Asynthesis, characterisation and biological activity of bismuth and antimony 1,1- dithiolates / Dyg Hazwani Abang Ishak
Motivated by the success of metal-based drugs in treatment of various diseases, 12 complexes of antimony (7-12) and bismuth (13-18) metal were synthesized and characterized by using 1HNMR, 13CNMR, FTIR, CHNanalyser, TGA, DSC, PXRD, SCXRD, UV-Visible and Fluorescence characterisation. After having...
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| Format: | Thesis |
| Published: |
2017
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| Online Access: | http://studentsrepo.um.edu.my/9649/1/Dayang_Hazwani_Abang_Ishak.pdf http://studentsrepo.um.edu.my/9649/6/Synthesis%2C_characterisation_and_biological_activity_of_bismuth_and_antimony_1%2C1%2D_dithiolates..pdf http://studentsrepo.um.edu.my/9649/ |
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| Summary: | Motivated by the success of metal-based drugs in treatment of various diseases, 12
complexes of antimony (7-12) and bismuth (13-18) metal were synthesized and
characterized by using 1HNMR, 13CNMR, FTIR, CHNanalyser, TGA, DSC, PXRD,
SCXRD, UV-Visible and Fluorescence characterisation. After having verified the
structure of the complexes, the prepared complexes were tested for their biological
activity, anticancer in particular against a range of carcinoma cell lines, together with an
evaluation of anti-microbial activities. Bismuth compound [Bi(S2CNR2)](13) with
R=CH2CH3 was found to be cytotoxic towards an array of human carcinoma, more
pronounced in HepG2 cells (liver cancer cells). This compoundalso induced apoptosis
in the cell the death mechanism pathway and expressed death receptor-dependent
pathway by generating CD40, CD40L and TNF-R1 (p55) protein. Moreover, complex
13 promotes tumour-suppressor, DAPK1 enzyme which naturally comes hand in hand
with the down-regulation of XIAP gene and NF-?B, protein complex that controls the
DNA transcription. The inhibition growth of HepG2 cells is in parallel with the findings
that cell cycle arrest occurred at S and G2/M phases. However, another bismuth
compound in the testing, [Bi(S2CNR2)] (16) with R=CH2CH2OH, is found to be less
formidable in almost all of the study performed. This result is further supported by the
cell invasion rate study whereby the invasion rate of 16 is 10-fold higher than that of 13,
again, correlated with the down-regulation of XIAP and Survivin protein, extracted by
13. Complexes 13 and 16 were also discovered to have different binding motifs in DNA
where 13 interacts at AT- and TA- specific sites followed by inhibition digestion of
restriction enzyme; 16 display an adverse effect. |
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