RATIONALLY DESIGNED LAWSONE DERIVATIVES AS ANTIMICROBIALS AGAINST MULTIDRUG-RESISTANT STAPHYLOCOCCUS AUREUS

    公开(公告)号:US20220273586A1

    公开(公告)日:2022-09-01

    申请号:US17637581

    申请日:2020-08-26

    摘要: Naphthoquinone derivatives of Lawsone have been found to be effective against Staphylococcus aureus and methicillin resistant Staphylococcus aureus (MRSA). Such compounds generally contain a substituent group at the 3-position of a specific naphthoquinone compound, i.e. 2-hydroxy-1,4-naphthoquinone. One of these derivatives referred to as compound 6c in the series exhibits potent antimicrobial activity that is comparable to that of the two commercial antibiotics ofloxacin and ciprofloxacin against the two strains of methicillin sensitive Staphylococcus aureus (MSSA; ATCC 29213 and ATCC 6538). In the case of two strains of MRSA (ATCC BAA-44 and ATCC BAA-1717) that have developed drug resistance to both ofloxacin and ciprofloxacin, the antimicrobial activity of 6c can almost rival that of vancomycin and daptomycin. Furthermore, 6c is also effective against vancomycin-intermediate and daptomycin non-susceptible strain of MRSA (ATCC 700699). Besides the efficacy, 6c has a much improved drug resistance profile in comparison with the conventional antibiotics.

    NANO-PARTICULATE COMPOSITIONS FOR STIMULATING HOST INNATE IMMUNE RESPONSES FOR THERAPEUTIC APPLICATIONS

    公开(公告)号:US20220409576A1

    公开(公告)日:2022-12-29

    申请号:US17765262

    申请日:2020-11-18

    摘要: Novel biocompatible Fenton-catalytic nano-particulate composites preferably based on nanoparticle (NP)-based catalysts, one or more reducing agents, and one or more peroxide compounds are formulated to take advantage of their ability to stimulate bactericidal as well as anti-tumor immune response by means of eliciting the generation of reactive oxygen species (ROS) in immune cells, in particular, in macrophages. The therapeutic composition can serve as a treatment for wound infections by, but not limited to, Staphylococcus aureus, Pseudomonas aeruginosa, Staphylococcus epidermidis, Klebsiella pneumoniae, and Acinetobacter baumannii, as a wound/lesion dressing that provide an anti-bacterial immune environment for the accelerated wound healing. In a similar principle, the therapeutic composition can serve as a treatment for solid tumors by providing an anti-tumor immune environment that inhibits tumor growth.