Research Articles (SAHSMI)
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Item Bioassay-guided fractionation leads to the detection of cholic acid generated by the rare thalassomonas sp.(Pubmed, 2023) Schneider, Yannik K.-H.; Pheiffer, Fazlin; Holst Hansen, Espen; Hammer Andersen, JeanetteBacterial symbionts of marine invertebrates are rich sources of novel, pharmaceutically relevant natural products that could become leads in combatting multidrug-resistant pathogens and treating disease. In this study, the bioactive potential of the marine invertebrate symbiont Thalassomonas actiniarum was investigated. Bioactivity screening of the strain revealed Gram-positive specific antibacterial activity as well as cytotoxic activity against a human melanoma cell line (A2058). The dereplication of the active fraction using HPLC-MS led to the isolation and structural elucidation of cholic acid and 3-oxo cholic acid. T. actiniarum is one of three type species belonging to the genus Thalassomonas. The ability to generate cholic acid was assessed for all three species using thin-layer chromatography and was confirmed by LC-MS. The re-sequencing of all three Thalassomonas type species using long-read Oxford Nanopore Technology (ONT) and Illumina data produced complete genomes, enabling the bioinformatic assessment of the ability of the strains to produce cholic acid. Although a complete biosynthetic pathway for cholic acid synthesis in this genus could not be determined based on sequence-based homology searches, the identification of putative penicillin or homoserine lactone acylases in all three species suggests a mechanism for the hydrolysis of conjugated bile acids present in the growth medium, resulting in the generation of cholic acid and 3-oxo cholic acid. With little known currently about the bioactivities of this genus, this study serves as the foundation for future investigations into their bioactive potential as well as the potential ecological role of bile acid transformation, sterol modification and quorum quenching by Thalassomonas sp. in the marine environmentItem In vitro evaluation of the antiproliferative activity of Carpobrotus edulis on human neuroblastoma cells(Elsivier, 2021) Ekpo, Okobi Eko; Enogieru, Adaze Bijou; Omoruyi, Sylvester IfeanyiNeuroblastoma is a solid neuroendocrine tumour located outside the cranial cavity and contributes about 15% of all cancer‑associated deaths in children. Treatment of neuroblastoma is quite challenging and involves the use of chemotherapy, surgery and radiotherapy. Despite treatment strategies, systemic toxicity are setbacks to patient well-being, hence the need for a new and affordable approach. Medicinal plants are of importance in the field of drug discovery for cancer as some notable anti-cancer agents have been isolated from them. In the present study, the anti-cancer activity of aqueous extract of Carpobrotus edulis (C. edulis), a ground-creeping edible medicinal plant was investigated in SK-N-BE(2) and SH-SY5Y neuroblastoma cells. The effect of C. edulis on cell viability and survival was determined using MTT (3-[4,5-dimethylthiazol-2-yl] 2,5 diphenyltetrazolium bromide) and clonogenic assays respectively. Apoptosis was determined using a Caspase-9 assay kit and flow cytometry was used to measure intracellular reactive oxygen species (ROS) and depolarization of mitochondrial membrane potential. The results show that C. edulis inhibits cell viability (IC50 of 0.86 mg/ml and 1.45 mg/ml for SK-N-BE (2) and SHSY5Y cells respectively) and colony formation in the neuroblastoma cells as well as induce apoptosis, which is evidenced by an increase in caspase-9 activity in the cells. C. edulis also led to a loss of mitochondrial membrane potential and increased production of ROS. Collectively, these results suggest that C. edulis induces cell death via induction of mitochondrial-mediated apoptosis and accumulation of intracellular ROS, thus providing a rationale for further investigations.Item Sutherlandia frutescens: The meeting of science and traditional knowledge(Mary Ann Liebert, 2013) Aboyade, Oluwaseyi; Styger, Gustav; Gibson, Diana; Hughes, GailSutherlandia frutescens (L.) R.Br. (syn. Lessertia frutescens (L.) Goldblatt and J.C. Manning) is an indigenous medicinal plant extensively used in South Africa to treat a variety of health conditions. It is a fairly widespread, drought-resistant plant that grows in the Western, Eastern, and Northern Cape provinces and some areas of KwaZulu-Natal, varying in its chemical and genetic makeup across these geographic areas.1 Sutherlandia is widely used as a traditional medicine. Extensive scientific studies are being carried out on the safety, quality, and the efficacy of this medicinal plant to validate the traditional claims, elucidate the bioactive