Antimalarial Activity of Acetylenic Thiophenes from Echinops hoehnelii Schweinf
Abstract
:1. Introduction
2. Results and Discussion
2.1. Acute Oral Toxicity
2.2. Antimalarial Activity of 80% Methanol Root Extract of E. hoehnelii
2.3. Antimalarial Activity of Fractions
2.4. Isolation and Structural Elucidation of Compounds from the Dichloromethane Fraction
2.5. Antimalarial Activity of Isolated Compounds
3. Materials and Methods
3.1. General
3.2. Plant Material
3.3. Experimental Animals and Parasite
3.4. Preparation of Extract and Fractions
3.5. Isolation of Compounds
3.6. Acute Oral Toxicity Test
3.7. Antimalarial Activity Test of 80% Methanol Root Extract of E. hoehnelii
3.8. Antimalarial Activity Test of the Fractions
3.9. Antimalarial Activity of Isolated Compounds
3.10. Data Analyses
4. Conclusions
Supplementary Materials
Acknowledgments
Author Contributions
Conflicts of Interest
References
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Sample Availability: Samples of the compounds are available from the authors. |
Dose | % Parasitaemia ± SD | % Suppression | Mean Survival Time (Days) ± SD |
---|---|---|---|
Vehicle | 24.2 ± 2.3 | - | 6.4 ± 0.9 |
50 mg/kg | 23.1 ± 2.5 | 4.6 b3d1e3f3 | 7 ± 0.7 b3 |
100 mg/kg | 17.5 ± 5.4 | 27.8 a2b3c1e3f3 | 7.4 ± 0.5 b3 |
200 mg/kg | 7.6 ± 0.9 | 68.5 a3b2c3d3 | 7.8 ± 1.1 b3 |
400 mg/kg | 5.2 ± 1.2 | 78.7 a3c3d3 | 8 ± 0.7 a1b3 |
CQ (25 mg/kg) | 0 ± 0.00 | 100 a3c3d3e2 | >28 a3c3d3e3f3 |
Dose | Wt (g) D0 ± SD | Wt (g) D4 ± SD | % Change |
---|---|---|---|
Vehicle | 25.6 ± 0.3 | 24.9 ± 1.1 | −2.5 |
50 mg/kg | 25.0 ± 0.2 | 25.7 ± 2.1 | 2.9 |
100 mg/kg | 25.1 ± 0.3 | 25.7 ± 1.2 | 2.5 |
200 mg/kg | 25.6 ± 0.2 | 26.1 ± 0.6 | 2.3 |
400 mg/kg | 24.9 ± 0.7 | 25.6 ± 0.3 | 3.0 |
CQ (25 mg/kg) | 23.9 ± 0.3 | 26.8 ± 0.6 | 12.0 3 |
Fraction | Dose (mg/kg/Day) | % Parasitaemia ± SD | % Suppression | Mean Survival Time (Days) ± SD |
---|---|---|---|---|
Hexane | 100 | 28.2 ± 11.7 | 11.6 b3 | 7.2 ± 0.8 b3 |
Hexane | 200 | 27.8 ± 1.5 | 12.9 b3 | 8.2 ± 0.8 a2b3 |
Hexane | 400 | 22.6 ± 3.3 | 29.1 b3 | 8.2 ± 0.8 a2b3 |
Vehicle | 0.5 mL | 31.9 ± 3.00 | 0 | 6.4 ± 0.5 |
CQ | 25 | 0.00 ± 0.00 | 100 a3c3d3e3 | >28 ± 0.00 a3c3d3e3 |
Dichloromethane | 100 | 32.3 ± 2.5 | 24.8 a3b3e3 | 8.0 ± 1.9 b3 |
Dichloromethane | 200 | 28.6 ± 1.8 | 33.5 a3b3e3 | 8.4 ± 1.9 b3 |
Dichloromethane | 400 | 24.5 ± 1.5 | 43.0 a3b3c3d1 | 9.0 ± 0.7 a1b3 |
Vehicle | 0.5 mL | 43.00 ± 2.9 | 0 | 7.0 ± 1.6 |
CQ | 25 | 0.00 ± 0.00 | 100 a3c3d3e3 | >28 ± 0.00 a3c3d3e3 |
Ethyl acetate | 100 | 37.3 ± 7.3 | 9.8 b3 | 7.25 ± 1.3 b3 |
Ethyl acetate | 200 | 37.0 ± 1.6 | 10.5 b3 | 7.0 ± 1.3 b3 |
Ethyl acetate | 400 | 39.4 ± 2.1 | 4.80 b3 | 6.4 ± 0.9 b3 |
Vehicle | 0.5 mL | 41.4 ± 4.0 | 0.00 | 6.54 ± 1.3 |
CQ | 25 | 0.00 ± 0.00 | 100 a3c3d3e3 | >28 ± 0.00 a3c3d3e3 |
Aqueous | 100 | 33.2 ± 4.0 | 19.8 b3 | 7.6 ± 1.3 b3 |
Aqueous | 200 | 38.1 ± 15.1 | 7.8 b3 | 6.80 ± 1.3 b3 |
Aqueous | 400 | 40.0 ± 1.4 | 3.3 b3 | 6.80 ± 0.1 b3 |
