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... [10] Others reported that essential oil of R. rosifolius contained β-caryophyllene, dihydroagarofuran, isokessane and β-kessane, [11] ellagic acid, euscaphic acid, pomolic acid, β-sitosterol -glucoside-6′-acetate, trachelosperogenin A, and some had activity against the carcinogen-activating CYP1B1 enzyme. [12] Some Rubus were reported to have potential activity as inhibitor enzyme such as elastase, collagenase, hyaluronidase, and tyrosinase. [13][14][15][16][17] So, the objective of this research was to examine the potential of R. rosifolius leaves as an elastase inhibitor and to dock different ligands of its constituents against target protein porcine pancreatic elastase (PPE) receptor. ...
... Pomolic acid and euscaphic acid were isolated from ethyl acetate extract. [12] Both of these compounds showed a large Ki even though ethyl acetate extract showed weak activity. Ellagic acid and gallic acid were the most predominant of the phenolic compound isolated from methanol extract. ...
... Ellagic acid and gallic acid were the most predominant of the phenolic compound isolated from methanol extract. [12] Docking test and in vitro test showed that methanol extract has potential activity as an elastase inhibitor. ...
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Objective: Elastases are protease enzymes, which mainly hydrolyze proteins of the connective tissue, so they have a significant impact on human disease. Rubus rosifolius is one of the Rubus species found in Indonesian mountains, and it has potential as an elastase inhibitor. The objective of this research was to examine the in vitro elastase inhibitor activity of R. rosifolius leaves and to dock different ligands of its constituents against target protein of Porcine Pancreatic Elastase (PPE) receptor. Method: Dried leaves powder of R. rosifolius was extracted using Soxhlet apparatus with n-hexane, ethyl acetate, and methanol. The extract was evaporated, and in vitro elastase inhibitor activity was determined using PPE with the quercetin used as control positive. Selected nine constituents of R. rosifolius were evaluated on the docking behavior of elastase receptor using Protein-Ligand ANT System (PLANTS) computational software with PPE enzyme with Protein Data Bank (PDB) file 1BRU. Result: The methanol extract showed significantly inhibited elastase with IC50 186.13 μg/mL, but ethyl acetate extract showed weak activity, and n-hexane extract did not show any activity. Docking studies and binding free energy calculations and hydrogen bonding with some amino acids revealed that ellagic acid showed the least binding energy for the target enzyme. Conclusion: This research has opened new insights into understanding that constituents of R. rosifolius methanol extract are potential inhibitors against elastase, and suggested the active compound is ellagic acid.
... Two varieties of Rubus rosifolius, "Red" and "Wine Red" (R and WR, respectively), have been described by our research group . Their phytochemistry along with their antioxidant and cytochrome P450 (CYP) inhibitory activity were determined and they were found to possess potential chemopreventive activity (Campbell, McKenzie, Murray, Delgoda, & Bowen-Forbes, 2017). To the best of our knowledge, the antidiabetic or antihypoglycemic activity of these R. rosifolius plants however has not been reported to date. ...
... We also examined possible mechanisms for the oxidation of a mixture of triacylglycerols (TAGs). The extraction protocol was previously reported (Campbell et al., 2017). Briefly, ripe R. rosifolius berries were freeze-dried using a Labconco Freezone Freeze Dryer system (Kansas City, MO, USA) and a specific mass of each (160 g and 202 g for the R and WR fruit powders, respectively) extracted successively with n-hexane, ethyl acetate, and methanol, with a solvent to plant ratio of 4:1 (v/w). ...
... Each solvent extract (n-hexane, EtOAc, and MeOH) from the two R. rosifolius varieties was analyzed in a preliminary oral glucose tolerance test (OGTT) study, and based on other studies conducted on the extracts from the two fruit varieties, R Hex , WR EtOAc , and R MeOH were the most promising and were therefore the focus of this study (Campbell et al., 2017). The hypoglycemic effects of the crude extracts were assessed using a previously reported OGTT with minor modifications (Alexander-Lindo, Salmon, & McGrowder, 2017). ...
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Oral glucose tolerance test on male Sprague–Dawley rats was done to determine the hypoglycemic effect of the n‐hexane, ethyl acetate and methanol fruit extracts (50 mg/kg BW; oral administration) of two varieties of Rubus rosifolius . Metformin was used as a positive control (15 mg/kg BW; intravenous administration). The n‐hexane extract was most potent and was investigated phytochemically to yield compound 1 , a mixture of triacylglycerols. In its oxidized state compound 1 produced a significant hypoglycemic effect which was more effective than metformin for the first 30 min of the assay (p = .03) and not significantly different for up to 120 min. Mechanisms through which the oxidized triacylglycerol species could form were explored and presented. This is the first account of the hypoglycemic activity of R. rosifolius and it is also the first account of this activity being credited to compounds other than polyphenols and terpenes in Rubus plants. Practical applications A significant percentage of the world’s population is affected by diabetes and diabetes‐related illnesses. One of the most popular antidiabetic drug on the market is metformin which is used to lower blood glucose concentrations. The findings of this study indicate that an oxidized mixture of triacylglycerols is more fast‐acting than metformin for the first 30 min of an oral glucose tolerance test. This effect was also not significantly different from that of the popular drug up to 120 min. These results demonstrate the hypoglycemic activity of an oxidized R. rosifolius fruit extract and indicate its potential use in applications such as functional food product development and drug discovery. Therapeutic applications can also include the plant extract as a potential primary treatment or as adjunct therapy to conventional medications.
... From an agro-processing perspective, it is important for the sake of product consistency to know if the variation noted in fruit colour, and possibly other attributes, is random or due to intrinsic differences. Profiling of their phenolic contents, chemopreventative properties (via cytochrome P450 inhibitory analysis), antioxidant, antimicrobial, and hypoglycemic activities revealed notable differences between these two morphotypes (Campbell et al. 2017;Rambaran and Ginigini 2020;. The same was true for their anthocyanins, essential oils, and several sensory parameters (Rambaran and Ginigini 2020;. ...
... We decided to undertake this task by using 59 different descriptors to determine which could be used to separate the two Rubus morphotypes in the field, and thus to recommend the most useful ones for further studies. Phytochemical analysis reported in Campbell et al. (2017), , Rambaran and Ginigini (2020), and were also undertaken to see if statistically relevant variations could be found between these two morphotypes. ...
Article
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Precise identification of plants is critical for informed agriculture where nutraceutical properties and productivity are simultaneously important. The Jamaican-grown West Indian raspberry (Rubus rosifolius) falls into this category. The first step to taking this wild-growing plant into agricultural production is morphological identification. Although there are no botanical reports of multiple varieties of this species in Jamaica, two morphotypes were found, which were named ‘Red' and ‘Wine Red’ based on fruit colour. Morphological methods were used to characterise these plants growing at Holywell (located over 900 m above sea level), in the Blue Mountain region of Jamaica. Morphological analyses revealed that growth form, leaf, flower, and fruit characteristics of the morphotypes were statistically distinctive between the two morphotypes for 48 of the 59 measured parameters. Several descriptors allowed the morphotypes to be distinguished before their fruits became visible. These findings support the hypothesis that there is a standard morphotype having a scrambling morphology, smaller leaves, and darker red, oblong, solitary fruits (Wine Red, WR), and a distinct morphotype with more upright stems, larger leaves, and lighter red, spherical, bunched fruits (Red, R). This information can now be used to facilitate molecular analyses and ramp-up clonal production of these morphotypes to determine the agricultural factors that are linked to yield and nutritionally relevant traits.
... The antimicrobial activity of the methanol extracts may be due to the presence of tannins. The presence of these compounds in the methanol extracts was previously reported in our research group by Campbell et al. [35] . Two mechanisms through which tannins are believed to impart their antimicrobial effects are deprivation of substrates needed to sustain microbial growth and inhibition of extracellular microbial enzymes. ...
... Additionally, the three mentioned solvent extracts of the two R. rosifolius varieties were also assessed previously for their chemo preventive properties against cytochromes P450 (CYP) enzymes and it was found that the methanol extract from the R variety (99.2% inhibition) and the hexane and ethyl acetate extracts from the WR variety (81.1 and 82.0% inhibition, respectively) were most effective [35] . These findings do not support claims of any strong correlation between the brine shrimp lethality of the extracts and their chemo preventive effects; however, some similarity exists between the former and the anticancer effects reported. ...
