The genus Canthium: A comprehensive summary on its traditional use, phytochemistry, and pharmacological activities.

Canthium Lam. is a genus of flowering plants of the Rubiaceae family with about 80-102 species mainly distributed in Asia, tropical and subtropical Africa. The genus is closely related to Keetia E. Phillips and Psydrax Gaertn. and plants of this genus are used in folk medicine for the treatment of diarrhea, worms, leucorrhoea, constipation, snake bites, diabetes, hypertension, venereal diseases, and malaria. The present review covers a period of 52 years of biological and chemical investigations into the genus Canthium and has resulted in the isolation of about 96 secondary metabolites and several reported biological properties. For the Rubiaceae family, iridoids were reported as being the chemotaxonomic markers of this genus (∼25%). Other reported classes of compounds include alkaloids, flavonoids, phenolic compounds, cyanogenic glycosides, coumarins, sugar alcohols, lignans, triterpenoids, and benzoquinones. The main reported pharmacological properties of most species of this genus include antioxidant, antiplasmodial, antipyretic, anti-inflammatory, antidiabetic, neuroprotective and antimicrobial activities with the latter being the most prominent. Considering the diversity of compounds reported from plants of this genus and their wide range of biological activities, it is considered to be worthy to further investigate them for the discovery of potentially new and cost effective drugs.

Three Selected Edible Crops of the Genus Momordica as Potential Sources of Phytochemicals: Biochemical, Nutritional, and Medicinal Values.

Momordica species (Family Cucurbitaceae) are cultivated throughout the world for their edible fruits, leaves, shoots and seeds. Among the species of the genus Momordica, there are three selected species that are used as vegetable, and for medicinal purposes, Momordica charantia L (Bitter melon), Momordica foetida Schumach (Bitter cucumber) and Momordica balsamina L (African pumpkin). The fruits and leaves of these Momordica species are rich in primary and secondary metabolites such as proteins, fibers, minerals (calcium, iron, magnesium, zinc), ß-carotene, foliate, ascorbic acid, among others. The extracts from Momordica species are used for the treatment of a variety of diseases and ailments in traditional medicine. Momordica species extracts are reputed to possess anti-diabetic, anti-microbial, anthelmintic bioactivity, abortifacient, anti-bacterial, anti-viral, and play chemo-preventive functions. In this review we summarize the biochemical, nutritional, and medicinal values of three Momordica species (M. charantia, M. foetida and M. balsamina) as promising and innovative sources of natural bioactive compounds for future pharmaceutical usage.

Exploration of Modern Chromatographic Methods Coupled to Mass Spectrometric Techniques for Trace Element and Chemical Composition Analyses in the Leaf Extracts of Kigelia africana.

The use of Kigelia africana (Lam.) Benth. plant dates back to last century. The different parts of the plant exhibited various pharmacological activities. But literature search revealed scanty use of the leaf extract owing to few information regarding the various phytochemical constituents. The aim of this study is, therefore, to profile the chemical compounds through the use of omics-based approach. Ultrahigh-pressure liquid chromatography quadrupole-time-of-flight tandem mass spectrometry (qTOF-UPLC/MS) alongside gas chromatography quadrupole time-of-flight tandem mass spectrometry (qTOF-GC/MS) were used to profile these chemical compounds. Inductively coupled plasma optical emission spectrometry (ICP-OES) was used to determine the concentration of trace elements as well as limit of detection (LOD) and quantification (LOQ). For broader metabolite determination, a modified sample preparation was employed and to ascertain the cytoprotective potential of the leaf extract, MTT assay on A375 human melanoma cell lines was carried out. Sixty-eight peaks were characterized with the identification of 275 metabolites where 8 of these were confirmed. Of importance is the identification of eugenol; a polyphenolic compound at m/z 165.09 on fragments 119.09, 147.08, 109.10, 137.10, and 137.06. for qTOF-GC/MS analysis, 232 metabolites were identified consisting of terpenes, fatty acids, furans, amines, amides, and alkanes. The concentration of trace elements in the leaf extract ranged from 0.08 for Zn to 0.28 mg/kg for Fe with low concentrations of Cd according to the recommendation of European Legislation. The leaf showed higher inhibition of growth against A375 human melanoma cell lines in a dose-dependent manner. The results showed that K. africana leaf contained various pharmaceuticals, nutraceuticals, designer drugs, and phytochemicals, and these chemicals have minimal cytotoxic side effects. To the best of our knowledge, this is the first study providing information on the various secondary metabolites in the leaf extract through the use of omics-based approach. Therefore, the leaves of K. africana plant can be used as antiinflammatory, antimicrobial, antibacterial, antifungal, and antiproliferative agents for industrial, therapeutic, and medicinal applications. Graphical Abstract.

