ESCULIN

Short summary description of the oil:

• Categories/Mainstream: Active pharmaceutical ingradient
• IUPAC Name: 7-hydroxy-6-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxychromen-2-one
• Botanical Source: Fraxinus ornus
• CAS number: 1953-04-4
• Molecular formula: C15H16O9.1,5 H2O
• Molecular mass: 340.28 (anhydrous); 367.31 (crystallization water not inserted in the crystals).
• Country of origin: Bulgaria

The origin of raw material

Ash tree (Fraxinus ornus) is from the Oleaceae family and grows in dry rocky places in bushes and broad-leaved forests up to 1200 m altitude in the foothills and mountains zones of the whole Bulgarian country. The Ash tree is a high bush or tree with round crown and brown buds. Leaves are opposite, unpaired pinnate, usually with elliptical or oval-lancet form. The calyx retains after the mature of the fruit as four small teeth disposed on its bottom. The blossoms have calyxes and garlands collected in long brooms with different colors and appear after the tree comes into leaf. The fruit is flat semen. The tree blooms in May – June and the fruits mature in September – October. The outside color of the barks is pale gray to brawn-grey with greenish nuance (shade). In the inside, they are pale brawn to brawn. The breaking is almost white.

The herbal is with light bitter and tart taste, odorless.Collection of barks is usually done in Spring or Summer time. After the bark is separated from the tree stems, the bark is dried naturally or by dryers, and no differences in quality are observed between the two types of processing.

Technological process

Esculoside (esculin) is a glucoside that represents a mixture between the coumarin derivative esculetin and the monosaccharide glucose. The API (active pharmaceutical ingredient) produced by the manufacturing cite of Galen-N is 100 percent traceable from the raw material source to the final quantity of active substance.

The extraction of the substance is achieved through a process of diffusion of the substance into a solvent, resulting in a mixture between the extract and the solvent. The obtained intermediate product undergoes multiple purification processes. The final product is packaged in a double polyethylene bag and a fibber drum.

Properties

Esculin, found in the barks of the ash tree, has been used in various medical applications due to its beneficial effects on health. It is often included in anti-inflammatory creams and gels applied to inflamed areas of the skin, helping to relieve pain and reduce inflammation. Similarly, esculin is used in medications and supplements that support circulation and the health of blood vessels. Venous insufficiency and chronic venous insufficiency are other conditions where esculin may be used for treatment. Finally. It is also offered as a dietary supplement that promotes the health of the circulatory system and circulation.

Antiviral activity

An interesting new study by the Chinese Academy of Fishery Sciences demonstrates a favorable antiviral effect of esculin. Largemouth bass ranavirus (LMBRaV), a double-stranded DNA (dsDNA) virus, poses significant challenges to the largemouth bass (Micropterus salmoides) aquaculture industry due to its high mortality rates and economic consequences. In this study, compounds derived from Chinese herbs were screened for their effectiveness against LMBRaV. Among them, esculin demonstrated remarkable inhibitory activity, with a 73% inhibition rate on LMBRaV major capsid protein (MCP) gene expression at a concentration of 60 mg/L in cellular environments. Furthermore, esculin exhibited a notable reduction in cytopathic effects (CPE), safeguarding infected cells from nuclear damage caused by LMBRaV and impeding viral infection by modulating viral entry mechanisms. In vivo experiments revealed that esculin increased the survival rate of LMBRaV-infected largemouth bass by 60.0% in prevention trials and by 53.3% in treatment trials. Additionally, esculin demonstrated a significant decrease in viral loads and stimulated the upregulation of antiviral-associated genes, indicating its potential for immunoregulation. In conclusion, esculin shows promise for both the prevention and treatment of LMBRaV infections in the aquaculture sector (Mingyang Xue et. al.,)

Anti inflammatory activity

Esculin, a natural product drawn attention as a new therapeutic modulator of inflammation. However, little is known about its effect on ulcerative colitis (UC). This study aims to investigate the protective effects and mechanisms of esculin in colitis. The results demonstrate that esculin exhibits low cytotoxicity in vivo and in RAW264.7 macrophages, while significantly alleviating symptoms of DSS-induced colitis and limiting the expression of inflammatory factors, including iNOS, IL-1β, TNF-α, in both peritoneal macrophages and colon tissues from DSS-induced mice and RAW264.7 macrophages. It should be noted that aesculin actively attenuates NF-κB signaling activity while promoting nuclear localization of PPAR-γ in both rectal tissues from DSS-induced mice and LPS-stimulated macrophages. These findings suggest that the protection of aesculin against ulcerative colitis may be attributed to its regulation of the PPAR-γ and NF-κB pathways. Therefore, aesculin may serve as a potential therapeutic agent for the treatment of ulcerative colitis.

Cognitive impact

The protective effects and underlying mechanism of esculin on cognitive impairment in experimental diabetic nephropathy (DN) were investigated. Male C57BL/6J mice were induced with streptozotocin (STZ) and then treated with various doses of esculin. The results showed that esculin significantly improved behaviour and recognition memory in STZ-induced diabetic rats, as observed in the Morris water maze test. Additionally, esculin treatment inhibited inflammatory markers and oxidative stress levels in the kidney, suggesting its potential as a therapeutic target for cognitive impairment in DN (Yu Song et. al., 2018)

Chemical strocture

Physicochemical characteristics