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An anxiolytic fraction of Tilia americana standardized in tiliroside, rutin, quercitrin, quercetin glucoside, and kaempferol was obtained. After oral administration of the fraction, the above-mentioned flavonoids were not detected in plasma over 24 h. However, meta and para hydroxyphenylacetic acid and dihydroxyphenylacetic acid (m-HPAA, p-HPAA and DOPAC) were monitored. These are the biotransformation compounds of the aglycones of kaempferol and quercetin; these aglycones are products of the other flavonoids present in the anxiolytic fraction. The analytical methods (HPLC) for flavonoids and the related compounds (m-HPAA, p-HPAA and DOPAC) were validated, determining the parameters of accuracy, precision, specificity or selectivity, limit of detection, quantification range, and robustness. The pharmacokinetic assay was performed with ICR mice strains, which were given 200 mg/kg of the standardized active fraction. The results of validation of the analytical methods were obtained, allowing it to be established in a validated way that no flavonoids present in the anxiolytic fraction of T. americana were detected in plasma. However, detection and follow up was possible for the serum levels of m-HPAA, p-HPAA, and DOPAC. The three compounds follow a two-compartment model with very similar parameters between m-HPAA and p-HPAA, some being different from the ones characterized in the pharmacokinetics of DOPAC. [ABSTRACT FROM AUTHOR]

In this study the effect of the ethanol concentration of Bougainvillea x buttiana extracts on the flavonoids content, and its antioxidant and cytoprotective activities in vitro were determined and compared. For the elucidation of the chemical constituents, the high-performance liquid chromatography method (HPLC) was used, and verification of the antioxidant activity was carried out using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical method. The cytoprotective effects of extracts were determined by exposure to hydrogen peroxide. The HPLC analysis showed the presence of rutin, quercetin-3-glucoside and quercetin rhamnoside. Among the extracts investigated the best recuperation of the rutin content was observed in extracts with 80% ethanol (83 ± 5 mg/mL). The amounts of rutin present in all extracts contribute to the antioxidant capacity and the IC50 was 427.49 (0%), 275.41 (50%), 271.61 (80%), and 272.14 (100%) µg/mL. The lowest percentage of viability was found in the cultures exposed to 100% ethanol (92%). In cultures exposed to hydrogen peroxide the percentages of protection were 25%, 33%, 78%, and 65% for cultures treated for 72 h at 0%, 50%, 80%, and 100% ethanol, respectively. The ethanolic extract of B. x buttiana was confirmed to have high rutin content with potent antioxidant activity, low cytotoxic and strong cytoprotective effects. [ABSTRACT FROM AUTHOR]

In this research, we evaluated the aphicidal effect of the ethanolic extract of stems and bark of Ficus petiolaris Kunth (Moraceae), in laboratory bioassays in an artificial diet against apterous adult females of Melanaphis sacchari Zehntner (Hemiptera: Aphididae). The extract was evaluated at different concentrations (500, 1,000, 1,500, 2,000, and 2,500 ppm), and the highest percentage of mortality (82%) was found at 2,500 ppm after 72 h. The positive control imidacloprid (Confial®) at 1% eliminated 100% of the aphids, and the negative control (artificial diet) only presented mortality of 4%. The chemical fractionation of the stem and bark extract of F. petiolaris yielded five fractions of FpR1-5, which were each evaluated at 250, 500, 750, and 1,000 ppm. FpR2 had the strongest aphicidal effect, with 89% mortality at 72 h at 1,000 ppm. The pure xanthotoxin compound extracted from this fraction was even more effective, with 91% aphid mortality after 72 h at 100 ppm. The lethal concentration (LC 50 ) of xanthotoxin was 58.7 ppm (72 h). Our results indicate that the extract of F. petiolaris showed toxic activity against this aphid, and its xanthotoxin compound showed strong aphicidal activity at low concentrations., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 The Authors. Published by Elsevier Inc. All rights reserved.)

The aim of this study was to obtain pharmacokinetic data for the anxiolytic compound galphimine-A (G-A) from Galphimia glauca. G-A is the most abundant anxiolytic compound in this plant, while Galphimine-E (G-E) is the most abundant galphimine, but inactive. G-E was transformed chemically into G-A. The pharmacokinetic study was carried out in ICR mice, which were orally administered a single 200 mg/kg dose of G-A. Samples of blood and brain were taken at different times after administration of G-A. Previously, we established the validation of methods for determining the concentration of G-A. The G-A was detected in plasma 5 min after oral administration, and its concentration reached 2.47 μg/mL. Data from concentration-time curves allowed us to establish the main pharmacokinetic parameters in two models: one- and/or two-compartment. C(max) values were 3.33 and 3.42 μg/mL respectively, likewise AUC(0→1440 min) were 1,951.58 and 1,824.95 μg/mL·min. The G-A in brain tissue was noted to cross the blood-brain barrier, reaching C(max) 2.74 μg/mL, T(max) 81.6 min, and then drop gradually to 0.32 μg/mL detected at 24 h. The presence of G-A in brain tissue, confirmed that this anxiolytic compound can access the target organ and acts directly on the CNS.