Investigations on the anti-inflammatory activity of Cardiospermum halicacabum

Cardiospermum halicacabum L. (Sapindaceae), known also as balloon vine, is an important medicinal plant used in European phytotherapy and in Ayurveda for the treatment of a variety of inflammatory diseases like rheumatism, arthritis and atopic dermatitis [1]. The aim of this study was to investigate the anti-inflammatory effects of C. halicacabum. Enzymatic in-vitro assays using COX-1 from ram seminal vesicles and human recombinant COX-2 were performed in a 96-well plate format to test the inhibitory activities of the extract and its fractions (n-hexane, dichloromethane, ethyl acetate and n-butanol), as previously described [2]. Indomethacin and celecoxib were used as positive controls. NF-κB inhibitory activity of the extract and fractions of C. halicacabum was evaluated by SEAP (secreted embryonic alkaline phosphatase) reporter assay in the HEK-Blue hTLR4 cell line. BMS-3445541 was used as positive control. Cardiospermum extract showed potent COX-1 and COX-2 enzyme inhibitory activity with IC₅₀ values of 24.9 and 4.1 μg/ml, respectively. All extract fractions exhibited a considerable COX-2 inhibitory effect at a concentration of 5.0 μg/ml, whereas only the n-hexane and dichloromethane fractions showed a relevant COX-1 inhibitory effect at 5.0 μg/ml. Cardiospermum extract and all of the fractions suppressed cell viability of HEK-Blue cells at all concentrations. Only the dichloromethane and n-butanol fractions at concentrations of 5.7 and 3.7 μg/ml, respectively, exhibited an inhibitory effect on SEAP without showing cytotoxicity. In both experiments the aqueous fraction did not exhibit any effect. Investigations are in progress to elucidate the anti-inflammatory active constituents.

Acknowledgement: We are grateful for the funding of the project by Dr. Willmar Schwabe GmbH & Co. KG.

Publication History

Article published online:
13 December 2021

• References

• 1 DOI: 10.1016/j.jep.2010.11.005
• 2 DOI: 10.1016/j.sajb.2018.03.007