Avarol derivatives as competitive AChE inhibitors, non hepatotoxic and neuroprotective agents for Alzheimer’s disease

Tommonaro, Giuseppina; García-Font, Nuria; Vitale, Rosa Maria; Pejin, Boris; Iodice, Carmine; Cañadas, S.; Marco‐Contelles, José; Oset-Gasque, María Jesús

doi:10.1016/j.ejmech.2016.06.036

Cited by 44 publications

(17 citation statements)

References 45 publications

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“…Trigonothyrins A–C ( 125 – 127 ) have been isolated from the stems of Trigonostemonthyrsoideum [6]. Among them, trigonothyrin C has shown significant activity to prevent the cytopathic effects of HIV-1 in C8166 cells, with an EC 50 value of 2.19 µg/mL [35]. Compounds genkwanines F, I, and J ( 93 , 113 , 114 ) have been isolated from the flower buds of Daphne genkwa [14].…”

Section: Species Of Daphnane-type Diterpenoids and Their Bioactivementioning

confidence: 99%

A Review on Daphnane-Type Diterpenoids and Their Bioactive Studies

Jin

Shi²,

Zhang

et al. 2019

Molecules

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Natural daphnane diterpenoids, mainly distributed in plants of the Thymelaeaceae and Euphorbiaceae families, usually include a 5/7/6-tricyclic ring system with poly-hydroxyl groups located at C-3, C-4, C-5, C-9, C-13, C-14, or C-20, while some special types have a characteristic orthoester motif triaxially connectedat C-9, C-13, and C-14. The daphnane-type diterpenoids can be classified into five types: 6-epoxy daphnane diterpenoids, resiniferonoids, genkwanines, 1-alkyldaphnanes and rediocides, based on the oxygen-containing functions at rings B and C, as well as the substitution pattern of ring A. Up to now, nearly 200 daphnane-type diterpenoids have been isolated and elucidated from the Thymelaeaceae and Euphorbiaceae families. In-vitro and in-vivo experiments of these compounds have shown that they possess a wide range of biological activities, including anti-HIV, anti-cancer, anti-leukemic, neurotrophic, pesticidal and cytotoxic effects. A comprehensive account of the structural diversity is given in this review, along with the cytotoxic activities of daphnane-type diterpenoids, up to April 2019.

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Section: Species Of Daphnane-type Diterpenoids and Their Bioactivementioning

confidence: 99%

A Review on Daphnane-Type Diterpenoids and Their Bioactive Studies

Jin

Shi²,

Zhang

et al. 2019

Molecules

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“…Plant products as isolates or synthetic derivatives have been widely reported for their biological efficacies against various diseases (Pejin, Iodice, Tommonaro, & De Rosa, 2008; Pejin et al, 2014; Tommonaro et al, 2016). Thymoquinone (Tq) is one such active ingredient of Black Caraway seed ( Nigella Sativa ), which is widely used in traditional medicine of the Middle East (Padhye, Banerjee, Ahmad, Mohammad, & Sarkar, 2008).…”

Section: Introductionmentioning

confidence: 99%

Thymoquinone attenuates IgE‐mediated allergic response via pi3k‐Akt‐NFκB pathway and upregulation of the Nrf2‐HO1 axis

et al. 2020

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IgE‐dependent reactions mediate the majority of allergic diseases. This study explores the effects of thymoquinone (Tq) on IgE‐mediated allergic response in activated mast cells, basophils, and neutrophils. Tq treatment resulted in a dose‐dependent decrease in levels of TNF‐α and IL‐4 in activated RBL‐2H3 cells. Tq inhibited the degranulation of these cells with an IC50 value of 56.37 µM. Moreover, the compound suppressed basophil activation induced through FcεRI receptors with an IC50 value of 45.76 µM in heparinized human whole blood. Likewise, neutrophil migration and elastase activity were dose‐dependently reduced. While Tq decreased the phosphorylation of Akt and NFκB in activated RBL‐2H3 cells, it increased nuclear Nrf2 and HO‐1 antioxidant proteins. Our results indicate that Tq possesses demonstrable activity in cellular models of IgE‐mediated allergic reactions. Practical applications The current study sheds light on the mechanistic pathways of Tq on IgE‐based response in activated mast cells, basophils, and neutrophils. The output of this preclinical in vitro study may be translated into better chemotherapeutic applications of Tq and its analogs in the treatment of allergic inflammation. However, a detailed investigation of in vivo models is recommended.

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“…Also, zonarol from the brown alga Dictyopteris undulata can protect mice against dextran-sulfate-sodium-induced UC via the inhibition of both inflammation and apoptosis [38]. It is speculated that some compounds with similar structure to zonarol may also have the effect of treating UC based on its anti-inflammatory effect, such as avarol, avarone, avarol-3'-thiosalicylate, and so on [39][40][41].…”

Section: Discussionmentioning

confidence: 99%

Improvement of Oxazolone-Induced Ulcerative Colitis in Rats Using Andrographolide

et al. 2019

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Ulcerative colitis (UC) is usually accompanied with symptoms of abdominal pain, diarrhea, and bloody stool, which impair the quality of life of patients. Previous studies have shown that Andrographis paniculata extracts, which have andrographolide (AND) as their main compound, can relieve UC symptoms in patients. The aim of the study was to investigate the alleviating effect of AND on UC using the oxazolone (OXZ)-induced UC rat model. A total of 66 healthy male Sprague Dawley rats were used to evaluate the efficacy and mechanism of AND on UC (n = 11 per group) and grouped into control, model, SASP (sulfasalazine, positive control group, 500 mg/kg), AND-L (40 mg/kg), AND-M (80 mg/kg), and AND-H (120 mg/kg). The colonic disease activity index (DAI), colon length, spleen coefficient, pathological damage, and inflammation-related cytokine and protein expression levels were used as indices for evaluation. Results showed that the AND groups had reduced DAI and mortality, and significantly improved colon length and spleen coefficient compared with the model group. Furthermore, OXZ-induced histological injury was relieved significantly after AND treatment due to an improved crypt structure and reduced infiltration of inflammatory cells. Moreover, AND inhibited myeloperoxidase (MPO) activity and the secretion of interleukin-4 (IL-4), IL-13, and tumor necrosis factor α (TNF-α). The results of the anti-inflammatory mechanism revealed that AND blocked the signal transduction by reducing IL-4/IL-13 specific binding to IL-4 receptor (IL-4R) and inhibiting the phosphorylation of the signal transducer and activator of transcription 6 (p-STAT6). In conclusion, aside from natural plants, AND may be a candidate ingredient for UC therapy.

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Avarol derivatives as competitive AChE inhibitors, non hepatotoxic and neuroprotective agents for Alzheimer’s disease

Cited by 44 publications

References 45 publications

A Review on Daphnane-Type Diterpenoids and Their Bioactive Studies

A Review on Daphnane-Type Diterpenoids and Their Bioactive Studies

Thymoquinone attenuates IgE‐mediated allergic response via pi3k‐Akt‐NFκB pathway and upregulation of the Nrf2‐HO1 axis

Improvement of Oxazolone-Induced Ulcerative Colitis in Rats Using Andrographolide

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