Anti-breast cancer activity of the essential oil from grapefruit mint (Mentha suaveolens × piperita).

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.

Extraction of pectins from renewable grapefruit (Citrus paradisi) peels using deep eutectic solvents and analysis of their structural and physicochemical properties.

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.

Ex Vivo Anti-Leukemic Effect of Exosome-like Grapefruit-Derived Nanovesicles from Organic Farming-The Potential Role of Ascorbic Acid.

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.

Examining the Naringin Content and Sensory Characteristics of Functional Chocolate Fortified with Grapefruit Peel Extract.

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.

Chondroprotective Effects of Grapefruit (Citrus paradisi Macfad.) Juice in a Complete Freund's Adjuvant Rat Model of Knee Osteoarthritis.

Osteoarthritis (OA) is a common disorder that can affect any joint in the human body. This study aimed to examine the anti-arthritic properties of high and low doses of grapefruit juice (GFJ), as grapefruit appears to contain anti-inflammatory biochemicals. Forty male Sprague-Dawley rats weighing 170-180 g were divided into five groups. These groups comprised the untreated control group and osteoarthritic (Osteo) rats administered intra-articular injections of Freund's complete adjuvant (CFA; 0.5 mL; 1 mg/mL) as follows: OA rats administered low doses of GFJ (Osteo+GFJ (low); 5 mL/kg body weight (BW)); OA rats administered high doses of GFJ (Osteo+GFJ (high); 27 mL/kg BW); and OA rats administered diclofenac sodium (Osteo+Diclo) as a reference drug. Injections of CFA induced OA, as indicated by a significant increase in the serum levels of the inflammatory biomarkers C-reactive protein (CRP), interleukin-1ß (IL-1ß), and (prostaglandin (PGE2), as well as matrix metalloproteinases (MMP-1) and cathepsin K. The synovial levels of glycosaminoglycans (GAGs), tumor necrosis factor (TNF-α), and interleukin 6 (IL-6) also increased, with a concomitant reduction in osteocalcin levels. The administration of either high or low doses of GFJ reduced CRP, IL-1ß, PGE2, MMP-1, cathepsin K, and osteocalcin while increasing the synovial levels of GAGs, TNF-α, and IL-6, slowing cartilage degradation and boosting joint function. The results showed comparable histopathological and biochemical responses. A comparison of the treatments showed that high-dose GFJ had a greater chondroprotective effect than low-dose GFJ.

Coumarinolignoid and Indole Alkaloids from the Roots of the Hybrid Plant Citrus × paradisi Macfad (Rutaceae).

A phytochemical investigation of the roots of Citrus × paradisi Macfad. (Rutaceae) led to the isolation of two new compounds, namely 1-formyl-5-hydroxy-N-methylindolin-1-ium (1) and decyloxycleomiscosin D (2), along with ten known compounds: 1,1-dimethylpyrrolidin-1-ium-2-carboxylate (3), furan-2,3-diol (4), 5-methoxyseselin (5), umbelliferone (6), scopoletin (7), citracridone I (8), citracridone II (9), citracridone III (10), limonin (11) and lupeol (12). The structures were determined through the comprehensive spectroscopic analysis of 1D and 2D NMR and EI- and ESI-MS, as well as a comparison with the published data. Notably, compounds 3 and 4 from the genus Citrus are reported here for the first time. In addition, the MeOH extract of the roots and compounds 1-7 were screened against the human adenocarcinoma alveolar basal epithelial cell line A549 and the Caucasian prostate adenocarcinoma cell line PC3 using the MTT assay. While the extract showed significant activity, with IC50 values of 35.2 and 38.1 µg/mL, respectively, compounds 1-7 showed weak activity, with IC50 values of 99.2 to 250.2 µM and 99.5 to 192.7 µM, respectively.

Grapefruit Seed Extract-Added Functional Films and Coating for Active Packaging Applications: A Review.

Recently, consumers have been increasingly inclined towards natural antimicrobials and antioxidants in food processing and packaging. Several bioactive compounds have originated from natural sources, and among them, grapefruit seed extract (GSE) is widely accepted and generally safe to use in food. GSE is a very commonly used antimicrobial in food; lately, it has also been found very effective as a coating material or in edible packaging films. A lot of recent work reports the use of GSE in food packaging applications to ensure food quality and safety; therefore, this work intended to provide an up-to-date review of GSE-based packaging. This review discusses GSE, its extraction methods, and their use in manufacturing food packaging film/coatings. Various physical and functional properties of GSE-added film were also discussed. This review also provides the food preservation application of GSE-incorporated film and coating. Lastly, the opportunities, challenges, and perspectives in the GSE-added packaging film/coating are also debated.

