Epilepsy is a chronic neurological disorder with significant treatment challenges, necessitating the search for alternative therapies. This study evaluates the anticonvulsant activity and toxicological profile of Verbesina persicifolia leaf extracts. Methanolic and sequential fractions (hexane, dichloromethane, ethyl acetate, and methanol) were tested using a pentylenetetrazole (PTZ)-induced seizure model in zebrafish (Danio rerio), measuring seizure latency, severity, and survival rates. Phytochemical screening confirmed the presence of flavonoids, alkaloids, and steroids, suggesting potential neuroactive properties. The hexane extracts significantly increased seizure latency and survival rates, with co-administration of hexane extract (5 µg/mL) and diazepam (35.5 µM) further enhancing these effects. Toxicity assessment in Artemia salina indicated low to moderate toxicity in methanolic extracts, while sequential fractions exhibited higher toxicity, particularly in hexane and ethyl acetate extracts. These findings suggest that V. persicifolia extracts exert anticonvulsant effects, likely through GABAergic modulation, and exhibit a favorable safety profile at therapeutic doses. The results support further investigations to isolate active constituents, confirm their mechanisms of action, and explore their potential as plant-derived anticonvulsant agents.

Epilepsy remains a widespread neurological disorder, with approximately 30% of patients showing resistance to current antiepileptic therapies. To address this unmet need, a series of 2-(isoindolin-2-yl) esters derived from natural amino acids were designed and evaluated for their potential interaction with the GABA_A receptor. Sixteen derivatives were subjected to in silico assessments, including physicochemical and ADMET profiling, virtual screening–ensemble docking, and enhanced sampling molecular dynamics simulations (metadynamics calculations). Among these, compounds derived from the aromatic amino acids, phenylalanine, tyrosine, tryptophan, and histidine, exhibited superior predicted affinity, attributed to π–π stacking interactions at the benzodiazepine binding site of the GABA_A receptor. Based on computational performance, the tyrosine and tryptophan derivatives were synthesized and further assessed in vivo using the pentylenetetrazole-induced seizure model in zebrafish (Danio rerio). The tryptophan derivative produced comparable behavioral seizure reduction to the reference drug diazepam at the tested concentrations. The results implies that aromatic amino acid-derived isoindoline esters are promising anticonvulsant candidates and support the hypothesis that π–π interactions may play a critical role in modulating GABA_A receptor binding affinity.

Epilepsy is a chronic neurological disorder with significant treatment challenges, necessitating the search for alternative therapies. This study evaluates the anticonvulsant activity and toxicological profile of Verbesina persicifolia leaf extracts. Methanolic and sequential fractions (hexane, dichloromethane, ethyl acetate, and methanol) were tested using a pentylenetetrazole (PTZ)-induced seizure model in zebrafish (Danio rerio), measuring seizure latency, severity, and survival rates. Phytochemical analysis identified flavonoids, alkaloids, and steroids, suggesting neuroactive potential. Ethyl acetate and hexane fractions significantly increased seizure latency and survival rates, with co-administration of hexane extract and diazepam enhancing these effects. Toxicity assessment in Artemia salina indicated low to moderate toxicity in methanolic extracts, whereas sequential fractions exhibited higher toxicity, particularly in hexane and ethyl acetate extracts. Cell viability assays in chicken embryo fibroblasts confirmed a concentration-dependent safety profile. The findings suggest that V. persicifolia extracts exert anticonvulsant effects, likely through GABAergic modulation, and have a favorable safety profile at therapeutic doses. These results support further investigations to isolate active constituents and explore their potential as plant-derived anticonvulsant agents.

The global health crisis driven by Antimicrobial Resistance (AMR) necessitates an urgent pivot toward novel therapeutic agents, with traditional medicinal plants serving as a critical resource. The Asteraceae genus Verbesina, particularly utilized in Mexican ethnobotany, has garnered scientific attention due to its potent bioactive profile against infection and inflammation. This review provides a comprehensive and critical synthesis of the pharmacological landscape of Verbesina species, focusing specifically on the dual role of its major secondary metabolites, the Sesquiterpene Lactones (SLs), as both cytotoxic and antimicrobial agents. We systematically compile and analyze reported in vitro data, including IC50 values from cancer and non-cancerous cell lines, and MIC values against clinically relevant drug-resistant strains like S. aureus and E. coli. A core focus is placed on establishing the therapeutic index (SI = IC50/MIC) for lead compounds, providing a crucial indicator of drug feasibility. Furthermore, we review the proposed molecular mechanisms of SL action, such as the crucial role of the α-methylene-γ-lactone moiety in alkylating cellular targets, which underpins both their antiproliferative and bactericidal effects. By critically bridging ethnopharmacology with modern mechanistic data, this review validates the translational potential of Verbesina metabolites and highlights clear directions for bioassay-guided isolation and optimization as next-generation anti-resistance scaffolds.

El uso terapéutico de plantas medicinales como sustitutos de medicamentos, o en combinación con estos, ha sido objeto de debate en los últimos años debido a la falta de evidencia científica que respalde sus efectos terapéuticos y a la escasa documentación sobre sus efectos biológicos y farmacológicos. Por lo tanto, es importante continuar investigando su utilización terapéutica, especialmente en términos de su toxicidad. En México, al igual que en otras partes del mundo, las plantas medicinales se utilizan como tratamiento primario para malestares moderados a leves, principalmente debido a la falta de acceso y/o a los altos costos de los medicamentos, así como al arraigo cultural de la medicina ancestral. El uso de plantas medicinales como alternativa terapéutica podría ser una opción viable, sin embargo, es necesario estar bien informado sobre su uso y eficacia para obtener los resultados esperados.

México es un país con una riqueza vegetal importante, ya que concentra alrededor del 10% de todas las especies vegetales existentes en el mundo. La familia Asteraceae es amplia y contiene una gran variedad de metabolitos secundarios, los cuales tienen potencial como nuevos tratamientos para una diversa gama de enfermedades. Un ejemplo es el género Verbesina, el cual tiene actividad antiinflamatoria, antioxidante, antibacteriana, antifúngica, anticriptocócica, antiacné y cicatrizante. Por otro lado, dentro del género Verbesina se han reportado familias de metabolitos secundarios tales como: terpenoides y triterpenoides, flavonoides, alcaloides, sesquiterpenos, eudesmanos y saponinas. Una especie de interés perteneciente a este género es Verbesina persicifolia DC, la cual se distribuye ampliamente desde Canadá hasta Sudamérica. En México, Verbesina persicifolia DC también es conocida popularmente como “Huichín”, “Taxiwua”, “Xilpopotok” y “Tlamacas”. Aun cuando existen pocos estudios, se ha reportado que esta planta ejerce efectos antiobesidad, antiinflamatorio, hipoglucemiante y antiproliferativo. Asimismo, los estudios fitoquímicos indican que esta especie tiene sesquiterpenlactonas, eudesmanos y terpenos. Sin embargo, la escasa información relacionada con la actividad farmacológica y la caracterización química de esta planta, aunado a los diferentes usos etnomédicos que tiene, pone de relieve la necesidad de estudios sistemáticos que permitan validar su uso e identificar los metabolitos responsables de los efectos farmacológicos de Verbesina persicifolia DC.