Browsing by Author "Sibuyi, Nicole Remaliah Samantha"
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Item Anticancer and drug-sensitizing activities of gold nanoparticles synthesized from cyclopia genistoides (honeybush) extracts(MDPI, 2023) Sharma, Jyoti Rajan; Sibuyi, Nicole Remaliah Samantha; Fadaka, Adewale OluwaseunSynthesis of gold nanoparticles (AuNPs) using phytochemicals has become tremendously prominent in biomedical applications because of its enhanced bioactivity and biocompatibility. In this study, water extracts from the leaves of Cyclopia genistoides (C. genistoides), commonly known as honeybush (HB), were used to synthesize honeybush gold nanoparticles (HB-AuNPs). The HB water extracts (HBE) served as both reducing and capping agents in the synthesis of HB-AuNPs. The HB-AuNPs were characterized by UV–Vis spectrophotometry, dynamic light scattering (DLS), and transmission electron microscopy (TEM). The cytotoxicity and apoptotic effects of the HBE and HB-AuNPs, alone and in combination with doxorubicin (Dox), were examined against various human cell lines. Spherical-shaped HB-AuNPs with a hydrodynamic diameter range of 63 to 121 nm were produced.Item Aptamer-Based Diagnostic Systems for the Rapid Screening of TB at the Point-of-Care(MDPI, 2021) Darius, Riziki; Sibuyi, Nicole Remaliah Samantha; Oluwaseun, Fadaka AdewaleThe transmission of Tuberculosis (TB) is very rapid and the burden it places on health care systems is felt globally. The effective management and prevention of this disease requires that it is detected early. Current TB diagnostic approaches, such as the culture, sputum smear, skin tuberculin, and molecular tests are time-consuming, and some are unaffordable for low-income countries. Rapid tests for disease biomarker detection are mostly based on immunological assays that use antibodies which are costly to produce, have low sensitivity and stability. Aptamers can replace antibodies in these diagnostic tests for the development of new rapid tests that are more cost effective; more stable at high temperatures and therefore have a better shelf life; do not have batch-to-batch variations, and thus more consistently bind to a specific target with similar or higher specificity and selectivity and are therefore more reliable. Advancements in TB research, in particular the application of proteomics to identify TB specific biomarkers, led to the identification of a number of biomarker proteins, that can be used to develop aptamer-based diagnostic assays able to screen individuals at the point-of-care (POC) more efficiently in resource-limited settings.Item Computational insight of dexamethasone against potential targets of SARS-CoV-2(Taylor and Francis Group, 2022) Fadaka, Adewale Oluwaseun; Sibuyi, Nicole Remaliah Samantha; Madiehe, Abram MadimabeThe health sector has been on the race to find a potent therapy for coronavirus disease (COVID)-19, a diseases caused by severe acute respiratory syndrome coronavirus (SARS-CoV)-2. Repurposed anti-viral drugs have played a huge role in combating the virus, and most recently, dexamethasone (Dex) have shown its therapeutic activity in severe cases of COVID-19 patients. The study sought to provide insights on the anti-COVID-19 mechanism of Dex at both atomic and molecular level against SARSCoV-2 targets. Computational methods were employed to predict the binding affinity of Dex to SARSCoV-2 using the Schrodinger suite (v2020-2). The target molecules and ligand (Dex) were retrieved from PDB and PubChem, respectively. The selected targets were SARS-CoV-2 main protease (Mpro), and host secreted molecules glucocorticoid receptor, and Interleukin-6 (IL-6). Critical analyses such as Protein and ligand preparation, molecular docking, molecular dynamic (MD) simulations, and absorption, distribution, metabolism, excretion (ADME), and toxicity analyses were performed using the targets and the ligand as inputs.Item Development of a receptor targeted nanotherapy using a proapoptotic peptide(University of the Western Cape, 2015) Sibuyi, Nicole Remaliah Samantha; Meyer, Mervin; Madiehe, Abram M.The prevalence of obesity amongst South Africans is alarming, with more than 29% of men and 56% of women considered to be obese. Angiogenesis, a process for development of new blood vessels play a major role in growth and survival of the adipose tissues. Pharmacological inhibitors of angiogenesis are therefore a sensible strategy to reduce excess body weight. Current anti-obesity drugs have limitations because of their lack of selectivity and