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Anti-histamine release and anti-inflammatory activities of aqueous extracts of citrus fruits peels
Abstract
In this study, aqueous extracts of peels of best known citrus fruits namely grapefruit (Citrus paradisi), lemon (C. limon), lime (C. aurantifolia) and orange (C. sinensis) were used. Depending on polyphenols content, the extracts were graded as orange > lemon > lime > grapefruit. Effects of the extracts on the release of histamine from rat peritoneal exudate cells (PECs) was measured to know anti-allergic activity. All extracts inhibited the release of histamine from rat PECs induced by the calcium ionophore A23187. Heating of the extracts at 100 °C for 10 min enhanced inhibition of histamine release. Effect of the oral administration of aqueous extract of grapefruit peel on the effusion of Chicago sky blue dye into the intraperitoneal cavity of mice was measured to know the anti-inflammatory activity. The extract potentially suppressed inflammation in the mice cavity as like indometacin, an anti-inflammatory drug. Therefore, the extracts of citrus peels are useful for developing anti-allergic and anti-inflammatory foods and supplements.
... Ekstrakty z owoców C. limon przyspieszają gojenie ran cukrzycowych, działają przeciwalergicznie, hepatoregenerująco, zwiększają pamięć krótkoterminową, obniżają ciśnienie krwi, mają korzystny wpływ na układ kostny [6,[24][25][26][27][28]. Najnowsze badania dowodzą aktywności przeciwnowotworowej na komórki raka piersi [29,30]. ...
... Hamowanie aktywności czynnika NF-kB, syntazy tlenku azotu(II) (iNOS), cyklooksygenazy indukowanej (COX-2) (hesperydyna, hesperytyna) [33] Działanie przeciwalergiczne Hamowanie wydzielania histaminy w komórkach otrzewnej szczurów [6,25] Działanie hepatoregenerujące Normalizacja stężenia aminotransferazy alaninowej (ALAT), fosfatazy alkalicznej (ALP) i bilirubiny Redukcja dialdehydu malonowego (MDA), peroksydacji lipidów, dysmutazy ponadtlenkowej (SOD) i katalazy [26] Zaburzenia miesiączkowania Indukcja okresu przy nieregularnych cyklach miesiączkowych [31] Przeciwdziałanie cukrzycy i leczenie objawów ...
... Pobudzanie apoptozy komórek raka jelita grubego [38] Ponadto ekstrakty z owocni C. limon posiadają również udowodnione naukowo działanie przyspieszające regenerację ran cukrzycowych, a olejek eteryczny działanie przeciwzapalne, przeciwalergiczne, a także odchudzające [24,25,35,39]. ...
The paper presents a brief botanical characteristic of citrus species, which are a source of citrus fruits with valuable culinary, pharmaceutical and cosmetic properties. The history of the dissemination of the main representatives of the genus Citrus-Citrus limon (lemon) in the world, has been recalled. The information about chemical composition and biological activities of the main raw materials extracted from C. limon (fruit extract, essential oil), which are the basis for their therapeutic applications, was presented. Particular attention has been paid to the possible cosmetic applications, confirmed by scientific researches. The information was supplemented with a list of cosmetic ingredients based on C. limon (acc. to CosIng database), examples of patents, as well as numerous cosmetics formulations. The potential phototoxicity of the raw materials from C. limon was notified. Furthermore, the potential, applicable significance of biotechnological studies on C. limon has been stressed. W pracy przedstawiono krótką charakterystykę botaniczną gatunków rodzaju Citrus będących źródłem owoców cytrusowych o cennych walorach spożywczych, farmaceutycznych i kosmetycznych. Przypomniano historię rozpowszechnienia jednego z głównych przedstawicieli rodzaju Citrus-Citrus limon (cytryna zwyczajna) na świecie. Przedstawiono informacje dotyczące składu chemicznego oraz aktywności biologicznej głównych surowców pozyskiwanych z C. limon (ekstrakt z owoców, olejek eteryczny), które stanowią podstawy do zastosowań terapeutycznych. Szczególną uwagę zwrócono na możliwe aplikacje kosmetyczne potwierdzone badaniami naukowymi. Informacje wzbogacono o listę surowców kosmetycznych bazujących na C. limon (wg. bazy CosIng), przykłady patentów i licznych kosmetyków. Zasygnalizowano możliwą fototoksyczność surowców pozyskiwanych z C. limon. Ponadto zwrócono uwagę na potencjalne aplikacyjne znaczenie badań biotechnologicznych dotyczących C. limon. Słowa kluczowe: skład chemiczny, aktywność biologiczna, zastosowanie kosmetyczne, potencjalna fototoksyczność, badania biotechnologiczne, ekstrakty z owoców, olejek eteryczny
... In addition, using by-products for functional material development is the best choice for a sustainable economy [3,20,21]. Like citrus peel (Citri Reticulatae Pericarpium), lemon peel is rich in various polyphenols, flavonoids, terpenes, limonoids, lower molecular weight phenolic acids, and organic acids, such as eriocitrin, hesperidin, limonene, and malic acid [22][23][24]. A previous study found that the sensory properties of Eureka black lemon slices manufactured at high temperature and humidity (HHL) were similar to those of commercial Chenpi and highly marketable among consumers. ...
... FL peel contains various physiologically active components, such as flavanone glycosides and lower molecular weight phenolic acids, which benefit human physiological health [21,24,43]. Previous studies have highlighted that citrus fruits have α-glucosidase inhibitory activity, which is mainly found in the villi of the small intestine and can decompose macromolecular sugars such as polysaccharides and disaccharides into glucose, thereby increasing postprandial blood glucose concentration [10,13,56]. ...
This study evaluated the antioxidant and anti-glycemic properties of black lemon Chenpi (BLC) (Citrus limon (L.) Burm. f. cv. Eureka), processed using three thermal browning models—hot-air drying (HAL), high temperature and humidity, and steam-drying cycle (SCL)—and compared them to fresh lemon peel and commercial Chenpi. The moisture-assisted aging technology (MAAT) is an environmentally friendly process for inducing browning reactions in the lemon peel, enhancing its functional properties. Our results demonstrated significant increases in sucrose, total flavonoid content, and antioxidant capacities (2,2-diphenylpicrylhydrazyl: 12.86 Trolox/g dry weight; ferric reducing antioxidant power: 14.92 mg Trolox/g dry weight) with the MAAT-HAL model. The MAAT-SCL model significantly improved the browning degree, fructose, total polyphenol content, narirutin, and 5-hydroxymethylfurfural synthesis (p < 0.05). Additionally, aged lemon peel exhibited potential α-glucosidase inhibitory activity (28.28%), suggesting its role in blood sugar regulation after meals. The multivariate analysis (principal component and heatmap analyses) indicated that BLC processed using the MAAT-SCL model exhibited similarities to commercial Chenpi, indicating its potential for functional food development. Our results indicate that MAAT-SCL can enhance the economic value of lemon by-products, offering a sustainable and functional alternative to traditional Chenpi.
... Anti-allergic activity -Inhibition of histamine secretion in peritoneal cells of rats. [1,59] Hepatoregenerative activity -Normalization of alanine aminotransferase (ALAT), alkaline phosphatase (ALP) and bilirubin; -Reduction in malonic dialdehyde (MDA), lipid peroxidation, superoxide dismutase (SOD) and catalase. ...
... Furthermore, C. limon pericarp extracts, too, exhibit scientifically proven activity that helps to accelerate the regeneration of diabetic wounds. In addition, the essential oil derived from C. limon pericarp has shown anti-inflammatory, anti-allergic and slimming properties [49,59,60,62]. Table 9. Biological activity of C. limon fruit extracts, essential oil and its ingredients compounds significant from the cosmetics point of view, confirmed by scientific research. ...
This review presents important botanical, chemical and pharmacological characteristics of Citrus limon (lemon)—a species with valuable pharmaceutical, cosmetic and culinary (healthy food) properties. A short description of the genus Citrus is followed by information on the chemical composition, metabolomic studies and biological activities of the main raw materials obtained from C. limon (fruit extract, juice, essential oil). The valuable biological activity of C. limon is determined by its high content of phenolic compounds, mainly flavonoids (e.g., diosmin, hesperidin, limocitrin) and phenolic acids (e.g., ferulic, synapic, p-hydroxybenzoic acids). The essential oil is rich in bioactive monoterpenoids such as D-limonene, β-pinene, γ-terpinene. Recently scientifically proven therapeutic activities of C. limon include anti-inflammatory, antimicrobial, anticancer and antiparasitic activities. The review pays particular attention, with references to published scientific research, to the use of C. limon in the food industry and cosmetology. It also addresses the safety of use and potential phototoxicity of the raw materials. Lastly, the review emphasizes the significance of biotechnological studies on C. limon.
