Pusat Penyelidikan Dadah dan Ubat-Ubatan - Tesis

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    Discovery Of Multi-Targeting Inhibitors In Parkinson’S Disease Using Molecular Modelling, In Silico Admet Profiling, And Behavioural Analysis Of Zebrafish Larvae
    (2025-01)
    Yahaya, Sani Najib
    Parkinson's disease (pd) is a neurodegenerative disorder that usually leads to physical disability. This research aims to identify inhibitors targeting multi-target proteins involved in the progression of pd. Ligand-based pharmacophore models (lbp) were developed and validated using α-synuclein (α-syn) protein and prolyl oligopeptidase (pop) enzyme inhibitors. Lbp model-3 for α-syn and model-2 for pop inhibitors were selected based on the gunner henry score and enrichment factor techniques. These models were employed for the screening of potential pd inhibitors. The α-syn model-3 has pharmacophoric properties consisting of 4 hydrogen bond acceptors, 5 hydrogen bond donors and 1 aromatic ring and is used to screen the maybridge, ibs, and arsinex databases, which in total have 254,870 compounds. The pop model-2, on the other hand, features 1 hydrophobic group, 1 positive ionized group, and 2 aromatic rings and is used to screen the ibs database, which consists of 69,543 compounds. Model-3 and model-2, respectively, managed to identify 281 and 177 compounds through the virtual screenings.
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    Design, Synthesis And Biological Evaluation Of New Opioid Analgesics Based On Tetrahydro-Β-Carboline Scaffold In Zebrafish (Danio Rerio) Larvae
    (2024-03)
    Alananzeh, Waleed Abdullah Ahmad
    The present study aims to design, synthesise, and evaluate the analgesic activities of THβC derivatives. A database of 25,227 THβC analogues was prepared from structure based virtual screening of the ZINC database for bromine fragments and linking the fragments at the N2 position of the THβC scaffold.
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    The Effect Of Mitragynine Addiction In Rats On Histone Regulations And Neuroplasticity
    (2024-01)
    Suleiman, Yunusa
    Mitragynine (MIT) was reported to develop addiction and impair cognitive functions. In acute studies, MIT was found to disrupt hippocampal synaptic transmission and distort memory via unknown mechanisms. This project evaluated the impact of 14 days of MIT exposure on the modulation of histone, synaptic transmission, and its potential mechanisms as well as dopaminergic, GABAergic, cholinergic, and glutamatergic systems in the rats’ brains. The impact of pharmacological inhibition of histone deacetylase enzyme on MIT action was also evaluated.
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    Determination Of Haematological And Endogenous Steroids Profiles In Malaysian Junior Athletes
    (2019-04)
    Mohd Rodhi, Ainolsyakira
    Haematological and steroidological profiles have been used by World Anti-Doping Agency (WADA) to monitor the use of banned substances among athletes. These profiles can be highly influenced by many factors such as gender, physical activity, dietary, geographical factors and genetic origins. Establishing reference values of steroids and haematology profile in laboratory could be beneficial as it can compensate for the difference in local athletes. The aims of this study were to establish haematological and steroidological reference values for local athletes and to compare the variation of these values on several subpopulations. Blood and urine samples were collected from 126 athlete and 39 non-athlete subjects from three major ethnic groups within five consecutive weeks.
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    Studies On The Chemistry, Anticholinesterase Activity And Toxicity Of Mitragyna Speciosa (Kratom) Alkaloids
    (2024-06)
    Chear, Nelson Jeng Yeou
    Mitragyna speciosa (korth) havil. Is a medicinal plant native to malaysia, traditionally used to treat pain, diabetes, hypertension, and drug addiction. It is also consumed as a tonic beverage to enhance alertness, attention and working performance among labourers and farmers. Most pharmacological activities documented for m. Speciosa focus on opioid-related activities. Research on the potential therapeutic effects of m. Speciosa on the cholinergic neurotransmission system is still scarce. Only one study has reported the anticholinesterase activity of the methanol extract and mitragynine prepared from thai m. Speciosa. Therefore, this study aims to identify potential cholinesterase inhibitors from m. Speciosa using a bioassay-guided isolation approach. A total of thirteen alkaloids were isolated and characterized from the alkaloid extract using modern chromatographic techniques and spectroscopic methods. The isolated alkaloids were mitragynine (87), speciociliatine (88), speciogynine (89), mitraciliatine (90), paynantheine (91), corynantheidine (101), corynoxine (81), corynoxine b (82), mitrafoline (125), mitragynine oxindole b (117), mitragynine oxindole a (116), 17(z)-speciociliatine (146), and speciociliatine n-oxide (98). Two of these alkaloids, 17(z)-speciociliatine (146) and speciociliatine n-oxide (98), are the new compounds from m. Speciosa. Notably, 17(z)-speciociliatine (146) is the fourth isomer of mitragynine (87), in addition to (88), (89) and (90).