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PAF antagonists in foods: Isolation and identification of PAF antagonists in honey and wax
Abstract
The lipids of honey and wax were extracted and separated by successive TLC with a variety of solvent systems. Every isolated fraction was tested for its ability to aggregate washed rabbit platelets or to inhibit PAF or thrombin induced aggregation. The biologically active compounds were subjected to FTIR, MS and 1H-NMR analysis. None of the honey lipids caused platelet aggregation, but six of them inhibited PAF and thrombin induced aggregation, although at remarkably higher concentrations than PAF. Their activity varies according to the origin of honey; The proposed structures for these compounds are: a) an 1-0-alkenyl-2-acetyl-3-acyl glycerol or an 1-O-alkenyl-2-acetyl-3-keto-acyl glycerol (for the most active) ; b) a polyhydroxysterol; c) and d) neutral lipids with ether and esters bonds and one of them ester with acetic acid. The results explain the pharmaceutical application of honey in cases of inflammation, as the above mentioned compounds are antagonists of the well know inflammatory mediator, PAF.
... Re-cently, an in silico research revelad that honey may be able to bind SARS-CoV-2 protease, and so inhibit SARS-CoV-2 proteases and some compounds of honey [2]. Also, honey shows anti-thrombotic activity due to the inhibiton of PAF [3,4]. Therefore, honey may parts of plants, after being collected by honey bee combining with unique substances, reducing water content and storing in honeycomb [6]. ...
Recently encountered pandemic SARS-CoV-2 infection is a serious concern in the worldwide. In order to prevent this disease and to avoid the side effects of the drugs used during the treatment of SARS-CoV-2 infection, humans turned to the consumption of natural foods including bee products. Honey is an important bee product rich in antioxidants, but should be suitable for consumption in terms of food control and safety. Therefore, the present study was undertaken to determine the physico-chemical and the antioxidant characteristics of commercial honey samples originated from 7 different regions of Turkey as well as, to interpret the results with the Turkish Food Codex and European Commission Regulation. Total antioxidant capacity including polyphenols was highest in 100g honey from Agean Region (100 mmol Ascorbic acid Eq and mg Gallic acid Eq, respectively) whereas flavonoid content was the highest in honey from Mediterranean Region. It was found that 19 honey samples (63.3%) were suitable for the Codex Honey Communiqué in terms of sucrose, invert sugar (glucose and fructose), moisture content, number of diastases, hydroxymethylfurfural (HMF), commercial glucose and pollen analyzes. The honey samples originated from seven different regions of Turkey showed more than half good quality. Their quality depends on various factors such as floral source, geographical origin, harvest seasons, packaging, processing conditions, and storage conditions. Therefore, the consumer’s awareness and the education of beekeepers can improve the production and sales for good quality honey.
... Among several ingredients of N. sativa seed, thymiquinone, nigellidine, and α-hederin might be the efficient herbal drugs against COVID-19 [90]. Honey can be considered as another alternative because it has protective function to combat various enveloped viruses, and it is also an antagonist for plateletactivating factor (PAF) involving in COVID-19 [91,92]. By boosting immune response, honey may play a beneficial role in COVID-19 patients [93]. ...
The COVID-19 pandemic caused by SARS-CoV-2 has been showing a speedy
growth in the number of infected patients with a remarkable mortality rate,
thus it has become a worldwide public health concern. From March 8, 2020, the
virus started spreading in Bangladesh. Since then, people got infected so
exponentially that the country positions at the list of top infected countries in
the world. Therefore, the objective of this comprehensive review was
representing overall scenario of COVID-19 in different sectors of Bangladesh.
Because of insufficient scientific publications, we chose materials published by
several agencies, media outlets, newspapers, and policy experts to retrieve
details information. Up to 4 March 2021, 547,930 confirmed cases and 8,428
deaths were reported in Bangladesh. An alarming fact is that while the global
mutation rate of coronavirus is 7.23 % in average, the rate is 12.6 % in
Bangladesh. Although the government ruled preventive strategies such as
nationwide lockdown, social distancing, contact monitoring, quarantine, and
isolation, it was difficult to implement those due to lack of public awareness,
inappropriate attitudes and so on. Moreover, the overburdened healthcare
system had a weak response at initial stage because of insufficient healthcare
facilities. Consequently, this pandemic affected severely almost all the
important sectors of the country, specifically the economy, agriculture,
education, and health sector. Hence, focusing on healthcare system,
maintaining social distance, and other essential precautions can limit the spread
of infection and help to alleviate the severity of this pandemic.
... Moreover, it has been suggested to have a role against COVID-19 epidemic [174,175], it has six compounds related to the receptor active site of COVID-19's main protease according to a in silico approach [176] and is currently being tested in a clinical trial (clinical trial NCT04323345) [176]. It is noted that honey displays anti-thrombotic activity [177] and it especially acts as a PAF inhibitor [178]. In total, the antibacterial, the anti-thrombotic and anti-PAF effects of honey render it a potentially useful food against the COVID epidemic. ...
