Structure Elucidation Of Antitrypanosomal Compounds From Archidendron Clypearia (Jack) I.C Nielsen Ssp. Clypearia Var. Clypearia Leaf Extracts

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Date
2017-08
Authors
Amanah, Azimah
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Publisher
Universiti Sains Malaysia
Abstract
Human African Trypanosomiasis (HAT), also known as sleeping sickness, which is caused by a protozoan parasite, can cause death if not treated. Trypanosoma brucei rhodesiense has been used as a model in this study. Currently, the medications used for treatment of this ailment such as pentamidine, melarsoprol, suramine and eflornithineare problematic because these compound are toxic, expensive and ineffective when the disease has reached an advanced stage. Therefore, screening of antitrypanosomal and cytotoxicity activities were conducted on the plant leaf extracts and the isolated compounds of Archidendron clypearia (Jack) IC Nielsen ssp. clypearia var. clypearia (A.clypearia) against Trypanosoma brucei rhodesiense and rat skeletal muscle cell (L-6) by using Alamar Blue assay. The isolation and identification process of active compounds from the leaves of A. clypearia was carried out using bioassay guided isolation approach. The methanol extract of this plant has been found to be active against trypanosome with an IC50 value of 0.44 + 0.46 μg/ml [Selective Index (SI): 129.58]. Liquid-liquid extraction of the methanol extract was carried out and resulted in hexane, diethyl ether (DE) and ethyl acetate (EtOAC) extracts which showed IC50 values of 2.32 +1.19 μg/ml (SI: 23.11), 0.42 + 0.32 μg/ml (SI: 44.03) and 2.02+0.27μg/ml (SI: 6.84) respectively. The active diethyl ether extract was subjected to column chromatography and characterized using analytical and spectroscopy analysis such as HPLC, TLC, NMR, IR and MS. An active antitrypanosomal compound (AC-AA1) methyl-3,4,5- trihydroxybenzoate with an IC50 value of 0.38 + 0:35 μg/ml (SI: 142.22) while (ACAA2) mixture compound 7-O-galloyltricetiflavan [with an IC50 value of 0.53 + 0.40 μg/ml (SI: 34.74)] and a pure compound (AC-AA3) 7-4’-O-di-galloyltricetiflavan [with an IC50 value of 0.57 + 0.27 μg/ml (SI: 34.82)] respectively showed moderate antitrypanosomal activity were isolated from A. clypearia.
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Keywords
Human African Trypanosomiasis , caused by a protozoan parasite
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