Hispidulin: A novel natural compound with therapeutic potential against human cancers

Abstract

Cancer is one of the most devastating disease and leading cause of death worldwide. The conventional anticancer drugs are monotarget, toxic, expensive and suffer from drug resistance. Development of multi‐targeted drugs from natural products has emerged as a new paradigm to overcome aforementioned conventionally encountered obstacles. Hispidulin (HIS), is a biologically active natural flavone with versatile biological and pharmacological activities. The anticancer, antimutagenic, antioxidative and anti‐inflammatory properties of HIS have been reported. The aim of this review is to summarize the findings of several studies over the last few decades on the anticancer activity of HIS published in various databases including PubMed, Google Scholar, and Scopus. HIS has been shown to reduce the growth of cancer cells by inducing apoptosis, arresting cell cycle, inhibiting angiogenesis, invasion and metastasis via modulating multiple signaling pathways implicated in cancer initiation and progression. Multitargeted anticancer activity of HIS remains the strongest point for developing it into potential anticancer drug. We also highlighted the natural sources, anticancer mechanism, cellular targets, and chemo‐sensitizing potential of HIS. This review will provide bases for design and conduct of further pre‐clinical and clinical trials to develop HIS into a lead structure for future anticancer therapy.

Antioxidant and Antiproliferation Activities of Lemon Verbena (Aloysia citrodora): An In Vitro and In Vivo Study

“…In another in vivo study using breast cancer cells, observations suggested decreased secretion of TGF-β1 and accumulation of intracellular TGF-β1, and inhibition of TGF-β1 transport from the trans-Golgi network and PKC activity [ 113 ]. Also, 5,6,4′-Trihydroxy-7,3′-Dimethoxyflavone (5- TDMF), hispidulin in-vivo anti-proliferation activity, and antioxidant properties were reported [ 40 , 114 ]. These compounds may work synergistically to inhibit cancer either by a direct effect on cancer cells or by an indirect effect through antioxidant activity and other mechanisms [ 115 ].…”

Hispidulin Ameliorates Endotoxin-Induced Acute Kidney Injury in Mice

“…Similar to our findings, under inflammatory conditions, hispidulin has been shown to exert anti-apoptotic effects in podocytes [ 62 ] and neurons [ 63 ]. Because hispidulin can induce apoptosis in tumor cells [ 64 ], this compound appears to have differing actions between normal and tumor cells.…”

Hispidulin modulates epithelial‑mesenchymal transition in breast cancer cells

“…Our study demonstrated that the inhibitory effects of hispidulin on EMT can be modulated against both MCF-7 (moderately invasive) and HCC38 (highly invasive) breast cancers. Most studies using hispidulin have focused on anti-cancer effects, including apoptosis signaling including mitochondrial ROS, cell cycle mediated apoptosis using various cancer cells ( 57 ). However, the role of hispidulin in TGF-β1-induced EMT in human breast cells has not been elucidated.…”