specificity, which lead to undesirable side effects and reduced drug efficacy. Future anti-obesity therapeutic strategies should be target-specific, with minimal toxicity towards healthy tissues will be more appropriate for obesity treatment. Targeted nano-therapeutic agents are currently being developed to overcome the drawbacks associated with conventional drug therapies. The nano-based delivery vehicles that specifically target diseased cells are appealing as they could reduce drug toxicity towards healthy tissues and be more effective at lower dosages. The main aim of this study was to develop a receptor-mediated nanotherapy that specifically targets the white adipose tissue vasculature and trigger the death of these cells through apoptosis. The 14 nm gold nanoparticles (AuNPs) were synthesized using theTurkevich method following reduction of gold aurate by sodium citrate salt. Different chemistries were used to functionalise the AuNPs for biological application by conjugating with either vascular targeting peptide or pro-apoptotic peptide on their surface or both. The nanomaterials were characterised by UV-Vis, Zeta potential and transmission electron microscopy (TEM). The sensitivity and specificity of various AuNP conjugates were tested in vitro on colon and breast cancer cell lines. A human (Caco-2) cell line that expresses the receptor for the adipose homing peptide was chosen as an in vitro model system. Cellular toxicity and uptake of the nanoparticles was evaluated using the WST-1 assay, Inductively Coupled Plasma-Optical Emission Spectra (ICP-OES) and TEM. The induction of apoptosis following exposure to the nanoparticles was examined by Western blot and flow cytometric analysis. The anti-proliferative activity of the targeted therapeutic nanoparticles on the cells was more pronounced on the cells expressing the receptor for the adipose homing peptide. The uptake of unfunctionalised AuNPs was higher compared to functionalised nanoparticles, but this did not impair cell viability. The activity of the therapeutic peptide was retained and enhanced following conjugation to AuNPs as shown by Western blot and flow cytometric analysis. The nanotherapy under study demonstrated receptor mediated targeting, and enhanced activity on the cells expressing the receptor. However, the therapeutic and efficacy of the targeted nanotherapy still need to be tested in animal models of obesity to confirm the treatment specificity.Item Development of Effective Therapeutic Molecule from Natural Sources against Coronavirus Protease(MDPI, 2021) Fadaka, Adewale Oluwaseun; Sibuyi, Nicole Remaliah Samantha; Martin, Darius Riziki; Klein, AshwilAbstract: The SARS-CoV-2 main protease (Mpro) is one of the molecular targets for drug design. Effective vaccines have been identified as a long-term solution but the rate at which they are being administered is slow in several countries, and mutations of SARS-CoV-2 could render them less effective. Moreover, remdesivir seems to work only with some types of COVID-19 patients. Hence, the continuous investigation of new treatments for this disease is pivotal. This study investigated the inhibitory role of natural products against SARS-CoV-2 Mpro as repurposable agents in the treatment of coronavirus disease 2019 (COVID-19). Through in silico approach, selected flavonoids were docked into the active site of Mpro. The free energies of the ligands complexed with Mpro were computationally estimated using the molecular mechanics-generalized Born surface area (MM/GBSA) method. In addition, the inhibition process of SARS-CoV-2 Mpro with these ligands was simulated at 100 ns in order to uncover the dynamic behavior and complex stability. The docking results showed that the selected flavonoids exhibited good poses in the binding domain of Mpro. The amino acid residues involved in the binding of the selected ligands correlated well with the residues involved with the mechanism-based inhibitor (N3) and the docking score of Quercetin-3-O- Neohesperidoside (−16.8 Kcal/mol) ranked efficiently with this inhibitor (−16.5 Kcal/mol). In addition, single-structure MM/GBSA rescoring method showed that Quercetin-3-O-Neohesperidoside (−87.60 Kcal/mol) is more energetically favored than N3 (−80.88 Kcal/mol) and other ligands (Myricetin 3-Rutinoside (−87.50 Kcal/mol), Quercetin 3-Rhamnoside (−80.17 Kcal/mol), Rutin (−58.98 Kcal/mol), and Myricitrin (−49.22 Kcal/mol). The molecular dynamics simulation (MDs) pinpointed the stability of these complexes over the course of 100 ns with reduced RMSD and