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Abstract South Africa was the most affected country in Africa by the coronavirus disease 2019 (COVID-19) pandemic, where over 4 million confirmed cases of COVID-19 and over 102,000 deaths have been recorded since 2019. Aside from clinical methods, artificial intelligence (AI)-based solutions such as machine learning (ML) models have been employed in treating COVID-19 cases. However, limited application of AI for COVID-19 in Africa has been reported in the literature. This study aimed to investigate the performance and interpretability of several ML algorithms, including deep multilayer perceptron (Deep MLP), support vector machine (SVM) and Extreme gradient boosting trees (XGBoost) for predicting COVID-19 mortality risk with an emphasis on the effect of cross-validation (CV) and principal component analysis (PCA) on the results. For this purpose, a dataset with 154 features from 490 COVID-19 patients admitted into the intensive care unit (ICU) of Tygerberg Hospital in Cape Town, South Africa, during the first wave of COVID-19 in 2020 was retrospectively analysed. Our results show that Deep MLP had the best overall performance (F1 = 0.92; area under the curve (AUC) = 0.94) when CV and the synthetic minority oversampling technique (SMOTE) were applied without PCA. By using the Shapley Additive exPlanations (SHAP) model to interpret the mortality risk predictions, we identified the Length of stay (LOS) in the hospital, LOS in the ICU, Time to ICU from admission, days discharged alive or death, D-dimer (blood clotting factor), and blood pH as the six most critical variables for mortality risk prediction. Also, Age at admission, Pf ratio (PaO2/FiO2 ratio), troponin T (TropT), ferritin, ventilation, C-reactive protein (CRP), and symptoms of acute respiratory distress syndrome (ARDS) were associated with the severity and fatality of COVID-19 cases. The study reveals how ML could assist medical practitioners in making informed decisions on handling critically ill COVID-19 patients with comorbidities. It also offers insight into the combined effect of CV, PCA, and SMOTE on the performance of ML models for COVID-19 mortality risk prediction, which has been little explored.

Rooibos tea, traditionally consumed by Indigenous populations, is naturally caffeine-free and contains unique polyphenols with strong antioxidant, anti-inflammatory and anti-hyperglycaemic properties. As such, a systematic review was conducted following PRISMA 2020 guidelines (PROSPERO ID: CRD42023467829) to evaluate the potential association between rooibos tea consumption and health outcomes. Relevant articles were searched from journal inception until October 2024 using five electronic databases (CINAHL, MEDLINE, Scopus, Web of Science Core Collection and Google Scholar) and one register (Cochrane Clinical Register of Controlled Trials). Included studies involved consumption of any rooibos tea beverage or supplement in humans 18 years or older and reported any health outcomes measured pre- and post-intervention. Following article screening and full text review, eight studies (175 participants) fulfilled the inclusion criteria and investigated the effects of rooibos consumption on biological [blood (n = 6); urine (n = 1)] and physiological [heart metrics (n = 2); muscle strength (n = 1)] health markers. Based on the included studies, the findings suggest benefits of rooibos consumption, particularly related to cardiometabolic health, with five studies supporting significant (p < 0.05) results. However, there is insufficient evidence to support the health benefits of rooibos consumption given the limited studies meeting inclusion criteria, the narrow scope of markers assessed and interstudy heterogeneity.

Background COVID-19 vaccines offer different levels of immune protection but do not provide 100% protection. Vaccinated persons with pre-existing comorbidities may be at an increased risk of SARS-CoV-2 breakthrough infection or reinfection. The aim of this study is to identify the critical variables associated with a higher probability of SARS-CoV-2 breakthrough infection using machine learning. Methods A dataset comprising symptoms and feedback from 257 persons, of whom 203 were vaccinated and 54 unvaccinated, was used for the investigation. Three machine learning algorithms – Deep Multilayer Perceptron (Deep MLP), XGBoost, and Logistic Regression – were trained with the original (imbalanced) dataset and the balanced dataset created by using the Random Oversampling Technique (ROT), and the Synthetic Minority Oversampling Technique (SMOTE). We compared the performance of the classification algorithms when the features highly correlated with breakthrough infection were used and when all features in the dataset were used. Result The results show that when highly correlated features were considered as predictors, with Random Oversampling to address data imbalance, the XGBoost classifier has the best performance (F1 = 0.96; accuracy = 0.96; AUC = 0.98; G-Mean = 0.98; MCC = 0.88). The Deep MLP had the second best performance (F1 = 0.94; accuracy = 0.94; AUC = 0.92; G-Mean = 0.70; MCC = 0.42), while Logistic Regression had less accurate performance (F1 = 0.89; accuracy = 0.88; AUC = 0.89; G-Mean = 0.89; MCC = 0.68). We also used Shapley Additive Explanations (SHAP) to investigate the interpretability of the models. We found that body temperature, total cholesterol, glucose level, blood pressure, waist circumference, body weight, body mass index (BMI), haemoglobin level, and physical activity per week are the most critical variables indicating a higher risk of breakthrough infection. Conclusion These results, evident from our unique data source derived from apparently healthy volunteers with cardiovascular risk factors, follow the expected pattern of positive or negative correlations previously reported in the literature. This information strengthens the body of knowledge currently applied in public health guidelines and may also be used by medical practitioners in the future to reduce the risk of SARS-CoV-2 breakthrough infection.

