ABSTRACT
Natural products are considered important sources of potential chemotherapeutic agents. Here, we evaluated the antiproliferative activity and the toxicological effects of the methanolic extract and a pure compound obtained from Solanum capsicoides seeds. The phytochemical profile was analyzed by chromatographic and spectroscopy methods. The acute toxicity was assessed in mice orally treated with the extract (2000 mg/kg), in vitro hemolytic activity and micronucleus test. The mutagenicity, developmental toxicity, and lethal dose (LD50) of carpesterol were estimated by the Toxicity Estimation Software Tool (TEST) software. A sulforhodamine B assay was employed to evaluate the antiproliferative activity. The toxicological assays did not observe signs of toxicity, either during the behavioral observations or in the autopsies, as well as no mutagenicity and hemolytic activity. The carpesterol did not present mutagenic effect and hemolytic activity but presents developmental toxicology and LD50 of 410 mg/kg in toxicity estimations by the TEST software. The S. capsicoides extract exhibited antiproliferative activity mainly in leukemia (K562) cell lineage. However, carpesterol presented antiproliferative activity in glioma (U251), breast (MCF-7), kidney (786-0), ovary (OVCAR-03), and K562 cell lineages. The data obtained show that S. capsicoides extract presents antiproliferative and does not present toxicological effects. In addition, it was shown for the first time the antiproliferative and toxicological parameters of carpesterol.
Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Cell Proliferation/drug effects , Methanol/chemistry , Neoplasms/drug therapy , Phytosterols/pharmacology , Plant Extracts/pharmacology , Seeds , Solanum , Solvents/chemistry , Animals , Antineoplastic Agents, Phytogenic/isolation & purification , Antineoplastic Agents, Phytogenic/toxicity , Female , Hemolysis/drug effects , Humans , K562 Cells , Lethal Dose 50 , MCF-7 Cells , Mice , Micronucleus Tests , Neoplasms/pathology , Phytosterols/isolation & purification , Phytosterols/toxicity , Phytotherapy , Plant Extracts/isolation & purification , Plant Extracts/toxicity , Plants, Medicinal , Seeds/chemistry , Solanum/chemistryABSTRACT
This study shows the evaluation the antiproliferative effect of the extract, fractions, and uncommon compounds isolated from R. rosaefolius leaves. The compounds were identified by conventional spectroscopic methods such as NMR-H(1) and C(13) and identified as 5,7-dihydroxy-6,8,4'-trimethoxyflavonol (1), 5-hydroxy-3,6,7,8,4'-pentamethoxyflavone (2), and tormentic acid (3). Both hexane and dichloromethane fractions showed selectivity for multidrug-resistant ovary cancer cell line (NCI-ADR/RES) with total growth inhibition values of 11.1 and 12.6 µg/ml, respectively. Compound 1 also showed selective activity against the same cell line (18.8 µg/ml); however, it was especially effective against glioma cells (2.8 µg/ml), suggesting that this compound may be involved with the in vitro antiproliferative action.
