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Cationic Amphiphilic - DOAJ

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Last Updated: 13 August 2022

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Identification and characterization of the anti-SARS-CoV-2 activity of cationic amphiphilic steroidal compounds

COVID-19 patients' treatment is difficult, but specific procedures to reduce COVID-19 aggravation and mortality are still needed. Both the LNB167 and LNB169 cell lines were chosen because of their ability to reduce infectious viral progeny and viral RNA levels in Vero CCL81, HEK293, and HuH7. 5 cell lines. LNB167 and LNB169 inhibited the first phase of viral replication by mechanisms that involved modification of membrane lipids and cholesterol in host cells, according to experimental results in Vero CCL81 cells. SARS-CoV-2 disease could not be alleviated by LNB167 therapy, according to in vivo testing using the hACE2 transgenic mouse model. We conclude that the anti-SARS-CoV-2 activities of steroidal compounds LNB167 and LNB169 are likely host-targeted, consistent with the properties of cationic amphiphilic compounds that modulate host cell lipid metabolisms.

Source link: https://doi.org/10.1080/21505594.2022.2085793


Antibacterial activity and therapeutic efficacy of Fl-PRPRPL-5, a cationic amphiphilic polyproline helix, in a mouse model of staphylococcal skin infection

Fl-PRPRPL-5 showed potent activity against all clinical isolates of S. auus tested, including methicillin- and vancomycin-resistant S. aureus. Staphylococcus aureus, biofilms, anti-inflammatory, skin inflammation, and skin inflammation are among the study's findings. In conclusion, the findings of this research point to the possibility of using Fl-PRPL-5 in the treatment of staphylococcal skin infections.

Source link: https://doaj.org/article/73d3b7108cbc4c0fa508700e1159c76f


A Cationic Amphiphilic Random Copolymer with pH-Responsive Activity against Methicillin-Resistant Staphylococcus aureus.

At neutral pH, the polymer was effective in killing S. aureus, but it was inactive under acidic conditions. The polymer did not have any significant hemolytic activity against human red blood cells or display cytotoxicity to human dermal fibroblasts in a variety of pH values compared to a range of pH levels. We suggest a new skin cancer treatment with this pH-sensitive antimicrobial polymer agent that will selectively target infections at pH-neutral wound sites, but not the acidic, healthy skin.

Source link: https://doi.org/10.1371/journal.pone.0169262


Aggregation of Cationic Amphiphilic Block and Random Copoly(vinyl ether)s with Antimicrobial Activity

The polymer aggregate of B3826 appears to have low-density polymer chains without any defined microscopic structures, according to the cryo-TEM results. B3826 bonds to E. coli cell surfaces were shown by fluorescence microscopy photographs, and these bacterial cells were stained by propidium iodide, indicating that the cell membranes had been significantly damaged. Block copolymers, according to the results, may provide a new platform to design and produce antimicrobial materials that can be used in assembled structures and properties.

Source link: https://doi.org/10.3390/polym10010093


Repurposing Cationic Amphiphilic Antihistamines for Cancer Treatment

We screened a cationic amphiphilic drug library for cytotoxicity against NSCLC cells and discovered several CAD antihistamines as inducers of lysosomal cell death in our search for new NSCLC treatments. Between 1995 and 2011, we then conducted a cohort study on the effect of CAD antihistamine use on mortality of patients with non-localized cancer in Denmark. CAD antihistamine use and reduced mortality in patients with concurrent chemotherapy history were more prevalent among those without such records.

Source link: https://doi.org/10.1016/j.ebiom.2016.06.013


Development of a Cationic Amphiphilic Helical Peptidomimetic (B18L) As A Novel Anti-Cancer Drug Lead

BST-2, a novel cause of cancer progression, whose expression gives breast cancer cells oncogenic properties. As such, targeting BST-2 in tumors could be a highly effective therapeutic therapy against breast cancer. Furthermore, molecular biology studies reveal that B18L dysregulates cancer signaling pathways, leading to decreased Src and Erk1/2 phosphorylation, elevated expression of pro-apoptotic Bcl2 proteins, caspase 3 cleavage products, as well as processing of the caspase substrate, polymerase-1, to the characteristic apoptotic fragment.