Abstract Chronic psychosocial stress is implicated in the onset and progression of noncommunicable diseases, and mechanisms underlying this relationship include alterations to the intracellular redox state. However, such changes are often investigated in isolation, with few studies adopting a system level approach. Here, male Wistar rats were exposed to 9.5 weeks of chronic unpredictable mild stress and redox status assays were subsequently performed on cardiac, hepatic, and brain tissues versus matched controls. The stressed rats displayed an anxious phenotype, with lowered plasma corticosterone levels (p = 0.04 vs. Controls) and higher plasma epinephrine concentrations (p = 0.03 vs. Controls). Our findings showed organ‐specific redox profiles, with stressed rats displaying increased myocardial lipid peroxidation (p = 0.04 vs. Controls) in the presence of elevated nonenzymatic antioxidant capacity (p = 0.04 vs. Controls). Conversely, hepatic tissues of stressed rats exhibited lowered nonenzymatic antioxidant capacity (p

Cardiovascular diseases (CVDs) are considered the predominant cause of death globally. An abnormal increase in biomarkers of oxidative stress and inflammation are consistently linked with the development and even progression of metabolic diseases, including enhanced CVD risk. Coffee is considered one of the most consumed beverages in the world, while reviewed evidence regarding its capacity to modulate biomarkers of oxidative stress and inflammation remains limited. The current study made use of prominent electronic databases, including PubMed, Google Scholar, and Scopus to retrieve information from randomized controlled trials reporting on any association between coffee consumption and modulation of biomarkers of oxidative stress and inflammation in healthy individuals or those at increased risk of developing CVD. In fact, summarized evidence indicates that coffee consumption, mainly due to its abundant antioxidant properties, can reduce biomarkers of oxidative stress and inflammation, which can be essential in alleviating the CVD risk in healthy individuals. However, more evidence suggests that regular/prolonged use or long term (>4 weeks) consumption of coffee appeared to be more beneficial in comparison with short-term intake (

The consumption of food-derived products, including the regular intake of pepper, is increasingly evaluated for its potential benefits in protecting against diverse metabolic complications. The current study made use of prominent electronic databases including PubMed, Google Scholar, and Scopus to retrieve clinical evidence linking the intake of black and red pepper with the amelioration of metabolic complications. The findings summarize evidence supporting the beneficial effects of black pepper (Piper nigrum L.), including its active ingredient, piperine, in improving blood lipid profiles, including reducing circulating levels of total cholesterol, low-density lipoprotein cholesterol, and triglycerides in overweight and obese individuals. The intake of piperine was also linked with enhanced antioxidant and anti-inflammatory properties by increasing serum levels of superoxide dismutase while reducing those of malonaldehyde and C-reactive protein in individuals with metabolic syndrome. Evidence summarized in the current review also indicates that red pepper (Capsicum annum), together with its active ingredient, capsaicin, could promote energy expenditure, including limiting energy intake, which is likely to contribute to reduced fat mass in overweight and obese individuals. Emerging clinical evidence also indicates that pepper may be beneficial in alleviating complications linked with other chronic conditions, including osteoarthritis, oropharyngeal dysphagia, digestion, hemodialysis, and neuromuscular fatigue. Notably, the beneficial effects of pepper or its active ingredients appear to be more pronounced when used in combination with other bioactive compounds. The current review also covers essential information on the metabolism and bioavailability profiles of both pepper species and their main active ingredients, which are all necessary to understand their potential beneficial effects against metabolic diseases.

Chromatographic fractionation of a methanol extract of Helichrysum rutilans afforded seven known compounds. The isolated compounds were identified as 5,7,8-trihydroxy-3,6-dimethoxyflavone-8-O-2-methyl-2-butanoate (C-1), 5,7-dihydroxy-3,6,8-trimethoxyflavone (C-2), 5-hydroxy-3,6,7,8-tetramethoxyflavone (C-3), 5-hydroxy-3,6,7-trimethoxyflavone (C-4), ent-kaurenoic acid (C-5), ent-kauran-18-al (C-6), and 15-α-hydroxy-(-)-ent-kaur-16-en-19-oic acid (C-7). Compounds C-1–C-4 demonstrated high antioxidant capacities on ORAC hydroxyl radical (2.114 ± 4.01; 2.413 ± 6.20; 1.924 ± 16.40; 1.917 ± 3.91) × 106; ORAC peroxyl radical (3.523 ± 3.22; 2.935 ± 0.13; 2.431 ± 8.63; 2.814 ± 5.20) × 103 µMTE/g; and FRAP (1251.45 ± 4.18; 1402.62 ± 5.77) µMAAE/g, respectively. Moderate inhibitory activities against Fe2+-induced lipid peroxidation were observed for C-1–C-4 as IC50 values of 13.123 ± 0.34, 16.421 ± 0.92, 11.64 ± 1.72, 14.90 ± 0.06 µg/mL, respectively, while their respective anti-tyrosinase activities with IC50 values of 25.735 ± 9.62, 24.062 ± 0.61, 39.03 ± 13.12, 37.67 ± 0.98 µg/mL were also observed. All compounds demonstrated TEAC values within the range of 1105–1424 µMTE/g. The result is an indication that a methanol extract of H. rutilans might possibly be a good source of natural antioxidants against ailments caused by cellular oxidative stress and as inhibitors against skin depigmentation, as well as possible raw materials needed for slowing down perishable agricultural products. This is the first report on the phytochemical and biological evaluation of H. rutilans.