... Islam et al. (2019a) reported that (+)-catechin inhibits histamine, bradykinin, and serotonin release and opens the ATP-sensitive K + channel resulting in antinociceptive effects. Various studies on fruits and medicinal plants showed analgesic, anti-inflammatory, and anti-histamine activities (Hossain et al., 2008(Hossain et al., , 2009Mubassara et al., 2011;Tsujiyama et al., 2013;Hossain et al., 2017). presented as mean ± SD (bar). ...
Carbohydrate and carbohydrate-based therapeutics are used in treating various diseases. In this study, carbohydrate-enriched (Cah) and ethanol-methanol (1:1; Eth-Met) extracts were prepared from the mangrove fruits of Aegiceras corniculatum in the Sundarbans composed of high content of carbohydrate. The amounts of total carbohydrate, protein, and lipid in Cah extract were 70.4, 7.8, and 2.2% whereas those for Eth-Met extract were 43.9, 8.1, and 2%, respectively. Cah extract had the higher antioxidant activity as it showed significantly (P < 0.05) high total polyphenol content (73.5 mg gallic acid equivalent (GAE)/g extract), 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging (at 50 μg extract/mL 85.2%), and total antioxidant capacity (155.5 mg GAE or 120.4 mg ascorbic acid equivalent (AAE)/g extract) than Eth-Met extract. Eth-Met extract showed significantly higher analgesic activity than Cah extract. When mice were orally treated with 250 mg Eth-Met extract/kg body weight showed acetic acid-induced writhing inhibition of 43.1% and needed 14.8 s for response time on a hot plate (55°C). Both Cah and Eth-Met extracts exhibited strong anthelmintic activity with similar concentrations for death time 50 (CDT50) of 11.5 and 10.6 mg/mL respectively for the parasite, Paramphistomum cervi. Therefore, Cah extract can be exploited as a potential source of functional carbohydrates and polyphenols with high antioxidant and anthelmintic activities.
... Bioethanol is a clean potential biofuel [177], and grapefruit peel represents a lucrative biomass for bioethanol production as it comprises cellulose, pectin, and hemicellulose that can be hydrolyzed by enzymes to monomer sugars, for bioethanol production [178]. In one study, glucose, 1. Inhibited the release of histamine from rat peritoneal exudate cells, and also suppressed the effusion of Chicago sky blue through capillary vessels caused by the intraperitoneal injection of acetic acid in mice 2. Heating of the extracts increased both the inhibitory activity and the suppression 3. Extracts have beneficial activities such as antioxidative, anti-hydrogen peroxide, and anti-allergic effects and may serve as sources of new supplements [157] Current Food Science and Technology Reports can be achieved in fixed-bed columns, working in continuous mode [171] fructose, galactose, arabinose, xylose, and galacturonic acid (GA) were produced using the enzymes pectinase, cellulase, and beta-glucosidase, with a pH range of 3.8-4.8 found to be optimal for sugar yields from peel hydrolysis [179]. ...
This study aims to communicate updated information on the recent innovations in grapefruit byproduct valorization.
Grapefruit is an important fruit of the citrus genus which has commercial importance and its processing generates waste in bulk, mainly in the form of peels, seeds, and pomace, which only leads to a strenuous waste stream that ends up in landfills causing environmental issues if overlooked. However, grapefruit byproducts are rich in high-value compounds including dietary fiber, polyphenols, pectin, and essential oil, which therefore could be valorized for different applications in the food sector and other realms as well. In line with the United Nations Sustainable Development Goals (UN-SDGs) to ensure sustainable consumption and production patterns, the valorization of these byproducts in the most efficient and environment-friendly manner is of great importance for the future.
The valorization of grapefruit byproducts can be addressed through environmentally friendly extraction procedures that allow recovery of target high-value compounds and open new vistas for their applications. Overall, this work describes an updated tapestry of reports about the characteristics and compositions of grapefruit byproducts. In parallel, it offers an updated vision of high-value compounds and the various extraction techniques used for their extraction have been discussed. Comprehensively, the current review summarizes the latest advancements in the application of high-value compounds from grapefruit waste in the numerous areas of the food, pharma, and cosmetics realm, along with the utilization for development of environmentally sustainable materials, fostering a sustainable economy.
... Polyphenols such as (+)-catechin showed an antinociceptive effect by opening the ATP-sensitive K + channel and inhibiting the release of histamine, serotonin, and bradykinin (Islam et al. 2019a). Moreover, different studies showed the anti-histaminic and/or anti-inflammatory activities of citrus fruit peels, and various edible fruits (Hossain et al. 2008, Mubassara et al. 2011, Tsujiyama et al. 2013). The parasite, Paramphistomum cervi was used to examine the anthelmintic activity of the fruit extracts. ...
The analgesic and anthelmintic activities of the common fruits in the Sundarbans forest, Bangladesh were evaluated. Acetic acid-induced writhing test and hot plate test in mice model were demonstrated for examining the analgesic activity whereas an anthelmintic test was performed using a flatworm, Paramphistomum cervi of livestock ruminants. Among the fruits, Ceriops decandra showed the strongest analgesic activity through inhibiting acetic acid-induced writhing (45%) and increasing response time (16.8 sec) on a hot plate in mice at 250 mg extract/kg body weight (b.w.). Diclofenac sodium (25 mg/kg b.w.), a positive control, demonstrated writhing inhibition of 51.3% whereas morphine (10 mg/kg b.w.), a wellknown centrally active analgesic drug, increased response time of 18.2 sec. The fruits showed inhibition of acetic acid-induced writhing in mice with strong correlations to both the total polyphenols (r2 = 0.85) and the total flavonoids (r2 = 0.81) contents. Similar results were also observed for an increase of response time in mice on hot plate test. Therefore, both the peripheral and the central analgesic activities of the fruits were profoundly related to their total contents of polyphenols as well as flavonoids. Extract of Aegiceras corniculatum fruit displayed the strongest anthelmintic activity with the lowest CDT50 (concentration for death time 50) of 0.69 mg extract/ml whereas albendazole, a positive control, had CDT50 of 5.60 mg/ml for the parasite. The anthelmintic activity of the fruits was not dependent on their contents of polyphenols (r2 = 0.30) or flavonoids. The chromatograms of HPLC-DAD analysis detected caffeic acid, (+)-catechin hydrate, p-coumaric acid, (-)-epicatechin, rutin hydrate, and syringic acid in C. decandra fruit extract and quantified as 10.6, 598.4, 1.5, 28.5, 2 and 1.3 mg/100 g extract, respectively. Results revealed that C. decandra and A. corniculatum fruits are the potentials to treat pain and helminthiasis, respectively. Bangladesh J. Bot. 52(1): 79-86, 2023 (March)
... (Murali and Saravanan, 2012). In addition, studies have shown that the essential oil extracted from lemon fruits has a significant anti-inflammatory effect (Amorim et al. 2016), an anti-allergic effect (Tsujiyama et al. 2013) and slimming properties by reducing body weight and body fat mass (Kim et al. 2015). ...
Lemon trees (Citrus lemon L.) are among the trees scattered in Southeast Asia, especially Malaysia, The importance of lemons has increased in recent times, especially after the spread of the Covid-19 epidemic around the world, as lemon juice rich in vitamin C is fortified for the immunity of the human body. Also, it is an important source of Flavonoids, known as antioxidants, which remove free radicals that damage tissue cells within the body. Bio-fertilizers are products containing multiple genera of microorganisms in large numbers and beneficial to both plants and soil in an integrated manner. In addition bio-fertilizers have proved that increase the nutrient content inside plants, whether in leaves or fruits,which is reflected in the quantity and quality of fruits and also balance the ratio between plant nutrients in the soil. This review discussed the nutritional and health benefits of lemon and the importance of bio-fertilizer on fruit growth, yield and fruit quality of lemon.
... However, involvement of autonomic receptors in the anti-nociceptive and anti-inflammatory effects of honey has also been reported (27). Antihistaminic and/or anti-inflammatory activities of citrus fruit peels and various edible fruits have also been reported in various studies (28,29). ...
