Evaluation of in vitro and in vivo Anti-neuroinflammatory and Genotoxic Activities of the Alkaloid Tryptophol-5-O-β-D-glucopyranoside from Ocotea minarum

Pub Date : 2023-03-04 DOI:10.1080/22311866.2023.2225482
Ana Paula de Araújo Boleti, Pedro Hernique de Oliveira Cardoso, Breno Frihling, Zaira da Rosa Guterres, Ana Francisca Gomes da Silva, A. A. A. de Rezende, F. Garcez, W. Garcez, U. Graf, M. Spanó, Lillian May Grespan Estodutto da Silva, L. Migliolo
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Abstract

Abstract Ocotea minarum (Nees & Mart.) Mez is a tree belonging to the Lauraceae family and found in the Brazilian Cerrado ecosystem. Although the chemical composition of this species has already been described, little is known about the biological activities of one of the constituents of its fruits-the alkaloid tryptophol-5-O-β-D-glucopyranoside. In the present study, we assessed the anti-neuroinflammatory, mutagenic and recombinogenic properties of this indole alkaloid. Cytotoxicity and anti-inflammatory activities were performed using a model of LPS-stimulated microglia BV-2. Mutation detection and somatic recombination were performed in Drosophila melanogaster wing cells. The results showed that tryptophol-5-O-β-D-glucopyranoside was not cytotoxic to BV-2 cells at the concentrations tested. The results also showed that this alkaloid inhibited by 75% the inflammatory response induced by LPS at the concentration of 189 μM with IC50 = 12.07±0.35 μM. The analysis of the MH offspring showed that different concentrations of the alkaloid did not induce statistically significant increases in the frequencies of mutant spots when compared to those observed in the negative control. With these results, we can conclude that tryptophol-5-O-β-D-glucopyranoside presents therapeutic potential for the treatment of neurodegenerative diseases with no mutagenic effects. GRAPHICAL ABSTRACT
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八角生物碱色氨酸5-O-β-D-吡喃葡糖苷的体内外抗炎和基因毒性活性评价
摘要:印度洋樟树(Nees&Mart.)Mez是樟科的一种树木,发现于巴西塞拉多生态系统中。尽管已经描述了该物种的化学组成,但对其果实的一种成分生物碱色氨醇-5-O-β-D-吡喃葡糖苷的生物活性知之甚少。在本研究中,我们评估了这种吲哚生物碱的抗炎、诱变和重组特性。使用LPS刺激的小胶质细胞BV-2的模型进行细胞毒性和抗炎活性。对果蝇翅膀细胞进行了突变检测和体细胞重组。结果表明,在试验浓度下,色氨醇-5-O-β-D-吡喃葡糖苷对BV-2细胞无细胞毒性。结果还表明,该生物碱在189μM浓度下对LPS诱导的炎症反应有75%的抑制作用,IC50为12.07±0.35μM。对MH后代的分析表明,与阴性对照中观察到的相比,不同浓度的生物碱没有引起突变点频率的统计学显著增加。根据这些结果,我们可以得出结论,色氨醇-5-O-β-D-吡喃葡糖苷在治疗神经退行性疾病方面具有潜在的治疗潜力,没有诱变作用。图形摘要
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