review · Natural Product Research
Gigantol is a naturally occurring bibenzyl compound derived from medicinal plants that exhibits notable anti-inflammatory characteristics. In pre-clinical test systems, the compound lowers levels of pro-inflammatory markers and arachidonic acid metabolites by acting through biological signalling pathways, including NF-kappaB, AKT, PI3K, and JNK/cPLA2/12-LOX. Computational analyses identified the MMP-13 enzyme as the most promising molecular target for gigantol, showing strong binding affinity. In addition, computational profiling of absorption, distribution, metabolism, excretion, and toxicity showed that gigantol meets key physicochemical, pharmacokinetic, and safety requirements. Together, these findings indicate that gigantol possesses appropriate biological activity and pharmacological properties to serve as a candidate for treating inflammatory conditions.
Inflammatory conditions represent a substantial healthcare challenge, driving demand for safer and more effective therapies. Identifying natural compounds that target key inflammatory pathways provides valuable starting points for therapeutic design. By identifying specific enzyme targets and establishing favourable drug-like properties, this research highlights a plant-derived molecule that could contribute to future anti-inflammatory drug discovery.
This work is relevant to pharmaceutical and biotechnology companies developing anti-inflammatory treatments. It identifies gigantol as a potential drug candidate targeting the MMP-13 enzyme. However, the findings are based on literature review, pre-clinical systems, and computational profiling, indicating that the research is at an early discovery stage and requires extensive experimental validation and clinical testing before practical medical use.
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Gigantol, a bibenzyl compound extracted from various medicinal plants, has shown a number of biological activities, making it an attractive candidate for potential medical applications. This systematic review aims to shed light on gigantol's promising role in inflammation treatment and its underlying mechanisms. Gigantol exhibits potential anti-inflammatory properties in pre-clinical pharmacological test systems. It effectively reduced the levels of pro-inflammatory markers and arachidonic acid metabolites through various pathways, such as NF-κB, AKT, PI3K, and JNK/cPLA2/12-LOX. The in-silico investigations demonstrated that the MMP-13 enzyme served as the most promising target for gigantol with highest binding affinity (docking score = -8.8 kcal/mol). Encouragingly, the absorption, distribution, metabolism, excretion, and toxicity (ADMET) analysis of gigantol confirmed its compatibility with the necessary physiochemical, pharmacokinetic, and toxicity properties, bolstering its potential as a drug candidate. Gigantol, with its well-documented anti-inflammatory properties, could be a promising agent for treating inflammation in the near future.
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DOI: 10.1080/14786419.2024.2340042
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