Plant-derived quinones, triterpenoids, and indenopyran compounds targeting metabolic enzymes for antiproliferative and antiplasmodial applications
Novel semi-synthetic compounds derived from plant sources, designed as inhibitors of glyceraldehyde 3-phosphate dehydrogenase, glutamate dehydrogenase 2, and dual oxidase 1. Potential applications in malaria treatment, cancer therapy, and neurodegenerative disease research, available for optimization through chemical transformation.
Overview
This research program focuses on the design and chemical transformation of three classes of bioactive compounds isolated from plant sources: quinones with antiproliferative and antiplasmodial activities, triterpenoids with antimalaria and neurodegenerative disease potential, and indenopyran compounds synthesized through a novel oxidative approach. These compounds are being developed as targeted inhibitors of three key enzymes: glyceraldehyde 3-phosphate dehydrogenase (GAPDH), glutamate dehydrogenase 2 (GDH2), and dual oxidase 1 (DUOX1). By disrupting these metabolic and oxidative pathways, the compounds offer promising leads for pharmaceutical development in areas of significant global health need, particularly malaria and cancer.
Technical specifications
Target enzymes and rationale:
- Glyceraldehyde 3-phosphate dehydrogenase (GAPDH): a central enzyme in glycolysis; inhibition disrupts energy metabolism in rapidly proliferating cells and parasites
- Glutamate dehydrogenase 2 (GDH2): involved in amino acid metabolism and neurotransmitter regulation; relevant to both parasitic survival and neurodegenerative processes
- Dual oxidase 1 (DUOX1): a reactive oxygen species-generating enzyme implicated in inflammatory signaling and cellular proliferation
Compound classes:
- Quinones with demonstrated antiproliferative and antiplasmodial activity
- Triterpenoids showing potential against malaria and neurodegenerative targets
- Indenopyran derivatives produced via a novel oxidative synthetic route
Approach: natural product isolation followed by chemical transformation to optimize potency, selectivity, and drug-like properties.
Technology readiness level
The compounds are at an early discovery stage. Initial isolation from plant sources has been completed, and the compounds are considered strong candidates for further optimization through chemical transformation. Biological validation against the target enzymes and in disease-relevant models is the next step required to advance these leads toward preclinical development.
About University of Yaoundé
University of Yaoundé I is a comprehensive public research university in Cameroon’s capital with a national role in training and innovation. Industry engages through co‑located applied engineering facilities and shared labs that support joint prototyping, testing, and talent pipelines, with partnerships to major national enterprises. Integration with the University Teaching Hospital of Yaoundé enables clinical translation and validation in the local health system. Research is backed by competitive national funding and international development partners, alongside contract work with public and private organizations. An on‑campus incubator has launched ventures, while technology transfer is coordinated through research administration rather than a stand‑alone TTO.
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