Norcantharidin is a potential new anticancer drug currently undergoing research and evaluation due to new findings showing inhibitory effects on some cancerous cells. In the past, Norcantharidin was used in its raw form Cantharidin (CTD) by Chinese herbalists to treat a variety of ailments. Cantharidin can be found in the dried skin of almost 1500 different …show more content…
The known mechanism for Norcantharidin (NCTD) work by either interrupting DNA replication, retardation of cell cycle progression and induction of apoptosis, the process of controlled cell death via the regulation of p53 (specific-sequence transcription factor) and Bcl-1 gene expression. Some have also demonstrated that the CTD and NCTD can also inhibit protein phosphatases 1 (PP1) and 2A (PP2A). (2) This is vital as these two protein phosphatases play a crucial role in different cell processes such as mitotic events and cell cycle progression. (1) Most research facilities are looking at controlling the anticancer activity to these phosphatases by either increasing their selectivity or potency. (1, 2, …show more content…
There is a vast series of simple and overly complicated additions that can be made to NCTD from which some work and some do not. CTD and NCTD are both potent anticancer agents and target different cancerous cells over a broad spectrum. The reason why current and previous drugs that work undergo constant evaluation and experimentation is in order to continue to increase their effectiveness.
Many groups have expanded a lot of work in looking at acquiring a greater understanding of the structural requirements of CTD and NCTD analogues as PP1 and PP2A inhibitors, and thus validate how effective they would become as anti-cancer agents. Many studies have led to the development of a variety of modified analogues, some focus on CTD and NCTD based anhydride analogues that are acid-ester based or acid-amide based. Others have looked at developing skeletally modified analogues in which an infinite number of substituents are attached to the bicyclo [2.2.1] heptane backbone shown below.