Investigation of exosomal tetraspanin profile in sepsis patients as a promising diagnostic biomarker.

INTRODUCTION: Sepsis, a leading cause of mortality globally, has a complex and multifaceted pathophysiology which still requires elucidation. Therefore, this study aimed to analyze and quantify the number of exosomes in sepsis patients from a South African cohort using the ExoView (NanoView Biosciences, Boston, MA) platform. METHODS: Blood samples were collected from black South African patients attending the local Intensive Care Unit (ICU) hospital. Exosomes were isolated and characterize via TEM and CD63 ELISA kits. ExoView was used to determine particle count, particle size distribution and colocalization of different tetraspanin markers. RESULTS: Exosomal levels in sepsis patients were significantly higher compared to the control group (p < 0.05). Sepsis exosomes showed a homogenous size distribution ranging from 55 to 70 nm. Tetraspanin colocalization analysis revealed that sepsis exosomes have significantly higher CD63/CD9, CD63/CD81 and CD63/CD9/CD81 colocalization percentages than the control group. CONCLUSION: This unique tetraspanin colocalization pattern of sepsis exosomes could serve as a potential sepsis biomarker. Further investigations are required to identify sepsis exosomal cargo signatures for further understanding of sepsis pathophysiology in order to develop effective diagnostics and treatments.

Hesperidin improves physiological outcomes in an arginine vasopressin rat model of pre-eclampsia.

BACKGROUND: Hesperidin, a flavanone commonly found in citrus fruits and herbal formulations, has emerged as a potential new therapeutic agent for modulating several diseases. Since pre-eclampsia is a growing public health threat, it may negatively impact the economy and increase the disease burden of South Africa. Phytocompounds are easily accessible, demonstrate minimal side effects, and may confer novel medicinal options as a treatment and preventive preference. OBJECTIVE: To investigate the physiological, biochemical, and hematological outcomes of hesperidin in an arginine vasopressin (AVP)-induced rodent model of pre-eclampsia. METHODS: Female Sprague-Dawley rats were surgically implanted with mini-osmotic pumps to deliver AVP (200 ng/h) subcutaneously. Animals were treated with hesperidin at 200 mg/kg.b.w via oral gavage for 14 days. Systolic and diastolic blood pressures were measured on GD 7, 14, and 18 using a non-invasive tail-cuff method and were euthanized on GD 21. RESULTS: The findings showed that hesperidin administration significantly decreased blood pressure (P < 0.05) and urinary protein levels in pregnant rats (P < 0.001). Placental and individual pup weight also increased significantly in the pregnant hesperidin-treated groups compared to AVP untreated groups (P < 0.001). Biochemical and hematological markers such as white blood cell count and lymphocyte levels differed significantly (P < 0.05) in AVP groups treated with and without hesperidin. CONCLUSION: Our results suggest that hesperidin is an antihypertensive agent with modes of action associated with its diuretic and blood pressure lowering effects and reduction of proteinuria in AVP-induced pre-eclamptic rats.

In vitro effects of 2-methyl-3-propylbutane-1,4-diol purified from Alstonia boonei on erythrocyte membrane stabilization and mitochondrial membrane permeabilization.

A recent review on the ethnomedicinal, chemical, pharmacological, and toxicological properties of Alstonia boonei revealed the plant's potential in the treatment and management of a range of diseases. However, most of these pharmacological effects are only traceable to the crude form of the plant extract and not specific natural products. Phytochemical investigation of the methanol fraction of the methanol extract of the stem-bark of Alstonia boonei led to the isolation and identification of 2-methyl-3-propylbutane-1,4-diol. The structures were elucidated by the application of 1D-, and 2D-NMR spectroscopic analyses and by comparison with literature data. In this study, the membrane stabilizing activity, mitochondrial membrane permeability transition pore opening, cytochrome c release, mitochondrial ATPase activity, and prevention of mitochondrial lipid peroxidation activity of 2-methyl-3-propylbutane-1,4-diol (MPBD) isolated from A. boonei were determined. The results showed that MPBD significantly (p < .05) prevented peroxidation of mitochondrial membrane lipids and hemolysis using both the heat-induced and hypotonic solution-induced membrane stabilization assays. On the contrary, the compound caused large amplitude swelling of rat liver mitochondria in the absence of calcium, significant (p < .05) cytochrome c release and enhancement of mitochondrial ATPase activity in vitro. Our findings suggest that MPBD showed characteristic biological properties useful in modulating cell death.

