Euphorbia is a large genus of flowering plants with a great diversity in metabolic pattern. Testing the cytotoxic potential of fifteen Euphorbia species revealed highest activity of E. officinarum L. against human colon adenocarcinoma (CACO2) cell line (IC50 7.2 µM) and of E. lactea Haw. against human hepatoma (HepG2) and human breast adenocarcinoma (MCF-7) cell lines (IC50 5.2 and 5.1 µM, respectively). Additionally, metabolic profiling of the fifteen tested species, using LC-HRMS, for dereplication purposes, led to the annotation of 44 natural compounds. Among the annotated compounds, diterpenoids represent the major class. Dereplication approach and multivariate data analysis are adopted in order to annotate the compounds responsible for the detected cytotoxic activity. Results of Principle component analysis (PCA) come in a great accordance with results of biological testing, which emphasized the cytotoxic properties of E. lactea Haw. A similarity correlation network showed that the two compounds with the molecular formula C16H18O8 and C20H30O10, are responsible for cytotoxic activity against MCF-7 and HepG2 cell lines. Similarly, the compound with molecular formula C18H35NO correlates with cytotoxic activity against CACO2.

Background Euphorbia is the largest genus in family Euphorbiaceae with a great biological and genetic diversity. The anti-trypanosomal activity of the crude extract of 15 Euphorbia species against Trypanosoma brucei brucei was carried out. Furthermore, DNA fingerprinting of the tested species using ISSR and SCoT markers was also investigated. Results The anti-trypanosomal activity of the 15 Euphorbia species revealed the highest activity of E. officinarum L. and E. milli Des Moul. against Trypanosoma brucei brucei with IC50 values < 10 μg/mL after 48- and 72-h incubation. Moreover, the assessment of the genetic diversity among the 15 tested species showed similar correlation coefficients of 0.76–0.98 which classified Euphorbia species into two main groups, one contained two species and the other contained 13 species. Conclusions Some Euphorbia species exhibited significant growth inhibitory activity toward Trypanosoma brucei strain TC221. Results also indicated the suitability of both markers for genetic fingerprinting of the tested Euphorbia species. To our knowledge, this is the first detailed comparison of the performance of two targeted DNA molecular markers (SCoT and ISSR) on the tested 15 Euphorbia species. The results guide future efficient use of these molecular markers in the genetic analysis of Euphorbia.

Human African trypanosomiasis is an endemic infectious disease caused by Trypanosoma brucei via the bite of tsetse-fly. Most of the drugs used for the treatment, e.g., Suramin, have shown several problems, including the high level of toxicity. Accordingly, the discovery of anti-trypanosomal drugs from natural sources has become an urgent requirement. In our previous study on the anti-trypanosomal potential of Euphorbia species, Euphorbia abyssinica displayed significant anti-trypanosomal activity. Therefore, a phytochemical investigation of the methanolic extract of E. abyssinica was carried out. Twelve compounds, including two triterpenes (1, 2); one sterol-glucoside (4); three ellagic acid derivatives (3, 9, 11); three gallic acid derivatives (5, 6, 10); and three flavonoids (7, 8, 12), were isolated. The structures of isolated compounds were determined through different spectroscopic techniques. Compound (10) was obtained for the first time from genus Euphorbia while all other compounds except compound (4), were firstly reported in E. abyssinica. Consequently, an in silico study was used to estimate the anti-trypanosomal activity of the isolated compounds. Several compounds displayed interesting activity where 1,6-di-O-galloyl-d-glucose (10) appeared as the most potent inhibitor of trypanosomal phosphofructokinase (PFK). Moreover, molecular dynamics (MD) simulations and ADMET calculations were performed for 1,6-di-O-galloyl-d-glucose. In conclusion, 1,6-di-O-galloyl-d-glucose revealed high binding free energy as well as desirable molecular dynamics and pharmacokinetic properties; therefore, it could be suggested for further in vitro and in vivo studies for trypanosomiasis.