Analgesic, antipyretic, anti-inflammatory and toxic effects of
andrographolide derivatives in experimental animals.
Suebsasana S, Pongnaratorn P, Sattayasai J, Arkaravichien T, Tiamkao
S, Aromdee C.
Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Khon
Kaen University, Khon Kaen, Thailand.
Andrographolide (1) and 14-deoxy-11,12-didehydroandrographolide (2)
are active constituents of Andrographis paniculata (Burm. f.), family
Acanthaceae. A. paniculata extracts are reported to have antiviral,
antipyretic, immunostimulant and anticancer activities. In this study,
1 and its 14-acetyl- (4) and 3,19-isopropylidenyl- (3) derivatives, as
well as 2 and its 3,19-dipalmitoyl-derivative (5), were
intraperitoneally tested for their analgesic, antipyretic,
anti-inflammatory and acute toxicity effects in animal models.
Analgesic effects were tested in mice using hot plate and writhing
tests to distinguish the central and peripheral effects, respectively.
The results showed that, at 4 mg/kg, all tested substances have
significant analgesic effects, and the highest potency was seen with
3, 4 and 5. Increasing the dose of 3 and 5 to 8 mg/kg did not increase
the analgesic effect. In the writhing test, 3 and 5, but not 1, showed
significant results. In a baker's yeast-induced fever model, 3 and 5
significantly reduced rats' rectal temperature (p < 0.05). In a
carrageenan-induced inflammation model, 1, 3 and 5 significantly
reduced rats' paw volume. Doses of 3 and 5 up to 100 mg/kg did not
show any serious toxic effects. From this study, 3 and 5 are the most
interesting derivatives, showing much greater potency than their
parent compounds. These could be further developed as analgesic,
antipyretic and anti-inflammatory agents, without any serious
toxicity.
PMID: 19784573 [PubMed - in process]
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