Molnár J, Földeák S, Nakamura M J, Rausch H, Domonkos K, Szabó M
Institute of Microbiology, Albert Szent-Györgyi Medical University, Szeged, Hungary.
APMIS Suppl. 1992;30:24-31.
The antiplasmid activity of tricyclic compounds, e.g. phenothiazines, dibenzoazepines, dibenzocykloheptene derivatives and some stereoisomers, was shown on E. coli in vitro. Some ring-substituted phenothiazine and cannabis derivatives had only an antibacterial effect. Promethazine, a selected phenothiazine, cured antibiotic resistance and lactose fermentation of E.coli, tumour inducing ability of Agrobacterium tumefaciens and nodule formation of Rhizobium meliloti. Plasmids of different E.coli strains were eliminated with varying frequency. The antiplasmid activity of the compounds can be due to the increased membrane permeability. Inhibition of DNA gyrase and complex formation with the supercoiled form of plasmid DNA can lead to the cessation of plasmid replication in the bacterial cells. In addition, in vivo plasmid curing was demonstrated at a low frequency.
三环化合物，如吩噻嗪、二苯并氮杂䓬、二苯并环庚烯衍生物及一些立体异构体，在体外对大肠杆菌显示出抗质粒活性。一些环取代吩噻嗪和大麻衍生物仅具有抗菌作用。选定的吩噻嗪异丙嗪可消除大肠杆菌的抗生素抗性和乳糖发酵、根癌土壤杆菌的肿瘤诱导能力以及苜蓿根瘤菌的结瘤形成。不同大肠杆菌菌株的质粒以不同频率被消除。这些化合物的抗质粒活性可能归因于膜通透性的增加。抑制DNA促旋酶以及与质粒DNA的超螺旋形式形成复合物可导致细菌细胞中质粒复制的停止。此外，在体内也证实了低频的质粒消除。