This study evaluated the antidiarrheal, analgesic, and anthelmintic activities of honey samples from the Sundarbans mangrove forest of Bangladesh. Composite raw honey (RH), and its diethyl ether (DEH), ethanol (ETH), methanol (MEH), and distilled water (DWH) fractions were investigated. RH and its fractions strongly inhibited castor oil-induced diarrheal episodes in mice at a concentration of 250 mg/kg body weight (b.w.) (P<0.05). At this concentration, RH, DEH, ETH, MEH, and DWH showed inhibitory activity on diarrheal episodes at 43.8, 47.4, 29.8, 12.3, and 38.5%, respectively, whereas for the inhibitory activity for the positive control (PC, 3 mg loperamide/kg b.w.) was 47.4%. Similarly, DEH (250 mg/kg b.w.) showed strongest inhibition (63.5%) of acetic acid-induced writhing in mice, followed by RH (55.7%), ETH (46.2%), MEH (37.6%), and DWH (32.9%). In a hot plate test, mice treated with DEH at a concentration 250 mg/kg b.w. showed the greatest increase in response time, followed by treatment with RH. RH was further used in an anthelmintic test, where it showed a strong dose-dependent reduction in both the paralysis time and the time until death of the parasite, Paramphistomum cervi. Honeys in the Sundarbans could therefore be of great use as nutraceuticals.
... "Verdello", or summer lemon is particularly rich in eriocitrin (Amenta et al. 2015). Recent evidence has revealed plant-derived polyphenols as a promising tool to prevent allergy (Tsujiyama et al. 2013;Chirumbolo 2014). ...
Citrus fruits are rich sources of bioactive compounds and their consumption is associated to health-promoting effects. Citrus processing wastes contain bioflavonoids and other high added value compounds. The aim of this study was to evaluate the antiallergic properties of a new phytoextract obtained by citrus wastes and peels. Blood orange and lemon processing wastes were used to produce a Red orange and Lemon Extract (RLE). Blood samples from 30 allergic donors were collected and used to evaluate the basophil activation (CD203c) and degranulation (CD63) by stimulation trough allergen with and without the RLE. Reduced basophil expression of CD203c and CD63 were observed in RLE + Allergen treated samples, with −20.21% of CD203c expression (p < 0.0001) and −54.11% of CD63 expression (p < 0.0001), compared to Allergen treated samples. The RLE evidenced a good antiallergic activity, mainly acting on basophils degranulation, and therefore reducing the key event of pro-inflammatory mediators release after allergic stimuli.
... Phenolicenriched extracts of copao fruits effectively inhibited proinflammatory enzymes-LOX and COX-2, and thus showed anti-inflammatory activity (23). The antihistaminic and/ or anti-inflammatory activities of citrus fruit peels, and various edible fruits were also reported in different studies (24,25). ...
Fruits of Sonneratia apetala (Buch.-Ham.), (English: mangrove apple, Bengali: keora) both seeds and pericarps,
are largely consumed as food besides their enormous medicinal application. The fruit seeds have high content of nutrients
and bioactive components. The seeds powder of S. apetala was successively fractionated using n-hexane, diethyl ether,
chloroform, ethyl acetate, and methanol. The fractions were used to evaluate antibacterial, anti-diarrhoeal, analgesic, and
cytotoxic activities. Methanol fraction of seeds (MeS) stronly inhibited Escherichia coli strains, Salmonella Paratyphi A, Salmonella
Typhi, Shigella dysenteriae, and Staphylococcus aureus except Vibrio cholerae at 500 μg/disc. All the fractions strongly inhibited
castor oil induced diarrhoeal episodes and onset time in mice at 500 mg extract/kg body weight (P<0.001). At the
same concentration, MeS had the strongest inhibitory activity on diarrhoeal episodes, whereas the n-hexane fraction (HS)
significantly (P<0.05) prolonged diarrhoeal onset time as compared to positive control. Similarly, HS (P<0.005) inhibited
acetic acid induced writhing in mice at 500 mg extract/kg, more than any other fraction. HS and diethyl ether fractions of
seed strongly increased reaction time of mice in hot plate test at 500 mg extract/kg. All the fractions showed strong cytotoxic
effects in brine shrimp lethality tests. Gas chromatography-mass spectrometry analysis of HS led to the identification
of 23 compounds. Linoleic acid (29.9%), palmitic acid (23.2%), ascorbyl palmitate (21.2%), and stearic acid (10.5%)
were the major compounds in HS. These results suggest that seeds of S. apetala could be of great use as nutraceuticals.
... aurantifolia, L.), lemon (C. limon, L.) inhibited the release of histamine from rat peritoneal exudate cells (PECs) induced by the calcium ionophore A23187 [164]. Citrus natsudaidai (natsumikan) is a typical citrus fruit containing several anti-oxidative nutrients which are found in higher concentration in the peel than in the pulp of the fruit. ...
... These typical symptoms and functional abnormalities are due to lung inflammation and airway remodeling (Noble et al., 2012). Asthma is a form of immune dysfunction (Tsujiyama et al., 2013). Asthma is a multi-cellular process involving helper T cells, eosinophils, mast cells and neutrophils (Wardlaw et al., 2000(Wardlaw et al., , 2002Brightling et al., 2003;Humbles et al., 2004;Holgate, 2009). ...
Ethnopharmacological relevance:
PM014 is a modified form of the Chung-Sang-Bo-Ha-Tang (CSBHT) herbal formula that has been used to treat chronic pulmonary diseases in Korea for centuries. Previously, we developed a formulation of PM014 based on a series of in vitro and in vivo screening efforts that comprises seven herbal extracts. The PM014 formula includes the root of Rehmannia glutinosa, the cortex of Paeonia suffruticosa, the fruit of Schizandra chinensis, the root of Asparagus cochinchinensis, seeds of Prunus armeniaca, the root of Scutellaria baicalensis and the root of Stemona sessilifolia. Asthma is a chronic inflammatory disease of the lungs that is characterized by wheezing, bronchial contraction, and chest tightness. In addition, the airway becomes hypersensitive and narrows through an inflammatory reaction mediated by Th2 cells. The present study was conducted to evaluate the ability of PM014 to prevent allergic airway inflammation and to attenuate airway responses in a cockroach allergen-induced mouse model.
Materials and methods:
Mice sensitized to and challenged with cockroach allergen were treated with oral administration of PM014. Airway resistance was determined by whole body plethysmography. In addition, Th2 cytokines and immune cell profiles of bronchoalveolar lavage (BAL) fluid and inflammatory mediators in serum were analyzed by ELISA. A series of histological examinations were also conducted to demonstrate the effects of PM014 on airway remodeling, goblet cell hyperplasia and inflammatory responses in the lung.
Results:
PM014 significantly inhibited the number of total cells, eosinophils, neutrophils, macrophages and lymphocytes in the BAL fluid of mice that were challenged with cockroach allergen. In addition, PM014 reduced the levels of Th2 cytokines (IL-4, IL-5 and IL-13) in the BAL fluid and inflammatory mediators such as IgE in the serum, as measured by enzyme-linked immunosorbent assay (ELISA). Histopathological analysis also showed that PM014 substantially inhibited eosinophil infiltration into the airway, goblet cell hyperplasia and smooth muscle hypertrophy.
Conclusions:
In this study, our results indicate that PM014 has significant effects on allergic airway inflammation upon exposure to cockroach allergen in a mouse model. According to these outcomes, PM014 may have therapeutic potential as a treatment for allergic asthma.
... Many types of cells play important roles in the development of bronchial asthma, including T lymphocytes, eosinophils, macrophages, neutrophils, mast cells and epithelial cells [3][4][5]. Th2 cells play a central role and control the allergic response through the production of cytokines such as interleukin (IL)-4, IL-5, and IL-13 [6][7][8]. IL-4 plays an important role in eosinophil infiltration into lung tissues, B cell maturation, and IgE synthesis. ...
Chronic allergic asthma is characterized by Th2-typed inflammation, and contributes to airway remodeling and the deterioration of lung function. Viticis Fructus (VF) has long been used in China and Korea as a traditional herbal remedy for treating various inflammatory diseases. Previously, we have isolated a novel phytochemical, pyranopyran-1, 8-dione (PPY), from VF. This study was conducted to evaluate the ability of PPY to prevent airway inflammation and to attenuate airway responses in a cockroach allergen-induced asthma model in mice. The mice sensitized to and challenged with cockroach allergen were treated with oral administration of PPY. The infiltration of total cells, eosinophils and lymphocytes into the BAL fluid was significantly inhibited in cockroach allergen-induced asthma mice treated with PPY (1, 2, or 10 mg/kg). Th2 cytokines and chemokine, such as IL-4, IL-5, IL-13 and eotaxin in BAL fluid were also reduced to normal levels following treatment with PPY. In addition, the levels of IgE were also markedly suppressed after PPY treatment. Histopathological examination demonstrated that PPY substantially inhibited eosinophil infiltration into the airway, goblet cell hyperplasia and smooth muscle hypertrophy. Taken together, these results demonstrate that PPY possesses a potent efficacy on controlling allergic asthma response such as airway inflammation and remodeling.
