The<i>in silico</i>and<i>in vivo</i>evaluation of puerarin against Alzheimer's disease

Liu, Song; Cao, Xiaolu; Liu, Guang-Qi; Zhou, Tong; Yang, Xiliang; Ma, Bing-Xin

doi:10.1039/c8fo01696h

Cited by 41 publications

(22 citation statements)

References 52 publications

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“…Puerarin was isolated from Gegen (Chinese name), which has been employed as a food source and medicine for thousands of years and is a relatively safe medicinal herb that was utilized in ancient China (Prasain et al, 2003). It was previously found that the continuous use of a Gegen preparation for 2 months did not affect the behavior, hepatic, renal function, and blood routine of the animals (Liu et al, 2019;Zhou et al, 2014). Puerarin has previously been used to treat fever, colds, coughs, and influenza in Asian countries (Wu et al, 2011).…”

Section: Discussionmentioning

confidence: 99%

Antiviral activity of puerarin as potent inhibitor of influenza virus neuraminidase

Wang

Zeng

et al. 2020

Phytotherapy Research

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Puerarin is a major isofiavone compound isolated from the root of Pueraria lobata. It was reported that puerarin had antioxidant, antiinflammatory, antitumor, cholesterol lowering, liver protective, and neuroprotective properties. However, few studies have explored the antiviral effect of puerarin and its target mechanism related to influenza virus. Here, the antiinfluenza activity of puerarin in vitro and in vivo and its mode of action on the potential inhibition of neuraminidase (NA) were investigated. Puerarin displayed an inhibitory effect on A/FM/1/1947(H1N1) (EC50 = 52.06 μM). An indirect immunofluorescence assay indicated that puerarin blocked the nuclear export of viral NP. The inhibition of NA activity confirmed that puerarin can block the release of newly formed virus particles from infected cells. Puerarin (100 and 200 mg/kg/d) exhibited effective antiviral activity in mice, conferring 50% and 70% protection from death against H1N1, reducing virus titers, and effectively alleviating inflammation in the lungs. The molecular docking results showed that puerarin had a strong binding affinity with NA from H1N1. The results of the molecular dynamics simulation revealed that puerarin had higher stable binding at the 150‐loop region of the NA protein. These results demonstrated that puerarin acts as a NA blocker to inhibit influenza A virus both in cellular and animal models. Thus, puerarin has potential utility for the treatment of the influenza virus infection.

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Section: Discussionmentioning

confidence: 99%

Antiviral activity of puerarin as potent inhibitor of influenza virus neuraminidase

Wang

Zeng

et al. 2020

Phytotherapy Research

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“… 7 , 8 , 71 , 72 , 73 Research studies have shown that PUE holds intensively neuroprotective effects for various kinds of CNS disorders, including stroke, SAH, TBI, PD, AD, and SCI, through multiple activities, such as antioxidation, anti‐inflammation, and antiapoptosis. 7 , 8 , 17 , 18 , 19 , 20 , 21 , 22 , 23 , 24 , 26 , 27 , 28 , 29 , 30 , 31 , 32 , 33 PUE can exert brain‐protective effects on ischemia/reperfusion‐mediated brain injury by the suppression of apoptosis/necrosis, autophagy activation, and/or inflammatory response 9 , 10 , 11 , 12 , 13 , 14 , 15 by the promotion of X‐chromosome‐linked inhibitor of apoptosis protein, 15 erythropoietin activity, 13 stimulation of Janus‐activated kinase‐2 and signal transducers and activators of transcription‐3, 12 inhibition of caspase‐3 activity and expression, 15 NF‐κB signal pathway, 11 , 12 Toll‐like receptor‐4, myeloid differentiation factor‐88, 11 and autophagy level. 9 Besides, PUE could also reduce hypobaric hypoxia‐mediated acute lung and cerebrum injury, 74 nickel‐induced liver injury, 75 and diabetes and chronic constriction injury‐induced neuropathic pain by suppressing the activation of the NF‐κB pathway.…”

Section: Discussionmentioning

confidence: 99%

“…Puerarin (PUE), as a primary bioactive compound of Pueraria lobata roots, 7 , 8 has exhibited potently neuroprotective activity in multiple central nervous system (CNS) disorders, including stroke, 9 , 10 , 11 , 12 , 13 , 14 , 15 , 16 subarachnoid hemorrhage (SAH), 17 traumatic brain injury (TBI), 18 spinal cord injury (SCI), 19 , 20 , 21 , 22 , 23 Alzheimer's disease (AD), 24 , 25 , 26 , 27 , 28 and Parkinson's disease (PD). 29 , 30 , 31 , 32 , 33 Research studies have shown that PUE can generate brain‐protective effects by activating the phosphatidylinositol 3‐kinase (PI3K)/Akt signal against acute CNS disorders 18 , 19 , 34 and neurodegenerative diseases.…”

