RESUMEN
Thiosemicarbazones have become one of the promising compounds as new clinical candidates due to their wide spectrum of pharmaceutical activities. The wide range of their biological activities depends generally on their related aldehyde or ketone groups. Here, we report the pharmacological activities of some thiosemicarbazones synthesized in this work. Benzophenone and derivatives were used with N(4)-phenyl-3-thiosemicarbazide to synthesize corresponding five thiosemicarbazones (1-5). Their structures were characterized by spectrometrical methods analysis IR, NMR (1)H & (13)C and MS. The compounds were then screened in vitro for their antiparasitic activity and toxicity on Trypanosoma brucei brucei and Artemia salina Leach respectively. The selectivity index of each compound was also determined. Four thiosemicarbazones such as 4, 2, 3 and 1 reveal interesting trypanocidal activities with their half inhibitory concentration (IC50) equal to 2.76, 2.83, 3.86 and 8.48 µM respectively, while compound 5 (IC50 = 12.16 µM) showed a moderate anti-trypanosomal activity on parasite. In toxicity test, except compound 1, which showed a half lethal concentration LC50 >281 µM, the others exerted toxic effect on larvae with LC50 of 5.56, 13.62, 14.55 and 42.50 µM respectively for thiosemicarbazones 4, 5, 3 and 2. In agreement to their selectivity index, which is greater than 1 (SI >1), these compounds clearly displayed significant selective pharmaceutical activities on the parasite tested. The thiosemicarbazones 2-5 that displayed significant anti-trypanosomal and cytoxicity activities are suggested to have anti-neoplastic and anti-cancer activities.
Asunto(s)
Artemia/efectos de los fármacos , Tiosemicarbazonas/farmacología , Trypanosoma brucei brucei/efectos de los fármacos , Tripanosomiasis Africana/tratamiento farmacológico , Animales , Humanos , Tiosemicarbazonas/síntesis química , Trypanosoma brucei brucei/patogenicidad , Tripanosomiasis Africana/parasitología , Tripanosomiasis Africana/patologíaRESUMEN
BACKGROUND: Since ancient times, invertebrates have played an important role in the traditional medicine in many parts of the world. In south-eastern Benin, more specifically in the Plateau Department, invertebrates are widely used in folk medicine. However, studies on their therapeutic use has been neglected and their magical-religious purposes are poorly understood. The present study aims to document traditional knowledge related to the use of invertebrates for medicinal and magical-religious purposes by traditional healers and indigenous people of Plateau Department. METHODS: An ethno-sociological survey was conducted with 145 informants (80 traditional healers, 12 merchants of medicinal animals and 53 households) belonging to six ethnic groups, in 20 villages located in Plateau of Benin. Data were collected through the participatory rural appraisal method involving individual interviews and direct observations with semi-structured questionnaires. The collected data regarding various medicinal and magical-religious uses of invertebrates were analysed through informant consensus factor (ICF), use value (UV) and, fidelity level (FL). RESULTS: A total of 20 families and 38 species of invertebrates, distributed among 6 taxonomic categories, were found to be used to treat 50 different ailments. Insects occupied 64.7% of the total invertebrates listed. The African earthworm Eudrilus eugeniae K. and African giant snail Achatina achatina L. had the highest use values. The highest ICF value (1.0) was cited for diseases of the blood or blood-forming organs. A principal component analysis (PCA) revealed the influence of ethnic groups in the diseases treated with invertebrates. The highest FL (100%) was recorded for 12 invertebrate species treating various ailments. Most of invertebrate-based remedies were associated with plant species. The mode of administration was mainly oral and topical. Most of the invertebrate drugs were traditionally collected in nature or imported, mainly from Nigeria. In addition, 7 magical-religious practices are documented. CONCLUSIONS: Our results reveal that several invertebrate species play an important role in healing practices and magical-religious rituals in the Plateau Department. We suggest further studies to confirm the presence of any bioactive compounds on invertebrate species use in traditional medicine. In addition, this study highlights the need for ecological investigations of these species, in order to develop strategies for their conservation and sustainable use.