Article
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The essential oil composition of two varieties of the red raspberry, Rubus rosifolius (Red, R and Wine red, WR) was examined and the antimicrobial activity and brine shrimp lethality of their extracts determined. Plant samples were obtained and their essential oil profiles assessed using GC-MS analysis. Antimicrobial activity of the crude extracts of both plant varieties was assessed against drug-resistant and foodborne pathogens and the brine shrimp ethality assay was used to assess the potential lethality of the extracts. The quantity and identified essential oil components of the fruits varied between the varieties with the R variety having in greatest quantity the monoterpene, linalool, while that of the WR variety was found to be the sesquiterpene, α-cadinol. Analysis of the antimicrobial activity of the extracts against the growth of drug resistant pathogens showed the methanol extracts having greatest activity with zones of inhibition of 11 and 13 mm (for the R and WR varieties, respectively) against methicillin-resistant Staphylococcus aureus (MRSA). The methanol extracts also exhibited minimal activity against several food-borne pathogens including two strains of Escherichia coli, Listeriamono cytogenes and Enterobacter aerogenes. Brine shrimp lethality of the various extracts revealed that the essential oils of both plant varieties had the greatest activity with a LC50 value of 63 and 48 ppm for RHex and WRHex, respectively. The biological activities of the fruit extracts indicate that their utilization in the production of functional foods, nutraceuticals and pharmaceuticals should be further explored.
... In addition, anthocyanins [28]. Also, ellagic acid, detected in both acerola and camu-camu extracts, has shown potent antioxidant activity in previous reports [34]. ...
... For instance, euscaphic acid, isolated from R. rosifolius, has been reported to show significant antioxidant activity. Ellagic acid, quercetin, and kaempferol, identified from R. rosifolius were related to the chemopreventive properties of the plant (Campbell et al., 2017). Phenolic rich extracts of R. rosifolius presented antimicrobial properties with anti-quorum sensing properties and antioxidant activity ( Oliveira et al., 2016). ...
Article
In the present study, the biological properties, including, the enzyme inhibitory and antioxidant activities, as well as, the phytochemical profile of the ethyl acetate, methanol, and water extracts of Rubus sanctus Schreb. and Rubus ibericus Juz. leaves were determined using in vitro bioassays. Wide range of phytochemicals, including, hydroxybenzoic acids, hydroxycinnamic acids, acylquinic acids, ellagitannins, flavonoids, and triterpenoid saponins were determined using UHPLC-ESI/HRMS technique. The ethyl acetate and methanol extracts of the studied Rubus species effectively inhibited acetyl and butyryl cholinesterase. On the other hand, R. sanctus water extract showed low inhibition against α-amylase and prominent inhibitory action against α-glucosidase. Data collected from this study reported the radical scavenging and reducing potential of the studied Rubus species. Investigation of the protective effects of the different extracts of R. sanctus and R. ibericus in experimental model of ulcerative colitis was performed. The extracts were also tested on spontaneous migration of human colon cancer cells (HCT116) in wound healing experimental paradigm. Only R. sanctus methanol extract inhibited spontaneous HCT116 migration in the wound healing test. Our results suggested that R. sanctus and R. ibericus may be potential candidates as sources of biologically-active compounds for the development of nutraceuticals, pharmaceuticals, and/or cosmetics.
... Wild strawberry (Rubus rosifolius Sm.) belongs to the Rosaceae family and is a species introduced in southern Brazil (Jacques and Zambiazi, 2011;Donadio, 2014). It has high economical value, being source of antioxidants such as vitamin C and carotenoids, and could be used as dyes, foods and medicines (Jacques and Zambiazi, 2011;Donadio, 2014;Campbell et al., 2017). On the medicinal point of view, strawberries have been used in the popular medicine by presenting antimicrobial activity, in the treatment of diabetes and to reduce pain (Mauro et al., 2002) Although some studies have been published about R. rosifolius, variations on maturation, cultivation practices, location and harvest conditions may imply on different plant properties. ...
Article
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The objective of the present work was to evaluate polyphenols, trace elements and compounds with antioxidant, antimicrobial and anti-hypertensive activity in wild strawberries cultivated in Southern Brazil. Fruits present high fiber, iron, potassium and sodium concentrations. Polyphenolic content was 242.12 mg of gallic acid equivalent per 100g and monomeric anthocyanin concentration was 100.50 mg of cyanidin 3-glucoside per 100g. Wild strawberries presented the capacity of scavenging 89% of ABTS•+ radical and 61% of DPPH• radicals and chelating power of 3.1, meanwhile the inhibition of the angiotensin-converting enzyme I activity was 12.5%. Fruits presented compounds with capacity to inhibit Staphylococcus aureus, Bacillus cereus, Listeria monocytogenes and Aeromonas hydrophyla. Thus, wild strawberries are important source of functional compounds and their consumption is a way to promote the Brazilian biodiversity and improve human diet.
... Nonvolatile terpenoids in the roots may be involved in defense against competing plants and for signaling root development(Tholl 2015). The positive results for A. bunius fruit, C. ovatum pulp, and R. rosifolius were in agreement with previous reports(Ragasa et al. 2015;Campbell et al. 2017). C. ovatum nut oil was reported to contain terpenoid derivatives (Pham and Dumandan 2015). ...
Article
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Nine Philippine indigenous fruits were screened for phytochemical constituents and assessed for total phenolics and antioxidant and antibacterial activities. Qualitative tests revealed the presence of alkaloids in Canarium ovatum, cardiac glycosides in Ficus pseudopalma and C. ovatum, and terpenoids in Antidesma bunius and C. ovatum. Total phenolics were highest in Garcinia binucao and Mangifera altissima with 758 and 694 mg gallic acid equivalent (GAE) / 100 g fresh matter (FM), respectively. The DPPH radical scavenging activities ranged from 82-516 mg ascorbic acid equivalent antioxidant activity (AEAC) /100 g FM, with M. altissima having the highest value and followed by Rubus rosifolius (513 mg AEAC / 100 g FM). Ferric reducing activities were highest for M. altissima and G. binucao with 111 mg and 121 mg ascorbic acid equivalents (AAE) / 100 g FM, respectively. Phenolic and flavonoid contents were strongly and positively correlated (P < 0.05). Moreover, phenolic contents may have significant contributions to the observed radical scavenging and ferric reducing activities based on their strong positive correlations (P < 0.05). For the antibacterial activities, extracts from Citrus hystrix and R. rosifolius were the most effective against Escherichia coli (MIC 80 = 1.70 mg GAE/mL), while the F. pseudopalma extract was the most effective against Staphylococcus aureus (MIC 80 = 0.56 mg GAE / mL). Present results showed that the selected indigenous fruits could be valuable sources of phytochemicals, such as phenolics and flavonoids, with potential antioxidant and antibacterial activities.
... Nonvolatile terpenoids in the roots may be involved in defense against competing plants and for signaling root development(Tholl 2015). The positive results for A. bunius fruit, C. ovatum pulp, and R. rosifolius were in agreement with previous reports(Ragasa et al. 2015;Campbell et al. 2017). C. ovatum nut oil was reported to contain terpenoid derivatives (Pham and Dumandan 2015). ...
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Nine Philippine indigenous fruits were screened for phytochemical constituents and assessed for total phenolics and antioxidant and antibacterial activities. Qualitative tests revealed the presence of alkaloids in Canarium ovatum, cardiac glycosides in Ficus pseudopalma and C. ovatum, and terpenoids in Antidesma bunius and C. ovatum. Total phenolics were highest in Garcinia binucao and Mangifera altissima with 758 and 694 mg gallic acid equivalent (GAE) / 100 g fresh matter (FM), respectively. The DPPH radical scavenging activities ranged from 82-516 mg ascorbic acid equivalent antioxidant activity (AEAC) /100 g FM, with M. altissima having the highest value and followed by Rubus rosifolius (513 mg AEAC / 100 g FM). Ferric reducing activities were highest for M. altissima and G. binucao with 111 mg and 121 mg ascorbic acid equivalents (AAE) / 100 g FM, respectively. Phenolic and flavonoid contents were strongly and positively correlated (P < 0.05). Moreover, phenolic contents may have significant contributions to the observed radical scavenging and ferric reducing activities based on their strong positive correlations (P < 0.05). For the antibacterial activities, extracts from Citrus hystrix and R. rosifolius were the most effective against Escherichia coli (MIC 80 = 1.70 mg GAE/mL), while the F. pseudopalma extract was the most effective against Staphylococcus aureus (MIC 80 = 0.56 mg GAE / mL). Present results showed that the selected indigenous fruits could be valuable sources of phytochemicals, such as phenolics and flavonoids, with potential antioxidant and antibacterial activities.
