In vitro evaluation of the antimicrobial properties of Mallotus oppositifolium decoction leaf extracts and fractions

In order to verify the in vitro antimicrobial properties of Mallotus oppositifolium (Euphorbiaceae), the qualitative phytochemical screening and the antimicrobial activities on Shigella dysenteriae A2, Salmonella typhi, Escherichia coli, Enterococcus faecalis, Staphyllococcus aureus and Candida albicans strains of the aqueous decoction (DEMO) hexane (HEMO) and methanol (MEMO) fractions of leaves were assessed. The screening was performed using colorimetric methods. The antimicrobial activity was carried out using disc diffusion assays. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined by the dilution methods. The screening revealed the presence of metabolites such as alkaloids, flavonoids, phenolic compounds, tannins, saponins, lipids, carbohydrates, mucilages, proteins, triterpens and steroids. DEMO, HEMO, MEMO showed a concentration-dependent activity against Shigella dysenteriae A2 and Salmonella typhi, with inhibition zone ranging from 9.44±0.44 to 19.00±0.24 mm, 8.94±0.05 to 20.03±0.17 mm and 8.13±0.17 to 16.76±0.11 mm respectively. The MIC showed ranges from 0.25 to 1.00 mg.mL-1, 0.20 to 0.50 mg.mL-1 and 1.00 to 3.00 mg.mL-1, while the MBC ranged from 1.00 to 5.00 mg.mL-1, 0.50 to 1.00 and 3.00 to 10.00 mg.mL-1 respectively. The leaves decoction and fractions activity on the two strains showed promising activities to justify the use of the plant against diarrhoea in folk medicine.Keywords: Folk medicine, phytochemical analysis, Mallotus oppositifolium diarrhea, antimicrobial

Inhibitory activity of limonoids from Khaya grandifoliola C.DC (Meliaceae) against hepatitis C virus infection in vitro

Objective: A fraction from Khaya grandifoliola has recently been shown to inhibit hepatitis C virus (HCV) infection and three limonoids (17-epi-methyl-6-hydroxylangolensate, 7-deacetoxy-7-oxogedunin and 7-deacetoxy-7R-hydroxygedunin) were purified from this fraction. The present study aimed at assessing the inhibitory effect of these limonoids on HCV using cell-culture derived HCV (HCVcc) system. Materials and Methods: Cytotoxic effects of the limonoids on Huh7.5 cells were assessed by MTT assay. Huh7.5 cells were transfected with RNA transcripts of the plasmid Jc1/GLuc2a, carrying a Gaussia luciferase reporter gene to rescue the HCVcc particles which were used to infect naïve cells in the presence or absence of the studied limonoids during 72 hr. Infection and replication rates were monitored by luciferase reporter assay and immunofluorescence assay (IFA) while cellular gene expression was analyzed by western blot, respectively. Results: The limonoids inhibited HCV infection mostly by targeting entry and replication stage. Their inhibitory effect on entry step, comparable to that of anti-CD81 antibody, was related to the blocking of CD81 receptor. In the replication step, the limonoids decreased the expression of NS5B similar to danoprevir. These compounds also significantly decreased but up-regulated the expression of Class-III phosphatidylinositol 4-kinase alpha and 2’,5’-oligoadenylate synthase-3, respectively. Conclusion: The present findings suggest that limonoids from K. grandifoliola are potential anti-HCV agents and may offer an advantage in the treatment of HCV infection

Heterophynone and methyl ester of Colic acid, two new compounds with antimicrobial activity from Cola heterophylla (Sterculiaceae)

peer reviewe

Natural compounds isolated from African mistletoes (loranthaceae) exert anti-inflammatory and acetylcholinesterase inhibitory potentials : in vitro and in silico studies

DATA AVAILABILITY STATEMENT: All data generated or analysed during this study are included in this published article.Please read abstract in article.The Central University of Technology operational expenses and the National Research Foundation (NRF) of South Africa.https://www.mdpi.com/journal/applsciParaclinical Science

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

Synthesis and anticancer activity evaluation of some new 1,2,3,5-tetrazine derivatives attached to benzothiazole moiety