This article presents the potential health benefits of Rooibos to be considered a support during the COVID-19 pandemic. The recent pandemic of COVID-19 has led to severe morbidity and mortality. The highly infectious SARS-CoV-2 is known to prime a cytokine storm in patients and progression to acute lung injury/acute respiratory distress syndrome. Based on clinical features, the pathology of acute respiratory disorder induced by SARS-CoV-2 suggests that excessive inflammation, oxidative stress, and dysregulation of the renin angiotensin system are likely contributors to the COVID-19 disease. Rooibos, a well-known herbal tea, consumed for centuries, has displayed potent anti-inflammatory, antioxidant, redox modulating, anti-diabetic, anti-cancer, cardiometabolic support and organoprotective potential. This article describes how Rooibos can potentially play a supportive role by modulating the risk of some of the comorbidities associated with COVID-19 in order to promote general health during infections.

Helichrysum species are prominent South African medicinal plants. From the essential oils (EOs) of three Helichrysum species, H. petiolare, H. odoratissimum, and H. cymosum, sixty-three constituent components were identified, with hydrocarbons and oxygenated monoterpenes and sesquiterpenes as major components. The compounds were analyzed by gas chromatography-mass spectrometry (GC-MS) and nuclear magnetic resonance (NMR) spectroscopy. In H. petiolare EO, the major components were faurinone (20.66%) and (E)-β-ocimene (17.21%). Faurinone was isolated from this EO for the first time. In H. odoratissimum, 1,8-cineole (17.44%) and α-pinene, and γ-curcumene (15.76%) were the major components whereas, in H. cymosum, α-pinene (29.82%) and (E)-caryophyllene (19.20%) were the major components. In the antibacterial activity study, the EOs were tested against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa. The EOs were found to possess low antibacterial, anti-tyrosinase, and photoprotection activities and moderate antioxidant capacities, thus establishing these Helichrysum EOs as valuable antioxidant agents.

Lipopolysaccharide (LPS), a well-conserved cell wall component of Gram positive bacteria, exerts its toxic effects via inducing oxidative and pro-inflammatory responses. Red palm oil (RPO) is a unique natural product with a balanced ratio of saturated and unsaturated fatty acids, with reported antioxidant and anti-inflammatory effects. In this study, we assess the protective effect and mechanistic action of RPO using a lipopolysaccharide (LPS)-induced hepatic injury model. Male Wistar rats were assigned into four groups (10 animals/group): normal control (NC), RPO, LPS and RPO + LPS. Animals in the RPO and RPO + LPS groups were administered RPO (200 μL/day) for 28 days. On the 27th day of experiment, animals in LPS and RPO + LPS groups were injected with LPS (0.5 mg/kg body weight). Animals were sacrificed 24 h later, and blood and liver tissues harvested for biochemical and molecular analysis. RPO resolved hepatic histological dysfunction induced by LPS, and lowered alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase and γ-glutamyl transferase activities in the serum. Hepatic malondialdehyde and conjugated dienes, as well as pro-inflammatory cytokines, including interleukin (IL)-1β, IL-6 and TNFα were significantly diminished (p < 0.05) by RPO pre-treatment. Activity of hepatic antioxidant enzymes including superoxide dismutase, glutathione reductase, glutathione peroxidase, as well as glutathione redox status (GSH:GSSG), and markers of antioxidant capacity that decreased as a result of LPS injection were improved by RPO pre-treatment. Mechanistically, RPO up-regulated mRNA expression of redox sensitive transcription factor Nrf2 and its downstream targets GCL and HO-1, while also suppressing the expression of NFκβ and associated inflammatory protein, Iκβ kinase (IκKβ). In conclusion, this study highlights the ameliorating effects of RPO against LPS-induced hepatic injury and revealed the Nrf2/GCL/HO-1 and NFκβ signaling axis as potential contributing mechanisms.

