A1 Vertaisarvioitu alkuperäisartikkeli tieteellisessä lehdessä
Antispasmodic Effect of Alstonia boonei De Wild. and Its Constituents: Ex Vivo and In Silico Approaches
Tekijät: Akinmurele, Opeyemi Josephine; Sonibare, Mubo Adeola; Elujoba, Anthony A.; Ogunlakin, Akingbolabo Daniel; Yeye, Oloruntoba Emmanuel; Gyebi, Gideon Ampoma; Ojo, Oluwafemi Adeleke; Alanzi, Abdullah R.
Kustantaja: MDPI
Kustannuspaikka: BASEL
Julkaisuvuosi: 2023
Journal: Molecules
Tietokannassa oleva lehden nimi: MOLECULES
Lehden akronyymi: MOLECULES
Artikkelin numero: 7069
Vuosikerta: 28
Numero: 20
Sivujen määrä: 23
eISSN: 1420-3049
DOI: https://doi.org/10.3390/molecules28207069
Tiivistelmä
Background: Alstonia boonei, belonging to the family Apocynaceae, is one of the best-known medicinal plants in Africa and Asia. Stem back preparations are traditionally used as muscle relaxants. This study investigated the antispasmodic properties of Alstonia boonei Stem back and its constituents. Method: The freeze-dried aqueous Stem back extract of A. boonei, as well as dichloromethane (DCM), ethyl acetate, and aqueous fractions, were evaluated for their antispasmodic effect via the ex vivo method. Two compounds were isolated from the DCM fraction using chromatographic techniques, and their antispasmodic activity was evaluated. An in silico study was conducted by evaluating the interaction of isolated compounds with human PPARgamma-LBD and human carbonic anhydrase isozyme. Results: The Stem back crude extract, DCM, ethyl acetate, and aqueous fractions showed antispasmodic activity on high-potassium-induced (K+ 80 mM) contractions on isolated rat ileum with IC50 values of 0.03 +/- 0.20, 0.02 +/- 0.05, 0.03 +/- 0.14, and 0.90 +/- 0.06 mg/mL, respectively. The isolated compounds from the DCM fraction were beta-amyrin and boonein, with only boonein exhibiting antispasmodic activity on both high-potassium-induced (IC50 = 0.09 +/- 0.01 mu g/mL) and spontaneous (0.29 +/- 0.05 mu g/mL) contractions. However, beta-amyrin had a stronger interaction with the two proteins during the simulation. Conclusion: The isolated compounds boonein and beta-amyrin could serve as starting materials for the development of antispasmodic drugs.
Background: Alstonia boonei, belonging to the family Apocynaceae, is one of the best-known medicinal plants in Africa and Asia. Stem back preparations are traditionally used as muscle relaxants. This study investigated the antispasmodic properties of Alstonia boonei Stem back and its constituents. Method: The freeze-dried aqueous Stem back extract of A. boonei, as well as dichloromethane (DCM), ethyl acetate, and aqueous fractions, were evaluated for their antispasmodic effect via the ex vivo method. Two compounds were isolated from the DCM fraction using chromatographic techniques, and their antispasmodic activity was evaluated. An in silico study was conducted by evaluating the interaction of isolated compounds with human PPARgamma-LBD and human carbonic anhydrase isozyme. Results: The Stem back crude extract, DCM, ethyl acetate, and aqueous fractions showed antispasmodic activity on high-potassium-induced (K+ 80 mM) contractions on isolated rat ileum with IC50 values of 0.03 +/- 0.20, 0.02 +/- 0.05, 0.03 +/- 0.14, and 0.90 +/- 0.06 mg/mL, respectively. The isolated compounds from the DCM fraction were beta-amyrin and boonein, with only boonein exhibiting antispasmodic activity on both high-potassium-induced (IC50 = 0.09 +/- 0.01 mu g/mL) and spontaneous (0.29 +/- 0.05 mu g/mL) contractions. However, beta-amyrin had a stronger interaction with the two proteins during the simulation. Conclusion: The isolated compounds boonein and beta-amyrin could serve as starting materials for the development of antispasmodic drugs.