Thesis (Ph. D.)--City University of New York, 2007. / Includes bibliographical references (leaves 100-120) and index. Also available for educational and research purposes in PDF format on the Internet.

Thesis (M.S.)--Oregon State University, 2009. / Printout. Includes bibliographical references. Also available on the World Wide Web.

Thesis (Ph. D.)--Washington State University, May 2009. / Title from PDF title page (viewed on Apr. 19, 2010). "College of Pharmacy." Includes bibliographical references.

Thesis (Ph.D.) - University of Queensland, 2005. / Includes bibliography.

Bioassay directed fractionation of the methyl ethyl ketone extract of Crescentia cujete resulted in the isolation of nine bioactive compounds, and detailed spectroscopic interpretation led to the assignment of their structures as (2S,3S)-3-hydroxy-5,6-dimethoxy dehydroiso-α-Iapachone [2.10], (2R)-5,6- dimethoxydehydroiso-α-Iapachone [2.11], (2R)-5-methoxy dehydroiso-alapachone [2.12], 5-hydroxy-2-(1'-hydroxyethyl)naphtho[2,3-b ]furan-4,9-dione [2.13], 2-(1 '-hydroxyethyl)naphtho[2,3-b ]furan-4,9-dione [2.14]' 2-isopropenylnaphtho[ 2,3-b ]furan-4,9-dione [2.15], 5-hydroxydehydro-iso-a-Iapachone [2.16], 3-hydroxymethylfuro[3,2-b ]naphtho[2,3-d]furan-5,10-dione [2.17], and 9- hydroxy-3-hydroxymethylfuro[3,2-b ]naphtho[2,3-d]furan-5,10-dione [2.18]. Compounds 2.10-2.12 are new, showing selective activity towards DNA repair-deficient yeast mutants. The selective DNA damaging activity of known compounds 2.13-2.16 is reported herein for the first time. Compounds 2.17 and 2.18 also show DNA damaging activity, and possess a novel fused ring system. The bioactive sterols ergosta-5-24(28)-diene-3β,7α-diol [3.1] and 24,28- epoxyergost-5-ene-3β,7α-diol [3.2], originally isolated from <i>Pseudobersama mossambicensis</i>, have been synthesized from stigmasterol. In addition to these sterols, some of their analogs were prepared, and the bioactivity of all compounds were assessed. / Ph. D.

Submitted in fulfillment for the Degree of Doctor of Philosophy (Biotechnology), Durban University of Technology, Durban, South Africa, 2016. / Mycobacterium tuberculosis (MTB), the causative agent of tuberculosis (TB) has infected approximately one-third of the world population, with 9.6 million TB cases in 2014. The emergence of multi-drug resistant (MDR) and extensively-drug resistant (XDR) strains of MTB has further complicated the problem of TB control. It is now imperative that novel antimycobacterial compounds are discovered in order to treat infections and reduce the duration of current TB therapy courses. For centuries, medicinal plants have been used globally worldwide for the treatment and prevention of various ailments. This occurs particularly in developing countries where infectious diseases are endemic and modern health facilities and services are inadequate. In recent years, the use and search for plant drug derivatives have been fast-tracked. Ethnopharmacologists, botanists, microbiologists, and natural product chemists are trying to discover phytochemicals which could be developed for the treatment of infectious diseases, especially TB. Plants are rich in a wide variety of secondary metabolites, such as tannins, terpenoids, alkaloids, and flavonoids, which have been found in vitro to have antimycobacterial activity. In the search for new lead compounds, nine medicinal plant species, Buddleja saligna, Capparis tomentosa, Carpobrotus dimidiatus, Dichrostachys cinerea, Ekerbergia capensis, Ficus Sur, Gunnera perpensa, Leonotis leonurus and Tetradenia riparia were collected in Kwa-Zulu Natal (KZN) following report of their therapeutic use in traditional medicine to treat symptoms and infections related to TB. They were tested in vitro for their activity against Mycobacterium smegmatis, Mycobacterium tuberculosis H37Rv (ATCC 25177) and three well-characterized clinical isolates of MDR-TB and XDR-TB using the agar incorporation method. The minimum inhibitory concentration of the active plant extracts was determined using the broth microdilution method. Our findings show that five of the nine plants screened have antimycobacterial activity with concentrations ranging from 125 µg/ml to 1000 µg/ml. The aqueous extracts of G. perpensa and T. riparia; and the methanolic extracts of B. saligna, C. tomentosa, and C. dimidiatus possessed significant activity against M. smegmatis, M. tuberculosis H37Rv (ATCC 25177) and the three well-characterized clinical isolates of MDR-TB and XDR-TB. The cytotoxic effect of the active plant extracts was evaluated against the mouse BALB/C monocyte-macrophage (J774.2) and peripheral blood mononuclear cells (PBMCs). The toxic effects of the active plant extracts were evaluated using the brine shrimp lethality assay. Except for a high concentration of G. perpensa none of the other plants which possessed antimycobacterial activity showed any toxic or cytotoxic activity. The active plant extracts were thereafter assessed to determine if they had any effect on the survival or death of mycobacterial species, M. smegmatis, bound within the macrophage (J774.2) cell line at a concentration of 100 µg/ml. B. saligna had inactivated most of the phagocytosed bacilli after 24 hours of treatment therefore, it has a bactericidal effect on the mycobacteria located within the mouse macrophage. A phytochemical investigation of the leaves of B. saligna led to the isolation of two isomeric pentacyclic triterpene compounds namely Oleanolic Acid (OA) and Ursolic Acid (UA) using thin layer chromatography followed by silica gel column chromatography. The structures of these compounds were fully characterized by detailed NMR investigations, which included 1H and 13C NMR. Ursolic acid was isolated from this plant for the first time. Two-dimensional (2D) and three-dimensional (3D) quantitative structure-activity relationship (QSAR) studies were carried out to provide insight on the interaction of the compounds with the enzyme. Molecular docking studies predicted the free binding energy of the triterpenes inside the steroid binding pocket of Mycobacterium tuberculosis fadA5 thiolase compared to a reported inhibitor. Thus, their ability to inhibit the growth of Mycobacterium tuberculosis was predicted and was confirmed to possess significant antimycobacterial activity when tested against M. smegmatis, M. tuberculosis H37Rv (ATCC 25177), clinical isolates of MDR-TB and XDR-TB using the Microplate Alamar Blue Plate (MABA) assay. The present study has scientifically validated the traditional use of medicinal plant B. saligna. / D

