Data in Brief | |
Structural and antitrypanosomal data of different carbasones of piperitone | |
Simeon O. Kotchoni1  Urbain C. Kasséhin2  Amoussatou Sakirigui3  Georges C. Accrombessi3  Fernand Gbaguidi3  Jacques Poupaert4  | |
[1] Department of Biology, Rutgers University, 315 Penn St., Camden, NJ 08102, USA;Laboratoire de Chimie Pharmaceutique Organique, Faculté des Sciences de la Santé, Université d׳Abomey-Calavi, Campus du Champ de Foire, 01 BP 188, Cotonou, Bénin;University of Abomey-Calavi (UAC), Faculty of Sciences and Technics (FAST), Department of Chemistry, Laboratory of Physic and Synthesis Organic Chemistry (LaCOPS), 01 PB: 4521, Cotonou, Benin;Université catholique de Louvain (UCL), Louvain Drug Research Institute (LDRI), B1 7203 Av. E. Mounier 72, B-1200 Bruxelles, Belgium; | |
关键词: Hemi-synthesized; Piperitone carbazones; Essential oil; Cymbopogon shoenantus; Trypanosoma brucei brucei; Artemia salina; | |
DOI : 10.1016/j.dib.2016.11.044 | |
来源: DOAJ |
【 摘 要 】
This article reports data on four carbazones of piperitone: semicarbazone 1, thiosemicarbazone 2, 4-phenyl semicarbazone 3 and 4-phenyl thiosemicarbazone 4 prepared directly in situ from essential oil of Cymbopogon schoenantus, whose GC-FID and GC–MS analysis revealed piperitone as major component (68.20%). The structures of hemi-synthesized compounds were confirmed by high throughput IR, MS, 1H and 13C NMR based spectrometric analysis. Their antiparasitic activities were evaluated in vitro on Trypanosoma brucei brucei (Tbb). The compound 3 (IC50=8.63±0.81 µM) and 4 (IC50=10.90±2.52 µM) exhibited antitrypanosomal activity, 2 had a moderate activity (IC50=74.58±4.44 µM) but 1 was void of significant activity (IC50=478.47 µM). The in vitro tests showed that all compounds were less cytotoxic against the human non cancer fibroblast cell line (WI38) (IC50>80 µM) while only 2 (IC50=21.16±1.37 μM) and 4 (IC50=32.22±1.66 µM) were cytotoxic against the Chinese Hamster Ovary (CHO) cells and toxic on Artemia salina (Leach) larvae. Piperitone 4-phenyl semicarbazone 3, the best antitrypanosomal compound, showed also a selectivity index (SI) higher than 7 on the larvae and the tested cells and therefore might be further studied as antitrypanosomal agent. Also, all compounds except 3 showed selectivity between the two tested cell lines (SI>2). This data reveals for the first time the antitrypinosomal properties of thiosemicarbazones, their cytotoxicity on mammalian cells as well as their activities against Tbb and A. salina Leach.
【 授权许可】
Unknown