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Frontiers in Endocrinology 2023In this comprehensive review, we examine the main preclinical and clinical investigations assessing the effects of different forms of choline supplementation currently... (Review)
Review
In this comprehensive review, we examine the main preclinical and clinical investigations assessing the effects of different forms of choline supplementation currently available, including choline alfoscerate (CHNOP), also known as alpha-glycerophosphocholine (α-GPC, or GPC), choline bitartrate, lecithin, and citicoline, which are cholinergic compounds and precursors of acetylcholine. Extensively used as food supplements, they have been shown to represent an effective strategy for boosting memory and enhancing cognitive function.
Topics: Choline; Glycerylphosphorylcholine; Acetylcholine; Dietary Supplements; Cytidine Diphosphate Choline
PubMed: 36950691
DOI: 10.3389/fendo.2023.1148166 -
European Journal of Drug Metabolism and... Apr 2019The importance of quercetin and flavonoids in the diet and as food supplements is well known, and literature studies support their potential use to treat several human... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND AND OBJECTIVES
The importance of quercetin and flavonoids in the diet and as food supplements is well known, and literature studies support their potential use to treat several human diseases. Many beneficial properties have been described for quercetin, so much effort has been directed into overcoming the major drawbacks of this natural compound-its poor solubility and low oral absorption. The aims of this study were to compare a new food-grade lecithin-based formulation of quercetin, Quercetin Phytosome, to unformulated quercetin in terms of solubility in simulated gastrointestinal fluids and oral absorption in a randomized crossover pharmacokinetic study of healthy volunteers.
METHODS
The solubility of the new formulation was determined by in vitro incubation in simulated gastrointestinal fluids, and quercetin was detected by ultra performance liquid chromatography. A single-dose, randomized, six-sequence/three-period crossover clinical trial (3 × 3 × 3 crossover design) with a balanced carryover effect was conducted in healthy volunteers under fasting conditions. Twelve healthy volunteers of both sexes with an age range of 18-50 years were recruited; one dose of quercetin and two different doses of Quercetin Phytosome were administered orally as film-coated tablets. Pharmacokinetic samples were collected at twelve time points (from 0 h to 24 h) after administration, and quercetin levels were measured by HPLC/MS/MS. Data were analyzed using the Phoenix WinNonlin (v.6.4) software package, and the most significant pharmacokinetic parameters were calculated. Statistical analysis involved performing a two-way ANOVA with repeated measures followed by post hoc analysis (Tukey's test).
RESULTS
Significant improvements in both in vitro solubility and oral absorption (in terms of both exposure and maximum concentration achieved) by healthy volunteers in a human clinical study were obtained with the Quercetin Phytosome formulation as compared to unformulated quercetin.
CONCLUSIONS
A more soluble formulation of quercetin based on lecithin, Quercetin Phytosome, has recently been developed, and was found to facilitate the attainment of very high plasma levels of quercetin-up to 20 times more than usually obtained following a dose of quercetin-when the novel formulation was administered orally in human volunteers, and it did not have any notable side effects. These results suggest that Quercetin Phytosome allows the oral administration of quercetin in a safe and bioavailable manner, thus facilitating the effective utilization of this natural compound to treat various human diseases.
Topics: Administration, Oral; Adolescent; Adult; Cross-Over Studies; Dose-Response Relationship, Drug; Drug Delivery Systems; Fasting; Female; Humans; Lecithins; Liposomes; Male; Middle Aged; Oral Mucosal Absorption; Quercetin; Young Adult
PubMed: 30328058
DOI: 10.1007/s13318-018-0517-3 -
Proceedings of the Japan Academy.... 2014Since the phospholipase B (PLB) was reported as a deacylase of both lecithin and lysolecithin yielding fatty acids and glycerophosphocholine (GPC), there was a question... (Review)
Review
Since the phospholipase B (PLB) was reported as a deacylase of both lecithin and lysolecithin yielding fatty acids and glycerophosphocholine (GPC), there was a question as to whether it is a single enzyme or a mixture of a phospholipase A2 (PLA2) and a lysophospholipase (LPL). We purified the PLB in Penicillium notatum and showed that it catalyzed deacylation of sn-1 and sn-2 fatty acids of 1,2-diacylphospholipids and also sn-1 or sn-2 fatty acids of 1- or 2-monoacylphospholipids (lysophospholipids). Further, it also has a monoacyllipase activity. The purified PLB is a glycoprotein with m.w. of 91,300. The sugar moiety is M9 only and the protein moiety consists of 603 amino acids. PLB, different from PLA2, shows other enzymatic activities, such as transacylase, lipase and acylesterase. PLB activity is influenced by various substances, e.g. detergents, deoxycholate, diethylether, Fe(3+), and endogenous protease. Therefore, PLB might have broader roles than PLA2 in vivo. The database shows an extensive sequence similarity between P. notatum PLB and fungal PLB, cPLA2 and patatin, suggesting a homologous relationship. The catalytic triad of cPLA2, Ser, Asp and Arg, is also present in P. notatum PLB. Other related PLBs, PLB/Lipases are discussed.
