Cytotoxic activities against Ehrlich carcinoma and human K562 leukaemia of alkaloids and flavonoid from two Solanum Species

Abstract

Diversas espécies do gênero Solanum apresentam glicoalcalóides e flavonóides com grande variedade de atividades biológicas. O flavonóide tiliroside (1), uma fração rica em glicoalcalóides denominada GB e o glicoalcalóide solasonina (2) foram obtidos dos tricomas de galhos jovens e frutos de Solanum crinitum Lam e o alcalóide estereoidal solasodina (3), extraído das partes aéreas de S. jabrense Agra & M. Nee, tiveram sua atividade citotóxica avaliada frente a células do carcinoma de Ehrlich e da leucemia humana K562. O efeito antiproliferativo destas substâncias mostrou comportamento dose-dependente após avaliação através do método do MTT, para ambos os casos. Os resultados indicaram atividade citotóxica para 1, GB e 2, com IC 50 = 69,50 µM, 19,5 µg mL -1 e 74,20 µM, respectivamente, quando ensaiadas frente ao carcinoma de Ehrlich, e IC 50 = 118,40 µM, 13,65 µg mL -1 , 60,35 µM e 76,92 µM para 1, GB, 2 e 2a (derivado peracetilado da solasonina) frente a leucemia K562. A baixa atividade da aglicona solasodina (3) indicou a importância da presença dos açúcares na estrutura do glicoalcalóide e permitiu postular a substância 2, presente na fração rica em glicoalcalóides (GB), como um dos principios ativos. Além disso, os resultados mostraram a possibilidade de biomonitoramento através do ensaio do MTT na busca de metabólitos com atividade citotóxica.Steroidal alkaloids, flavonoids and their glycosides occurring in numerous species of Solanum genus are known to possess a variety of biological activities. The flavonoid tiriloside (1), a rich in glycoalkaloids total fraction named GB and the glycoalkaloid solasonine (2) isolated from thricomes of young branches and fruits from Solanum crinitum Lam, and the aglycone solasodine (3) isolated from Solanum jabrense Agra & M. Nee, were assayed against murine Ehrlich carcinoma and human K562 leukaemia cultured cells. The exposure in vitro of these cancer cells to these products resulted in a dose-dependent growth inhibition evaluated by the MTT method. The results indicated significant cytotoxic activities with IC 50 = 69.50 µM, 19.5 µg mL -1 , and 74.20 µM for 1, GB and 2, respectively, against Ehrlich carcinoma, and IC 50 = 186.50 µM, 13.65 µg mL -1 and 76.92 µM, for 1, GB, 2 and 2a, respectively, against K562 leukaemia cells. The low activity of the aglycone 3 indicates that the role of the sugar moiety is very important in the cytotoxic activity of glycoalkaloid solsonine. The cytotoxic activity revealed by the GB fraction may be attributed to the presence of 2. Additionally, these results show the viability of the MTT assay for monitoring phytochemical bioactive compounds. K562 Leukaemia Vol. 13, No. 6, 2002 Kolaviron for the treatment of various diseases, including hepatitis and laryngitis, 3 and several Leguminosae plants containing isoflavonoids with potent estrogenic activity. 4 Many plants in the Solanaceae family accumulate steroidal alkaloids based on a C 27 cholestane skeleton, e.g. solasodine and tomatidine. These compounds are essentially nitrogen analogues...

Estudo farmacobotânico comparativo de folhas de Solanum crinitum Lam., Solanum gomphodes Dunal e Solanum lycocarpum A. St.-Hil., Solanaceae

“…Solanum crinitum possui frutos considerados tóxicos (Agra & Bhattacharyya, 1999), dos quais já foram isolados alcalóides e flavonóides, que apresentaram atividade citotóxica (Esteves-Souza et al, 2002;Cornelius et al, 2004). A outra espécie, Solanum gomphodes, também nativa da flora brasileira é usada popularmente com as mesmas indicações de S. lycocarpum, entretanto, seus constituintes químicos e atividades biológicas são desconhecidos.…”

Contribuição da fitoquímica para o desenvolvimento de um país emergente

“…30 A solavetivona (58) e a solasodina (59) foram isoladas de S. jabrense. 31,32 Um alcaloide esteroidal isolado de Solanum criticum foi recentemente caracterizado como 20-episolasodina (59a).…”

Citotoxicity and immune response induced by organopalladium(II) compounds in mice bearing Ehrlich ascites tumour

“…For in vitro assays, 1.0 mL of RPMI-1640-Complete, RPMI-1640-C (containing 5% fetal calf serum, mercaptoethanol, penicillin and streptomycin) was added to the cells, adjusting the concentration to 1 × 10 6 cell/ mL. 16 For in vivo assays 1.0 mL of phosphate-buffered saline (PBS), pH 7.2 was employed, adjusting the concentration to 1 × 10 3 cell /mL. 14 Assessment of citotoxicity using MTT assay for EAT cells 100.0 μL samples of tumour peritoneal cell suspension (1 × 10 6 cell/ mL, adjusted in RPMI-1640-C), obtained from 10 EAT-bearing mice, were added to each well of a 96-well tissue culture plate (Corning) containing 100.0 μL of the compounds (1), (2) and cis-DDP in different concentrations (between 100.0 and 5.0 μmol L -1 ) or RPMI 1640-Complete medium with 0.3% of dimethylsulphoxyde (DMSO) or only RPMI 1640-Complete as cell control of viability, using the Mossman assay.…”

“…For in vitro assays, 1.0 mL of RPMI-1640-Complete, RPMI-1640-C (containing 5% fetal calf serum, mercaptoethanol, penicillin and streptomycin) was added to the cells, adjusting the concentration to 1 × 10 6 cell/ mL. 16 For in vivo assays 1.0 mL of phosphate-buffered saline (PBS), pH 7.2 was employed, adjusting the concentration to 1 × 10 3 cell /mL. 14 …”