... ;Gou et al., 2011), antifungal activities(De Lucca and Walsh, 1999), antioxidative activities(Campbell et al., 2017; Kawanishi et al., 2005), anti-inflammatory activities(Nonn et al., 2007), and anticancer activities(Kim et al., 2012). Among the anticancer properties, several reports have demonstrated that chemopreventive agents can suppress multiple pathways through a specific molecular target, such as the inhibition of NF-kB(Bharti and Aggarwal, 2002), AP-1(Manna et al., 2000), COX2(Muller-Decker et al., 2002;Subbaramaiah et al., 1998), and JAK-STAT(Bharti et al., 2003) activation pathways, as inhibitors of cell proliferation(Surh, 2003), cell cycling(Mukhopadhyay et al., 2002), angiogenesis(Chen et al., 2004), and multidrug resistance(Anuchapreeda et al., 2002; Hong et al., 2003). ...
Article
Background: Duchesnea indica (Andr.) Focke, an herb in folk medicine used extensively in traditional Chinese medicine, has cytostatic properties as well as antioxidant and antimetastasis activities in various cancer cells. However, the effects and underlying mechanisms of Duchesnea indica extracts (DIEs) on human oral squamous cell carcinoma (OSCC) metastases remain unclear. Purpose: In this study, we posit the hypothesis that DIE possesses antimetastatic effects on human OSCC cells. Methods: The effects of DIE on cell viability, motility, migration, and invasion were investigated. Gelatin zymography, Western blotting, migration and invasion assays were used to further study the underlying mechanisms involved in the antimetastatic effects of DIE in OSCC cells. Results: The results from MTT assay revealed that DIE did not affect the cell viability of OSCC cells. Moreover, DIE significantly attenuated OSCC cells' motility, migration, and invasion by reducing the MMP-2 protein expression and MMP-2 activity in a dose-dependent manner. In addition, DIE reduced the phosphorylation of both ERK1/2 and its upstream kinase but had no effect on the phosphorylation of p38 and JNK. Conclusion: DIE triggers the antimetastatic activity in OSCC cells by suppressing the MMP-2 activity via the MEK/ERK signaling pathways. Therefore, these findings are promising for the use of DIE antimetastatic activity in oral cancer metastasis treatment.
... Numerous biological properties have been suggested for polyphenols and included among these are antioxidant, antimicrobial, anti-cancer, anti-inflammatory and anti-diabetic effects [4][5][6][7][8]. For this review we will however focus only on their anti-diabetic activity. ...
Article
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Polyphenols are believed to possess numerous health benefits and can be grouped as phenolic acids, flavonoids or non-flavonoids. Research involving the synthesis of nanopolyphenols has attracted interest in the areas of functional food, nutraceutical and pharmaceutical development. This is in an effort to overcome current challenges which limit the application of polyphenols such as their rapid elimination, low water-solubility, instability at low pH, and their particle size. In the synthesis of nanopolyphenols, the type of nanocarrier used, the nanoencapsulation technique employed and the type of polymers that constitute the drug delivery system are crucial. For this review, all mentioned factors which can influence the therapeutic efficacy of nanopolyphenols were assessed. Their efficacy as anti-diabetic agents was also evaluated in 33 publications. Among these were phenolic acid (1), flavonoids (13), non-flavonoids (17) and polyphenol-rich extracts (2). The most researched polyphenols were quercetin and curcumin. Nanoparticles were the main nanocarrier and the size of the nanopolyphenols ranged from 15 to 333 nm with encapsulation efficiency and drug loading capacities of 56–97.7% and 4.2–53.2%, respectively. The quantity of nanomaterial administered orally ranged from 1 to 300 mg/kg/day with study durations of 1–70 days. Most studies compared the effect of the nanopolyphenol to its free-form and, in all but three cases, significantly greater effects of the former were reported. Assessment of the polyphenol to understand its properties and the subsequent synthesis of its nanoencapsulated form using suitable nanocarriers, polymers and encapsulation techniques can result in effective therapeutic agents for the treatment of diabetes.
... There are numerous observational and experimental accounts of suggested health benefits of phenolic compounds, and berry fruits are believed to be a significant source of these compounds in the diet (4)(5)(6)(7). The most predominant berry polyphenols include tannins and flavonoids, with the latter group accounting for approximately twothirds of all the phenolics in the diet (8,9). ...
Article
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The effect of berry polyphenols on glucose metabolism has been evaluated in several studies; however, the results are conflicting. A systematic review and meta-analysis was therefore conducted to evaluate the effect of berry polyphenol consumption on glucose metabolism in adults with impaired glucose tolerance or insulin resistance. PubMed/MEDLINE, Cochrane Central Register of Controlled Trials (CENTRAL), CINAHL (EBSCO), and Scopus were searched for randomized controlled trials published by June 2019. Of the 3240 articles found, 21 met our inclusion criteria. Study-specific effects were calculated as mean differences (MDs), which were pooled using fixed-effect, inverse-variance weighting. Overall, berry polyphenol consumption did not have a clear effect on biomarkers of glucose metabolism compared to placebo or no treatment. Although some analyses showed statistically significant effects, these effects were too small to be of clinical relevance. The review protocol was registered in the PROSPERO International Prospective Register of Systematic Reviews (CRD42019130811).
... The phenolic profiles of the fruits were also previously analysed by LC-MS. Ellagic acid, which was the major phenolic compound identified, was found to be an important contributor to the CYP1B1 activity of the methanol extracts of the two varieties [3]. ...
Article
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Raspberries are economically important fruits, being highly valued for their taste and medicinal properties. Prior to our recent finding, the occurrence of different varieties of Rubus rosifolius growing in Jamaica had not been previously reported. Upon close observation of the plants, differences in various physical features pointed to the existence of two distinct plant morphotypes, which were described as Red “R” and Wine Red “WR.” With an aim to determine which variety may be more favourable for value-added food production, we undertook their physicochemical and sensory analysis. This characterisation led to the rationalisation of the differences in the perceived sensory properties of these biologically active fruits. Total phenolic content was determined using the Folin-Ciocalteu reagent assay, and the identification and quantification of anthocyanins were done via HPLC-MS and HPLC-UV, respectively. Proximate and physicochemical analyses were also carried out. The findings of the analyses were associated with those of a consumer sensory analysis. The WR fruits had a greater quantity of the deep red anthocyanin, cyanidin-3-glucoside (66.2 mg/100 g FW), and a significantly lower lightness value. They also received a significantly higher sweetness score, which is associated with their higher total sugar content (4.8 g/100 g) and maturity index (6.7). The R fruits had a higher quantity of the orange-coloured pelargonidin-3-rutinoside (17.2 mg/100 g FW) and significantly higher titratable acidity (1.3 g citric acid/100 mL), the latter being associated with its significantly more sour taste. The high total phenolic contents suggest a health-functional value of these R. rosifolius berry fruits. Our findings, which revealed that the WR variety was the preferred choice among consumers, may be used to guide future product-development endeavours of these commercially valuable fruits.
... Ellagic acid (m/z 300.9990), which was detected in Ese, belongs to the class of organic compounds known as ellagitannin. This compound is well known for its antioxidant activity with free radical scavenging properties [19]. Ellagitannin compounds were found in both samples, although galloyl-HHDP-hexoside (m/z 633.0559) was detected only in F3. ...
Article
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Brazilian native fruits are a rich source of polyphenolic compounds that can act as anti-inflammatory and antioxidant agents. Here, we determined the polyphenolic composition, anti-inflammatory mechanism of action, antioxidant activity and systemic toxicity in Galleria mellonella larvae of Eugenia selloi B.D.Jacks. (synonym Eugenia neonitida Sobral) extract (Ese) and its polyphenol-rich fraction (F3) obtained through bioassay-guided fractionation. Phenolic compounds present in Ese and F3 were identified by LC-ESI-QTOF-MS. The anti-inflammatory activity of Ese and F3 was tested in vitro and in vivo through NF-κB activation, cytokine release and neutrophil migration assays. The samples were tested for their effects against reactive species (ROO•, O2•-, HOCl and NO•) and for their toxicity in Galleria mellonella larvae model. The presence of hydroxybenzoic acid, ellagitannins and flavonoids was identified. Ese and F3 reduced NF-κB activation, cytokine release and neutrophil migration, with F3 being three-fold more potent. Overall, F3 exhibited strong antioxidant effects against biologically relevant radicals, and neither Ese nor F3 were toxic to G. mellonella larvae. In conclusion, Ese and F3 revealed the presence of phenolic compounds that decreased the inflammatory parameters evaluated and inhibited reactive oxygen/nitrogen species. E. selloi is a novel source of bioactive compounds that may provide benefits for human health.
