Abstract
Norcantharidin (NCTD) is a demethylated derivative of cantharidin, which is an anticancer active ingredient of traditional Chinese medicine, and is currently used clinically as a routine anti-cancer drug in China. Clarifying the anticancer effect and molecular mechanism of NCTD is critical for its clinical application. Here, we summarized the physiological, chemical, pharmacokinetic characteristics and clinical applications of NCTD. Besides, we mainly focus on its potential multi-target anticancer activities and underlying mechanisms, and discuss the problems existing in clinical application and scientific research of NCTD, so as to provide a potential anticancer therapeutic agent for human malignant tumors.
Highlights
Since Tu Youyou was awarded the 2015 Nobel Prize in physiology or medicine for the discovery of artemisinin used for malaria treatment, traditional Chinese medicines (TCMs) and natural medicine are getting more attention
Norcantharidin (NCTD), a demethylated derivative of cantharidin which is an active ingredient of TCM—Mylabris [1–3], is currently used clinically as an optional anticancer drug in China, because of its relatively synthesized facility, potential anticancer activity, and less side-effects such as myelosuppression, gastrointestinal and urinary tract toxicity [1–5]
NCTD can be used as an antitumor drug alone in the treatment of liver cancer, gastric cancer and other tumors, especially for advanced malignant tumors that have lost the opportunity of operation
Summary
Since Tu Youyou was awarded the 2015 Nobel Prize in physiology or medicine for the discovery of artemisinin used for malaria treatment, traditional Chinese medicines (TCMs) and natural medicine are getting more attention. Clinical uses As an efficacious anticancer drug, NCTD has been used to treat cancer patients clinically in China for many years. The inhibitory effect of NCTD on proliferation is mainly achieved through cell cycle arrest and inhibition of DNA synthesis by inhibiting the expression of cyclins, cyclin-dependent kinases (CDKs) and increasing the expression of cyclindependent kinase inhibitors (CDKIs, such as p21Cip/ Waf1, p27kip1); On the other hand, NCTD can induce apoptosis by increasing the expression of pro-apoptotic protein such as P53, Bax, Caspases, and reducing the expression of anti-apoptotic proteins such as Bcl-2 (B-cell lymphoma-2) and survivin These mechanisms have been confirmed in a variety of tumor cell lines such as leukemia K562 and HL-60 [18, 55], hepatoma HepG2, SMMC7721 and BEL-7402 [56–58], colorectal cancer CT26 and HCT-15 cells [59, 60], etc. It was reported that NCTD inhibited the expression of GBC-SD cell proliferation-related gene proteins PCNA (proliferating cell nuclear antigen) and Ki-67, this may be one of the mechanisms by which NCTD inhibit the proliferation and growth of tumor cells [12, 67]
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