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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.
Aims:
Lactate dehydrogenase (LDH)-A is highly expressed in diverse human malignant tumors, parallel to aggressive metastatic disease, resistance to radiation/chemotherapy and clinically poor outcome. Although this enzyme constitutes a plausible target in treatment of advanced cancer, there are few known LDH-A inhibitors.
Study Design:
In this work, we utilized a high-throughput enzyme micro-array format to screen and evaluate > 900 commonly used medicinal plant extracts (0.00001-.5 mg/ml) for capacity to inhibit activity of recombinant full length human LDHA; EC .1.1.1.27.
Methodology:
The protein sequence of purified enzyme was confirmed using 1D gel electrophoresis- MALDI-TOF-MS/MS, enzyme activity was validated by oxidation of NADH (500μM) and kinetic inhibition established in the presence of a known inhibitor (Oxalic Acid).
Results:
Of the natural extracts tested, the lowest IC50s [<0.001 mg/ml] were obtained by: Chinese Gallnut (Melaphis chinensis gallnut), Bladderwrack (Fucus vesiculosus), Kelp (Laminaria Japonica) and Babul (Acacia Arabica). Forty-six additional herbs contained significant LDH-A inhibitory properties with IC50s [<0.07 mg/ml], some of which have common names of Arjun, Pipsissewa, Cinnamon, Pink Rose Buds/Petals, Wintergreen, Cat's Claw, Witch Hazel Root and Rhodiola Root.
Conclusion:
These findings reflect relative potency by rank of commonly used herbs and plants that contain human LDH-A inhibitory properties. Future research will be required to isolate chemical constituents within these plants responsible for LDH-A inhibition and investigate potential therapeutic application.
Insights
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.
