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A Customizable Approach for the Enzymatic Production and Purification of Diterpenoid Natural Products
Published on: October 4, 2019
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Antimycobacterial labdane diterpenes from Leucas stelligera
Roshan R Kulkarni1, Ketaki Shurpali, Vedavati G Puranik
1Division of Organic Chemistry, CSIR-National Chemical Laboratory , Pune 411008, India.
Journal of Natural Products
|October 15, 2013
Summary
Four new labdane diterpenes from Leucas stelligera showed selective antimycobacterial activity against Mycobacterium tuberculosis. These compounds, along with two known flavones, offer potential for new tuberculosis treatments.
Area of Science:
- Natural Product Chemistry
- Medicinal Chemistry
- Pharmacology
Background:
- Leucas stelligera is a plant species with a history of traditional medicinal use.
- Diterpenoids and flavones are classes of natural products known for diverse biological activities.
- Tuberculosis remains a significant global health challenge, necessitating the discovery of novel therapeutic agents.
Purpose of the Study:
- To isolate and characterize new chemical constituents from Leucas stelligera.
- To evaluate the antimycobacterial activity of the isolated compounds against Mycobacterium tuberculosis.
- To explore the potential of Leucas stelligera as a source for anti-tuberculosis drug discovery.
Main Methods:
- Phytochemical investigation using solvent extraction (acetone) of aerial plant parts.
- Structure elucidation of new compounds employing 1D and 2D Nuclear Magnetic Resonance (NMR) spectroscopy.
- Single-crystal X-ray crystallography was utilized for definitive structural confirmation of a key compound.
- In vitro antimycobacterial activity assay against Mycobacterium tuberculosis using IC50 determination.
Main Results:
- Four new labdane diterpene compounds (1-4) were successfully isolated and characterized.
- Two known flavones, velutin (5) and chrysoeriol (6), were also identified.
- Compounds 1-4 demonstrated selective inhibitory activity against Mycobacterium tuberculosis.
- The IC50 values for compounds 1-4 ranged from 5.02 to 9.80 μg/mL, indicating moderate to good potency.
Conclusions:
- Leucas stelligera is a rich source of structurally novel labdane diterpenes.
- The isolated new labdane diterpenes possess significant selective antimycobacterial activity.
- These findings support the ethnobotanical use of Leucas stelligera and highlight its potential for developing new anti-tuberculosis agents.
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