/g after 15 days and sustaining a red color over a 21-day storage period. Additionally, a significant reduction in the lipid oxidation of the minced pork was observed. These CNF/Zn-GFP-CD composite films have a great potential for active food packaging applications to extend shelf life and maintain the visual quality of packaged meat.


Subject(s)
Carbon , Cellulose , Citrus paradisi , Food Packaging , Nanofibers , Quantum Dots , Zinc , Quantum Dots/chemistry , Nanofibers/chemistry , Cellulose/chemistry , Food Packaging/methods , Zinc/chemistry , Citrus paradisi/chemistry , Carbon/chemistry , Antioxidants/chemistry , Antioxidants/pharmacology , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Animals , Swine
4.
Molecules ; 29(6)2024 Mar 11.
Article in English | MEDLINE | ID: mdl-38542873

ABSTRACT

Type 2 diabetes mellitus is a multifactorial disorder whose primary manifestation usually initiates with elevated blood sugar levels. Several antidiabetic agents are used to manage type 2 diabetes mellitus, of which empagliflozin is an oral sodium-glucose co-transporter (SGLT-2) inhibitor in the kidney. This research aims to develop and validate a simple analytical method for determining empagliflozin levels in biological fluid and to further evaluate grapefruit juice's impact on empagliflozin pharmacokinetics in rats. High-Performance Liquid Chromatography (HPLC) was used to establish a simple, rapid, and accurate method for determining empagliflozin levels in rat plasma, in the presence of grapefruit juice. Four groups of rats (n = 10 rats in each) were used in the preclinical study. Group A (healthy rats) received empagliflozin alone; Group B (healthy rats) received empagliflozin with grapefruit; Group C (diabetic rats) received empagliflozin with grapefruit; and Group D (healthy, negative control) received no medication. The rats (n = 10) were given grapefruit juice instead of water for seven days before receiving the empagliflozin dose (0.16 mg/kg). Some pharmacokinetic parameters for each group were determined. The maximum plasma concentration (Cmax) and area under the curve (AUC) of empagliflozin in Group A without grapefruit intake were 730 ng/mL and 9264.6 ng × h/mL, respectively, with Tmax (2 h). In Group B, Cmax was 1907 ng/mL and AUC was 10,290.75 ng × h/mL in the presence of grapefruit, with Tmax (1 h); whereas, in Group C, the Cmax was 2936 ng/mL and AUC was 18657 ng × h/mL, with Tmax (2 h). In conclusion, our results showed that the co-administration of grapefruit with empagliflozin should be cautiously monitored and avoided, in which grapefruit elevates the plasma level of empagliflozin. This may be attributed to the inhibition of the uridine enzyme in the grapefruit by hesperidin, naringin, and flavonoid.


Subject(s)
Benzhydryl Compounds , Citrus paradisi , Citrus , Diabetes Mellitus, Experimental , Diabetes Mellitus, Type 2 , Glucosides , Rats , Animals , Chromatography, High Pressure Liquid , Citrus/chemistry , Beverages , Area Under Curve
5.
J Food Drug Anal ; 32(1): 39-53, 2024 Mar 15.
Article in English | MEDLINE | ID: mdl-38526589

ABSTRACT

Pomelo sponge layer (PSL) had been considered as a potential source of soluble dietary fiber (SDF), while they were mostly disposed of as waste. To promote high-value utilization of pomelo wastes, this study extracted SDF from PSL of six varieties of pomelo, and their physicochemical, structural and functional properties were investigated. Results indicated that all PSL-SDFs showed good physicochemical and functional properties. Among them, PSL-SDF from grapefruit (GRSDF) showed better water holding capacity and swelling capacity, whereas Shatian pomelo PSL-SDF and Guanxi pomelo PSL-SDF had the highest thermal stability and oil holding capacity, respectively. Furthermore, compared with other PSL-SDFs, GRSDF displayed the lowest hydrolysis degree coupled with the best antioxidant and probiotic growth-promoting abilities. Finally, the correlation analysis showed that multiple beneficial effects of PSL-SDFs were markedly associated with their molecular weight and the concentrations of total phenolic, total flavonoids, rhamnose, galacturonic acid, glucose and arabinose. Collectively, these findings contributed to a better understanding of the physicochemical and functional properties of SDFs extracted from different PSLs, which provided a scientific basis for the development of PSL-SDFs into functional foods.


