In-vitroevaluation of bridelia ferruginea extract gold nanoparticles for the treatment of colon cancer

Colorectal cancer (CRC) has become a health burden, being the third common cancer worldwide. Treatment of colorectal cancer is very important to manage the high prevalence rate of this disease. The available treatments for CRC have their drawbacks and side effects. Available treatments of colon cancer include surgery, chemotherapy, and radiation. Due to the side effects associated with these treatments, alternative treatments that pose less side effects are being developed worldwide. Nanotechnologies have gained global consideration due to their potential to improve the current standards and techniques for the diagnosis and treatment. The use of plants for synthesis of gold nanoparticles has opened a new venture of synthesizing environmentally friendly and cost-effective nanoparticles which possess great properties for CRC treatment. The aim of this study was to investigate the use of green synthesized AuNPs from Bridelia ferruginea for potential cancer treatment. In this work study gold nanoparticles were synthesized utilizing Bridelia ferruginea stem bark extract. The nanoparticles were characterized using UV–Vis spectroscopy, Dynamic Light Scattering (DLS), Fourier Transform Infrared Spectroscopy (FTIR) and High-Resolution Transmission Electron Microscopy (HRTEM). The in vitroanti cancer activity of the AuNPs was investigated using Presto Blue assay, cellular morphology, caspase 3/7 assay on the human colon cancer cell line at different times to assess the optimum time for cell death. The cellular uptake and localization of AuNPs was investigated using HRTEM to assess uptake and location of the AuNPs within the cell. Results obtained from this study showed that the AuNP synthesis from Bridellia ferrugenia was successful. The Presto Blue cell viability results showed that the AuNPs reduced cell viability (%) significantly (p<0.05) after 24 h. The optimum treatment time of HT-29 cells with AuNPs was determined to be 24 h. The apoptotic effects of the AuNPs were assessed using Cell Event reagent, and the results from this assay indicated that caspase 3/7 was activated with treatment with AuNPs which induced cell death via apoptosis. The HRTEM results indicated that there was no uptake of AuNP targeting in HT-29 therefore localization could not be determined. It can be concluded that the AuNPs synthesized from Bridellia ferrugenia have anti-cancer properties and are able to induce cell death through apoptosis. Furthermore, this study revealed that optimization of the AuNPs for cellular uptake is needed to further understand the interaction between the nanoparticles and the cells. This will provide more insight on how cellular death is induced by the nanoparticles.Thesis (MSc) -- Faculty of Science, Department of Biochemistry and Microbiology (including Physiology), 202

In-vitroevaluation of bridelia ferruginea extract gold nanoparticles for the treatment of colon cancer

Colorectal cancer (CRC) has become a health burden, being the third common cancer worldwide. Treatment of colorectal cancer is very important to manage the high prevalence rate of this disease. The available treatments for CRC have their drawbacks and side effects. Available treatments of colon cancer include surgery, chemotherapy, and radiation. Due to the side effects associated with these treatments, alternative treatments that pose less side effects are being developed worldwide. Nanotechnologies have gained global consideration due to their potential to improve the current standards and techniques for the diagnosis and treatment. The use of plants for synthesis of gold nanoparticles has opened a new venture of synthesizing environmentally friendly and cost-effective nanoparticles which possess great properties for CRC treatment. The aim of this study was to investigate the use of green synthesized AuNPs from Bridelia ferruginea for potential cancer treatment. In this work study gold nanoparticles were synthesized utilizing Bridelia ferruginea stem bark extract. The nanoparticles were characterized using UV–Vis spectroscopy, Dynamic Light Scattering (DLS), Fourier Transform Infrared Spectroscopy (FTIR) and High-Resolution Transmission Electron Microscopy (HRTEM). The in vitroanti cancer activity of the AuNPs was investigated using Presto Blue assay, cellular morphology, caspase 3/7 assay on the human colon cancer cell line at different times to assess the optimum time for cell death. The cellular uptake and localization of AuNPs was investigated using HRTEM to assess uptake and location of the AuNPs within the cell. Results obtained from this study showed that the AuNP synthesis from Bridellia ferrugenia was successful. The Presto Blue cell viability results showed that the AuNPs reduced cell viability (%) significantly (p<0.05) after 24 h. The optimum treatment time of HT-29 cells with AuNPs was determined to be 24 h. The apoptotic effects of the AuNPs were assessed using Cell Event reagent, and the results from this assay indicated that caspase 3/7 was activated with treatment with AuNPs which induced cell death via apoptosis. The HRTEM results indicated that there was no uptake of AuNP targeting in HT-29 therefore localization could not be determined. It can be concluded that the AuNPs synthesized from Bridellia ferrugenia have anti-cancer properties and are able to induce cell death through apoptosis. Furthermore, this study revealed that optimization of the AuNPs for cellular uptake is needed to further understand the interaction between the nanoparticles and the cells. This will provide more insight on how cellular death is induced by the nanoparticles.Thesis (MSc) -- Faculty of Science, Department of Biochemistry and Microbiology (including Physiology), 202

