- Title
- Synthesis, characterization and in vitro biological studies of cholesterol-based carriers as potential therapeutic agents
- Creator
- Ruwizhi, Ngonidzashe
- Subject
- Drug delivery systems
- Subject
- Cholesterol
- Date Issued
- 2021-03
- Date
- 2021-03
- Type
- Master's theses
- Type
- text
- Identifier
- http://hdl.handle.net/10353/20708
- Identifier
- vital:46443
- Description
- Malaria, cancer and bacterial infections are numbered among the highest causes of fatalities. Most of the drugs used to combat these diseases suffer from resistance, poor absorption and bioavailability and high toxicity. Therefore, delivering a drug requires an excellent drug delivery system that must provide the medication at the site of action in the minimum time possible. Cholesterol is a sterol that is abundantly found in the human body and forms a part in the structure and organization of cell membranes. Many researchers have used cholesterol, especially in organic synthesis, because of its ready availability, low cost and functional groups that can be readily derivatized. In this research, different therapeutic agents (anticancer, antimalarial and antibacterial) were conjugated to cholesterol, and the synthesized compounds were characterized using FTIR, 1H and 13C NMR, Mass Spectroscopy, 2D 1H-13C, HSQC NMR and tested for in vitro biological activity. Thirteen compounds were successfully synthesized. CHS-Cur was the most effective against all Gram-positive bacterial strains, while CHS-Cur, CHS-ZD and C-CAC-ZD were effective against all the bacterial strains. C-CAC-Pyr showed good antiplasmodial activity with 97.75 and 97.83% inhibition at 20 and 10 μg/ml concentrations, respectively. The biological activity of some of the compounds was increased by the conjugation of cholesterol, while others displayed reduced biological activity. In vitro cytotoxicity of the synthesized compounds on HeLa (cervical cancer) cells showed that compounds 2 (7.559 μg/mL), 3 (5.840 μg/mL), 5 (1.44 mg/mL), 7 (4.308 μg/mL) and 11 (3.295 μg/mL) exhibited some good anticancer activity with IC50 values of less than 10 μg/mL. Treating T3T fibroblast cells with compounds 2, 4, 5, 6, and 10 did not reveal a cytotoxic effect on the normal cells when compared to the control, cisplatin.
- Description
- Thesis (MSc) (Chemistry) -- University of Fort Hare, 2021
- Format
- computer
- Format
- online resource
- Format
- application/pdf
- Format
- 1 online resource (151 pages)
- Format
- Publisher
- University
- Publisher
- Faculty of Science and Agriculture
- Language
- English
- Rights
- University of Fort Hare
- Rights
- All Rights Reserved
- Rights
- Open Access
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UFH Department of Chemistry
| Thumbnail | File | Description | Size | Format | |||
|---|---|---|---|---|---|---|---|
| View Details Download | SOURCE1 | Full Dissertation new Ruwizhi.pdf | 3 MB | Adobe Acrobat PDF | View Details Download |