Anti-Diabetic Potential of Plant-Based Pentacyclic Triterpene Derivatives: Progress Made to Improve Efficacy and Bioavailability

Abstract

Diabetes mellitus (DM) results from the inability of the pancreas to produce sufficient insulin or weakened cellular response to the insulin produced, which leads to hyperglycemia. Current treatments of DM focus on the use of oral hypoglycemic drugs such as acarbose, alpha-glucose inhibitors, sulphonylureas, thiazolidinediones, and biguanides to control blood glucose levels. However, these medications are known to have various side effects in addition to their bioavailability, efficacy, and safety concerns. These drawbacks have increased interest in the anti-diabetic potential of plant-derived bioactive compounds such as oleanolic and maslinic acids. Although their efficacy in ameliorating blood glucose levels has been reported in several studies, their bioavailability and efficacy remain of concern. The current review examines the anti-diabetic effects of oleanolic, maslinic, asiatic, ursolic, and corosolic acids and their derivatives, as well as the progress made thus far to enhance their bioavailability and efficacy. The literature for the current review was gathered from leading academic databases—including Google Scholar and PubMed—the key words listed below were used. The literature was searched as widely and comprehensively as possible without a defined range of dates.

Progress in Research on the Alleviation of Glucose Metabolism Disorders in Type 2 Diabetes Using Cyclocarya paliurus

“…Pentacyclic triterpenoids and their derivatives inhibit α-glucosidase, α-amylase, and pancreatic lipase activity, regulating blood glucose levels and reducing insulin resistance. They have become one of the most widely studied anti-diabetic compounds [ 43 ]. The total triterpenoid content of C. paliurus has also been shown to ameliorate glucose and lipid metabolism disorders [ 20 ].…”

Recent Advances Regarding the Molecular Mechanisms of Triterpenic Acids: A Review (Part I)

“…It has become very clear that, considering their very large plethora of biologic effects, triterpenic acids presumably act on multiple pathways; indeed, there are many reviews published in the past 10 years regarding their mechanism of action responsible for various activities, such as anticancer [ 15 , 16 , 17 , 18 , 19 , 20 , 21 , 22 ], immunomodulatory [ 23 , 24 ], antidiabetic [ 25 , 26 , 27 , 28 , 29 , 30 ], anti-inflammatory [ 31 ], cardioprotective [ 32 ], antiurolithic [ 33 ], antiviral [ 34 ], and wound healing [ 35 , 36 ]. This review aims to summarize the most recent (last five years) discoveries on triterpenic acids’ mechanisms of action in order to provide scientists with exhaustive knowledge, which in turn might propel and diversify future studies.…”

Enhanced Water Solubility and Anti-Tumor Activity of Oleanolic Acid through Chemical Structure Modification

“…The main biological activities of these compounds include liver protection, anti-inflammatory, anti-blood sugar, anti-blood lipid, anti-virus, anti-AIDS, anti-tumor, and so on [ 14 , 15 , 23 , 24 , 25 , 26 , 27 ]. Oleanolic acid (OA), as a pentacyclic triterpene compound, has strong liver protection, anti-inflammatory, anti-virus, anti-diabetes, anti-tumor and other activities ( Figure 2 ) [ 28 , 29 , 30 , 31 , 32 ]. Although OA has demonstrated certain anti-tumor activity and safety, its poor water solubility is still the main obstacle to improve its efficacy and clinical application [ 33 , 34 , 35 ].…”