One-pot synthesis, characterisation and biological activities of gold nanoparticles prepared using aqueous seed extract of Garcinia kola

Recently, biogenic synthesis of gold nanoparticles (AuNPs) has become a focus area in cancer research owing to the eco-friendliness and cost effectiveness of the synthetic method. In this study, aqueous extract of Garcinia kola seed (AEGKs) was used for the bio-reduction of Au3+ to Au0. The synthesised AEGKs-AuNPs was characterised by ultraviolet-visible (UV-Vis) spectroscopy, dynamic light scattering (DLS), high-resolution transmission electron microscopy (HRTEM) and Fourier transform-infrared (FT-IR) spectroscopy. The in vitro antioxidant activity of the AEGKs and AEGKs-AuNPs was evaluated using 2,2-diphenyl-1-picrylhydrazyl radical scavenging ability and ferric reducing antioxidant power assays. The AEGKs-AuNPs showed an absorption maximum at 512 nm, and the HRTEM images revealed mostly, spherical-shaped AuNPs in the size range of 2–17 nm. The FT-IR spectroscopy revealed that polyphenolic compounds and proteins were predominant, and responsible for the reduction and capping of the AuNPs. The AEGKs-AuNPs showed concentration dependent antioxidant activities, while dose dependent in vitro anti-cancer activity of the AEGKs-AuNPs was demonstrated against lungs, prostrate, human cervical and human colon cancer cells, using the 3-(4,5-dimethylthiazol-2-yl)− 2,5-diphenyltetrazolium bromide tetrazolium reduction (MTT) assay. The antioxidant and anti-cancer activities of the AEGKs-AuNPs could be attributed to the presence of phytochemicals and physicochemical properties of the AuNPs

Antithrombotic/anticoagulant and anticancer activities of selected medicinal plants from South Africa

Nine plants available in the Eastern Cape Province of South Africa were tested for antithrombotic and/or anticoagulant activity. Organic (methanol) and aqueous (distilled water) extractions were performed on the various plant parts. The thrombin assay and clotting time assays (thrombin-induced and CaCl 2 -induced) were utilised. Several extracts displayed activity, but in most cases this was due to the presence of tannins. Only the aqueous extracts displayed activity after tannin removal. The Sutherlandia frutescens leaf extract displayed antithrombotic activity, with an IC 50 value of 2.17 mg/ml. Gloriosa superba and Zantedeschia aethiopica leaf extracts displayed anticoagulant properties by inhibiting thrombin-induced clotting, with IC 50 values of 2.97 and 3.05 mg/ml, respectively. The Leonotis leonurus root extract was found to decrease the CaCl 2 -induced clotting time by 50% at 8.88 mg/ml. A decrease in this value accompanied by a decrease in fibrin formation was preferable for the CaCl 2 -induced assay, since decreased fibrin formation may have a role in the prevention of cancer metastasis. As tannins were found to contribute minimally to the anticoagulant effect of L. leonurus, the cytotoxicity potential of the extracts of this species against five cell lines was determined. Only the organic extract yielded significant cytotoxity

Antithrombotic/anticoagulant and anticancer activities of selected medicinal plants from South Africa

Nine plants available in the Eastern Cape Province of South Africa were tested for antithrombotic and/or anticoagulant activity. Organic (methanol) and aqueous (distilled water) extractions were performed on the various plant parts. The thrombin assay and clotting time assays (thrombin-induced and CaCl 2 -induced) were utilised. Several extracts displayed activity, but in most cases this was due to the presence of tannins. Only the aqueous extracts displayed activity after tannin removal. The Sutherlandia frutescens leaf extract displayed antithrombotic activity, with an IC 50 value of 2.17 mg/ml. Gloriosa superba and Zantedeschia aethiopica leaf extracts displayed anticoagulant properties by inhibiting thrombin-induced clotting, with IC 50 values of 2.97 and 3.05 mg/ml, respectively. The Leonotis leonurus root extract was found to decrease the CaCl 2 -induced clotting time by 50% at 8.88 mg/ml. A decrease in this value accompanied by a decrease in fibrin formation was preferable for the CaCl 2 -induced assay, since decreased fibrin formation may have a role in the prevention of cancer metastasis. As tannins were found to contribute minimally to the anticoagulant effect of L. leonurus, the cytotoxicity potential of the extracts of this species against five cell lines was determined. Only the organic extract yielded significant cytotoxity