Section: Introductionmentioning

confidence: 99%

Puerarin attenuates intracerebral hemorrhage‐induced early brain injury possibly by PI3K/Akt signal activation‐mediated suppression of NF‐κB pathway

Zeng

Zheng

Chen

et al. 2021

J Cellular Molecular Medi

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Intracerebral hemorrhage (ICH) can induce intensively oxidative stress, neuroinflammation, and brain cell apoptosis. However, currently, there is no highly effective treatment available. Puerarin (PUE) possesses excellent neuroprotective effects by suppressing the NF‐κB pathway and activating the PI3K/Akt signal, but its role and related mechanisms in ICH‐induced early brain injury (EBI) remain unclear. In this study, we intended to observe the effects of PUE and molecular mechanisms on ICH‐induced EBI. ICH was induced in rats by collagenase IV injection. PUE was intraperitoneally administrated alone or with simultaneously intracerebroventricular injection of LY294002 (a specific inhibitor of the PI3K/Akt signal). Neurological deficiency, histological impairment, brain edema, hematoma volume, blood–brain barrier destruction, and brain cell apoptosis were evaluated. Western blot, immunohistochemistry staining, reactive oxygen species (ROS) measurement, and enzyme‐linked immunosorbent assay were performed. PUE administration at 50 mg/kg and 100 mg/kg could significantly reduce ICH‐induced neurological deficits and EBI. Moreover, PUE could notably restrain ICH‐induced upregulation of the NF‐κB pathway, pro‐inflammatory cytokines, ROS level, and apoptotic pathway and activate the PI3K/Akt signal. However, LY294002 delivery could efficaciously weaken these neuroprotective effects of PUE. Overall, PUE could attenuate ICH‐induced behavioral defects and EBI possibly by PI3K/Akt signal stimulation‐mediated inhibition of the NF‐κB pathway, and this made PUE a potential candidate as a promising therapeutic option for ICH‐induced EBI.

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“…been thoroughly studied and has attracted increasing attention from researchers. PU can improve the learning and memory abilities of ageing mice, and the mechanism underlying its anti-ageing effects is related to the inhibition of mitochondrial dysfunction and the enzyme activity of caspase-3 (13). PU can also significantly improve the activity of superoxide dismutase in ageing mice and enhance its ROS scavenging function.…”

Section: Puerarin Alleviates the Ototoxicity Of Gentamicin By Inhibiting The Mitochondria-dependent Apoptosis Pathwaymentioning

confidence: 99%

Puerarin alleviates the ototoxicity of gentamicin by inhibiting the mitochondria‑dependent apoptosis pathway

et al. 2021

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Gentamicin (GM) is a commonly used antibiotic, and ototoxicity is one of its side effects. Puerarin (PU) is an isoflavone in kudzu roots that exerts a number of pharmacological effects, including antioxidative and free radical scavenging effects. The present study investigated whether PU could protect against GM-induced ototoxicity in C57BL/6J mice and House Ear Institute-Organ of Corti 1 (HEI-OC1) cells. C57BL/6J mice and HEI-OC1 cells were used to establish models of GM-induced ototoxicity in this study. Auditory brainstem responses were measured to assess hearing thresholds, and microscopy was used to observe the morphology of cochlear hair cells after fluorescent staining. Cell viability was examined with Cell Counting Kit-8 assays. To evaluate cell apoptosis and reactive oxygen species (ROS) production, TUNEL assays, reverse transcription-quantitative PCR, DCFH-DA staining, JC-1 staining and western blotting were performed. PU protected against GM-induced hearing damage in C57BL/6J mice. PU ameliorated the morphological changes of mouse cochlear hair cells and reduced the apoptosis rate of HEI-OC1 cells after GM-mediated damage. GM-induced ototoxicity may be closely related to the upregulation of p53 expression and the activation of endogenous mitochondrial apoptosis pathways, and PU could protect cochlear hair cells from GM-mediated damage by reducing the production of ROS and inhibiting the mitochondria-dependent apoptosis pathway.

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Thein silicoandin vivoevaluation of puerarin against Alzheimer's disease

Abstract: In silico methods were used to screen the anti-AD effect of puerarin, further mutually verified by an in vivo study.

Cited by 41 publications

References 52 publications

Antiviral activity of puerarin as potent inhibitor of influenza virus neuraminidase

Antiviral activity of puerarin as potent inhibitor of influenza virus neuraminidase

Puerarin attenuates intracerebral hemorrhage‐induced early brain injury possibly by PI3K/Akt signal activation‐mediated suppression of NF‐κB pathway

Puerarin alleviates the ototoxicity of gentamicin by inhibiting the mitochondria‑dependent apoptosis pathway

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