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This book reviews the applications of polyphenols in cancer treatment. The initial chapter of the book classifies different polyphenols and discusses their biological and chemical properties. The subsequent chapters then explore the diverse role of polyphenols in modulating signal transduction pathways in cancer including, cellular proliferation, differentiation, apoptosis, inflammation, angiogenesis, and metastasis. This book highlights the usefulness of polyphenol enriched seafood in modulating the anti-tumor and anti-inflammatory cytokine IFN-γ. The book also presents nanoformulation of polyphenol as a promising strategy for their enhanced bioavailability and targeted delivery. Lastly, the book examines the toxicity and safety evaluations of polyphenols as anticancer agents.
Chapter
Nanotechnology is an emerging technique, implementing widely in various fields of sciences, including pharmaceutical design, delivery, and targeting of drugs. The small size and flexibility to tune their physicochemical properties render them high biocompatibility and diverse functionality. Polyphenols have been extensively researched and demonstrated essential characteristics such as antimicrobial, antidiabetic, antioxidant, and anticancer activities. However, mere use of these molecules is encountered with several challenges including poor stability, solubility, and bioavailability that limited their applications and usefulness. To circumvent these limitations and to enhance polyphenols’ applications as therapeutics, drug delivery system-based nanotechnology is envisaged to pose a promising strategy. The main objective of this chapter is to highlight the recent advancement in polyphenols-based nanotechnology for pharmaceutical applications. The focus will be on the most studied molecules including quercetin, resveratrol, epigallocatechin-3-gallate, and curcumin.
Chapter
Despite the concerted efforts in pursuit of developing effective therapy, the human race has merely succeeded in its fight against cancer. The limited success in this battle against cancer may be attributed to the development of resistance to the available therapeutic regimens, frequent recurrence, metastasis, tumor heterogeneity, and immune evasion. The sub-populated cancer stem cells (CSCs) are often held responsible for cancer relapse, therapy resistance, and metastasis. The stemness and tumorigenicity of CSCs are regulated by various pathways such as Wnt/β-catenin, hedgehog, PI3K-AKT, JAK-STAT, TGF-β, and notch signaling. Various therapeutic agents targeting CSCs are now being considered for the treatment of various malignancies. However, conventional therapies are associated with various side effects. Therefore, current therapeutic approaches are witnessing a paradigm shift towards natural compounds. To this end, dietary polyphenols are considered promising drug candidates for their both preventive as well as therapeutic properties. In this chapter, the non-flavonoid polyphenols are discussed in the context of their ability to target CSCs and their role in attenuation of fundamental pathways involved in the maintenance of CSCs such as Wnt/β-catenin, hedgehog, notch, and induction of programmed cell death pathways has been explored. The overview of this chapter will help the oncologist to devise more efficacious combinatorial therapies, utilizing naturally occurring non-flavonoid polyphenols and their derivatives along with chemotherapeutic drugs, which will offer the advantage of eliminating both the CSCs and other malignant cells in the heterogeneous tumor mass as a multipronged approach. The traditional knowledge of phytomedicines along with the current advancements of molecular and precision medicine and suitable delivery system hold a great promise to combat cancer and exterminate it from the root.
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Brazilian native fruits (BNF) remain unexplored and underutilized resources with a high potential to improve human health and wellness. In our study, five new BNF (Eugenia stipitata, Sageretia elegans, Byrsonima arthropoda, Spondias mombin and Rubus rosaefolius) were evaluated for their phenolic composition by LC-ESI-QTOF-MS; and for their ROS and RNS scavenging effects (ROO[rad], O2[rad]−, NO[rad], HOCl); in vivo anti-inflammatory activity (neutrophil migration); and in vivo acute toxicity in Galleria mellonella. Eighty-six phenolic compounds were identified, including hydroxybenzoic acids, hydroxycinnamic acids, flavonoids, anthocyanins and ellagitannins, several of which had never been reported in BNF. The BNF exhibited high antioxidant effects against biologically relevant radicals, and treated animals showed decreased neutrophil influx and NF-kB activation. Thus, these BNF are good sources of antioxidant and anti-inflammatory molecules that can be beneficial for human health as functional foods. Based on their bioactivity, they can be considered as new Brazilian superfruits.
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Quassinoids often exhibit antioxidant and antiproliferative activity. Emerging evidence suggests that these natural metabolites also display chemopreventive actions. In this study, we investigated the potential for the quassinoid glaucarubulone glucoside (Gg), isolated from the endemic Jamaican plant Castela macrophylla (Simaroubaceae), to display potent cytotoxicity and inhibit human cytochrome P450s (CYPs), particularly CYP1A enzymes, known to convert polyaromatic hydrocarbons into carcinogenic metabolites. Gg reduced the viability of MCF-7 breast adenocarcinoma cells (IC50 = 121 nm) to a greater extent than standard of care anticancer agents 5-fluorouracil, tamoxifen (IC50 >10 μm) and the tamoxifen metabolite 4-hydroxytamoxifen (IC50 = 2.6 μm), yet was not cytotoxic to non-tumorigenic MCF-10A breast epithelial cells. Additionally, Gg induced MCF-7 breast cancer cell death. Gg blocked increases in reactive oxygen species in MCF-10A cells mediated by the polyaromatic hydrocarbon benzo[a]pyrene (B[a]P) metabolite B[a]P 1,6-quinone, yet downregulated the expression of genes that promote antioxidant activity in MCF-7 cells. This implies that Gg exhibits antioxidant and cytoprotective actions in non-tumorigenic breast epithelial cells and pro-oxidant, cytotoxic actions in breast cancer cells. Furthermore, Gg inhibited the activities of human CYP1A according to non-competitive kinetics and attenuated the ability of B[a]P to induce CYP1A gene expression in MCF-7 cells. These data indicate that Gg selectively suppresses MCF-7 breast cancer cell growth without impacting non-tumorigenic breast epithelial cells and blocks B[a]P-mediated CYP1A induction. Taken together, our data provide a rationale for further investigations of Gg and similar plant isolates as potential agents to treat and prevent breast cancer. Copyright © 2017 John Wiley & Sons, Ltd.
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Corosin (8; R = R ¹ = H) has been reisolated through a modified procedure, as its acetate (8; R=H, R ¹ = Ac), in an overall yield of 0.2% from jute roots. On pyrolysis in vacuo, corosin gave pyro corosin (1a; R ¹ = OH, R ² = COOH, R ³ = R ⁵ = H, R ⁴ = R ⁶ = Me), shown to have a 12:18 (17) di-ene formed by elimination of the 19-OH and the angular C-28 carboxyl in the molecule. On rearrangement with concentrated sulphuric acid in acetic acid, corosin acetate gave corosin anhydro lactone acetate (7; R ¹ = Ac, R = H), having a 13(18) double bond and a lactone bridge between the 28-carboxyl and the 20-carbon atom. Corosin acetate ester (8; R = Me, R 1 = Ac), on treatment with sulphuric-acetic acid reagent, gave as the main product anhydro corosin acetate ester (7; R = Me, R ¹ = A c), with a 12:18(19)-diene. The structure of corosin is proposed to be urs-12-ene-2α, 3β, 19α-trihydroxy-24, 28-dioic acid (8; R = R ¹ = H).