Source link: https://doi.org/10.3390/cancers12092448


Efficient Percutaneous Delivery of the Antimelanogenic Agent Glabridin Using Cationic Amphiphilic Chitosan Micelles.

A cationic amphiphilic chitosan derivative, pyrrolidone carboxylate, is a Partially myristoylated chitosan pyrrolidone carboxylate. Glabridin is a hydrophobic antimelanogenic agent produced by licorice root extracts. Using a human skin model, we investigated the effects of cationic Glab-containing polymeric micelles isolated from PMCP on the skin's ability and inhibit melanogenesis. Glab/PMCP-PM ratio was about four times higher than that of traditional oil-in-water micelles prepared using Tween 60. Hence, Glab/PMCP-PM has the potential to be an effective transdermal delivery system for treating skin hyperpigmentation.

Source link: https://doi.org/10.1371/journal.pone.0164061


Cationic amphiphilic drugs are potent inhibitors of yeast sporulation.

Meiosis is a tightly controlled developmental process that occurs in almost all eukaryotes that participate in sexual reproduction. Two different high-throughput assays were used to determine how organic compounds influence meiotic growth of the model organism Saccharomyces cerevisiae, which was exposed to 446 bioactive molecules during meiotic growth. Several chemicals were identified that strongly inhibited spore formation, but did not affect vegetative growth. In addition, we found that yeast cells that are growing and sporulating for the aminophospholipid translocase, NEO1, are haploinsufficient in the absence of the drug.

Source link: https://doi.org/10.1371/journal.pone.0042853


Synthesis and Characterization of Radiogallium-Labeled Cationic Amphiphilic Peptides as Tumor Imaging Agents

SVS-1 is a cationic amphiphilic peptide with a preferred cytotoxicity against cancer cells over normal cells. Epidermoid carcinoma KB cells exhibited a significant rise in epidermoid carcinoma KB cells in all three peptides. Cell uptake of 67 Ga-NOTA-KV6 and 67 Ga-NOTA-HV6 into 3T3-L1 cells was much lower than that in KB cells, despite a significant decrease in KB cells. After administration, the incidence of these peptides in tumor tissue has gradually reduced, 67 Ga-NOTA-KV6, 67 Ga-NOTA-RV6, and 67 Ga-NOTA-HV6 all reached high tumor/blood ratios and tumor/muscle ratios in 120 minutes, according to a 67 Ga-NOTA-HV6. Overall, the substitution of lysine in SVS-1 with other basic amino acids significantly enhanced its adhesion and internalization into cancer cells, as well as its in vivo pharmacokinetic profile. The sensitivity of these peptides to tumors and their ability to penetrate cancer cell surface membranes make radiolabeled CAPs excellent candidates for use in tumor theranostics.

Source link: https://doi.org/10.3390/cancers13102388


Hemolytic and Antimicrobial Activities of a Series of Cationic Amphiphilic Copolymers Comprised of Same Centered Comonomers with Thiazole Moieties and Polyethylene Glycol Derivatives

By reversible addition-fragmentation chain transfer polymerization, a series of well-defined antimicrobial polymers made up of comonomers bearing thiazole ring and non-hemotoxic poly side chains was synthesized. Polymers were quaternized with either butyl or octyl iodides resulting in cationic amphiphilic copolymers containing thiazolium groups and, accordingly, with a variable hydrophobic/hydrophilic balance variable throughout the length of the alkylating agent. In addition, the molar percentage of PEGMA in the copolymers was modulated, impacting the amphiphilicity. Minimum inhibitory concentration was found to be dependent on both the length of the alkyl hydrophobic chain and the amount of PEGMA in the copolymers. Copolymers that were more hydrophobic were found to be more effective against all test microorganisms. The hemolytic properties of polymers tested against human red blood cells were greatly affected by the copolymers' hydrophobic/hydrophilic balance and PEGMA's content, which significantly reduces hemotoxicity.

Source link: https://doi.org/10.3390/polym12040972

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions

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* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions