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Pharmaceutical Biology 2011-Dec

A novel sesquiterpene acid and an alkaloid from leaves of the Eastern Nigeria mistletoe, Loranthus micranthus with potent immunostimulatory activity on C57BL6 mice splenocytes and CD69 molecule.

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Edwin Ogechukwu Omeje
Patience Ogoamaka Osadebe
Chukwuemeka Sylvester Nworu
Justina Ngozi Nwodo
Wilfred Ofem Obonga
Akira Kawamura
Charles Okechukwu Esimone
Peter Proksch

キーワード

概要

BACKGROUND

The Eastern Nigeria mistletoe, Loranthus micranthus Linn. (Loranthaceae), is used in the treatment of several diseases including immune-modifying diseases and thus there is a need to identify the immunoactive constituents.

OBJECTIVE

This research isolated and characterized the immunoactive constituents in the Eastern Nigeria mistletoe.

METHODS

Bioassay-guided fractionation was employed in the isolation and purification of the constituents. The characterized compounds were screened for immunostimulatory activities on isolated C57BL/6 mice splenocytes and early activation marker, CD69 at concentrations of 10, 25, and 100 μg/mL using flow cytometry techniques and compared to lipopolysaccharide (LPS; 10 μg/mL) and concanavalin A (ConA; 2 μg/mL) as standards.

RESULTS

Two compounds, a novel sesquiterpene, 2, 3-dimethoxy-benzo [a, b] cyclopentenyl-3′,3′,5′-trimethyl pyran-4-carboxylic acid, and a known alkaloid, lupinine were isolated and characterized. The compounds (25 μg/mL) showed statistically significantly (p < 0.05) stimulatory activity on the splenocytes with values of 56.34 ± 0.26% and 69.84 ± 0.19%, respectively, compared to 7.58 ± 0.42% recorded for the unstimulated control. Similarly, the CD69 expression assay showed immunostimulation with statistically significant values (p < 0.05) of 2.31 ± 0.07% and 2.71 ± 0.03%, respectively, compared to 1.69 ± 0.05% recorded for the nonstimulated control.

CONCLUSIONS

These data suggest that the isolated compounds possess immunomodifying abilities. In addition, the activation of the CD69 molecule is possibly one of its mechanisms of action.

CONCLUSIONS

These compounds may be responsible in part, for the immunostimulatory activities already established for the Eastern Nigeria mistletoes.

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