A series of novel tetrazine derivatives, containing benzothiazole framework, were prepared during the coupling reactions of some diazotized 2-aminobenzo[d]thiazole derivatives with p-acetaminophen. Their structures were elucidated based on NMR and MS spectrometry. The anticancer activity and the safety of the synthesized compounds along with the entire precursors were assessed against three human cancer cell lines and a normal cell line. All the synthesized compounds showed selective cytotoxic activity against the cancer cell lines used in comparison to the normal Vero cell line. Their IC50 values varied from 2.02 to 171.67 μM.The Cameroonian Ministry of Higher Education special research allocation, the German Academic Exchange Service (DAAD) and the University of Pretoria.https://www.arkat-usa.org/arkivoc-journalam2023Paraclinical Science

A characterization of the antimalarial activity of the bark of Cylicodiscus gabunensis Harms

ETHNOPHARMACOLOGICAL RELEVANCE AND AIM: A decoction of the bark of Cylicodiscus gabunensis Harms is used as a traditional medicine in the treatment of malaria in Nigeria. This study aims to validate the antimalarial potency of this decoction in vitro against Plasmodium falciparum and define potential bioactive constituents within the C. gabunensis bark. MATERIALS AND METHODS: A bioassay-guided separation and fractionation protocol was applied to C. gabunensis extracts, exploiting the use of a Malaria Sybr Green I Fluorescence assay method to monitor antiproliferative effects on parasites as well as define 50% inhibition concentrations. Spectroscopic techniques, including GC-MS, TOF LC-MS and (1)H NMR were used to identify phytochemicals present in bioactive fractions. Analogues of gallic acid were synthesized de novo to support the demonstration of the antimalarial action of phenolic acids identified in C. gabunensis bark. In vitro cytotoxicity of plant extracts, fractions and gallate analogues was evaluated against the HepG2 cell line. RESULTS: The antimalarial activity of ethanolic extracts of C. gabunensis bark was confirmed in vitro, with evidence for phenolic acids, primarily gallic acid and close analogues such as ethyl gallate, likely providing this effect. Further fraction produced the most potent fraction with a 50% inhibitory concentration of 4.7µg/ml. Spectroscopic analysis, including (1)H NMR, LC-MS and GC-MS analysis of this fraction and its acid hydrolyzed products, indicated the presence of conjugates of gallic acid with oligosaccharides. The extracts/fractions and synthetic alkyl gallate showed moderate selectivity against P. falciparum. CONCLUSIONS: These results support the use of the bark of C. gabunensis as a traditional medicine in the treatment of human malaria, with phenolic acid oligosaccharide complexes evident in the most bioactive fractions

Cytotoxicity, nitric oxide and acetylcholinesterase inhibitory activity of three limonoids isolated from Trichilia welwitschii (Meliaceae)

BACKGROUND: Limonoids are highly oxygenated compounds with a prototypical structure. Their occurrence in the plant kingdom is mainly confined to plant families of Meliaceae and Rutaceae. Owing to their wide range of pharmacological and therapeutic properties, this study was aimed at investigating the potential nitric oxide (NO) and acetylcholinesterase (AChE) inhibitory activity and the cytotoxicity of three limonoids: trichilia lactone D5 (1), rohituka 3 (2) and dregeanin DM4 (3), isolated from Trichilia welwitschii C.DC RESULTS: Results indicated that the three limonoids had low cytotoxicity towards Vero cells with LC50 values ranging from 89.17 to 75.82 (μg/L. Compounds (2) and (3) had lower cytotoxicity compared to puromycin and doxorubicin used as reference cytotoxic compounds. Compound (1) (LC50 of 23.55 (μg/L) had good antiproliferative activity against RAW 264.7 cancer cells. At the lowest concentration tested (0.5 μg/mL), compound (2) and (3) released the lowest amount of nitric oxide (2.97 and 2.93 μM, respectively). The three limonoids had anti-AChE activity with IC50 values ranged of 19.13 (μg/L for (1), 34.15 (μg/L for (2) and 45.66 (μg/L for (3), compared to galantamine (IC50 of 8.22 ( g/mL) used as positive control CONCLUSION: The limonoid compounds studied in this work inhibited nitric oxide production in LPS-stimulated macrophages and had anti-AChE activity. Trichilia lactone D5 had potential antiproliferative activity against RAW 264.7 cancer cells. The limonoids had low cytotoxicity towards Vero cells lines. This study provided further examples of the importance of limonoids compounds as potential AChE inhibitors and anti-inflammatory agents targeting the inhibition of NO productio