Studies on the antimicrobial activity and brine shrimp toxicity of Zeyheria tuberculosa (Vell.) Bur. (Bignoniaceae) extracts and their main constituents

<p>Abstract</p> <p>Background</p> <p>Due to the indiscriminate use of antimicrobial drugs, the emergence of human pathogenic microorganisms resistant to major classes of antibiotics has been increased and has caused many clinical problems in the treatment of infectious diseases. Thus, the aim of this study was to evaluate for the first time the <it>in vitro </it>antimicrobial activity and brine shrimp lethality of extracts and isolated compounds from <it>Zeyheria tuberculosa </it>(Vell.) Bur., a species used in Brazilian folk medicine for treatment of cancer and skin diseases.</p> <p>Methods</p> <p>Using the disc diffusion method, bioautography assay and brine shrimp toxicity test (<it>Artemia salina </it>Leach), we studied the antimicrobial activity and lethality of extracts and isolated compounds against three microorganisms strains, including Gram-positive (<it>Staphylococcus aureus</it>) and Gram-negative (<it>Pseudomonas aeruginosa</it>) bacteria and yeasts (<it>Candida albicans</it>).</p> <p>Results</p> <p>In this study, the extracts inhibited <it>S. aureus </it>(8.0 ± 0.0 to 14.0 ± 0.0 mm) and <it>C. albicans </it>(15.3 ± 0.68 to 25.6 ± 0.4 mm) growth. In the brine shrimp test, only two of them showed toxic effects (LC₅₀29.55 to 398.05 μg/mL) and some extracts were non-toxic or showed weak lethality (LC₅₀705.02 to > 1000 μg/mL). From these extracts, four flavones [5,6,7,8-tetramethoxyflavone (1), 5,6,7-trimethoxyflavone (2), 4'-hydroxy-5,6,7,8-tetramethoxyflavone (3), and 4'-hydroxy-5,6,7-trimethoxyflavone (4)] were isolated through bioassay-guided fractionation and identified based on the 1D and 2D NMR spectral data. By bioautography assays, compounds 1 [<it>S. aureus </it>(16.0 ± 0.0 mm) and <it>C. albicans </it>(20.0 ± 0.0 mm)] and 3 [<it>S. aureus </it>(10.3 ± 0.6 mm) and <it>C. albicans </it>(19.7 ± 0.6 mm)] inhibited both microorganisms while 2 inhibited only <it>S. aureus </it>(11.7 ± 0.6 mm). Compound 4 did not restrain the growth of any tested microorganism.</p> <p>Conclusion</p> <p>Our results showed that extracts and isolated flavones from <it>Z. tuberculosa </it>may be particularly useful against two pathogenic microorganisms, <it>S. aureus </it>and <it>C. albicans</it>. These results may justify the popular use this species since some fractions tested had antimicrobial activity and others showed significant toxic effects on brine shrimps. However, in order to evaluate possible clinical application in therapy of infectious diseases, further studies about the safety and toxicity of isolated compounds are needed.</p

Antinociceptive and Anti-Inflammatory Effects of Octacosanol from the Leaves of Sabicea grisea var. grisea in Mice

Sabicea species are used in the Amazon for treatment of fever and malaria, which suggests that its chemical constituents may have some effect on pain and inflammation. Phytochemical analysis of the hexane fraction obtained from the crude ethanol extract from Sabicea grisea var. grisea Cham. & Schltdl (Rubiaceae), an endemic plant in Brazil, resulted in the isolation of octacosanol. This study investigated the antinociceptive and anti-inflammatory effects of the octacosanol in different experimental models. The crude ethanolic extract and hexane fraction obtained from the leaves of S. grisea produced an inhibition of acetic acid-induced pain. Moreover, octacosanol isolated from the hexane fraction produced a significant inhibition of pain response elicited by acetic acid. Pre-treatment with yohimbine, an alpha 2-adrenergic receptor antagonist, notably reversed the antinociceptive activity induced by octacosanol in the abdominal constriction test. Furthermore, mice treated with octacosanol did not exhibit any behavioral alteration during the hot plate and rota-rod tests, indicating non-participation of the supraspinal components in the modulation of pain by octacosanol with no motor abnormality. In the formalin test, octacosanol did not inhibit the licking time in first phase (neurogenic pain), but significantly inhibited the licking time in second phase (inflammatory pain) of mice. The anti-inflammatory effect of octacosanol was evaluated using carrageenan-induced pleurisy. The octacosanol significantly reduced the total leukocyte count and neutrophils influx, as well as TNF-α levels in the carrageenan-induced pleurisy. This study revealed that the mechanism responsible for the antinociceptive and anti-inflammatory effects of the octacosanol appears to be partly associated with an inhibition of alpha 2-adrenergic transmission and an inhibition of pathways dependent on pro-inflammatory cytokines. Finally, these results demonstrated that the octacosanol from the leaves of S. grisea possesses antinociceptive and anti-inflammatory activities, which could be of relevance for the pharmacological control of pain and inflammatory processes

Two clerodane diterpenes and flavonoids from Croton brasiliensis

Two new clerodane diterpenes, crotobrasilin A and crotobrasilin B, were isolated in addition to four known 3-methoxyflavones: casticin, penduletin, chrysosplenol-D and artemetin from leaves and stems of Croton brasiliensis. The structural elucidation of these compounds was made on the basis of spectroscopic data analyses, especially NMR, including 2D techniques (COSY, HMQC, HMBC and NOESY)