Neuroprotective effects of prenylated flavanones isolated from Dalea species, in vitro and in silico studies

Santi, María Daniela; Arredondo, Florencia; Carvalho, Diego B.; Echeverry, Carolina; Prunell, Giselle; Peralta, Mariana Andrea; Cabrera, José Luis; Ortega, María Gabriela; Savio, Eduardo; Abin-Carriquiry, Juan Andrés

doi:10.1016/j.ejmech.2020.112718

Cited by 10 publications

(4 citation statements)

References 60 publications

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“…LBP crude plant extract, instead of an isolated compound, can present multi-target effects and better pharmacokinetic parameters such as greater solubility, agent interactions, and modulation of adverse events, as demonstrated in cannabis studies [ 30 ]. Among the natural compounds, flavonoids have been studied for their multi-target behavior in the CNS and have neuroprotective activity with different mechanisms of action [ 31 ]. Quercetin 3-O-α-L-arabinopyranosyl-(1→2)-O-α-L-rhamnopyranoside ( 2 ), the major compound present in LBP, can be easily extracted using water [ 32 ]; however, the effects observed using the crude plant extract are not expected to be due to this compound alone, as the hydrolysis of a range of flavonol and isoflavone glycosides by the enzyme lactase phrorizin hydrolase, found in the small intestine of mammals, makes it difficult to absorb these compounds as a whole molecule [ 33 , 34 ].…”

Section: Discussionmentioning

confidence: 99%

The psychoactive effects of Bryophyllum pinnatum (Lam.) Oken leaves in young zebrafish

et al. 2022

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Bryophyllum pinnatum (Lam.) Oken (BP) is a plant that is used worldwide to treat inflammation, infections, anxiety, restlessness, and sleep disorders. While it is known that BP leaves are rich in flavonoids, the extent of the beneficial and toxic effects of its crude extracts remains unclear. Although some neurobehavioral studies using leaf extracts have been conducted, none has examined the effects of water-extracted leaf samples. The zebrafish is a powerful animal model used to gain insights into the efficacy and toxicity profiles of this plant due to its high fecundity, external development, and ease of performing behavioral assays. In this study, we performed behavioral testing after acute exposure to different concentrations of aqueous extract from leaves of B. pinnatum (LABP) on larval zebrafish, investigating light/dark preference, thigmotaxis, and locomotor activity parameters under both normal and stressed conditions. LABP demonstrated dose-and time-dependent biphasic effects on larval behavior. Acute exposure (25 min) to 500 mg/L LABP resulted in decreased locomotor activity. Exposure to 300 mg/L LABP during the sleep cycle decreased dark avoidance and thigmotaxis while increasing swimming velocity. After sleep deprivation, the group treated with 100 mg/L LABP showed decreased dark avoidance and increased velocity. After a heating stressor, the 30 mg/L and 300 mg/L LABP-treated groups showed decreased dark avoidance. These results suggest both anxiolytic and psychoactive effects of LABP in a dose-dependent manner in a larval zebrafish model. These findings provide a better understanding of the mechanisms underlying relevant behavioral effects, consequently supporting the safe and effective use of LABP for the treatment of mood disorders.

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Section: Discussionmentioning

confidence: 99%

The psychoactive effects of Bryophyllum pinnatum (Lam.) Oken leaves in young zebrafish

et al. 2022

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“…Santi et al discovered that prenylation in flavonoids enhanced the neuroprotective effect of the parent flavonoid. Moreover, they found that prenylation at C-8 of the A-ring, when accompanied by an unsubstituted B-ring, contributed to a more potent effect [33]. Previous study also suggested that prenylated flavonoids might interact with estrogen receptor α (ERα) to exert their neuroprotective activities [20].…”

Section: The Neuroprotective Activity Of Wushanicaritinmentioning

confidence: 99%

“…As one of the important bioactive compounds found in Epimedium, wushanicaritin showed promising intercellular antioxidant activities, suggesting its potential application in functional foods or food supplements for neuroprotection. Moreover, prenylated flavonoids have been proved to be promising nutraceuticals with neuroprotective activity [32,33]. Santi et al discovered that prenylation in flavonoids enhanced the neuroprotective effect of the parent flavonoid.…”

Section: The Neuroprotective Activity Of Wushanicaritinmentioning

confidence: 99%

From Epimedium to Neuroprotection: Exploring the Potential of Wushanicaritin

Luo,

Shi,

Wen

2024

Foods

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Epimedium has been used for functional foods with many beneficial functions to human health. Wushanicaritin is one of the most important chemicals int Epimedium. This study investigated the neuroprotective effects of wushanicaritin and potential underlying mechanisms. The results demonstrated that wushanicaritin possessed superior intercellular antioxidant activity compared to icaritin. Wushanicaritin, with an EC50 value of 3.87 μM, showed better neuroprotective effect than quercetin, a promising neuroprotection agent. Wushanicaritin significantly reversed lactate dehydrogenase release, reactive oxygen species generation, cell apoptosis, and mRNA expression related to cell apoptosis and oxidative defense, in glutamate-induced PC-12 cells. Wushanicaritin could also maintain the enzymatic antioxidant defense system and mitochondrial function. The suppression of caspase-3 activation and amelioration of mitochondrial membrane potential loss and nucleus morphology changes were involved in the antiapoptotic effect of wushanicaritin. These findings suggested that wushanicaritin possesses excellent intercellular antioxidant and neuroprotective activities, showing potential promise in functional foods.