Chemical Constituents of the Stem Bark of the Hybrid Plant Citrus × paradisi Macfad. (Rutaceae).

The stem bark of Citrus × paradisi Macfad. (Rutaceae) gave (23S)-isolimonexic acid (1), limonin (2), citracridone II (3), citpressine II (4), citpressine I (5), grandisine (6), 2-hydroxynoracronycine (7), citracridone I (8), 5-methoxyseselin (9), umbelliferone (10), scopoletin (11), naringenin (12), apigenin (13), friedelin (14), agrostophyllinone (15) and stigmasterol-3-O-ß-D-glucopyranoside (16). The structures of the compounds were determined using NMR and MS spectroscopic data, and by comparison with published data. The relative configuration of 1 was proposed as (23S)-isolimonexic acid using NOE studies. Hydrogenation reaction of compound 3 led to the new derivative 3',4'-dihydrocitracridone II (3a). Cytotoxicity activities against the human adenocarcinoma alveolar basal epithelial cell lines A549 and the Caucasian prostate adenocarcinoma cell lines PC3, using the MTT assays showed that the methanol crude extract was significant with IC50 values of 30.1 and 31.7 µg/mL, respectively, with the positive control, doxorubicin giving an IC50 of 0.9 µM. In addition, compounds 3, 7 and 8 gave moderate cytotoxic activities with IC50 values of 33.1, 31.2 and 32.5 µM for A549 cells and 35.7, 33.8 and 34.9 µM for PC3 cells, respectively. The hydrogenated 3a was less active than 3, suggesting that the presence of the double bond in pyrans is important for structure-activity relationship.

Antimicrobial, antioxidant, and pH-sensitive polyvinyl alcohol/chitosan-based composite films with aronia extract, cellulose nanocrystals, and grapefruit seed extract.

Aronia or black chokeberry (Aronia melanocarpa), cellulose nanocrystals (CNCs), and grapefruit seed extract (GSE) were used for the preparation of multifunctional polyvinyl alcohol/chitosan (PVA/CS) composite films with pH-sensitivity, antimicrobial, antioxidant, and UV-barrier properties. Aronia extract showed total phenolic content of 297 ± 0.5 µg GAE/mg aronia extract, potent antioxidant activity, and high color-response efficiency. Isolated CNCs showed a needle-like structure with a length of 470 nm and a width of 35 nm. The tensile strength of the PVA/CS composite film increased by 74% after the incorporation of CNCs, whereas the film flexibility was enhanced by 75% after adding GSE. The PVA/CS-A (aronia extract) composite film showed a significant color change at different pHs and potent antioxidant activity. At the same time, the PVA/CS-G (GSE) showed the highest antimicrobial activity against Escherichia coli (Gram-negative) and Listeria monocytogenes (Gram-positive) bacteria. The PVA/CS-CGA composite film, reinforced with CNCs/GSE/Aronia extract, showed the highest UV-barrier (95.5%), highest antioxidant activity (95%), potent antimicrobial activity, pH-sensitivity, lowest water vapor permeability (WVP), and desirable mechanical properties. The multifunctional properties of the produced composite films encourage their use as active and intelligent food packaging films to extend shelf life and monitor food quality.

Grapefruit peel extract mitigates paroxetine-induced erectile dysfunction in rats through stimulation of erectile response, antioxidant status, and inhibition of key enzymes related with impaired penile erection.