Subject(s)
Citrus paradisi , Citrus , Antioxidants , Flavonoids , Dietary Fiber
6.
Fitoterapia ; 174: 105875, 2024 Apr.
Article in English | MEDLINE | ID: mdl-38417678

ABSTRACT

Grapefruit mint (Mentha suaveolens × piperita) is a hybrid, perennial, and aromatic plant widely cultivated all over the world and used in the food, cosmetics, and pharmaceutical industries mostly for its valuable essential oil. Herein, we evaluated the anticancer activity of the grapefruit mint essential oil, cultivated in Iran. For the chemical composition analysis of essential oil, GC-MS was used. MTT assay was utilized for assessing the cytotoxic activity of the essential oil. The type of cell death was determined by annexin V/PI staining. Essential oil effect on the expression of maternally expressed gene 3 (MEG3), a regulatory lncRNA involved in cell growth, proliferation, and metastasis, was studied using qRT-PCR. Linalool (43.9%) and linalool acetate (40.1%) were identified as the dominant compounds of essential oil. Compared with MCF-7, the MDA-MB-231 cells were more sensitive to essential oil (IC50 = 7.6 µg/ml in MCF-7 and 5.9 µg/ml in MDA-MB-231 after 48 h). Essential oil induced cell death by apoptosis. Wound healing scratch assay confirmed the anti-invasive effect of essential oil. In addition, essential oil upregulated the tumor suppressor MEG3 in breast cancer cells. These results provide new insights into grapefruit mint essential oil potential application as an anticancer adjuvant in combination treatments for breast cancer patients.


Subject(s)
Acyclic Monoterpenes , Breast Neoplasms , Citrus paradisi , Mentha , Oils, Volatile , Humans , Female , Oils, Volatile/pharmacology , Oils, Volatile/chemistry , Mentha/chemistry , Molecular Structure , Breast Neoplasms/drug therapy , Mentha piperita
7.
Cells ; 13(4)2024 Feb 18.
Article in English | MEDLINE | ID: mdl-38391968

ABSTRACT

In this study, we investigated the beneficial effects of grapefruit IntegroPectin, derived from industrial waste grapefruit peels via hydrodynamic cavitation, on microglia cells exposed to oxidative stress conditions. Grapefruit IntegroPectin fully counteracted cell death and the apoptotic process induced by cell exposure to tert-butyl hydroperoxide (TBH), a powerful hydroperoxide. The protective effects of the grapefruit IntegroPectin were accompanied with a decrease in the amount of ROS, and were strictly dependent on the activation of the phosphoinositide 3-kinase (PI3K)/Akt cascade. Finally, IntegroPectin treatment inhibited the neuroinflammatory response and the basal microglia activation by down-regulating the PI3K- nuclear factor kappa-light-chain-enhancer of activated B cells (NF-kB)- inducible nitric oxide synthase (iNOS) cascade. These data strongly support further investigations aimed at exploring IntegroPectin's therapeutic role in in vivo models of neurodegenerative disorders, characterized by a combination of chronic neurodegeneration, oxidative stress and neuroinflammation.


Subject(s)
Citrus paradisi , Microglia , Humans , Microglia/metabolism , Citrus paradisi/metabolism , Phosphatidylinositol 3-Kinases/metabolism , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/metabolism , Cell Line
8.
Biol Pharm Bull ; 47(1): 72-78, 2024.
Article in English | MEDLINE | ID: mdl-38171780

