Background: Sexually transmitted diseases (STD's) have a major impact on sexual and reproductive health worldwide. Each year, the World Health Organization (WHO) estimates 448 million new cases of curable STD's are diagnosed. The emergence of drug resistance in STD related microorganisms and potential side effects demand the discovery of newer drugs. The exploration of newer anti-microbial substances from natural sources may serve as promising alternatives. In this study, twelve medicinal plant species used traditionally in the treatment of STD's are investigated in this regard. Methods: Ethanol plant extracts and three flavonoids were evaluated for their antimicrobial properties against one fungi and three bacteria, through the micro-dilution assay. To determine the anti-inflammatory activities of the extracts and compounds, the inhibitory effect was measured on the pro-inflammatory enzyme lipoxygenase, 15-LOX. Extracts were further evaluated for their inhibitory effect on the supercoiling activity of bacterial DNA gyrase by using the DNA gyrase kit. The extracts and compounds were lastly investigated for their anti-HIV activities against recombinant HIV-1 enzyme using non-radioactive HIV-RT colorimetric assay. Results: Acacia karroo and Rhoicissus tridentata extracts showed good antimicrobial activity with MIC values ranging between 0.4 and 3.1 mg/ml. Extracts of Jasminum fluminense, Solanum tomentosum and flavonoid 2 and 3 had good anti-inflammatory activity with IC50 less than the positive control quercetin (IC50 = 48.86 ug/ml). Extracts of Diospyros mespiliformis, Peltophorum africanum, Rhoicissus tridentata and flavonoids 1 and 2 showed the best inhibitory activity against the bacterial DNA gyrase. A. karroo and flavonoid 3 exhibited moderate HIV RT inhibition activity of 66.8 and 63.7 % respectively. R. tridentata and Terminalia sericea had the best RT inhibition activity (75.7 and 100 %) compared to the positive control doxorubicin (96.5%) at 100 ug/ml concentration. Conclusion: The observed activities may lead to new multi-target drugs against sexually transmitted diseases. / Dissertation (MSc)--University of Pretoria, 2017. / Plant Science / MSc / Unrestricted

OBJECTIVE: To determine the effect of anti-inflammatory drugs (4- methoxybenzophenone) and (kavain) on bone formation and bone resorption models using a three-dimensional (3D) live calvarial bone METHODS: Utilizing neonatal mouse calvarial bones on a grid system with media designed to cause bone formation or resorption. These models were used to study the effect of 4- methoxybenzophenone and kavain on bone remodeling. The spent media were evaluated by quantitative analysis of tartrate resistant acid phosphatase (TRAP), alkaline phosphatase (ALP) activity and calcium release. The calvaria were stained with neutral red and silver nitrate for histological analysis. RESULTS: Kavain and 4-methoxybenzophenone affected the calvarial bone remodeling by inhibiting resorption. Kavain stimulated bone formation as shown by ALP activity and prevented the transformation of macrophages into osteoclasts as shown by neutral red staining. Kavain prevented resorption as shown by silver nitrate staining. Histological examination of kavain treated bone showed new osteoid formation. The other factor, 4-methoxybenzophenone, had inconsistent effects on bone. Neutral red staining showed no osteoclast differentiation and silver nitrate staining showed no resorption. However calcium release increased in the resorption model and calcium uptake increased in the formation model. There was no effect on ALP or trap activities in either model.

A dissertation submitted to the Faculty of Science, University of the Witwatersrand, Johannesburg for the degree of Master of Science / The antiinflammatory effects of lnterleukin-4 (IL-4) and the synthetic glucocorticoid dexamethasone were studied in adhered monocytes and the leukaemic cells HL-60 and THP-1, with respect to the expression of interleukin-l.B (IL-l.B), the (signalling) IL-l receptor type I (JL..IRtI), and the (inhibitory) JT_,.l receptor type n (IL-lRtII). (Abbreviation abstract) / AC 2018

Study Design: A single-blind, 2-factor (4 treatments by 8 time points) repeated-measures study design. Objective: To analytically determine dexamethasone and dexamethasone phosphate concentrations in plasma derived from proximal effluent venous blood, following cathodic iontophoresis. Methods and Measures: Six volunteers received the following dexamethasone phosphate (2.5 ml, 4 mg/ml) treatments to their wrists on separate occasions: cathodic iontophoresis (4 mA, 10 minutes or 4 mA, 20 minutes), passive application (10 or 20 minutes). Plasma samples from the ipsilateral antecubital vein were obtained 10 minutes prior to and half way through the treatment (5 or 10 minutes), at the end of the treatment (10 or 20 minutes), and posttreatment (15, 30, 60, 90, and 120 minutes). The present investigation examined: (1) the sensitivity and linearity of extraction and analysis of dexamethasone and dexamethasone phosphate; (2) the necessity for determining both; and (3) the plasma levels from proximal effluent venous blood following cathodic iontophoresis. Results: The aggregate (n= 18) of the 6-point standard curves were linear for dexamethasone (r > 0.974) and dexamethasone phosphate (r > 0.829). In vitro dephosphorylation of dexamethasone phosphate to dexamethasone occurred in plasma at 37°C and during freeze-thaw. Measurable dexamethasone or dexamethasone phosphate concentrations were absent at all time points and under all conditions in the human subjects. Conclusions. These results demonstrate the sensitivity of the current assay and the need for evaluating both forms of the drug, as in vitro dephosphorylation results in the presence of dexamethasone and dexamethasone phosphate in samples. Absence of measurable dexamethasone or dexamethasone phosphate in the proximal effluent venous blood may require re-evaluation of the extent of drug delivery during the clinical iontophoresis of dexamethasone phosphate.

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The role of inflammation poses a number of interesting facets. Frequently it appears as a mechanism of defense: at other times it appears to present itself as a pathologic situation of unknown etiology. In neither case have the underlying mechanisms been fully identified. A variety of tissues can be involved, but when occurring as a pathology entity, it is more frequently observed in the synovial tissues. As a general rule, inflammation used as a defense mechanism in benign and self- limiting. This is not the case whore it become matter of pathology. It is here where mankind has looked for effective weapons for relief.

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