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Red fruits (blueberry, blackberry, chokeberry, strawberry, red raspberry, sweet cherry, sour cherry, elderberry, black currant and red currant) were analyzed for flavonols (quercetin, myricetin, and kaempferol), hydroxycinnamic acids (caffeic, ferulic, p-coumaric acid) and hydroxybenzoic acids (p-hydroxybenzoic, ellagic acid) by using HPLC method. Compounds were analyzed as aglycons after acid hydrolysis with 1.2 mol dm–3 HCl. Each fruit sample was analyzed for total polyphenols (TP) and total anthocyanins (TA). TP ranged from 1763 to 7194 mg kg–1 fresh weight (FW) in red raspberries and chokeberries, respectively. TA ranged from 169 to 4069 mg kg–1 FW in strawberries and blueberries, respectively. Flavonols varied from 4 mg kg–1 in red raspberries to 183 mg kg–1 in blueberries. Hydroxycinnamic acids were found in relatively high concentrations in blueberries (92 mg kg–1) and in black currant (70 mg kg–1) and represented significant portion in sour and sweet cherry phenolics. The amount of ellagic acid was high in blackberry (121 mg kg–1), strawberry (41 mg kg–1) and red raspberry (32 mg kg–1). The strongest antioxidant activity determined by DPPH· and ABTS·+ assays showed chokeberry, followed by blueberry, black currant and elderberry. Antioxidant activity correlated better with TP than with TA, total flavonols (TF), or total hydroxycinnamic acids. Additionally, linear relationship was observed between antioxidant activity of fruits and content of caffeic acid, quercetin and p-coumaric acid. Overall results showed that red fruits can serve as good source of bioactive polyphenols in human diet, but due to high concentrations of anthocyanins, flavonols, phenolic acids and strong antioxidant activity, chokeberry, blueberry, elderberry and black currant can be regarded as good candidates for nutritional supplement formulations.
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The flowers of Sesnania grandiflora (Linn.) Pers. afforded a 3:2 mixture of B-stigmasterol (1a) and B-sitosterol (1b), and oleanolic acid (2), while the leaves of Heliotropium indicum Linn. yielded B. carotene (3), lutein (4), a mixture of polyprenols (5), and a mixture of B. stigmasterol and B-sitosterol. The structures of 1a, 1b and 3 were elucidated by extensive 1D and 2D NMR analyses. Antimicrobial activity tests on 3 indicated that it has high activity against Pseudomonas aeruginosa and Aspergillus niger, slight activity against Staphylococcus auresu, Escherichia coli, Candida albicans and Trichophyton mentagrophytes, and inactive against Bacillus subtilis.
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Background The aim of this study was to screen various solvent extracts of whole plant of Torilis leptophylla to display potent antioxidant activity in vitro and in vivo, total phenolic and flavonoid contents in order to find possible sources for future novel antioxidants in food and pharmaceutical formulations. Material and methods A detailed study was performed on the antioxidant activity of the methanol extract of whole plant of Torilis leptophylla (TLM) and its derived fractions {n-hexane (TLH), chloroform (TLC) ethyl acetate (TLE) n-butanol (TLB) and residual aqueous fraction (TLA)} by in vitro chemical analyses and carbon tetrachloride (CCl4) induced hepatic injuries (lipid peroxidation and glutathione contents) in male Sprague-Dawley rat. The total yield, total phenolic (TPC) and total flavonoid contents (TFC) of all the fractions were also determined. TLM was also subjected to preliminary phytochemical screening test for various constituents. Results The total phenolic contents (TPC) (121.9±3.1 mg GAE/g extract) of TLM while total flavonoid contents (TFC) of TLE (60.9 ±2.2 mg RTE/g extract) were found significantly higher as compared to other solvent fractions. Phytochemical screening of TLM revealed the presence of alkaloids, anthraquinones, cardiac glycosides, coumarins, flavonoids, saponins, phlobatannins, tannins and terpenoids. The EC50 values based on the DPPH (41.0±1 μg/ml), ABTS (10.0±0.9 μg/ml) and phosphomolybdate (10.7±2 μg/ml) for TLB, hydroxyl radicals (8.0±1 μg/ml) for TLC, superoxide radicals (57.0±0.3 μg/ml) for TLM and hydrogen peroxide radicals (68.0±2 μg/ml) for TLE were generally lower showing potential antioxidant properties. A significant but marginal positive correlation was found between TPC and EC50 values for DPPH, hydroxyl, phosphomolybdate and ABTS, whereas another weak and positive correlation was determined between TFC and EC50 values for superoxide anion and hydroxyl radicals. Results of in vivo experiment revealed that administration of CCl4 caused a significant increase in lipid peroxidation (TBARS) while decrease in GSH contents of liver. In contrast, TLM (200 mg/kg bw) and silymarin (50 mg/kg bw) co-treatment effectively prevented these alterations and maintained the antioxidant status. Conclusion Data from present results revealed that Torilis leptophylla act as an antioxidant agent due to its free radical scavenging and cytoprotective activity.
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Polyphenols are among a wide variety of active photochemicals present in the human diet. Basic researches and epidemiological studies have shown the inverse association between risk of cancer, CVDs, diabetes, several age related chronic diseases and intake of diet rich in polyphenols. Recent researches have opened the possibility of dietary polyphenols to be considered as phytomedicine. Most of the studies on the bioactivity of polyphenols have been conducted on animal models and in in vitro systems, direct studies on humans are few and results inconclusive. The bioavailability and biotransformation of polyphenols in humans needs to be studied. The present review provides an update about dietary polyphenols covering their nature, occurrence, bioavailability, and possible health benefits in relation to human diseases.
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Total equivalent antioxidant capacities (TEAC) and phenolic contents of 32 spices extracts from 21 botanical families grown in Poland were investigated. The total antioxidant capacity was estimated by the following methods: ABTS+ (2,2′azinobis-(3-ethylbenzthiazoline-6-sulfonic acid)), DPPH (1,1-diphenyl-2-picrylhydrazyl radical) and ferric reducing/antioxidant power (FRAP) expressed as TEAC. The total phenolics were measured using a Folin–Ciocalteu assay. Qualitative and quantitative analyses of major phenolics by reverse-phase high-performance liquid chromatography (RP-HPLC) were also used. Major phenolic acids identified in analyzed species were caffeic, p-coumaric, ferulic and neochlorogenic, while predominant flavonoids were quercetin, luteolin, apigenin, kaempferol and isorhamnetin. Myricetin was detected only in Epilobium hirsutum. Many investigated spices had high levels of phenolics and exhibited high antioxidant capacity. The TEAC values of the spices ranged from 1.76 to 346 μM trolox/100 g dw, from 7.34 to 2021 μM trolox/100 g dw, and 13.8 to 2133 μM trolox/100 g dw for ABTS+, DPPH and FRAP, respectively. The total phenolic content, measured using a Folin–Ciocalteu assay, ranged from 0.07 to 15.2 mg of gallic acid equivalents (GAE)/100 g dw. The herbs with the highest TEAC values were Syzygium aromaticum, E. hirsutum and the species belonging to the Labiatae and Compositae family. A positive relationship between TEAC (ABTS+ and FRAP) values and total phenolic content, measured by HPLC, was found only in family groups with many representative herbs within Labiatae and Compositae.
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Berries are a good source of natural antioxidants. In the present study, the total antioxidant capacity and phenolic composition of three berry fruits (blueberry, blackberry, and strawberry) cultivated in Nanjing were investigated. Blueberry, with a Trolox equivalent antioxidant capacity (TEAC) value of 14.98 mmol Trolox/100 g dry weight (DW), exhibited the strongest total antioxidant capacity using both the 2,2-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) and the 2,2-diphenyl-1-picrylhydrazyl (DPPH) methods. Blueberry also had the highest total phenolic content (TPC, 9.44 mg gallic acid/g DW), total flavonoid content (TFC, 36.08 mg rutin/g DW), and total anthocyanidin content (TAC, 24.38 mg catechin/g DW). A preliminary analysis using high performance liquid chromatography (HPLC) showed that the blueberry, blackberry, and strawberry samples tested contained a range of phenolic acids (including gallic acid, protocatechuic acid, p-hydroxybenzoic acid, vanillic acid, caffeic acid, p-coumaric acid, ferulic acid, ellagic acid, and cinnamic acid) and various types of flavonoids (flavone: luteolin; flavonols: rutin, myricetin, quercetrin, and quercetin; flavanols: gallocatechin, epigallocatechin, catechin, and catechin gallate; anthocyanidins: malvidin-3-galactoside, malvidin-3-glucoside, and cyanidin). In particular, the blueberries had high levels of proanthocyanidins and anthocyanidins, which might be responsible for their strong antioxidant activities. These results indicate a potential market role for berries (especially blueberries) as a functional food ingredient or nutraceutical.
