@article {1213, title = {Chemical Composition and Some Biological Activities of the Methanolic Encephalartos ferox Fruit Extract}, journal = {Pharmacognosy Journal}, volume = {12}, year = {2020}, month = {August 2020}, pages = {1190-1197}, type = {Review Article}, chapter = {1190}, abstract = {

Background: Although literature reports the therapeutic properties of Encephalartos ferox, there are limited pharmacological studies of its fruit. Objective: This study sought to evaluate the antibacterial, antioxidant, anti-quorum sensing and in vitro cytotoxic activities of the methanolic E. ferox fruit extract. Methods: The chemical constituent of the methanolic fruit extract was analysed using gas chromatography-mass spectrometry. Antibacterial activity of the extract was investigated against Staphylococcus aureus (ATCC 25923), Bacillus cereus (ATCC 10102), Escherichia coli (ATCC 25922) and Pseudomonas aeruginosa (ATCC 27853) using the broth dilution method. The standard 2.2-diphenyl-1-picrylhydrazyl (DPPH) and 2.2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) methods were used to evaluate the scavenging activities of the extract. Anti-quorum sensing activity was assessed against biosensor strain- Chromobacterium violaceum (ATCC 12472). Cytotoxicity in HepG2 cells was investigated using the tetrazolium-based colorimetric (MTT) assay. Results: The extract revealed eight volatile compounds with cis-Vaccenic acid (87.06\%) and 9-Octadecenoic acid, 1,2,3-propanetriyl ester (5.21\%) as the major components. Antibacterial activity against all tested strains with minimum inhibitory concentration range of 1.56 - 12.5 mg/mL was observed. The DPPH and ABTS assays demonstrated scavenging activities with the median inhibitory concentration (IC50) values of 0.09 mg/mL and 0.003 mg/mL, respectively. The extract also displayed strong anti-quorum sensing activity with 93\% inhibition of violacein production at 25 mg/mL. A half maximum inhibitory concentration (IC50) of 5370 μg/mL was computed in HepG2 cells. Conclusion: The extract has potential to be used as a source of therapeutic compounds in pharmaceutical applications.

}, keywords = {Anti-quorum sensing, Antibacterial, Antioxidant, Cytotoxicity}, doi = {10.5530/pj.2020.12.167}, author = {Phakamani Hopewell Tsilo and Sidney Tsolanku Maliehe and Jabulani Siyabonga Shandu and Rene Khan} } @article {1253, title = {Computational Evaluation of ADMET Properties and Bioactive Score of Compounds from Encephalartos ferox}, journal = {Pharmacognosy Journal}, volume = {12}, year = {2020}, month = {September 2020}, pages = {1357-1362}, type = {Research Article}, chapter = {1357}, abstract = {

Background: Plant based products are recognised as sources of drugs for treatment of diseases. Objective: The study aimed at predicting the physicochemical, pharmacokinetics, drug-likeness and toxicity of the compounds identified from the methanolic Encephalartos ferox fruit extract. Methods: The physicochemical, pharmacokinetics properties and bioactive scores of the compounds were predicted using SwissADME and Molinspiration computational tools. Drug-likeness of the compounds was evaluated based on the Lipinski rule of five (Ro5). In silico mutagenicity, carcinogenicity and inhibition of human ether-a-go-go-related (hERG) gene were also investigated using PreADMET web tool. Results: The physicochemical properties showed the compounds, except 9-Octadecenoic acid, 1, 2, 3-propanetriyl ester to adhere to Ro5. The evaluation of their inhibitory effects profile in several cytochrome P450 isoforms indicate that all the compounds are not the inhibitors of CYP2C19 and CYP3A4 whereas some inhibited CYP1A2, CYP2C9 and CYP2D6. The drug-likeness evaluation employed Ro5 as a filter and all compounds complied with it except for 9-Octadecenoic acid, 1, 2, 3-propanetriyl ester. About 50\% of the tested compound were found to be safe as they did not exhibit antimutagenic and carcinogenic effects. Moreover, the risk of inhibition of hERG gene revealed to be low to medium risk depending on the compound. Conclusion: The calculated physicochemical and pharmacokinetic properties suggest that most of the compounds are safe and have promising oral bioavailability.

}, keywords = {Bioactive score, Compounds, Pharmacokinetic; Drug-likeness, Toxicity}, doi = {10.5530/pj.2020.12.187}, author = {Tsolanku Sidney Maliehe and Phakamani Hopewell Tsilo and Jabulani Siyabonga Shandu} }