Isobavachalcone: A comprehensive review of its plant sources, pharmacokinetics, toxicity, pharmacological activities and related molecular mechanisms

Abstract

Isobavachalcone (IBC), also known as isobapsoralcone, is a natural flavonoid widely derived from many medicinal plants, including Fabaceae, Moraceae, and so forth. IBC has been paid more and more attention by researchers in recent years due to its pharmacological activity in many diseases. This review aims to describe in detail the plant sources, pharmacokinetics, toxicity, pharmacological activities, and molecular mechanisms of IBC on various diseases. We found that IBC can be obtained not only by extraction but also by chemical synthesis. Pharmacokinetic studies have shown that IBC has low bioavailability, but can penetrate the blood–brain barrier and is widely distributed in the brain. Its pharmacological activities mainly include anticancer, antibacterial, anti‐inflammatory, antiviral, neuroprotective, bone protection, and other activities. In particular, IBC shows strong anti‐tumor and anti‐inflammatory therapeutic potential due to its anti‐cancer and anti‐inflammatory activities. However, due to its hepatotoxicity, there may be more drug interactions. Therefore, more and more in‐depth studies are needed for its clinical application. Mechanically, IBC can induce the production of reactive oxygen species (ROS), inhibit AKT, ERK, and Wnt pathways, and promote apoptosis of cancer cells through mitochondrial or endoplasmic reticulum pathways. IBC can inhibit the NF‐κB pathway and the production of multiple inflammatory mediators by activating NRF2/HO‐1 pathway, thus producing anti‐inflammatory effects. Moreover, we discussed the limitations of current research on IBC and put forward some new perspectives and challenges, which provide a strong basis for clinical application and new drug development of IBC in the future.

Chalcones and Gastrointestinal Cancers: Experimental Evidence

“…Because TSP50-induced cell proliferation and tumorigenesis are dependent on the activation of the NF- k B signaling pathway [ 78 ], it has been suggested that the antiproliferative effect of cardamonin could be related to the inhibition of TSP50/NF-κB protein expression [ 79 ]. Furthermore, the ability to suppress cancer proliferation via the inhibition of NF-κB signaling has also been reported in several other chalcones, such as 4-Boc-piperidone chalcones [ 80 ], bichalcone analogs [ 81 ], IBC [ 82 ], hydroxysafflor yellow A [ 83 ] and butein [ 84 ].…”

Stereoselective Synthesis of Flavonoids: A Brief Overview

“…Flavonoids are well-known to possess a variety of biological activities with therapeutic interests such as antioxidant [ 5 ], antimalarial [ 6 ], anti-inflammatory [ 7 , 8 ], antiviral [ 9 , 10 ], antibacterial [ 11 ], antidiabetic [ 8 ], antifungal [ 12 ], and anticancer [ 1 , 13 , 14 , 15 , 16 ] potential. It is also reported that they protect the cardiovascular system from oxidative stress as a consequence of their ROS scavenger ability [ 17 ].…”

The Current State of Knowledge in Biological Properties of Cirsimaritin

“…These natural bioactive compounds belong to different chemical classes such as phenolic acids, terpenoids, flavonoids, alkaloids, and terpenoids [ 10 , 11 , 12 , 13 , 14 , 15 , 16 ]. Moreover, flavonoids are considered as the most abundant and diverse family [ 17 , 18 ] with promising therapeutic benefits since they are non-toxic molecules with many biological activities including anticancer [ 19 ], inflammatory [ 20 ], antibacterial [ 21 ], antiviral [ 22 ], neuroprotective effects [ 23 ], and other activities. On the other hand, if their proprieties are properly used, these natural products could be efficient, safe, and new therapeutic agents.…”