... Among the antidiabetic plants used in this study, F. racemosa (bark), S. chirata and S. cumini were very rich in total polyphenol, flavonoids and anthocyanins contents. In previous studies, we reported polyphenols content of various edible fruits (Hossain et al. 2008Tsujiyama et al. 2012) and plants (Hossain et al. 2009b), & mangroves (Hossain et al. 2009a;Mubassara et al. 2011). Polyphenols content (294 mg GAE/g extract) of the seeds of S. cumini was near to that of Phyllanthus emblica (Emblic Myrobalan, 339 mg GAE/g extract) (Hossain et al. 2008) and seeds of Sonneratia apetala (300.1 mg GAE/g extract) ). ...
Various literatures recorded approximately 60 medicinal plants in Bangladesh that have antidiabetic properties. Of these medicinal plants, only 14–16 are found in traditional herbal markets and they are being randomly used to treat diabetes. Since diabetes mellitus increases reactive free radicals along with various complications in the body, antidiabetic plants that can potentially neutralize free radicals, may be of central interest to manage the disease. Present study compares functional bioactive components such as total phenolics, flavonoids, anthocyanins contents and antioxidant potential of methanol extracts of antidiabetic medicinal plants that are common in traditional herbal markets. Among the 14 extracts, Syzygium cumini was very rich in total polyphenol content (294 mg gallic acid equivalent, GAE/g) followed by Swertia chirata (183 mg GAE/g) and Ficus racemosa (bark) (154 mg GAE/g). These three extracts also had elevated amount of flavonoids and anthocyanins. S. cumini showed very high DPPH and NO free radical scavenging activities with IC50 of 6.25 and 48.61 μg/mL respectively followed by S. chirata and F. racemosa (bark). S. cumini also showed very high reducing power and total antioxidant capacity followed by S. chirata and F. racemosa (bark). In addition, the study revealed strong correlation between phenolics and reducing power (r = 0.94). Hence, among the 14 extracts, S. cumini, S. chirata and F. racemosa (bark) are potential sources of antioxidant agents. Therefore, these three medicinal plants have diverse beneficial effects on physiological health and they might be the choice of plants to treat diabetes.
... aurantifolia, L.), lemon (C. limon, L.) inhibited the release of histamine from rat peritoneal exudate cells (PECs) induced by the calcium ionophore A23187 [164]. Citrus natsudaidai (natsumikan) is a typical citrus fruit containing several anti-oxidative nutrients which are found in higher concentration in the peel than in the pulp of the fruit. ...
Recent evidence has brought to the spotlight plant-derived polyphenols as a promising tool to prevent allergy. The worldwide increase of allergic disease, probably relying on many factors including immune response to stressors and its loss in complexity, environmental pressure by pollutants and chemical allergens, changes in lifestyle and lifespan, failure of conventional treatments to prevent and treat allergy, has strongly suggested people to refer to healthy promising nature-derived compounds, most of which contained in fruits and vegetables, e.g. in daily diet. Phenolic acids and polyphenols, such as flavonoids, are the best studied natural substances known to possess an anti-inflammatory and anti-allergic potential. Used as nutraceuticals, these compounds are thought to dampen the onset of allergic inflammation, by acting on several immune cells, but concerns still remain about their real employment by the organism who assumes polyphenols through diet, because of their bioavailability, gut transformation and pharmacokinetics. Other issues deals with the wide panoply of actions played by these compounds within cells, which has hampered a clear comprehension of their action on cell molecular signaling and function. In this review, special emphasis is placed on the effects of dietary polyphenols on allergy prevention, the possible mechanism of action of polyphenols-containing food and future perspectives for pharmacology design.
In the present work, phytoconstituents from Citrus limon are computationally tested against SARS‐CoV‐2 target protein such as Mpro ‐ (5R82.pdb), Spike ‐ (6YZ5.pdb) &RdRp ‐ (7BTF.pdb) for COVID‐19. Docking was done by glide model, QikProp was performed by in silico ADMET screening & Prime MM‐GB/SA modules were used to define binding energy. When compared with approved COVID‐19 drugs such as Remdesivir, Ritonavir, Lopinavir, and Hydroxychloroquine, plant‐based constituents such as Quercetin, Rutoside, Naringin, Eriocitrin, and Hesperidin. bind with significant G‐scores to the active SARS‐CoV‐2 place. The constituents Rutoside and Eriocitrin were studied in each MD simulation in 100 ns against 3 proteins 5R82.pdb, 6YZ5.pdb and 7BTF.pdb.We performed an assay with significant natural compounds from contacts and in silico results (Rutin, Eriocitrin, Naringin, Hesperidin) using 3CL protease assay kit (B.11529 Omicron variant). This kit contained 3CL inhibitor GC376 as Control. The IC50 value of the test compound was found to be Rutin −17.50 μM, Eriocitrin−37.91 μM, Naringin−39.58 μM, Hesperidine−140.20 μM, the standard inhibitory concentration of GC376 was 38.64 μM. The phytoconstituents showed important interactions with SARS‐CoV‐2 targets, and potential modifications could be beneficial for future development.
Fruits from the Citrus genus are broadly demanded for their flavor, nutritional value, and health benefits. Among the various biological activities of Citrus, antiallergic activity has been reported for some species, such as C. reticulata, C. medica, Citrus japonica, Citrus ×aurantifolia, and Citrus ×aurantium. These species have been shown to inhibit various allergic reactions, such as type I, II, and IV, in different pharmacological studies. The antiallergic compounds identified from these species include flavanone glycosides, such as naringin and hesperidin, and their aglycones (naringenin, hesperetin), which modulate the release of histamine and other inflammatory mediators from mast cells and basophils. These compounds have promising applications in preventing and treating allergic diseases, like allergic asthma, rhinitis, and atopic dermatitis. However, the cultivation and propagation of these Citrus species are limited by environmental factors, pests, and diseases. Therefore, in vitro propagation techniques have been used to enhance the production and quality of citrus. In this chapter, we will summarize the existing comprehension of the antiallergic activity and in vitro propagation techniques of these Citrus species.
Lemon-the fruit with valuable health benefits and cosmetic properties
Abstract: The fruit of lemon (Citrus limon) is a well-known plant raw material from which, on an industrial scale, it is obtained, among others, juice and essential oil. Noteworthy is the rich chemical composition of fruits, dominated by polyphenols, such as: flavonoids and phenolic acids, moreover: coumarins, amino acids, carbohydrates, vitamins and minerals, and in the essential oil, terpene compounds occur. This composition determines the outstanding, antioxidant profile of this plant raw material. In addition , the essential oil shows the valuable activities, e.g. aromatherapeutic, bactericidal and anti-cancer. The article presents information on the origin of lemon, its chemical composition, medicinal properties and importance in the diet. Especially the cosmetic applications.
Various foodstuffs were screened for the ability to prevent mast cell degranulation using a rat basophilic leukaemia cell line (RBL-2H3 cells); whey emerged as a candidate to alleviate allergic symptoms. Further exploration of the suppressive effect of whey on mast cell degranulation led to identification of β-lactoglobulin (BLG) as one of the active substances. The potential of BLG to modulate allergic responses of mast cells using the RBL-2H3 cells in vitro with the passive cutaneous anaphylaxis (PCA) reaction model mice in vivo is described. BLG was shown to suppress degranulation of RBL-2H3 cells. The molecular mechanism underlying the inhibitory effect of BLG on degranulation of RBL-2H3 cells included reduced phosphorylation of the tyrosine kinase Syk, phosphoinositide 3-kinase, and phospholipase C-γ1/2. Furthermore, oral administration of BLG tended to suppress the PCA reaction in the anti-dinitrophenol (DNP) IgE-sensitised, DNP-human serum albumin-challenged BALB/c mice, presenting a new biological functionality of BLG.
From the dried powder of bark of Excoecaria agallocha L. (Euphorbiaceae), hexane (Hex), chloroform (Chl), ethyl acetate (EtA), ethanol (Eth), and water (DW) fractions were prepared to study their polyphenol content, antioxidative and anti-histamine-release activities. DW had the highest total polyphenol content, 348 mg gallic acid equivalent (GAE)/g followed by Eth (160.5 mg GAE/g). Using DPPH free radical scavenging, reducing power, measurement of total antioxidant activity and ionophore A23187-induced histamine-release assays, it was found that DW and Eth had high antioxidative and anti-histamine-release activities compare to other fractions. Thin layer chromatography (TLC) revealed that ellagic acid-like and lupeol-like compounds are found in Eth, and Chl fractions, respectively. Testing standards of lupeol and ellagic acid at 100 μg/mL, lupeol had a little inhibitory effect on histamine release (24.5%) while ellagic acid showed no effect at all. However, our results showed that bark of E. agallocha, especially DW and Eth fractions would be considered a potential source of antioxidative and anti-histamine natural products.