Despite the antidepressant potency of paroxetine, its side effect of erectile dysfunction is burdensome. Grapefruit peels (GFPs) are underutilized cultivar wastes with wide range of therapeutic potentials which have been attributed to their antioxidant behavior and phenolic contents' abilities to effectively inhibit enzymatic activities and manage endothelial dysfunction in cardiovascular disorders. This study aims to investigate the erectogenic potentials of GFP extract in a rat model of paroxetine-induced ED. Experimental rats were sectioned into five groups: [1: control; 2: paroxetine (10 mg/kg); 3: paroxetine + sildenafil (5 mg/kg); 4: paroxetine + GFP (50 mg/kg); 5: paroxetine + GFP (100 mg/kg)] and treated for 28 days. Sexual behavior of rats was assessed and effect of GFP on ecto-5' nucleotidases, phosphodiesterase-5, and adenosine deaminase (ADA) activities was determined in rats' penile tissues. The levels of malondialdehyde, nitric oxide (NO) as well as superoxide dismutase (SOD) and catalase activities were also determined. HPLC-DAD analysis showed the presence of naringin, rutin, caffeic acid, quercitrin, quercetin, and kaempferol glycoside. Oral administration of paroxetine reduced erectile response as revealed by their low intromission and mounting numbers as well as high intromission and mounting latencies. Paroxetine caused a significant elevation of ADA and phosphodiesterase-5 activities and malondialdehyde levels with drastic reduction in levels of NO, SOD, and catalase activities in rats' penile tissues. However, GFP extract reversed PDE-5, ADA, and antioxidant activities to normal levels, raised the concentration of NO. These results suggest the erectogenic effects and protective potentials of GFP extract against paroxetine-induced erectile dysfunction. PRACTICAL APPLICATION: Grapefruit peels are an environmental menace in many countries and this study showed that the peels can be used in the prevention / management of erectile dysfunction. The therapeutic potentials of the peels are due to the presence of bioactive compounds such as flavonoids and phenolic acids. Therefore, exploring the erectogenic potentials of the peels will translate to conversion of the wastes to therapeutic products.

Antifungal activity of Zinc nitrate derived nano Zno fungicide synthesized from Trachyspermum ammi to control fruit rot disease of grapefruit.

Grapefruit (Citrus paradisi) is a widely grown citrus and its fruit is affected by a variety of biotic and abiotic stress. Keeping in view the hazardous effects of synthetic fungicides, the recent trend is shifting towards safer and eco-friendly control of fruit diseases. The present study was aimed to diagnose the fruit rot disease of grapefruit and its control by using zinc oxide green nanoparticles (ZnO NPs). Fruit rot symptoms were observed in various grapefruit growing sites of Pakistan. Diseased samples were collected, and the disease-causing pathogen was isolated. Following Koch's postulates, the isolated pathogen was identified as Rhizoctonia solani. For eco-friendly control of this disease, ZnO NPs were prepared in the seed extract of Trachyspermum ammi and characterized. Fourier transform infrared spectroscopy (FTIR) of these NPs described the presence of stabilizing and reducing compounds such as phenols, aldehyde and vinyl ether, especially thymol (phenol). X-ray diffraction (XRD) analysis revealed their crystalline nature and size (48.52 nm). Energy dispersive X-ray (EDX) analysis elaborated the presence of major elements in the samples, while scanning electron microscopy (SEM) confirmed the morphology of bio fabricated NPs. ZnO NPs exhibited very good anti-fungal activity and the most significant fungal growth inhibition was observed at 1.0 mg/ml concentration of green NPs, in vitro and in vivo. These findings described that the bioactive constituents of T. ammi seed extract can effectively reduce and stabilize ZnO NPs. It is a cost-effective method to successfully control the fruit rot disease of grapefruit.

Influence on grape aromatic compounds of natural fungicides used for the control of downy mildew.

BACKGROUND: The grape volatile fraction determines to a great extent its aroma, which is one of the most important characteristics influencing wine quality and consumer preferences. Grapevine downy mildew (GDM) is one of the most important and devastating diseases of grapevines worldwide. In this study, the impact on the volatile composition of cv. Verdicchio grapes of classical copper formulations, was compared to that of alternative products. Thus, 11 treatments were foliar applied throughout one grapevine cycle. RESULTS: Most of the volatile compounds present in the grapes were not affected by the treatments used in order to prevent GDM. In the case of the total C13 norisoprenoids, some differences were found between grapes untreated control and those applied with the grapefruit seed extract. Moreover, the content of alcohols was smaller in grapes from Bordeaux mixture treatment and higher in the samples from chitosan application. CONCLUSION: Therefore, from the qualitative point of view of the berry, treatment with tested products alternative to copper is recommended, which minimize the environmental and health problems that this heavy metal brings to the soil and in the winery, since it means that their applications did not affect the grape aroma. © 2022 Society of Chemical Industry.

Explore the antiproliferative phytocompounds from ethanolic extracts of Citrus paradisi against liver cancer cell line by chemical analysis using TLC and FT-IR spectroscopy.

