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In this study, we designed and synthesized 12 novel aloperine derivatives with different core structures. Among them, compound 3 with a ten-membered ring core was obtained through a special ring expansion reaction after γ-H Huffman elimination of quaternary ammonium salt, and the structure was verified by X-single crystal diffraction. Furthermore, their antiviral activity against human β-coronavirus HCoV-OC43 was evaluated by CCK-8 assay. Quaternary ammonium salt 2a and 3 had a good inhibitory effect against HCoV-OC43, and 2a had the highest anti-HCoV-OC43 activity with an EC50 values of 3.77 μmol·L-1 and a SI value of over 53.1. Schrӧdinger molecular docking results showed that both 2a and 3 might display their anti-HCoV-OC43 activity by directly acting on host TMPRSS2 and SR-B1. The results expanded the structural types of endocyclic aloperine and the function against coronavirus, and provided useful scientific data for the development of pharmaceutical applications of these compounds.
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OBJECTIVE@#This investigation aimed to develop a novel antibacterial dental adhesive containing nanoantibacterial inorganic fillers and measure the dentin bonding strength, mechanical properties, and antibacterial property of the novel adhesive in vitro.@*METHODS@#Novel nanoantibacterial inorganic fillers containing quaternary ammonium salt with long chain alkyl were synthesized on the basis of previous research. These novel nanoantibacterial inorganic fillers were added into the dental adhesive to prepare novel nanoantibacterial dental resin composite at mass fractions of 0%, 2.5%, 5.0%, 7.5%, and 10%; 0% was used as control. Dentin shear bonding test was used to evaluate the bonding strength. Flexural test was utilized to measure the novel resin composite flexural strength and elastic modulus. A dental plaque microcosm biofilm model with human saliva as inoculum was formed. Colony forming unit, lactic acid production, and live/dead assay of the biofilm on novel dental adhesive were calculated to assess the effect of novel dental adhesive on human dental plaque microcosm biofilm.@*RESULTS@#The dentin shear bond strength, flexural strength, and elastic modulus were 28.9 MPa, 86.6 MPa, and 4.2 GPa, respectively, when the nanoantibacterial inorganic filler mass fraction in the dental adhesive reached approximately 5.0%. Consequently, the dentin shear bond strength and mechanical properties significantly increased. Addition of 2.5% nanoantibacterial inorganic fillers into the dental adhesive exerted no adverse effect on the mechanical properties significantly (P>0.05). Dental adhesive containing 5% or more nanoantibacterial inorganic fillers inhibited the metabolic activity of the dental plaque microcosm biofilm significantly, thereby displaying a strong antibacterial potency (P<0.05).@*CONCLUSIONS@#This novel antibacterial dental adhesive, which contained 5.0% nanoantibacterial inorganic filler, exhibited promising bonding strength, mechanical property, and antibacterial ability. Hence, this adhesive can be potentially used in caries inhibition in dental application.
Subject(s)
Humans , Anti-Bacterial Agents , Biofilms , Dental Bonding , Dental Cements , Dental Plaque , Materials Testing , Methacrylates , Resin Cements , Shear StrengthABSTRACT
Objective To explore the possibities of routine disinfection for prosthetic sockets. Methods From June to August, 2016, 19 lower limbs prosthesis wearers wiped their prosthetic socket surfaces and sprayed the stump socks with a compound of quaternary ammoni-um salt every night for three weeks. Meanwhile, field investigation and sampling were carried out weekly. Staphylococcus aureus, Pseudo-monas aeruginosa, Escherichia Coli and Candida albicans were isolated and identified, and colony counting was carried out. Results After disinfection, the number of bacteria on the prosthetic socket reduced 1.8-3.0 log, and the number of fungi reduced 1.6-1.9 log. One strain of Staphylococcus aureus and one strain of Escherichia Coli were isolated before disinfection and one strain of Pseudomonas aeruginosa was isolated after disinfection. Eczema and itching symptoms relieved or disappeared and deodorant effect was distinguished after continuous disinfection. Conclusion Disinfection on prosthetic sockets with compound of quaternary ammonium salt may control the microbial contam-ination and odor, reduce the incidence of eczema and other skin diseases.
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OBJECTIVE To compare the disinfection effect of 3MTM object surface disinfectant(3M disinfectant) with that of chlorine-containing disinfectants in ICU environment. METHODS The floor, instrument panel board, ward bed tables,computer key boards and telephone keyings were sampled respectively before disinfection, 15 minutes and 4 hours after disinfetion in six ICUs. The bactericide rate of 3M disinfectant and chlorine-containing was compared. RESULTS In the 96 specimens collected, 26 from ward bed tables(48.15%)and 22 from instrument panel board, computer key boards and telephone keyings (26.83%)excede the standard of Ministry of Health(