Thesis (M.Sc.)--Memorial University of Newfoundland, 2005. / Restricted until October 2006. Bibliography: leaves 108-134.

Submitted in fulfillment of the requirements for the Degree of Master of Technology: Biotechnology, Durban University of Technology, 2009. / Dichrostachys cinerea, Carpobrotus dimidiatus, Capparis tomentosa and Leonotis leonurus are all plants that are indigenous to South Africa. These plants are used in traditional medicine to treat various ailments. However, there is little or no scientific data to justify these traditional uses. Furthermore, it is difficult to reconcile traditional knowledge with scientific evidence because of the overwhelming targeting of signal-responsive systems by plant defensive compounds, multiple sites of action and the connectedness of the signaling pathways, which provide many cures and have pleiotropic effects. In order to evaluate the action spectrum of these plants, and validate its widespread use, this research evaluated the antibacterial, antioxidant, anti-inflammatory, anti-mosquito and immunomodulatory properties of these plants. Antimicrobial activity of the extract was determined by evaluating the bactericidal and fungicidal action using the agar disc diffusion assay. Anti-oxidative properties of the extracts were tested using the DPPH photometric assay. Anti-inflammatory properties were carried out using the 5-lipoxygenase assay. The larvicidal, repellency and insecticidal assay was determined against A.arabiensis. The safe use of these plant extracts was determined by evaluating toxicity, a brine shrimp lethality assay and an in vitro cell culture system using human myelogenous leukemia cell line. Potential carcinogenic activity was evaluated using the Ames Salmonella Mutagenecity assay. The immunomodulatory activity of the extracts on human peripheral blood mononuclear cells 6 was evaluated on freshly harvested lymphocytes using the MTT assay. Cytokine response was evaluated by measuring the secretion of interferon-gamma and interleukin-10. Elucidation of the B cells, T cells, activated T cells, CD 4+, CD 8+ and NK cells was performed by flow cytometry. The extracts showed anti-microbial activity against Escherichia coli, Pseudomonas aeruginosa, Klebsiella oxytoca, Salmonella typhimurium, Serratia marcescens, Bacillus cereus and Tricoderm sp. The highest activity was shown by methanolic and aqueous extracts of L. leonurus leaves followed by methanolic and aqueous extracts of D. cinerea. Extracts of C. tomentosa and D.cinerea demonstrated a higher degree of free radical scavenging than rutin, which was used as a standard indicating that these plants have strong antioxidant properties. None of the plants showed significant anti-inflammatory activity when compared to NDGA. In the anti-mosquito assays, the extracts showed strong repellency and insecticidal activity. L. leonurus extracts demonstrated the highest insecticidal and repellency activity against the mosquito, and was also found to cause ‗knockdown‘ and mortality. The extracts display no toxicity, cytotoxicity and mutagenicity. The immunological studies for immune modulation showed that the methanol extracts of these plants induce a Th1- predominant immune response because they significantly suppressed the secretion of IL-10 and augment IFN-γ production, which are hallmarks used to indicate a stimulation of the innate immune response. This study also provides new information, with respect to the potential use of these plants in producing a mosquito repellent and an immunostimulant. / National Research Foundation

