Bleomycins

Bleomycins are glycopeptide compounds originally isolated from Streptomyces verticillus that demonstrate strong anticancer and antibiotic activity. Bleomycin Sulfate (Aladdin B107423 1.5-2.0 units/mg, B408760 10mM in DMSO), a mixture of bleomycin species, contains the major components used in clinical formulations. Bleomycin is widely applied in oncology for the treatment of squamous cell carcinoma, testicular cancer, and Hodgkin lymphoma, and is a key drug in the ABVD chemotherapy protocol.

The therapeutic action of bleomycin is primarily due to its ability to induce DNA strand breaks and inhibit thymidine incorporation into DNA. Structurally, bleomycin contains two critical domains: a bithiazole region that facilitates DNA binding, and a metal-binding site. At the latter, bleomycin can chelate iron, generating reactive oxygen species that promote DNA cleavage. In addition, bleomycin may directly interact with DNA, abstracting hydrogen atoms from nucleotide bases and thereby producing strand scission.

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