Anticancer effects of herbal medicine Emelia-M, Mshikazi and Delosma H against human leukaemia cells.

Background: Leukaemia is one of the three major types of blood cancers that lead to the overproduction of abnormal white blood cells. Emelia M (EMB), Mshikazi and Delosma H are herbal medicines that are being used by traditional healers in KwaZulu-Natal, South Africa to treat leukaemia and other diseases. Objectives: To gain insight into the safety (non-toxic effect), anti-cancer activity, mechanisms of action and phytochemical profiles of traditional herbal medicines (Emelia M (EMB), Mshikazi and Delosma H) in South Africa. Methods: The viability of human peripheral blood mononuclear cells (PBMCs), monocytic (THP-1) and T-lymphocyte (Jurkat) cell lines exposed to varying concentrations of aqueous extracts of the three herbal medicines were assessed using adenosine triphosphate (ATP) assay. Results: All three extracts showed a dose-dependent effect on the viability of PBMCs. Cell viability decreased with increasing concentrations of extracts when compared with the untreated cells at 24 and 48 hours. The inhibitory activities (IC50) of the extract were found in the order of Mshikazi > EMB, > Delosma H. All the extracts induced apoptosis with minimal necrosis. Many bioactive compounds that have been previously reported to have anticancer effects were identified in the extracts. Conclusion: Mshikazi extract significantly inhibited the growth of THP-1 and Jurkat cells and induced cell death through apoptosis than the other two extracts.

South African medicinal plants displaying angiotensin-converting enzyme inhibition: Potential use in the management of preeclampsia.

In resource-limited settings, such as South Africa, hypertensive disorders of pregnancy such as preeclampsia, is the most common direct cause of maternal deaths. Current management strategies of preeclampsia primarily involve the use of pharmaceutical drugs, which are frequently associated with undesirable side-effects. Moreover, these drugs are often not easily accessible due to financial and economic constraints. Consequently, many patients rely on traditional medicine obtained from medicinal plants to manage health-related conditions. Angiotensin-converting enzyme inhibitors are widely used drugs for the management of preeclampsia. This narrative review aims to highlight the use of indigenous medicinal plants from South Africa with Angiotensin-converting enzyme inhibitory activity whilst also evaluating their potential use in the treatment of hypertension in pregnancy. This information will influence traditional healers and sangomas in their patient management. Furthermore, the antihypertensive potential of these plants will be unraveled thus facilitating the development of new naturally occurring pharmaceutical products to reduce maternal and neonatal mortality and morbidity.

Testicular ultrastructure and hormonal changes following administration of tenofovir disoproxil fumarate-loaded silver nanoparticle in type-2 diabetic rats.

