Behavioral effects induced by antitumor cleronade diterpenes from Casearia sylvestris and in silico interactions with neuron receptors

Araújo, Éverton José Ferreira de; Almeida, Antônia Amanda Cardoso de; Silva, Oskar Almeida; Costa, Iwyson Henrique Fernandes da; Rezende-Júnior, Luís Mário; Lima, Francisco das Chagas Alves; Cavalheiro, Alberto José; Pessoa, Cláudia; Moraes, Manoel Odoríco de; Ferreira, Paulo Michel Pinheiro

doi:10.1016/j.jep.2017.01.006

Cited by 13 publications

(4 citation statements)

References 62 publications

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“…Exploratory activity was verified using an open field made of acrylic (transparent walls and black floor, with dimensions of 30 × 30 × 15 cm) divided into nine quadrants and based on the model described by Archer and Araújo et al . Thirty minutes after the treatment, animals were placed in the center of the open field.…”

Section: Methodsmentioning

confidence: 99%

Phytol as an anticarcinogenic and antitumoral agent: An in vivo study in swiss mice with DMBA‐Induced breast cancer

et al. 2018

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Phytol (PHY) (3,7,11,15‐tetramethylhexadec‐2‐en‐1‐ol) exhibits various pharmacological properties including toxicity and cytotoxicity, and exerts antitumor activity. Owing to the urgent need of new pharmaceutical formulations for breast cancer therapy, this study aimed at the evaluation of antitumor activity of PHY in 7,12‐dimethylbenzanthracene‐cancer‐induced animal model. Comet assay was employed to evaluate the cytogenetics, DNA repair, and antigenotoxic activities of PHY in neoplastic (breast) and non‐neoplastic rodent cells (bone marrow, lymphocytes, and liver). Additionally, hematological, biochemical, histopathological, and immunohistochemical analyses were carried out in experimental animals. Thirty nonpregnant female mice (n = 5) underwent 7 weeks treatment with 6 mg/kg pro‐carcinogen, PHY (4 mg/kg), and cyclophosphamide (25 mg/kg). Induction of cancer was confirmed by histopathology and immunohistochemistry for Ki‐67. Results suggest that PHY exhibits low toxicity in comparison with other groups in hematological, biochemical, histopathological, and organ size parameters. Additionally, PHY showed modulatory effects on the pro‐carcinogen, and induced genotoxicity and apoptosis in breast cancer cells. Furthermore, it showed a DNA damage repair capacity in mouse lymphocytes. These data indicate that PHY may have the potential as an anticancer candidate in pharmaceutical consumption. © 2018 IUBMB Life, 71(1):200–212, 2019

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Section: Methodsmentioning

confidence: 99%

Phytol as an anticarcinogenic and antitumoral agent: An in vivo study in swiss mice with DMBA‐Induced breast cancer

et al. 2018

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“…Chromatographic analysis of HCE-CS used in this study revealed the presence of several casearins including casearin-X, which was already implicated for its capability of coupling to GABA-A comples neuron receptors (de Araújo et al, 2017), what could influence pain phenomena. In the other hand, our results with the CRPS-I model demonstrate that a selective ALX/FPR2 antagonist (Shin et al, 2006), WRW4 prevented the antihyperalgesic action for HCE-CS or BML-111 implicating this receptor in modulatory mechanisms on nociception exerted by these treatments during the inflammatory phase of this experimental disease.…”

Section: Discussionmentioning

confidence: 74%

Hydroalcoholic crude extract of Casearia sylvestris Sw. reduces chronic post-ischemic pain by activation of pro-resolving pathways

Piovezan

Batisti

Benevides

et al. 2017

Journal of Ethnopharmacology

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Ethnopharmacological relevanceCasearia sylvestris Sw. is widely used in popular medicine to treat conditions associated with pain. Aim of the studyThe present study investigated the influence of hydroalcoholic crude extract of Casearia sylvestris (HCE-CS) and contribution of pro-resolving mediators on mechanical hyperalgesia in a mouse model of chronic post-ischemia pain (CPIP). Methods and resultsMale Swiss mice were subjected to ischemia of the right hind paw (3 h ConclusionThese results reveal significant antihyperalgesic effect of HCE-CS on CPIP, mediated at least in part, by the pathway of resolution of inflammation centred on the axis modulated by ALX/FPR2.

