Quantitative Determination of Andrographolide and Related Compounds in Andrographis paniculata Extracts and Biological Evaluation of Their Anti-Inflammatory Activity.

Emmanuelle Villedieu-Percheron,Chantal Pichon,Joana Filomena Campos,Sabine Berteina-Raboin,Emilie Destandau,Véronique Ferreira

doi:10.3390/foods8120683

Abstract

Extraction, isolation and characterization of Andrographis paniculata (A.p.) products were developed. Three natural diterpenes compounds were obtained and one was used for chemical modifications. Evaluation of their inhibition of TNFα induced NFκB transcriptional activity. A rapid analytical method for the determination and quantitation of three diterpenoid lactones (andrographolide 1, didehydroandrographolide 2, neoandrographiside 3) found in A. paniculata extracts was investigated. After some optimizations on column type and injection solvent, the separation was achieved in 9 min on a monolithic Chromolith Performance RP18e column (100 mm × 4.6 mm ID, 2 µm), with a gradient solvent system of water and methanol, UV detection at 220 nm and ELSD detection. The method was proved to be suitable for the quantitation of these three diterpenes in four different commercial Andrographis dietary supplements. The anti-inflammatory activities of a mixture of known composition have been evaluated showing differences in activity depending on the relative ratio of various diterpenes and also a possible synergic activity for some of them.

Highlights

Andrographis paniculata (Acanthaceae) (A.p.) is widely used as medicinal herb in traditional medicine [1,2,3]
In order to understand the mechanism of inhibition of NFκB by andrographolide, andrographolide 1 was treated
B and C where the quantity of 2 is not negligible, the inhibitory activity increases. These results could explain those reported in the literature [31], showing that there were other compounds than andrographolide in A. paniculata extracts that act as an immunostimulant, and we proved that there was a complementary activity of 2 at the studied concentrations

Summary

Introduction

Andrographis paniculata (Acanthaceae) (A.p.) is widely used as medicinal herb in traditional medicine [1,2,3]. Diterpenoid lactones isolated from these extracts have been the subject of intensive investigations and are reported to exhibit a wide spectrum of biological activities, including antibacterial [4], anti-inflammatory [5,6,7,8], hepatoprotective [9,10,11], neuroprotective [12], cardioprotective [13,14] and anticancer properties [15,16]. Andrographolide 1 (Figure 1) has been reported to be the main active compound in the plant [17,18]. Other minor diterpenoid lactones have been isolated from the plant, and their structures have been investigated [21] but their activities are not well studied. Studies about the pharmacological mechanism of its known anti-inflammatory actions have shown in 2004

Methods

Results

Conclusion