Multi-biphenyl aromatic hydrocarbon-based polypeptide conjugate and preparation method and application thereof
A technology for polybiphenyl aromatic hydrocarbons and biphenyl aromatic hydrocarbons, which is applied in the field of antibacterial conjugates and biomedicine, can solve the problems of low hemolytic toxicity, sensitivity, complicated manufacturing method, etc., achieves good biocompatibility, reduces hemolytic toxicity, and is suitable for The effect of promotion
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Embodiment 1
[0059] In this example, the synthesis method of the biphenyl-polypeptide conjugate is as follows:
[0060] A kind of synthesis of alkynyl substituted biphenyls, the method is as follows:
[0061] n=0,1,2
[0062] When n=0, the corresponding compound 1 is 2,2'-dimethoxybiphenyl, the corresponding compound 2 is named 2,2'-BP-OH, and the corresponding compound 3 is named 2,2'-BP -yn;
[0063] When n=1, the corresponding compound 1 is 2,2"-dimethoxyterphenyl, the corresponding compound 2 is named 2,2"-TP-OH, and the corresponding compound 3 is named 2,2"-TP -yn;
[0064] When n=2, the corresponding compound 1 is 2,2"'-dimethoxyquaterphenyl, the corresponding compound 2 is named 2,2"'-QP-OH, and the corresponding compound 3 is named 2,2 "'-QP-yn.
[0065] The following preparation of alkynyl-substituted polybiphenyl arene is an example of alkynyl-substituted biphenyl arene (n=0), and other preparation methods are similar to alkynyl quaterphenyl arene, and the specific steps ...
Embodiment 2
[0082] In this example, the in vitro antibacterial activity of the conjugate was evaluated as follows:
[0083] 1. Test sample
[0084] The conjugate was prepared by the method of Example 1.
[0085] Two freeze-dried strains of S.aureus (ATCC 25923) and E.coli (ATCC 25922) were purchased from Shanghai Fuxiang Biotechnology Co., Ltd.
[0086] 2. Test method
[0087] Bacterial recovery and culture: Take out the strains frozen at -20°C, streak inoculate them in solid medium, and incubate for 18h (37°C, 180r / min). Afterwards, 2-3 single colonies were picked out with a sterilization loop and placed in a 10 mL centrifuge tube filled with 5 mL of nutrient broth, and incubated for 18 hours with constant temperature shaking (37°C, 180r / min). Take it out and inoculate it into fresh broth, cultivate it for 5 hours until the bacteria are in logarithmic growth, adjust it to 0.5 McFarland turbidimetric standard with nutrient broth, and then dilute it at 1:1000 for later use.
[0088] De...
Embodiment 3
[0096] In this example, the toxicity evaluation method of the conjugate is as follows:
[0097] 1. Experimental samples
[0098] The conjugate was prepared by the method of Example 1.
[0099] Mouse fibroblast L929 was provided by Peking Union Medical College Cell Bank, and human red blood cells were provided by the Fifth Medical Center of PLA General Hospital.
[0100] 2. Test method
[0101] Cell culture: DMEM medium (containing 10% FBS, 1% penicillin / streptomycin) for L929 cells in 5% CO 2 , cultivated at a constant temperature of 37°C. Collect the cells grown in the logarithmic phase, adjust the concentration of the cell suspension, inoculate the cell suspension in a 96-well plate, plate the cell density to be about 10000 / well, 100 μL of the cell suspension per well, in 5% CO 2 , and incubated at a constant temperature of 37°C for 24h, ready to use.
[0102] Preparation of human red blood cell suspension: Take 4mL of heparin-anticoagulated human blood in a 10mL centri...
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