Analgesic, Anti-Inflammatory, Antipyretic and Haematological Effects of Aethiopinone, an o-Naphthoquinone Diterpenoid from Salvia aethiopis Roots and two Hemisynthetic Derivatives

Abstract

Aethiopinone (1), an o-naphthoquinone diterpene from Salvia aethiopis L. roots and two hemisynthetic derivatives 2 and 3 have been evaluated for toxicity, anti-inflammatory, analgesic, antipyretic, and haemostatic activities. The compounds tested showed low toxicity and a pharmacological profile similar to other NSAI substances on reducing the edema induced by carrageenan and contractions induced by phenyl-p-quinone; the most active compounds were 1 and 2. In the same way and as expected with these types of substances, the bleeding time increased. In the TPA-induced ear inflammation model, the three compounds showed a moderate reduction of edema, and 1 produced a significant increase in the reaction time against thermal painful stimuli in the tail immersion test. The results demonstrated strong anti-inflammatory, peripheral and central analgesic properties for 1, as well as antiedematose topical action and peripheral analgesic properties for 2 and 3.

Key words

Aethiopinone - Salvia aethiopis L. - Labiatae - diterpenoids - analgesic - anti-inflammatory - haematological activity