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Chemistry and Physics of Lipids
Elsevier Scientific Publishers Ireland Ltd
Chemistry and Physics of Lipids

Elsevier Scientific Publishers Ireland Ltd

0009-3084

Chemistry and Physics of Lipids/Journal Chemistry and Physics of LipidsSCIISTP
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    What different physical techniques can disclose about disruptions on membrane structure caused by the antimicrobial peptide Hylin a1 and a more positively charged analogue

    Muniz, Gabriel S. VignoliDuarte, Evandro L.Lorenzon, Esteban N.Cilli, Eduardo M....
    16页
    查看更多>>摘要：The present work monitors structural changes in anionic membranes (DPPG; 1,2-dipalmitoyl-sn-glycero-3-phospho-(1'-rac-glycerol)) caused by the native antimicrobial peptide (AMP) Hylin a1 (Hya1; IFGAIL-PLALGALKNLIK-NH2) and its synthetic analogue K0Hya1 (KIFGAILPLALGALKNLIK-NH2), with an extra positive residue of lysine at the N-terminus of the peptide chain. Anionic membranes were used to mimic anionic lipids in bacteria membranes. Differential scanning calorimetry (DSC) evinced that both peptides strongly disrupt the lipid bilayers. However, whereas the native peptide (+3) induces a space-average and/or time-average disrup-tion on DPPG bilayers, the more charged, K(0)Hya1 (+4), appears to be strongly attached to the membrane, clearly giving rise to the coexistence of two different lipid regions, one depleted of peptide and another one peptide-disrupted. The membrane fluorescent probe Laurdan indicates that, in average, the peptides increase the bilayer packing of fluid DPPG (above the lipid gel-fluid transition temperature) and/or decrease its polarity. Spin labels, incorporated into DPPG membrane, confirm, and extend the results obtained with Laurdan, indicating that the peptides increase the lipid packing both in gel and fluid DPPG bilayers. Therefore, our results confirm that Laurdan is often unable to monitor structural modifications induced on gel membranes by exogenous molecules. Through the measurement of the leakage of entrapped carboxyfluorescein (CF), a fluorescent dye, in DPPG large unilamellar vesicles it was possible to show that both peptides induce pore formation in DPPG bi-layers. Furthermore, CF experiments show that Hylin peptides are strongly bound to DPPG bilayers in the gel phase, not being able to migrate to other DPPG vesicles. Here we discuss the complementarity of different techniques in monitoring structural alterations caused on lipid bilayers by Hylin peptides, and how it could be used to help in the understanding of the action of other exogenous molecules on biological membranes.
      原文链接:
    • NSTL
    • Elsevier

    Alpha1-antitrypsin combined fatty acids induced angiopoietin-like protein 4, expression in breast cancer: A pilot study

    Preethika, A.Kumai, N. SuchethaSandeep, AilShetty, Jayarama...
    8页
    查看更多>>摘要：Introduction: The effect of nutrition on inflammation and breast cancer (BC) prognosis is still inconclusive. Mechanism of data suggests that different types of fatty acids (FAs) play an essential role in carcinogenesis, and binding of alpha 1 antitrypsin (A1AT) may modulate carcinogenesis. The increased expression in the bound form of A1AT and release of Angiopoietin-like protein 4 (Angptl4) targets the gene of peroxisome proliferator-activated receptor-gamma (PPAR-gamma). Our aim of the study was to compare the effect of FA-free (A1AT-0) and FAs bound forms of A1AT on levels of IL-18, PPAR-gamma, and Angplt4 in breast cancer and control women. Methodology: 10 women with breast cancer and ten control women within the age group 25-60 years with normal (Pi) M allele A1AT were recruited. Mononuclear cells were isolated and treated with different A1AT and FAs on the various combinations (linoleic acid, alpha-linolenic acid) for time-dependent study (2,4,18 and 24 h) and analyzed for the interleukin-1 beta(IL-1b), PPAR-gamma, and Angiopoietin-like protein 4 (Angptl4) expression by using ELISA method and gas chromatography for analyzing FAs. One-way ANOVA combined with multiple comparisons is used to compare the means. Results: 100% of the study subjects were homozygous for the normal allele of A1AT. Time-dependent effects of A1AT and A1AT conjugated fatty acids on IL-I b, PPAR-g and Angptl4 showed statistically significant P = 0.07, P = 0.001, and P = 0.02 respectively, compared to those of the former study subjects. But within the groups, PPARg levels in case group (F(15,40)1.606, P = 0.003) and Angptl4 in the control group (F(15,32)0.64, P = 0.043) differed significantly. Conclusion: To the best of our knowledge, it's the first kind of study, and we speculate that the A1AT complex with different types of FAs results in a new form of A1AT having a solid capability to regulate the inflammation induced synthesis, processing, and release of an active form of IL-18. Our experimental data shows that the anti-inflammatory property of A1AT combined FAs likely to be mediated PPAR gamma and Angptl4 activation, thereby inhibiting the IL-1b. These findings may be worth assessing BC's biological effects and therapeutic effectiveness.
      原文链接:
    • NSTL
    • Elsevier