Alcohol extracts of six Bangladeshi medicinal plants were investigated to search out new sources of supplements or drugs beneficial to human health. All the extracts had polyphenols and antioxidative activity, and inhibited the release of both histamine and leukotriene B 4 (LTB 4) induced by the calcium ionophore A23187 from rat peritoneal exudate cells. The extract of mangrove apple (S. caseolaris) had strong anti-oxidative activity and reducing power. The extracts of white mangrove (A. officinalis), pan lota (D. uliginosa), beach hibiscus (H. tiliaceous), sapodilla (M. zapota) and mangrove apple (S. caseolaris) inhibited both histamine and LTB 4 releases significantly, suggesting them to be useful for the development of an anti-allergic supplement and drugs.
The mangrove fruit Sonneratia apetala Buch.-Ham. is extensively consumed by the people of coastal Bangladesh especially adjacent to the Sundarbans’ forest. Seeds consist of very high content of polyphenols (300 ± 8.2 mg GAE/g extract), flavonoids (30.6 ± 0.7 CE/g extract), anthocyanins (2.3 ± 0.03 μmol/g extract) and vitamin C (4.0 ± 0.08 mg/g extract). The IC50 values for DPPH and NO free radical scavenging were 4.3 and 49.4 μg/mL for seed extract and that for pericarp extract were 59.8 and 751.6 μg/mL respectively. Seed extract also showed very high reducing power (O.D. 1.14 at 50 μg/mL extract) and total antioxidant capacity (280.8 GAE or 310.24 AAE/g extract). In streptozotocin (STZ) induced type 2 diabetes rats, seed extract treated group showed serum glucose decreased from 13.75 ± 2.21 mmol/L (at 30 min) to 10.3 ± 1.75 mmol/L (at 135 min) and in the pericarp treated group from 14.36 ± 2.16 to 11.32 ± 1.74 mmol/L. The area under the glucose curve was more profoundly decreased in the seed treated group than the pericarp treated group. Susceptibility test showed that seed extract inhibited the growth of both gram-positive and gram-negative pathogenic bacteria. Therefore, fruits of S. apetala, especially its seeds are functionally rich with phenolics, flavonoids, antioxidant, antidiabetic and antibacterial compounds.
As part of the search for new sources of mental health supplements, alcohol extracts of 11 Bangladeshi medicinal fruits and plants were investigated for neuropharmacological effects in mice and on ionotropic y-aminobutyric acid receptors (GABAA receptors). The extracts of S. caseolaris, T. bellirica, S. cumini, and T. arjuna significantly potentiated the GABA-induced response of GABAA receptors expressed in Xenopus oocytes, though the extracts alone induced no response. In mice, administration of these extracts prolonged pentobarbital-induced sleeping time. Potentiation of GABAA receptor response reportedly generates anxiolytic, sedative, sleep-inducing and anesthetic activities in the human brain. Thus, these extracts may have potential regarding the development of a supplement with tranquilizing and sleep-inducing effects that is beneficial for mental health.
From the dried powder of bark of Excoecaria agallocha L. (Euphorbiaceae), hexane (Hex), chloroform (Chl), ethyl acetate (EtA), ethanol (Eth), and water (DW) fractions were prepared to study their polyphenol content, antioxidative and anti-histamine-release activities. DW had the highest total polyphenol content, 348 mg gallic acid equivalent (GAE)/g followed by Eth (160.5 mg GAE/g). Using DPPH free radical scavenging, reducing power, measurement of total antioxidant activity and ionophore A23187-induced histamine-release assays, it was found that DW and Eth had high antioxidative and anti-histamine-release activities compare to other fractions. Thin layer chromatography (TLC) revealed that ellagic acid-like and lupeol-like compounds are found in Eth, and Chl fractions, respectively. Testing standards of lupeol and ellagic acid at 100 µg/mL, lupeol had a little inhibitory effect on histamine release (24.5%) while ellagic acid showed no effect at all. However, our results showed that bark of E. agallocha, especially DW and Eth fractions would be considered a potential source of antioxidative and anti-histamine natural products.
The goal of this investigation was to evaluate the antioxidant properties of some citrus fruits. The contents of dietary fibre, total polyphenols, essential phenolics, ascorbic acid and some trace elements of lemons, oranges and grapefruits were determined and compared with their total radical-trapping antioxidative potential (TRAP). There were no significant differences in the contents of total, soluble and insoluble dietary fibre in the studied peeled fruits or their peels. The contents of total, soluble and insoluble dietary fibre in peels were significantly higher than in peeled fruits (P< 0.05 in all cases). The peeled lemons, oranges and grapefruits contain 164±10.3; 154±10.2 and 135±10.1 and their peels 190±10.6; 179±10.5 and 155±10.3 mg/100 g of total polyphenols, respectively. The content of total polyphenols in peeled lemons and their peels was significantly higher than in peeled oranges and grapefruits and their peels, respectively. The content of total polyphenols in the peels was significantly higher than in peeled fruits (P< 0.05 in all cases). The same results were obtained in the investigation of essential phenolics and ascorbic acid. The content of Fe in peeled lemons and their peels was significantly higher than in peeled oranges and grapefruits and their peels, respectively. Also the TRAP was significantly higher in peeled lemons and their peels than in peeled oranges and grapefruits and their peels, respectively. In all three fruits, the TRAP was significantly higher in peels than in peeled fruits (P< 0.05). In conclusion, lemons possess the highest antioxidant potential among the studied citrus fruits and are preferable for dietary prevention of cardiovascular and other diseases. The peels of all citrus fruits are rich in dietary fibres and phenolic compounds and suitable for industrial processing.
The anti-allergic activities of polyphenol fractions extracted from immature fruits of apple (Rosaceae, Malus sp.) were evaluated by in vitro assays. A crude apple polyphenol (CAP) fraction, which had been obtained from the juice of immature apples by reverse-phase column chromatography, was further purified by LH-20 column chromatography to obtain an apple condensed tannin (ACT) fraction consisting of linear oligomeric epicatechins from the dimer to pentadecamer. ACT strongly inhibited the release of histamine from rat basophilic leukemia (RBL-2H3) cells stimulated by the antigen-stimulation and from rat peritoneal mast cells stimulated by compound 48/80. The IC50 values for histamine release were 30 micrograms/ml and 25 micrograms/ml, respectively. ACT also inhibited hyaluronidase activity and the increase in intracellular free calcium concentration in RBL-2H3 cells stimulated with the antigen. These results suggest that ACT affected early signal transduction including the calcium influx.
The intake of citrus fruits has been suggested as a way to prevent the development of some types of human cancer. Nitric oxide (NO) is closely associated with the processes of epithelial carcinogenesis. We attempted a search for NO generation inhibitors in Citrus unshiu. The active constituent was traced by an activity-guiding separation. NO and superoxide (O2-) generation was induced by a combination of lipopolysaccharide and IFN-gamma in mouse macrophage RAW 264.7 cells, and by 12-O-tetradecanoylphorbol-13-acetate (TPA) in differentiated human promyelocyte HL-60, respectively. Expression of inducible NO synthase and cyclooxygenase 2 proteins were detected by Western blotting. The in vivo anti-inflammatory and antitumor promoting activities were evaluated by topical TPA application to ICR mouse skin with measurement of edema formation, epidermal thickness, leukocyte infiltration, hydrogen peroxide production, and the rate of proliferating cell nuclear antigen-stained cells. As a result, nobiletin, a polymethoxyflavonoid, was identified as an inhibitor of both NO and O2- generation. Nobiletin significantly inhibited two distinct stages of skin inflammation induced by double TPA application [first stage priming (leukocyte infiltration) and second stage activation (oxidative insult by leukocytes)] by decreasing the inflammatory parameters. It also suppressed the expression of cyclooxygenase-2 and inducible NO synthase proteins and prostaglandin E2 release. Nobiletin inhibited dimethylbenz[a]anthracene (0.19 micromol)/TPA (1.6 nmol)-induced skin tumor formation at doses of 160 and 320 nmol by reducing the number of tumors per mouse by 61.2% (P < 0.001) and 75.7% (P < 0.001), respectively. The present study suggests that nobiletin is a functionally novel and possible chemopreventive agent in inflammation-associated tumorigenesis.