The new coronavirus disease 2019 (COVID-19) pandemic is an emerging situation with high rates of morbidity and mortality, in the pathophysiology of which inflammation and thrombosis are implicated. The disease is directly connected to the nutritional status of patients and a well-balanced diet is recommended by official sources. Recently, the role of platelet activating factor (PAF) was suggested in the pathogenesis of COVID-19. In the present review several micronutrients (vitamin A, vitamin C, vitamin E, vitamin D, selenium, omega-3 fatty acids, minerals), phytonutrients and Mediterranean diet compounds (olive oil, fish, honey, plant foods) with potential anti-COVID activity are presented. We further underline that the well-known anti-inflammatory and anti-thrombotic actions of the investigated nutrients and/ or holistic dietary schemes, such as the Mediterranean diet, are also mediated through PAF. In conclusion, although there is no single food to prevent coronavirus, the aim is to follow a healthy diet containing PAF inhibitors in order to target both inflammation and thrombosis and try to avoid or/and reduce the deleterious effects of the COVID-19 epidemic.
... It is already proved that honey plays a potential role against several enveloped viruses. Besides, honey acts as an antagonist of platelet-activating factor (PAF) which is involved in COVID-19 [98,99]. Therefore, we can say that honey may have a protective/beneficial effect on COVID-19. ...
Honey and its compounds are drawing attention as an effective natural therapy because of its ability to attenuate acute inflammation through enhancing immune response. Several studies have proved its potential healing capability against numerous chronic diseases/conditions, including pulmonary disorders, cardiac disorders, diabetes , hypertension, autophagy dysfunction, bacterial, and fungal infections. More importantly, honey has proved its virucidal effect on several enveloped viruses such as HIV, influenza virus, herpes simplex, and varicella-zoster virus. Honey may be beneficial for patients with COVID-19 which is caused by an enveloped virus SARS-CoV-2 by boosting the host immune system, improving comorbid conditions, and antiviral activities. Moreover, a clinical trial of honey on COVID-19 patients is currently undergoing. In this review, we have tried to summarize the potential benefits of honey and its ingredients in the context of antimicrobial activities, some chronic diseases, and the host immune system. Thus, we have attempted to establish a relationship with honey for the treatment of COVID-19. This review will be helpful to reconsider the insights into the possible potential therapeutic effects of honey in the context of the COVID-19 pandemic. However, the effects of honey on SARS-CoV-2 replication and/or host immune system need to be further investigated by in vitro and in vivo studies.
... Consequently, it was deduced that other lipid extracts could potentially inhibit PAF-induced platelet aggregation. This led to a series of studies investigating food lipid extracts starting around 1993, which initially lead to the discovery of PAF antagonists in the polar lipid fractions of olive oil [207], honey and wax [208], milk and yoghurt [209], mackerel (Scomber scombrus) [210], and wine [211] before the turn of the century. These studies deduced that mainly polar lipids such as glycerophospholipids and glycolipids exhibited potent inhibition against PAF-induced platelet aggregation through competitive binding to the PAF-R. ...
In the late 1960s, Barbaro and Zvaifler described a substance that caused antigen induced histamine release from rabbit platelets producing antibodies in passive cutaneous anaphylaxis. Henson described a 'soluble factor' released from leukocytes that induced vasoactive amine release in platelets. Later observations by Siraganuan and Osler observed the existence of a diluted substance that had the capacity to cause platelet activation. In 1972, the term platelet-activating factor (PAF) was coined by Benveniste, Henson, and Cochrane. The structure of PAF was later elucidated by Demopoulos, Pinckard, and Hanahan in 1979. These studies introduced the research world to PAF, which is now recognised as a potent phospholipid mediator. Since its introduction to the literature, research on PAF has grown due to interest in its vital cell signalling functions and more sinisterly its role as a pro-inflammatory molecule in several chronic diseases including cardiovascular disease and cancer. As it is forty years since the structural elucidation of PAF, the aim of this review is to provide a historical account of the discovery of PAF and to provide a general overview of current and future perspectives on PAF research in physiology and pathophysiology.
... The regulation of PAF actions is also succeeded by the daily ingestion of PAF inhibitors which are consumed through our diet (see Figures S1 and S2, in the Supplementary Material available online at https:// doi.org/10.1155/2017/6947034). Among all diets, the Mediterranean diet consists of numerous products that exert potent anti-PAF activities in the washed platelet aggregation assay, such as virgin or regular olive oil [73,74], wine and grapes [75][76][77][78], honey [79], fish [80][81][82], milk and yoghurt [83], and traditional Greek meals [84], the isolation and structural characterization of which demonstrated the presence of complex polar lipids as glycolipids and ganglioside derivatives, phenolics, and phenol glucosides [65]. Furthermore, from the acetylation of poplar lipids and phenolic compounds derived acetylated products with anti-PAF action [85,86], especially, olive oil was found to contain high levels of PAF antagonists among other vegetable oils and the structure of its most active fraction was found to be a glycerolglycolipid [74]. ...
