Induction Effects of Apigenin, Luteolin and Vinpocetin on Neutral Endopeptidase (NEP) and Angiotensin-Converting Enzyme Activity (ACE) of SK-N-SH Cells

Ayoub, Shereen; Melzig, Matthias F.

doi:10.1177/1934578x0600100807

Cited by 7 publications

(2 citation statements)

References 40 publications

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“…With regard to natural products, EGCG strongly increased the NEP activity, thus leading to Aβ degradation [21], and resveratrol significantly increased both the estradiol and NEP level, thus decreasing Aβ deposition [22]. Finally, apigenin, luteolin and curcumin were able to induce specific NEP activity in SK-N-SH cells [23,24]. Recently, the work of Rita P-Y Chen and her group identified four curcuminoid compounds, the dihydroxylated curcumin, the monohydroxylated demethoxycurcumin, and the mono-and di-hydroxylated bisdemethoxycurcumin that have the ability to increase NEP activity [25].…”

Section: Introductionmentioning

confidence: 96%

Synthesis and Biological Evaluation of Hydroxylated Monocarbonyl Curcumin Derivatives as Potential Inducers of Neprilysin Activity

Matiadis

Chen

et al. 2021

Biomedicines

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Background: Alzheimer’s disease (AD) involves impairment of Aβ clearance. Neprilysin (NEP) is the most efficient Aβ peptidase. Enhancement of the activity or expression of NEP may provide a prominent therapeutic strategy against AD. Aims: Ten hydroxylated monocarbonyl curcumin derivatives were designed, synthesized and evaluated for their NEP upregulating potential using sensitive fluorescence-based Aβ digestion and inhibition assays. Results: Compound 4 was the most active one, resulting in a 50% increase in Aβ cleavage activity. Cyclohexanone-bearing derivatives exhibited higher activity enhancement compared to their acetone counterparts. Inhibition experiments with the NEP-specific inhibitor thiorphan resulted in dramatic cleavage reduction. Conclusion: The increased Aβ cleavage activity and the ease of synthesis of 4 renders it an extremely attractive lead compound.

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Section: Introductionmentioning

confidence: 96%

Synthesis and Biological Evaluation of Hydroxylated Monocarbonyl Curcumin Derivatives as Potential Inducers of Neprilysin Activity

Matiadis

Chen

et al. 2021

Biomedicines

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“…[53][54][55][56][57][58] Apigenin has also been confirmed to take part in neuroprotective function in various neurological disorders, such as PD, AD, and dementia. [57][58][59][60][61][62][63][64][65] Besides this, APG also exhibits neuroprotection against cerebral ischemia, subarachnoid hemorrhage, MS, epilepsy, and depression. [66][67][68][69][70][71][72][73][74][75][76][77][78] Apigenin has also been identified as an inhibitor of c-JNK/p38MAPK in several diseases 79 , including AD, 58,59,80 PD, 60,81 diabetic neuropathy, 82 ischemia/reperfusion, 83 and renal injury.…”

Section: Introductionmentioning

confidence: 99%

Protective effects of apigenin on methylmercury-induced behavioral/neurochemical abnormalities and neurotoxicity in rats

et al. 2022

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Methylmercury (MeHg) is a neurotoxin that induces neurotoxicity and cell death in neurons. MeHg increases oligodendrocyte death, glial cell activation, and motor neuron demyelination in the motor cortex and spinal cord. As a result, MeHg plays an important role in developing neurocomplications similar to amyotrophic lateral sclerosis (ALS). Recent research has implicated c-JNK and p38MAPK overactivation in the pathogenesis of ALS. Apigenin (APG) is a flavonoid having anti-inflammatory, antioxidant, and c-JNK/p38MAPK inhibitory activities. The purpose of this study is to determine whether APG possesses neuroprotective effects in MeHg-induced neurotoxicity in adult rats associated with ALS-like neuropathological alterations. In the current study, the neurotoxin MeHg causes an ALS-like phenotype in Wistar rats after 21 days of oral administration at a dose of 5 mg/kg. Prolonged administration of APG (40 and 80 mg/kg) improved neurobehavioral parameters such as learning memory, cognition, motor coordination, and grip strength. This is mainly associated with the downregulation of c-JNK and p38MAPK signaling as well as the restoration of myelin basic protein within the brain. Furthermore, APG inhibited neuronal apoptotic markers (Bax, Bcl-2, and caspase-3), restored neurotransmitter imbalance, decreased inflammatory markers (TNF- and IL-1), and alleviated oxidative damage. As a result, the current study shows that APG has neuroprotective potential as a c-JNK and p38MAPK signaling inhibitor against MeHg-induced neurotoxicity in adult rats. Based on these promising findings, we suggested that APG could be a potential new therapeutic approach over other conventional therapeutic approaches for MeHg-induced neurotoxicity in neurobehavioral, molecular, and neurochemical abnormalities.

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Acute Treatment with the Nootropic CILTEP® Does Not Improve Cognitive Performance in Healthy Middle-Aged Participants

Possemis,

Caldenhove,

Sambeth

et al. 2024

J Cogn Enhanc

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This study investigated the acute effects of the dietary nootropic stack CILTEP®. It contains a combination of ingredients that have been individually reported to improve cognitive performance. Especially, the ingredients luteolin, which is considered a phosphodiesterase type 4 (PDE4) inhibitor, and forskolin, an adenylate cyclase stimulator, were of interest since they can increase the second messenger cAMP and thus also intracellular signaling. Numerous studies have shown that inhibition of PDE4 can improve memory in animals and humans. We examined whether acute dosing of 3 capsules of CILTEP® would improve cognitive function in healthy participants aged 30 to 40 (n = 33). We used a randomized, double-blind, placebo-controlled, two-way cross-over design. Our test battery was aimed at measuring memory performance, attention, and sensorimotor speed. The primary outcome measures were the performance on the verbal learning task and the spatial pattern separation task. Secondary outcomes included other cognitive tests, event-related potentials (ERPs), and assessment of the activity of the enzyme beta-glucuronidase and its effect on the bioavailability of luteolin, heart rate, and blood pressure. No relevant effects of acute CILTEP® treatment were found on any measure of the test battery or ERPs. Blood plasma concentrations of luteolin increased, yet about 2000 times too low to likely exert any PDE4 inhibition. CILTEP® treatment did neither affect heart rate nor blood pressure. In summary, there is no evidence that a single standardized dose of 3 capsules of CILTEP® can improve cognitive function in healthy middle-aged participants.

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Induction Effects of Apigenin, Luteolin and Vinpocetin on Neutral Endopeptidase (NEP) and Angiotensin-Converting Enzyme Activity (ACE) of SK-N-SH Cells

Cited by 7 publications

References 40 publications

Synthesis and Biological Evaluation of Hydroxylated Monocarbonyl Curcumin Derivatives as Potential Inducers of Neprilysin Activity

Synthesis and Biological Evaluation of Hydroxylated Monocarbonyl Curcumin Derivatives as Potential Inducers of Neprilysin Activity

Protective effects of apigenin on methylmercury-induced behavioral/neurochemical abnormalities and neurotoxicity in rats

Acute Treatment with the Nootropic CILTEP® Does Not Improve Cognitive Performance in Healthy Middle-Aged Participants

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