Brocaeloid D, a novel compound isolated from a wheat pathogenic fungus, Microdochium majus 99049
Jingyu Zhang1, Zhenzhen Wang1, Zhijun Song2,3
1State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, Shanghai, 200237, China.
Abstract:
Microbes serve as the most important resource for drug discovery. During our screening for bioactive compounds from our natural products library, a pathogenic fungus, Microdochium majus strain 99049, from wheat was selected for further investigation. A new alkaloid named brocaeloid D (1), together with six previously characterized compounds (2-7) were identified. Compound 1 belongs to 4-oxoquinoline with C-2 reversed prenylation and a succinimide substructure. All the structures of these newly isolated compounds were determined by different means in spectroscopic experiments. The absolute configurations of 1 was further deduced from comparison of its CD spectrum with that of known compound 2. The bioactivities of these identified compounds were evaluated against several pathogenic microorganisms and cancer cell lines. Compounds 1-5 showed activity against HUH-7 human hepatoma cells with IC50 values of 80 μg/mL. Compound 6 showed mild activity against HeLa cells (IC50 = 51.9 μg/mL), weak anti-MTB activity (MIC = 80 μg/mL), and moderate anti-MRSA activity (MIC = 25 μg/mL), and compound 7 showed weak anti-MRSA activity (MIC = 100 μg/mL).
Insights
A new alkaloid, brocaeloid D, was discovered from the fungus Microdochium majus. This compound and others showed potential anticancer and antimicrobial activities.
Area of Science:
- Natural Product Chemistry
- Medicinal Chemistry
- Microbiology
Background:
- Microbes are a vital source for novel drug discovery.
- Screening natural products libraries is crucial for identifying bioactive compounds.
- Pathogenic fungi can produce unique chemical structures with therapeutic potential.
Purpose of the Study:
- To isolate and characterize bioactive compounds from the pathogenic fungus Microdochium majus strain 99049.
- To evaluate the cytotoxic and antimicrobial activities of the isolated compounds.
Main Methods:
- Isolation and purification of compounds using spectroscopic techniques (NMR, MS, CD).
- Structure elucidation of a new alkaloid, brocaeloid D, and six known compounds.
- In vitro bioactivity assays against cancer cell lines (HUH-7, HeLa) and pathogenic microorganisms (MTB, MRSA).
Main Results:
- A new 4-oxoquinoline alkaloid, brocaeloid D (1), was identified along with six known compounds (2-7).
- Compounds 1-5 exhibited cytotoxic activity against HUH-7 human hepatoma cells (IC50 = 80 μg/mL).
- Compound 6 demonstrated moderate anti-MRSA activity (MIC = 25 μg/mL) and weak anti-MTB activity (MIC = 80 μg/mL).
Conclusions:
- Microdochium majus is a promising source of bioactive natural products.
- Brocaeloid D and related compounds warrant further investigation for their therapeutic potential.
- The identified compounds show promise as leads for anticancer and antimicrobial drug development.
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