RMSF. Based on the docking results and energy calculation, together with the RMSD of 1.98 ± 0.19 Å and RMSF of 1.00 ± 0.51 Å, Quercetin-3-O-Neohesperidoside is a better inhibitor of Mpro compared to N3 and other selected ligands and can be repurposed as a drug candidate for the treatment of COVID-19. In addition, this study demonstrated that in silico docking, free energy calculations, and MDs, respectively, are applicable to estimating the interaction, energetics, and dynamic behavior of molecular targets by natural products and can be used to direct the development of novel target function modulators.Item Differentially expressed serum proteins from obese Wistar rats as a risk factor for obesity-induced diseases(Springer Nature, 2020) Gabuza, Kwazi B.; Sibuyi, Nicole Remaliah Samantha; Mobo, Mmabatho PeggyObesity is a chronic disease that negatively affects life expectancy through its association with life-threatening diseases such as cancer and cardiovascular diseases. Expression proteomics combined with in silico interaction studies are used to uncover potential biomarkers and the pathways that promote obesity-related complications. These biomarkers can either aid in the development of personalized therapies or identify individuals at risk of developing obesity-related diseases. To determine the serum protein changes, Wistar rats were fed standard chow (low fat, LF), or chow formulated high fat (HF) diets (HF1, HF2 and HF3) for 8 and 42 weeks to induce obesity. Serum samples were collected from lean and obese rats at these time points.Item Encapsulation of variabilin in stearic acid solid lipid nanoparticles enhances its anticancer activity in vitro(MDPI, 2020) Lerata, Mookho S.; D’Souza, Sarah; Sibuyi, Nicole Remaliah SamanthaThe use of natural products as chemotherapeutic agents is well established; however, many of these are associated with undesirable side effects, including high toxicity and instability. Furthermore, the development of drug resistant cancers makes the search for new anticancer lead compounds a priority. In this study, the extraction of an Ircinia sp. sponge resulted in the isolation of an inseparable mixture of (7E,12E,20Z)-variabilin (1) and (7E,12Z,20Z)-variabilin (2) and structural assignment was established using standard 1D and 2D NMR experiments. The cytotoxic activity of the compound against three solid tumour cell lines displayed moderate anti-cancer activity through apoptosis, together with a general lack of selectivity among the cancer cell lines studied. Structural assignment and cytotoxic evaluation of variabilin was complicated and further aggravated by its inherent instability. Variabilin was therefore incorporated into solid lipid nanoparticles (SLNs) and the stability and cytotoxic activity evaluated. Encapsulation of variabilin into SLNs led to a marked improvement in stability of the natural product coupled with enhanced cytotoxic activity, particularly against the prostate (PC-3) cancer cell line, with IC50 values of 87.74 µM vs. 8.94 µM for the variabilin alone and Var-SLN, respectively. Both variabilin and Var-SLN revealed comparable activity to Ceramide against the MCF-7 breast cancer cell line, revealing IC50 values of 34.8, 38.1 and 33.6 µM for variabilin, Var-SLN and Ceramide, respectively.Item Enhanced anti-bacterial activity of biogenic silver nanoparticles synthesized from terminalia mantaly extracts(Dove Press, 2019) Majoumouo, Michele Stella; Sibuyi, Nicole Remaliah Samantha; Tincho, Marius BelmondoThe global increase in outbreaks and mortality rates associated with multidrug- resistant (MDR) bacteria is a major health concern and calls for alternative treatments. Natural-derived products have shown potential in combating the most dreadful diseases, and therefore serve as an effective source of bioactive compounds that can be used as antibacterial agents. These compounds are able to reduce metal ions and cap nanoparticles to form biogenic nanoparticles (NPs) with remarkable anti-bacterial activities. This study explores the use of Terminalia mantaly (TM) extracts for the synthesis of biogenic silver NPs (TM-AgNPs) and the evaluation of their antibacterial activity. TM-AgNPs were synthetized by the reduction of AgNO3 with aqueous andmethanolic TM extracts. UV–visible (UV-vis) spectrophotometry, Dynamic Light Scattering (DLS), Transmission Electron Microscopy, and Fourier Transform Infrared (FTIR) analyses were used to characterise the TM-AgNPs. Anti-bacterial activity of the TM extracts and TM-AgNPs was evaluated against eight bacterial strains