First Chemical Evaluation and Toxicity of Casinga-cheirosa to Balb-c Male Mice

Molecules

Dirce M. Estork³  Daniela F. Gusmão³  Mateus L. B. Paciencia²  Ingrit E. C. D໚z²  Antonio D. Varella²  Riad N. Younes²  Luiz F. L. Reis¹  Edna F. S. Montero⁴  Maria M. Bernardi³ 

[1] Education and Research Center, Sírio Libanês Hospital, R. Adma Jafet, 91, Bela Vista, São Paulo 01308-000, SP, Brazil; E-Mail:;Center for Research in Biodiversity, Botany Laboratory and Herbarium UNIP and Extraction Laboratory, Paulista University, Av. Paulista, 900, 1° andar, Cerqueira César, São Paulo 01310-100, Brazil; E-Mails:;Graduate Program in Veterinary, Graduate and Research Vice-Dean Office, Paulista University, R. Dr. Bacelar, 1212, Vila Clementino, São Paulo 04026-002, Brazil; E-Mails:;Medicine College, São Paulo University, LIM-62, Av. Dr. Arnaldo, 455, Pinheiros, São Paulo 01246-000, SP, Brazil; E-Mail:

关键词: Laetia suaveolens;    Salicaceae;    toxicity;    α-tocopherol;    isoquercitrin;   

DOI  :  10.3390/molecules19043973

来源: mdpi

【 摘 要 】

Laetia suaveolens, known as “casinga-cheirosa”, crude extract EB719 has previously shown cytotoxic activity against prostate cancer and squamous cell carcinoma. For the first time, seven molecules were isolated from its apolar—α-tocopherol (1) and sitosterol (2)—and polar—3-O-caffeoylquinic acid (3), 4-O-caffeoylquinic acid (4), 5-O-feruloylquinic acid (5), hyperoside (6), and isoquercitrin (7)—fractions. Acute toxicity was determined in a two-stage experiment: (1) a reduced number of Balb-c male mice received 5000 mg/kg of EB719 to allow evaluation of general activity and other 27 parameters, plus death, up to the establishment of non-lethal dose (NLD), as well as lethal dose 50% (LD₅₀); (2) NLD was administered and diazepam introduced as reference drug. EB719 showed LD₅₀ = 178.0 mg/kg, and NLD 156.3 mg/kg. In stage one EB719 did not influence general activity, but provoked impairment in grasp reflexes, tail squeeze and breathing; piloerection and cyanosis were increased. In stage two, alterations occurred in auricular reflex, piloerection and breathing after diazepam administration, but not in response to EB719. Intestinal hemorrhage caused by local bleeding was observed after necropsy, and may be the main cause of animals’ death other than a systemic effect of the extract. Although the isolated compounds are biologically and pharmacologically active in both men and animal systems, it is premature to relate their occurrence in EB719 to the observed intestine hemorrhage in mice.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.