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Iridoids are monoterpenes, generally in the form of cyclopentanepyrans, found in a variety of plants and some animals. They are obtained from 8-oxogeranial biosynthesis. Iridoids are usually found in plants as glycosides, most often bound to glucose. Their chemical structure is exemplified by iridomyrmecin, a defensive chemical produced by the ant genus Iridomyrmex. Structurally, they are bicyclic cis-conjugated cyclopentane-pyrans. The breakage of bonds in the cyclopentane ring produces subclasses called iridoids ether terpenes, such as olive bitter glucoside and bitter amygdalin. As the active ingredients of natural drugs, iridoids mainly have biological effects such as neuroprotection, antitumor and hepatoprotection. Different iridoids have different biological activities and dose-dependent properties due to their different structures.
Iridoids belong to monoterpenes, which are acetal derivatives of cyclic enol ether terpenes. Due to the unstable nature of their C1 -OH groups, iridoids often react with sugars to form glycosides. Based on the integrity of the cyclopentane unit, they can be classified into iridoids glycosides (including gardenia glycosides, strychnine, acetylbareside, deacetyl geranoside acid, and brassinolide) and open cyclic enol ether terpene glycosides (including swertia bitter glycosides, gentian bitter glycosides, qinghuoside A, qinghuoside B, angelica glycosides, and olive bitter glycosides).
Iridoids compounds have potential neuroprotective effects and can be used to treat a variety of neurological disorders such as depression, Alzheimer's disease and Parkinson's disease.
Iridoids have a variety of antitumor activities, acting against gastric, lung, colon and breast cancers without damaging their normal cells. It was found that the iridoidside glycosides themselves are inactive forms and that the glycosides are inhibited only after hydrolysis by β-glucosidase, but there is no inhibition if the glycosides of the compounds are used as controls, indicating that hydrolysis by β-glucosidase is necessary for the compounds to show biological activity.
Diabetes mellitus is a common endocrine metabolic disease, characterized by chronic hyperglycemia and multi-system and multi-organ targeted damage, with a high disability rate. The identification and structural optimization of active ingredients from TCM is an important way for drug development.
Numerous studies have shown that iridoids ether terpenoids are anti-inflammatory and antioxidant molecules. They have been shown to have significant anti-inflammatory effects in neurodegenerative diseases, cardiovascular diseases, cancer, hepatoprotective effects, acute pancreatitis, hyperhomocysteinemia, diabetic complications, acute lung injury, multiple sclerosis and various lipopolysaccharide (LPS)-induced inflammation models.
The hepatoprotective effects of sweretin and sweretoxanthin were evaluated using an α-naphthol isocyanate (ANIT)-induced liver injury model. After 7 days of oral administration of sweretin or sweretin, alanine aminotransferase, aspartate aminotransferase and total direct bilirubin levels in mice were significantly reduced at α-naphthylisothiocyanate induced levels, while bile flow was significantly increased.
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