Antisickling compounds from Cnidoscolus acontifolius leaf extract

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  J Pharm Pharmacogn Res 8(6): 580-590, 2020. DOI: https://doi.org/10.56499/jppres20.864_8.6.580 Original Article Bioactivity-directed isolation of antisickling compounds from Cnidoscolus acontifolius (Mill.) I.M. Johnst leaf extract [Aislamiento dirigido por bioactividad de compuestos anti-sicklémicos de extracto de hoja de Cnidoscolus acontifolius (Mill.) I.M. Johnst] Mojisola C. Cyril-Olutayo*, Temitope A. Adeyemo, Ayodeji O. Oriola, Joseph M. Agbedahunsi Drug Research and … Continue reading Antisickling compounds from Cnidoscolus acontifolius leaf extract

 

J Pharm Pharmacogn Res 8(6): 580-590, 2020.

DOI: https://doi.org/10.56499/jppres20.864_8.6.580

Original Article

Bioactivity-directed isolation of antisickling compounds from Cnidoscolus acontifolius (Mill.) I.M. Johnst leaf extract

[Aislamiento dirigido por bioactividad de compuestos anti-sicklémicos de extracto de hoja de Cnidoscolus acontifolius (Mill.) I.M. Johnst]

Mojisola C. Cyril-Olutayo*, Temitope A. Adeyemo, Ayodeji O. Oriola, Joseph M. Agbedahunsi

Drug Research and Production Unit, Faculty of Pharmacy, Obafemi Awolowo University, Ile-Ife, Nigeria.
Abstract

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 n-hexane, 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.

Keywords: antisickling; Cnidoscolus aconitifolius; 5β-pregnane; sickle cell anemia; tetramethyl bicosahydropicen-3-ol.

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Resumen

Contexto: Existe una búsqueda continua de agentes terapéuticos a partir de plantas autóctonas que puedan emplearse en el tratamiento de la anemia de células falciformes.

Objetivos: Evaluar el potencial anti-sicklémico del extracto de hoja de Cnidoscolus aconitifolius, determinar la fracción más activa y aislar los compuestos putativos.

Métodos: Se extrajeron hojas secadas al horno de C. aconitifolius (CA) mediante maceración en etanol durante 72 h. El extracto se fraccionó en n-hexano, diclorometano, acetato de etilo y metanol usando cromatografía líquida de vacío (VLC). El extracto crudo de CA y las fracciones se sometieron a ensayos anti-sicklémicos inhibidores y de reversión en un intervalo de concentración de 0,25-4,00 mg/mL. El fraccionamiento dirigido por bioactividad de la fracción más activa se realizó mediante cromatografía en columna de gel de sílice repetida, seguido de cromatografía en capa fina preparativa y sus análisis en cromatografía en capa fina. Los compuestos aislados se caracterizaron utilizando métodos espectroscópicos de resonancia magnética nuclear 1H y 13C, COSY, HMBC, HSQC y LC-MS.

Resultados: Los resultados mostraron que CA tuvo 80,4 ± 0,15% de inhibición y 56,0 ± 2.90% de reversión a 4 mg/mL. La fracción de acetato de etilo proporcionó actividades inhibidoras (68,0 ± 4,32%) y de inversión (61,4 ± 6,2%) a 4 mg/mL mayores que las otras fracciones de VLC (p <0,05). El control positivo Ciklavit® tuvo 59,8 ± 0,3% de inhibición y 56,6 ± 0,2% de reversión. Se aislaron dos compuestos, T1 y T2 de la fracción de acetato de etilo, y se identificaron como tetrametil bicosahidropicen-3-ol y 5β-pregnane, respectivamente. El compuesto T1 demostró un efecto inhibidor del 83,6 ± 0.11%.

Conclusiones: El estudio concluyó que la fracción de acetato de etilo del extracto etanólico de C. aconitifolius tiene la mayor propiedad anti-sicklémica e identificó al tetrametilbicosahidropicen-3-ol como un potencial agente anti-sicklémico.

Palabras Clave: anti-sicklémico; Cnidoscolus aconitifolius; 5β-pregnano; anemia falciforme; tetrametil bicosahidropicen-3-ol.

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Citation Format: Cyril-Olutayo MC, Adeyemo TA, Oriola AO, Agbedahunsi JM (2020) Bioactivity-directed isolation of antisickling compounds from Cnidoscolus acontifolius (Mill.) I.M. Johnst leaf extract. J Pharm Pharmacogn Res 8(6): 580–590. DOI: https://doi.org/10.56499/jppres20.864_8.6.580

© 2020 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

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