Chloropeptins, New Anti-HIV Antibiotics Inhibiting gp120-CD4 Binding from Streptomyces sp: I. Taxonomy, Fermentation, Isolation, and Physico-chemical Properties and Biological Activities

Chloropeptins I and II, which are gp120-CD4 binding inhibitors, were isolated as pale yellow-brown powders from the mycelia of a soil actinomycete, Streptomyces sp. WK-3419. Their physico-chemical properties showed that they are chlorinated pep tides. Chloropeptin I (C61H45N7O15Cl6) is a novel compo...

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Bibliographic Details
Published in:Journal of antibiotics 1997/01/25, Vol.50(1), pp.58-65
Main Authors: TANAKA, HARUO, MATSUZAKI, KEIICHI, NAKASHIMAC, HIDEKI, OGINO, TOMOAKI, MATSUMOTO, ATSUKO, IKEDA, HODAKA, WOODRUFF, H. BOYD, OMURA, SATOSHI
Format: Article
Language:English
Subjects:
AIDS/HIV
Anti-Bacterial Agents - isolation & purification
Anti-Bacterial Agents - pharmacology
Anti-HIV Agents - isolation & purification
Anti-HIV Agents - pharmacology
Antibiotics, microbial producers, chemotherapic agents, antiseptics, disinfecting agents
Applied microbiology
Biological and medical sciences
CD4-Positive T-Lymphocytes - metabolism
Chemotherapic agents
Chlorophenols - isolation & purification
Chlorophenols - pharmacology
Fermentation
Fundamental and applied biological sciences. Psychology
HeLa Cells
HIV Envelope Protein gp120 - metabolism
human immunodeficiency virus
Humans
Microbiology
Oligopeptides - isolation & purification
Oligopeptides - pharmacology
Peptides, Cyclic
Streptomyces
Streptomyces - classification
Streptomyces - metabolism
Zidovudine - pharmacology
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Summary:Chloropeptins I and II, which are gp120-CD4 binding inhibitors, were isolated as pale yellow-brown powders from the mycelia of a soil actinomycete, Streptomyces sp. WK-3419. Their physico-chemical properties showed that they are chlorinated pep tides. Chloropeptin I (C61H45N7O15Cl6) is a novel compound, but chloropeptin II was identified as complestatin. Both compounds inhibited gp120-CD4 binding (IC50: 1.3 and 2.0 μM, respectively), the cytopathic effect of HIV in MT-4 cells (EC50: 1.6 and 1.7 μM, respectively) and syncytium formation in co-cultured HIV-1-infected and uninfected MOLT-4 cells (IC50: 0.5 and 1.1 μM, respectively). Chloropeptin I was synergistic in the inhibition of the cytopathic effect when combined with other anti-HIV drugs such as zidovudine (AZT), didanosine (ddl), zalcitabine (ddC) and nevirapine.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.50.58