Topics: Amino Acid Sequence; Animals; Carbohydrates; Catalytic Domain; Cattle; Fatty Acids; Glycoproteins; Hydrolysis; Intestinal Mucosa; Lecithins; Lysophospholipase; Mass Spectrometry; Molecular Sequence Data; Pancreas; Penicillium chrysogenum; Phospholipases A2; Saccharomyces cerevisiae; Sequence Homology, Amino Acid; Solanum tuberosum; Substrate Specificity
PubMed: 25391318
DOI: 10.2183/pjab.90.333 -
International Journal of Molecular... Apr 2023The aim of this study was to investigate the effects of soybean lecithin and plasmalogens concentrating on a variety of physiological tests and biochemical analyses in...
The aim of this study was to investigate the effects of soybean lecithin and plasmalogens concentrating on a variety of physiological tests and biochemical analyses in healthy Wistar rats. For six weeks, male Wistar rats were given a standard diet that included plasmalogens or soybean lecithin. We measured anxiety levels, overall exploratory activity, short- and long-term memory, cognitive abilities, and grip strength. Lecithin increased significantly anxiety and enhanced memory and cognitive functions. Plasmalogens significantly improved appetite and increased grip strength. When compared to plasmalogens, lecithin significantly raised HDL levels while lowering LDL levels. The plasmalogens group showed a significant increase in the C16:0DMA/C16:0 ratio, which led us to assume that plasmalogen consumption could increase their synthesis in neural tissue. The study's findings imply that, despite their various modes of action, soy lecithin and plasmalogens may both be significant nutritional components for enhancing cognitive functions.
Topics: Rats; Male; Animals; Cattle; Plasmalogens; Rats, Wistar; Lecithins; Glycine max; Brain
PubMed: 37108804
DOI: 10.3390/ijms24087643 -
PloS One 2023Extracellular vesicles (EVs) (exossomes, microvesicles and apoptotic bodies) have been well acknowledged as mediators of intercellular communications in prokaryotes and...
Extracellular vesicles (EVs) (exossomes, microvesicles and apoptotic bodies) have been well acknowledged as mediators of intercellular communications in prokaryotes and eukaryotes. Lipids are essential molecular components of EVs but at the moment the knowledge about the lipid composition and the function of lipids in EVs is limited and as for now none lipidomic studies in Giardia EVs was described. Therefore, the focus of the current study was to conduct, for the first time, the characterization of the polar lipidome, namely phospholipid and sphingolipid profiles of G. lamblia trophozoites, microvesicles (MVs) and exosomes, using C18-Liquid Chromatography-Mass Spectrometry (C18-LC-MS) and Tandem Mass Spectrometry (MS/MS). A total of 162 lipid species were identified and semi-quantified, in the trophozoites, or in the MVs and exosomes belonging to 8 lipid classes, including the phospholipid classes phosphatidylcholine (PC), phosphatidylethanolamine (PE), phosphatidylglycerol (PG), phosphatidylinositol (PI), cardiolipins (CL), the sphingolipid classes sphingomyelin (SM) and ceramides (Cer), and cholesterol (ST), and 3 lipid subclasses that include lyso PC (LPC), lyso PE (LPE) and lyso PG (LPG), but showing different abundances. This work also identified, for the first time, in G. lamblia trophozoites, the lipid classes CL, Cer and ST and subclasses of LPC, LPE and LPG. Univariate and multivariate analysis showed clear discrimination of lipid profiles between trophozoite, exosomes and MVs. The principal component analysis (PCA) plot of the lipidomics dataset showed clear discrimination between the three groups. Future studies focused on the composition and functional properties of Giardia EVs may prove crucial to understand the role of lipids in host-parasite communication, and to identify new targets that could be exploited to develop novel classes of drugs to treat giardiasis.