UHPLC/GC-TOF-MS metabolomics, MTT assay, and molecular docking studies reveal physostigmine as a new anticancer agent from the ethyl acetate and butanol fractions of Kigelia africana (Lam.) Benth. fruit extracts.

Kigelia africana plant is widely used as a herbal remedy in preventing the onset and the treatment of cancer-related infections. With the increase in the research interest of the plant, the specific chemical compound or metabolite that confers its anticancer properties has not been adequately investigated. The ethyl acetate and butanol fractions of the fruit extracts were evaluated by 2-(4,5-dimethylthiazol-2-yl)-3,5-diphenyl-2H-tetrazolium bromide assay against four different cell lines, with the ethyl acetate fraction having inhibition concentration values of 0.53 and 0.42 µM against Hep G2 and HeLa cells, respectively. More than 235 phytoconstituents were profiled using UHPLC-TOF-MS, while more than 15 chemical compounds were identified using GC-MS from the fractions. Molecular docking studies revealed that physostigmine, fluazifop, dexamethasone, sulfisomidine, and desmethylmirtazapine could favorably bind at higher binding energies of -8.3, -8.6, -8.2, and -8.1 kcal/mol, respectively, better than camptothecin with a binding energy of -7.9 kcal/mol. The results of this study showed that physostigmine interacted well with topoisomerase IIα and had a high score of pharmacokinetic prediction using absorption, distribution, metabolism, excretion, and toxicity profiles, thereby suggesting that drug design using physostigmine as a base structure could serve as an alternative against the toxic side effects of doxorubicin and camptothecin.

Azole antifungal resistance in fungal isolates from wastewater treatment plant effluents.

Wastewater treatment plants (WWTPs) can be significant sources of antifungal resistant fungi, which can disseminate further in the environment by getting into rivers together with effluents discharged from WWTPs and pose a risk for human health. In this study, the presence of azole resistance was determined in fungal isolates from treated effluents of two WWTPs using the standard microdilution method from Clinical and Laboratory Standards Institute (CLSI). A total of 41 fungal isolates representing 23 fungal species and 16 fungal genera were obtained. Fungal genera related to the known human and/or plant pathogens such as Aspergillus, Fusarium, and Candida were detected. Among the observed species, the susceptibility of Aspergillus fumigatus and Fusarium oxysporum was tested against fluconazole (FCZ), ketoconazole (KTZ), itraconazole (ITZ), and voriconazole (VCZ). The isolate A. fumigatus was susceptible to KTZ, ITZ, and VCZ, while it showed resistance against FCZ. On the contrast, the isolate F. oxysporum showed resistance to KTZ, ITZ, and VCZ. Comparatively, VCZ showed highest activity against both A. fumigatus and F. oxysporum. Analysis of the gene Cyp51A for the A. fumigatus isolate showed no evidence of drug resistance that could be related to point mutations and/or tandem repeats in the gene. To the best of our knowledge, this is the first susceptibility test study on A. fumigatus and F. oxysporum isolates from the WWTPs of South Africa. In conclusion, this study indicated an urgent need for thorough investigation with larger group of fungal isolates from different regions of South Africa to broadly understand the role of WWTPs in the dissemination of azole antifungal drug resistance.

Metabolome modulatory effects of Kigelia africana (Lam.) Benth. fruit extracts on oxidative stress, hyperlipidaemic biomarkers in STZ-induced diabetic rats and antidiabetic effects in 3T3 L1 adipocytes.

OBJECTIVES: The management of diabetes is considered a global problem, and a cure is yet to be discovered. This study investigated the modulatory effect of Kigelia africana fruit on oxidative stress and hyperlipidaemic biomarkers in STZ-induced diabetic rats, profiled phytoconstituents using GC-TOF-MS and evaluated antidiabetic effects on 3T3 L1 adipocytes. METHODS: Thirty male Wistar rats (120-150 g) were divided into six groups (n = 5). Diabetes was induced by a single intraperitoneal injection of STZ (60 mg/kg) and treated with 100, 200 and 400 of hexane fraction of KA for 28 days. Immunohistochemical evaluation was carried out using avidin-biotin immunoperoxidase (ABI) method. Catalase and SOD activities as well as the levels of total protein, albumin, bilirubin, triglyceride, cholesterol, and high-density lipoprotein were measured. KEY FINDINGS: The expressions of oxidative stress and hyperlipidaemic biomarkers alongside fasting blood glucose concentrations were remarkedly decreased in KA-treated diabetic rats. Moreover, there was a significant increase in endocrine cell distribution, area covered with increase in ß-cell mass, composition and morphology of KA-treated animals. Additionally, there was constant up-regulation in 3T3 L1 adipocytes due to the presence of phytoconstituents. CONCLUSION: Kigelia africana fruit can act as a modulatory agent due to its ameliorative effects against oxidative stress.

