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Review
. 2019 Mar 12;24(5):995.
doi: 10.3390/molecules24050995.

Pleiotropic Pharmacological Actions of Capsazepine, a Synthetic Analogue of Capsaicin, against Various Cancers and Inflammatory Diseases

Min Hee Yang  1 , Sang Hoon Jung  2 , Gautam Sethi  3 , Kwang Seok Ahn  4   5   6
Affiliations
Review

Pleiotropic Pharmacological Actions of Capsazepine, a Synthetic Analogue of Capsaicin, against Various Cancers and Inflammatory Diseases

Min Hee Yang et al. Molecules. .

Abstract

Capsazepine is a synthetic analogue of capsaicin that can function as an antagonist of TRPV1. Capsazepine can exhibit diverse effects on cancer (prostate cancer, breast cancer, colorectal cancer, oral cancer, and osteosarcoma) growth and survival, and can be therapeutically used against other major disorders such as colitis, pancreatitis, malaria, and epilepsy. Capsazepine has been reported to exhibit pleiotropic anti-cancer effects against numerous tumor cell lines. Capsazepine can modulate Janus activated kinase (JAK)/signal transducer and activator of the transcription (STAT) pathway, intracellular Ca2+ concentration, and reactive oxygen species (ROS)-JNK-CCAAT/enhancer-binding protein homologous protein (CHOP) pathways. It can inhibit cell proliferation, metastasis, and induce apoptosis. Moreover, capsazepine can exert anti-inflammatory effects through the downregulation of lipopolysaccharide (LPS)-induced nuclear transcription factor-kappa B (NF-κB), as well as the blockage of activation of both transient receptor potential cation channel subfamily V member 1 (TRPV1) and transient receptor potential cation channel, subfamily A, and member 1 (TRPA1). This review briefly summarizes the diverse pharmacological actions of capsazepine against various cancers and inflammatory conditions.

Keywords: ROS; TRPV1; cancer; capsazepine; inflammatory diseases.

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Conflict of interest statement

The authors declare no conflict of interests.

Figures

Figure 1
Figure 1
The chemical structures of capsaicin and capsazepine.
Figure 2
Figure 2
Pharmacological properties of capsazepine.
Figure 3
Figure 3
Potential mechanisms underlying reported anti-cancer effects of capsazepine.
Figure 4
Figure 4
Potential mechanisms regulating anti-inflammatory effects of capsazepine.
See this image and copyright information in PMC

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