This study aimed to obtain a microbial active compound as a novel antimalarial drug from Indonesian isolates. Target-based assays were used to screen for antimalarial activity against the parasite mitochondrial, malate:quinone oxidoreductase (MQO) enzyme. In total, 1600 crude extracts, composed from 800 fungi and 800 actinomycetes extracts, were screened against MQO, yielding six active extracts as primary hits. After several stages of stability tests, one extract produced by sp. BioMCC f.T.8501 demonstrated stable MQO inhibitory activity. Several purification stages, including OCC, TLC, and HPLC, were performed to obtain bioactive compounds from this active extract. All purification steps were followed by an assay against MQO. We identified the active compound as nornidulin based on its LC-MS and UV spectrum data. Nornidulin inhibited MQO activity at IC of 51 µM and 3D7 proliferation in vitro at IC of 44.6 µM, however, it had no effect on the growth of several mammalian cells. In conclusion, we isolated nornidulin from Indonesian sp. BioMCC f.T.8501 as a novel inhibitor of MQO, which showed inhibitory activity against the proliferation of 3D7 in vitro.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9964459 | PMC |
| http://dx.doi.org/10.3390/ph16020268 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Development of hybrid biomicroparticles: cellulose exposing functionalized fusion proteins.
Microb Cell Fact
March 2024
Department of Molecular Biotechnology, Faculty of Chemistry, University of Gdansk, Gdansk, 80-308, Poland.
Background: One of the leading current trends in technology is the miniaturization of devices to the microscale and nanoscale. The highly advanced approaches are based on biological systems, subjected to bioengineering using chemical, enzymatic and recombinant methods. Here we have utilised the biological affinity towards cellulose of the cellulose binding domain (CBD) fused with recombinant proteins.
View Article and Find Full Text PDFGenomic alterations in ovarian endometriosis and subsequently diagnosed ovarian carcinoma.
Hum Reprod
May 2024
Department of Obstetrics and Gynecology, Sahlgrenska Center for Cancer Research, Institute of Clinical Sciences, Sahlgrenska Academy at University of Gothenburg, Gothenburg, Sweden.
Study Question: Can the alleged association between ovarian endometriosis and ovarian carcinoma be substantiated by genetic analysis of endometriosis diagnosed prior to the onset of the carcinoma?
Summary Answer: The data suggest that ovarian carcinoma does not originate from ovarian endometriosis with a cancer-like genetic profile; however, a common precursor is probable.
What Is Known Already: Endometriosis has been implicated as a precursor of ovarian carcinoma based on epidemiologic studies and the discovery of common driver mutations in synchronous disease at the time of surgery. Endometrioid ovarian carcinoma and clear cell ovarian carcinoma are the most common endometriosis-associated ovarian carcinomas (EAOCs).
Nornidulin, A New Inhibitor of Malate: Quinone Oxidoreductase (MQO) from Indonesian sp. BioMCC f.T.8501.
Pharmaceuticals (Basel)
February 2023
Department of Pharmaceutical Science, Faculty of Pharmacy, Universitas Airlangga, Surabaya 60115, East Java, Indonesia.
This study aimed to obtain a microbial active compound as a novel antimalarial drug from Indonesian isolates. Target-based assays were used to screen for antimalarial activity against the parasite mitochondrial, malate:quinone oxidoreductase (MQO) enzyme. In total, 1600 crude extracts, composed from 800 fungi and 800 actinomycetes extracts, were screened against MQO, yielding six active extracts as primary hits.
View Article and Find Full Text PDFGentisyl alcohol and homogentisic acid: Plasmodium falciparum dihydroorotate dehydrogenase inhibitors isolated from fungi.
J Gen Appl Microbiol
July 2021
Graduate School of Infection Control Sciences, Kitasato University.
Article Synopsis
- - Two Indonesian fungi, *Aspergillus assiutensis* and *Penicillium pedernalense*, along with a Japanese fungus, *Hypomyces pseudocorticiicola*, have been identified as producers of gentisyl alcohol, a compound that inhibits the enzyme PfDHODH associated with the malaria parasite.
- - Gentisyl alcohol has a strong inhibitory effect on PfDHODH, with a half-maximal inhibitory concentration (IC) value of 3.4 μM, indicating its potential as an anti-malarial agent.
- - Another Indonesian fungus, *Penicillium citrinum*, produces homogentisic acid, which is a less effective analog of gent
Microbial inhibitors active against Plasmodium falciparum dihydroorotate dehydrogenase derived from an Indonesian soil fungus, Talaromyces pinophilus BioMCC-f.T.3979.
J Gen Appl Microbiol
November 2020
Graduate School of Infection Control Sciences, Kitasato University.
Article Synopsis
- Researchers isolated a fungus called Talaromyces pinophilus to discover new inhibitors for an enzyme (PfDHODH) linked to the malaria-causing parasite Plasmodium falciparum.* -
- The main compound identified, altenusin, inhibited PfDHODH with a potency of 5.9 μM, and other metabolites, mitorubrinol and mitorubrinic acid, also showed inhibitory effects.* -
- While compounds 1 and 2 effectively targeted PfDHODH and hindered parasite growth, they did not affect the human version of the enzyme, whereas compound 3 had minimal inhibitory properties.*
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!