Spinel ferrite nanoparticles and nanocomposites for biomedical applications and their toxicity.

This review focuses on the biomedical applications and toxicity of spinel ferrite nanoparticles (SFNPs) with more emphasis on the recently published work. A critical review is provided on recent advances of SFNPs applications in biomedical areas. The novelty of SFNPs in addressing the bottleneck problems encountered in the areas of health; in particular, for diagnosis and treatment of tumour cells are well reviewed. Furthermore, research gaps, toxicity of SFNPs and areas which still need more attention are highlighted. Based on the result of this review, the SFNPs have unlimited capacity in cancer treatment, disease diagnosis, magnetic resonance imaging, drug delivery and release. Overall, stepping out of the conventional way of treatment is difficult but also essential in bringing long lasting solution for cancer and other diseases treatment. In fact, the toxicity study and commercialisation of the SFNPs based cancer treatment options are the main challenges and need further study, in order to reduce unforeseen consequences.

Evaluation of Phytochemicals, Antioxidants, Trace Elements in Kigelia africana Fruit Extracts and Chemical Profiling Analysis Using UHPLC-qTOF-MS2 Spectrometry.

The study aimed at evaluating the phytochemical composition, antioxidant potentials and the levels of trace elements in the fruit extract of Kigelia africana obtained by different extraction solvents in order to ascertain its numerous pharmacological activities and identify the different chemical compounds responsible for these activities. The crude extract in ethanol and four other solvent fractions (hexane, ethylacetate, butanol and aqueous) were obtained for phytochemical screening. Antioxidant potentials of K. africana fruit were investigated spectrophotometrically using hydroxyl ion scavenging (OH-) activity, metal ion chelating activity, anti-lipid peroxidation activity as well as total antioxidant capacity assays. Trace element (Mn, Zn, Cd, Ni, Cu, Pb, Cr, Co and Fe) levels were measured using a plasma-emission spectrometer that has an auto sampler AS 93-plus and coupled with Nebulizer CETAC U-6000AT+ after microwave acid digestion of the fruit extracts. Chemical identification was performed using ultra-high-pressure liquid chromatography-quadrupole time-of-flight tandem mass spectrometry (UHPLC-qTOF-MS2). Kigelia africana fruit extracts obtained showed a variety of bioactive phytochemical compounds including phenolic acids, flavonoids, saponins, tannins and glycosides. The total antioxidant capacity activities of the aqueous, butanol, ethanol, hexane and ethylacetate extracts are 15.04, 52.11, 44.95, 79.27 and 175.20 mg AAE/g. Metal ion chelating activity showed significant correlation with lipid peroxidation inhibition activity at p ≤ 0.01 and with OH- scavenging activity at p ≤ 0.05. PCA analysis revealed that all the extract/fractions have higher total antioxidant activities compared to aqueous extract with hexane extract exhibiting the highest radical scavenging potential. HCA showed similarities with three well-defined clusters and PLS regression was used to predict total antioxidant activity. High sensitivity by low values of limits of detection and quantification was observed ranging from 0.021 to 0.085 mg/ml and 0.063 to 0.258 mg/ml for Zn and Fe respectively. Ethylacetate extract had high concentration of Fe (0.5656 mg/kg). For the standardization of the K. africana fruit extract, 244 chemical compounds were identified by measuring m/z values with threshold override of 100,000 and analysing mass spectrometer fragmentation behaviour while 16 of these were confirmed. Kigelia africana fruit extract is a good source of antioxidant and possess maximum accepted concentration of trace elements according to European legislation (1881/2006/EC). The metabolites identified exhibited numerous pharmacological activities. The method and results suggest the applicability for commercial use of this K. africana fruit in the treatment of oxidative-related diseases. Graphical abstract The phytochemical, antioxidant and trace element composition of crude ethanol extract, hexane, butanol, aqueous and ethylacetate extracts of Kigelia africana fruit were determined. The fruit extracts were found to possess good antioxidant activity, maximum acceptable amount of essential trace elements as well as the presence of bioactive phytochemicals. K. africana fruit would be an ideal candidate in improving human health and thus the management of oxidative-related diseases such as diabetes, by involving in the antioxidant defense system against free radical generation.

