Some structural requirements for the antibiotic action of distamycins

Prakash, Chandra; Götz, A.; Wacker, A.; Verini, M.A.; Casazza, Anna Maria; Fioretti, A.; Arcamone, Federico; Ghione, M

doi:10.1016/0014-5793(71)80362-9

Cited by 31 publications

(10 citation statements)

References 8 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…b) The nature of the variable sidechain has an additional importance in the antiviral activity as it was found that Distamycin A is more effective than its derivative compound II [ 1, 21. This conclusion is in agreement with the findings of Chandra et al [8] that the antiviral activity of Distamycins and their action on the template activity of DNA are dependent on the number of pyrrole rings and that the sidechain l-methyl-pyrrole-2carboxamide (present in Distamycin A and compound XIII) might be involved in the binding of the antibiotic to DNA…”

Section: Discussionsupporting

confidence: 93%

Effect of distamycin A and congocidine on DNA synthesis by rous sarcoma virus reverse transcriptase

Kotler

Becker

1972

FEBS Letters

View full text Add to dashboard Cite

Section: Discussionsupporting

confidence: 93%

Effect of distamycin A and congocidine on DNA synthesis by rous sarcoma virus reverse transcriptase

Kotler

Becker

1972

FEBS Letters

View full text Add to dashboard Cite

“…It might be noted that the CC 50 value found on Vero cells in the present study falls at the low extreme of the range of CC 50 values reported in the literature. In fact, available data show CC 50 values ranging from 35 M in a Hep-2 cell line [28] to 154 M in a HeLa cell line [16] and 385 M in rabbit primary kidney cells [29] . ACV sensitivity assays confirmed the occurrence of ACV-resistant strains among transplanted patients.…”

Section: Discussionmentioning

confidence: 99%

“…Cytotoxicity of free and liposomal DA is unlikely to represent an impediment to the development of a topical formulation of the drug. It has been reported that cytotoxicity of DA may reach 154 M in human cells (HeLa cell line) [16] and 385 M in rabbit primary kidney cells, in other experimental conditions [29] , increasing the DA therapeutic index. Moreover the reported DA CC 50 values on human cells are far from the drug concentration required for antiviral activity.…”

Section: Discussionmentioning

confidence: 99%

“…DNA sequence reading agents [14] . The antiviral activity of DA against prototype strains of herpesvirus in cell culture has been reported [15][16][17] . No effect was shown on total protein or DNA synthesis or on DNA polymerase levels in HeLa cell cultures infected with the HF strain of HSV (ATCC) in the presence of DA concentrations that reduced by more than two orders of magnitude the production of infectious virus [18] .…”

Section: In Vitro Antiviral Activity Of Distamycinmentioning

confidence: 99%

See 1 more Smart Citation

In vitro Antiviral Activity of Distamycin A against Clinical Isolates of Herpes Simplex Virus 1 and 2 from Transplanted Patients

Matteoli

Bernardini²,

Iuliano³

et al. 2008

Intervirology

View full text Add to dashboard Cite

Objective(s): Herpes simplex virus (HSV) infections in immunocompromised individuals may require prolonged antiviral therapy resulting in the emergence of viral strains resistant to the currently employed antiviral drugs. Distamycin A (DA), a basic antibiotic belonging to the lexitropsin DNA minor groove binding drugs, exhibits antiviral properties. In this study we evaluated the in vitro cytotoxicity and antiviral activity of DA against HSV type 1 and HSV type 2 clinical isolates from transplanted patients and compared them with those of acyclovir (ACV) in search of alternative antiviral drugs. Methods: Viral detection and typing was performed by multiplex PCR and immunofluorescence assay; the in vitro cytotoxicity of DA and the antiviral activity of ACV and DA was evaluated respectively by neutral red uptake assay and plaque reduction assay for HSV2 isolates and fluorescence reduction assay for HSV1 isolates. Results: Tissue culture 50% cytotoxic concentration of DA was 58 µM. Tissue culture 50% inhibitory concentration values ranged from 0.16 to 7.4 µM for the ACV-sensitive and from 5.4 to 32 µM for the ACV-resistant viral strains. Conclusions: In spite of the lower activity against ACV-resistant strains, DA may be used as an antiherpetic drug.

show abstract

“…Cytotoxic activity, like cytostatic and antiviral activity, requires specific structural entities in a molecule [4][5][6][7]. All these activities may be derived from the same structural moiety, or various parts of the molecule may be responsible for them.…”

Section: Ntroduetionmentioning

confidence: 99%

Tilorone hydrochloride: The drug profile

Prakash¹,

Wright²

Medicinal Chemistry

View full text Add to dashboard Cite

Some structural requirements for the antibiotic action of distamycins

Cited by 31 publications

References 8 publications

Effect of distamycin A and congocidine on DNA synthesis by rous sarcoma virus reverse transcriptase

Effect of distamycin A and congocidine on DNA synthesis by rous sarcoma virus reverse transcriptase

In vitro Antiviral Activity of Distamycin A against Clinical Isolates of Herpes Simplex Virus 1 and 2 from Transplanted Patients

Tilorone hydrochloride: The drug profile

Contact Info

Product

Resources

About