using the broth microdilution assay.Item Gene expression alterations and molecular analysis of CHEK1 in solid tumors(MDPI, 2020) Fadaka, Adewale Oluwaseun; Bakare, Olalekan Olanrewaju; Sibuyi, Nicole Remaliah SamanthaAlterations in the Checkpoint kinase (CHEK1) gene, its regulation, and the possible clinical outcomes in human solid tumors have not been previously examined. Therefore, the present study was carried out to evaluate the expression of CHEK1 in solid tumors as well as the mechanism by which it can be regulated through non-coding RNAs. The expression of CHEK1 was investigated using Oncomine analysis. cBioPortal, Kaplan–Meier Plotter, and PrognoScan were performed to identify the prognostic roles of this gene in solid tumors. The copy number alteration, mutation, interactive analysis, and visualization of the altered networks were performed by cBioPortal. The molecular binding analysis was carried out by Schrodinger suite, PATCHDOCK, and discovery studio visualizer. The study demonstrated that the CHEK1 gene was differentially expressed in four different cancers, and that reduced CHEK1 mRNA expression is an unfavorable prognostic factor for patients with gastric and colorectal cancer. The molecular docking results showed that the CHEK1 gene can be regulated by microRNAs (miR-195-5p) due to the number of stable hydrogen atoms observed within the distance of 2.0 Å and the favorable amino acids (Ala221, Ile353, Ile365, Ile756, Val797, Val70, Val154, Ile159, Val347, Tyr804, Phe811, Tyr815, and Phe156) identified in the binding pocket of the argonaute protein.Item Gold nanoparticles synthesized using extracts of cyclopia intermedia, commonly known as honeybush, amplify the cytotoxic effects of doxorubicin(MPDI, 2021) Sibuyi, Nicole Remaliah Samantha; Aboyewa, Jumoke A.; Meyer, MervinCyclopia intermedia (C. intermedia) is an indigenous South African shrub used to prepare the popular medicinal honeybush (HB) tea. This plant contains high levels of mangiferin (MGF), a xanthonoid that was reported to have numerous biological activities, including anti-tumor activity. MGF and extracts that contain high concentrations of MGF, such as extracts from Mangifera indica L. or mango have been used to synthesize gold nanoparticles (AuNPs) using green nanotechnology. It has previously been shown that when AuNPs synthesized from M. indica L. extracts are used in combination with doxorubicin (DOX) and Ayurvedic medicine, the anti-tumor effects appear to be augmented. It has also been demonstrated that MGF used in combination with DOX resulted in enhanced anti-tumor effects. In this study, C. intermedia (HB) and MGF were used to synthesize HB-AuNPs and MGF-AuNPs, respectively. The physicochemical properties of the AuNPs were characterized by the UV-Visible Spectroscopy (UV-Vis), dynamic light scattering (DLS), Fourier transform infra-red spectroscopy (FTIR), X-ray diffraction spectroscopy (XRD) and high-resolution transmission electron microscopy (HR-TEM). The cytotoxicity of HB-AuNPs and MGF-AuNPs were assessed on human colon (Caco-2), prostate (PC-3) and glioblastoma (U87) cancer cells; as well as normal breast epithelial (MCF-12A) cells using the MTT assay. Both HB-AuNPs and MGF-AuNPs demonstrated relatively low cytotoxicity in these cells. However, when these nanoparticles were used in combination with DOX, the cytotoxicity of DOX was significantly augmented.Item Green synthesis of metallic nanoparticles using some selected medicinal plants from southern africa and their biological applications(MDPI, 2021) Sibuyi, Nicole Remaliah Samantha; Meyer, Mervin; Aboyewa, J.A.; Oguntibeju, O.O.The application of metallic nanoparticles (MNPs), especially that of silver, gold, cobalt, and zinc as antimicrobial, anticancer, drug delivery, contrast, and bioimaging agents has transformed the field of medicine. Their functions, which are attributed to their physicochemical properties, have gained prominence in various technological fields. Although MNPs can be produced via rigorous physical and chemical techniques, in recent years, a biological approach utilizing natural materials has been developed. With the increasing enthusiasm for safe and efficient nanomaterials, the biological method incorporating microorganisms and plants is preferred over physical and chemical methods of nanoparticle synthesis. Of these bio-entities, plants have received great attention owing to their capability to reduce and stabilize MNPs in a single one-pot protocol. South Africa is home to ~10% of the world’s plant species, making it a