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1.
Chem Biodivers ; 21(3): e202301807, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38284478

RESUMEN

The Piper genus, known for its pharmacological potential, comprises 2,263 species primarily found in tropical regions. Despite recent advancements in pain therapies, the demand for more effective and well-tolerated analgesics and anti-inflammatories, particularly for chronic pain, remains. This study assessed the effects of essential oils from Piper caldense, Piper mosenii, and Piper mikanianum on nociceptive behavior induced by formalin and capsaicin, as well as their anti-inflammatory impact induced by carrageenan, using adult zebrafish models. Results indicated non-toxic essential oils with antinociceptive properties in both neurogenic and inflammatory phases of formalin-induced nociception through interaction with the TRPA1 receptor. Additionally, P. mosenii essential oil also blocked the nociceptive effect of capsaicin, a TRPV1 receptor agonist. Furthermore, essential oils from P. caldense and P. mikanianum exhibited significant anti-inflammatory effects by reducing carrageenan-induced abdominal edema. These findings highlight the pharmacological potential of Piper's essential oils as antinociceptive and anti-inflammatory agents.


Asunto(s)
Aceites Volátiles , Piper , Animales , Carragenina/efectos adversos , Pez Cebra , Aceites Volátiles/farmacología , Aceites Volátiles/uso terapéutico , Capsaicina , Analgésicos/farmacología , Analgésicos/uso terapéutico , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Extractos Vegetales/farmacología , Formaldehído/efectos adversos , Edema/inducido químicamente , Edema/tratamiento farmacológico
2.
Fundam Clin Pharmacol ; 36(5): 818-826, 2022 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-35261066

RESUMEN

Drugs used to manage type 2 diabetes mellitus cause adverse effects. Therefore, the search for new drugs as an alternative for the treatment of diabetes increases. The effect of triterpene 3ß-6ß-16ß-trihydroxylup-20(29)-ene isolated from the leaves of C. leprosum (CLF-1) on sucrose-induced hyperglycemia in adult zebrafish (Danio rerio) was evaluated. Initially, adult zebrafish (n = 6/group) underwent hyperglycemia induction by sucrose at 83.25 mM/L for 7 days by immersion. The hyperglycemic groups were treated with CLF-1 (4, 20, and 40 mg/kg), metformin (200 mg/kg), and acarbose (300 mg/kg) for 4 days. The in silico interaction of CLF-1, metformin, and acarbose with the enzyme maltase-glucoamylase (CtMGAM) was investigated. CLF-1 reduced sucrose-induced hyperglycemia after 4 days of treatment, in addition to having better affinity energy with CtMGAM than metformin and acarbose. Thus, CLF-1 may be a new pharmacological alternative as a hypoglycemic agent for the treatment of diabetes.


Asunto(s)
Combretum , Diabetes Mellitus Tipo 2 , Hiperglucemia , Metformina , Triterpenos , Acarbosa/farmacología , Animales , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Hiperglucemia/inducido químicamente , Hiperglucemia/tratamiento farmacológico , Hipoglucemiantes/farmacología , Extractos Vegetales/farmacología , Hojas de la Planta , Sacarosa , Triterpenos/farmacología , Triterpenos/uso terapéutico , Pez Cebra
3.
J Biomol Struct Dyn ; 40(20): 9801-9814, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-34121622

RESUMEN

Combretaceae are reported in the literature for presenting neuroprotective and anxiolytic effects in animal models. Combretum lanceolatum Pohl. has few scientific reports on its pharmacological effects. The aim of this study was to evaluate the anxiolytic and anticonvulsant effects of the ethanol extract from the leaves of C. lanceolatum Pohl. (EtFoCl) and its possible mechanism of GABAergic action in adult zebrafish. EtFoCl was subjected to determination of the total phenol concentration, identification of phytochemical flavonoids by HPLC and in vitro antioxidant activity test, open field test and 96-hour acute toxicity in zebrafish. Anxiolytic doses were tested for pentylenetetrazole-induced seizures in adult zebrafish. To study the mechanisms of action, molecular docking simulations were performed between the main phytochemicals and the GABAA receptor (anxiolytic activity) and carbonic anhydrase II (anticonvulsant). The non-toxic doses that caused motor impairment were assessed in acute and chronic anxiety using the light and dark test. EtFoCl had altered the animals' locomotion, presenting an effect similar to the anxiolytic and anticonvulsant. These effects were prevented with flumazenil (GABAA antagonist). The phytochemicals homoorientin and quercetin-3-O-galactoside coupling in a region close to that of the inhibitor diazepam (GABAA receptor). Regarding the anticonvulsant mechanism, Homoorientina and Isovitexina were identified as the most favorable for the complex form with the carbonic anhydrase enzyme. C. lanceolatum has pharmacological potential for the treatment of acute and chronic anxiety and seizures, which can be partially explained by an interaction with the GABAA receptor.Communicated by Ramaswamy H. Sarma.


Asunto(s)
Ansiolíticos , Combretum , Animales , Ansiolíticos/efectos adversos , Pez Cebra , Receptores de GABA-A , Anticonvulsivantes/farmacología , Simulación del Acoplamiento Molecular , Convulsiones/inducido químicamente , Convulsiones/tratamiento farmacológico , Ansiedad/tratamiento farmacológico , Extractos Vegetales/farmacología
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