Diabetes mellitus (DM) is a group of systemic metabolic disorders with a high rate of morbidity and mortality worldwide. Due to the detrimental side effects of the current treatment, there is a great need to develop more effective antidiabetic drugs with fewer side effects. Natural products are a well-known source for the discovery of new scaffolds for drug discovery, including new antidiabetic drugs. The genus Helichrysum has been shown to produce antidiabetic natural products. In this investigation, the methanolic extract of H. cymosum and H. pandurifolium resulted in the isolation and identification of eleven known compounds viz 5,8-dihydroxy-7-methoxy-2-phenyl flavanone (1), pinostrobin (2), dihydrobaicalein (3), glabranin (4), allopatuletin (5), pinostrobin chalcone (6), helichrysetin (7), 5-hydroxy-3,7-dimethoxyflavone (8), 3,5-dihydroxy-6,7,8-trimethoxyflavone (9), 3-O-methylquercetin (10), and 3-methylethergalangin (11). The in vitro bio-evaluation of isolated compounds against alpha-glucosidase showed that 10, 5, and 11 demonstrated the highest alpha-glucosidase inhibitory activity with IC50 values of 9.24 ± 0.4, 12.94 ± 0.2, and 16.00 ± 2.4 μM respectively, followed by 7 and 3 with IC50 values of 18.16 ± 1.2 and 44.44 ± 0.2 μM respectively. However, none of these compounds showed a measurable inhibitory effect on alpha-amylase under the experimental conditions used except compound 10 which showed a poor alpha-amylase inhibitory activity with an IC50 value of 230.66 ± 15.8 μM. Additionally, strong total antioxidant capacities were demonstrated by 10, 5 and 7 in ferric-ion reducing antioxidant power assay (374.34 ± 69.7; 334.37 ± 1.7; 279.93 ± 0.8) µmol AAE/mmol. This is the first scientific report to be carried out on alpha-glucosidase inhibitory activities and antioxidant capacities of H. cymosum constituents and a first report on the isolation and identification of methoxyflavanoids from H. pandurifolium. Our findings suggest that these compounds are promising candidates to inhibit alpha-glucosidase as well as oxidative stress related to diabetes. Results from molecular docking provided insight into the observed in vitro alpha-glucosidase inhibitory activities for 5, 7, 10, and 11. It is envisaged that the isolated phytochemicals from these plants may contribute to the development of hypoglycemic lead compounds with anti-diabetic potential.

Shortage in insulin secretion or degradation of produced insulin is the principal characteristic of the metabolic disorder of diabetes mellitus (DM). However, because the current medications for the treatment of DM have many detrimental side effects, it is necessary to develop more effective antidiabetic drugs with minimal side effects. Alpha-glucosidase and alpha-amylase inhibitors are directly implicated in the delay of carbohydrate digestion. Pharmacologically, these inhibitors could be targeted for the reduction in glucose absorption rate and, subsequently, decreasing the postprandial rise in plasma glucose and the risk for long-term diabetes complications. The main objectives of this research study were to isolate different phytochemical constituents present in the methanolic extract of Plectranthusecklonii and evaluate their alpha-glucosidase and alpha-amylase inhibitory activities and antioxidant capacity. The phytochemical investigation of the methanolic extract of P. ecklonii yielded three known compounds, viz. parvifloron D, F, and G (1–3, respectively). Parvifloron G was isolated for the first time from P. ecklonii. The in vitro bio-evaluation of the methanolic extract of P. ecklonii and its isolated compounds against alpha-glucosidase showed that 3 exhibited moderate inhibitory activity with IC50 values of 41.3 ± 1.2 μg/mL. Molecular docking analysis confirmed the alpha-glucosidase inhibitory activity demonstrated by 3. Additionally, strong antioxidant capacities were demonstrated by 3 and 1 on ORAC (28726.1 ± 8.1; 3942.9.6.6 ± 0.1 µM TE/g), respectively, which were comparable with the reference antioxidant epigallocatechingallate (EGCG). Furthermore, 3 also showed strong activity on TEAC (3526.1 ± 0.6 µM TE/g), followed by 2 (1069.3 ± 2.4 µM TE/g), as well as on FRAP (1455.4 ± 2.0 µM AAE/g). The methanolic extract of P. ecklonii is a rich source of abietane diterpenes with strong antioxidant activities. This is the first scientific report on alpha-glucosidase and alpha-amylase inhibitory activities, molecular docking, and antioxidant capacities of P. ecklonii constituents.

Rooibos is brewed from the medicinal plant Aspalathus linearis. It has a well-established wide spectrum of bio-activity properties, which in part may be attributed to the phenolic antioxidant power. The antioxidant capacity (AOC) of rooibos is related to its total phenolic content (TPC). The relation between TPC and AOC of randomly selected 51 fermented (FR) and 47 unfermented (UFR) rooibos samples was studied after extraction using water and methanol separately. The resulted extracts were assessed using two antioxidant assays, trolox equivalent antioxidant capacity (TEAC) and ferric reducing antioxidant power (FRAP). The results were analyzed using both simple statistical methods and machine learning. The analysis showed different trends of TPC and AOC correlations of FR and UFR samples, depending on the solvent used for extraction. The results of the water extracts showed similar TPC and higher AOC of FR than UFR samples, while the methanolic extracted samples showed higher TPC and AOC of UFR than FR. As a result, the methanolic extracts showed better agreement between TPC and AOC than water extracts. Possible explanations are given for these observed results. Although, the current literature demonstrates direct correlations of the TPC and AOC of rooibos water extracts. This study showed deviation and highlighted the importance of solvent selection and analysis methodology as an important factor in determining the TPC/AOC correlation and subsequently the expectation of the actual health benefits of rooibos herbal tea. In particular, unfermented and fermented samples can be accurately identified on the basis of a combination of assays (any two of TPC, FRAP and TEAC), especially if methanol is the solvent used. Machine learning analysis of assay data provides nearly identical results with classical statistical analytical methods. This is the first report on machine learning analysis and comparison of the TPC and AOC of rooibos herbal tea extracted with methanol and water, and highlights the importance of using methanol as a solvent to evaluate its AOC.