constituents, and conduct clinical trials. This has resulted in a unique situation in South Africa’s history, where traditional knowledge and science intersect to provide insight into this popular plant. This photoessay attempts to illustrate the interlinkage of science with the indigenous knowledge of traditional healers, the local knowledge of people who care for the sick, product development, and innovation agenda of the country as it relates to this plant.Item Photosynthetic adaptation of two semi-arid species of Gethyllis (Kukumakranka) to drought-and-shade stress(Elsevier, 2013) Daniels, C.W.; Mabusela, Wilfred T.; Marnewick, Jeanine L.; Valentine, A.J.Gethyllis multifolia and Gethyllis villosa are winter-growing, summer-blooming, deciduous and bulbous geophytes that grow naturally in the semi-arid ‘Succulent Karoo Biome’ of South Africa. G. multifolia is threatened in its natural habitat and resides in the ‘Vulnerable’ category of the ‘Red Data List of Southern African Plants’. Previous investigations suggested that G. multifolia is more sensitive to drought stress than G. villosa and that both species adopted certain morphological changes in their leaves during shade stress. Current models indicate that this biome is being exposed to increasingly drier conditions and shading from encroaching indigenous plant species. In this study, the photosynthetic gas exchange responses of both species to drought and shade stresses were investigated and the ‘Vulnerable’ conservation status of G. multifolia. This investigation found that during drought stress G. villosa had a more enhanced photosynthetic performance than G. multifolia which appears not to be related to foliar adaptations such as specific leaf mass (SLM), but to the G. villosa's leaves maintaining their stomatal conductance (Gs), photosynthetic light compensation (LCP) and photon yields. Furthermore, during shade stress G. villosa also had an improved photosynthetic performance by not altering its photosynthetic LCP during reduced light conditions. It can be concluded that G. multifolia has a lower capacity than G. villosa to adapt its photosynthetic apparatus to changing environments such as increasing drought and shaded conditions. This may be a contributing factor to the threatened conservation status of G. multifolia.Item Challenges relating to comparison of flavonoid glycosides dissolution profiles from Sutherlandia frutescens products(De Gruyter Open, 2017) Mbamalu, Oluchi; Syce, James; Samsodien, HalimaUnlike the case of conventional drug formulations, dissolution tests have hitherto not been required for herbal medicinal products commercially available in South Africa. This study investigated dissolution of the South African Sutherlandia frutescens using selected flavonoid glycosides as marker compounds. Dissolution of markers was assessed in three dissolution media at pH 1.2, 4.5 and 6.8, and samples were analysed using a validated HPLC method. The dissolution profile of each marker varied for the different materials investigated. All three media utilised showed differences in flavonoid glycoside dissolution between the S. frutescens products evaluated, with f2 values <50 for comparison of flavonoid dissolution from any two of the materials. Dissolution of S. frutescens materials could thus be characterised using the markers in all the media tested. This tool may be employed in the future for comparison of orally administered S. frutescens products, provided between batch variability is evaluated and found less than between-sample variability.Item Antimicrobial activities of a novel biflavonoid and other constituents from Rhus natalensis(Academic Journals, 2013) Mwangi, Henry M.; Mabusela, Wilfred T.; Abegaz, Berhanu M.; Martin, Onani O.Phytochemical studies on Rhus natalensis root bark collected from Kenya led to the isolation and identification of a new biflavonoid (3-(1-(2,4-dihydroxyphenyl)-3,3-bis(4-hydroxyphenyl)-1-oxopropan-2- yl)-7-methoxy-4H-chromone-4-one (1), named rhuschromone, in addition to two other known compounds; 2',4'-dihydroxychalcone-(4-O-5''')-4'',2''',4'''-trihydroxychalcone (2) and 3-((Z)-heptadec-13- enyl) benzene-1,2-diol (3). The chemical structures of the isolated compounds were established using spectroscopic techniques including high field nuclear magnetic resonance (NMR). The total extracts and the isolated compounds were tested for their antimicrobial activities against different strains of bacteria.Item Some alkaloids and flavonoids from Cissampelos capensis(Academic Journals, 2015) Babajide, Jelili Olalekan; Mabusela, Wilfred T.; Green, IvanFollowing the screening of several plant species from an inventory of common medicinal plants from South Africa for medicinal properties, Cissampelos capensis was selected for further investigation due to its interesting and useful ethnomedicinal properties. This study attempts to relate specific constituents present in this plant with its widespread ethnomedicinal uses. Six compounds were isolated and their structures were unambiguously established by spectroscopic methods. The compounds are: 5,6-dehydro-4,5-dihydroxy-1,3,6-trimethoxy-17-methylmorphinan-7-one (1); 1,2-methylenedioxy-3-hydroxy -9,10-dimethoxyaporphine (2); 5,6-didehydro-4-hydroxy-3,6-dimethoxy-17-methylmorphinan-7-one (3); 3,7,8,3'-tetramethoxy- 6 - C-methyl- 5,4'-dihydroxyflavone (6 -C-methylquercetin 3, 3',7, 8 -tetramethyl ether) (4); 5, 7, 8 -trihydroxy-2?, 5?