Melittin (ME), a linear 26-residue non-cell-selective antimicrobial peptide, displays strong lytic activity against bacterial and human red blood cells. To design ME analogue with improved cell selectivity, we synthesized a melittin diastereomer (ME-D) with D-amino acid in the leucine zipper sequence (Leu-6, Lue-13 and Ile-20). Compared to ME, ME-D exhibited the same or 2-fold higher antibacterial activity but 8-fold less hemolytic activity. Circular dichroism analysis revealed that ME-D has much less alpha-helical content in alpha-helical content in the presence of zwitterionic EYPC/cholesterol (10 : 1, w/w) liposomes compared to negatively charged EYPE/EYPG (7 : 3, w/w) liposomes. The blue shift of the fluorescence emission maximum of ME-D in zwitterionic EYPC/ cholesterol (10 : 1, w/w) liposomes was much smaller than in negatively charged EYPE/EYPG (7 : 3, w/w) liposomes. These results suggested that the improvement in therapeutic index/cell selectivity of ME-D is correlated with its less permeability to zwitterionic membranes.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.5483/bmbrep.2007.40.6.1090 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Preparation of sodium hyaluronate coated liposomes: effect of polymer molecular weight, coating concentration, amount of charged lipids and type of hydration medium on the stability.
J Liposome Res
January 2025
SiteDel Group, Department of Pharmacy, University of Oslo, Blindern, Oslo, Norway.
In this study, liposomes consisting of soybean phosphatidyl choline (SoyPC) and different molar concentrations (10 mol% and 20 mol%) of dioleoyl trimethylammoniumpropane (DOTAP) were prepared by the thin film hydration method and coated with sodium hyaluronate (NaHA) of different MWs (8-15 kDa, 30-50 kDa and 90-130 kDa) and concentrations (0.01-0.2% w/w) using phosphate buffer (PB) or glycerol phosphate buffer (G-PB) as the hydration medium.
View Article and Find Full Text PDFSpontaneous nanosized liposome formation from crude dried lecithin upon addition of glycerol.
Sci Rep
December 2024
School of Engineering, University of Guelph, Guelph, ON, N1G2W1, Canada.
Nanosized liposomal vesicles (NLV) were successfully prepared using natural sunflower lecithin without the use of high-pressure homogenization or filtration. Upon glycerol addition to dispersions of lecithin multilamellar vesicles (MLVs), these broke down spontaneously to liposomes with diameters in the range of 100-200 nm. Static light scattering demonstrated that glycerol addition above 30% (w/w) induced the complete transformation of MLVs into NLVs.
View Article and Find Full Text PDFNanoassemblies with Gd-chelating lipids (GMO@DTPA-BSA-Gd) as a potential new type of high molecular weight contrast agents.
J Mater Chem B
November 2024
NanoBioMedical Centre, Adam Mickiewicz University, Wszechnicy Piastowskiej 3, 61-614 Poznań, Poland.
Self-assembled lipid nanoparticles containing Gd-chelating lipids are a new type of positive magnetic resonance imaging contrast agents (MRI CAs). High molecular weight imposes reduced molecular reorientation () and corresponding longer reorientation correlation times (), finally resulting in overall high relaxivity () of such contrast agents. Therefore, we report nanoassemblies based on two types of amphiphile molecules: glyceryl monooleate (GMO) as a matrix embedded with DTPA-bis(stearylamide) and its gadolinium salt (DTPA-BSA-Gd) as a Gd-chelating lipid, stabilized by surfactant Pluronic F127 molecules.
View Article and Find Full Text PDFAtorvastatin loaded glycerosomal patch as an effective transdermal drug delivery: optimization and evaluation.
Ther Deliv
November 2024
Faculty of Pharmacy, The Maharaja Sayajirao University of Baroda, Vadodara, 390001, Gujarat, India.
The study explores glycerosomes as effective vesicular systems for transdermal delivery of atorvastatin (ATO) to overcome drawbacks related to its oral administration. The objectives of this study were to formulate, by thin-film hydration method, optimize using definitive screening design and evaluate ATO-loaded glycerosomes (ATOG) which were then incorporated into patch followed by the evaluation of glycerosomes containing different concentration of glycerol. Vesicle size, Polydispersity index (PDI), zeta potential, entrapment efficiency and loading capacity of spherical ATOG (0-30%w/w) showed 137.
View Article and Find Full Text PDFBaicalin (BCL), a well-known flavonoid molecule, has numerous therapeutic applications. However, its low water solubility and bioavailability limit its applicability. Microfluidics is a new method for liposome preparation that provides efficient and rapid control of the process, improving the stability and controllability.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!