The green chemistry approach has continuously been applied for the synthesis of functional nanomaterials to reduce waste, environmental hazards, and the use of toxic chemicals among other reasons. Bioactive natural compounds have been found great potential in this regard and are used to improve the stability, activity, and biodistribution of metal nanoparticles (MNPs). Aspalathin (ASP) from Aspalathus linearis (rooibos) has a well-defined pharmacological profile and functional groups capable of both reducing and capping agents in the synthesis of metallic nanoparticles (NP). This study provides the first report of the phytomediated synthesis of gold and silver nanoparticles (AuNPs/AgNPs) via ASP and the green rooibos (GR) extract. The study demonstrated a green chemistry approach to the biosynthesis of nanoparticles of GR-AuNPs, ASP-AuNPs, GR-AgNPs, and ASP-AgNPs. The results showed that GR and ASP could act both as reducing and stabilising agents in the formation of crystalline, with different shapes and dispersity of NPs in the ranges of 1.6–6.7 nm for AgNPs and 7.5–12.5 nm for the AuNPs. However, the ASP NPs were less stable in selected biogenic media compared to GR NPs and were later stabilised with polyethene glycol. The cytotoxicity studies showed that GR-AgNPs were the most cytotoxic against SH-SY5Y and HepG2 with IC50 108.8 and 183.4 μg/mL, respectively. The cellular uptake analysis showed a high uptake of AuNPs and indicated that AgNPs of rooibos at a lower dose (1.3–1.5 μg/mL) is favourable for its anticancer potential. This study is a contribution to plant-mediated metallic nanoparticles using a pure single compound that can be further developed for targeted drug delivery for cancer cells treatments in the coming years.

Skin cells suffer continuous damage from chronic exposure to ultraviolet light (UV) that may result in UV-induced oxidative stress and skin thinning. This has necessitated the formulation of cosmeceutical products rich in natural antioxidants and free radical scavengers. Aspalathus linearis (rooibos) is an endemic South African fynbos plant growing naturally in the Western Cape region. The plant is rich in phenolics and other bioactives with a wide spectrum of health benefits. The chemical study of an acetonic extract of green A. linearis afforded a novel compound named linearthin (1) and two known dihydrochalcones, aspalathin (2) and nothofagin (3). The chemical structure of the novel compound was elucidated based on spectroscopic data analysis. The bio-evaluation of the isolated chalcones in vitro for protection against UVB-induced oxidative stress were systematically assessed by examining cell viability, metabolic activity, apoptosis, and cytotoxicity using HaCaT and SK-MEL-1 skin cells models. It was observed that pre-treatment with tested samples for 4- and 24 h at low concentrations were sufficient to protect skin cells from UVB-induced damage in vitro as evidenced by higher cell viability and improved metabolic activity in both keratinocytes (HaCaT) and melanocytes (SK-MEL-1). The results further show that the pre-treatment regimen employed by this study involved some degree of cellular adaptation as evidenced by higher levels of reduced glutathione with a concomitant decrease in lipid peroxidation and lowered caspase 3 activity. Furthermore, compound 1 was most cytoprotective against UVB irradiation of HaCaT cell line (over 24 h) with an IC50 of 282 µg/mL and SK-MEL-1 cell line with IC50 values of 248.3 and 142.6 µg/mL over 4 and 24 h, respectively. On the other hand, HaCaT cells exposed to 2 over 4 h before UVB irradiation showed the highest degree of cytoprotection with an IC50 of 398.9 µg/mL among the four studied samples. These results show that linearthin (1) and the two glycoside dihydrochalcone of A. linearis have the potential to be further developed as antioxidant cosmeceutical ingredients that may protect skin against UVB-induced damage.

The South African medicinal plant Oncosiphon suffruticosum (L.) Källersjö is an important remedy used to treat chronic, respiratory, and skin ailments. From the essential oil (EO) extracted by the hydrodistillation, sixteen constituent components were identified with oxygenated monoterpenes: camphor (31.21%), filifolone (13.98%), chrysanthenone (8.72%), 1,8-cineole (7.85%), and terpinen-4-ol (7.39%) as predominant constituents. In the antibacterial activity study, the EO was found most susceptible against Pseudomonas aeruginosa with an MIC of 6.4 mg/mL; however, it showed the same activity against Staphylococcus aureus and Escherichia coli with an MIC value of 12.8 mg/mL. The sun protecting factor (SPF) of the EO was found to be 2.299 and thus establishing it as a potentially important cosmeceutical for sunscreen applications. This is the first report investigating the essential oil of O. suffruticosum for its chemical composition and skin-related in vitro biological activities viz antibacterial, antioxidant capacity, antityrosinase, and sun protection factor.