    Synthesis, aggregation behavior and drug-binding interactions of fatty acid-imidazolium-based surface-active ionic liquids

    Arif, RabiaMir, Ab WaheedShaheen, Arifa
    12页
    查看更多>>摘要：The renewable fatty acid-based surface-active ionic liquids (SAILs) containing ethyl-substituted imidazolium head groups were prepared and structurally analyzed by Fourier transform infrared spectroscopy (FTIR), (HNMR)-H-1 and (CNMR)-C-13 spectroscopy. The products were named as; 3-ethyl-1-(2-dodecanoyl oxy) ethylimidazolium bromide [C(12)Eeim]Br, 3-ethyl-1-(2-tetradecanoyl oxy) ethylimidazolium bromide [C(14)Eeim]Br and 3-ethyl-1-(2-hexadecanoyl oxy) ethylimidazolium bromide [C(16)Eeim]Br. The critical micelle concentration (cmc) values of the three SAILs have been evaluated using conductivity measurements, probe-less UV-visible spectroscopy and fluorescence spectroscopy. The obtained cmc values were compared with the earlier reported non-functionalized SAILs such as [C(n)mim]Br and [C(n)eim]Br where n = 12, 14, 16. The values were found to be 3-9 times lower mainly due to the presence of ester chain and also ethyl substituted imidazole ring. Thermodynamic parameters were evaluated by conductivity data at three different temperatures. Further, the aggregation behavior of SAILs with anesthetic drug, lidocaine hydrochloride (LC) has been studied using fluorescence. The fluorescence and UV-visible studies showed strong synergistic interactions operating between SAILs and drug molecules involving H bonding and cation-pi interactions. The interactions grew stronger with the elongation of SAIL-chain length (12-16C). Dynamic light scattering (DLS) and transmission electron microscopy (TEM) measurements suggested the formation of vesicles in SAIL-LC mixtures. These studies may thus offer an effective candidate which would serve as vectors for drug molecules in terms of their enhanced solubilization, permeability and target-specific delivery.
      原文链接:
    • NSTL
    • Elsevier

    Nose-to-brain lipid nanocarriers: An active transportation across BBB in migraine management

    Kataria, IshantIPShende, Pravin
    7页
    查看更多>>摘要：The present study focused on the development and evaluation of nanotechnology-based carrier systems of solid lipid nanoparticles (SLNs) to enhance the permeation and bioavailability of zolmitriptan across blood-brain barrier (BBB). SLNs are the emerging field of nanotechnology with numerous applications like cosmetics and pharmaceutical research. Zolmitriptan-loaded SLNs were prepared by high-pressure homogenization method for targeted drug delivery to the brain. The SLNs were found to be round in shape with particle size ranging from 110 to 200 nm and zeta potential upto 24.83 +/- 3.03 mV which indicates good colloidal stability. The maximum entrapment efficiency of zolmitriptan in SLNs was found to be 84.17 +/- 12.24%. The in-vitro drug release and ex vivo release studies exhibited 95.85 +/- 2.44% and 82.06 +/- 2.94% drug release, respectively for 24 h. In-vivo studies was performed on male Wistar rats wherein the concentration of zolmitriptan was estimated in cerebrospinal fluid by LC-MS method. The selected formulation incorporated with SLNs showed significant enhancement in pharmacokinetic parameters like AUC (37.05 +/- 2.45 ng/mL), C-max (42.08 +/- 1.32 ng/mL), T-max (30 min), and t(1/2) (1.28 h). Zolmitriptan-loaded SLNs via intranasal administration offers a novel approach to effectively circumvent first-pass hepatic metabolism than conventional oral route with 4-fold alleviation in permeation and 2-fold improvement in bioavailability.
      原文链接:
    • NSTL
    • Elsevier

