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Norcantharidin: research advances in pharmaceutical activities and derivatives in recent years

Authors :
Jianbo Zhou
Yali Ren
Lu Tan
Xiaominting Song
Miao Wang
Yuzhi Li
Zhixing Cao
Chuanjie Guo
Source :
Biomedicine & Pharmacotherapy, Vol 131, Iss , Pp 110755- (2020)
Publication Year :
2020
Publisher :
Elsevier, 2020.

Abstract

Cantharidin (CTD) is the main bioactive component of Cantharides, which is called Banmao in Traditional Chinese Medicine (TCM). Norcantharidin (NCTD) is a structural modifier of CTD. To compare with CTD, NCTD has lighter side effects and stronger bioactivity in anti-cancer through inhibiting cell proliferation, causing apoptosis and autophagy, overwhelming migration and metastasis, affecting immunity as well as lymphangiogenesis. Examples of these effects include suppressing Protein Phosphatase 2A and modulating Wnt/beta catenin signal, with Caspase family proteins, AMPK pathway and c-Met/EGFR pathway involving respectively. Moreover, NCTD has the effects of immune enhancement, anti-platelet aggregation and inhibition of renal interstitial fibrosis with distinct signaling pathways. The immunological effects induced by NCTD are related to the regulation of macrophage polarization and LPS-mediated immune response. The antiplatelet activity that NCTD induced is relevant to the inhibition of platelet signaling and the downregulation of α2 integrin. Furthermore, some of novel derivatives designed and synthesized artificially show stronger biological activities (e.g., anticancer effect, enzyme inhibition effect, antioxidant effect) and lower toxicity than NCTD itself. Plenty of literatures have reported various pharmacological effects of NCTD, particularly the anticancer effect, which has been widely concerned in clinical application and laboratory research. In this review, the pharmaceutical activities and derivatives of NCTD are discussed, which can be reference for further study.

Details

Language :
English
ISSN :
07533322
Volume :
131
Issue :
110755-
Database :
Directory of Open Access Journals
Journal :
Biomedicine & Pharmacotherapy
Publication Type :
Academic Journal
Accession number :
edsdoj.81f4c381b44cb9328a95c4b53c79e
Document Type :
article
Full Text :
https://doi.org/10.1016/j.biopha.2020.110755