major contributor to the world’s ecological scenery. Despite the documented contribution of South African plants, particularly in herbal medicine, very few of these plants have been explored for the synthesis of noble MNPs. This paper provides a review of some important South African medicinal plants that have been utilized for the synthesis of MNPs. The enhanced biological properties of the biogenic MNPs attest to their relevance in medicine. In this endeavor, more of the African plant biodiversity must be explored for the synthesis of MNPs and be validated for their potential to be translated into future nanomedicine. © 2021 by the authors. Licensee MDPI, Basel, Switzerland.Item Heterocyclic (pyrazine)carboxamide Ru(II) complexes: structural, experimental and theoretical studies of interactions with biomolecules and cytotoxicity†(Royal Society of Chemistry, 2024) Tsaulwayo, Nokwanda; Sibuyi, Nicole Remaliah Samantha; Meyer, MervinTreatments of N-(1H-benzo[d]imidazol-2-yl)pyrazine-2-carboxamide (HL1) and N-(benzo[d]thiazol-2-yl)pyrazine-2-carboxamide carboxamide ligands (HL2) with [Ru(p-cymene)Cl2]2 and [Ru(PPh3)3Cl2] precursors afforded the respective Ru(ii) complexes [Ru(L1)(p-cymene)Cl] (Ru1), [Ru(L2)(p-cymene)Cl] (Ru2), [Ru(L1)(PPh3)2Cl] (Ru3), and [Ru(L2)(PPh3)2Cl] (Ru4). These complexes were characterized by NMR, FT-IR spectroscopies, mass spectrometry, elemental analyses, and crystal X-ray crystallography for Ru2. The molecular structure of complex Ru2 contains one mono-anionic bidentate bound ligand and display pseudo-octahedral piano stool geometry around the Ru(ii) atom. The interactions with calf thymus DNA (CT-DNA) and bovine serum albumin (BSA) were investigated by spectroscopic techniques. The experimental binding studies suggest that complexes Ru1-Ru4 interact with DNA, primarily through minor groove binding, as supported by molecular docking results. Additionally, these complexes exhibit strong quenching of the fluorescence of tryptophan residues in BSA, displaying static quenching. The in vitro cytotoxicity studies of compounds Ru1-Ru4 were assessed in cancer cell lines (A549, PC-3, HT-29, Caco-2, and HeLa), as well as a non-cancer line (KMST-6). Compounds Ru1 and Ru2 exhibited superior cytotoxicity compared to Ru3 and Ru4.Item Immunoinformatics design of a novel epitope-based vaccine candidate against dengue virus(Springer, 2021-10) Oluwaseun, Fadaka Adewale; Sibuyi, Nicole Remaliah Samantha; Darius, RizikiDengue poses a global health threat, which will persist without therapeutic intervention. Immunity induced by exposure to one serotype does not confer long-term protection against secondary infection with other serotypes and is potentially capable of enhancing this infection. Although vaccination is believed to induce durable and protective responses against all the dengue virus (DENV) serotypes in order to reduce the burden posed by this virus, the development of a safe and efficacious vaccine remains a challenge. Immunoinformatics and computational vaccinology have been utilized in studies of infectious diseases to provide insight into the host–pathogen interactions thus justifying their use in vaccine development. Since vaccination is the best bet to reduce the burden posed by DENV, this study is aimed at developing a multi-epitope based vaccines for dengue control. Combined approaches of reverse vaccinology and immunoinformatics were utilized to design multi-epitope based vaccine from the sequence of DENV. Specifically, BCPreds and IEDB servers were used to predict the B-cell and T-cell epitopes, respectively. Molecular docking was carried out using Schrödinger, PATCHDOCK and FIREDOCK. Codon optimization and in silico cloning were done using JCAT and SnapGene respectively. Finally, the efficiency and stability of the designed vaccines were assessed by an in silico immune simulation and molecular dynamic simulation, respectively. The predicted epitopes were prioritized using in-house criteria. Four candidate vaccines (DV-1–4) were designed using suitable adjuvant and linkers in addition to the shortlisted epitopes. The binding interactions of these vaccines against the receptors TLR-2, TLR-4, MHC-1 and MHC-2Item Inhibitory potential of repurposed drugs against the SARS-CoV-2 main protease: A computational-aided approach(Taylor and Francis, 2020) Fadaka, Adewale Oluwaseun; Aruleba, Raphael Taiwo; Sibuyi, Nicole Remaliah SamanthaThe exponential increase in cases and mortality of coronavirus disease (COVID-19) has called for a need to develop drugs to treat this infection. Using