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To investigate the antimicrobial properties of phenolic compounds present in Finnish berries against probiotic bacteria and other intestinal bacteria, including pathogenic species. Antimicrobial activity of pure phenolic compounds representing flavonoids and phenolic acids, and eight extracts from common Finnish berries, was measured against selected Gram-positive and Gram-negative bacterial species, including probiotic bacteria and the intestinal pathogen Salmonella. Antimicrobial activity was screened by an agar diffusion method and bacterial growth was measured in liquid culture as a more accurate assay. Myricetin inhibited the growth of all lactic acid bacteria derived from the human gastrointestinal tract flora but it did not affect the Salmonella strain. In general, berry extracts inhibited the growth of Gram-negative but not Gram-positive bacteria. These variations may reflect differences in cell surface structures between Gram-negative and Gram-positive bacteria. Cloudberry, raspberry and strawberry extracts were strong inhibitors of Salmonella. Sea buckthorn berry and blackcurrant showed the least activity against Gram-negative bacteria. Different bacterial species exhibit different sensitivities towards phenolics. These properties can be utilized in functional food development and in food preservative purposes.
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Phenolic compounds are plant secondary metabolites that present many biological effects including antioxidant and antimicrobial activities. Studies have shown that these compounds can also inhibit quorum sensing bacterial communication. The aim of this study was to characterize the centesimal composition, mineral and phenolic content, to determine the antioxidant and antimicrobial effect as well as the inhibition of quorum sensing by the phenolic extract obtained from wild strawberry (Rubus rosaefolius). Centesimal composition and minerals were in the range expected for fruits of the Rubus generum, even though Fe and Zn presented higher levels. The phenolic content was 5902.89 mg GAE/L, also approaching the levels found for fruits of Rubus sp. The antioxidant activity determined through the ABTS method was 162.4 ± 5.6 and 120.8 ± 1.5 μM Trolox/g of fruit in the DPPH assay, indicating an elevated potential for ABTS and medium potential for DPPH method. The phenolic extract was able to inhibit all the evaluated bacteria presenting MICs in the range of 491.90–1475.74 mg GAE/L. In sub-MIC concentrations, the phenolic extract inhibited all the phenotypes typically regulated by quorum sensing in bacteria, including violacein production, swarming motility and biofilm formation. The phenolic extract of R. rosaefolius presented antioxidant, antimicrobial and anti-quorum sensing activities which are in agreement with previous studies linking phenolic compounds to these properties.
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From the methanolic extract of the leaves of Planchonella duclitan, 2α,3α,19α,23-tetrahydroxy-13,27-cyclours-11-en-28-oic acid (1), myrianthic acid (2), 2-hydroxyursolic acid (3), ursolic acid (4), pomolic acid (5), rotundic acid (6), and jacoumaric acid (7) were isolated, and their structures were elucidated on the basis of their spectroscopic analysis. Among them, compound 1 was a new cyclopropyl ursane-type triterpene acid. Additionally, compounds 4 and 7 showed significant cytotoxicity toward human colorectal carcinoma cell line HT29 and human breast carcinoma cell line MCF-7 with IC50 values ranging from 5.8 ± 1.4 to 6.5 ± 1.9 μM.
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Fresh or processed berries are considered to be beneficial for health by many consumers. Fruits of closely related species of plants sometimes possess strikingly different phytochemistry and biological activities. Therefore, even though similar research has been conducted on a number of Rubus berries, there is much relevance associated with the investigation of species that have not been previously studied. In the current report, the fruits of three wild Jamaica-grown species: Rubus jamaicensis, Rubus rosifolius and Rubus racemosus, and of the Michigan-grown Rubus acuminatus, Rubus idaeus cv. Heritage and Rubus idaeus cv. Golden were analyzed for their anthocyanin contents, and lipid peroxidation, cyclooxygenase enzyme and human tumor cell proliferation inhibitory activities. It was revealed that the fruits contained superior levels of anthocyanins (146–2199 mg/100 g fresh weight) to those previously reported for other raspberry and blackberry species, and their hexane, EtOAc and MeOH extracts showed good antioxidant activity, the majority of the extracts exhibiting over 50% lipid peroxidation inhibitory activity at 50 μg/mL. The hexane extracts of the Jamaican Rubus spp. demonstrated moderate COX inhibitory activity (27.5–33.1%) at 100 μg/mL, and exhibited the greatest potential to inhibit cancer cell growth, inhibiting colon, breast, lung, and gastric human tumor cells by 50, 24, 54 and 37%, respectively. The high anthocyanin content and biological activities of these fruits indicate that their consumption would be beneficial to health, and that they may be useful in the production of functional foods containing an efficacious dose of anthocyanins.
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Constituents of Schisandra propinqua (Wall.) Bail var. sinensis Oliv were investigated and 8 compounds were isolated from the stems and their structures were elucidated as (+)-catechin (1), (-)-gallocatechin (2), p-(2-hydroxyethyl)-phenol--D-glucopyranoside (3), daucosterol (4), manwuweizic acid (5), cerotic acid 1-monoglyceride (6), octocosoic acid (7) and -sitosterol (8) respectively. Based on MS and NMR techniques, (+)-Catechin, (-)-gallocatechin, p-(2-hydroxyethyl)-phenol-β β β β-D-glucopyranoside, manwuweizic acid, cerotic acid 1-monoglyceride and octocosoic acid were isolated from the plant for the first time. (+)-Catechin and (-)-gallocatechin mediated DNA cleavage with good efficiency at 1 µ µ µ µg/ml. (-)-Gallocatechin show DNA strand-scission activity for the first time.
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From the underground parts ofRosa rugosa(Rosaceae), 28-O-glucosides of euscaphic acid, tormentic acid and arjunic acid were isolated and characterized by spectral data.
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The Rubus genus produces numerous species that are known for their medicinal properties. Rubus rosifolius, called the red raspberry, grows wild in elevated regions in Jamaica. Phytochemical examination of the ethyl acetate extract of the fruit yielded eight compounds of the 19-α-hydroxyursane type: euscaphic acid (1), 1-β-hydroxyeuscaphic acid (2), hyptatic acid B (3), 19α-hydroxyasiatic acid (4), trachelosperogenin (5), 4-epi-nigaichigoside F1 (6), nigaichigoside F1 (7), and trachelosperoside B-1 (8), as confirmed by NMR spectroscopy. Inhibition of cell proliferation by these compounds were determined by using MCF-7 (breast), SF-268 (CNS), NCI H460 (lung), HCT-116 (colon) and AGS (gastric) human tumour cells. Among the human tumour cell lines assayed, only compounds 3 and 6 displayed significant growth inhibition and was specific to colon tumour cells by 56% and 40%, respectively. These ursolic acid analogues were also tested for anti-inflammatory activity using in vitro cycloxegenase-1 (COX-1) and cycloxegenase-2 (COX-2) enzyme inhibitory assays. Compounds 1, 2 and 3 showed selective COX-1 enzyme inhibitory activity (13%, 25% and 35%) at 25 μg/ml. In the lipid peroxidation (LPO) inhibitory assays, compounds 2, 4, 7 and 6 inhibited LPO by 62%, 60%, 53% and 68%, respectively, at 25 μg/ml.
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The antioxidant properties of the essential oil from oregano in relation to its chemical composition were examined. The antioxidant activity was investigated with three different methods: the β-carotene bleaching (BCB) test, the 2,2′-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method and the thiobarbituric acid reactive species (TBARS) assay. It was found that the total essential oil, its fraction as well as its pure constituents have a significant antioxidant effect when tested by each method, respectively. Generally the antioxidant activity of the oregano essential oil is less effective than the ascorbic acid, but comparable with the α-tocopherol and the synthetic antioxidant butylated hydroxytoluene (BHT). The synergy among minor oxygen containing compounds was suggested as possible factor, which influenced the antioxidant power of the oregano essential oil. The antioxidant concentrations influenced its antioxidant power, too.
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The effects of various fruit maturities and different light intensities on berry fruit quality, antioxidant capacity and phytonutrient levels in red raspberries (Rubus ideaus L.) were determined. At harvest, immature berries contained significantly lower levels of sugars and acids than ripe berries. When berries were harvested at 5% or 20% maturity, they never developed the levels of soluble solids content (SSC) and titratable acid (TA) values observed in ripe berries at harvest. However, fruit harvested at 50% or more advanced maturity had the capacity of attaining comparable levels of SSC, TA and sugars as those harvested at 100% maturity. When 5% and 20% berries were stored under light, higher level of SSC and lower levels of TA values were observed than those kept in the dark. However, light condition showed little effect in 50% and 80% maturity fruit after 4 days at 24/16 °C (day/night). Ripe raspberries (100%) had stronger antioxidant activities and higher total anthocyanin content when compared with the pink stage (50% maturity). Fruit harvested at greener stages (5% and 20%) also consistently showed higher antioxidant activities and total phenolics than those harvested at 50%. Cyanindin-based anthocyanins increased during postharvest period. On the other hand, other polyphenols such as ellagic acid, quercetin 3-glucoside, quercetin derivative, and kaempferol 3-glucuronide were initially present at high levels but decreased drastically during storage. Red raspberries harvested at different developmental stages continued their development during storage even under the dark conditions. The antioxidant activity of red raspberries was directly related to the total amount of phenolics and flavonoids. Results of this study indicate that red raspberries harvested at 50% or more advanced maturity could develop comparable quality and antioxidant levels as those harvested at full maturity.