    Resveratrol loaded in cationic glucosylated liposomes to treat Staphylococcus epidermidis infections

    Pagano, LiviaGkartziou, FoteiniAiello, StefanoSimonis, Beatrice...
    10页
    查看更多>>摘要：Glucosylated liposomes composed of the natural saturated phospholipid 1,2-dipalmitoyl-sn-glycero-3-phos-phocholine (DPPC), cholesterol (Chol) and a cationic amphiphile featuring a glucosyl moiety (GL4), have been developed for delivering the antimicrobial trans-Resveratrol (RSV) to S. epidermidis , characterized by carbohydrate-specific adhesins able to recognize glucose. The cationic derivative of cholesterol, DC-Chol, was also included in liposome formulations, alone or in combination with GL4 , in order to explore the role of both cationic charge and sugar moiety in the interaction of liposomes with bacterial cells. RSV was included inside glucosylated cationic liposomes by the thin film method, coupled with either extrusion or sonication; liposome mean diameter, polydispersity index, surface charge, RSV entrapment efficiency and concentration have been measured by DLS, electrophoretic mobility, and HPLC. The antimicrobial activity of RSV-loaded liposomes was evaluated by monitoring the bacterial growth curves of two cell lines of Staphylococcus epidermidis , a slime positive strain (i.e. a strain able to form a biofilm) and a slime negative one. Results point out that, when the glucosylamphiphile GL4 is included in the formulation, only the extrusion protocol allows obtaining mono disperse liposomes with high RSV entrapment efficiency. The mean diameters of empty and resveratrol-loaded liposomes are all around 120-140 nm and size distribution are narrow, except for samples including GL4 at 5 molar percentage. Here the higher polydispersity index may be the indication of the occurrence of a restructuring phenomenon. The microbiological tests put in evidence a different response of the two bacterial cell lines to liposome treatments, in fact, the slime negative bacterial cells, that are not able to produce the extracellular polymeric substances, are more susceptible to the cationic charge of the liposomes and to the detergent effect of GL4. The most interesting results concern DPPC/Chol/GL4 liposomes on the slime positive strain: this formulation, non-toxic in itself, displays an enhanced antibacterial efficacy with respect to free RSV, killing bacteria even at concentration tenfold under the MIC.
      原文链接:
    • NSTL
    • Elsevier

    A comparative study of the effects of crab derived exosomes and doxorubicin in 2 & 3-dimensional in vivo models of breast cancer

    Rezakhani, LeilaRahmati, ShimaGhasemi, SorayyaAlizadeh, Morteza...
    10页
    查看更多>>摘要：Introduction: Using tissue engineering and modifying the tumor microenvironment, three-dimensional (3D) in vitro and in vivo cancer modeling can be performed with appropriate similarity to native. Exosomes derived from different sources have recently been used in cancer studies due to their anticancer effects. In this study, the effect of crab derived exosomes in 2 & 3-dimensional (2& 3D) in vivo models of breast cancer (BC) were investigated and compared with the doxorubicin (DOX). Methods: 2D and 3D models of BC were induced using the chitosan/beta-glycerol phosphate hydrogel (Ch/beta-GP) and 1 x 106 4T1 cells in the female mice aged 6-8 weeks. 1 mg/ml exosome and 5 mg/kg DOX were injected by intratumoral (IT), intravenous (IV), and intraperitoneal (IP) methods into mice on day 9, 13, and 17 with and without hydrogel as a drug delivery system. After 21 days, the mice were sacrificed, and the tissues (lung, liver, and tumor) were removed. The weight and size of the tumor were measured. Real-time PCR assessed changes of VEGF, Bcl2, and P53 genes expression levels. Nitric oxide (NO) secretion from the cancer 3D model was evaluated by Griess assay. Results and Conclusion: Based on the results, the size and weight of tumors in treated groups with exosomes and DOX were reduced significantly (P < 0.001, P < 0.002, P < 0.02) in 2D and 3D models. Changes in VEGF, Bcl2 and P53 gene expression levels were less in the 3D model than in the 2D model. Drug delivery with hydrogel increased tumor inhibition compared to drug injection without hydrogel. Decreased NO secretion was observed in all treatment groups compared to the control group (untreated). Crab exosomes showed anti cancer effects on 2&3D models of BC. 3D model of BC showed greater drug resistance than the 2D model after treating with crab derived exosomes and DOX. 3D model of BC mimics native tumor better than 2D and can be used in cancer studies and for drug screening with greater confidence than 2D model. Also, the use of slow release drug delivery system reduced drug resistance in both models.
      原文链接:
    • NSTL
    • Elsevier