Topics: Animals; Giardia lamblia; Lipidomics; Tandem Mass Spectrometry; Extracellular Vesicles; Giardiasis; Giardia; Ceramides; Lecithins; Phospholipids; Sphingolipids; Cardiolipins; Gastropoda
PubMed: 37683041
DOI: 10.1371/journal.pone.0291292 -
Poultry Science Mar 2022The purpose of this study was to investigate the effect of dietary supplementation of different levels of soybean lecithin and vitamin E on semen quality parameters and...
The purpose of this study was to investigate the effect of dietary supplementation of different levels of soybean lecithin and vitamin E on semen quality parameters and some reproductive hormones in Hubbard grandparent roosters. The experiment was conducted in a 3 × 2 factorial arrangement with 3 levels of soybean lecithin (0, 1, and 2%) and 2 levels of vitamin E (0 and 300 mg/kg). Semen samples were collected on d 0, 20, 40 and 60 of the experiment and analyzed. Adding 1% soybean lecithin and vitamin E into the diet increased semen volume and sperm concentration, membrane integrity and viability (P < 0.05). Supplementing diets with 1 or 2% lecithin in addition to vitamin E significantly improved total motility and progressive motility (P < 0.05). Vitamin E significantly increased the amplitude of lateral head displacement (ALH) of sperm (P < 0.05). Although there was no effect on LH and FSH when diets were supplemented with vitamin E and 1 or 2% lecithin, testosterone concentration was increased (P < 0.05). Malondialdehyde (MDA) concentration was significantly lower in all 3 treatments containing vitamin E (P < 0.05). It can be concluded that supplementation of rooster diets with vitamin E and 1% lecithin can improve fertility related parameters in Hubbard grandparent roosters.
Topics: Animals; Chickens; Diet; Dietary Supplements; Fertility; Grandparents; Humans; Lecithins; Semen Analysis; Glycine max; Spermatozoa; Vitamin E
PubMed: 35007931
DOI: 10.1016/j.psj.2021.101635 -
Molecules (Basel, Switzerland) Dec 2020The present work aimed to assess the chondroprotective influence of chitosan and lecithin in a monoiodoacetate (MIA)-induced experimental osteoarthritis (OA) model....
The present work aimed to assess the chondroprotective influence of chitosan and lecithin in a monoiodoacetate (MIA)-induced experimental osteoarthritis (OA) model. Forty male rats weighing 180-200 g were randomly distributed among the following five experimental groups (eight per group): control, MIA-induced OA, MIA-induced OA + chitosan, MIA-induced OA + lecithin, and MIA-induced OA + chitosan + lecithin. The levels of TNF-α, IL6, RF, ROS, and CRP, as well as mitochondrial markers such as mitochondrial swelling, cytochrome C oxidase (complex IV), MMP, and serum oxidative/antioxidant status (MDA level) (MPO and XO activities) were elevated in MIA-induced OA. Also, SDH (complex II) activity in addition to the levels of ATP, glutathione (GSH), and thiol was markedly diminished in the MIA-induced OA group compared to in control rats. These findings show that mitochondrial function is associated with OA pathophysiology and suggest that chitosan and lecithin could be promising potential ameliorative agents in OA animal models. Lecithin was more effective than chitosan in ameliorating all of the abovementioned parameters.
Topics: Adenosine Triphosphate; Animals; Antioxidants; Chitosan; Disease Models, Animal; Electron Transport Complex IV; Glutathione; Interleukin-6; Iodoacetic Acid; Lecithins; Male; Matrix Metalloproteinases; Osteoarthritis; Rats; Reactive Oxygen Species; Tumor Necrosis Factor-alpha
PubMed: 33291821
DOI: 10.3390/molecules25235738 -
Biomolecules Jun 2018Pinocembrin is a natural flavonoid compound which is capable of antioxidant, antibacterial, anti-inflammatory, and antineoplastic activities. The present study aimed to...
