[DOWNLOAD] "Analysis of Soy Natural Products and Esterase Enzymes for Drug Development" by Crystal A. Jurkiewicz # eBook PDF Kindle ePub Free

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eBook details

• Title: Analysis of Soy Natural Products and Esterase Enzymes for Drug Development
• Author : Crystal A. Jurkiewicz
• Release Date : January 19, 2013
• Genre: Medical,Books,Professional & Technical,
• Pages : * pages
• Size : 6647 KB

Description

Two broad subjects of the drug development process are covered in this thesis, because of this the first chapter gives needed background information in order to fully understand the projects presented in the next two chapters. The first chapter deals with identification of a source for scale-up production of an active pharmaceutical ingredient (API) for possible future investigational new drug submission. Glyceollin’s (GLY’s) or phytoestrogens that are made in soy plants in response to stress, have been implicated in the treatment for breast and prostate cancer. In order to determine relative amounts of the GLY’s in the plants, we have undertaken several studies. Firstly, we have performed preliminary tests on extracts from various parts of the plant (roots, stems, leaf, seed and seed pod) to determine the amounts of GLY produced. It has been demonstrated that most of the GLY is generally found in the roots as this is where the cyst root nematode (CRN) attacks the plant. Decreasing amounts of GLY are found further away from the roots>>stem>>leaf>>seed pod>>seeds. Extraction of the GLY’s from the roots of CRN infected soybean plants is a viable source for the anti-estrogenic GLY I (-). Lastly, we investigated the possibility that the soybean plant stores glycosylated forms of the GLY’s for use when the plant is attacked or stressed. Extractions taken from the roots of the soybean plant were incubated with the enzyme β-glucosidase. The results showed no evidance of glycosylated forms of the GLY’s present in the roots of the plant. The second chapter shows the development of a screening assay that could be used to help identify or narrow the list of lead candidates for pre-clinical drug testing. Carboxylesterase (CES) is a drug metabolizing enzyme present predominatly in the liver. It is involved in not only the biotransformation of API’s for purposes of excretion, but also largly associated with the activation of prodrugs. A spectrophotometric assay was designed to measure the kinetic parameters of CES with the intensily studied and characterized drug procaine. This assay is intended to be used to identify activity of this enzyme with new drug products, along with characterizing it’s pharmacokinetic behavior using comparisons of Km and Vmax. Verification of the most ideal conditions to test the rate of conversion were conducted, proving a pH of 7.4 and a temperature of 37°C to be optimal. These conditions were used to measure the Km and Vmax of procaine with the CES enzyme.

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