Pharmacokinetic characterization of phosphatidylserine liposomes in the rat

Palatini, Pietro; Viola, Giampietro; Bigon, E.; Menegus, A. M.; Bruni, A.

doi:10.1111/j.1476-5381.1991.tb12176.x

Cited by 21 publications

(11 citation statements)

References 31 publications

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“…Consequently, PtdSer supplementation regimes that are successful in elevating extracellular PtdSer will probably enhance intracellular PtdSer. In support of this hypothesis, Palatini et al (1991) demonstrated that radioactively labelled PtdSer was present in organ tissues as well as in the plasma of rats 60 min following the bolus intravenous (i.v.) injection of radioactively labelled PtdSer liposomes.…”

Section: Fate Of Exogenous Phosphatidylserinementioning

confidence: 76%

“…lipoproteins. In addition, the analysis of biotransformation products suggested that decarboxylation to phosphatidylethanolamine and extensive hydrolytic degradation probably reflected the mechanisms of PtdSer uptake, incorporation into the plasma membrane and internalisation by endocytosis, respectively (Palatini et al, 1991).…”

Section: Fate Of Exogenous Phosphatidylserinementioning

confidence: 99%

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Effects of Phosphatidylserine Supplementation on Exercising Humans

Kingsley

2006

Sports Medicine

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Phosphatidylserine (PtdSer) is a ubiquitous phospholipid species that is normally located within the inner leaflet of the cell membrane. PtdSer has been implicated in a myriad of membrane-related functions. As a cofactor for a variety of enzymes, PtdSer is thought to be important in cell excitability and communication. PtdSer has also been shown to regulate a variety of neuroendocrine responses that include the release of acetylcholine, dopamine and noradrenaline. Additionally, PtdSer has been extensively demonstrated to influence tissue responses to inflammation. Finally, PtdSer has the potential to act as an effective antioxidant, especially in response to iron-mediated oxidation. The majority of the available research that has investigated the effects of PtdSer supplementation on humans has concentrated on memory and cognitive function; patients experiencing some degree of cognitive decline have traditionally been the main focus of investigation. Although investigators have administered PtdSer through intravenous and oral routes, oral supplementation has wider appeal. Indeed, PtdSer is commercially available as an oral supplement intended to improve cognitive function, with recommended doses usually ranging from 100 to 500 mg/day. The main sources that have been used to derive PtdSer for supplements are bovine-cortex (BC-PtdSer) and soy (S-PtdSer); however, due to the possibility of transferring infection through the consumption of prion contaminated brain, S-PtdSer is the preferred supplement for use in humans. Although the pharmacokinetics of PtdSer have not been fully elucidated, it is likely that oral supplementation leads to small but quantifiable increases in the PtdSer content within the cell membrane.A small number of peer-reviewed full articles exist that investigate the effects of PtdSer supplementation in the exercising human. Early research indicated that oral supplementation with BC-PtdSer 800 mg/day moderated exercise-induced changes to the hypothalamo-pituitary-adrenal axis in untrained participants. Subsequently, this finding was extended to suggest that S-PtdSer 800 mg/day reduced the cortisol response to overtraining during weight training while improving feeling of well-being and decreasing perceived muscle soreness. However, equivocal findings from our laboratory might suggest that the dose required to undertake this neuroendocrine action may vary between participants.Interestingly, recent findings demonstrating that short-term supplementation with S-PtdSer 750 mg/day improved exercise capacity during high-intensity cycling and tended to increase performance during intermittent running might suggest an innovative application for this supplement. With the findings from the existing body of literature in mind, this article focuses on the potential effects of PtdSer supplementation in humans during and following exercise.

