Antiplasmodial activity of artecyclopentyl mether a new artemisinin derivative and its effect on pathogenesis in Plasmodium yoelii nigeriensis infected mice

• Published in: Parasitology research (1987) Vol. 109; no. 4; pp. 1003 - 1008
• Main Authors: Agarwal, Jyoti, Singh, Suriya Pratap, Chanda, Debabrata, Bawankule, Dnyaneshwar Umrao, Bhakuni, Rajendra Singh, Pal, Anirban
• Format: Journal Article
• Language: English
• Published: Berlin/Heidelberg Springer-Verlag 01.10.2011; Springer
• Subjects: Anemia; Animals; Antimalarials - administration & dosage; Antimalarials - chemical synthesis; Antimalarials - therapeutic use; Artemisinins - administration & dosage; Artemisinins - chemical synthesis; Artemisinins - therapeutic use; Biological and medical sciences; Biomedical and Life Sciences; Biomedicine; Cytokines - analysis; Cytokines - immunology; Drug Resistance, Multiple; Enzyme-Linked Immunosorbent Assay; Erythrocytes - drug effects; Erythrocytes - parasitology; Female; Fundamental and applied biological sciences. Psychology; General aspects; General aspects and techniques. Study of several systematic groups. Models; Immunology; Interferon; Invertebrates; Lipid peroxidation; Lipid Peroxidation - drug effects; Malaria - drug therapy; Malaria - immunology; Malaria - metabolism; Malaria - mortality; Malaria - pathology; Medical Microbiology; Mice; Microbiology; Nitric oxide; Nitric Oxide - analysis; Nitric Oxide - biosynthesis; Original Paper; Oxidative Stress - drug effects; Parasitemia - drug therapy; Plasmodium yoelii - drug effects; Plasmodium yoelii - physiology; Plasmodium yoelii nigeriensis; Rodent Diseases - drug therapy; Rodent Diseases - immunology; Rodent Diseases - metabolism; Rodent Diseases - mortality; Rodent Diseases - pathology; Survival Rate; Tumor necrosis factor; Antimalarial Activity; Cerebral Malaria; Malaria; Artesunate; Artemisinin; Protozoa; Apicomplexa; Vertebrata; Mammalia; Mouse; Pathogenesis; Rodentia; Parasite; Activity; Plasmodium yoelii nigeriensis
• ISSN: 0932-0113; 1432-1955; 1432-1955
• DOI: 10.1007/s00436-011-2344-1

In an effort to evaluate novel derivatives from artemisinin, possessing potential antimalarial activity, a new derivative artecyclopentyl mether (CPM-1) was derivatized and evaluated for its dose-dependent efficacy in Plasmodium yoelii nigeriensis infected mice. The survivability of mice at 7.5 mg/kg was >28 days with negligible parasitaemia and recovered anemia (66.16–72.62%). Artecyclopentyl mether was also found to modulate the pro- and anti-inflammatory cytokines (IFN-γ, 39.64–56.92%; TNF, 49.10–74.31%; IL-4, 11.53–43.22%; IL-10, 37.60–53.52%) favourably besides optimizing the oxidative stress to the infected subjects as evident by the nitric oxide (88.76–95.43%), lipid peroxidation (59.30–76.05%) and glycaemic data (62.70–76.66%). The results indicate the potentiality of the new derivative as an antimalarial against asexual stages of the parasite.