The aim of the present study was to evaluate the in vitro antiproliferative activity of ethanolic extract of leaves and fruits Citrus paradisi plant on HepG-2 liver cell lines by MTT (3-(4, 5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-terazolium bromide) assay and to isolate and characterize the antiproliferative compounds by TLC (Thin layer chromatography) and FT-IR (Fourier transforms Infrared) spectroscopy. Qualitative phytochemical screening tests were performed to detect phytochemicals compounds from the crude extracts. Antioxidant activity of the plant extracts were characterized by using DPPH (2,2-Diphenyl-1-picrylhydrazyl) free radical scavenging method. The results showed that antioxidant activity using DPPH were found to be increased in a concentration dependent manner and decreased cell viability and cell growth inhibition in a dose dependent manner. The findings from this study indicated that fruit extract exhibited good antiproliferation and antioxidant potential. The seven functional groups of phytocompounds such as carboxylic acid, amine salt, aromatic compounds, cyclic alkene, aldehyde, fluoro compounds and alkene were detected by FT-IR which indicated that fruit extracts of Citrus paradisi possessed vast potential as a medicinal drug especially in liver cancer treatment.

Effects of Citri Reticulatae Pericarpium and grapefruit juice on the pharmacokinetics of omeprazole in rats.

The effects of Citri Reticulatae Pericarpium (CRP) and grapefruit juice (GFJ) on the pharmacokinetics of omeprazole were investigated in this study. Sprague-Dawley rats were pretreated with CRP decoction or GFJ for 28 consecutive days. After a single intragastric administration of 6.0 mg/kg, the concentration of omeprazole in the plasma was determined by high-performance liquid chromatography (HPLC), and the pharmacokinetic parameters were calculated by Kinetica software 5.0. A high-performance liquid chromatography-quadrupole-time-of-flight mass spectrometry (HPLC-Q-TOF-MS) method was established to identify the chemical components in CRP decoction and GFJ. The results showed that the AUCt-∞ was significantly increased when coadministrated with CRP. The AUC0-t and AUC0-∞ was remarkably increased; the Cl was decreased when coadministrated with GFJ. A total of 31 and 28 bioactive compounds were identified in the CRP decoction and GFJ, respectively. Flavonoids and furanocoumarins, including hesperidin, hesperetin, naringenin, sinensetin, tangeretin, nobiletin, and 6',7'-dihydroxybergamottin, were simultaneously identified in CRP decoction and GFJ. This study indicates that the increased bioavailability of omeprazole may be due to the inhibition of hepatic cytochrome P450 enzymes, and the systemic exposure should be monitored when concomitant administration with CRP and GFJ. PRACTICAL APPLICATIONS: Citri Reticulatae Pericarpium (CRP) has been widely consumed as a daily condiment, functional food, and a traditional Chinese medicine. Omeprazole, primary metabolized by CYP450 enzymes, was usually coadministered with CRP for the treatment of gastrointestinal disease. Studies have confirmed that much fruit juices, including grapefruit juice, may affect drug metabolism enzymes. CRP and grapefruit (Citrus paradisi Macf.) belong to the genus Citrus and family Rutaceae with different species. Therefore, the pharmacokinetic interaction of CRP decoction and grapefruit juice with omeprazole is worthy of attention. The results of this study can provide basic pharmacological data support for the safe and effective clinical use of omeprazole. It can also provide a theoretical basis for the development of new functional products and daily application of CRP.

Explore the antiproliferative phytocompounds from ethanolic extracts of Citrus paradisi against liver cancer cell line by chemical analysis using TLC and FT-IR spectroscopy / Explorar os fitocompostos antiproliferativos de extratos etanólicos de Citrus paradisi contra linhagem de células de câncer de fígado por análise química usando espectroscopia de TLC e FT-IR

The aim of the present study was to evaluate the in vitro antiproliferative activity of ethanolic extract of leaves and fruits Citrus paradisi plant on HepG-2 liver cell lines by MTT (3-(4, 5-dimethyl-2-thiazolyl)-2,5-diphenyl-2Hterazolium bromide) assay and to isolate and characterize the antiproliferative compounds by TLC (Thin layer chromatography) and FT-IR (Fourier transforms Infrared) spectroscopy. Qualitative phytochemical screening tests were performed to detect phytochemicals compounds from the crude extracts. Antioxidant activity of the plant extracts were characterized by using DPPH (2,2-Diphenyl-1-picrylhydrazyl) free radical scavenging method. The results showed that antioxidant activity using DPPH were found to be increased in a concentration dependent manner and decreased cell viability and cell growth inhibition in a dose dependent manner. The findings from this study indicated that fruit extract exhibited good antiproliferation and antioxidant potential. The seven functional groups of phytocompounds such as carboxylic acid, amine salt, aromatic compounds, cyclic alkene, aldehyde, fluoro compounds and alkene were detected by FT-IR which indicated that fruit extracts of Citrus paradisi possessed vast potential as a medicinal drug especially in liver cancer treatment.