ABSTRACT

We recently reported that the gastrointestinal (GI) fluid volume is influenced by the solution osmolality, and proposed that this effect may play a role in beverage-drug interactions. Here, we investigated whether osmolality-dependent fluid secretion can explain the difference in the magnitudes of fruit juice-drug interactions depending on the type of fruit juice (grapefruit juice (GFJ), orange juice (OJ), and apple juice (AJ)). The osmolality of GFJ, OJ, and AJ used in this study was found to be 552, 686, and 749 mOsm/kg, respectively. Measurements of intestinal fluid movement following beverage administration by the in situ closed-loop technique revealed the following rank order for fluid volume in rat ileum: AJ > OJ > GFJ > purified water, suggesting that water movement is dependent on the osmolality of these beverages. Such changes in GI fluid volume are expected to alter the luminal drug concentration, potentially contributing to the magnitude of beverage-drug interactions. Indeed, in vivo pharmacokinetic study in rats revealed that the plasma concentration of atenolol, a low-permeability drug, was the highest after oral administration in purified water, followed by GFJ and OJ, and was the lowest after administration in AJ. In contrast, antipyrine, a high-permeability drug, showed no significant difference in plasma concentration after administration in purified water and fruit juices, suggesting that the absorption of high-permeability drugs is less affected by solution osmolality. Our findings indicate that differences in the magnitude of beverage-drug interactions can be at least partly explained by differences in the osmolality of the beverages ingested.


Subject(s)
Citrus paradisi , Citrus sinensis , Malus , Rats , Animals , Fruit and Vegetable Juices , Food-Drug Interactions , Beverages/analysis , Osmolar Concentration , Water , Fruit
9.
Int J Biol Macromol ; 259(Pt 2): 129274, 2024 Feb.
Article in English | MEDLINE | ID: mdl-38199546

ABSTRACT

In this study, the key prebiotic fraction of grapefruit peel sponge layer soluble dietary fiber (GSLSDF) was identified, and its structure characteristics and modulatory effect on intestinal microorganisms were investigated. Firstly, two fractions (GSLSDF-1 and GSLSDF-2) were isolated from GSLSDF, and the GSLSDF-1 showed a better prebiotic activity. Subsequently, GSLSDF-1 was found to have a low molecular weight and crystallinity, a loose and porous microstructure, and a high glucose content. Meanwhile, GSLSDF-1 was a dextran with a main chain linked by ß-1, 4 glycosidic bonds and branched by a ß-1, 6 glycosidic bonds. These structural characteristics were responsible for the favorable prebiotic activity of GSLSDF-1. Finally, the regulation effect of GSLSDF-1 on gut microbiota was analyzed in vitro fecal fermentation. Compared with the blank and GSLSDF groups, GSLSDF-1 could increase the relative abundances of Lactobacillus, Bacteroides, Bifidobacterium and Faecalibacterium coupled with decrease the relative abundances of Clostridium and Clostridioides. Furthermore, GSLSDF-1 promoted the production of short-chain fatty acids (SCFAs) by modulating the SCFAs synthesis pathway of intestinal microorganisms, while the NH3-N synthesis of intestinal microorganisms was inhibited by GSLSDF-1. Above results indicated that GSLSDF-1 was the key prebiotic fraction of GSLSDF, which could effectively optimize the intestinal microorganism composition.


Subject(s)
Citrus paradisi , Gastrointestinal Microbiome , Fatty Acids, Volatile/metabolism , Feces/microbiology , Fermentation , Dietary Fiber/analysis , Prebiotics/analysis
10.
Int J Biol Macromol ; 254(Pt 2): 127785, 2024 Jan.
Article in English | MEDLINE | ID: mdl-37931867

ABSTRACT

This study presents an innovative attempt to extract high-quality pectins from grapefruit (Citrus paradisi) peels by using deep eutectic solvents (DESs) as extraction agents. The maximum yield of betaine-citric acid (BC)-extracted pectin (BC-P) reached 36.47 % under the optimum process conditions: an L/S ratio of 25 mL/g, a pH of 2.0, and a temperature of 85 °C for 120 min. The yield of BC-P was significantly higher than HCl-extracted pectin (HCl-P, 8.76 %) under a pH of 2.0. In addition, the structural, physicochemical, and emulsifying properties of the purified pectins (BC-P and HCl-P) and commercial pectin (CP) were comparatively analyzed. Results showed that BC-P exhibited higher RG-I value, more arabinan side-chains, bigger Mw and Mn value than HCl-P. Moreover, the viscosity, G' and G'' of BC-P were significantly higher than those of HCl-P and CP. More importantly, BC-P demonstrated better emulsifying activity and stability compared to HCl-P and CP. When the concentration of BC-P was increased to 1.50 %, a stable emulsion containing a 50 % soybean oil fraction could be obtained. Our results confirmed that DESs can be considered as high-effective agents for pectin extraction. Pectins extracted from grapefruit peels can be as a promising natural emulsifiers that can be used in the food industry.