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“…All efforts were made to minimize animal pain, suffering, or discomfort. Doses used were based on previous pharmacological investigations of the group [19,21,23].…”

Section: Animals and Ethical Aspectsmentioning

confidence: 99%

“…Among them, Casearia (Salicaceae) comprises about 180 species distributed in sub-tropical and tropical regions [16] and has promising anticancer effects [17][18][19]. In Brazil, Casearia sylvestris Sw. is the most known species and has shown antifungal [20], anxiolytic [21], antibacterial [22], antioxidant [23,24], antileishmanial [25], anti-inflammatory [26,27], and antimicrobial [24,28] activities.…”

Section: Introductionmentioning

confidence: 99%

Promising Effects of Casearins in Tumor-Bearing Mice and Antinociceptive Action against Oncologic Pain: Molecular Docking and In Vivo Findings

Silva,

Beserra Filho,

Acha

et al. 2024

Pharmaceuticals

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Safer analgesic drugs remain a hard challenge because of cardiovascular and/or gastrointestinal toxicity, mainly. So, this study evaluated in vivo the antiproliferative actions of a fraction with casearins (FC) from Casearia sylvestris leaves against human colorectal carcinomas and antihyperalgesic effects on inflammatory- or opiate-based pain relief and oncologic pain in Sarcoma 180 (S180)-bearing mice. Moreover, docking investigations evaluated the binding among Casearin X and NMDA(N-methyl-D-aspartate)-type glutamate receptors. HCT-116 colorectal carcinoma-xenografted mice were treated with FC for 15 days. Antinociceptive assays included chemically induced algesia and investigated mechanisms by pharmacological blockade. Intraplantar region S180-bearing animals received a single dose of FC and were examined for mechanical allodynia and behavior alterations. AutoDock Vina determined molecular interactions among Cas X and NMDA receptor subunits. FC reduced tumor growth at i.p. (5 and 10 mg/kg) and oral (25 mg/kg/day) doses (31.12–39.27%). FC reduced abdominal pain, as confirmed by formalin and glutamate protocols, whose antinociception activity was blocked by naloxone and L-NAME (neurogenic phase) and naloxone, atropine, and flumazenil (inflammatory phase). Meanwhile, glibenclamide potentiated the FC analgesic effects. FC increased the paw withdrawal threshold without producing changes in exploratory parameters or motor coordination. Cas X generated a more stable complex with active sites of the NMDA receptor GluN2B subunits. FC is a promising antitumor agent against colorectal carcinomas, has peripheral analgesic effects by desensitizing secondary afferent neurons, and inhibits glutamate release from presynaptic neurons and/or their action on cognate receptors. These findings emphasize the use of clerodane diterpenes against cancer-related pain conditions.

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Behavioral effects induced by antitumor cleronade diterpenes from Casearia sylvestris and in silico interactions with neuron receptors

Abstract: Findings indicate a probable anxiolytic action of the FC since it reduces the number of crossings and rearings and prolonged the time spent in open arms, without sedative and myorelaxant effects, probably due to the interaction of Cas X with dopaminergic system.

Cited by 13 publications

References 62 publications

Phytol as an anticarcinogenic and antitumoral agent: An in vivo study in swiss mice with DMBA‐Induced breast cancer

Phytol as an anticarcinogenic and antitumoral agent: An in vivo study in swiss mice with DMBA‐Induced breast cancer

Hydroalcoholic crude extract of Casearia sylvestris Sw. reduces chronic post-ischemic pain by activation of pro-resolving pathways

Promising Effects of Casearins in Tumor-Bearing Mice and Antinociceptive Action against Oncologic Pain: Molecular Docking and In Vivo Findings

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