O objetivo do presente estudo foi avaliar a atividade antiproliferativa in vitro do extrato etanólico de folhas e frutos da planta Citrus paradisi em linhagens de células hepáticas HepG-2 por MTT (3- (4, 5-dimetil-2-tiazolil) -2, Ensaio de brometo de 5-difenil-2H-terazólio) e isolar e caracterizar os compostos antiproliferativos por espectroscopia de TLC (cromatografia de camada fina) e FT-IR (infravermelho com transformadas de Fourier). Testes qualitativos de triagem fitoquímica foram realizados para detectar compostos fitoquímicos nos extratos brutos. A atividade antioxidante dos extratos vegetais foi caracterizada pelo método de eliminação de radicais livres DPPH (2,2-difenil-1-picrilhidrazil). Os resultados mostraram que a atividade antioxidante usando DPPH aumentou de uma maneira dependente da concentração e diminuiu a viabilidade celular e a inibição do crescimento celular de uma maneira dependente da dose. Os resultados deste estudo indicaram que o extrato de fruta exibiu bom potencial antiproliferação e antioxidante. Os sete grupos funcionais de fitocompostos, como ácido carboxílico, sal de amina, compostos aromáticos, alceno cíclico, aldeído, compostos de flúor e alceno, foram detectados por FT-IR, o que indicou que extratos de frutas de Citrus paradisi possuíam vasto potencial como medicamento, especialmente no tratamento de câncer do fígado.

Role of Citrus Fruit Juices in Prevention of Kidney Stone Disease (KSD): A Narrative Review.

To explore the relationship between citrus fruit juices (oranges, grapefruits, and lemonades) and kidney stone disease (KSD). METHODS: A systematic review was performed using the Medline, EMBASE, and Scopus databases, in concordance with the PRISMA checklist for all English, French, and Spanish language studies regarding the consumption of citrus fruit juices and the relationship to urinary stone disease. The main outcome of interest was the association of citrus fruit juices with KSD. RESULTS: Thirteen articles met the criteria for inclusion in the final review. Three large epidemiological studies found that grapefruit juice was a risk factor for stone formation, while orange juice did not increase the risk for KSD. Ten small prospective clinical studies found that orange, grapefruit, and lemon juices all increased urinary citrate levels. Only orange and grapefruit juices had an alkalinizing effect and while lemon juice has a protective effect by raising urinary citrate levels, it lacked a significant alkalinizing effect on urine pH. Orange juice and grapefruit juices significantly increased urinary oxalate levels, while orange juice also had a high carbohydrate content. CONCLUSION: While orange juice seems to play a protective role against stone formation, grapefruit was found to raise the risk of KSD in epidemiological studies but had a protective role in smaller clinical studies. Lemon juice had a smaller protective role than orange juice. Larger amounts of, as well as more accurate, data is needed before recommendations can be made and a high carbohydrate content in these juices needs to be taken into consideration.

Antioxidant and antibacterial activities of Artemisia absinthium and Citrus paradisi extracts repress viability of aggressive liver cancer cell line.

BACKGROUND: Numerous reports show that herbal medicines can be utilized in the treatment of different liver disorders. In this study, antioxidant, antibacterial, and anticancer activities of individual as well as combined 80% ethanolic extracts of Artemisia absinthium leaves and Citrus paradisi peels were investigated. METHODS AND RESULTS: Values of total phenolic contents (TPC), total flavonoid contents (TFC), DPPH-radical scavenging activity, and ferric reducing antioxidant power (FRAP) were measured to explore the antioxidant capacity. To assess antibacterial activity, four bacterial strains (Escherichia coli, Staphylococcus aureus, Salmonella enterica, and Klebsiella pneumoniae) were used. Anticancer activity was assessed on Huh-7 (liver cancer) and Vero (non-cancerous) cell lines. FRAP activity of combined plants extract was higher as compared to their individual effect; the trend did not hold in the case of DPPH-radical scavenging activity. Antibacterial activity of combined extracts by disk diffusion method was observed only against E.coli. MTT results indicated that both plants had a cytotoxic effect on Huh-7 cell line but did not show any effect on Vero cell line. Our data showed a strong negative correlation between the amount of TPC, TFC, & DPPH radicals-scavenging activity and viability of Huh-7 cell line.However, no effect was shown on the non-cancerous cell line. CONCLUSION: The ethanolic extracts of Artemisia absinthium leaves and Citrus paradisi peels can be used against liver cancer because of their antioxidant, antibacterial, and anticancer activities.