Diabetes mellitus (DM) is one of the most dangerous metabolic diseases with a high rate of mortality worldwide. It is well known that insulin resistance and deficiency in insulin production from pancreatic β-cells are the main characteristics of DM. Due to the detrimental side effects of the current treatment, there is a considerable need to develop new effective antidiabetic drugs, especially alpha-glucosidase and alpha-amylase inhibitors with lesser adverse effects. These inhibitors are known to be directly involved in the delay of carbohydrate digestion, resulting in a reduction of glucose absorption rate and, consequently, reducing the postprandial rise of plasma glucose, which can reduce the risk of long-term diabetes complications. Furthermore, natural products are well-known sources for the discovery of new bioactive compounds that can serve as scaffolds for drug discovery, including that of new antidiabetic drugs. The phytochemical investigation of Salvia aurita collected from Hogobach Pass, Eastern Cape Province, South Africa (SA), yielded four known abietane diterpenes namely carnosol (1), rosmanol (2), 7-methoxyrosmanol (3), 12-methoxycarnosic acid (4), and one flavonoid named 4,7-dimethylapigenin (5). Structural characterization of these isolated compounds was conducted using 1 and 2D NMR, in comparison with reported spectroscopic data. These compounds are reported for the first time from S. aurita. The biological evaluation of the isolated compound against alpha-glucosidase exhibited strong inhibitory activities for 3 and 2 with the half maximal inhibitory concentration (IC50) values of 4.2 ± 0.7 and 16.4 ± 1.1 µg/mL respectively, while 4 and 1 demonstrated strong alpha-amylase inhibitory activity amongst the isolated compounds with IC50 values of 16.2 ± 0.3 and 19.8 ± 1.4 µg/mL. Molecular docking analysis confirms the strong inhibitory activity of 3 against alpha-glucosidase. Additionally, excellent antioxidant capacities were displayed by 2, 1, and 3, respectively, with oxygen radical absorbance capacity (ORAC) (25.79 ± 0.01; 23.96 ± 0.01; 23.94 ± 0.02) mM Trolox equivalent (TE)/g; 1 and 2 as ferric-ion reducing antioxidant power (FRAP) (3.92 ± 0.002; 1.52 ± 0.002) mM ascorbic acid equivalent (AAE)/g; 5 and 2 as Trolox equivalent absorbance capacity (TEAC) (3.19 ± 0.003; 2.06 ± 0.003) mM TE/g. The methanolic extract of S. aurita is a rich source of abietane diterpenes with excellent antioxidant and antidiabetic activities that can be useful to modulate oxidative stress and might possibly be excellent candidates for the management of diabetes. This is the first scientific report on the phytochemical isolation and biological evaluation of the alpha-glucosidase and alpha-amylase inhibitory activities of Salvia aurita.

In this study, procyanidin dimers and Leucosidea sericea total extract (LSTE) were employed in the synthesis of silver nanoparticles (AgNPs) and characterized by ultraviolet-visible (UV-Visible) spectroscopy, high-resolution transmission electron microscopy (HRTEM), selected area electron diffraction (SAED), X-ray diffraction (XRD), and dynamic light scattering (DLS) techniques. AgNPs of about 2–7 nm were obtained. DLS and stability evaluations confirmed that the AgNPs/procyanidins conjugates were stable. The formed nanoparticles exhibited good inhibitory activities against the two enzymes studied. The IC50 values against the amylase enzyme were 14.92 ± 1.0, 13.24 ± 0.2, and 19.13 ± 0.8 µg/mL for AgNPs coordinated with LSTE, F1, and F2, respectively. The corresponding values for the glucosidase enzyme were 21.48 ± 0.9, 18.76 ± 1.0, and 8.75 ± 0.7 µg/mL. The antioxidant activities were comparable to those of the intact fractions. The AgNPs also demonstrated bacterial inhibitory activities against six bacterial species. While the minimum inhibitory concentrations (MIC) of F1-AgNPs against Pseudomonas aeruginosa and Staphylococcus aureus were 31.25 and 15.63 µg/mL respectively, those of LSTE-AgNPs and F2-AgNPs against these organisms were both 62.50 µg/mL. The F1-AgNPs demonstrated a better bactericidal effect and may be useful in food packaging. This research also showed the involvement of the procyanidins as reducing and capping agents in the formation of stable AgNPs with potential biological applications.