Reproductive dysfunctions (RDs) characterized by impairment in testicular parameters, and metabolic disorders such as insulin resistance and type 2 diabetes mellitus (T2DM) are on the rise among human immunodeficiency virus (HIV) patients under tenofovir disoproxil fumarate (TDF) and highly active antiretroviral therapy (HAART). These adverse effects require a nanoparticle delivery system to circumvent biological barriers and ensure adequate ARVDs to viral reservoir sites like testis. This study aimed to investigate the effect of TDF-loaded silver nanoparticles (AgNPs), TDF-AgNPs on sperm quality, hormonal profile, insulin-like growth factor 1 (IGF-1), and testicular ultrastructure in diabetic rats, a result of which could cater for the neglected reproductive and metabolic dysfunctions in HIV therapeutic modality. Thirty-six adult Sprague-Dawley rats were assigned to diabetic and non-diabetic (n = 18). T2DM was induced by fructose-streptozotocin (Frt-STZ) rat model. Subsequently, the rats in both groups were subdivided into three groups each (n = 6) and administered distilled water, TDF, and TDF-AgNP. In this study, administration of TDF-AgNP to diabetic rats significantly reduced (p < 0.05) blood glucose level (268.7 ± 10.8 mg/dL) from 429 ± 16.9 mg/dL in diabetic control and prevented a drastic reduction in sperm count and viability. More so, TDF-AgNP significantly increased (p < 0.05) Gonadotropin-Releasing Hormone (1114.3 ± 112.6 µg), Follicle Stimulating Hormone (13.2 ± 1.5 IU/L), Luteinizing Hormone (140.7 ± 15.2 IU/L), testosterone (0.2 ± 0.02 ng/L), and IGF-1 (1564.0 ± 81.6 ng/mL) compared to their respective diabetic controls (383.4 ± 63.3, 6.1 ± 1.2, 76.1 ± 9.1, 0.1 ± 0.01, 769.4 ± 83.7). Also, TDF-AgNP treated diabetic rats presented an improved testicular architecture marked with the thickened basement membrane, degenerated Sertoli cells, spermatogenic cells, and axoneme. This study has demonstrated that administration of TDF-AgNPs restored the function of hypothalamic-pituitary-gonadal axis, normalized the hormonal profile, enhanced testicular function and structure to alleviate reproductive dysfunctions in diabetic rats. This is the first study to conjugate TDF with AgNPs and examined its effects on reproductive indices, local gonadal factor and testicular ultrastructure in male diabetic rats with the potential to cater for neglected reproductive dysfunction in HIV therapeutic modality.

New Alk(en)ylhydroxycyclohexanes with Tyrosinase Inhibition Potential from Harpephyllum caffrum Bernh. Gum Exudate.

This work presents the first report on the phytochemical investigation of Harpephyllum caffrum Bernh. gum exudate. A known cardanol, 3-heptadec-12'-Z-enyl phenol (1) and three new alk(en)ylhydroxycyclohexanes, namely, (1R,3R)-1,3-dihydroxy-3-[heptadec-12'(Z)-enyl]cyclohexane (2) (1S,2S,3S,4S,5R)-1,2,3,4,5-pentahydroxy-5-[octadec-13'(Z)-enyl]cyclohexane (3) and (1R,2S,4R)-1,2,4-trihydroxy-4-[heptadec-12'(Z)-enyl]cyclohexane (4) were isolated from the gum. The structures of the compounds were determined by extensive 1D and 2D NMR spectroscopy and HR-ESI-MS data. The ethanolic extract of the gum was found to be the most potent tyrosinase inhibitor with IC50 of 11.32 µg/mL while compounds 2 and 3, with IC50 values of 24.90 and 26.99 µg/mL, respectively, were found to be potential anti-tyrosinase candidates from the gum. Gum exudate may be a potential source for non-destructive harvesting of selective pharmacologically active compounds from plants. The results also provide evidence that H. caffrum gum may find application in cosmetics as a potential anti-tyrosinase agent.

Studies on testicular ultrastructural and hormonal changes in type-2 diabetic rats treated with highly active antiretroviral therapy conjugated silver nanoparticles.