Thesis (MTech (Chemistry))--Cape Peninsula University of Technology, 2016. / In Africa, herbal medicines are often used as primary treatments for a variety of ailments and diseases including HIV/AIDS and for HIV-related problems. In general, traditional medicines are not well researched scientifically in controlled studies, and are poorly regulated. Since the pharmacological effectiveness of natural products is affected by several native and foreign factors, studies on the variations of chemical composition and biological activity of these medicines are necessary. The processes of investigating plants to identify chemical substances are of great interest to natural product researchers because there is a need to discover new drugs for treating old and new diseases. These facts underscore an urgent need to develop new anti HIV and AIDS drugs with fewer or no side effects. Research into drug discovery and development using natural products is increasingly becoming better established. Marine organisms as a source of natural products delivered numerous novel compounds with multiple pharmacological properties. Natural products give endless opportunities for discovering novel compounds that can be used as drugs or backbones of drug leads. Manayi is a natural product that has been used to treat and manage people with HIV, but no scientific studies have been done to prove its efficacy on the HIV under controlled conditions. For the purposes of this study, cooked and uncooked Manayi product was evaluated for its efficacy on HIV in vitro. Manayi samples were collected in East London, Eastern Cape and sequentially extracted with hexane, chloroform, dichloromethane, butanol, methanol, and water as a series of increasingly polar solvents for its bioactive chemical constituents.

Orientador: Cristiano Soleo de Funari / Coorientador: William de Melo Silva / Banca: Rondinelli Donizetti Herculano / Resumo: O café conquistou o paladar de inúmeros povos, em diversas regiões do planeta, devido às suas características sensoriais e o seu poder estimulante. É uma planta arbustiva, com duas espécies principais, a Coffea arabica L. e a Coffea conephora L. As duas espécies de café verde mais consumidas e exploradas diferem entre si pelas suas características organolépticas, físicas e químicas. O café arábica possui aroma e sabor mais apreciado, e suas aplicações estão nas bebidas. Já o café robusta é utilizado pelo segmento farmacêutico, devido aos seus mais altos teores de ácido clorogênico e cafeína. O alto consumo mundial do café verde tem estimulado o desenvolvimento de estudos relacionados aos constituintes do café, como a cafeína e o ácido clorogênico, e também os estudos relacionados à atividades biológicas. Nas últimas décadas, aumentou consideravelmente a busca por compostos bioativos de origem natural, e diversos métodos extrativos estão sendo utilizados com o objetivo de extrair a maior quantidade de princípios ativos oriundos das plantas vegetais. Visando desenvolver um novo extrato de café verde com maior teor de cafeína e ácido clorogênico, o presente trabalho tem por objetivo otimizar um processo de extração de grãos verdes de Coffea conephora L. com o intuito de se obter teores de cafeína e de ácido clorogênico superiores aos obtidos pela empresa Centroflora Nutra. Inicialmente, foi desenvolvido um método de análise por cromatografia líquida de ultra eficiência acoplada ... (Resumo completo, clicar acesso eletrônico abaixo) / Abstract: Coffee has conquered the palate of countless peoples, in diverse regions of the planet, due to its sensorial characteristics and its stimulating power. It is a shrub, with two main species, Coffea arabica L. and Coffea conephora L. The two most consumed and exploited green coffee species differ in their organoleptic, physical and chemical characteristics. Arabica coffee has the most appreciated aroma and flavor, and its applications are in beverages. Robusta coffee is used by the pharmaceutical segment, due to its higher contents of chlorogenic acid and caffeine. The high world consumption of green coffee has stimulated the development of studies related to coffee constituents, such as caffeine and chlorogenic acid, as well as studies related to biological activities. In the last decades, the search for bioactive compounds of natural origin has increased considerably, and several extractive methods are being used with the objective of extracting the greatest amount of active principles from plant plants. Aiming to develop a new green coffee extract with higher caffeine and chlorogenic acid content, the present work aims to optimize a process of extraction of green grains of Coffea conephora L. in order to obtain higher levels of caffeine and chlorogenic acid those obtained by Centroflora Nutra. Initially, an ultra high performance liquid chromatography coupled to a UV spectrophotometer (UHPLC-PAD / UV) analysis method was developed from a sample of green coffee extract market... (Complete abstract click electronic access below) / Mestre