Rubiaceae-Type Cyclopeptides from Galianthe thalictroides
Patrícia O Figueiredo1, Maria de Fatima C Matos2, Renata T Perdomo2
1Instituto de Química, Universidade Federal de Mato Grosso do Sul , Campo Grande, MS 79074-460, Brazil.
Journal of Natural Products
|February 26, 2016
Summary
Two cyclopeptides isolated from Galianthe thalictroides roots, 6-O-methylbouvardin and 5β-hydroxy-RA-III, show potent anticancer activity against kidney, prostate, and colon cancer cell lines.
Area of Science:
- Natural Product Chemistry
- Pharmacology
- Medicinal Chemistry
Background:
- The Rubiaceae family is a known source of bioactive cyclopeptides.
- Galianthe thalictroides is a plant species within the Rubiaceae family.
- Cyclopeptides often exhibit significant biological activities, including anticancer properties.
Purpose of the Study:
- To isolate and characterize cyclopeptides from Galianthe thalictroides roots.
- To evaluate the in vitro anticancer activity of the isolated compounds.
- To report the first isolation of Rubiaceae-type cyclopeptides from a genus outside of Rubia or Bouvardia.
Main Methods:
- Isolation and purification of compounds from plant extracts.
- Structure elucidation using spectroscopic methods (implied).
- Sulforhodamine B assay for cytotoxicity testing against cancer cell lines.
Main Results:
- Two Rubiaceae-type cyclopeptides were isolated: 6-O-methylbouvardin (1) and a new compound, 5β-hydroxy-RA-III (2).
- Both compounds demonstrated in vitro anticancer activity with GI50 values ranging from 0.06 to 1.80 μg mL(-1) against 786-0, PC-3, and HT-29 cancer cell lines.
- This marks the initial discovery of these cyclopeptides in the Galianthe genus.
Conclusions:
- Galianthe thalictroides is a novel source of bioactive Rubiaceae-type cyclopeptides.
- The isolated cyclopeptides possess significant cytotoxic effects against various human cancer cell lines.
- These findings expand the known chemical diversity and potential therapeutic applications of Rubiaceae cyclopeptides.
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