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本文运用“违法传送”概念,根据白念珠菌对寡肽的传送特点,设计并合成了十个含L-4-氧代赖氨酸(以下称I-677)的寡肽,以提高I-677的抗白念珠菌活性。体外抗白念珠菌试验表明:I-677-肽(I-677-X_1,I-677-X_1-X_2和I-677-X_1-X_2-Gly,其中X_1,X_2=Met,Leu,Ile,Ala,β-Ala,Gly)较I-677单体摩尔活性提高了2.1～28倍,其摩尔最低抑菌浓度为8.7×10~(-8)～9.3×10~(-9)mol/ml,传送肽和赖氨酸分别逆转I-677-肽抗菌活性的实验结果证实了I-677的“违法传送”途径。
In this paper, we use the concept of “illegal transmission” to design and synthesize ten oligopeptides containing L-4-oxo-lysine (hereinafter referred to as I-677) according to the transmission characteristics of Candida albicans on oligopeptides, 677 against Candida albicans activity. In vitro anti-Candida albicans tests showed that I-677-peptide (I-677-X_1, I-677-X_1-X_2 and I-677-X_1-X_2-Gly with X_1, X_2 = Met, Leu, Ile, Ala , β-Ala, Gly) was 2.1 ~ 28 times higher than that of I-677, and its minimum inhibitory concentration was 8.7 × 10 -8 ~ 9.3 × 10 -9 mol / ml. Experimental results of the delivery of peptide and lysine, respectively, to reverse the antibacterial activity of I-677-peptide confirm the “illegal delivery” pathway of I-677.