Archives of Pharmacal Research

, Volume 32, Issue 9, pp 1191–1200 | Cite as

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

  • Supawadee Suebsasana
  • Panicha Pongnaratorn
  • Jintana Sattayasai
  • Tarinee Arkaravichien
  • Siriporn Tiamkao
  • Chantana Aromdee
Research Articles Drug Design

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.

Key words

Andrographolide derivatives Antipyretic Analgesic Anti-inflammatory Acute toxicity 

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Copyright information

© The Pharmaceutical Society of Korea and Springer Netherlands 2009

Authors and Affiliations

  • Supawadee Suebsasana
    • 1
    • 3
  • Panicha Pongnaratorn
    • 2
  • Jintana Sattayasai
    • 2
  • Tarinee Arkaravichien
    • 2
  • Siriporn Tiamkao
    • 2
  • Chantana Aromdee
    • 1
  1. 1.Pharmaceutical Chemistry, Faculty of Pharmaceutical SciencesKhon Kaen UniversityKhon KaenThailand
  2. 2.Department of Pharmacology, Faculty of MedicineKhon Kaen UniversityKhon KaenThailand
  3. 3.Pharmaceutical Chemistry, Faculty of Pharmaceutical SciencesKhon Kaen UniversityKhon KaenThailand

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