PUBLICATION

Discovery of specific activity of 2-hydroxypentanoic acid acting on the mPR alpha (Paqr7) from the marine algae Padina

Authors
Amin, M.T., Acharjee, M., Sarwar Jyoti, M.M., Rezanujjaman, M., Hassan, M.M., Hossain, M.F., Ahamed, S., Kodani, S., Tokumoto, T.
ID
ZDB-PUB-250209-9
Date
2025
Source
Biochemical and Biophysical Research Communications   751: 151433151433 (Journal)
Registered Authors
Tokumoto, Toshinobu
Keywords
2-Hydroxypentanoic acid, Antagonist, Marine algae, Membrane progesterone receptor, Oocyte maturation, Padina
MeSH Terms
  • Zebrafish
  • Humans
  • Oocytes/drug effects
  • Oocytes/metabolism
  • Receptors, Progesterone*/antagonists & inhibitors
  • Receptors, Progesterone*/metabolism
  • Animals
  • Female
PubMed
39922053 Full text @ Biochem. Biophys. Res. Commun.
Abstract
Membrane progesterone receptors (mPRs) are members of the progestin and adipoQ (PAQR) receptor family that are stimulated by endogenous steroids to initiate rapid intracellular signaling through a nongenomic pathway. Previously, water-soluble compounds with mPRα binding activity from the marine algae Padina arborescens were fractionated by HPLC. Nuclear magnetic resonance spectroscopy revealed that the major component of the HPLC fraction was 2-hydroxypentanoic acid (2-HPA). In this study, the physiological activity of 2-HPA and its analogues was investigated using in vitro goldfish and in vivo zebrafish oocyte maturation and ovulation assays. Only 2-HPA showed inhibitory activity on oocyte maturation and ovulation of fish oocytes. The inhibitory activity of 2-HPA was compared between S- and R-type 2-HPA. The results showed that both types had the same level of activity. Furthermore, the interaction of 2-HPA with mPRα was analyzed by binding assay. 2-HPAs showed a substantial competitive binding affinity for the human membrane progesterone receptor α (hmPRα) in the graphene quantum dots (GQDs)-hmPRα binding assay. In contrast, synthetic structural analogues of 2-HPA showed no competitive binding activity. These results indicate that 2-HPA is a novel mPRα antagonist, and its chemical structure is highly restricted to show its activity.
Genes / Markers
Figures
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Antibodies
Orthology
Engineered Foreign Genes
Mapping