Sikiru Olaitan Balogun1, Iberê Ferreira da Silva1, Edson Moleta Colodel2, Ruberlei Godinho de Oliveira1, Sérgio Donizeti Ascêncio3, Domingos Tabajara de Oliveira Martins4. 1. Department of Basic Sciences in Health, Faculty of Medicine, Federal University of Mato Grosso (UFMT), 78060-900 Cuiabá, MT, Brazil. 2. Laboratory of Veterinary Pathology, Faculty of Agronomy and Veterinary Medicine, Federal University of Mato Grosso (UFMT), 78060-900 Cuiabá, MT, Brazil. 3. Faculty of Medicine, Federal University of Tocantins (UFT), Av. NS15, BALA Block,11 C Room, Palmas 77020-210, Tocantins, Brazil. 4. Department of Basic Sciences in Health, Faculty of Medicine, Federal University of Mato Grosso (UFMT), 78060-900 Cuiabá, MT, Brazil. Electronic address: taba@terra.com.br.
Abstract
ETHNOPHARMACOLOGICAL RELEVANCE: Helicteres sacarolha, popularly known in Brazil as 'rosquinha', 'sacarolhas', 'semente-de-macaco', is widely distributed in different phytogeographic zones in Brazil. Preparations from its roots and leaves are employed in popular Brazilian medicine in the treatments of ailments such as peptic ulcer, hypertension among others. Cytotoxicity, acute oral and subchronic toxicity of the hydroethanolic extract of Helicteres sacrolha was investigated as well as the classes of phytochemical present in the extract. MATERIALS AND METHODS: Hydroethanolic (70%) extract of Helicteres sacarolha (HEHs) was prepared by maceration. Potential cytotoxicity was evaluated in CHO-k1 cells. Acute administration of HEHs was done in mice as a single dose up to 5000mg/kg and subchronic oral toxicity study for 30 days in Wistar rats at daily oral doses of 0, 250 and 750mg/kg b.w. Clinical observations and toxicological related parameters were determined every 6 days. Blood was collected for biochemical and hematological analyses, while histological examinations were performed on selected organs. Selected secondary metabolites detected were quantified by UV-spectrophotometry and high performance liquid chromatography (HPLC). RESULTS: The extract was non-cytotoxic to CHO-k1 cells. In acute oral toxicity, there was no mortality or clinical alterations in the female mice, at all doses, except for the transient diarrhea observed at 5000mg/kg acute. Doses up to 2000mg/kg caused no mortality or treatment-related clinical manifestations in the male mice, but treatment-related alterations were however observed at 4000mg/kg, with mortalities recorded at 5000mg/kg. During the subchronic oral toxicity study, no mortality or treatment-related clinical signs were observed. Differences in relative organ weight, hematological parameters and histopathology observations between the treated and the control groups were considered not to be treatment-related. Spectrophotometric analysis revealed the presence of relatively high content of phenolics and flavonoids in HEHs. HPLC analysis confirmed the presence of the quantified compounds and demonstrated the presence of ellagic acid, morin and naringin. CONCLUSION: Our results confirmed that HEHs have a broad safety margin for therapeutic use.
ETHNOPHARMACOLOGICAL RELEVANCE: Helicteres sacarolha, popularly known in Brazil as 'rosquinha', 'sacarolhas', 'semente-de-macaco', is widely distributed in different phytogeographic zones in Brazil. Preparations from its roots and leaves are employed in popular Brazilian medicine in the treatments of ailments such as peptic ulcer, hypertension among others. Cytotoxicity, acute oral and subchronic toxicity of the hydroethanolic extract of Helicteres sacrolha was investigated as well as the classes of phytochemical present in the extract. MATERIALS AND METHODS:Hydroethanolic (70%) extract of Helicteres sacarolha (HEHs) was prepared by maceration. Potential cytotoxicity was evaluated in CHO-k1 cells. Acute administration of HEHs was done in mice as a single dose up to 5000mg/kg and subchronic oral toxicity study for 30 days in Wistar rats at daily oral doses of 0, 250 and 750mg/kg b.w. Clinical observations and toxicological related parameters were determined every 6 days. Blood was collected for biochemical and hematological analyses, while histological examinations were performed on selected organs. Selected secondary metabolites detected were quantified by UV-spectrophotometry and high performance liquid chromatography (HPLC). RESULTS: The extract was non-cytotoxic to CHO-k1 cells. In acute oral toxicity, there was no mortality or clinical alterations in the female mice, at all doses, except for the transient diarrhea observed at 5000mg/kg acute. Doses up to 2000mg/kg caused no mortality or treatment-related clinical manifestations in the male mice, but treatment-related alterations were however observed at 4000mg/kg, with mortalities recorded at 5000mg/kg. During the subchronic oral toxicity study, no mortality or treatment-related clinical signs were observed. Differences in relative organ weight, hematological parameters and histopathology observations between the treated and the control groups were considered not to be treatment-related. Spectrophotometric analysis revealed the presence of relatively high content of phenolics and flavonoids in HEHs. HPLC analysis confirmed the presence of the quantified compounds and demonstrated the presence of ellagic acid, morin and naringin. CONCLUSION: Our results confirmed that HEHs have a broad safety margin for therapeutic use.
Authors: Rafael Sebastián Fort; Juan M Trinidad Barnech; Juliette Dourron; Marcos Colazzo; Francisco J Aguirre-Crespo; María Ana Duhagon; Guzmán Álvarez Journal: Pharmaceuticals (Basel) Date: 2018-08-14