First chemical evaluation and toxicity of Casinga-cheirosa to Balb-c male mice
| Autor: | Antonio Drauzio Varella, Luiz F. L. Reis, Maria Martha Bernardi, Ingrit Elida Collantes Díaz, Daniela F. Gusmão, Edna Frasson de Souza Montero, Riad Naim Younes, Ivana Barbosa Suffredini, Dirce M. Estork, Mateus Luís Barradas Paciencia |
|---|---|
| Rok vydání: | 2014 |
| Předmět: |
Male
medicine.medical_specialty Salicaceae alpha-Tocopherol Quinic Acid Pharmaceutical Science Pharmacology Median lethal dose Laetia suaveolens toxicity α-tocopherol isoquercitrin Article Analytical Chemistry BALB/c Intestinal Hemorrhage Piloerection lcsh:QD241-441 Lethal Dose 50 Mice lcsh:Organic chemistry Drug Discovery medicine Animals Humans Physical and Theoretical Chemistry Mice Inbred BALB C Diazepam biology Plant Extracts Respiration Organic Chemistry Body Weight Organ Size biology.organism_classification Sitosterols Acute toxicity Surgery Chemistry (miscellaneous) Toxicity Reflex Molecular Medicine Quercetin Gastrointestinal Hemorrhage medicine.drug |
| Zdroj: | Molecules Molecules, Vol 19, Iss 4, Pp 3973-3987 (2014) Molecules; Volume 19; Issue 4; Pages: 3973-3987 |
| ISSN: | 1420-3049 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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