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Section: Fate Of Exogenous Phosphatidylserinementioning

confidence: 76%

Section: Fate Of Exogenous Phosphatidylserinementioning

confidence: 99%

Effects of Phosphatidylserine Supplementation on Exercising Humans

Kingsley

2006

Sports Medicine

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“…However, the PUFA content of plasma PE is greater than that of plasma PC [42]. Feeding omega-3 fatty acid to humans increases the DHA content of membrane PE more than that of membrane PC [42], and the administration of bovine brain PS significantly raises the level of plasma DHA-PE [43]. Therefore PE could be an important source of DHA for the brain, through the generation of DHA lysoPE by the action of EL.…”

Section: Discussionmentioning

confidence: 99%

Phospholipid and fatty acid specificity of endothelial lipase: Potential role of the enzyme in the delivery of docosahexaenoic acid (DHA) to tissues

Chen¹,

Subbaiah

2007

Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biolog

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Docosahexaenoic acid (DHA; 22:6 n-3) is an essential fatty acid required for the normal function of several tissues, especially the brain. Previous studies suggested that lysophosphatidylcholine (lysoPC) is a preferred carrier of DHA to the brain, although the pathways of the formation of DHA-containing lysophospholipids in plasma have not been delineated. We propose that endothelial lipase (EL), a phospholipase A1 that plays an important role in the metabolism of high density lipoproteins, may be responsible for the generation of DHA lysophospholipids in plasma. Here we studied the substrate specificity of EL using deuterium-labeled phospholipids with different polar head groups, as well as DHA-enriched natural phospholipids to test this hypothesis. Glycerol-stabilized phospholipids were treated with recombinant EL, and the products were analyzed by liquid chromatography/electrospray ionization mass spectrometry. EL showed the polar head group specificity in the order of phosphatidylethanolamine>phosphatidylcholine>phosphatidylserine>phosphatidic acid. Within the same phospholipid class, the enzyme showed preference for the species containing DHA at the sn-2 position, and was inactive in the hydrolysis of phospholipids containing an ether linkage. Since EL is known to be secreted by the cells of blood-brain barrier, we suggest that it plays an important role in the delivery of DHA lysophospholipid carriers to the brain.

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“…Following IV administration to rats and mice, Phosphatidylserine was eliminated from plasma in a biphasic manner and largely distributed to several major organs, including the liver spleen and brain. [45][46][47][48][49] Conversely, orally administered Phosphatidylserine was extensively hydrolyzed by phospholipase A 2 to lysophosphatidylserine in the gastrointestinal tract prior to absorption, as is the case for all other dietary phospholipids. 45,50,51 In rats, approximately 60% of an orally administered dose of Phosphatidylserine (20 mg/kg body weight) was recovered in the feces, of which 50% was identified as lysophosphatidylserine.…”

Section: Nonhumanmentioning

confidence: 99%

“…48 Studies in which animals were injected IV with radiolabled Phosphatidylserine also indicate that phospholipids undergo hydrolytic cleavage to the monoacyl derivative lysophosphatidylserine in the plasma as well as decarboxylation of the serine moiety to phosphatidylethanolamine in circulating blood cells. 46,47,49 Lysophosphatidylserine and *It is possible that these products may be sprays, but it is not specified whether the reported uses are sprays. **It is possible that these products may be powders, but it is not specified whether the reported uses are powders.…”

Section: Nonhumanmentioning

confidence: 99%

Safety Assessment of Lecithin and Other Phosphoglycerides as Used in Cosmetics

Johnson¹,

Bergfeld²,

Belsito³

et al. 2020

Int J Toxicol

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The phosphoglycerides considered in this safety assessment are reported to function primarily as skin and hair conditioning agents, emulsifying agents, and surfactants in cosmetic products and are used up to a maximum reported concentration of 50%. Although phospholipids exert physiologic effects, these are not reproduced by application of phospholipid ingredients to the skin. Given the possibility that Lecithin may be derived from animal sources, it should be noted that the Food and Drug Administration does not permit the use of ingredients made from bovine specified risk materials in cosmetic products. The Expert Panel for Cosmetic Ingredient Safety concluded that the 17 phosphoglycerides are safe in the present practices of use and concentration in cosmetics, as described in this safety assessment.

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Pharmacokinetic characterization of phosphatidylserine liposomes in the rat

Cited by 21 publications

References 31 publications

Effects of Phosphatidylserine Supplementation on Exercising Humans

Effects of Phosphatidylserine Supplementation on Exercising Humans

Phospholipid and fatty acid specificity of endothelial lipase: Potential role of the enzyme in the delivery of docosahexaenoic acid (DHA) to tissues

Safety Assessment of Lecithin and Other Phosphoglycerides as Used in Cosmetics

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