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8365031 
Journal Article 
Aislamiento dirigido por bioactividad de compuestos anti-sicklémicos de extracto de hoja de Cnidoscolus acontifolius (Mill.) I.M. Johns 
Cyril-Olutayo, MC; Adeyemo, TA; Oriola, AO; Agbedahunsi, JM 
2020 
Academic Association of Pharmaceutical Sciences from Antofagasta (ASOCIFA) 
8 
6 
580-590 
English 
Context: There is continuous search for therapeutic agents from indigenous plants that can be employed in the treatment of sickle cell anemia. Aims: To evaluate the antisickling potential of Cnidoscolus aconitifolius leaf extract, determine the most active fraction, and isolate the putative compounds. Methods: Oven dried leaves of C. aconitifolius (CA) were extracted by maceration in ethanol for 72 h. The extract was fractionated into nhexane, dichloromethane, ethyl acetate and methanol using vacuum liquid chromatography (VLC). The crude CA extract and fractions were subjected to inhibitory and reversal antisickling assays at 0.25-4.00 mg/mL concentration range. Bioactivity-directed fractionation of the most active fraction was done on repeated silica gel column chromatography, followed by preparative thin-layer chromatography, and their analyses on thin-layer chromatography. The isolated compounds were characterized using spectroscopic methods of 1H- and 13C- Nuclear Magnetic Resonance, COSY, HMBC, HSQC, and LC-MS. Results: The results showed that CA had 80.4 ± 0.15% inhibitory and 56.0 ± 2.90% reversal effects at 4 mg/mL. The ethyl acetate fraction gave significantly higher (p<0.05) inhibitory (68.0 ± 4.32%) and reversal (61.4 ± 6.2%) activities at 4 mg/mL than the other VLC fractions. The positive control Ciklavit® had 59.8 ± 0.3% inhibitory and 56.6 ± 0.2% reversal properties. Two compounds, T1 and T2 were isolated from the ethyl acetate fraction and identified as tetramethyl bicosahydropicen-3-ol and 5β-pregnane, respectively. Compound T1 demonstrated an inhibitory effect of 83.6 ± 0.11%. Conclusions: The study concluded that the ethyl acetate fraction of the ethanol extract of C. aconitifolius has the highest antisickling property and identified tetramethylbicosahydropicen-3-ol as a potential antisickling agent. © 2020 Academic Association of Pharmaceutical Sciences from Antofagasta (ASOCIFA). All rights reserved. 
5β-pregnane; Antisickling; Cnidoscolus aconitifolius; Sickle cell anemia; Tetramethyl bicosahydropicen-3-ol