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“…Senyawa inhibitor asetilkolinesterase efektif dalam pengobatan gangguan kognitif serta untuk mengurangi demensia. Contoh senyawa obat dari golongan inhibitor asetilkolinesterase yang sering digunakan untuk penyakit Alzheimer yaitu donepezil, rivastigmine, dan galantamine (Santi et al, 2020). Senyawa yang terkandung dalam tanaman juga dapat memberikan efek neuroprotektif untuk mencegah penurunan fungsi kognitif pada penderita penyakit Alzheimer, salah satunya yaitu Asiatikosida yang berasal dari tanaman pegagan.…”

Section: Aunclassified

Studi In Silico Senyawa Asiatikosida H dan I pada Centella asiatica sebagai Senyawa Neuroprotektor

Larasati

Wisnuwardhani

Fakih

2022

BCSP

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Abstract. Alzheimer’s is a neurodegenerative disease characterized by a gradual decline in cognitive function and it leads cause of dementia in the world. To prevent cognitive function decline in patients with Alzheimer’s disease, Asiaticoside compounds in Centella asiatica can be used as an alternative to provide neuroprotective effects. Acetylcholinesterase (AChE) is an important target in pathogenesis of Alzheimer’s disease. This enzyme plays a role in break down acetylcholine as a neurotransmitter. The purpose of this study was to determine the activity of Asiaticoside H and I in inhibiting acetylcholinesterase (AChE) through an in silico approach. In this study, identification of the physicochemical properties of Asiaticoside compounds was carried out using the SwissADME website. Furthermore, Asiaticoside compounds was optimized using Gaussian version 09®. Then a molecular docking simulation of Asiaticoside compounds towards the acetylcholinesterase (AChE) was carried out using MGL Tools version 1.5.6 which has been equipped with Autodock Tools version 4.2. The toxicity prediction of Asiaticoside compounds was carried out using Toxtree version 3.1.0 and Pre-ADMET. Docking simulation results showed that the compound with the lowest binding energy is Asiaticoside E and the best inhibitory activity towards acetylcholinesterase receptor is Asiaticoside D. It can be concluded that the new compounds of Asiaticoside namely Asiaticoside H and I had potential as acetylcholinesterase inhibitors. However, the two new compounds has lower activity and interactions compared to other Asiaticoside derivates. Abstrak. Alzheimer merupakan salah satu penyakit neurodegeneratif yang ditandai dengan penurunan fungsi kognitif secara bertahap dan menjadi penyebab utama demensia di dunia. Untuk mencegah penurunan fungsi kognitif pada penderita penyakit Alzheimer, senyawa Asiatikosida pada tanaman pegagan (Centella asiatica) dapat dijadikan alternatif untuk memberikan efek neuroprotektif. Asetilkolinesterase (AChE) merupakan target penting dalam patogenesis penyakit Alzheimer. Enzim ini berperan memecah asetilkolin sebagai neurotransmitter. Tujuan dilakukannya penelitian ini yaitu untuk mengetahui aktivitas dari senyawa Asiatikosida H dan I dalam menghambat asetilkolinesterase (AChE) melalui pendekatan in silico. Pada penelitian ini dilakukan identifikasi sifat fisikokimia pada senyawa Asiatikosida menggunakan website SwissADME. Selanjutnya senyawa Asiatikosida dilakukan optimasi menggunakan Gaussian 09®. Simulasi molecular docking senyawa uji Asiatikosida terhadap reseptor asetilkolinesterase (AChE) dilakukan dengan menggunakan software MGL Tools 1.5.6 yang telah dilengkapi dengan Autodock Tools versi 4.2. Uji toksisitas dilakukan menggunakan software Toxtree versi 3.1.0 dan website Pre-ADMET. Hasil simulasi docking menunjukkan bahwa senyawa dengan nilai energi bebas ikatan terendah adalah Asiatikosida E dan aktivitas penghambatan pada reseptor asetilkolinesterase (AChE) yang paling baik adalah Asiatikosida D. Hasil penelitian menunjukkan bahwa senyawa Asiatikosida H dan I berpotensi untuk dijadikan sebagai inhibitor asetilkolinesterase, namun aktivitas dan interaksi yang dihasilkan lebih rendah dibandingkan dengan turunan senyawa Asiatikosida yang lainnya.

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Neuroprotective effects of prenylated flavanones isolated from Dalea species, in vitro and in silico studies

Cited by 10 publications

References 60 publications

The psychoactive effects of Bryophyllum pinnatum (Lam.) Oken leaves in young zebrafish

The psychoactive effects of Bryophyllum pinnatum (Lam.) Oken leaves in young zebrafish

From Epimedium to Neuroprotection: Exploring the Potential of Wushanicaritin

Studi In Silico Senyawa Asiatikosida H dan I pada Centella asiatica sebagai Senyawa Neuroprotektor

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