Endogenous heparin levels in the controlled asthmatic patient

Background. Since heparin possesses anti-inflammatory properties, it is hypothesised that asthmatic patients have decreased levels of circulating heparin compared with healthy individuals. Design. We compared endogenous heparin levels in controlled asthmatic patients (53 adults) from the Asthma Clinic at Johannesburg General Hospital with those of healthy controls (26 adults) from the general population. Heparin levels in the blood samples were tested using the Chromogenix Coatest Heparin kit. Result. The blood of the patients contained significantly lower levels of endogenous heparin compared with that of the healthy individuals, indicating that the anti-inflammatory properties afforded by heparin are absent in these patients

In vitro analysis of the combinatory effects of novel aminonaphthoquinone derivatives and curcumin on breast cancer progression

CITATION: Pereira, Melanie C. et al. 2020. In vitro analysis of the combinatory effects of novel aminonaphthoquinone derivatives and curcumin on breast cancer progression. Anticancer Research, 40(1):229-238, doi:10.21873/anticanres.13944.The original publication is available at: https://pubmed.ncbi.nlm.nih.govBackground/aim: We previously reported the potential of aminonaphthoquinone derivatives as therapeutic agents against breast and other oestrogen-responsive tumours when combined with curcumin. This study aimed at screening of novel aminonaphthoquinone derivatives (Rau 008, Rau 010, Rau 015 and Rau 018) combined with curcumin for cytotoxic, anti-angiogenic and anti-metastatic effects on MCF-7 and MDA-MB-231 breast cancer cells. Materials and methods: Cytotoxic and anti-angiogenic effects were analysed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay and enzyme-linked immunosorbent assay; while anti-metastatic effects were measured using adhesion assay, Boyden chambers and Matrigel. Results: Curcumin combined with Rau 008 elicited marked cytotoxic effects in MCF-7 cells compared with the individual treatments, whereas when it was combined with Rau 015 and with Rau 018, it displayed similar effects in MDA-MB-231 cells. The anti-angiogenic effect of Rau 015 plus curcumin in MCF-7 cells and Rau 018 plus curcumin in MDA-MB-231 cells was more effective than individual treatments, while the metastatic capability of MDA-MB-231 cells was significantly reduced after treatment with the aminonaphthoquinone-curcumin combinations. Conclusion: Aminonaphthoquinones may offer significant promise as therapeutic agents against breast cancer, particularly when combined with curcumin.Publisher's versio

Development and evaluation of a reconstitutable dry suspension containing isoniazid for flexible pediatric dosing

Tuberculosis (TB) is a major cause of childhood death. Despite the startling statistics, it is neglected globally as evidenced by treatment and clinical care schemes, mostly extrapolated from studies in adults. The objective of this study was to formulate and evaluate a reconstitutable dry suspension (RDS) containing isoniazid, a first-line anti-tubercular agent used in the treatment and prevention of TB infection in both children and adults. The RDS formulation was prepared by direct dispersion emulsification of an aqueous-lipid particulate interphase coupled with lyophilization and dry milling. The RDS appeared as a cream-white free-flowing powder with a semi-crystalline and microparticulate nature. Isoniazid release was characterized with an initial burst up to 5 minutes followed by a cumulative release of 67.88% ± 1.88% (pH 1.2), 60.18% ± 3.33% (pH 6.8), and 49.36% ± 2.83% (pH 7.4) over 2 h. An extended release at pH 7.4 and 100% drug liberation was achieved within 300 min. The generated release profile best fitted the zero order kinetics (R2 = 0.976). RDS was re-dispersible and remained stable in the dried and reconstituted states over 4 months and 11 days respectively, under common storage condition

Endogenous heparin levels in the controlled asthmatic patient

Background. Since heparin possesses anti-inflammatory properties, it is hypothesised that asthmatic patients have decreased levels of circulating heparin compared with healthy individuals. Design. We compared endogenous heparin levels in controlled asthmatic patients (53 adults) from the Asthma Clinic at Johannesburg General Hospital with those of healthy controls (26 adults) from the general population. Heparin levels in the blood samples were tested using the Chromogenix Coatest Heparin kit. Result. The blood of the patients contained significantly lower levels of endogenous heparin compared with that of the healthy individuals, indicating that the anti-inflammatory properties afforded by heparin are absent in these patients

Synthesis and in vitro growth inhibitory activity of novel silyl- and trityl-modified nucleosides

Seventeen silyl- and trityl-modified (5′-O- and 3′,5′-di-O-) nucleosides were synthesized with the aim of investigating the in vitro antiproliferative activities of these nucleoside derivatives. A subset of the compounds was evaluated at a fixed concentration of 100 μM against a small panel of tumor cell lines (HL-60, K-562, Jurkat, Caco-2 and HT-29). The entire set was also tested at varying concentrations against two human glioma lines (U373 and Hs683) to obtain GI50 values, with the best results being values of ∼25 μM.SCOPUS: ar.jinfo:eu-repo/semantics/publishe