Morozova Elena, Kulikova Vitalia, Koval Vasily, Anufrieva Natalya, Chernukha Marina, Avetisyan Lusine, Lebedeva Lada, Medvedeva Olga, Burmistrov Egor, Shaginyan Igor, Revtovich Svetlana, Demidkina Tatyana
Engelhardt Institute of Molecular Biology of the Russian Academy of Sciences, Vavilov str. 32, Moscow 119991, Russia.
National Research Center for Epidemiology and Microbiology Named after the Honorary Academician N. F. Gamaleya, Healthcare Ministry of Russia, Gamalei st. 18, Moscow 123098, Russia.
ACS Omega. 2020 Apr 2;5(14):7782-7786. doi: 10.1021/acsomega.9b03555. eCollection 2020 Apr 14.
Lung disease caused by is the leading reason for death in cystic fibrosis patients. Therapeutic efficacy of the pharmacological pairs, the naked/encapsulated mutant form of methionine γ-lyase and the substrates, sulfoxides of S-substituted l-cysteine, generating thiosulfinates, was evaluated on the murine model of experimental sepsis caused by the multidrug-resistant 203-2 strain. The pairs containing the naked enzyme and substrates did not have antibacterial activity. The treatment of mice with the pair encapsulated enzyme and -methyl-l-cysteine sulfoxide, generating dimethyl thiosulfinate, led to a complete recovery of the animals of the model, with the infecting dose equal to LD. The pair generating diallyl thiosulfinate (allicin) proved to be less effective. So, the substituents, attached to the thiosulfinate moiety, affect the antibacterial activity of thiosulfinates against .
由……引起的肺部疾病是囊性纤维化患者死亡的主要原因。在由多重耐药的203 - 2菌株引起的实验性败血症小鼠模型上,评估了药理学组合(甲硫氨酸γ-裂合酶的裸型/包封突变形式与底物,即S-取代的L-半胱氨酸的亚砜,生成硫代亚磺酸盐)的治疗效果。含有裸酶和底物的组合没有抗菌活性。用包封酶与生成二甲基硫代亚磺酸盐的甲基-L-半胱氨酸亚砜组合治疗小鼠,导致模型动物完全康复,感染剂量等于半数致死量。生成二烯丙基硫代亚磺酸盐(大蒜素)的组合效果较差。因此,连接到硫代亚磺酸盐部分的取代基会影响硫代亚磺酸盐对……的抗菌活性。