In vitro and in vivo inhibition of Helicobacter pylori by Lactobacillus plantarum pH3A, monolaurin, and grapefruit seed extract.

Helicobacter pylori infection is the most common cause of gastritis and gastric ulcers. Considering the severe side effects of current antibiotic therapies, it is crucial to find an alternate treatment for H. pylori infection. In this study, we investigated the anti-H. pylori effects of a newly isolated strain of Lactobacillus plantarum (pH3A), monolaurin, grapefruit seed extract (GSE), and their synergies in vitro and in vivo. Monolaurin and GSE suppressed H. pylori growth and urease activity at a minimal inhibitory concentration (MIC) of 62.5 ppm. Live cells and cell-free culture supernatant (CFCS) of L. plantarum pH3A with or without pH adjustment also significantly inhibited H. pylori growth. Although synergy was not observed between monolaurin and GSE, the addition of CFCS significantly enhanced their anti-H. pylori activities. Moreover, L. plantarum pH3A significantly decreased the ability of H. pylori to adhere to AGS cells and interleukin (IL)-8 production in the H. pylori-stimulated AGS cell line. The addition of GSE or monolaurin strengthened these effects. In the in vivo study, H. pylori colonization of the mouse stomach and total serum IgG production were significantly reduced by L. plantarum pH3A treatment, but the addition of monolaurin or GSE did not contribute to these anti-H. pylori activities. Therefore, the L. plantarum pH3A strain can potentially be applied as an alternative anti-H. pylori therapy, but evidence of its synergy with monolaurin or GSE in vivo is still lacking.

Bergamottin a CYP3A inhibitor found in grapefruit juice inhibits prostate cancer cell growth by downregulating androgen receptor signaling and promoting G0/G1 cell cycle block and apoptosis.

Prostate cancer is the second leading cause of cancer related death in American men. Several therapies have been developed to treat advanced prostate cancer, but these therapies often have severe side effects. To improve the outcome with fewer side effects we focused on the furanocoumarin bergamottin, a natural product found in grapefruit juice and a potent CYP3A inhibitor. Our recent studies have shown that CYP3A5 inhibition can block androgen receptor (AR) signaling, critical for prostate cancer growth. We observed that bergamottin reduces prostate cancer (PC) cell growth by decreasing both total and nuclear AR (AR activation) reducing downstream AR signaling. Bergamottin's role in reducing AR activation was confirmed by confocal microscopy studies and reduction in prostate specific antigen (PSA) levels, which is a marker for prostate cancer. Further studies revealed that bergamottin promotes cell cycle block and accumulates G0/G1 cells. The cell cycle block was accompanied with reduction in cyclin D, cyclin B, CDK4, P-cdc2 (Y15) and P-wee1 (S642). We also observed that bergamottin triggers apoptosis in prostate cancer cell lines as evident by TUNEL staining and PARP cleavage. Our data suggests that bergamottin may suppress prostate cancer growth, especially in African American (AA) patients carrying wild type CYP3A5 often presenting aggressive disease.

Protective, Antioxidant and Antiproliferative Activity of Grapefruit IntegroPectin on SH-SY5Y Cells.

Tested in vitro on SH-SY5Y neuroblastoma cells, grapefruit IntegroPectin is a powerful protective, antioxidant and antiproliferative agent. The strong antioxidant properties of this new citrus pectin, and its ability to preserve mitochondrial membrane potential and morphology, severely impaired in neurodegenerative disorders, make it an attractive therapeutic and preventive agent for the treatment of oxidative stress-associated brain disorders. Similarly, the ability of this pectic polymer rich in RG-I regions, as well as in naringin, linalool, linalool oxide and limonene adsorbed at the outer surface, to inhibit cell proliferation or even kill, at high doses, neoplastic cells may have opened up new therapeutic strategies in cancer research. In order to take full advantage of its vast therapeutic and preventive potential, detailed studies of the molecular mechanism involved in the antiproliferative and neuroprotective of this IntegroPectin are urgently needed.