in silico and molecular docking approaches, this study investigated the inhibitory effects of Pradimicin A, Lamivudine, Plerixafor and Lopinavir against SARS-CoV-2 Mpro. ADME/Tox of the ligands, pharmacophore hypothesis of the co-crystalized ligand and the receptor, and docking studies were carried out on different modules of Schrodinger (2019-4) Maestro v12.2. Among the ligands subjected to ADME/Tox by QikProp, Lamivudine demonstrated drug-like physico-chemical properties. A total of five pharmacophore binding sites (A3, A4, R9, R10, and R11) were predicted from the co-crystalized ligand and the binding cavity of the SARS-CoV-2 Mpro. The docking result showed that Lopinavir and Lamivudine bind with a higher affinity and lower free energy than the standard ligand having a glide score of −9.2 kcal/mol and −5.3 kcal/mol, respectively.Item MicroRNA-based regulation of Aurora A kinase in breast cancer(Impact Journals, 2020) Sibuyi, Nicole Remaliah Samantha; Fadaka, Adewale Oluwaseun; Madiehe, Abram MadimabeThe involvement of non-coding RNAs (ncRNAs) in cellular physiology and disease pathogenesis is becoming increasingly relevant in recent years specifically in cancer research. Breast cancer (BC) has become a health concern and accounts for most of the cancer-related incidences and mortalities reported amongst females. In spite of the presence of promising tools for BC therapy, the mortality rate of metastatic BC cases is still high. Therefore, the genomic exploration of the BC subtype and the use of ncRNAs for possible regulation is pivotal. The expression and prognostic values of AURKA gene were assessed by Oncomine, GEPIA, KM-plotter, and bc-GenExMiner v4.4, respectively. Associated proteins and functional enrichment were evaluated by Cytoscape and DAVID databases. Additionally, molecular docking approach was employed to investigate the regulatory role of hsa-miR-32-3p assisted argonaute (AGO) protein of AURKA gene in BC. AURKA gene was highly expressed in patients with BC relative to normal counterpart and significantly correlated with poor survival. The docking result suggested that AURKA could be regulated by hsa-miR-32-3p as confirmed by the reported binding energy and specific interactions. The study gives some insights into role of AURKA and its regulation by microRNAs through AGO protein. It also provides exciting opportunities for cancer therapeutic intervention. © 2020 Fadaka et al.Item Nanotechnology advances towards development of targeted-treatment for obesity(Journal of Nanobiotechnology, 2019) Sibuyi, Nicole Remaliah SamanthaObesity through its association with type 2 diabetes (T2D), cancer and cardiovascular diseases (CVDs), poses a serious health threat, as these diseases contribute to high mortality rates. Pharmacotherapy alone or in combination with either lifestyle modifcation or surgery, is reliable in maintaining a healthy body weight, and preventing progression to obesity-induced diseases. However, the anti-obesity drugs are limited by non-specifcity and unsustainable weight loss efects. As such, novel and improved approaches for treatment of obesity are urgently needed. Nanotechnology-based therapies are investigated as an alternative strategy that can treat obesity and be able to overcome the drawbacks associated with conventional therapies. The review presents three nanotechnology-based anti-obesity strategies that target the white adipose tissues (WATs) and its vasculature for the reversal of obesity. These include inhibition of angiogenesis in the WATs, transformation of WATs to brown adipose tissues (BATs), and photothermal lipolysis of WATs. Compared to conventional therapy, the targeted-nanosystems have high tolerability, reduced side efects, and enhanced efcacy. These efects are reproducible using various nanocarriers (liposomes, polymeric and gold nanoparticles), thus providing a proof of concept that targeted nanotherapy can be a feasible strategy that can combat obesity and prevent its comorbiditiesItem Nanotechnology-based delivery systems for antimicrobial peptides(MDPI, 2021) Adewale, Oluwaseun Fadaka; Sibuyi, Nicole Remaliah Samantha; Madiehe, Abram Madimabe; Meyer, MervinAntimicrobial resistance (AMR) is a significant threat to global health. The conventional antibiotic pool has been depleted, forcing the investigation of novel and alternative antimicrobial strategies. Antimicrobial peptides (AMPs) have shown potential as alternative diagnostic and therapeutic agents in biomedical applications. To date, over 3000 AMPs have been identified, but only a