Abstract

Amentoflavone is an active phenolic compound isolated from Selaginella tamariscina over 40 years. Amentoflavone has been extensively recorded as a molecule which displays multifunctional biological activities. Especially, amentoflavone involves in anti-cancer activity by mediating various signaling pathways such as extracellular signal-regulated kinase (ERK), nuclear factor kappa-B (NF-κB) and phosphoinositide 3-kinase/protein kinase B (PI3K/Akt), and emerges anti-SARS-CoV-2 effect via binding towards the main protease (Mpro/3CLpro), spike protein receptor binding domain (RBD) and RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2. Therefore, amentoflavone is considered to be a promising therapeutic agent for clinical research. Considering the multifunction of amentoflavone, the current review comprehensively discuss the chemistry, the progress in its diverse biological activities, including anti-inflammatory, anti-oxidation, anti-microorganism, metabolism regulation, neuroprotection, radioprotection, musculoskeletal protection and antidepressant, specially the fascinating role against various types of cancers. In addition, the bioavailability and drug delivery of amentoflavone, the molecular mechanisms underlying the activities of amentoflavone, the molecular docking simulation of amentoflavone through in silico approach and anti-SARS-CoV-2 effect of amentoflavone are discussed.

Highlights

  • Amentoflavone (AMF, Figure 1), a natural biflavonoid compound, is widely used in traditional Chinese medicine

  • AMF treatment increases the phosphorylation of insulin receptor (IR) which is essential for the insulin signaling cascade in 32D cells with high-expressing IR

  • These results demonstrate that AMF enhances the activation of insulin signaling through inhibiting protein tyrosine phosphatase 1B (PTP1B) activity (Na et al, 2007)

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Summary

INTRODUCTION

Amentoflavone (AMF, Figure 1), a natural biflavonoid compound, is widely used in traditional Chinese medicine. AMF has been shown to exhibit multiple biological activities including anti-inflammatory (Tordera et al, 1994; Kim et al, 1998; Oh et al, 2013; An et al, 2016; Cai et al, 2019), antibacterial (Hwang et al, 2013), antifungal (Jung et al, 2006; Jung et al, 2007; Hwang et al, 2012), antivirus (Lin et al, 1997; Wilsky et al, 2012; Coulerie et al, 2013), anti-oxidative (Bonacorsi et al, 2012; Li et al, 2020), antiangiogenesis (Guruvayoorappan and Kuttan, 2008c; Tarallo et al, 2011; Zhang et al, 2014), neuroprotection (Cao et al, 2017; Chen et al, 2018; Rong et al, 2019; Zhao et al, 2019; Cao. Multifunction of Amentoflavone: An Overview et al, 2021), osteogenesis (Zha et al, 2016), anti-arthritis (Bais et al, 2017; Vasconcelos et al, 2019), radioprotection (Park et al, 2011; Xu et al, 2014; Qu et al, 2019), antidiabetic (Qin et al, 2018; Su et al, 2019) and antidepressant (Ishola et al, 2012). The biological activities of AMF will be discussed comprehensively

CHEMISTRY OF AMENTOFLAVONE
THE MULTIFUNCTIONAL BIOLOGICAL ACTIVITIES OF AMENTOFLAVONE
Anti-inflammatory Activity
Anti-Microorganism Activity
Neuroprotective Activity
Musculoskeletal Protection
Radioprotection
Metabolism Regulation
Anti-cancer Effect
THE TOXICITY OR UNDESIRABLE EFFECTS OF AMENTOFLAVONE
MOLECULAR DOCKING SIMULATION OF AMENTOFLAVONE THROUGH IN SILICO APPROACH
ANTI-SARS-COV-2 EFFECT OF AMENTOFLAVONE
BIOAVILABILITY AND DRUG DELIVERY OF AMENTOFLAVONE
CLINICAL PROSPECTIVE
CONCLUSION
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