AIM: This study investigated the impact of highly active antiretroviral therapy (HAART) loaded silver nanoparticles (AgNPs) as HAART-AgNPs on the sperm count, viability, serum hormonal profile, insulin-like growth factor I (IGF-1), and testicular ultrastructure. METHODS: Thirty-six adult male Sprague-Dawley rats were allocated into diabetic and non-diabetic groups (n = 18). The rats in the diabetic group were induced experimental type 2 diabetes using fructose and streptozotocin (frt-STZ). Animals in both groups were subdivided into three groups each, A-C and DF (n = 6), and received distilled water, HAART, and HAART-AgNP, respectively. FINDINGS: Treatment with HAART-AgNP displayed a significant increase (p < 0.05) in serum gonadotropin-releasing hormone (GnRH), follicle-stimulating hormone (FSH), luteinizing hormone (LH), and testicular IGF-1 in diabetic rats. Also, electron microscopy revealed ameliorated testicular ultrastructure upon administration of HAART-AgNP in diabetic rats that were previously marked with architectural and cellular alterations. In addition, treatment with HAART-AgNP significantly reduced (p < 0.05) the blood glucose levels of diabetic rats. In contrast, the treatment of non-diabetic rats with HAART caused a significant decrease (p < 0.05) in the sperm count, serum GnRH, and testicular IGF-1, however, this treatment induced ultrastructural changes and a significant increase (p < 0.05) in serum testosterone levels in diabetic and non-diabetic rats. SIGNIFICANCE: This study has demonstrated the beneficial impact of HAART-AgNP on the hypothalamic-pituitary-gonadal axis, IGF-1, and testicular architecture in male frt-STZ induced diabetic rats. This nanoconjugate could be a potential nano-drug candidate to cater for testicular dysfunction and metabolic derangements while managing HIV-infected male individuals.

Tenofovir-silver nanoparticles conjugate ameliorates neurocognitive disorders and protects ultrastructural and cytoarchitectonic properties of the prefrontal cortex in diabetic rats.

Tenofovir disoproxil fumarate (TDF) is the highly recommended antiretroviral drug in human immunodeficiency virus management. Although research has shown the neurological and metabolic disorders associated with TDF administration, the effect of TDF-silver nanoparticles conjugate (TDF-AgNPs) on the disorders has not been fully elucidated. Thus, this study evaluated the neuroprotective effects of TDF-AgNPs on ultrastructural and cytoarchitectonic properties of the prefrontal cortex (PFC) in diabetic rats. Forty-two adult male Sprague-Dawley rats (250 ± 13 g) were randomly divided into non-diabetic groups (1-3) and diabetic groups (4-6), each administered distilled water (0.5 ml/100g, p.o), TDF (26.8 mg/kg/bw, p.o) or TDF-AgNPs (6.7 mg/kg, i.p). After eight weeks of administration, cognitive function, oxidative injury and tissue inflammation were evaluated. Also, PFC ultrastructure was observed using transmission electron microscopy, Nissl staining and immunohistochemistry. Diabetic rats administered TDF exhibited cognitive deficits; and increases in blood glucose, malondialdehyde and interleukin-1 beta (IL-1ß) levels, which correlate with decreases in glutathione level, and superoxide dismutase (SOD) and catalase activities. Furthermore, loss of PFC astrocytes and neuronal organelles was observed. Conversely, TDF-AgNPs administration to diabetic rats improved cognitive deficits; and increased glutathione, SOD, and catalase, but reduced PFC malondialdehyde and IL-1ß concentrations. Notably, TDF-AgNPs prevented loss of PFC neurons and astrocytic cells, and morphology aberration of neuronal organelles. This study suggests that TDF-AgNPs attenuated cognitive deficits via silver nanoparticles' antioxidant and anti-inflammatory properties, preventing the loss of PFC astrocytes and neurons. The TDF-AgNPs may be utilized to ameliorate the neurological dysfunction caused by prolonged TDF administration.

Anti-Pseudomonas aeruginosa activity of a C16-terpene dilactone isolated from the endophytic fungus Neofusicoccum luteum of Kigelia africana (Lam.).

