Abstract
Phenolic compounds from Dipteryx alata Vogel were assayed against the in vitro neurotoxic effect induced by Bothrops jararacussu (Bjssu) venom. Mutagenicity was assessed by the Ames test using Salmonella typhimurium strains TA98, TA97a, TA100, and TA102, in experiments with and without metabolic activation. Anti-bothropic activity was obtained by using mouse phrenic nerve-diaphragm (PND) preparation and myographic technique. Control experiments with physiological Tyrode solution were used for keeping the PND preparations alive (n = 4). Concentrations of phe-nolic compounds were as follow: protocatechuic and vanillic acids (200 μg/mL, n = 4), vanillin (50 μg/mL, n = 4). These compounds were used alone or pre-incubated with the venom (40 μg/mL), 30 min prior the addition to the organ bath (n = 4). Phenolic compounds significantly inhibited the neuromuscular blockade of Bjssu in the following order of potency: vanillic acid > protocatechuic = vanillin. Vanillic acid added 10 min after the Bjssu venom was also able to avoid the venomblockade evolution. The mutagenicity assay indicated that all phytochemicals were unable to in-crease the number of revertants, demonstrating the absence of mutagenic activity. This study demonstrated both the safety and therapeutical potential of the three phenolic compounds as novel complementary anti-bothropic agents.
Highlights
Natural phenolic compounds have an aromatic ring bearing one or more hydroxyl or etherified substituents, being known due the ability to complex proteins by hydrogen bonding. Compounds such as protocatechuic (1, PCA) and vanillic (2, VA) acids, both universal among the angiosperms [1]; and the aldehyde vanillin (3, VN) have closely related structures (Figure 1), which justify the similarity in their biological activity [2]
Plants with medicinal properties take important role in the sustainability concept. This concept creates and maintains the condition in which human beings and nature can coexist in a productive harmony, allowing social, economic and other requirements of the present and future generations [26]
Phenolic compounds from D. alata significantly protected the neuromuscular preparation against the irreversible neuromuscular blockade-induced by B. jararacussu venom, at different levels: VA > PCA = VN, by unclear mechanisms
Summary
Natural phenolic compounds have an aromatic ring bearing one or more hydroxyl or etherified substituents, being known due the ability to complex proteins by hydrogen bonding Among them, compounds such as protocatechuic (1, PCA) and vanillic (2, VA) acids, both universal among the angiosperms [1]; and the aldehyde vanillin (3, VN) have closely related structures (Figure 1), which justify the similarity in their biological activity [2]. The biological activity of these compounds has been characterized, and revealed their potential as antioxidants [5], scavengers of active oxygen species and electrophiles [6], blockers of nitration [7], and metal chelators [8] Despite of their environmental relevance considering the endangered situation of the Brazilian Cerrado biome, a preliminary survey for biological activities justifies the bio-prospection, due to the potential of baru as a source for medicinal use, nutritional food, pharmaceutical, and cosmetic compounds. The controlled bio-prospection could allow the valorization of Cerrado’s plants, and their sustainable use, contributing to the environment protection
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