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Vaccine Adjuvants in Immunotoxicology
Published in Mesut Karahan, Synthetic Peptide Vaccine Models, 2021
All adjuvants in commercial vaccines are in an oil-based formulation, except for aluminum- and virus-like particle-based adjuvants. Oils take the role of “dangerous signal” in the immune system by activating TLR receptors on the surface of the APCs. Oil-based vaccines are used to improve the amphiphilic properties of lipid-peptide conjugates. The length, number, and position of the conjugate oils play an important role in the administration of a vaccine. Although lipid-peptide conjugates can induce a strong immune response, potential toxicities such as membrane degradation caused by lipopeptides should be considered (Zhao et al. 2017).
Marine Natural Products for Human Health Care
Published in Hafiz Ansar Rasul Suleria, Megh R. Goyal, Health Benefits of Secondary Phytocompounds from Plant and Marine Sources, 2021
Some peptides of sponge origin also showed antimicrobial and anti-viral activity such as callyaerins -A to -F, and H from the Callyspongia aerizusa off Indonesian coast [130], and the antifungal bicyclic peptide-theonellamides [208]. Other sponge derived antimicrobial peptides are amino-lipopeptides [234]. Furthermore, two novel cyclic hexapeptides had antifungal and antibacterial activity [332]. The fungal species also produced some novel aspochracin-type cyclic tripeptides, named as sclerotiotides -A to -K [331].
CD14, An Innate Immune Receptor for Various Bacterial Cell Wall Components
Published in Helmut Brade, Steven M. Opal, Stefanie N. Vogel, David C. Morrison, Endotoxin in Health and Disease, 2020
Artur J. Ulmer, Volker T. El-Samalouti, Ernst T. Rietschel, Hans-Dieter Flad, Roman Dziarski
LPS and PG are not the only bacterial cell wall compounds that express inflammatory properties. Lipoarabinomannan, lipoteichoic acid, lipopeptides, sphingolipids, and various bacterial cell wall preparations also induce the production of cytokines in monocytes/macrophages (16,37–44) and, therefore, may contribute to an inflammatory reaction in an infected host. In addition, nonbacterial and synthetic polymers are known to mediate inflammatory reactions at least in vitro (36,45).
Comparing the pharmacokinetics and organ/tissue distribution of anti-methicillin-resistant Staphylococcus aureus agents using a rat model of sepsis
Published in Xenobiotica, 2022
Shinji Kobuchi, Naoya Kanda, Taichi Okumi, Yuma Kano, Himawari Tachi, Yukako Ito, Toshiyuki Sakaeda
For patients infected with methicillin-resistant Staphylococcus aureus (MRSA), glycopeptide vancomycin (VCM) is empirically the first-line drug; however, various anti-MRSA agents, including aminoglycoside arbekacin (ABK), oxazolidinone linezolid (LZD), and lipopeptide daptomycin (DAP) are available. VCM is also prescribed for treating sepsis or septic shock because of its extensive clinical use. However, dose modification is essential to achieve effective plasma VCM concentrations with minimal side effects, such as renal failure. Clinical studies have shown that decreased susceptibility of MRSA to VCM is associated with treatment failure and poor prognosis (Holmes et al. 2012; Britt et al. 2017; Egi et al. 2021; Hort et al. 2021). Therefore, pharmacokinetic and pharmacodynamic/toxicodynamic information on drugs other than VCM is required to expand the treatment selection for sepsis.
Novel temporin L antimicrobial peptides: promoting self-assembling by lipidic tags to tackle superbugs
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Rosa Bellavita, Annarita Falanga, Elisabetta Buommino, Francesco Merlino, Bruno Casciaro, Floriana Cappiello, Maria Luisa Mangoni, Ettore Novellino, Maria Rosaria Catania, Rossella Paolillo, Paolo Grieco, Stefania Galdiero
To induce self-assembling properties in cationic peptides and influence their interaction with bacterial membranes and consequently their antimicrobial and broad-spectrum activity, we designed a library of lipopeptides by the addition of fatty acids of variable length at the N- and C-termini of peptide 1B and its parent peptide 1A. Valeric, heptanoic, undecanoic and tridecanoic acids were linked at the N-terminus of 1A and 1B (Table 1), to obtain, respectively, peptides 2A–5A and 2B–5B. Moreover, we designed peptide C, characterised by an alkyl chain of 5 carbon atom (C-5) in para position of the Phe1 aromatic ring, but preserving the net positive charge of +4. Besides, we investigated the effects of C-5 and C-7 hydrophobic lipid tails attached to the side chain of the ornithine residue at C-terminus of peptide 1B achieving peptides D and E.
Strong inhibitory activities and action modes of lipopeptides on lipase
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Mei-chun Chen, Tian-tian Liu, Jie-ping Wang, Yan-ping Chen, Qing-xi Chen, Yu-jing Zhu, Bo Liu
Results showed that lipase inhibition was dose dependent. After adding these four inhibitors, the relative enzyme activity decreased significantly with increasing concentration of effectors. The half maximal inhibitory concentration (IC50) of crude lipopeptide, purified fengycin, iturin, and surfactin standards were 0.011, 0.005, 0.056, and 0.005 mg/mL, respectively. We have previously reported that furoic acid and oxalic acid inhibited lipase with IC50 of 0.242 and 1.425 mg/mL, respectively21. Moreover, we found that the inhibitory effects of the lipopeptides were within one order of magnitude of orlistat (IC50 = 0.004 mg/mL)7. These results suggest that lipopeptides have strong lipase inhibition activity and could act as lipase inhibitors to prevent obesity.