Fungal endophytes have the capacity to biosynthesize secondary metabolites that are produced by their host plants. In this study, a dilactone terpenoid of C16 architecture was isolated from the fungal endophytes of Kigelia africana, in our attempt to identify anti-Pseudomonas aeruginosa metabolites. Thirty-eight fungal isolates were cultured for biomolecule production over a period of thirty days. Extracts from three (ZF 34, ZF 52 and ZF 91) of the fungi showed good anti-P. aeruginosa activity, with ZF 52 presenting the best MIC of 19.53 µg/mL and was accordingly subjected to chromatographic separation. Based on nuclear magnetic resonance (NMR) spectroscopy, high resolution mass spectrometry and single crystal X-ray diffraction (XRD) analyses, the isolated compound was identified as a C16-terpene dilactone, with a structure consistent with that of the known diterpene, CJ-14445. The isolated dilactone showed anti-P. aeruginosa activity with MIC of 0.61 µg/mL, signifying the antibacterial potential of the biomolecule. The bioactive fungal isolate (ZF 52) was identified as Neofusicoccum luteum based on genomic DNA sequencing. This is the first report of the endophyte N. luteum from K. africana and the first reported occurrence of CJ-14445 in the fungus.

Unravelling the drugability of MSI2 RNA recognition motif (RRM) protein and the prediction of their effective antileukemia inhibitors from traditional herb concoctions.

MSI2 is a homolog 2 of the Musashi RNA binding proteins (MSI) and is known to contribute to acute myeloid leukaemia (AML) and expressed up to 70% in AML patients. High expression of MSI2 has been found to lead to the lower overall survival of patients with AML. This study proposed the potential antagonists of MSI2 RNA-recognition motifs (MSI2 RRM1) derived from the LC-MS analysis of three traditional herbal samples. The LC-MS analysis of the three traditional herbs concoctions yields a total of 271 unique molecules of which 262 were screened against MSI2 RRM1 protein. After the dynamic study of the selected 8 top molecules from the virtual screening, the five most promising ligands emerged as potential MSI2 antagonists compare to the reference experimental molecule. The results show that the dynamic of MSI2 RRM1 protein is accompanied by a rare even of protein chain dissociation and re-association as evident in both the bound and unbound state of the protein. The unbound protein experience earlier chain dissociation compare to ligand-bound protein indicating that ligand binding to the protein slows down the dissociation time but thereafter increases the frequency of alternation between the protein chain association and dissociation after the first experience. Interestingly, the re-association of the protein chain is also accompanied by full restoration of the ligands to the binding site. The drug candidate Methotrexate (M3) and rescinnamine (M9) are listed among the promising antagonist of MSI2 with unique properties compared to a less promising molecule Ergotamine (M6).Communicated by Ramaswamy H. Sarma.

The effect of hesperidin and luteolin isolated from Eriocephalus africanus on apoptosis, cell cycle and miRNA expression in MCF-7.

This study investigates the molecular mechanisms underlying the anticancer activity of hesperidin and luteolin, isolated from Eriocephalus africanus, in the human breast carcinoma cell line (MCF-7). The viability of MCF-7 cells, upon treatment with hesperidin and luteolin, was evaluated using the 3-[4,5-dimethylthiazole-2-yl]-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assay; apoptotic activity and effect on cell cycle progression were analysed by flow cytometry; effect on expression of key apoptotic regulatory genes (caspase-3, -8, -9, Bcl-2 and Bax) and apoptotic microRNAs (-16, -21 and -34a) were evaluated using quantitative real-time PCR. Hesperidin and luteolin reduced cell viability in a dose and time-dependent manner, caused a significant accumulation of apoptotic cells into the G0/G1 and sub-G1 cell cycle phases, induced apoptosis through the intrinsic and extrinsic pathways, down-regulated anti-apoptotic, Bcl-2, and upregulated pro-apoptotic, Bax. In addition, hesperidin and luteolin significantly downregulated the expression of miR-21 and upregulated that of miR-16 and -34a in MCF-7. Spearman`s rank analysis revealed a positive correlation between Bcl-2 and miR-21 and negative correlation between Bcl-2, miR-16 and -34a. Findings from this study provide new evidence on the molecular basis of the anticancer activity of luteolin and hesperidin in breast cancer cell lines.Communicated by Ramaswamy H. Sarma.

Highly active antiretroviral therapy conjugated silver nanoparticle ameliorates testicular injury in type-2 diabetic rats.