-dimethoxy-3?,4?- methylenedioxyisoflavanone (5); 3 -methoxy-6 -C-methyl-3',4',5,7,8 -pentahydroxyflavone (6 -C- methylquercetin -3-methyl ether) (6). Five of the isolated compounds, (viz., 1,2,4,5 and 6) have, to our knowledge, not been reported previously. The crude fractions and isolates were tested for cytotoxicity using the brine shrimp lethality test and for antimicrobial properties using nine microbes, including three Gram -ve, three Gram +ve bacteria and three fungi. The Gram-negative bacteria were Pseudomonas aeruginosa (NCTC 10332), Proteus vulgaris (NCTC 4175) and Escherichia coli Sero type 1 (NCTC 09001), while the Gram-positive bacteria were Bacillus subtilis (NCTC 8236), Staphylococcus aureus (NCTC 13134) and Bacillus licheniformis (NCTC 01097). The Fungal species used were Candida albicans (ATCC 90028), Candida eropiralis (ATCC 750) and Aspergillus niger (ATCC 10578). The n-Hex fractions were not active while the highest activities were found in the methanolic extracts. The total tertiary alkaloid fraction (TTA) showed the highest activity against the Bacillus substillis. Compounds 1, 2 and 5 appear to be the most promising with regards to the prospects of drug development.Item Phytochemical screening and biological activity studies of five South African indigenous medicinal plants(Academic Journals, 2010) Babajide, Jelili Olalekan; Mabusela, Wilfred T.; Green, Ivan; Ameer, Farouk; Weitz, Frans; Iwuoha, Emmanuel I.Different extracts and fractions of five selected indigenous South African medicinal plants, namely, Cissampelos capensis, Geranium incanum and three Gethyllis species, were subjected to phytochemical screening and testing for cytotoxicity using the brine shrimp lethality bioassay, and antimicrobial activity assays against nine microbes, which included three fungal species, three Gram negative and three Gram positive bacteria.The majority of the extracts tested positive for the presence of tannins, phenolics and flavonoids, while in selected cases, phytochemical tests suggested the presence of essential oils, glycosides or alkaloids. The methanol extract of Gethyllis gregoriana displayed the highest cytotoxicity levels. Generally, the highest levels of biological activity were shown to reside in the methanolic extracts, while hexane extracts revealed very low to zero activity. The total tertiary alkaloid (TTA) of C. capensis was mostly active against Bacillus subtilis, a Gram +ve bacteria. The trends observed for the cytotoxicity assay were in agreement with those observed for the antimicrobial assay.Item HPLC determination of selected flavonoid glycosides and their corresponding aglycones in Sutherlandia frutescens materials(OMICS, 2016) Mbamalu, Oluchi; Antunes, E.; Silosini, N.; Samsodien, Halima; Syce, JamesSutherlandia frutescens is a popular South African plant commercially available in a range of formulations. However, reference standards for quality and stability assessment are lacking. This work reports the development and validation of a reversed phase HPLC method for the analysis of flavonoid glycosides and their corresponding aglycones in S. frutescens products. Five materials containing either leaf powder (LP) or spray-dried aqueous extract (SDAE) of S. frutescens were analysed for flavonoid content. A primary objective was to isolate non-commercially available flavonoid glycoside compounds (sutherlandins) for use as reference standards. Sutherlandins A, B, C and D were successfully isolated, and used, with other flavonoid compounds for HPLC assay development. The developed HPLC method was linear in the range of 0.2 to 60 µg/ml for quercitrin; 0.2 to 120 µg/ml for quercetin and kaempferol; 0.2 to 200 µg/ml for rutin and kaempferol-3-O-rutinoside; 4 to 180 µg/ml for sutherlandins A and D; and 4 to 200 µg/ml for sutherlandins B and C. Percentage content of sutherlandins A, B, C and D, quercetin and kaempferol in different plant materials were significantly different (P<0.001). The developed HPLC method is simple, precise and robust; and can be employed for the simultaneous determination of flavonoid glycosides and aglycones for quality control of S. frutescens products.