Removal Efficiency of Faecal Indicator Organisms, Nutrients and Heavy Metals from a Peri-Urban Wastewater Treatment Plant in Thohoyandou, Limpopo Province, South Africa.

Wastewater treatment facilities are known sources of fresh water pollution. This study was carried out from January to June 2014 to assess the reduction efficiency of some selected contaminants in the Thohoyandou wastewater treatment plant (WWTP). The pH and electrical conductivity of the effluent fell within the South African wastewater discharge guidelines. The WWTP showed the chemical oxygen demand reduction efficiency required by the Department of Water Affairs (DWA) guidelines of 75 mg/L for the months of April and June, although it was below this standard in March and May. Free chlorine concentration varied between 0.26-0.96 mg/L and exceeded the DWA guideline value of 0.25 mg/L. The concentration of nitrate-nitrogen (NO3(-) N) in the influent and effluent varied between 0.499-2.31 mg/L and 7.545-19.413 mg/L, respectively. The concentration of NO3- N in the effluent complied with DWA effluent discharge standard of 15 mg/L, except in April and May. Phosphate concentrations in the influent and effluent were in the ranges of 0.552-42.646 mg/L and 1.572-32.554 mg/L, respectively. The WWTP showed reduction efficiencies of E. coli and Enterococci during some sampling periods but the level found in the effluent exceeded the recommended guideline value of 1000 cfu/100 mL for faecal indicator organisms in wastewater effluents. Consistent removal efficiencies were observed for Al (32-74%), Fe (7-32%) and Zn (24-94%) in most of the sampling months. In conclusion, the Thohoyandou WWTP is inefficient in treating wastewater to the acceptable quality before discharge.

The simultaneous stripping of arsenic and selenium from wastewaters using hollow-fibre supported liquid membranes.

The extraction of total arsenic and selenium using hollow-fibre supported liquid membranes (HFSLMs), with specific interest in the optimal conditions for the extraction in wastewater, is reported. The extraction time, type of liquid membrane, sample and donor pH and stirring rate were optimised, and thereafter, the developed method was tested in real wastewater samples. The optimal HFSLMs adopted, after optimisation tests, comprised of Aliquat 336, 0.8 M NaOH, 200 rpm and 80 min as the extractant, stripping phase, stirring rate and reaction time, respectively. The developed method had reasonable-to-high extraction efficiencies in real wastewater samples with the final effluent recording as high as 73 and 78 % removal efficiencies for Se and As, respectively. Considering the initial concentrations found in the samples, use of this developed method could bring down the concentrations to levels admissible by the United States Environmental Protection Agency (US-EPA) and World Health Organisation (WHO).

Cytotoxicity, phytochemical analysis and antioxidant activity of crude extracts from rhizomes of Elephantorrhiza elephantina and Pentanisia prunelloides.

BACKGROUND: Elephantorrhiza elephantina (Ee) and Pentanisia prunelloides (Pp) are two medicinal plants which are widely used to remedy various ailments including diarrhoea, dysentery, inflammation, fever, rheumatism, heartburn, tuberculosis, haemorrhoids, skin diseases, perforated peptic ulcers and sore joints in southern Africa (South Africa, Swaziland, Botswana and Zimbabwe). The following study was conducted to explore the in vitro cytotoxicity, antioxidant properties and phytochemical profile of the two medicinal plants. MATERIALS AND METHODS: The cytotoxicity of the aqueous and methanol extracts and fractions of both species was studied using the brine shrimp lethality tests (BST) for the first time. RESULTS: The results demonstrated that the lethality (LC50) for crude extracts for both plants ranged between 1.8 and 5.8 ppm and was relatively greater than that for the methanol, ethyl acetate and chloroform fractions of the extracts which ranged between 2.1 ppm and 27 ppm. This suggested that crude extracts were more potent than their respective fractions, further explaining that the different fractions of phytochemicals in these plant species work jointly (in synergy) to exert their therapeutic efficacy. Both aqueous and methanol extracts of the two medicinal plants demonstrated a high degree of antioxidant capacity against the DPPH radical with the Duh and Yen inhibition percentage ranging between 4.5% and 72%. Phytochemical studies of the rhizome extracts showed that the major compounds present include flavonoids, tannins, anthocyanidins, anthraquinones, triterpenoids (oleanolic acid), the steroidal saponin Diosgenin, the sugars, rhamnose, glucuronic acid, Arabinose and hexoses. CONCLUSION: This is the first report of the detection and isolation of diosgenin and oleanolic acid from the rhizome extracts of Ee and Pp. All structures were determined using spectroscopic/spectrometric techniques (1H NMR and 13C and LC-ESI-MS) and by comparison with literature data.