Subject(s)
Citrus paradisi , Citrus , Pectins/chemistry , Citrus paradisi/chemistry , Deep Eutectic Solvents , Emulsifying Agents/chemistry , Emulsions/chemistry , Citrus/chemistry
11.
ACS Nano ; 17(24): 24773-24789, 2023 Dec 26.
Article in English | MEDLINE | ID: mdl-38055864

ABSTRACT

As the prevalence of vascular calcification (VC), a strong contributor to cardiovascular morbidity and mortality, continues to increase, the need for pharmacologic therapies becomes urgent. Sodium thiosulfate (STS) is a clinically approved drug for therapy against VC; however, its efficacy is hampered by poor bioavailability and severe adverse effects. Plant-derived extracellular vesicles have provided options for VC treatment since they can be used as biomimetic drug carriers with higher biosafety and targeting abilities than artificial carriers. Inspired by natural grapefruit-derived extracellular vesicles (EVs), we fabricated a biomimetic nanocarrier comprising EVs loaded with STS and further modified with hydroxyapatite crystal binding peptide (ESTP) for VC-targeted delivery of STS. In vitro, the ESTP nanodrug exhibited excellent cellular uptake capacity by calcified vascular smooth muscle cells (VSMCs) and subsequently inhibited VSMCs calcification. In the VC mice model, the ESTP nanodrug showed preferentially the highest accumulation in the calcified arteries compared to other treatment groups. Mechanistically, the ESTP nanodrug significantly prevented VC via driving M2 macrophage polarization, reducing inflammation, and suppressing bone-vascular axis as demonstrated by inhibiting osteogenic phenotype trans-differentiation of VSMCs while enhancing bone quality. In addition, the ESTP nanodrug did not induce hemolysis or cause any damage to other organs. These results suggest that the ESTP nanodrug can prove to be a promising agent against VC without the concern of systemic toxicity.


Subject(s)
Citrus paradisi , Extracellular Vesicles , Vascular Calcification , Animals , Mice , Biomimetics , Vascular Calcification/drug therapy , Vascular Calcification/metabolism , Vascular Calcification/prevention & control , Extracellular Vesicles/metabolism
12.
Int J Mol Sci ; 24(21)2023 Oct 27.
Article in English | MEDLINE | ID: mdl-37958646

ABSTRACT

Citrus fruits are a natural source of ascorbic acid, and exosome-like nanovesicles obtained from these fruits contain measurable levels of ascorbic acid. We tested the ability of grapefruit-derived extracellular vesicles (EVs) to inhibit the growth of human leukemic cells and leukemic patient-derived bone marrow blasts. Transmission electron microscopy and nanoparticle tracking analysis (NTA) showed that the obtained EVs were homogeneous exosomes, defined as exosome-like plant-derived nanovesicles (ELPDNVs). The analysis of their content has shown measurable amounts of several molecules with potent antioxidant activity. ELPDNVs showed a time-dependent antiproliferative effect in both U937 and K562 leukemic cell lines, comparable with the effect of high-dosage ascorbic acid (2 mM). This result was confirmed by a clear decrease in the number of AML blasts induced by ELPDNVs, which did not affect the number of normal cells. ELPDNVs increased the ROS levels in both AML blast cells and U937 without affecting ROS storage in normal cells, and this effect was comparable to ascorbic acid (2 mM). With our study, we propose ELPDNVs from grapefruits as a combination/supporting therapy for human leukemias with the aim to improve the effectiveness of the current therapies.