Cardiometabolic complications such as the metabolic syndrome and Type 2 Diabetes Mellitus (T2DM) are major causes of global morbidity and mortality. As sugar-sweetened beverages (SSBs) are implicated in this process, this study aimed to obtain greater mechanistic insights. Male Wistar rats (~200 g) were gavaged with a local SSB every day for a period of six months while the control group was gavaged with an iso-volumetric amount of water. Experimental dosages were calculated according to the surface area-to-volume ratio and were equivalent to 125 mL/day (in human terms). A proteomic analysis was performed on isolated liver samples and thereafter, markers of endoplasmic reticulum (ER) stress, antioxidant/oxidant capacity, calcium regulation, and mitochondrial functionality were assessed. These data show that SSB consumption resulted in (a) the induction of mild hepatic ER stress; (b) altered hepatic mitochondrial dynamics; and (c) perturbed calcium handling across mitochondria-associated ER membranes. Despite significant changes in markers of ER stress, the antioxidant response and calcium handling (proteomics data), the liver is able to initiate adaptive responses to counteract such stressors. However, the mitochondrial data showed increased fission and decreased fusion that may put the organism at risk for developing insulin resistance and T2DM in the longer term.

Aims: Although there is evidence linking sugar-sweetened beverage (SSB) intake with the development of cardio-metabolic diseases, the underlying mechanisms remain unclear. The current study therefore evaluated the effects of SSB consumption by establishing a unique in-house in vivo experimental model. Main methods: Male Wistar rats were divided into two groups: a) one consuming a popular local SSB (SSB- Jive), and b) a control group (Control-water) for a period of three and six months (n = 6 per group), respectively. Rats were gavaged on a daily basis with an experimental dosage amounting to half a glass per day (in human terms) (SSB vs. water). Cardiac function was assessed at baseline (echocardiography) and following ex vivo ischemia-reperfusion of the isolated perfused working rat heart. Oral glucose tolerance tests and mitochondrial respiratory analyses were also performed. In addition, the role of non-oxidative glucose pathways (NOGPs), i.e. the polyol pathway, hexosamine biosynthetic pathway (HBP) and PKC were assessed. Key findings: These data show that SSB intake: a) resulted in increased weight gain, but did not elicit major effects in terms of insulin resistance and cardiac function after three and six months, respectively; b) triggered myocardial NOGP activation after three months with a reversion after six months; and c) resulted in some impairment in mitochondrial respiratory capacity in response to fatty acid substrate supply after six months. Significance: SSB intake did not result in cardiac dysfunction or insulin resistance. However, early changes at the molecular level may increase risk in the longer term.

Background: Rooibos types and forms and how prepared and flavoured influence the total polyphenol content and total antioxidant capacity (TAC). Aim: To denote an optimal rooibos cup as having the highest total polyphenol content and TAC, considering the different types, forms, preparation methods and flavourings and amounts (Phase 1), and determine the demographic, lifestyle and rooibos consumption characteristics of adult rooibos consumers, and the association of these characteristics with drinking the optimal cup (Phase 2). Setting: Assays: Oxidative Stress Research Centre, Cape Peninsula University of Technology; Consumer survey: George area, South Africa. Method: Phase 1 entailed determining the total polyphenol content (Folin–Ciocalteau method) and TAC (Trolox equivalent antioxidant capacity and ferric-reducing antioxidant power assay) of the prepared rooibos samples. For Phase 2, a developed, pilot tested questionnaire was used to profile adult rooibos consumers. Results: Phase 1: the following samples delivered higher total polyphenol content and TAC: green (type), green leaves and powdered extract (forms), and sample steeped for 10 min or longer (preparation method). The identified optimal cup was sample steeped for 10 min or longer. Phase 2: a total of 308 respondents completed the questionnaire. Few consumed more than one rooibos cup per day (25.3%; n = 78) and the optimal cup (15.9%; n = 49). These latter respondents comprised those who steeped rooibos in a teapot (not a cup or mug) (p < 0.05). Conclusions: The optimal cup was identified as sample steeped for 10 min or longer. The rooibos consumers did not consume it sufficiently, nor steeped it long enough.

Phytochemical investigation of aerial parts of Helichrysum niveum (H. niveum) using different chromatographic methods including semi-preparative HPLC afforded three new (1–3) and six known (4–10) acylphloroglucinols alongside a known dialcohol triterpene (11). The structures of the isolated compounds were characterized accordingly as 1-benzoyl-3 (3-methylbut-2-enylacetate)-phloroglucinol (helinivene A, 1), 1-benzoyl-3 (2S-hydroxyl-3-methylbut-3-enyl)-phloroglucinol (helinivene B, 2), 8-(2-methylpropanone)-3S,5,7-trihydroxyl-2,2-dimethoxychromane (helinivene C, 3), 1-(2-methylbutanone)-4-O-prenyl-phloroglucinol (4), 1-(2-methylpropanone)-4-O-prennyl-phloroglucinol (5), 1-(butanone)-3-prenyl-phloroglucinol (6), 1-(2-methylbutanone)-3-prenyl-phloroglucinol (7), 1-butanone-3-(3-methylbut-2-enylacetate)-phloroglucinol (8), 1-(2-methylpropanone)-3-prenylphloroglucinol (9), caespitate (10), and 3β-24-dihydroxyterexer-14-ene (11). Excellent total antioxidant capacities were demonstrated by helinivenes A and B (1 and 2) when measured as oxygen radicals absorbance capacity (ORAC), ferric-ion reducing antioxidant power (FRAP), trolox equivalent absorbance capacity (TEAC) and including the inhibition of Fe2+-induced lipid peroxidation (IC50 = 5.12 ± 0.90; 3.55 ± 1.92) µg/mL, while anti-tyrosinase activity at IC50 = 35.63 ± 4.67 and 26.72 ± 5.05 µg/mL were also observed for 1 and 2, respectively. This is the first chemical and in vitro biological study on H. niveum. These findings underpin new perspectives for the exploitation of these natural phenolic compounds in applications such as in the natural cosmeceutical and pharmaceutical sectors.

