In Vitro and in Vivo Antimalarial Activities of a Non-glycosidic 18-Membered Macrolide Antibiotic, Borrelidin, against Drug-resistant Strains of Plasmodia

In vitro and in vivo antimalarial activity of puberulic acid and its new analogs, viticolins A–C, produced by Penicillium sp. FKI-4410

“…[3][4][5][6][7][8] Recently, we have isolated some tropolone compounds from a culture broth of Penicillium sp. FKI-4410.…”

Borrelidin, a potent antimalarial: stage-specific inhibition profile of synchronized cultures of Plasmodium falciparum

“…[3][4][5][6][7][8] In the course of our screening, we found borrelidin, produced by an actinomycete strain OM-0060, that proved to be more potent than chloroquine or artemether (using in vivo oral administration) against drug-resistant P. yoelii. 6 The reported biological activities of borrelidin are suggested to be the results of protein synthesis inhibition, caused by the effect on threonyl-tRNA synthetase. 9 Borrelidin is also known to inhibit yeast (Saccharomyces cerevisiae) cyclin-dependent kinase (CDK), where the target is cdc28/cln2 complex formation.…”

In vitro and in vivo antiprotozoal activities of bispolides and their derivatives

“…We have previously reported various microbial metabolites exhibiting potent antimalarial [1][2][3][4] and antitrypanosomal properties. [5][6][7] We have recently found that the known 20-membered ring macrodiolide antibiotics, the bispolides, 8 together with new derivatives, exhibit selective antitrypanosomal and potent antimalarial activities, both in vitro and in vivo.…”