<p>Abietane-type diterpene ferruginol, found in the Podocarpaceae, Cupressaceae, Lamiaceae and Verbenaceae families, is a promising natural product with broad spectrum pharmacological effects. The present review summarize an integrated evaluation of the biological effects of ferruginol; anticancer, anti-inflammatory, antioxidant, gastroprotective, antimicrobial, antiparasitic, and antiviral activity based on in vitro, in vivo, and in silico studies. Ferruginol is a multifunctional, highly cytotoxic agent against many different cancerous cell lines through the induction of mitochondrial dysfunction, apoptosis, ROS production, and cell cycle arrest. It has a potent anti-inflammatory effect which is mediated by the inhibition of NF-KB, COX-2, iNOS and pro-inflammatory cytokines and its gastroprotective effect by increasing endogenous prostaglandins, gastric secretions, and antioxidant action. Ferruginol also revealed antimicrobial and antiparasitic effects as it disrupts the membrane integrity, inhibits enzymes, disrupts ergosterol biosynthesis, mitochondrially impairs, and increases ROS. The molecular docking and network pharmacology further identified the major target genes (NR3C1, ESR1/2, PTGS2, AR, SRC) and pathways, such as estrogen signaling, VEGF signaling, serotonergic synapse, and regulation of inflammatory mediators, which support the multi-target therapeutic potential of ferruginol. Together, the existing evidence suggests that ferruginol is a useful bioactive metabolite with good ADME properties and potential to be used as a versatile platform to develop new drugs.</p>

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Ferruginol as multifunctional abietane diterpenoid-comprehensive pharmacological evaluation and computational drug discovery insight

  • Iqra Farzeen,
  • Maryam Batool,
  • Zunaira Jaan,
  • Saira Saeed,
  • Muhammad Muzammil Nazir,
  • Shahla Faisal,
  • Asma Ashraf

摘要

Abietane-type diterpene ferruginol, found in the Podocarpaceae, Cupressaceae, Lamiaceae and Verbenaceae families, is a promising natural product with broad spectrum pharmacological effects. The present review summarize an integrated evaluation of the biological effects of ferruginol; anticancer, anti-inflammatory, antioxidant, gastroprotective, antimicrobial, antiparasitic, and antiviral activity based on in vitro, in vivo, and in silico studies. Ferruginol is a multifunctional, highly cytotoxic agent against many different cancerous cell lines through the induction of mitochondrial dysfunction, apoptosis, ROS production, and cell cycle arrest. It has a potent anti-inflammatory effect which is mediated by the inhibition of NF-KB, COX-2, iNOS and pro-inflammatory cytokines and its gastroprotective effect by increasing endogenous prostaglandins, gastric secretions, and antioxidant action. Ferruginol also revealed antimicrobial and antiparasitic effects as it disrupts the membrane integrity, inhibits enzymes, disrupts ergosterol biosynthesis, mitochondrially impairs, and increases ROS. The molecular docking and network pharmacology further identified the major target genes (NR3C1, ESR1/2, PTGS2, AR, SRC) and pathways, such as estrogen signaling, VEGF signaling, serotonergic synapse, and regulation of inflammatory mediators, which support the multi-target therapeutic potential of ferruginol. Together, the existing evidence suggests that ferruginol is a useful bioactive metabolite with good ADME properties and potential to be used as a versatile platform to develop new drugs.