Despite advances in managing human immunodeficiency virus (HIV) infection and success in the treatment prognosis using highly active antiretroviral therapy (HAART). The clinical efficacy of this regimen has been associated with increased adverse effects such as metabolic derangements and reproductive dysfunctions. These adverse effects necessitate a nanoparticle delivery vehicle like silver nanoparticles (AgNPs), a multi-functional drug delivery system, to transport the HAART to the viral reservoir site like testis. This study was therefore designed to evaluate the effects of HAART loaded AgNPs (HAART-AgNPs) on testicular oxidative stress markers, an inflammatory biomarker, and histomorphology in a rat model of diabetes. Thirty-six adult male Sprague-Dawley rats were randomly divided into two groups (n = 18) non-diabetic and fructose-streptozotocin (Frt-STZ) induced type 2 diabetes (T2DM). Thereafter, both groups were subdivided into three (n = 6) and treated with distilled water, HAART and HAART-AgNPs. HAART-AgNPs caused a significant increase (p < 0.05) in catalase (23.43 ± 0.92) level vs diabetic control (16.95 ± 1.04). Also, HAART-AgNP caused a significant reduction (p < 0.05) in malondialdehyde, interleukin-6 and blood glucose levels (1.94 ± 0.06, 93.65 ± 3.6, 287.33 ± 22.85 respectively), compared to their respective diabetic control values (2.18 ± 0.12, 143.4 ± 9.2, 372.16 ± 23.16). Furthermore, HAART-AgNPs mitigated tubular atrophy, basement membrane thickening, interstitial distension, fibrous elemental distortion and peri-interstitial tissue alterations in the testis of diabetic rats. The results from this study showed that administration of HAART-AgNPs to diabetic rats reduced testicular inflammation, improved glycaemic control, antioxidant status, and testicular histology. Therefore, conjugation of AgNP with HAART may cater for the reproductive dysfunction during the management of HIV infection.

Hesperidin-loaded nanoemulsions improve cytotoxicity, induce apoptosis, and downregulate miR-21 and miR-155 expression in MCF-7.

Hesperidin, a ubiquitous plant-based flavanone, was encapsulated into nanoemulsions (HP-NEM) using a spontaneous emulsification method to improve its solubility and enhance bioavailability and efficacy in breast cancer treatment using MCF-7 cell lines. The cytotoxic and apoptotic effects of HP-NEM against MCF-7 and its impact on oncomiRs, microRNA-21, and microRNA-155 expression were also assessed. The optimised HP-NEM displayed a spherical shape with 305 ± 40.8 nm, 0.308 ± 0.04, and -11.6 ± 3.30 mV and 93 ± 0.45% for particle size, polydispersity index (PDI), zeta-potential (ζ), and encapsulation efficiency, respectively. Cytotoxicity studies using MTT assay showed selective toxicity of the HP-NEM against MCF-7 without affecting normal cells (HEK 293). Treatment with the HP-NEM induced cell death through apoptosis, cell cycle arrest in the G2/M phase, and downregulated miR-21 and miR-155 expression in MCF-7. This study supports the use of HP-NEM as a potential therapeutic agent in breast cancer treatment.

Elemental analysis of soils along the South African National Road (N3) - a combined approach including statistics, pollution indicators, and geographic information system (GIS).

The South African National Road (N3) in the KwaZulu-Natal province is one of the major transportation routes from the Durban harbor. In this study, metal concentrations in Bidens pilosa L., which grows alongside the N3, and soil were determined using inductively coupled plasma - optical emission spectrometry to evaluate the impact of soil quality on the uptake. Furthermore, the distribution of Pb and Cd was mapped using the geographic information system (GIS) approach to identify the potential benefits of spatial data applications in soil studies. Plant concentrations of toxic metals, especially Pb, were high and were linked to high soil concentrations. The target hazard quotients indicated a low risk of adverse effects due to Cd exposure and increased risk due to As and Pb exposure. The carcinogenic risk was high for As and Cd exposure at all sites and Pb at 40% of the sites. Soil quality indicators (geoaccumulation indices and enrichment factors) showed soils to be moderate to heavily contaminated. Principal component analysis indicated different anthropogenic sources of contamination, including vehicular emissions and a combination of industrial, agricultural, and social impacts. Kriging interpolation depicted the spatial diffusion of Cd and Pb concentrations throughout the study area with different hot-spot areas of metal contamination for these two metals. The study demonstrated that the plants growing along national roads are not suitable for human consumption.

