Polygodial is a sesquiterpene dialdehyde compound with bactericidal rather than bacteriostatic properties. Polygodial has broad-spectrum antibacterial effects, especially against yeast and filamentous microorganisms. Polygodial's antibacterial effect is pH-dependent. Polygodial showed no antifungal activity against Saccharomyces cerevisiae, Candida utilis, Schizosaccharomyces pombe, or Hansenula anomala at pH 7.0 even at 25μg/mL, whereas its activity increased at acidic pH and was effective at 0.2μg/mL and 0.78μg/mL against Saccharomyces cerevisiae and Candida utilis, respectively, at pH 3.1. Polygodial exerts its activity by targeting the cytoplasmic membrane and disrupting organelles, leading to lethal leakage of intracellular components such as proteins and carbohydrates[1].
In vitro, Polygodial (0-100µM; 6d) were not toxic to hepatocytes and 3T3-J2 fibroblasts[2]. Polygodial (0-50μM; 24-72h) dose-dependently inhibited the viability of Taxane-Resistant castration-resistant prostate cancer (CRPC; PC3-TXR and DU145-TXR), with IC50 values of approximately 20μM in both cell lines[2]. Polygodial (5-20μM; 1-3w) substantially decreased the number of colonies in PC3-TXR and DU145-TXR cell lines in a concentration-dependent manner[2]. Polygodial (5-50μM; 24-72h) inhibited migration in PC3-TXR and DU145-TXR cell lines in a concentration-dependent manner[2]. Polygodial (5-50μM; 48h) induced apoptosis in PC3-TXR and DU145-TXR cell lines in a concentration-dependent manner[2].
In vivo, Polygodial (0.1-10mg/kg; i.p.; 0.5h) dose-dependently and almost completely inhibited acetic acid-, zymosan-, and kaolin-induced abdominal constrictions in male Swiss mice, with ID50 values of 0.8, 2.1, and 2.6mg/kg and maximal inhibitions of 90%, 97%, and 98%, respectively[3].
References:
[1] Kubo, I, and M Taniguchi. “Polygodial, an antifungal potentiator.” Journal of natural products vol. 51,1 (1988): 22-9.
[2] Venkatesan R, Hussein MA, Moses L, Liu JS, Khetani SR, Kornienko A, Munirathinam G. Polygodial, a Sesquiterpene Dialdehyde, Activates Apoptotic Signaling in Castration-Resistant Prostate Cancer Cell Lines by Inducing Oxidative Stress. Cancers. 2022; 14(21):5260.
[3] Mendes, G L et al. “Anti-hyperalgesic properties of the extract and of the main sesquiterpene polygodial isolated from the barks of Drymis winteri (Winteraceae).” Life sciences vol. 63,5 (1998): 369-81.