Ten flavonoid-related structures viz. heliteretifolin (1), isoxanthohumol (2), 2',4',6'-trihydroxy-3'-prenylchalcone (3), isoglabranin (4), glabranin (5), 7-methoxy-isoglabranin (6), quercetin (7), 4'-methoxyquercetin (8), 4'-methoxykaempferol (9) and mosloflavone (10) were isolated from a H. teretifolium methanolic extract and identified. One of them (compound 1) is reported for the first time from a natural source, while compounds 6, 8–10 were isolated for the first time from the genus Helichrysum. The total extract of H. teretifolium showed potent antioxidant activity. When tested for total antioxidant capacity compound 3 possesses moderate biological activity compared to 2, which displayed some of the highest TEAC values (4529.01 ± 2.44; 4170.66 ± 6.72) µM TE/g, respectively. Compounds 7 and 8 demonstrated the highest inhibitory activities on Fe2+-induced lipid peroxidation (IC50 = 2.931; 6.449 µg/mL); tyrosinase (8.092; 27.573) and elastase (43.342; 86.548). Additionally, the total antioxidant capacities measured as FRAP (4816.31 ± 7.42; 3584.17 ± 0.54) µM AAE/g, and ORAC for hydroxyl radical (7.265 ± 0.71; 6.779 ± 3.40) × 106 and peroxyl radical (17.836 ± 2.90; 12.545 ± 5.07) × 103 µM TE/g were also observed for compounds 7 and 8, respectively. In conclusion, H. teretifolium total extract represents a rich source of bioactive constituents with potent antioxidant and moderate anti-tyrosinase and anti-elastase activities that can help to avert accumulation of free radicals in the body, and could therefore be good candidates for the prevention and/or treatment of skin-related conditions, such as aging. This is the first scientific report on the chemical and biological profile of H. teretifolium.

In this study, procyanidins fractions of dimers and trimers (F1−F2) from the Leucosidea sericea total extract (LSTE) were investigated for their chemical constituents. The total extract and the procyanidins were employed in the synthesis of gold nanoparticles (Au NPs) and fully characterized. Au NPs of 6, 24 and 21 nm were obtained using LSTE, F1 and F2 respectively. Zeta potential and in vitro stability studies confirmed the stability of the particles. The enzymatic activity of LSTE, F1, F2 and their corresponding Au NPs showed strong inhibitory alpha-amylase activity where F1 Au NPs demonstrated the highest with IC50 of 1.88 µg/mL. On the other hand, F2 Au NPs displayed the strongest alpha-glucosidase activity at 4.5 µg/mL. F2 and F2 Au NPs also demonstrated the highest antioxidant activity, 1834.0 ± 4.7 μM AAE/g and 1521.9 ± 3.0 μM TE/g respectively. The study revealed not only the ability of procyanidins dimers (F1 and F2) in forming biostable and bioactive Au NPs but also, a significant enhancement of the natural products activities, which could improve the smart delivery in future biomedical applications.

The re-investigation of a methanolic extract of Salvia africana-lutea collected from the Cape Floristic Region, South Africa (SA), afforded four new abietane diterpenes, namely 19-acetoxy-12-methoxycarnosic acid (1), 3β-acetoxy-7α-methoxyrosmanol (2), 19-acetoxy-7α-methoxyrosmanol (3), 19-acetoxy-12-methoxy carnosol (4), and two known named clinopodiolides A (5), and B (6), in addition to four known triterpenes, oleanolic, and ursolic acids (7, 8), 11,12-dehydroursolic acid lactone (9) and β-amyrin (10). The chemical structural elucidation of the isolated compounds was determined on the basis of one and two dimensional nuclear magnetic resonance (1D and 2D NMR), high-resolution mass spectrometry (HRMS), ultra violet (UV), fourier transform infrared (IR), in comparison with literature data. The in vitro bio-evaluation against alpha-glucosidase showed strong inhibitory activities of 8, 10, and 7, with the half inhibitory concentration (IC50) values of 11.3 ± 1.0, 17.1 ± 1.0 and 22.9 ± 2.0 µg/mL, respectively, while 7 demonstrated the strongest in vitro alpha-amylase inhibitory activity among the tested compounds with IC50 of 12.5 ± 0.7 µg/mL. Additionally, some of the compounds showed significant antioxidant capacities. In conclusion, the methanolic extract of S. africana-lutea is a rich source of terpenoids, especially abietane diterpenes, with strong antioxidant and anti-diabetic activities that can be helpful to modulate the redox status of the body and could therefore be an excellent candidate for the prevention of the development of diabetes, a disease where oxidase stress plays an important role.