    Synthesis and bioactivity of readily hydrolysable novel cationic lipids for potential lung delivery application of mRNAs

    Pei, YihuaBao, YanjieSacchetti, CristianoBrady, Juthamart...
    11页
    查看更多>>摘要：Lipid nanoparticles (LNPs) mediated mRNA delivery has gained prominence due to the success of mRNA vaccines against Covid-19, without which it would not have been possible. However, there is little clinical validation of this technology for other mRNA-based therapeutic approaches. Systemic administration of LNPs predominantly targets the liver, but delivery to other organs remains a challenge. Local approaches remain a viable option for some disease indications, such as Cystic Fibrosis, where aerosolized delivery to airway epithelium is the preferred route of administration. With this in mind, novel cationic lipids (L1-L4) have been designed, synthesized and co formulated with a proprietary ionizable lipid. These LNPs were further nebulized, along with baseline control DOTAP-based LNP (DOTAP(+)), and tested in vitro for mRNA integrity and encapsulation efficiency, as well as transfection efficiency and cytotoxicity in cell cultures. Improved biodegradability and potentially superior elimination profiles of L1-L4, in part due to physicochemical characteristics of putative metabolites, are thought to be advantageous for prospective therapeutic lung delivery applications using these lipids.
      原文链接:
    • NSTL
    • Elsevier

    Influence of humectants on the thermotropic behaviour and nanostructure of fully hydrated lecithin bilayers

    Li, Ngai Ying DeniseMoore, David J.Thompson, Michael A.Welfare, Eloise...
    10页
    查看更多>>摘要：Humectants are used widely in topical formulations as they provide cosmetic and health benefits to skin. Of particular interest to our laboratories is the interaction of humectants in phospholipid based topical skin care formulations. This study probed the effects of three exemplary humectants on a fully hydrated lecithin system (DPPC) by use of X-ray scattering and differential scanning calorimetry. While the three humectants affected the nanostructure of 1, 2-dipalmitoyl-sn-glycero-3-phosphocholine, DPPC, bilayers in a similar manner, leading to an increased membrane order, differences in the effect on the thermal behaviour of DPPC suggest that betaine and sarcosine interacted via a different mechanism compared to acetic monoethanolamide, AMEA. At concentrations above 0.4 M, betaine and sarcosine stabilised the gel phase by depletion of the interfacial water via the preferential exclusion mechanism. At the same time, a slight increase in the rigidity of the membrane was observed with an increase in the membrane thickness. Overall, the addition of betaine or sarcosine resulted in an increase in the pre-and main transition temperatures of DPPC. AMEA, on the other hand, decreases both transition temperatures, and although the interlamellar water layer was also decreased, there was evidence from the altered lipid chain packing, that AMEA molecules are present also at the bilayer interface, at least at high concentrations. Above the melting point in the fluid lamellar phase, none of the humectants induced significant structural changes, neither concerning the bilayer stacking order nor its overall membrane fluidity. An humectant-induced increase in the Hamaker constant is the most plausible explanation for the observed reduction of the inter-bilayer distances, both in the gel and fluid phase.
      原文链接:
    • NSTL
    • Elsevier