Preparation of S-Acetyl-L-glutathione

An efficient one-step synthesis of S-acetyl-l-glutathione has been developed in a DMF–TFA mixed solvent with CoCl2 as catalyst. This process not only has the advantages of selective acylation of the glutathione thiol group without involving the free amino but also highlights recycling of the relatively costly solvent TFA, which improves the yield to 91% and quality to 99.7%. The reaction is cost-effective, efficient, and easy to scale-up.

Benefits of S-Acetyl-L-glutathione

S-Acetyl-L-glutathione (SAG) is a prodrug of glutathione (GSH) and is one of the effective methods of supplementing endogenous glutathione. GSH (γ-L-glutamyl-L-cysteinylglycine) is an endogenous tripeptide found mainly in liver tissues, which are the main tissues involved in its biosynthesis. Intracellularly, GSH is maintained in its thiol-reduced form by NADPH-dependent enzymes (glutathione disulfide bond (GSSG) reductase). An additional amount of GSH is present in the form of GSSG and glutathione coupling (GS-R). Maintaining an optimal GSH:GSSG ratio is essential for cell survival because GSH is one of the most important endogenous antioxidant defences, removing lipids and hydrogen peroxide. GSH also plays an important role in energy metabolism. This key molecule protects cells and mitochondria from free radical damage. Mitochondria are the powerhouses in the cell responsible for energy production, and by keeping them free from oxidative damage, the cell achieves optimal performance, thus promoting optimal health and increased energy.

Studies have shown that GSH levels are high in the young body and low in the elderly population, and even lower in the sick and hospitalised elderly. The level of GSH in our bodies is closely related to our health, and low levels can increase the risk of disease and infection. Therefore, timely supplementation of GSH is needed. when GSH is taken orally, it has low bioavailability and is easily broken down by the stomach and is not effective. Therefore, a more easily absorbed and highly stable form of glutathione, S-Acetyl-L-glutathione, can be chosen.

SAG has the ability to penetrate the mitochondrial membrane, helping to maintain its integrity and function. It also crosses the blood-brain barrier, allowing it to directly detoxify and protect the brain. In addition, it has been shown that SAG pretreatment significantly prevents CCl4-induced cytotoxicity, is protective in restoring mitochondrial autophagy, and attenuates fibrosis, collagen deposition, hepatocellular damage and organ dysfunction. It also has anti-inflammatory effects, decreasing the pro-inflammatory cytokines TNF-α, IL-6, MCP-1 and IL-1β in serum and liver, and inhibiting the TLR4/NFkB pathway.

SAG + Vitamins helps to detoxify the body, particularly in the liver. It helps in the breakdown and elimination of toxins and harmful substances. This combination helps maintain a healthy liver and overall detoxification pathways by supporting detoxification. This drug promotes skin health and may contribute to a more youthful and radiant appearance.

Side effects of S-Acetyl-L-glutathione

S-Acetyl-L-glutathione is for the most part well tolerated with no serious adverse reactions. However, possible side effects of SAG + Vitamins include nausea, bloating, diarrhoea or allergic reactions. Contact your doctor promptly if you experience any serious symptoms.

References:

[1] KAI FU. An Improved Process for Preparation of S-Acetyl-l-glutathione[J]. Organic Process Research & Development, 2015. DOI:10.1021/acs.oprd.5b00081.

[2] LONIGRO N, MOHAMMED Z R, PERONDI F, et al. Antioxidant Effect of a Combination of S-Acetyl-L-Glutathione, Vitamin E, Silybum Marianumon Hepatic Cells under Oxidative Stress: An In Vitro Study[J]. Journal of Pharmacy and Nutrition Sciences, 2024. DOI:10.29169/1927-5951.2024.14.01.