Subject(s)
Citrus paradisi , Exosomes , Leukemia, Myeloid, Acute , Humans , Exosomes/metabolism , Ascorbic Acid/pharmacology , Ascorbic Acid/metabolism , Reactive Oxygen Species/metabolism , Organic Agriculture , Leukemia, Myeloid, Acute/metabolism
13.
Environ Sci Pollut Res Int ; 30(56): 119034-119049, 2023 Dec.
Article in English | MEDLINE | ID: mdl-37919501

ABSTRACT

The continuous and rapid development of textile industry intensifies rhodamine B dye (RhB) wastewater pollution. Meanwhile, massive red mud (RM) solid waste generated by the industrial alumina production process poses detrimental effects to the environment after leaching. For resource utilization and to reduce the expansion of RhB pollution, RM and peel red mud-biochar composite (RMBC) catalyst were synthesized in activating peroxydisulfate (PDS) for RhB degradation. Firstly, characterization results showed that compared to RM, RMBC had a higher content of catalytically active metals (Fe, Al, Ti) (higher than 0.92-4.18%), smaller pore size, and larger specific surface area (10 times), which verified RMBC had more potential catalytic oxidation activity. Secondly, under optimal dosage (catalyst, PDS), pH 4.6, and 20 mg L-1 RhB, it was found that the RhB degradation ratio of RM was 76.70%, which was reduced to 41% after three cycles, while that of RMBC was 89.98% and 67%, respectively. The results indicated that the performance of RMBC was significantly superior to that of RM. Furthermore, the quenching experiments, electron paramagnetic resonance spectroscopy tests, FTIR, and XPS analysis showed the function of O-H, C=O, C-O, Fe-O, and Fe-OH functional groups, which converted the PDS to the active state and hydrolyzed it to produce free radicals ([Formula: see text], 1O2, [Formula: see text]) for RhB degradation. And, Q Exactive Plus MS test obtained that RhB was degraded to CO2, H2O, and intermediate products. This study aimed to raise a new insight to the resource utilization of RM and the control of dye pollution.


Subject(s)
Citrus paradisi , Water , Charcoal
14.
Bioanalysis ; 15(22): 1327-1341, 2023 Nov.
Article in English | MEDLINE | ID: mdl-37902824

ABSTRACT

Aim: An eco-friendly ultra-performance liquid chromatography-tandem mass spectrometry method was developed to study the pharmacokinetics of rivaroxaban and ticagrelor in rat plasma, utilizing moxifloxacin as an internal standard. The food-drug interaction between grapefruit juice and these drugs was also investigated. Methods: Liquid-liquid extraction was used. A nonporous stationary phase Agilent® Poroshell 120EC C18 column was used with methanol: 0.1% aqueous formic acid (95:5 v/v) as a mobile phase. The detection was performed in multiple reaction monitoring mode using positive electrospray ionization. The method's validation was conducted in accordance with US FDA and European Medicines Agency guidelines. Results & conclusion: Grapefruit juice should be ingested with caution in patients treated with antithrombotic medications as it may increase their plasma concentration, inducing bleeding, and requires close clinical monitoring.


Subject(s)
Citrus paradisi , Tandem Mass Spectrometry , Rats , Humans , Animals , Tandem Mass Spectrometry/methods , Rivaroxaban , Ticagrelor , Chromatography, High Pressure Liquid/methods , Chromatography, Liquid
15.
Int J Biol Macromol ; 253(Pt 8): 127655, 2023 Dec 31.
Article in English | MEDLINE | ID: mdl-37884247

ABSTRACT

The development of edible packaging films was motivated due to resource waste and environmental damage caused by chemically produced plastic packaging. The development of edible packaging film based on grapefruit peel pomace dietary fiber has significant technological and functional potential because grapefruit processing waste is a potential source of high-quality dietary fiber. In this study, the first successful development of an edible packaging film based on dietary fiber using grapefruit soluble dietary fiber (GSDF) from grapefruit peel pomace as a substrate and nanocellulose (GNCC) as a filler was developed. Principal component analysis, membership function synthesis, and response surface methods were used to determine the optimal process to prepare the edible packaging films, and the impact of GNCC on this material was analyzed. The results showed that the overall performance score of the edible packaging film with 1 wt% GNCC was 0.764. The maximum pyrolysis temperature increased from 226.36 °C to 227.10 °C, the melting temperature (Tm) increased by 5.54 °C, the crystallinity increased by 2.95 %. The film solution exhibited non-Newtonian characteristics and a solid-like property. Our results showed that the edible packaging film developed from grapefruit peel pomace and dietary fiber could have several potential applications in the food packaging field.