Article
To evaluate the antihypertensive effect of Xinjiang red raspberry fruit ethyl acetate extract (EER) on spontaneously hypertensive rats (SHR) and its possible mechanism from antioxidant perspective. The SHR rats were randomly divided into 3 groups, and treated with EER low dose (EERL, 100 mg/kg/d), high dose (EERH, 200 mg/kg/d), and water (SHR) through gastric gavage daily for 5 weeks. Another 8 age-matched male Wistar-Kyoto rats were used as normotensive group (WKY). The systolic blood pressure (SBP) was measured by noninvasive tail-cuff method once a week. At the end of the treatment, blood samples were collected and serum concentrations of nitric oxide (NO), superoxide dismutase (SOD), malondialchehyche (MDA), and plasma endothelin (ET) were determined. Treatment of SHR rats with EER lowered the blood pressure compared with that treated with water (SHR), and the high dose showed more significant reduction in blood pressure. Treatment of SHR rats with EER increased serum NO and SOD levels and lowered ET and MDA levels. As compared with control group, NO levels were increased significantly in EERL (P < 0.01), SOD was elevated more significantly in both EERL and EERH (P < 0.01); MDA was decreased significantly in EERH group (P < 0.05), whereas plasma ET decreased more significantly in the EERH group (P < 0.05). The red raspberry extracts demonstrated a dose-dependent antihypertensive effects in SHR and this may be related to increased NO activation and improved vascular endothelial dysfunction via antioxidation. These results confirmed that raspberries rich in polyphenols have potential cardiovascular protective effects.
Article
Cytochrome P450 (CYP) 1B1 catalyzes 17beta-estradiol (E(2)) to predominantly carcinogenic 4-hydroxy-E(2), whereas CYP1A1 and 1A2 convert E(2) to non-carcinogenic 2-hydroxy-E(2). Hence, selective inhibition of CYP1B1 is recognized to be beneficial for the prevention of E(2) related breast cancer. In this study, we first evaluated the structure-property relationship of 18 major flavonoids on inhibiting enzymatic activity of CYP1A1, 1A2 and 1B1 by using an ethoxyresorufin O-deethylation assay. Flavones and flavonols indicated relatively strong inhibitory effects on CYP1s compared with flavanone that does not have the double bond between C-positions 2 and 3 on the C-ring. Flavonoids used in this study selectively inhibited CYP1B1 activity. In particular, methoxy types of flavones and flavonols such as chrysoeriol and isorhamnetin showed strong and selective inhibition against CYP1B1. To understand why selective inhibition was observed, we carried out a molecular docking analysis of these methoxyflavonoids with the 2-3 double bond and CYP1s. The results suggested that chrysoeriol and isorhamnetin fit well into the active site of CYP1B1, but do not fit into the active site of CYP1A2 and 1A1 because of steric collisions between the methoxy substituent of these methoxyflavonoids and Ser-122 in CYP1A1 and Thr-124 in CYP1A2. In conclusion, our results demonstrate: (1) strong inhibitory effects of flavonoids on CYP1 activities require the 2-3 double bond on the C-ring; (2) methoxyflavonoids with the 2-3 double bond had strong and selective inhibition against CYP1B1, suggesting chemopreventive flavonoids for E(2) related breast cancer; and (3) binding specificity of these methoxyflavonoids is based on the interactions between the methoxy groups and specific CYP1s residues.
Article
Anthocyanins are natural colorants belonging to the flavonoid family. They are widely distributed among flowers, fruits, and vegetables. Using the automated oxygen radical absorbance capacity (ORAC) assay developed in our laboratory, we determined the antioxidant capacity of 14 anthocyanins including the aglycons delphinidin, cyanindin, pelargonidin, malvidin, peonidin, and their derivatives with different sugar linkages. Among these anthocyanins, kuromanin (cyanidin-3-glucoside) had the highest ORAC activity, which was 3.5 times stronger than Trolox (vitamin E analogue), while pelargonin had the lowest antioxidant activity but was still as potent as Trolox. Different patterns of hydroxylation and glycosylation in anthocyanins appear to modulate their antioxidant properties. Therefore, in addition to their colorful characteristics, anthocyanins possess potent antioxidant properties.
Article
This study characterizes biologically active compounds of berry fruits, including non-nutritive compounds such as phenolic compounds, including anthocyanins, phenolic acids, stilbens and tannins, as well as nutritive compounds such as carotenoids and vitamin C. It discusses the biological activity of those compounds, in particular their antioxidant properties and the resulting health benefits.
Article
The anticarcinogen ellagic acid significantly reduces the incidence of polycyclic aromatic hydrocarbon induced carcinomas, in association with significant reductions in benzo[a]pyrene hydroxylase activity and CO reducible hepatic cytochrome P450. This suggested that ellagic acid reduced hepatic concentrations of CYP1A1, but these changes occurred without any alteration in CYP1A1 mRNA or in immunoreactive CYP1A1. Dietary ellagic acid results in muMolar concentrations of ellagic acid in hepatic tissue. Addition of similar concentrations of ellagic acid in vitro directly inhibited the measurement of benzo[a]pyrene hydroxylase activity and CO reducible cytochrome P450. Thus dietary ellagic acid does not alter the hepatic concentration of CYP1A1, but the dietary ellagic acid remaining in hepatic tissue appears to directly inhibit the measurement of benzo[a]pyrene hydroxylase activity and CO reducible cytochrome P450.
Article
Polycyclic aromatic hydrocarbons (PAHs) are ubiquitously distributed environmental chemicals. PAHs acquire carcinogenicity only after they have been activated by xenobiotic-metabolizing enzymes to highly reactive metabolites capable of attacking cellular DNA. Cytochrome P450 (CYP) enzymes are central to the metabolic activation of these PAHs to epoxide intermediates, which are converted with the aid of epoxide hydrolase to the ultimate carcinogens, diol-epoxides. Historically, CYP1A1 was believed to be the only enzyme that catalyzes activation of these procarcinogenic PAHs. However, recent studies have established that CYP1B1, a newly identified member of the CYP1 family, plays a very important role in the metabolic activation of PAHs. In CYP1B1 gene-knockout mice treated with 7,12-dimethylbenz[a]anthracene and dibenzo[a,l]pyrene, decreased rates of tumor formation were observed, when compared to wild-type mice. Significantly, gene expression of CYP1A1 and 1B1 is induced by PAHs and polyhalogenated hydrocarbons such as 2,3,7,8-tetrachlorodibenzo-p-dioxin through the arylhydrocarbon receptor. Differences in the susceptibility of individuals to the adverse action of PAHs may, in part, be due to differences in the levels of expression of CYP1A1 and 1B1 and to genetic variations in the CYP1A1 and 1B1 genes.
Article
This review summarizes the multifaceted aspects of antioxidants and the basic kinetic models of inhibited autoxidation and analyzes the chemical principles of antioxidant capacity assays. Depending upon the reactions involved, these assays can roughly be classified into two types: assays based on hydrogen atom transfer (HAT) reactions and assays based on electron transfer (ET). The majority of HAT-based assays apply a competitive reaction scheme, in which antioxidant and substrate compete for thermally generated peroxyl radicals through the decomposition of azo compounds. These assays include inhibition of induced low-density lipoprotein autoxidation, oxygen radical absorbance capacity (ORAC), total radical trapping antioxidant parameter (TRAP), and crocin bleaching assays. ET-based assays measure the capacity of an antioxidant in the reduction of an oxidant, which changes color when reduced. The degree of color change is correlated with the sample's antioxidant concentrations. ET-based assays include the total phenols assay by Folin-Ciocalteu reagent (FCR), Trolox equivalence antioxidant capacity (TEAC), ferric ion reducing antioxidant power (FRAP), "total antioxidant potential" assay using a Cu(II) complex as an oxidant, and DPPH. In addition, other assays intended to measure a sample's scavenging capacity of biologically relevant oxidants such as singlet oxygen, superoxide anion, peroxynitrite, and hydroxyl radical are also summarized. On the basis of this analysis, it is suggested that the total phenols assay by FCR be used to quantify an antioxidant's reducing capacity and the ORAC assay to quantify peroxyl radical scavenging capacity. To comprehensively study different aspects of antioxidants, validated and specific assays are needed in addition to these two commonly accepted assays.
