Abstract

Seeking an efficient and safe approach to eliminate tumors is a common goal of medical fields. Over these years, traditional Chinese medicine has attracted growing attention in cancer treatment due to its long history. Pristimerin is a naturally occurring quinone methide triterpenoid used in traditional Chinese medicine to treat various cancers. Recent studies have identified alterations in cellular events and molecular signaling targets of cancer cells under pristimerin treatment. Pristimerin induces cell cycle arrest, apoptosis, and autophagy to exhibit anti-proliferation effects against tumors. Pristimerin also inhibits the invasion, migration, and metastasis of tumor cells via affecting cell adhesion, cytoskeleton, epithelial-mesenchymal transition, cancer stem cells, and angiogenesis. Molecular factors and pathways are associated with the anti-cancer activities of pristimerin. Furthermore, pristimerin reverses multidrug resistance of cancer cells and exerts synergizing effects with other chemotherapeutic drugs. This review aims to discuss the anti-cancer potentials of pristimerin, emphasizing multi-targeted biological and molecular regulations in cancers. Further investigations and clinical trials are warranted to understand the advantages and disadvantages of pristimerin treatment much better.

Highlights

  • Cancer is a severe health problem worldwide, which has posed a threat to the public for a long time

  • The anti-tumor effects of pristimerin have been confirmed in various cancers, such as breast cancer (9), prostate cancer (24), and colorectal cancer (CRC) (6)

  • This review aims to provide a timely overview of recent researches regarding anti-cancer activities and critical mechanisms of pristimerin against malignancies, providing potential directions and developments for future studies

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Summary

INTRODUCTION

Cancer is a severe health problem worldwide, which has posed a threat to the public for a long time. Pristimerin suppresses cancer cell proliferation via G1 phase arrest (27), apoptosis (28) and autophagy induction (21). The anti-tumor effects of pristimerin have been confirmed in various cancers, such as breast cancer (9), prostate cancer (24), and colorectal cancer (CRC) (6). Emerging evidence has shown that pristimerin treatment gives rise to cell accumulation in G0/G1 phases and cell reduction in S and G2/M phases, indicating the induction of G0/G1 phase arrest to exhibit anti-proliferative effects on various cancers including CRC (22, 38), breast cancer (9, 21), uveal melanoma (UM) (18, 23, 30), chronic myelogenous leukemia (CML) (39), oral squamous cell carcinoma (OSCC) (27), esophageal cancer (40), pancreatic cancer (26, 41), prostate cancer (24, 25) and cholangiocarcinoma (42). Pristimerin has been reported to downregulate the levels of cyclinD1 and CDK4/6 in breast cancer cells (21), CML cells (39), and colorectal cancer (CRC) cells (38). It can be concluded that pristimerin induces G1 phase arrest in tumor cells via inhibiting the expression of cyclinD1/E and CDK2/4/6, while stimulating the expression of p53, p21 and p27

Phase Arrest Induction
CONCLUSION AND PERSPECTIVE
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