First chemical evaluation and toxicity of Casinga-cheirosa to Balb-c male mice.
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.
Graduate Program in Veterinary, Graduate and Research Vice-Dean Office, Paulista University, R. Dr. Bacelar, 1212, Vila Clementino, São Paulo 04026-002, Brazil. dirceestork@gmail.com.
Dirce M
DM
Estork
Graduate Program in Veterinary, Graduate and Research Vice-Dean Office, Paulista University, R. Dr. Bacelar, 1212, Vila Clementino, São Paulo 04026-002, Brazil. o@yahoo.com.br.
Daniela F
DF
Gusmão
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. mbpaciencia@hotmail.com.
Mateus L B
ML
Paciencia
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. ingrit-uni@hotmail.com.
Ingrit E C
IE
Díaz
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. drvarella@yahoo.com.br.
Antonio D
AD
Varella
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. rnyounes@yahoo.com.
Riad N
RN
Younes
Education and Research Center, Sírio Libanês Hospital, R. Adma Jafet, 91, Bela Vista, São Paulo 01308-000, SP, Brazil. luiz.reis@hsl.org.br.
Luiz F L
LF
Reis
Medicine College, São Paulo University, LIM-62, Av. Dr. Arnaldo, 455, Pinheiros, São Paulo 01246-000, SP, Brazil. edna.montero@gmail.com.
Edna F S
EF
Montero
Graduate Program in Veterinary, Graduate and Research Vice-Dean Office, Paulista University, R. Dr. Bacelar, 1212, Vila Clementino, São Paulo 04026-002, Brazil. marthabernardi@gmail.com.
Maria M
MM
Bernardi
Graduate Program in Veterinary, Graduate and Research Vice-Dean Office, Paulista University, R. Dr. Bacelar, 1212, Vila Clementino, São Paulo 04026-002, Brazil. ibsuffredini@yahoo.com.br.
Ivana B
IB
Suffredini
D000818:Animals; D001835:Body Weight; D003975:Diazepam / Q000633:toxicity; D006471:Gastrointestinal Hemorrhage / Q000139:chemically induced* / Q000473:pathology; D006801:Humans; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D009929:Organ Size; D010863:Piloerection / Q000187:drug effects; D010936:Plant Extracts / Q000737:chemistry / Q000633:toxicity*; D011794:Quercetin / Q000031:analogs & derivatives / Q000302:isolation & purification; D011801:Quinic Acid / Q000031:analogs & derivatives / Q000302:isolation & purification; D012119:Respiration / Q000187:drug effects; D031308:Salicaceae / Q000737:chemistry*; D012855:Sitosterols / Q000302:isolation & purification; D024502:alpha-Tocopherol / Q000302:isolation & purification
D010936:Plant Extracts; D012855:Sitosterols; D011801:Quinic Acid; C016527:isoquercitrin; C025473:gamma-sitosterol; C021304:hyperoside; D011794:Quercetin; D024502:alpha-Tocopherol; D003975:Diazepam