Bioguided Fractionation of Phyllanthus spp.: Unveiling Anticancer Potential through Metabolomic Correlation and ADMETox Insights.

Cancer remains a significant global health concern, with mortality rates steadily rising and prompting an urgent search for effective treatments. This study focuses on the medicinal properties of plants from the Phyllanthus genus, specifically Phyllanthus amarus and Phyllanthus niruri, which have shown promise in traditional medicine. Through bioguided fractionation using preparative high-performance liquid chromatography (HPLC), bioactive compounds were isolated and identified using ultra-performance liquid chromatography coupled to time-of-flight mass spectrometry (UHPLC-QTOF-MSE) and nuclear magnetic resonance (NMR) spectroscopy. Chemometric analyses such as principal component analysis (PCA) aided in understanding metabolite distribution. Biological assays demonstrated cytotoxic activities of specific fractions against cancer cell lines, notably the PhyN 4n fraction from P. niruri, which induced S-phase cell cycle arrest and apoptosis in HL60 cells. These findings underscore the anticancer potential of Phyllanthus species and lay the groundwork for future drug development efforts. The study's integration of advanced analytical techniques, chemometrics, and biological assays provides valuable insights for harnessing natural products in the fight against cancer.

Chemical composition, cytotoxicity and larvicidal activity against Aedes aegypti of essential oils from Vitex gardineriana Schauer / Composición química, citotoxicidad y actividad larvicida contra Aedes aegypti de aceites esenciales de Vitex gardneriana Schauer

Vitex gardneriana Schauer (Lamiaceae) popularly known as "jaramataia", is a shrub commonly found in caatinga biome located in Northeast Brazil. In folk medicine, its leaves have been used as analgesic and anti-inflammatory agents. The chemical composition of the essential oil from leaves obtained by hydrodistillation was analyzed and identified by GC-MS and GC-FID and showing a total of 26 constituents (95.9%) being 2 monoterpenes (0.4%) and 24 sesquiterpenes (95.4%). The main constituents identified were cis-calamenene (29.7%), 6,9-guaiadiene (14.5%) and caryophyllene oxide (14.0%). The essential oil has been demonstrated high larvicidal activity against Aedes aegypti (LC50 = 28.0 µg/mL). In the evaluation of the bioassay with Artemia salina the essential oil showed LC50 = 98.11 µg/mL. In addition, the essential oil did not show cytotoxicity (IC50 > 2.50 mg/mL) by the hemolysis assay.

Vitex gardneriana Schauer (Lamiaceae) popularmente conocido como "jaramataia", es un arbusto que se encuentra comúnmente en el bioma de caatinga ubicado en el noreste de Brasil. En medicina popular, sus hojas se han utilizado como analgésicos y agentes antiinflamatorios. La composición química de los aceites esenciales de las hojas obtenidas por hidrodestilación fue analizada e identificada por GC-MS y GC-FID y mostrando un total de 26 constituyentes (95.9%) siendo 2 monoterpenos (0.4%) y 24 sesquiterpenos (95.4%). Los componentes principales fueron cis-calamenene (29.7%), 6,9-guaiadiene (14.5%) y caryophyllene oxide (14.0%). El aceite esencial ha demostrado una alta actividad larvicida contra Aedes aegypti (CL50 = 28.0 µg/mL). En la evaluación del bioensayo con Artemia salina, el aceite esencial demostró CL50 = 98.11 µg/mL. Además, el aceite esencial no mostró citotoxicidad (IC50 > 2.5 mg / mL) mediante el ensayo de hemólisis.