期刊
CHEMISTRY & BIOLOGY
卷 20, 期 8, 页码 1022-1032出版社
CELL PRESS
DOI: 10.1016/j.chembiol.2013.06.014
关键词
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资金
- Spanish Ministry of Science and Innovation [BIO2009-07643]
- Plan Regional de Investigacion del Principado de Asturias [PC10-05]
- Spanish Ministry of Science and Innovation (MICINN, FPI)
Collismycin A is a member of the 2,2'-bipyridyl family of natural products that shows cytotoxic activity. Structurally, it belongs to the hybrid polyketides-nonribosomal peptides. After the isolation and characterization of the collismycin A gene cluster, we have used the combination of two different approaches (insertional inactivation and biocatalysis) to increase structural diversity in this natural product class. Twelve collismycin analogs were generated with modifications in the second pyridine ring of collismycin A, thus potentially maintaining biologic activity. None of these analogs showed better cytotoxic activity than the parental collismycin. However, some analogs showed neuroprotective activity and one of them (collismycin H) showed better values for neuroprotection against oxidative stress in a zebrafish model than those of collismycin A. Interestingly, this analog also showed very poor cytotoxic activity, a feature very desirable for a neuroprotectant compound.
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