Adenosine A1 receptor binding activity of methoxy flavonoids from orthosiphon stamineus
Orthosiphon stamineus Benth. (Orthosiphon grandiflorus Bold. or Clerodendranthus spicatus Thunb.) is an Indonesian medicinal herb traditionally used for diseases such as hypertension, diabetes, and kidney stones. Despite the importance of this last application, there are very few reports on it...
| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Thieme Verlagsgruppe
2009
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| Subjects: | |
| Online Access: | http://irep.iium.edu.my/33741/ http://irep.iium.edu.my/33741/ http://irep.iium.edu.my/33741/ http://irep.iium.edu.my/33741/1/Yuliana_et_al._2009.pdf |
| Summary: | Orthosiphon stamineus Benth. (Orthosiphon
grandiflorus Bold. or Clerodendranthus spicatus
Thunb.) is an Indonesian medicinal herb traditionally
used for diseases such as hypertension,
diabetes, and kidney stones. Despite the importance
of this last application, there are very few
reports on it. Diuretic action is an important factor
in kidney stone treatment, as an increase in
the volume of fluid flowing through the kidney
will help to dissolve the stones, assist their passing
to avoid further retention, and flush out the
deposits. Among the diverse roles of adenosine
A1 receptor antagonists in renal protection,
many studies have shown that they can induce
diuresis and sodium excretion. A bioassay-guided
fractionation of a methanol-water extract of
Orthosiphon stamineus leaves using the adenosine
A1 receptor binding assay resulted in the isolation
of seven methoxy flavonoids as active ligands
with Ki values in the micromolar range.
The Hill slope values are not significantly different
from unity (within 0.9–1.4), which indicates
the antagonist effect to A1-R. The results of this
study thus provide a scientific foundation for the
traditional use of Orthosiphon stamineus in kidney
stone treatment, as the affinity of the active
compounds isolated from it as adenosine A1 receptor
ligands allows them to be associated with
diuretic activity, which is one possible treatment
for renal lithiasis. |
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