Subject(s)
Citrus paradisi , Edible Films , Dietary Fiber , Food Packaging/methods
16.
Plant Foods Hum Nutr ; 78(3): 533-538, 2023 Sep.
Article in English | MEDLINE | ID: mdl-37594558

ABSTRACT

Grapefruit peel contains a high concentration of naringin- a potent antioxidant with strong bioactive properties. In this study, a new type of functional chocolate fortified with grapefruit peel extract and different concentrations of aqueous methanol and ethanol were evaluated as extraction solvents. A new high-performance liquid chromatography (HPLC) method to analyze the naringin content of the fortified chocolates was developed with a recovery of 107% ± 3.1% and repeatability below 3.5%. A sensory evaluation was conducted to assess the preference for the chocolates among individuals who self-described a preference for bitter flavors. No significant preference was observed in the cases of astringency and aftertaste while the increased bitterness proved to be favorable. However, taste, flavor and overall acceptability were regarded somewhat less favorably. While chocolate proved to be a satisfactory carrier for naringin and had several enjoyable characteristics, further research may focus on improving the organoleptic properties of chocolates fortified by naringin.


Subject(s)
Cacao , Chocolate , Citrus paradisi , Plant Extracts
17.
Ultrason Sonochem ; 98: 106505, 2023 Aug.
Article in English | MEDLINE | ID: mdl-37437368

ABSTRACT

In this work, the novel use of ultrasonic pre-treatment and edible coating treatment during osmosis dehydration to optimize the weight reduction, moisture loss, sucrose gain, rehydration, and surface shrinkage using a response surface methodology (RSM) based on a central composite design (CCD) technique was successfully conducted on grapefruit slices. The process parameters include sonication pre-treatment time (5-10 min), xanthan-gum-based edible coating (0.1%-0.3%, w/w), and sucrose concentration (20-50 Brix), were examined and optimized for osmosis dehydration of grapefruit slices. At each step, three grapefruit slices were immersed in an ultrasonic water bath at 40 kHz, 150 W, and 20 C. Then, the sonicated slices were placed in a container contain sucrose and xanthan, and the container was put in a 50 C water-bath for 1 h. The optimum concentration of xanthan gum, sucrose, and time of treatment were predicted to be 0.15%, 20.0 Brix, and 10.0  min, respectively. Under this optimum condition, estimated values of response variables are as follows: weight reduction 14.14%, moisture loss 25.92%, solids gain 11.78%, rehydration ratio 203.40%, and shrinkage 2.90%. The weight reduction and moisture loss increased when the sonication time and sucrose concentration increased. Results demonstrated that the experimental data could be adequately fitted into a linear model with p-value ranging from 0.0001 to 0.0309 for all the variables examined. The rehydration of dried samples increased when xanthan concentration increased. Also, the weight reduction, moisture loss, sucrose absorption, and shrinkage declined with increasing in the xanthan levels.


Subject(s)
Citrus paradisi , Dehydration , Osmosis , Sucrose , Water
18.
Clin Pharmacol Ther ; 114(2): 470-482, 2023 08.
Article in English | MEDLINE | ID: mdl-37307228

