Bioactivity-directed isolation of antisickling compounds from Cnidoscolus acontifolius (Mill.) I.M. Johnst leaf extract
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 compo...
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| Format: | Article |
| Language: | English |
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GarVal Editorial Ltda.
2020-11-01
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| Series: | Journal of Pharmacy & Pharmacognosy Research |
| Subjects: | |
| Online Access: | http://jppres.com/jppres/pdf/vol8/jppres20.864_8.6.580.pdf |
| _version_ | 1828288998321160192 |
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| author | Mojisola C. Cyril-Olutayo Temitope A. Adeyemo Ayodeji O. Oriola Joseph M. Agbedahunsi |
| author_facet | Mojisola C. Cyril-Olutayo Temitope A. Adeyemo Ayodeji O. Oriola Joseph M. Agbedahunsi |
| author_sort | Mojisola C. Cyril-Olutayo |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-04-13T10:13:56Z |
| format | Article |
| id | doaj.art-535ada5076d84484a036eaf252f7a5a4 |
| institution | Directory Open Access Journal |
| issn | 0719-4250 |
| language | English |
| last_indexed | 2024-04-13T10:13:56Z |
| publishDate | 2020-11-01 |
| publisher | GarVal Editorial Ltda. |
| record_format | Article |
| series | Journal of Pharmacy & Pharmacognosy Research |
| spelling | doaj.art-535ada5076d84484a036eaf252f7a5a42022-12-22T02:50:48ZengGarVal Editorial Ltda.Journal of Pharmacy & Pharmacognosy Research0719-42502020-11-0186580590Bioactivity-directed isolation of antisickling compounds from Cnidoscolus acontifolius (Mill.) I.M. Johnst leaf extractMojisola C. Cyril-Olutayo0Temitope A. Adeyemo1Ayodeji O. Oriola2Joseph M. Agbedahunsi3Drug Research and Production Unit, Faculty of Pharmacy, Obafemi Awolowo University, Ile-Ife, Nigeria.Drug Research and Production Unit, Faculty of Pharmacy, Obafemi Awolowo University, Ile-Ife, Nigeria.Drug Research and Production Unit, Faculty of Pharmacy, Obafemi Awolowo University, Ile-Ife, Nigeria.Drug Research and Production Unit, Faculty of Pharmacy, Obafemi Awolowo University, Ile-Ife, Nigeria.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.http://jppres.com/jppres/pdf/vol8/jppres20.864_8.6.580.pdfantisicklingcnidoscolus aconitifolius5β-pregnanesickle cell anemiatetramethyl bicosahydropicen-3-ol |
| spellingShingle | Mojisola C. Cyril-Olutayo Temitope A. Adeyemo Ayodeji O. Oriola Joseph M. Agbedahunsi Bioactivity-directed isolation of antisickling compounds from Cnidoscolus acontifolius (Mill.) I.M. Johnst leaf extract Journal of Pharmacy & Pharmacognosy Research antisickling cnidoscolus aconitifolius 5β-pregnane sickle cell anemia tetramethyl bicosahydropicen-3-ol |
| title | Bioactivity-directed isolation of antisickling compounds from Cnidoscolus acontifolius (Mill.) I.M. Johnst leaf extract |
| title_full | Bioactivity-directed isolation of antisickling compounds from Cnidoscolus acontifolius (Mill.) I.M. Johnst leaf extract |
| title_fullStr | Bioactivity-directed isolation of antisickling compounds from Cnidoscolus acontifolius (Mill.) I.M. Johnst leaf extract |
| title_full_unstemmed | Bioactivity-directed isolation of antisickling compounds from Cnidoscolus acontifolius (Mill.) I.M. Johnst leaf extract |
| title_short | Bioactivity-directed isolation of antisickling compounds from Cnidoscolus acontifolius (Mill.) I.M. Johnst leaf extract |
| title_sort | bioactivity directed isolation of antisickling compounds from cnidoscolus acontifolius mill i m johnst leaf extract |
| topic | antisickling cnidoscolus aconitifolius 5β-pregnane sickle cell anemia tetramethyl bicosahydropicen-3-ol |
| url | http://jppres.com/jppres/pdf/vol8/jppres20.864_8.6.580.pdf |
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