The methods described in this article are quick, simple, and inexpensive to perform. The Folin quantitation method can determine both free and total polyphenol antioxidants in foods and beverages as described, as well as botanical extracts. This assay may also be used to estimate the daily per capita consumption of polyphenols in foods. The dose-response in vitro lower density lipoprotein antioxidant activity measurement (IC50) can be employed to compare antioxidants as pure compounds, or in mixtures after quantitating the polyphenols. The ex vivo lipoprotein-binding antioxidant activity can be measured simply and rapidly to determine possible in vivo binding of pure compounds or extracts from foods. Supplementation and epidemiology studies can utilize the rapid and inexpensive affinity column isolation method of lower density lipoproteins for the determination of lipoprotein oxidative susceptibility.
The major polyphenol in green tea, (-)-epigallocatechin-3-gallate (EGCG), has been shown to prevent carcinogenesis. We have identified a receptor that mediates the anticancer activity of EGCG. Expression of the metastasis-associated 67-kDa laminin receptor confers EGCG responsiveness to cancer cells at physiologically relevant concentrations. Experiments using surface plasmon resonance demonstrate binding of EGCG to the 67-kDa laminin receptor with a nanomolar K (d) value.
The effect of heat treatment on the antioxidant activity of extracts from Citrus unshiu peels was evaluated. Citrus peels (CP) (5 g) were placed in Pyrex Petri dishes (8.0 cm diameter) and heat-treated at 50, 100, or 150 degrees C for 10, 20, 30, 40, 50, and 60 min in an electric muffle furnace. After heat treatment, 70% ethanol extract (EE) and water extract (WE) (0.1 g/10 mL) of CP were prepared, and total phenol contents (TPC), radical scavenging activity (RSA), and reducing power of the extracts were determined. The antioxidant activities of CP extracts increased as heating temperature increased. For example, heat treatment of CP at 150 degrees C for 60 min increased the TPC, RSA, and reducing power of EE from 71.8 to 171.0 microM, from 29.64 to 64.25%, and from 0.45 to 0.82, respectively, compared to non-heat-treated control. In the case of WE from CP heat-treated at the same conditions (150 degrees C for 60 min), the TPC, RSA, and reducing power also increased from 84.4 to 204.9 microM, from 15.81 to 58.26%, and from 0.27 to 0.96, respectively. Several low molecular weight phenolic compounds such as 2,3-diacetyl-1-phenylnaphthalene, ferulic acid, p-hydroxybenzaldoxime, 5-hydroxyvaleric acid, 2,3-diacetyl-1-phenylnaphthalene, and vanillic acid were newly formed in the CP heated at 150 degrees C for 30 min. These results indicated that the antioxidant activity of CP extracts was significantly affected by heating temperature and duration of treatment on CP and that the heating process can be used as a tool for increasing the antioxidant activity of CP.
Aging is a major risk factor for neurodegenerative diseases including Alzheimer's disease (AD), Parkinson's disease (PD), and amyotrophic lateral sclerosis (ALS). An unbalanced overproduction of reactive oxygen species (ROS) may give rise to oxidative stress which can induce neuronal damage, ultimately leading to neuronal death by apoptosis or necrosis. A large body of evidence indicates that oxidative stress is involved in the pathogenesis of AD, PD, and ALS. Several studies have shown that nutritional antioxidants (especially vitamin E and polyphenols) can block neuronal death in vitro, and may have therapeutic properties in animal models of neurodegenerative diseases including AD, PD, and ALS. Moreover, clinical data suggest that nutritional antioxidants might exert some protective effect against AD, PD, and ALS. In this paper, the biochemical mechanisms by which nutritional antioxidants can reduce or block neuronal death occurring in neurodegenerative disorders are reviewed. Particular emphasis will be given to the role played by the nuclear transcription factor -kB (NF-kB) in apoptosis, and in the pathogenesis of neurodegenerative disorders, such as AD, PD, and ALS. The effects of ROS and antioxidants on NF-kB function and their relevance in the pathophysiology of neurodegenerative diseases will also be examined.
Previously we have reported that the O-methylated derivative of (-)-epigallocatechin-3-O-gallate (EGCG), (-)-epigallocatechin-3-O-(3-O-methyl) gallate (EGCG3"Me), possesses anti-allergic activities such as inhibition of histamine release and suppression of the high-affinity IgE receptor (FcepsilonRI) expression. However, the underlying mechanism is still unclear. Recently we have identified the 67kDa laminin receptor (67LR) as a cell-surface receptor that can mediate biological activities of EGCG. Here we show that the suppression of myosin II regulatory light chain (MRLC) phosphorylation through the cell-surface binding to the 67 LR contributes to the inhibitory effect of EGCG3"Me on the histamine release from the human basophilic KU812 cells. The 67LR also mediated the EGCG3"Me-induced suppression of FcepsilonRI expression by reducing ERK1/2 phosphorylation. These results suggest that anti-allergic effects of EGCG3"Me may be triggered by the inhibition of MRLC or ERK1/2 phosphorylation mediated through the cell-surface 67LR.
Here, we investigated the structure-activity relationship of major green tea catechins and their corresponding epimers on cell-surface binding and inhibitory effect on histamine release. Galloylated catechins; (-)-epigallocatechin-3-O-gallate (EGCG), (-)-gallocatechin-3-O-gallate (GCG), (-)-epicatechin-3-O-gallate (ECG), and (-)-catechin-3-O-gallate (CG) showed the cell-surface binding to the human basophilic KU812 cells by surface plasmon resonance analysis, but their non-galloylated forms did not. Binding activities of pyrogallol-type catechins (EGCG and GCG) were higher than those of catechol-type catechins (ECG and CG). These patterns were also observed in their inhibitory effects on histamine release. Previously, we have reported that biological activities of EGCG are mediated through the binding to the cell-surface 67kDa laminin receptor (67LR). Downregulation of 67LR expression caused a reduction of both activities of galloylated catechins. These results suggest that both the galloyl moiety and the B-ring hydroxylation pattern contribute to the exertion of biological activities of tea catechins and their 67LR-dependencies.
Intraperitoneal injection of washed, preformed ovalbumin/anti-ovalbumin immune complexes caused the production of slow-reacting substance (SRS), prostaglandin E2, 6 keto prostaglandin F1a, vascular permeability (measured as extravazation of pontamine sky blue injected previously into the bloodstream), and polymorphonuclear leukocyte (PMN) infiltration in the mouse peritoneal cavity. Arachidonic acid metabolites appeared early in the response at 7.5 min; dye extravazation and PMN infiltration peaked at 30 min and 4 hr, respectively, after immune complex injection. BW755C and phenidone given orally 30 min before immune complex injection inhibited dye extravazation and SRS formation at 7.5 and 30 min. Indomethacin by the same regimen inhibited dye extravazation at 7.5 min but not at 30 min, while enhancing SRS formation at both times. Dexamethasone inhibited dye extravazation and to some extent SRS formation at both times. The data suggests that the mouse model may be useful for demonstrating an antiinflammatory activity of dual inhibitors that is clearly distinguishable from the activities shown by classical nonsteroidal antiinflammatory drugs and steroids.
Systemic anaphylaxis results from the sudden release of mediators from a variety of inflammatory cells. Most reactions are due to insect stings, food allergy, immunotherapy injections, or pharmaceutical products. Anaphylaxis is easily recognized in most cases, although persons found unresponsive or who exhibit hypotension without urticaria or cutaneous angioedema present special diagnostic problems. Most reactions respond promptly to aggressive therapy, although fatalities occasionally occur. Optimal long-term care of patients with anaphylaxis involves accurate identification of triggering agents, education regarding allergen avoidance, and self-administration of epinephrine in case of future reactions.
To seek out a cheap source of dietary polyphenols and antioxidants along with anti-amylase and antiglucosidase activities, ethanol extracts of eleven cheap Bangladeshi fruits were investigated. The extracts were also examined for anti-allergic activity using rat peritoneal exudate cells exposed to the calcium ionophore A23187. Phyllanthus emblica (emblic myrobalan) had the highest total polyphenol content (339 mg gallic acid equivalent (GAE)/g), followed by Syzygium cumini (Indian blackberry; 192.3 mg GAE/g), and Aegle marmelos (wood apple; 53.7 mg GAE/g). P. emblica, and S. cumini also exhibited the most potent DPPH radical scavenging activity, with an IC50 of 2.1 and 8.6 μg/mL respectively. These extracts also showed promising reducing powers with P. emblica having the greatest such activity (optical density (O.D.) 1.66), followed by S. cumini (O.D. 1.34), at a concentration of 0.2 mg/mL. The extracts of Artocarpus heterophyllus (jackfruit) and S. cumini showed promising chelating activities. At a concentration of 1 mg/ mL, Dillenia indica (chalta) showed the highest inhibition of a-amylase activity (60%), and A. marmelos, D. indica, P. emblica, Spondias dulcis (hog-plum) & S. cumini completely inhibited α-glucosidase activity (100%). Apart from A. heterophyllus, D. indica and Phyllanthus acidus (star-gooseberry), all other extracts inhibited the release of histamine from the peritoneal exudate cells, with S. cumini having the strongest effect. These fruits therefore have activities beneficial to physiological health.