Determination of heavy metals in selected fish species and seawater from the South Durban Industrial Basin, KwaZulu-Natal, South Africa.

The South Durban Industrial Basin (SDIB), South Africa, an economic hub that spans a long coastline, is a disaster management hotspot, which threatens the sustainability of the fishing industry in this region. This study investigated the elemental concentrations in fish and seawater from a mini-ecosystem in the SDIB, to determine if a direct relationship exists between these two matrices, and to assess for metal toxicities. The results showed As and Cr to be above the maximum permissible limits (MPLs) of the World Health Organization (WHO) for all fish species (blacktail, karanteen, five finger, mullet, and pompano), while fish from Isipingo Beach exceeded the WHO MPLs for Pb, As, and Cr. Fish did not display signs of metal toxicity indicating either a harmless form of metals or high tolerance levels. Typical concentrations of metals in seawater (mg L-1) at (Isipingo Beach, Cuttings Beach, and Amanzimtoti Beach) were found to be for Al (3, 2.7, and 16.4), As (0.17, 0.11, and 0.19), Cr (0.16, 0.17, and 0.23), Cu (0.15, 0.13, and 0.24), Fe (2.7, 3.45, and 33.9), and Zn (2, 2.1, and 2.12). Except for As, estimated daily intakes, target hazard quotients, and carcinogenic risks indicated no associated health risks due to consumption of the fish from the SDIB. However, due to target hazard quotients and carcinogenic risks for As being above 4 and 0.0001, respectively, fish from the SDIB should be consumed in moderation or not consumed to prevent long-term toxic effects of As.

Phytochemical constituents and in vitro anticancer screening of isolated compounds from Eriocephalus africanus‡.

This study investigated the in vitro anticancer potential of phytochemical constituents isolated from the methanolic extract of Eriocephalus africanus. One flavanone (hesperidin) and two flavones (luteolin and apigenin) were isolated for the first time from the plant using column chromatography. Standard MTT assay was used to evaluate the effect of the constituents on cell viability in MCF-7, A549, HepG2 and normal HEK 293 cell lines. The flavonoids decreased cell viability in a dose dependent manner in all tested cell lines. Hesperidin and luteolin were more sensitive against MCF-7, with EC50 values of 62.57 µg/mL and 70.34 µg/mL, respectively and apigenin showed the most potent activity against HepG2 (EC50 = 11.93 µg/mL). The results revealed E. africanus to be a rich source of flavonoids and natural anticancer agents, which could potentially be used in the development of new therapeutics for cancer treatment.

Phytochemical profile and in vitro antioxidant activity of Emelia M (EMB), Mshikazi and Delosma H herbal medicines as demonstrated in THP-1 and Jurkat leukaemia cell lines.

Background: Three decoctions, namely Emelia M (EMB), Mshikazi and Delosma H are used by traditional health practitioners in KwaZulu-Natal, South Africa to treat and manage leukaemia and related conditions. Objectives: This study evaluated the in vitro antioxidant activity and phytochemical profile of the aqueous extracts of Emelia M (EMB), Mshikazi and Delosma H decoctions. Methods: Antioxidant activity of the extracts was evaluated using1-diphenyl-2-picrylhydrazyl (DPPH), glutathione (GSH), phosphomolybdate and thiobarbituric acid reactive substance (TBARS) assays. Phytochemical screening was used to determine the presence of compounds. Results: The DPPH radical scavenging activity was similar to ascorbic acid for EMB and Delosma H, but not for Mshikazi. At 24 h, EMB increased GSH in both THP-1 and Jurkat cells similar to Delosma H while Mshikazi demonstrated the lowest activity. At 48 h, EMB and Delosma H revealed increased GSH in THP-1 cells with no significant decrease in GSH levels in Jurkat cells. However, EMB showed the lowest lipid peroxidation activity compared to Delosma H and Mshikazi after 24 h treatment of both cells. Phenols, flavonoids, terpenoids, saponins were present in all extracts. Conclusion: Extracts of the three decoctions possess both antioxidant and prooxidant properties through high scavenging activity and increased in lipid peroxidation.

