GSK-3β inhibition with antiplasmodial activities from the extracts of actinomycetes isolated from Malaysian forest soil.

Autor: Mahmud, Fauze, Ali, Amatul Hamizah, Azierah Fachyuni Abdul Aziz, Dg Nur, Maili, Salahaudin, Jembun, Mary, Sudi, Suhaini, Efani Dahari, Noor Dhiana, Lai, Ngit Shin, How, Siew Eng, Gansau, Jualang Azlan, Sidek, Hasidah Mohd, Embi, Noor, Ping-Chin Lee
Předmět:
Zdroj: Malaysian Journal of Microbiology; Dec2023, Vol. 19 Issue 6, p664-670, 7p
Abstrakt: 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 yeastbased 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. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index