A possible way to valorize citrus peels and seeds, which are byproducts of the juice extraction industry, is to use them as natural antioxidants. The antioxidant activity of several citrus peel and seed extracts obtained either by methanol extraction (free phenolic compounds) or by alkaline hydrolysis (bound phenolic compounds) was tested in a model system based on accelerated citronellal oxidation. Generally, seeds possessed greater antioxidant activity than peels. The composition of all tested samples was studied by HPLC: methanol extracts are rich in flavones and glycosylated flavanones, whereas hydrolyzed extracts contain mainly phenolic acids and flavonols. The phenolic composition of some citrus peels and seeds was described for the first time. No clear relationship could be shown between the antioxidant activity and the phenolic composition of the extracts. Keywords: Citrus fruits; byproducts; antioxidant activity; flavanones; phenolic acids
Hydrogen peroxide (H2O2) is gradually produced in bottle-packed beverages, including tea and coffee, after the cap has been opened, i.e, through exposure to air, though only a small amount of H2O2 is detected in the beverage immediately after the bottle is opened. Since, H2O2 is toxic, it is necessary to develop safe and simple ways of reducing its production in bottled beverages. The addition of an aqueous extract of citrus peel reduced the concentration of H2O2 in green tea. To characterise the active constituents in the citrus peel, the aqueous extract of the peel was fractionated using chloroform, ethyl acetate, and butanol, in that order, and subjected to gel chromatography. The active constituents in the citrus peel were water-soluble compounds of various molecular weights.
Only a small amount of H2O2 was detected in beverages, such as tea or coffee, immediately after opening caps of bottles, but H2O2 was gradually produced in the beverages after opening the caps, i.e. exposure to air. The beverages with high concentrations of polyphenols showed high 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging activities, but produced relatively high concentrations of H2O2 when they were exposed to air, possibly due to oxygen. The production of H2O2 increased both with duration of the exposure to air and rise in temperature. Since H2O2 is toxic, ways to prevent the deterioration of catechin-enriched green tea, i.e. H2O2 production, were studied. The addition of catalase, which is an enzyme decomposing H2O2, reduced the H2O2 concentration, but it was inactivated at a high temperature. The addition of l-cysteine or glutathione (reduced form), with a thiol residue, reduced the H2O2 concentration. Addition of citric acid, malic acid, succinic acid, fumaric acid, l-ascorbic acid, l-glutamic acid and l-aspartic acid also reduced it, possibly because they lower the pH of the tea.
Polymethoxy flavones (PMFs) are present in fruit tissues of Citrus species. It has been reported that flavonoids isolated from several Citrus have been shown to suppress the degranulation as inferred by histamine release in rat basophilic leukemia RBL-2H3 cells. In this study, we examined the effect of PMFs (PMF-1: 6,7,4',5'-tetramethoxy-5-monohydroxyflavone, PMF-2: 5,6,8,3',6'-pentamethoxy flavone, PMF-3: 5,6,7,3',4',5'-hexamethoxy flavone) on the degranulation in RBL-2H3 cells. All the PMFs suppressed the degranulation from Ag-stimulated RBL-2H3 cells. Interestingly, PMF-combination (PMF-1+PMF-2; PMF-1+PMF-3) treatment enhanced the inhibition of degranulation compared with PMF-single treatment. In order to clarify the inhibitory mechanism of degranulation by PMFs, we examined the activation of intracellular signaling molecules such as Lyn, Syk, and PLCgammas. All the PMFs significantly suppressed the activation of Syk and PLCgammas. In Ag-mediated activation of Fc epsilonRI on mast cells, three major subfamilies of mitogen-activated protein kinases, especially ERK44/42, were activated. These PMFs reduced the level of phospho-ERKs. The intracellular free Ca(2+) concentration ([Ca(2+)]i) was elevated by Fc epsilonRI activation, and PMF treatment reduced the elevation of [Ca(2+)]i by suppressing Ca(2+) influx. Thus, it was suggested that the suppression of Ag-stimulated degranulation by these PMFs mainly is due to the Syk/PLCgammas/PKC pathway and Ca(2+) influx. Furthermore, to be noted in the PMF-combination treatment, inactivation of Syk was enhanced compared with PMF-single treatment. But the inhibitory effect of degranulation by PMF-combination treatment was not associated with the suppression of Ca(2+) influx.
Mast cells participate in allergy and inflammation by secreting inflammatory mediators such as histamine and proinflammatory cytokines. Flavonoids are naturally occurring molecules with antioxidant, cytoprotective, and antiinflammatory actions. However, effect of flavonoids on the release of histamine and proinflammatory mediator, and their comparative mechanism of action in mast cells were not well defined. Here, we compared the effect of six flavonoids (astragalin, fisetin, kaempferol, myricetin, quercetin, and rutin) on the mast cell-mediated allergic inflammation. Fisetin, kaempferol, myricetin, quercetin, and rutin inhibited IgE or phorbol-12-myristate 13-acetate and calcium ionophore A23187 (PMACI)-mediated histamine release in RBL-2H3 cells. These five flavonoids also inhibited elevation of intracellular calcium. Gene expressions and secretion of proinflammatory cytokines such as tumor necrosis factor-alpha (TNF-alpha), interleukin (IL)-1beta, IL-6, and IL-8 were assessed in PMACI-stimulated human mast cells (HMC-1). Fisetin, quercetin, and rutin decreased gene expression and production of all the proinflammatory cytokines after PMACI stimulation. Myricetin attenuated TNF-alpha and IL-6 but not IL-1beta and IL-8. Fisetin, myricetin, and rutin suppressed activation of NF-kappaB indicated by inhibition of nuclear translocation of NF-kappaB, NF-kappaB/DNA binding, and NF-kappaB-dependent gene reporter assay. The pharmacological actions of these flavonoids suggest their potential activity for treatment of allergic inflammatory diseases through the down-regulation of mast cell activation.
In traditional Chinese medicine, dried citrus fruit peels are widely used as remedies to alleviate coughs and reduce phlegm in the respiratory tract. Induction of inducible nitric oxide synthase (iNOS) in inflammatory cells and increased airway production of nitric oxide (NO) are well recognized as key events in inflammation-related respiratory tract diseases. Despite the fact that the enhancing effect of heat treatment on the antioxidant activity of citrus fruit peels has been well documented, the impact of heat treatment on citrus peel beneficial activities regarding anti-inflammation is unclear. To address this issue, we determined the anti-inflammatory activities of heat-treated citrus peel extracts by measuring their inhibitory effect upon NO production by lipopolysaccharide-activated RAW 264.7 macrophages. Results showed that the anti-inflammatory activity of citrus peel was significantly elevated after 100 degrees C heat treatment in a time-dependent fashion during a period from 0 to 120 min. Inhibition of iNOS gene expression was the major NO-suppressing mechanism of the citrus peel extract. Additionally, the anti-inflammatory activity of citrus peel extract highly correlated with the content of nobiletin and tangeretin. Conclusively, proper and reasonable heat treatment helped to release nobiletin and tangeretin, which were responsible for the increased anti-inflammatory activity of heat-treated citrus peels.
Intraperitoneal injection of washed, preformed ovalbumin/anti-ovalbumin immune complexes caused the production of slow-reacting substance (SRS), prostaglandin E2, 6 keto prostaglandin Fla, vascular permeability (measured as extravazation of pontamine sky blue injected previously into the bloodstream), and polymorphonuclear leukocyte (PMN) infiltration in the mouse peritoneal cavity. Arachidonic acid metabolites appeared early in the response at 7.5 min; dye extravazation and PMN infiltration peaked at 30 min and 4 hr, respectively, after immune complex injection. BW755C and phenidone given orally 30 min before immune complex injection inhibited dye extravazation and SRS formation at 7.5 and 30 min. Indomethacin by the same regimen inhibited dye extravazation at 7.5 min but not at 30 min, while enhancing SRS formation at both times. Dexamethasone inhibited dye extravazation and to some extent SRS formation at both times. The data suggests that the mouse model may be useful for demonstrating an antiinflammatory activity of dual inhibitors that is clearly distinguishable from the activities shown by classical nonsteroidal antiinflammatory drugs and steroids.
