Noraslinda Muhamad Bunnori

Applications of calixarenes in cancer chemotherapy: facts and perspectives

Research on the therapeutic applications of calixarene derivatives is an emerging area of interest. The anticancer activity of various functionalized calixarenes has been reported by several research groups. Due to their superior geometric shape, calixarenes can accommodate drug molecules by forming inclusion complexes. Controlled release of anticancer drugs by calixarenes might help in targeted chemotherapy. This review summarizes the anticancer potential of the calixarenes and their drug loading properties. The potential use of calixarenes in chemoradiotherapy is also highlighted in brief.

Identification and characterization of Burkholderia pseudomallei K96243 serine and metallopeptidases

Burkholderia pseudomallei K96243, the causative agent of melioidosis, is reported to produce various extracellular products, including proteases. The role of these proteases in the melioidosis, however, remains obscure. Previous findings have hinted at the inherent pathogenicity of the protease during B. pseudomallei K96243 infection. We chose to study the two major families peptidases, i.e. serine peptidases and metallopeptidases present in B. pseudomallei K96243. The data mining revealed eighty ORFs (open reading frame) that potentially code for these peptidases and have prominent homology with B. pseudomallei K96243 based on prediction of function by bioinformatics approach. The annotations and classification lead forty eight and thirty two putative peptidases belong to serine peptidase and metallopeptidase, respectively. The distribution of 98% from the identified putative peptidase belongs to endopeptidases (EC 3.4.21. and EC 3.4.24.) and exopeptidases (EC 3.4.11., EC 3.4.13., EC 3.4.14., EC 3.4.16. and EC 3.4.17) and another 2% belong to EC 3.5.

Synthesis, in-Vitro and in Silico Studies of Azo-Based Calix[4]arenes as Antibacterial Agent and Neuraminidase Inhibitor: A New Look Into an Old Scaffold

Calixarene derivatives are reported as potential therapeutic agents. Azo derivatives of calixarenes have not been given much consideration to explore their biomedical applications. In the present study, some azo-based derivatives of calix[4]arene were synthesized and characterized and their antibacterial and antiviral potentials were studied. The mono azo products of sulphanilamide, sulfaguanidine and 2-methyl-4-aminobenzoic acid showed good activity against bacterial strains with minimum inhibition concentration values ranging from 0.97 to 62.5 μg/mL. For mono azo products, the diazotized salt was applied as a limiting reagent. The use of calix[4]arene and sodium acetate trihydrate in 1:3 (molar ratio) helped in partial substitution. Molecular docking was performed to see the interaction of the designed compounds with two bacterial and one viral (neuraminidase) receptor. Some of the derivatives showed good interaction with the active site of bacterial and neuraminidase enzymes through hydrogen, hydrophobic and pi-pi interactions, and could inhibit the activity of the selected enzymes.