Anti-Inflammatory Effects of Pyrroloquinoline Quinone (PQQ)

Pyrroloquinoline quinone (PQQ) is a small-molecule active substance naturally found in fermented soybean products, fruits, vegetables and human breast milk.

It was approved as a novel dietary supplement ingredient by the European Food Safety Authority (EFSA) in 2018.

In recent years, numerous in vitro and animal studies have investigated its cytoprotective properties at the cellular level, with redox regulation and modulation of inflammation-related signaling pathways serving as the core research focuses.

Unique Properties of PQQ

In terms of molecular structure, PQQ is classified as a tricyclic aromatic orthoquinone and features reversible redox cycling capacity, which constitutes its distinctive physicochemical characteristic.

Compared with other quinone bioactive compounds, its free radical scavenging efficiency is 100 to 1,000 times higher.

In addition, it resists auto-oxidation and deactivation via polymerization, enabling sustained electron transfer activity.

Inside cells, PQQ binds to aryloxyl radicals and peroxyl radicals to alleviate damage to cellular structures caused by the accumulation of reactive oxygen species (ROS).

Meanwhile, acting as a cofactor for lactate dehydrogenase, it participates in carbohydrate and lipid energy metabolism and helps maintain the normal cellular oxidative balance.

Promotion of Mitochondrial Biogenesis

Modern research has demonstrated that excessive ROS accumulation is frequently accompanied by dysregulation of local signaling molecules in the body, creating a mutually exacerbating vicious cycle, which is particularly prominent under conditions such as obesity, sedentary lifestyles and high-intensity exercise.

Relevant experiments have proven that PQQ modulates the associated signaling networks through multiple pathways:

on the one hand, it activates the endogenous Keap1/Nrf2 homeostatic pathway to enhance the cellular intrinsic capacity for regulating oxidative homeostasis;

on the other hand, it downregulates the activity of signaling cascades including NF-κB and NLRP3, reduces the secretion of inflammatory mediators such as TNF-α, IL-6 and IL-1β, and mitigates cascading reactions triggered by abnormal accumulation of signaling molecules at the cellular level.

As the core organelle for cellular energy metabolism and the primary site of ROS production, mitochondria can be protected by PQQ.

By activating the CREB pathway to upregulate the expression of PGC-1α, PQQ stimulates mitochondrial biogenesis, preserves mitochondrial membrane potential and mitochondrial DNA integrity, and curbs overproduction of free radicals resulting from disturbed oxidative metabolism, thereby establishing a positive feedback loop.

In animal models fed high-fat diets, models of exercise-induced muscle injury, as well as renal and cardiomyocyte models, PQQ supplementation has been observed to improve cellular oxidative homeostasis and lower the levels of inflammation-related markers.

A small number of short-term human trials have also recorded favorable changes in peripheral biomarkers.

Nevertheless, existing human trials are limited by small sample sizes and short intervention durations, and long-term large-sample randomized controlled trials are still required to validate its efficacy.

Safety Profile of PQQ

With regard to safety, the European Food Safety Authority sets 20 mg per day as the standard supplemental dosage for adults, which is far higher than the natural daily dietary intake of 0.1-2 mg.

Toxicological studies have detected no adverse reactions at a dosage of 100 mg per kilogram of body weight per day, indicating favorable tolerability for short-term standardized supplementation.

References

Charrier D, Cerullo G, Carpenito R, et al. Metabolic and Biochemical Effects of Pyrroloquinoline Quinone (PQQ) on Inflammation and Mitochondrial Dysfunction: Potential Health Benefits in Obesity and Future Perspectives[J]. Antioxidants, 2024, 13(9): 1027.

*Special note - This article is for informational purposes only and cannot replace a doctor's treatment diagnosis and advice. It should not be regarded as a recommendation or proof of efficacy of the medical products involved. If it involves disease diagnosis, treatment, and rehabilitation, please be sure to go to a professional medical institution to seek professional advice.

by GSHWORLD

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