Vehicle | 0.5 mL | 41.4 ± 4.0 | 0.00 | 6.54 ± 1.3 |
CQ | 25 | 0.00 ± 0.00 | 100 a3c3d3e3 | >28 ± 0.00 a3c3d3e3 |
Fraction | Dose (mg/kg/Day) | Wt (g) D0 ± SD | Wt (g) D4 ± SD | % Change |
---|---|---|---|---|
Hexane | 100 | 25.6 ± 0.2 | 26.0 ± 0.4 | 1.5 |
Hexane | 200 | 25.5 ± 1.3 | 26.2 ± 0.5 | 2.4 |
Hexane | 400 | 25.4 ± 0.3 | 26.3 ± 1.1 | 3.7 |
Vehicle | 0.5 mL | 26.2 ± 0.2 | 24.5 ± 0.5 | −6.3 2 |
CQ | 25 | 25.4 ± 0.5 | 26.5 ± 0.3 | 4.2 2 |
Dichloromethane | 100 | 28.3 ± 3.0 | 29.0 ± 1.5 | 2.6 |
Dichloromethane | 200 | 26.8 ± 3.4 | 27.7 ± 3.7 | 3.5 |
Dichloromethane | 400 | 25.9 ± 3.3 | 27.1 ± 3.7 | 4.7 |
Vehicle | 0.5 mL | 27.9 ± 3.00 | 26.3 ± 4.4 | −5.8 |
CQ | 25 | 25.4 ± 0.5 | 26.5 ± 0.3 | 4.2 2 |
Ethyl acetate | 100 | 26.2 ± 0.7 | 26.4 ± 1.6 | 0.6 |
Ethyl acetate | 200 | 25.0 ± 2.5 | 26.1 ± 2.5 | 4.3 |
Ethyl acetate | 400 | 25.6 ± 2.6 | 26.5 ± 3.1 | 3.4 |
Vehicle | 0.5 mL | 26.8 ± 3.5 | 26.1 ± 5.9 | −2.5 |
CQ | 25 | 28.8 ± 5.1 | 29.8 ± 4.5 | 3.6 |
Aqueous | 100 | 25.8 ± 2.1 | 26.7 ± 1.8 | 3.3 |
Aqueous | 200 | 25.1 ± 2.5 | 25.7 ± 2.4 | 2.8 |
Aqueous | 400 | 27.2 ± 2.3 | 27.9 ± 2.5 | 2.5 |
Vehicle | 0.5 mL | 26.8 ± 3.5 | 26.1 ± 5.9 | −2.5 |
CQ | 25 | 28.8 ± 5.1 | 29.8 ± 4.5 | 3.6 |
Test | Dose | %Parasitaemia ± SD | % Suppression | Mean Survival Time (Days) ± SD |
---|---|---|---|---|
EH-1 | 50 mg/kg | 23.5 ± 2.1 | 43.2 a3b3 | 9.4 ± 1.5 a1b3 |
EH-1 | 100 mg/kg | 15.3 ± 8.7 | 50.2 a3b3 | 9.7 ± 1.5 a1b3 |
Vehicle | 0.5 mL | 30.8 ± 6.5 | 0 | 7.2 ± 1.2 |
CQ | 25 mg/kg | 0.00 ± 0.00 | 100 a3c3d3 | >28 a3c3d3 |
EH-5 | 50 mg/kg | 28.0 ± 3.2 | 18.8 b3 | 7.2 ± 1.0 b3 |
EH-5 | 100 mg/kg | 23.2 ± 5.3 | 32.7 a2b3 | 7.8 ± 1.3 b3 |
Vehicle | 0.5 mL | 34.4 ± 3.9 | 0 | 7.2 ± 0.8 |
CQ | 25 mg/kg | 0.00 ± 0.00 | 100 a3c3d3 | >28 a3c3d3 |
Test | Dose | Wt(g) D0 ± SD | Wt (g) D4 ± SD | % Change |
---|---|---|---|---|
EH-1 | 50 mg/kg | 26.3 ± 2.4 | 26.6 ± 1.6 | 1.1 |
EH-1 | 100 mg/kg | 22.4 ± 1.9 | 22.6 ± 1.6 | 0.8 |
Vehicle | 0.5 mL | 23.5 ± 1.6 | 23.1 ± 1.8 | −1.5 |
CQ | 25 mg/kg | 27.6 ± 2.5 | 28.8 ± 2.7 | 4.4 1 |
EH-5 | 50 mg/kg | 22.0 ± 1.0 | 22.2 ± 2.1 | 0.9 |
EH-5 | 100 mg/kg | 24.2 ± 2.6 | 25.4 ± 3.0 | 4.9 |
Vehicle | 0.5 mL | 24.0 ± 3.3 | 23.6 ± 2.9 | −1.7 |
CQ | 25 mg/kg | 21.8 ± 1.6 | 24.1 ± 2.6 | 10.6 1 |
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Bitew, H.; Mammo, W.; Hymete, A.; Yeshak, M.Y. Antimalarial Activity of Acetylenic Thiophenes from Echinops hoehnelii Schweinf. Molecules 2017, 22, 1965. https://doi.org/10.3390/molecules22111965
Bitew H, Mammo W, Hymete A, Yeshak MY. Antimalarial Activity of Acetylenic Thiophenes from Echinops hoehnelii Schweinf. Molecules. 2017; 22(11):1965. https://doi.org/10.3390/molecules22111965
Chicago/Turabian StyleBitew, Helen, Wendimagegn Mammo, Ariaya Hymete, and Mariamawit Yonathan Yeshak. 2017. "Antimalarial Activity of Acetylenic Thiophenes from Echinops hoehnelii Schweinf" Molecules 22, no. 11: 1965. https://doi.org/10.3390/molecules22111965