Analgesic, antipyretic, anti-inflammatory and toxic effects of andrographolide derivatives in experimental animals.

Full Abstract

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.

Author information

Author/s: Suebsasana, Supawadee (S); Pongnaratorn, Panicha (P); Sattayasai, Jintana (J); Arkaravichien, Tarinee (T); Tiamkao, Siriporn (S); Aromdee, Chantana (C);

Affiliation: Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen, Thailand.

Journal and publication information

Publication Type: Journal Article; Research Support, Non-U.S. Gov't

Journal: Archives of pharmacal research (Arch Pharm Res), published in Korea (South). (Language: eng)

Reference: 2009-Sep; vol 32 (issue 9) : pp 1191-200

Dates: Created 2009/09/28; Completed 2009/10/15;

PMID: 19784573, status: MEDLINE (last retrieval date: 10/15/2009, IMS Date: )

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