Planta Med 2019; 85(18): 1487
DOI: 10.1055/s-0039-3399893
Main Congress Poster
Poster Session 1
© Georg Thieme Verlag KG Stuttgart · New York

Investigations of the pharmacological properties of carvotacetones isolated from Sphaeranthus africanus

HT Tran
1   Institute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz,, Universitaetsplatz 4, 8010 Graz, Austria
,
EM Pferschy-Wenzig
1   Institute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz,, Universitaetsplatz 4, 8010 Graz, Austria
,
N Kretschmer
1   Institute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz,, Universitaetsplatz 4, 8010 Graz, Austria
,
X Gao
1   Institute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz,, Universitaetsplatz 4, 8010 Graz, Austria
,
P Raab
1   Institute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz,, Universitaetsplatz 4, 8010 Graz, Austria
,
T Pirker
1   Institute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz,, Universitaetsplatz 4, 8010 Graz, Austria
,
J Solnier
1   Institute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz,, Universitaetsplatz 4, 8010 Graz, Austria
,
F Bucar
1   Institute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz,, Universitaetsplatz 4, 8010 Graz, Austria
,
O Kunert
2   Institute of Pharmaceutical Sciences, Department of Pharmaceutical Chemistry, University of Graz,, Universitaetsplatz 1, 8010 Graz, Austria
,
E Tuenter
3   Natural Products & Food Research and Analysis (NatuRA), Department of Pharmaceutical Sciences, and §Laboratory of Microbiology, Parasitology and Hygiene (LMPH), Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, University of Antwerp,, Universiteitsplein 1, 2610 Antwerp, Belgium
,
L Pieters
3   Natural Products & Food Research and Analysis (NatuRA), Department of Pharmaceutical Sciences, and §Laboratory of Microbiology, Parasitology and Hygiene (LMPH), Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, University of Antwerp,, Universiteitsplein 1, 2610 Antwerp, Belgium
,
L Huynh
4   Department of Botany and Pharmacognosy, Hong Bang International University,, Ho Chi Minh City, Vietnam
,
R Bauer
1   Institute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz,, Universitaetsplatz 4, 8010 Graz, Austria
› Author Affiliations
Further Information

Publication History

Publication Date:
20 December 2019 (online)

Also available at
 

Sphaeranthus africanus has been used in traditional medicine in Vietnam to treat sore throat, alleviate swelling and as a sedative [1].

Aim To evaluate the anti-inflammatory activity of the plant and explore the pharmacological properties of the isolated compounds.

Results Seven carvotacetones were isolated from the dichloromethane extract. All compounds exhibited significant anti-proliferative activity against several cancer cell lines: CCRF-CEM, MDA-MB-231, HCT-116 and U-251 [2]

Compounds 1 and 2 possess potent and selective COX-2 inhibitory activity with IC50 values of 3.6 and 0.5 μM, respectively.

Compounds 1-7 exhibited inhibitory effects on COX-2 gene expression in THP-1 macrophages. Compound 4 is the most active compound inhibiting the synthesis of COX-2 mRNA by 55% at 2.06 μM.

Carvotacetones inhibited NO production in BV2 and RAW cell lines with IC50 values ranging from 0.2 to 2.9 μM. Compound 4 showed potent inhibitory activity with IC50 values of 0.2 μM in both cell lines.

Carvotacetones 1 and 6 exerted strong antibacterial activities (MIC ≤ 31.25 mg/L) against M. aurum and M. bovis BCG. Compound 1 considerably increased the susceptibility of M. smegmatis towards ethidium bromide and rifampicin by an 8- and 2-fold reduction of their MICs.

Compounds 1-6 showed anti-plasmodial activity, with IC50 values ranging from 1.41 to 3.9 μM.

The activities of major constituents of S. africanus support the traditional medical application of this plant for the treatment of inflammation-related disorders. 1-7 may be interesting due to their antiproliferative and anti-plasmodial activities which should be considered for further testing and mechanistic studies.

Zoom Image
Fig. 1 Structures of compounds 1-7