Antiulcerogenic effects of Celosia trigyna plant extracts on ethanol-induced gastric ulcer in adult Wistar rats.

BACKGROUND AND AIM: Gastric ulcer is a chronic disease and serious health issue. Celosia trigyna is a medicinal plant used traditionally for wound healing. This study aimed to isolate the bioactive compounds from Celosia trigyna and to investigate the in vitro and in vivo anti-ulcerogenic effects of the extracts on ethanol-induced gastric ulcer on adult Wistar rats to determine their regenerative potential. EXPERIMENTAL PROCEDURE: Seven groups (A - negative control, B - vehicle control, C, D, E, F and G - positive control, n = 5) of five adult Wistar rats received treatment for ethanol-induced gastric ulcer. RESULTS AND CONCLUSION: Phytochemical analysis led to the isolation of chondrillasterol, lutein, pheophytin a and chondrillasterol acetate. The in vitro results showed dichloromethane and hexane extracts to have maximum chymotrypsin inhibition relative to the standard (chymostatin) while in vivo results showed a significant increase in ulcer parameters of the vehicle control relative to groups treated with plant extracts (P < 0.05). Ulcer parameters and DNA density in groups treated with dichloromethane and hexane extracts were comparable to the negative control. Gross and histopathological findings confirmed gastric mucosa lesions in the vehicle control. There were mild ulcerations in groups treated with the ethyl acetate and methanol extracts with no observable ulcerations in the groups treated with dichloromethane and hexane extracts as the histoarchitectural outlines do not show any form of necrosis, distortion or cellular vacuolation. It was concluded that non-polar, hydrophobic compounds are able to remediate the degree of ulceration but not polar compounds.

Nutritional value, antioxidant and antidiabetic properties of nettles (Laportea alatipes and Obetia tenax).

Nettles are commonly consumed in South Africa, Europe and Asia and are used in traditional medicine to treat a variety of ailments. In this study, the nutritional value of the leaves of nettles (Laportea alatipes and Obetia tenax) was evaluated and compared, when cooked and uncooked. The results showed a decrease in the concentrations of crude protein, vitamin A, vitamin E and metals after cooking of nettles. Although cooking reduced the concentrations of essential elements in nettles, their contribution to the diet remained adequate. L. alatipes presented with reduced levels of Cd (from 1.86 to 0.810 mg kg-1) and Pb (from 2.87 to 1.88 mg kg-1) after cooking. Similarly, Cd (from 2.97 to 0.780 mg kg-1) and Pb (from 2.21 to 0.795 mg kg-1) levels in O. tenax decreased after cooking, demonstrating the significance of cooking. The antioxidant activity of the nettles was determined using the 2,2-diphenyl-l-picrylhydrazyl (DPPH) free radical and ferric reducing antioxidant power (FRAP) assays. The methanol extract of Obetia tenax showed high ferric reducing power whilst the radical scavenging activity was due to the presence of the bioactive molecule, ß-carotene, in the plants which exhibited higher DPPH radical scavenging ability relative to test samples and standards. The in vitro antidiabetic activity of the extracts and compounds from the nettles was better than or comparable to that of the known standard, acarbose, which underscores the prospective antidiabetic properties of nettles. Overall, our study provides scientific validation for the ethno-medicinal use of nettles and supports their consumption, which highlights their potential as nutraceuticals.