In this minireview, we refer to recent results as far as the Platelet Activating Factor (PAF) inhibitors are concerned. At first, results of organic compounds (natural and synthetic ones and specific and nonspecific) as inhibitors of PAF are reported. Emphasis is given on recent results about a new class of the so-called metal-based inhibitors of PAF. A small library of 30 metal complexes has been thus created; their anti-inflammatory activity has been further evaluated owing to their inhibitory effect against PAF in washed rabbit platelets (WRPs). In addition, emphasis has also been placed on the identification of preliminary structure-activity relationships for the different classes of metal-based inhibitors.
Context
Atherosclerosis is a disease of chronic inflammation. Recent research has identified 2 novel inflammatory biomarkers: platelet-activating factor (PAF) and lipoprotein-associated phospholipase A2 (Lp-PLA2). Diet has been proposed as a mediator of inflammation, but to date, the focus for these novel biomarkers has been on individual foods and nutrients rather than overall dietary patterns.
Objective
To systematically review the literature on the association between dietary patterns and PAF and Lp-PLA2.
Data Sources
The PubMed, Embase, CINAHL, and Cochrane CENTRAL literature databases were searched.
Data Analysis
Study quality was evaluated using the Quality Criteria Checklist. Sixteen studies (n = 4 observational and n = 12 interventional) were included and assessed for associations between dietary patterns and PAF and Lp-PLA2.
Conclusion
Study quality varied from neutral (n = 10) to positive (n = 6). Mediterranean, heart healthy, and vegetarian dietary patterns were associated with improved levels of PAF and Lp-PLA2. Conversely, Western dietary patterns were less favorable. A range of well-established, healthier dietary patterns may lower inflammation and the risk of atherosclerosis. More well-designed studies are needed to confirm these findings and identify other dietary patterns that improve inflammation.
The new coronavirus disease 2019 (COVID-19) pandemic is an emerging situation with high rates of morbidity and mortality, in the pathophysiology of which inflammation and thrombosis are implicated. The disease is directly connected to the nutritional status of patients and a well-balanced diet is recommended by official sources. Recently, the role of platelet activating factor (PAF) was suggested in the pathogenesis of COVID-19. In the present review several micronutrients (vitamin A, vitamin C, vitamin E, vitamin D, selenium, omega-3 fatty acids, and minerals), phytochemicals and Mediterranean diet compounds with potential anti-COVID activity are presented. We further underline that the well-known anti-inflammatory and anti-thrombotic actions of the investigated nutrients and/or holistic dietary schemes, such as the Mediterranean diet, are also mediated through PAF. In conclusion, there is no single food to prevent coronavirus Although the relationship between PAF and COVID-19 is not robust, a healthy diet containing PAF inhibitors may target both inflammation and thrombosis and prevent the deleterious effects of COVID-19. The next step is the experimental confirmation or not of the PAF-COVID-19 hypothesis.
Cancer is the second leading cause of mortality worldwide. The role of unresolved inflammation in cancer progression and metastasis is well established. Platelet-activating factor (PAF) is a key proinflammatory mediator in the initiation and progression of cancer. Evidence suggests that PAF is integral to suppression of the immune system and promotion of metastasis and tumor growth by altering local angiogenic and cytokine networks. Interactions between PAF and its receptor may have a role in various digestive, skin, and hormone-dependent cancers. Diet plays a critical role in the prevention of cancer and its treatment. Research indicates that the Mediterranean diet may reduce the incidence of several cancers in which dietary PAF inhibitors have a role. Dietary PAF inhibitors such as polar lipids have demonstrated inhibitory effects against the physiological actions of PAF in cancer and other chronic inflammatory conditions in vitro and in vivo. In addition, experimental models of radiotherapy and chemotherapy demonstrate that inhibition of PAF as adjuvant therapy may lead to more favorable outcomes. Although promising, there is limited evidence on the potential benefits of dietary PAF inhibitors on cancer prevention or treatment. Therefore, further extensive research is required to assess the effects of various dietary factors and PAF inhibitors and to elucidate the mechanisms in prevention of cancer progression and metastasis at a molecular level.
A new normal phase high performance liquid chromatographic system has been developed that allows efficient separation of several polar lipids, such as phospholipids, glycolipids, and phenolics. By this method, hesperidin, naringin, cerebrosides, phosphatidylcholine, sphingomyelin, platelet activating factor, lysophosphatidylcholine, digalactosyldiglycerides, and phosphatidylethanolamine are separated within 60 min. A gradient elution with acetonitrile/methanol, methanol, and water was performed with a normal phase aminopropyl-modified silica gel HPLC column. The eluted lipids were monitored by UV detection. In addition, in this study, a successful application of the new method is represented for the polar lipids of olive oil and sunflower, which are also identified with chemical determinations.
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