ABSTRACT

Grapefruit is a moderate to strong inactivator of CYP3A4, which metabolizes up to 50% of marketed drugs. The inhibitory effect is mainly attributed to furanocoumarins present in the fruit, irreversibly inhibiting preferably intestinal CYP3A4 as suicide inhibitors. Effects on CYP3A4 victim drugs can still be measured up to 24 hours after grapefruit juice (GFJ) consumption. The current study aimed to establish a physiologically-based pharmacokinetic (PBPK) grapefruit-drug interaction model by modeling the relevant CYP3A4 inhibiting ingredients of the fruit to simulate and predict the effect of GFJ consumption on plasma concentration-time profiles of various CYP3A4 victim drugs. The grapefruit model was developed in PK-Sim and coupled with previously developed PBPK models of CYP3A4 substrates that were publicly available and already evaluated for CYP3A4-mediated drug-drug interactions. Overall, 43 clinical studies were used for model development. Models of bergamottin (BGT) and 6,7-dihydroxybergamottin (DHB) as relevant active ingredients in GFJ were established. Both models include: (i) CYP3A4 inactivation informed by in vitro parameters, (ii) a CYP3A4 mediated clearance estimated during model development, as well as (iii) passive glomerular filtration. The final model successfully describes interactions of GFJ ingredients with 10 different CYP3A4 victim drugs, simulating the effect of the CYP3A4 inactivation on the victims' pharmacokinetics as well as their main metabolites. Furthermore, the model sufficiently captures the time-dependent effect of CYP3A4 inactivation as well as the effect of grapefruit ingestion on intestinal and hepatic CYP3A4 concentrations.


Subject(s)
Citrus paradisi , Furocoumarins , Cytochrome P-450 CYP3A , Cytochrome P-450 Enzyme Inhibitors , Drug Interactions , Food-Drug Interactions , Furocoumarins/analysis , Furocoumarins/pharmacokinetics
19.
Chem Biodivers ; 20(7): e202300167, 2023 Jul.
Article in English | MEDLINE | ID: mdl-37211951

ABSTRACT

Grapefruit peel polysaccharide has antioxidant, antitumor, hypoglycemic and other biological activities, and chemical modification can further improve the properties of the polysaccharide. Acetylation modification of polysaccharides has the advantages of simple operation, low cost and little pollution, and is widely used at present. Different degrees of acetylation modification have different effects on the properties of polysaccharides, so it is necessary to optimize the preparation technology of acetylated grapefruit peel polysaccharides. In this article, acetylated grapefruit peel polysaccharide was prepared by acetic anhydride method. With the degree of acetyl substitution as the evaluation index, combined with the analysis of sugar content and protein content in the polysaccharide before and after modification, the effects of three feeding ratios of 1:0.6, 1 : 1.2 and 1 : 1.8 (polysaccharide: acetic anhydride, mass/volume) on acetylation modification were explored through single factor experiments. The results showed that the optimum ratio of material to liquid for acetylation modification of grapefruit peel polysaccharide was 1:0.6. Under these conditions, the degree of substitution of acetylated grapefruit peel polysaccharide was 0.323, the sugar content was 59.50 % and the protein content was 1.038 %. The results provide some reference for the study of acetylated grapefruit peel polysaccharide.


Subject(s)
Citrus paradisi , Acetic Anhydrides , Polysaccharides/pharmacology , Polysaccharides/chemistry , Sugars , Acetylation
20.
Molecules ; 28(7)2023 Mar 23.
Article in English | MEDLINE | ID: mdl-37049665

ABSTRACT

Much attention has been paid to the health benefits of including fruits and vegetables in the diet. However, for the compounds responsible for this beneficial effect to be effective at the level of the human organism, they must be available for absorption after digestion. In this sense, in vivo studies are needed to demonstrate the bioavailability of these compounds and their physiological activity. In order to provide information in this regard, this study collects data on the levels of vitamin C (VC) and naringenin (NAG) in the blood serum of the 11 volunteer participants in this trial, before and after consuming two different grapefruit juices. The juices were prepared by rehydrating the grapefruit powder obtained by freeze-drying (FD) the fruit puree or by spray-drying (SD) the liquefied grapefruit. No significant differences (p > 0.05) neither by juice nor by participant were observed in any case. The mean relative increase of VC, NAG and the radical scavenging ability (RSA) in blood serum due to grapefruit juices intake was 12%, 28% and 26%, respectively. Just VC showed a positive and significant Pearson's correlation with RSA. The mean bioavailability of VC was quantified as 1.529 ± 0.002 mg VC/L serum per 100 mg of VC ingested.


Subject(s)
Citrus paradisi , Humans , Ascorbic Acid/analysis , Beverages/analysis , Biological Availability , Flavonoids/analysis , Fruit and Vegetable Juices , Vitamins
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