Pinocembrin is a natural flavonoid compound which is capable of antioxidant, antibacterial, anti-inflammatory, and antineoplastic activities. The present study aimed to enhance the solubility and antioxidant activities of pinocembrin by complex formation with lecithin. The physicochemical characteristics of pinocembrin⁻lecithin complex were analyzed by ultraviolet (UV), fourier-transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and solubility assay, and the antioxidant activities of pinocembrin⁻lecithin complex were evaluated via radical scavenging capacities for 2,2′-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS), hydroxyl, and superoxide-anion. The results indicated that pinocembrin complex with lecithin could significantly improve the solubility of pinocembrin in water and -octane, the pinocembrin⁻lecithin complex displayed no characteristic endothermic peak and the appearance of amorphous state, compared to the pinocembrin, and no new covalent bond was produced in the pinocembrin and lecithin compound. It was demonstrated that the antioxidant activities of pinocembrin were obviously enhanced by the complex with lecithin, and the scavenging capacities for hydroxyl radical, DPPH, superoxide-anion radical, and ABTS radical of pinocembrin⁻lecithin complex were 82.44 ± 2.21%, 40.07 ± 1.32%, 59.15 ± 0.86%, and 24.73 ± 1.04% at 1.0 mg/mL, respectively. It suggested that the pinocembrin⁻lecithin complex had a great potential application prospect in the healthcare industry and in clinical practice.
Topics: Flavanones; Free Radical Scavengers; Lecithins; Solubility
PubMed: 29921807
DOI: 10.3390/biom8020041 -
Journal of Pharmacy & Pharmaceutical... 2012Topical drug treatment aims at providing high concentrations of drugs at the site of application so as to avoid adverse systemic effects associated with oral... (Review)
Review
Topical drug treatment aims at providing high concentrations of drugs at the site of application so as to avoid adverse systemic effects associated with oral administration. Smart polymers, or stimuli-responsive polymers, are able to respond to a stimulus by showing physical or chemical changes in their behaviour as, for example, the delivery of the drug carried by them. The thermo-responsive nature of Pluronic® F-127 (Basf, Ludwigshafen, Germany) makes it an excellent candidate for the delivery of drugs at various application sites. In recent years, PF-127, and later, Pluronic lecithin organogels (PLO), have attracted particular interest in the design of dermal and transdermal delivery systems with a view to promoting, improving or retarding drug permeation through the skin, bearing in mind that for topical delivery systems, accumulation in the skin with minimal permeation is desired, while for systemic delivery, the opposite behaviour is preferred. In this review, we discuss the properties and characteristics of PF-127 and Pluronic lecithin organogels (PLO), and present many examples and advantages of the application of these polymeric systems in topical and transdermal administration of drugs. This article is open to POST-PUBLICATION REVIEW. Registered readers (see "For Readers") may comment by clicking on ABSTRACT on the issue's contents page.
Topics: Administration, Cutaneous; Animals; Drug Delivery Systems; Humans; Lecithins; Poloxamer; Skin
PubMed: 23106961
DOI: 10.18433/j3hw2b -
European Journal of Pharmaceutics and... Jan 2022In previous studies, lecithin-based nanoemulsions (NEs) have been shown to be skin friendly drug carrier systems. Due to their nontoxic properties, NEs might also be...
In previous studies, lecithin-based nanoemulsions (NEs) have been shown to be skin friendly drug carrier systems. Due to their nontoxic properties, NEs might also be suitable as wound healing agents. Hence, different O/W NEs based on lecithin Lipoid® S 75 and plant oils or medium chain triglycerides were produced and characterised. Two lipophilic natural wound healing agents, a betulin-enriched extract from birch bark (BET) and a purified spruce balm (PSB), were successfully incorporated and their effects on primary human skin cells were studied in vitro. MTT, BrdU and scratch assays uncovered the positive influence of the drug-loaded NEs on cell viability, proliferation and potential wound closure. Compared to control formulations, the NEs loaded with either BET or PSB led to higher cell viability rates of fibroblasts and keratinocytes. Higher proliferative activity of keratinocytes and fibroblasts was observed after the treatment, which is a prerequisite for wound closure. Indeed, in scratch assays NEs with PSB and notably BET showed significantly ameliorated wound closure rates than the negative control (unloaded NEs) and the positive control (NEs with dexpanthenol). Our findings suggest that BET and PSB are outstanding wound healing drugs and their incorporation into lecithin-based NEs may represent a valid strategy for wound care.
Topics: Betula; Cell Proliferation; Cell Survival; Emulsions; Humans; In Vitro Techniques; Lecithins; Picea; Plant Oils; Skin; Triglycerides; Triterpenes; Wound Healing
PubMed: 34798283
DOI: 10.1016/j.ejpb.2021.11.004