Article Per Year (5 Year)
p-Index From 2019 - 2024
0
P-Index
This Author published in this journals
All Journal Indonesian Journal of Biotechnology INDONESIAN JOURNAL OF PHARMACY
Alexis Valentin, Alexis
Laboratoire de Parasitologie et Immunologie, Faculte de Pharmacie, Universite de Montpellier I, Montpellier, France
Biochemistry, Genetics & Molecular Biology Immunology & microbiology Materials Science & Nanotechnology Medicine & Pharmacology

Published : 2 Documents Claim Missing Document
Claim Missing Document
Check
Articles

Found 2 Documents
Search

 1 
In vitro Antiplasmodial Activity and Cytotoxicity of Vincadifformine and Its Semisynthetic Derivatives M, Mustofa; Mallié, Michèle; Valentin, Alexis; Lewin, Guy
Indonesian Journal of Biotechnology Vol 11, No 1 (2006)
Publisher : Universitas Gadjah Mada

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (66.057 KB)

Abstract

An indole alkaloid with aspidospemane structure possessing a potential antiplasmodial activity,vincadifformine, has been isolated from Aspidosperma pyrifolium Mart. Moreover, 10 derivatives were preparedfrom the vincadifformine. The study was conducted to evaluate the in vitro antiplasmodial and cytotoxic activity ofthe vincadifformine and their semisynthetic derivatives. The in vitro antiplasmodial activity was evaluated onPlasmodium falciparum chloroquine-resistant (FcM ) and –sensitive (Nigerian) strains after 24-h and 72-h incubation, 29while cytotoxic activity was estimated on Hela cells and Cytotoxicity Index (CI = IC on HeLa cells/IC on FcM strain) 50 50 29was calculated to evaluate the safety of tested compounds. Experiment results showed that two compounds (4 and 8)exhibited good antiplasmodial activities in comparison with parent compound, vincadifformine and other testedcompounds with IC ranging from 5.3 to 12.8 μM on FcM strain and 11.4 to 24.0 μM on Nigerian strain. In addition, 50 29the CI of two compounds were also lower after 24-h incubation (CI, 2.0 and 4.8) than that of after 72-h incubation (CI,9.5 and 11.5). Further study will be conducted to evaluate quantitative structure-activity relationship (QSAR) in orderto design new antimalarial drugs.Keywords : vincadifformine - antiplasmodial – Plasmodium falciparum – cytotoxic - HeLa
In Vivo ANTIPLASMODIAL ACTIVITY AND MECHANISM OF ACTION OF 1,10-PHENANTHROLINE DERIVATIVES ., Mustofa; Yapi, Ange Desire; Valentin, Alexis
Indonesian Journal of Pharmacy Vol 14 No 3, 2003
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (403.296 KB) | DOI: 10.14499/indonesianjpharm0iss0pp142-149

Abstract

The rapidly increasing resistance of Plasmodium falciparum to the most commonly used antimalarial drug indicates the urgent need for new antimalarial compounds. Previous study showed that among thirteen derivatives of 1,10-phenanthroline, four compounds were active in vitro and potential for further development. The study was conducted to provide the in vivo antiplasmodial activity of four 1,10-phenanthroline derivatives and to evaluate the possibility of their mechanism of action. The in vivo antiplasmodial activity of the four compounds was evaluated by a standard 4-day test on Plasmodium venckei petteri infected mice. The study of haem polymerization inhibitory activity (HPIA) and the potentiating of those compounds in combination with halofantrine and inhibitor protease (E64) were carried out to evaluate its mechanism of actions. The results showed that among four compounds tested, compound 1 (2,10-methyl-3-(2-chloroethyl)-4-chloropirydo [2,3-i] quinolineium iodide) was the most active compound with DE50 was 0.22 ± 0.03 mg/kg BW. This molecule less active than halofantrine, but more active than chloroquine. The HPIA of 1,10-phenanthroline derivatives tested (IC50 HPIA was 1.57-1.95 mmol/well) did not vary significantly. These IC50 HPIA values were significantly lower than halofantrine (CI50 HPIA was 0.12 ± 0.04 mmol/well) and than chloroquine (CI50 HPIA was 0.75 ± 0.03 mmol/well). Combination the 1,10-phenanthroline derivatives and halofantrine produced simple additive effect that implies that each drug posses a different mechanism of action. Conversely, there was antagonist interaction between 1,10-phenanthroline derivatives and E64 showing that the drugs have a similar mechanism of action. It can be concluded that the compound 1 appears as a potential antimalarial compound. In addition, the possible mechanism of action of this compound is inhibitation of protease involved in haemoglobine degradation within the malaria parasite.Key words : 1,10-phenanthroline – in vivo antiplasmodial – haem polymerization inhibitoryactivity – protease inhibitor .
Co-Authors Ange Desire Yapi, Ange Desire Guy Lewin, Guy Michèle Mallié, Michèle Mustofa M, Mustofa Mustofa Mustofa