Garcinol: A novel and potent inhibitor of hyaluronidase enzyme

Int J Biol Macromol. 2024 May;266(Pt 2):131145. doi: 10.1016/j.ijbiomac.2024.131145. Epub 2024 Apr 2.

Abstract

Extracellular matrix (ECM) contains hyaluronic acid (HA) as its integral part that is involved in numerous functional activities within the body. Degradation of HA by hyaluronidase enzyme involved in many pathophysiological conditions such as asthma, arthritis, COPD and in venom spreading during envenomation. Inhibitor of hyaluronidase enzyme has a wide range of application along with the hyaluronan-hyaluronidase system. In this present study, we have evaluated the inhibitory effect of garcinol against hyaluronidase from Hippasa partita spider venom (HPHyal), bovine testicular hyaluronidase (BTH) and human serum hyaluronidase. Garcinia indica fruit rind has been used to isolate the active component garcinol. Garcinol has been used in treatment of diverse ailments. Garcinol has exhibited anti-oxidant, anti-inflammatory, HAT inhibition and miRNA deregulator in development and progression of cancers. Experimental data have shown that garcinol completely inhibited all the three tested hyaluronidase enzymes. The inhibition was found to be non-competitive pattern with reversible type. In the docking study, garcinol with hyaluronidase enzyme has been stabilized by hydrogen bonding and hydrophobic interactions. Thus, garcinol could be a potent novel inhibitor of hyaluronidase enzyme which can be further used for pharmacotherapeutic applications.

Keywords: Garcinia indica; Garcinol; HPHyal; Hippasa partita; Hyaluronidase.

MeSH terms

  • Animals
  • Cattle
  • Enzyme Inhibitors* / chemistry
  • Enzyme Inhibitors* / pharmacology
  • Humans
  • Hyaluronoglucosaminidase* / antagonists & inhibitors
  • Hyaluronoglucosaminidase* / metabolism
  • Molecular Docking Simulation*
  • Terpenes* / chemistry
  • Terpenes* / pharmacology

Substances

  • Hyaluronoglucosaminidase
  • garcinol
  • Terpenes
  • Enzyme Inhibitors