fraction of these have been approved for clinical trials. Their clinical applications are limited to topical application due to their systemic toxicity, susceptibility to protease degradation, short half-life, and rapid renal clearance. To circumvent these challenges and improve AMP’s efficacy, different approaches such as peptide chemical modifications and the development of AMP delivery systems have been employed. Nanomaterials have been shown to improve the activity of antimicrobial drugs by providing support and synergistic effect against pathogenic microbes. This paper describes the role of nanotechnology in the targeted delivery of AMPs, and some of the nano-based delivery strategies for AMPs are discussed with a clear focus on metallic nanoparticle (MNP) formulations.Item Nanotechnology-based strategies for treatment of obesity, cancer and anti-microbial resistance: Highlights of the Department of Science and Innovation/mintek Nanotechnology Innovation centre biolabels research node at the University of the Western Cape(MDPI, 2022) Sibuyi, Nicole Remaliah Samantha; Moabelo, Koena Leah; Meyer, SamanthaNanotechnology has recently received much interest in various fields, including medicine. South Africa (SA) was the first country in Africa to adopt the technology with the aim of enhancing the national bio-economy and global competitiveness by using innovative nanotechnology-based solutions. Since its inception in 2005 in SA, researchers have seized opportunities to increase and develop niche areas for its application in the health, energy, food, agriculture, and water sectors. We ventured into this field and have performed pioneering work on nanotechnology-based treatment strategies over the years. This perspective highlights the journey, with associated successes over the years, in order to display the impact of our nanotechnology research in health. The focus is on the nanotechnology outputs that have emanated from the Department of Science and Innovation (DSI)/Mintek Nanotechnology Innovation Centre (NIC) Biolabels Research Node (BRN) at the University of the Western Cape (UWC).Item Phytonanotherapeutic applications of plant extract-synthesized silver nanoparticles in wound healing—a prospective overview(Springer, 2024) Oselusi, Samson Olaitan; Sibuyi, Nicole Remaliah Samantha; Madiehe, Abram MadimabeChronic wounds continue to pose severe threats to public health and the global economy. This is because the healing process is hindered by several factors, such as bacterial infections, comorbid conditions, age, and lifestyle. Medical wound therapy is currently based on long-term antibiotic use, and its activity has been limited by various factors, including treatment efficacy, toxicity, and increased risk of opportunistic infections. The advent of novel techniques such as nanotechnology can provide sustainable platforms for developing reliable, cost-effective, and innovative wound healing interventions. In this context, plant extract-synthesized silver nanoparticles (AgNPs) have become attractive to the clinical community because of their wide range of biological properties, such as antibacterial, anti-inflammatory, and wound healing effects. These AgNPs could be used in the development of better dressings for wounds.Item Prospects of using gum Arabic silver nanoparticles in toothpaste to prevent dental caries(MDPI, 2023) Ahmed, Omnia Abdelmoneim Khidir; Sibuyi, Nicole Remaliah Samantha; Fadaka, Adewale OluwaseunThere is growing interest in the use of green synthesized silver nanoparticles (AgNPs) to control and prevent dental diseases. The incorporation of green synthesized AgNPs into dentifrices to reduce pathogenic oral microbes is motivated by their presumed biocompatibility and broad-spectrum antimicrobial activity. In the present study, gum arabic AgNPs (GA-AgNPs) were formulated into a toothpaste (TP) using a commercial TP at a non-active concentration, to produce GA-AgNPs_TP. The TP was selected after evaluating the antimicrobial activity of four commercial TPs 1-4 on selected oral microbes using agar disc diffusion and microdilution assays. The less active TP-1 was then used in the formulation of GA-AgNPs_TP-1; thereafter, the antimicrobial activity of GA-AgNPs_0.4g was compared to GA-AgNPs_TP-1. The cytotoxicity of GA-AgNPs_0.4g and GA-AgNPs_TP-1 was also assessed on the buccal mucosa fibroblast (BMF) cells using the MTT assay. The study demonstrated that antimicrobial activity of GA-AgNPs_0.4g was retained after being combined with a sub-lethal or inactive concentration of TP-1.