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High-Throughput Screening to Identify Plant Derived Human LDH-A Inhibitors
S Deiab1, E Mazzio1, S Messeha1
1College of Pharmacy and Pharmaceutical Sciences, Florida A & M University, Tallahassee, Florida 32307, USA.
European Journal of Medicinal Plants
|January 31, 2014
Summary
Researchers screened over 900 plant extracts for Lactate dehydrogenase (LDH)-A inhibition. Several potent natural inhibitors were identified, including Chinese Gallnut and Bladderwrack, offering potential for cancer therapy development.
Area of Science:
- Biochemistry
- Pharmacology
- Oncology
Background:
- Lactate dehydrogenase (LDH)-A is overexpressed in many human cancers, correlating with aggressive disease and poor patient outcomes.
- LDH-A is a potential therapeutic target for advanced cancers, but effective inhibitors are scarce.
Purpose of the Study:
- To screen a large library of commonly used medicinal plant extracts for inhibitory activity against human LDH-A.
- To identify natural compounds with significant LDH-A inhibitory properties for potential anti-cancer drug development.
Main Methods:
- A high-throughput enzyme micro-array was employed to test over 900 plant extracts for their capacity to inhibit recombinant human LDH-A.
- Enzyme activity and kinetic inhibition were validated using standard biochemical assays and a known inhibitor, Oxalic Acid.
Main Results:
- Chinese Gallnut (Melaphis chinensis), Bladderwrack (Fucus vesiculosus), Kelp (Laminaria Japonica), and Babul (Acacia Arabica) demonstrated the lowest IC50 values (<0.001 mg/ml).
- An additional 46 herbs, including Arjun, Cinnamon, and Witch Hazel Root, exhibited significant LDH-A inhibition (IC50s <0.07 mg/ml).
Conclusions:
- This study identified and ranked several medicinal plants with potent human LDH-A inhibitory properties.
- Further research is warranted to isolate active constituents and explore their therapeutic potential in cancer treatment.
