Description
Borrelidin is a macrolide antibiotic initially produced by Streptomyces. Borrelidin exhibits anti-parasitic, antifungal, anticancer, and anti-angiogenic activities. This compound inhibits threonyl-tRNA synthetase/ligase, inhibiting growth and survival of Trypanosoma, Plasmodium, and Phytophthora. In acute lymphocytic leukemia (ALL) cells, borrelidin induces G1 phase cell cycle arrest, induces apoptosis, and inhibits proliferation. In endothelial cells, borrelidin inhibits formation of new capillary tubes and collapses pre-formed capillary tubes, inducing threonine- and caspase-dependent apoptosis.
References
Kalidas S, Cestari I, Monnerat S, et al. Genetic validation of aminoacyl-tRNA synthetases as drug targets in Trypanosoma brucei. Eukaryot Cell. 2014 Apr;13(4):504-16. PMID: 24562907.
Azcárate IG, Marín-García P, Camacho N, et al. Insights into the preclinical treatment of blood-stage malaria by the antibiotic borrelidin. Br J Pharmacol. 2013 Jun;169(3):645-58. PMID: 23488671.
Gao YM, Wang XJ, Zhang J, et al. Borrelidin, a potent antifungal agent: insight into the antifungal mechanism against Phytophthora sojae. J Agric Food Chem. 2012 Oct 3;60(39):9874-81. PMID: 22967236.
Habibi D, Ogloff N, Jalili RB, et al. Borrelidin, a small molecule nitrile-containing macrolide inhibitor of threonyl-tRNA synthetase, is a potent inducer of apoptosis in acute lymphoblastic leukemia. Invest New Drugs. 2012 Aug;30(4):1361-70. PMID: 21678129.
Otoguro K, Ui H, Ishiyama A, et al. In vitro and in vivo antimalarial activities of a non-glycosidic 18-membered macrolide antibiotic, borrelidin, against drug-resistant strains of Plasmodia. J Antibiot (Tokyo). 2003 Aug;56(8):727-9. PMID: 14563165.
