Background: Cancer poses a health threat, with an increased incidence worldwide. Thus, it is essential to develop new natural anticancer agents. Dypsis pembana (H.E.Moore) Beentje & J.Dransf (DP) is an ornamental plant belonging to the family Arecaceae. This study aimed to isolate and identify phytoconstituents from the leaves of this plant and evaluate their in vitro cytotoxic activities. Methods: Different chromatographic techniques were applied to fractionate the hydro-alcoholic extract of DP and separate the major phytoconstituents. The isolated compounds were structurally elucidated based on their physical and spectroscopic data. The in vitro cytotoxic activities of the crude extract and fractions thereof were evaluated against human colon carcinoma (HCT-116), human breast carcinoma (MCF-7), and human hepatocellular carcinoma (HepG-2) cell lines via MTT assay. Moreover, selected isolates were tested against HepG-2 cell line. Molecular docking analysis was performed to investigate the interactions of these compounds with two potential targets, the human topoisomerase IIα and cyclin-dependent kinase 2 enzymes. Results: Thirteen diverse compounds were reported for the first time from DP, providing significant chemotaxonomic biomarkers. Among tested compounds, vicenin-II (7) was the most cytotoxic against HepG-2 cell line, with an IC50 value of 14.38 µg/mL, followed by isovitexin (13) (IC50 of 15.39 µg/mL). These experimental findings were complemented by molecular docking, which demonstrated that vicenin-II exhibited superior enzyme-binding affinities to the studied vital targets and shed light on the structure–activity relationships among the investigated flavone-C-glycosides members. Conclusion: The phytochemical profile of DP was characterized for the first time, reflecting chemotaxonomic data about the concerned species, genus, or even the family. Biological and computational findings revealed that vicenin-II and isovitexin are possible lead structures as inhibitors of the human topoisomerase IIα and cyclin-dependent kinase 2 enzymes.
This study investigated the ethanolic leaf extract of Brazilian pepper tree (Schinus terebinthifolius Raddi) for its metabolite composition and effects on growth performance and intestinal immune gene expression in Nile tilapia (Oreochromis niloticus). Ultra-performance liquid chromatography-electrospray ionization-mass spectrometry (UPLC-ESI-MS/MS) in positive and negative modes revealed a diverse profile of 33 peaks in each polarity, identifying key compounds such as phenolic acids (e.g., gallic acid and ferulic acid), flavonoids (e.g., myricetin-O-glucoside and quercetin 3-O-glucoside), gallotannins (e.g., glucogallin and pentagalloylglucose), and triterpenoids (e.g., masticadienoic acid). A 60-day feeding trial with four groups (control and three extract doses; 0.5%; T0.5%, 1%; T1% and 2%; T2%) demonstrated dose-dependent enhancements in growth metrics, where final body weight increased by up to 106.9 ± 3.6 g, weight gain% by 197.3 ± 3.5%, and the growth rate got more than doubled in T2% (2.4 ± 0.1), alongside improved feed conversion ratio (1.24 ± 0.01) at 30 days and condition factor (stabilized at 2.1 ± 0.0) at 60 days post-feeding. Viscero- and gastro-somatic indices declined insignificantly in most feed groups, indicating improved muscle growth. Biphasic patterns were observed in intestinal gene expression as follows: over 60 days, the IL-1β gene upregulated at low doses but returned to normal at high doses. The IL-10 gene upregulated progressively, promoting an anti-inflammatory balance. In fish fed medium and high doses (T1% and T2%), the IgM gene is upregulated, supporting humoral immunity. These outcomes, linked to the extract’s previously described antioxidants, anti-inflammatory, and antimicrobial bioactive compounds, suggest that S. terebinthifolius is a promising natural feed additive for sustainable tilapia aquaculture and warrants further validation for commercial application.
7 March 2022 in Bulletin of Pharmaceutical Sciences. Assiut
Background: Hyphaene thebaica L. Mart. (Doum-palm), rich in total phenolics content, is known for its medicinal value in the treatment of several health conditions, such as hypertension, and diabetes mellitus.Aim of the study: To investigate the hypoglycaemic activity of the dichloromethane, ethyl acetate, and aqueous fractions from doum palm leaves. Then, to characterize the metabolic profile of the most active fraction by LC-HR-MS/MS analysis to detect the responsible metabolites for this activity.Material and methods: The present study examined the in vitro inhibitory effect of the extract fractions from Doum Palm Leaves at concentrations ranging from 7.81 to 1000.00 μg/ml on α-glucosidase activity, an enzyme responsible for carbohydrate-hydrolysis to monosaccharides and intestinal glucose absorption. Metabolic profiling for the dichloromethane fraction was obtained with LC-HR-MS/MS.Results: The dichloromethane (DCM) fraction inhibited α-glucosidase activity in vitro with an IC50 of 52.40 μg/ml. Twenty-three compounds were identified in the DCM fraction by LC-HR-MS/MS analysis. Most of them were reported for their potential antidiabetic activity. Nevertheless, the III-DCM subfraction (IC50 3.79 ± 0.17 μg/ml) and the IV-DCM subfraction (IC50 5.13 ± 0.24 μg/ml) had the best inhibitory activity against α-glucosidase compared with acarbose (IC50 2.33 ± 0.11 μg/ml). Conclusions: The results support the use of these fractions obtained from Doum palm leaves to effectively inhibit a crucial enzyme linked to type 2 diabetes and suppress carbohydrate absorption from intestine, and thereby reducing the postprandial increase of blood glucose.