Drug intelligence / Profile preview

puberulic acid

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Subcutaneous
01

Overview

**Puberulic acid** is a highly oxygenated tropolone derivative (C8H6O6; MW: 198.13) produced as a secondary metabolite by several Penicillium species, including Penicillium puberulum and Penicillium aurantiovirens[2][4][8]. It has been investigated as a potential **antimalarial** agent due to potent in vitro and in vivo efficacy against Plasmodium falciparum and other malaria parasites, with an IC50 as low as 0.044–0.05 μM[5][6][10]. However, puberulic acid is also strongly cytotoxic, causing nephrotoxicity (renal proximal tubule injury) in animal models and cultured human renal cells, and has been implicated in cases of food poisoning due to contamination of red yeast rice supplements[1][3][7]. Its cytotoxicity appears connected to inhibition/interaction with organic anion transporters (OAT1), interfering with renal cell transport functions[1]. Efforts are underway to develop less toxic derivatives for therapeutic use[5][3].

Other names
puberulic acidpuberulonate
02

Targets

MIOXSLC5A3 (Sodium/myo-inositol cotransporter 1 (SMIT1))SLC5A11 (Sodium-coupled myo-inositol transporter 2 (SMIT2))OAT1 (Organic anion transporter 1)

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