The effect of ten flavonoids was studied on the stimulation of washed human platelets by either arachidonic acid or thrombin. The oxygenated metabolites released were analyzed by radioimmunoassay, glass-capillary-column gas chromatography and high-pressure liquid chromatography. No effect was evidenced for naringenin, rutinose and phloridzin up to 1000 microM. Thromboxane B2 and 12-hydroxyeicosatetraenoic acid production was depressed simultaneously by all other compounds at different IC50. When tested for their effect on reversibility, however, cyclooxygenase and lipoxygenase inhibition was found to be different depending upon the flavonoid used. All compounds, except morin and rutin, inhibited platelet aggregation and [14C]serotonin release with parallel inhibition of thromboxane synthesis when tested on arachidonic acid-induced platelet-rich plasma stimulation. Some flavonoids inhibited the metabolism of human neutrophils stimulated by ionophore A23187 as assessed by high-performance liquid chromatography. Our results show that flavonoids interfere with the different oxidative metabolisms of arachidonic acid. No clearcut specificity could be found between one compound and one metabolic pathway.
Plasma and urine histamine levels were measured during sequential infusions of histamine (0.05, 0.1, 0.25, 0.5, and 1.0 microgram/kg/min histamine base for 30 min each) to determine the plasma level required to elicit flushing, headaches, tachycardia, and diastolic hypotension. Each study was performed with subjects on no medications or after pretreatment with hydroxyzine and/or cimetidine in order to confirm the receptor subtype involved in each of the responses. Resting plasma histamine levels were 0.62 +/- 0.12 ng/ml, and levels rose progressively indirect proportion to the concentration of infused histamine. Plasma levels of histamine required to elicit symptoms were as follows: 1.61 +/- 0.30 ng/ml = 30% increase in heart rate, 2.39 +/- 0.52 ng/ml = significant flush and headache, and 2.45 +/- 0.13 ng/ml = 30% increase in pulse pressure. Cimetidine pretreatment failed to influence the histamine level required to elicit symptoms, hydroxyzine pretreatment significantly raised the level required to increase heart rat by 30%, and the combination of antihistamines significantly raised the threshold for histamine to elicit all the response. Urine histamine was increased in direct proportion to the histamine infusions, and because of stability, accessibility, and the capacity for retrospective diagnosis, urine is the suggested fluid to employ to measure histamine release in humans.
The human diet contains a great variety of natural mutagens and carcinogens, as well as many natural antimutagens and anticarcinogens.
Many of these mutagens and carcinogens may act through the generation of oxygen radicals. Oxygen radicals may also play a
major role as endogenous initiators of degenerative processes, such as DNA damage and mutation (and promotion), that may be
related to cancer, heart disease, and aging. Dietary intake of natural antioxidants could be an important aspect of the body's
defense mechanism against these agents. Many antioxidants are being identified as anticarcinogens. Characterizing and optimizing
such defense systems may be an important part of a strategy of minimizing cancer and other age-related diseases.
Metabolism, like other aspects of life, involves tradeoffs. Oxidant by-products of normal metabolism cause extensive damage to DNA, protein, and lipid. We argue that this damage (the same as that produced by radiation) is a major contributor to aging and to degenerative diseases of aging such as cancer, cardiovascular disease, immune-system decline, brain dysfunction, and cataracts. Antioxidant defenses against this damage include ascorbate, tocopherol, and carotenoids. Dietary fruits and vegetables are the principal source of ascorbate and carotenoids and are one source of tocopherol. Low dietary intake of fruits and vegetables doubles the risk of most types of cancer as compared to high intake and also markedly increases the risk of heart disease and cataracts. Since only 9% of Americans eat the recommended five servings of fruits and vegetables per day, the opportunity for improving health by improving diet is great.
Allergic reactions to food are more common among infants and children but occur in adults as well. Foods that are most often implicated in allergic reactions are eggs, cow's milk, nuts, wheat, soy products, whitefish, and crustacea. Gastrointestinal, respiratory tract, and dermatologic symptoms, as well as systemic anaphylaxis, may develop. In addition to history taking and physical examination, the workup may include skin testing, the radioallergosorbent test, and double-blind oral food challenge. Avoidance of offending antigens is the most important aspect of treatment. If exposure occurs, antihistamines and epinephrine may be needed for treatment of an acute reaction.
Male Wistar rats were given purified diets containing safflower (SAF), perilla (PER), or palm (PAL) oils with or without 1% tea polyphenols (TP) for 3 weeks, and chemical mediator releasing activity from rat peritoneal exudate cells (PEC) was measured. Histamine releasing activity was not influenced by TP, while histamine release and intracellular histamine content were significantly increased in the PAL-fed group. On the contrary, leukotriene B4 (LTB4) release was significantly lower in rats fed PER than in those fed SAF and PAL, and TP significantly decreased the release in all fat groups. TP also significantly inhibited the release of LTB5, which was generated only in rats fed PER. TP significantly decreased the proportion of arachidonic acid (AA) in PEC in the SAF-fed group and that of eicosapentaenoic acid (EPA), the precursor of LTB5 in the PER-fed group, but did not influence that of AA in the PAL- and PER-fed group. These results suggest that ingestion of TP improves type I allergic symptom through the inhibition of LT release though the inhibition by TP could not be totally explained by the reduction of substrate fatty acid.
"Bioactive compounds" are extranutritional constituents that typically occur in small quantities in foods. They are being intensively studied to evaluate their effects on health. The impetus sparking this scientific inquiry was the result of many epidemiologic studies that have shown protective effects of plant-based diets on cardiovascular disease (CVD) and cancer. Many bioactive compounds have been discovered. These compounds vary widely in chemical structure and function and are grouped accordingly. Phenolic compounds, including their subcategory, flavonoids, are present in all plants and have been studied extensively in cereals, legumes, nuts, olive oil, vegetables, fruits, tea, and red wine. Many phenolic compounds have antioxidant properties, and some studies have demonstrated favorable effects on thrombosis and tumorogenesis and promotion. Although some epidemiologic studies have reported protective associations between flavonoids or other phenolics and CVD and cancer, other studies have not found these associations. Various phytoestrogens are present in soy, but also in flaxseed oil, whole grains, fruits, and vegetables. They have antioxidant properties, and some studies demonstrated favorable effects on other CVD risk factors, and in animal and cell culture models of cancer. However, because phytoestrogens act both as partial estrogen agonists and antagonists, their effects on cancer are likely complex. Hydroxytyrosol, one of many phenolics in olives and olive oil, is a potent antioxidant. Resveratrol, found in nuts and red wine, has antioxidant, antithrombotic, and anti-inflammatory properties, and inhibits carcinogenesis. Lycopene, a potent antioxidant carotenoid in tomatoes and other fruits, is thought to protect against prostate and other cancers, and inhibits tumor cell growth in animals. Organosulfur compounds in garlic and onions, isothiocyanates in cruciferous vegetables, and monoterpenes in citrus fruits, cherries, and herbs have anticarcinogenic actions in experimental models, as well as cardioprotective effects. In summary, numerous bioactive compounds appear to have beneficial health effects. Much scientific research needs to be conducted before we can begin to make science-based dietary recommendations. Despite this, there is sufficient evidence to recommend consuming food sources rich in bioactive compounds. From a practical perspective, this translates to recommending a diet rich in a variety of fruits, vegetables, whole grains, legumes, oils, and nuts.
Polymethoxyflavones (PMFs) from citrus genus have been of particular interest because of their broad spectrum of biological activities, including antiinflammatory, anticarcinogenic, and antiatherogenic properties. There have been increasing interests in the exploration of health beneficial properties of PMFs in citrus fruits. Therefore, the isolation and characterization of PMFs from sweet orange (Citrus sinensis) peel will lead to new applications of the byproducts from orange juice processes and other orange consumption in nutraceutical and pharmaceutical products. In our study, eight hydroxylated PMFs, six PMFs, one polymethoxyflavanone, one hydroxylated polymethoxyflavanone, and two hydroxylated polymethoxychalcones were isolated from sweet orange peel and their structures were elucidated by various MS, UV, and different NMR techniques. Some of the hydroxylated PMFs and chalcones are newly isolated from sweet orange peel.
Determination of quantity and quality of polyphenol antioxidants in food and beverages
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