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

Author(s)

Estork, Dirce M. ^[1] ; Gusmao, Daniela F. ^[1] ; Paciencia, Mateus L. B. ^{[2, 3, 4]} ; Diaz, Ingrit E. C. ^{[2, 3, 4]} ; Varella, Antonio D. ^{[2, 3, 4]} ; Younes, Riad N. ^{[2, 3, 4, 5]} ; Reis, Luiz F. L. ^[6] ; Montero, Edna F. S. ^[7] ; Bernardi, Maria M. ^{[1, 8]} ; Suffredini, Ivana B. ^{[1, 2, 3, 4, 8]}

Affiliation

^[1] Univ Paulista, Grad & Res Vice Dean Off, Grad Program Vet, BR-04026002 Sao Paulo - Brazil

^[2] Univ Paulista, Bot Lab, Ctr Res Biodivers, BR-01310100 Sao Paulo - Brazil

^[3] Univ Paulista, Herbarium UNIP, BR-01310100 Sao Paulo - Brazil

^[4] Univ Paulista, Extract Lab, BR-01310100 Sao Paulo - Brazil

^[5] Hosp Sao Jose, BR-1321001 Sao Paulo - Brazil

^[6] Sirio Libanes Hosp, Educ & Res Ctr, BR-01308000 Sao Paulo - Brazil

^[7] Univ Sao Paulo, Coll Med, BR-01246000 Sao Paulo - Brazil

^[8] Univ Paulista, Grad & Res Vice Dean Off, Grad Program Dent, BR-04026002 Sao Paulo - Brazil

• Document type: Journal article
• Source: Molecules; v. 19, n. 4, p. 3973-3987, APR 2014.
• Web of Science Citations: 11

Abstract

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-alpha-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. (AU)