Article
To study the chemical constituents in seeds of Helicia nilagirica. The ethanol extract was seperated by petroleum ether, dichloromethane, n-butanol in sequence, then isolated by silica gel column chromatography. The structures were identified and elucidated by physicochemical properties and spectral analysis. Five compounds were isolated from the dichloromethane and n-butanol extracts, identified as p-hydroxybenzaldehyde (1), p-hydroxybenzoic acid (2), gallic acid (3), helicide (4), 4-formylpymyl-O-beta-D-glucopyranoside (5). All the compounds except IV were isolated from the plant for the first time. The compounds I, II and III were isolated from the genus Helicia for the first time.
Article
CYP 1B1 is involved in metabolizing both polycyclic aromatic hydrocarbons and estradiol to potentially carcinogenic intermediates, and it is also over-expressed in human cancer cells. In order to investigate whether flavonoids could specifically inhibit CYP 1B1, seven flavonoids in St. John's wort and apigenin were screened for their inhibition of recombinant human CYP 1B1 and CYP 1A1. While seven flavonoids (myricetin, apigenin, kaempferol, quercetin, amentoflavone, quercitrin and rutin) were slightly more selective for CYP 1B1 EROD inhibition (K(i)s 0.06-5.96 microM) compared to CYP 1A1 (K(i)s 0.20-1.6 microM) the difference in K(i)s for the P450s were not significantly different. Rutin did not inhibit CYP 1A1 at concentrations up to 10 microM. Kinetic analyses determined that apigenin and amentoflavone were competitive inhibitors of CYP 1B1, while quercetin showed mixed type inhibition. To characterize the inhibition potential of these flavonoids, five were studied further for their ability to inhibit TCDD-induced EROD activity in 22Rv1 human prostate cancer cells. 22Rv1 cells express constitutive and TCDD-inducible CYP 1A1 and CYP 1B1 mRNA. In the cells, the IC(50)s were similar to those measured for the recombinant CYP 1A1 except for amentoflavone. Quercetin (IC(50): 4.1 microM), kaempferol (3.8 microM), myricetin (3.0 microM) and apigenin (3.1 microM) caused significant inhibition of EROD activity whereas amentoflavone did not cause inhibition. Depending on their bioavailability, flavonoids that can selectively inhibit CYP1 enzymes may be useful as chemoprotective agents in prostate cancer prevention.
Article
A new ursane-type triterpenoid, weigelic acid (1), and seven known compounds, ursolic acid (2), ilekudinol A (3), corosolic acid (4), ilekudinol B (5), esculentic acid (6), pomolic acid (7), and asiatic acid (8) were isolated from the leaf and stem of Weigela subsessilis. The structure of the new triterpenoid was established as 1beta,2alpha,3alpha,23-tetrahydroxyurs-12-en-28-oic acid on the basis of spectroscopic analyses. In addition, the isolated compounds were evaluated for their anti-complement activity against the classical pathway of the complement system. Of these, compounds 1-2 and 4-8 exhibited anti-complement activity with IC50 values of 152, 90, 130, 51, 56, 4, and 163 microM, respectively, whereas 3 was inactive. This shows that a carboxylic group of ursane-type triterpenoids seems to play an important role in inhibiting the hemolytic activity of human serum against erythrocytes.
Article
The Rubus species has been used in folk medicine to treat several ailments, including infectious and dolorous diseases. In this work we evaluate the phytochemical and analgesic activity of hydroalcoholic extract (HE), some fractions (hexane, dichloromethane, ethyl acetate and butanolic), as well as a pure compound denoted as 28-methoxytormentic acid (1) obtained from aerial parts of R. rosaefolius. The compounds were isolated and identified by chromatographic and spectroscopic analysis. The antinociceptive action was evaluated by two well know models of pain in mice: writhing and formalin induced-pain. The results showed that the HE, fractions and compound (1), exhibits potent and dose-related analgesic activity when evaluated in both models of pain. Compound (1), which seems to be the main active principle, showed promising analgesic effects, being several times more potent than aspirin and paracetamol, two well-known analgesic and antiinflammatory drugs used as reference. In the writhing test, it showed an ID(50) of 5.10 (3.64-7.14) mg kg(-1) and maximum inhibition (MI) of 64.22%. When analyzed by formalin induced-pain test, this compound showed ID(50) values of 9.98 (8.08-12.31) and 6.31 (5.07-7.98) mg kg(-1) and MI of 59.37 and 90.37% for the first and second phases, respectively. The results justify, at least partially the popular use of this plant for the treatment of dolorous processes, suggesting that 1 is one of the active principles of this plant.
Article
An overwhelming body of research has now firmly established that the dietary intake of berry fruits has a positive and profound impact on human health, performance, and disease. Berry fruits, which are commercially cultivated and commonly consumed in fresh and processed forms in North America, include blackberry ( Rubus spp.), black raspberry ( Rubus occidentalis), blueberry ( Vaccinium corymbosum), cranberry (i.e., the American cranberry, Vaccinium macrocarpon, distinct from the European cranberry, V. oxycoccus), red raspberry ( Rubus idaeus) and strawberry ( Fragaria x ananassa). Other berry fruits, which are lesser known but consumed in the traditional diets of North American tribal communities, include chokecherry ( Prunus virginiana), highbush cranberry ( Viburnum trilobum), serviceberry ( Amelanchier alnifolia), and silver buffaloberry ( Shepherdia argentea). In addition, berry fruits such as arctic bramble ( Rubus articus), bilberries ( Vaccinuim myrtillus; also known as bog whortleberries), black currant ( Ribes nigrum), boysenberries ( Rubus spp.), cloudberries ( Rubus chamaemorus), crowberries ( Empetrum nigrum, E. hermaphroditum), elderberries ( Sambucus spp.), gooseberry ( Ribes uva-crispa), lingonberries ( Vaccinium vitis-idaea), loganberry ( Rubus loganobaccus), marionberries ( Rubus spp.), Rowan berries ( Sorbus spp.), and sea buckthorn ( Hippophae rhamnoides), are also popularly consumed in other parts of the world. Recently, there has also been a surge in the consumption of exotic "berry-type" fruits such as the pomegranate ( Punica granatum), goji berries ( Lycium barbarum; also known as wolfberry), mangosteen ( Garcinia mangostana), the Brazilian açaí berry ( Euterpe oleraceae), and the Chilean maqui berry ( Aristotelia chilensis). Given the wide consumption of berry fruits and their potential impact on human health and disease, conferences and symposia that target the latest scientific research (and, of equal importance, the dissemination of this information to the general public), on the chemistry and biological and physiological functions of these "superfoods" are necessary.
Article
Quercetin, a member of the flavonoids family, is one of the most prominent dietary antioxidants. It is ubiquitously present in foods including vegetables, fruit, tea and wine as well as countless food supplements and is claimed to exert beneficial health effects. This includes protection against various diseases such as osteoporosis, certain forms of cancer, pulmonary and cardiovascular diseases but also against aging. Especially the ability of quercetin to scavenge highly reactive species such as peroxynitrite and the hydroxyl radical is suggested to be involved in these possible beneficial health effects. Consequently, numerous studies have been performed to gather scientific evidence for these beneficial health claims as well as data regarding the exact mechanism of action and possible toxicological aspects of this flavonoid. The purpose of this review is to evaluate these studies in order to elucidate the possible health-beneficial effects of the antioxidant quercetin. Firstly, the definitions as well as the most important aspects regarding free radicals, antioxidants and oxidative stress will be discussed as background information. Subsequently, the mechanism by which quercetin may operate as an antioxidant (tested in vitro) as well as the potential use of this antioxidant as a nutraceutical (tested both ex vivo and in vivo) will be discussed.
Oceans and human health: Risks and remedies from the sea
  • K B Tierney
  • C J Kennedy
Tierney, K. B., & Kennedy, C. J. (2008). Background toxicology. In P. J. Walsh, S. L. Smith, L. E. Fleming, H. M. Solo-Gabriele, & W. H. Gerwick (Eds.), Oceans and human health: Risks and remedies from the sea (pp. 101-105). New York: Elsevier.