1.GSK-3β inhibition with antiplasmodial activities from the extracts of actinomycetes isolated from Malaysian forest soil
Fauze Mahmud ; Amatul Hamizah Ali ; Dg Nur Azierah Fachyuni Abdul Aziz ; Salahaudin Maili ; Mary Jembun ; Suhaini Sudi ; Noor Dhiana Efani Dahari ; Ngit Shin Lai ; Siew Eng How ; Jualang Azlan Gansau ; Hasidah Mohd Sidek ; Noor Embi ; Ping-Chin Lee
Malaysian Journal of Microbiology 2023;19(no.6):664-670
Aims:
Glycogen synthase kinase-3 (GSK-3 (EC:2.7.11.1)) is one of the main therapeutic targets for treating cancer, diabetes, neurological illness and parasitic infection. Due to their distinctive structural characteristics and wide-ranging biological actions, small compounds from soil bacteria have been the most sought-after source for GSK-3 inhibitors. This study assessed the activities of soil actinomycetes isolated from Sabah, Malaysia, against human GSK-3β.
Methodology and results:
A total of 514 actinomycetes strains were isolated from 144 soil samples. The activities of the crude extracts were evaluated against GSK-3β and its upstream regulators (MKK1 and PP1/GLC7) using yeast-based assays. Eight actinomycetes extracts showed selective human GSK-3β inhibition without affecting MKK1 and PP1/GLC7. The extract from one of these eight isolates, FA013, also showed potent and selective anti-plasmodial activities against Plasmodium falciparum 3D7 strain (IC50 = 0.18 μg/mL, SI = 13,850) with a non-toxic effect against Chang liver cells.
Conclusion, significance and impact of study
This study identified FA013 as a potential isolate from Malaysian rainforest soil with inhibitory activities against GSK-3β and malaria parasites for future drug development.
Result Analysis
Print
Save
E-mail