ABSTRACT
Croton cajucara Benth showed several pharmacological properties such as: anti-inflammatory, antinociceptive hypoglycemic, lipid-lowering, antiulcer, antiestrogenic, antitumor, antigenotoxic, antimutagenic, and cardiovascular. The 19-nor-clerodane diterpene trans-dehydrocrotonin (t-DCTN or DCTN) is the major bioactive constituent extracted from the bark of this Croton. Patents for Croton cajucara Benth in the period 2015 to 2022 comprises 14 published documents. Among them 4 patents are colloidal systems (SM/SNEDDS) loading t-DCTN for pharmacological applications. Patent registrations highlighted the huge promising biotechnological potential of Croton cajucara Benth especially in the phytotherapy field, and the correlation with its bioactive constituents of which t-DCTN showed the foremost results, so this herbal could become an alternative in the treatment of Covid-19. However, investigation of more recently published patents for clerodane diterpenes with similar chemical structure of t-DCTN, who previously showed antiviral property must be carried out and should be searched on several patent data bases.
ABSTRACT
This study examined the effect of trans-dehydrocrotonin (DCTN), a 19-nor-clerodane diterpene isolated from Croton cajucara Benth (Euphorbiaceae), as analgesic and its effect on the central nervous system (CNS) of rodents using different animal models. The DCTN intraperitoneally exhibited mild analgesic activity on hot-plate test, but exhibited strong antinociceptive activity against acetic acid-induced abdominal writhing and the ED50 was calculated to be 44.88 mg/kg. At higher doses (100 mg/kg) it exhibited mild CNS depressant activities in laboratory animals. Moreover, it has negligible antidepressant activity. After taking consideration of the drug interaction, the DCTN can be used as a potent analgesic agent in case of peripheral algesia, without affecting the CNS.
Neste estudo avaliou-se o efeito analgésico do diterpeno 19-nor-clerodano trans-desidrocrotonina (DCTN) isolado de Croton cajucara Benth (Euphorbiaceae), bem como seu efeito no sistema nervoso central utilizando-se diferentes tipos de modelos de animais roedores. A administração intraperitoneal deste diterpeno, no teste da placa quente, revelou sua atividade analgésica moderada. No entanto, no teste de contrações abdominais desencadeadas por ácido acético, a DCTN apresentou forte atividade antinociceptiva com DE50 de 44,88 mg/kg. Doses elevadas de DCTN (100 mg/kg) apresentaram moderada atividade depressiva do sistema nervoso central (SNC), não tendo sido evidenciado ação antidepressiva. Após algumas considerações da ação de DCTN em algesia periférica, concluiu-se que esta substância pode ser utilizada como um potente agente analgésico, sem afetar o SNC.
