In vitro antiproliferative, anti-inflammatory effects and molecular docking studies of natural compounds isolated from Sarcocephalus pobeguinii (Hua ex Pobég)

DATA AVAILABILITY STATEMENT : The original contributions presented in the study are included in the article/Supplementary Material, further inquiries can be directed to the corresponding authors.BACKGROUND : Sarcocephalus pobeguinii (Hua ex Pobég) is used in folk medicine to treat oxidative-stress related diseases, thereby warranting the investigation of its anticancer and anti-inflammatory properties. In our previous study, the leaf extract of S. pobeguinii induced significant cytotoxic effect against several cancerous cells with high selectivity indexes towards non-cancerous cells. AIM : The current study aims to isolate natural compounds from S. pobeguinii, and to evaluate their cytotoxicity, selectivity and anti-inflammatory effects as well as searching for potential target proteins of bioactive compounds. METHODS : Natural compounds were isolated from leaf, fruit and bark extracts of S. pobeguinii and their chemical structures were elucidated using appropriate spectroscopic methods. The antiproliferative effect of isolated compounds was determined on four human cancerous cells (MCF-7, HepG2, Caco-2 and A549 cells) and non-cancerous Vero cells. Additionally, the anti-inflammatory activity of these compounds was determined by evaluating the nitric oxide (NO) production inhibitory potential and the 15-lipoxygenase (15-LOX) inhibitory activity. Furthermore, molecular docking studies were carried out on six putative target proteins found in common signaling pathways of inflammation and cancer. RESULTS : Hederagenin (2), quinovic acid 3-O-[α-D-quinovopyranoside] (6) and quinovic acid 3-O-[β-D-quinovopyranoside] (9) exhibited significant cytotoxic effect against all cancerous cells, and they induced apoptosis in MCF-7 cells by increasing caspase-3/-7 activity. (6) showed the highest efficacy against all cancerous cells with poor selectivity (except for A549 cells) towards noncancerous Vero cells; while (2) showed the highest selectivity warranting its potential safety as a chemotherapeutic agent. Moreover, (6) and (9) significantly inhibited NO production in LPS-stimulated RAW 264.7 cells which could mainly be attributed to their high cytotoxic effect. Besides, the mixture nauclealatifoline G and naucleofficine D (1), hederagenin (2) and chletric acid (3) were active against 15-LOX as compared to quercetin. Docking results showed that JAK2 and COX-2, with the highest binding scores, are the potential molecular targets involved in the antiproliferative and anti-inflammatory effects of bioactive compounds. CONCLUSION : Overall, hederagenin (2), which selectively killed cancer cells with additional anti-inflammatory effect, is the most prominent lead compound which may be further investigated as a drug candidate to tackle cancer progression.The Central University of Technology operational expenses and the National Research Foundation (NRF), South Africa. The APC was funded by the Central University of Technology research expenses (TM).http://www.frontiersin.org/Pharmacologyam2024Paraclinical SciencesSDG-03:Good heatlh and well-bein

Anticoccidial constituents from the stem bark of Turraeanthus africanus

International audienceIn order to study some biological active products, phytochemical investigation of the stem bark of Turraeanthus africanus have led to the isolation of a novel compound 1, a new benzoic acid derivative, named turraeanthin C, and two known compounds sesamin (2) and stigmasterol. The structures of these compounds were established by spectral analysis, including two-dimensional nuclear magnetic resonance. The extract and the isolated compounds 1 and 2 showed noteworthy activity against Toxoplasma gondii intracellular parasite in mammals

Two new secondary metabolites with antibacterial activities from Conyza aegyptiaca (Asteraceae)

Mbarga PE, Fouotsa H, Ndemangou B, et al. Two new secondary metabolites with antibacterial activities from Conyza aegyptiaca (Asteraceae). Natural Product Research . 2022.The bio guided fractionation of the dichloromethane/methanol (1:1) crude extract of the air-dried whole plant of C. aegyptiaca led to the isolation of one new flavone derivative designated conyflavone (1) and one new clerodane diterpene type designated conyclerodane (2) along with five known compounds including two flavonoids Gardenin C (3), chrysosplenetin (4) and two steroids glucoside of beta-sitosterol (5), the mixture of stigmasterol (6) and beta-sitosterol (6') and ent-2b,18,19trihydroxycleroda-3,13-dien-16,15-olide (7). The structures were established by spectroscopic methods including IR, 1D and 2D NMR in conjunction with mass spectroscopy and by comparison to data of related compounds described in literature. The stereocentres in compound 2 were determined by SC-XRD analysis. Crude extract as well as fractions and pure compounds were evaluated in vitro for their antibacterial activities against four pathogenic and two clinical isolate strains using microdilution methods. Extracts and compounds displayed a moderate antibacterial activity with MIC values ranging from 125 to 500g/mL