Browsing by Author "Adebayo, J. O."

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    Effects of 3-O-[6-deoxy-3-O-methyl-β-D-allopyranosyl-(14)-β-D-canaropyranosyl]-17β-marsdenin on selected indices of cardiovascular diseases in mouse
    (Springer Nature, 2022-02) Adebayo, J. O.; Orire, A. B.; Gyebi, G.A.; Olorundare, O. E.; Babatunde, A. S.
    Some anticancer pregnane glycosides, e.g., 3-O-[6-deoxy-3-O-methyl-β-d-allopyranosyl-(1 → 4)-β-d-canaropyranosyl]-17β- marsdenin (3DMACM), have been isolated from Gongronema latifolium leaves which have not been evaluated for their effects on the cardiovascular system. Thus, this study was carried out to evaluate the effects of 3DMACM on selected indices of cardiovascular diseases in albino mice. Forty mice were randomly divided into four groups (ten mice each). Group A mice were orally administered 5% DMSO while mice in groups B, C, and D were orally administered 0.25, 0.5, and 1 mg/ kg body weight of the compound for 14 days, after which various indices of cardiovascular diseases were determined. The results revealed that the total cholesterol, triacylglycerol, very low density lipoprotein-, and high-density lipoprotein-cholesterol concentrations in the plasma and heart Na+- K+-ATPase activity were significantly reduced (p < 0.05) at the doses of 0.25 and 1 mg/kg body weight of the compound compared to controls. Also, atherogenic index, plasma LDH activity, and heart Mg2+- ATPase activity of the mice were significantly (p < 0.05) reduced at all doses of the compound compared to controls. Heart and plasma creatine kinase activities and heart Ca2+- Mg2+-ATPase activity of mice were significantly (p < 0.05) reduced at doses higher than 0.25 mg/kg body weight of the compound compared to controls. AST activities in the heart and plasma of mice were significantly increased (p < 0.05) at doses of 0.25 and 1 mg/kg body weight compared to controls. The results suggest that 3DMACM may not predispose subjects to atherosclerosis but may adversely affect cardiac muscle contraction/relaxation, especially at higher doses.
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    Iloneoside, an antimalarial pregnane glycoside isolated from Gongronema latifolium leaf, potentiates the activity of chloroquine against multidrug resistant Plasmodium falciparum
    (Elsevier, 2022-03) Adebayo, J. O.; Ceravolo, I. P.; Gyebi, G.A.; Olorundare, O. E.; Babatunde, A. S.; Penna-Coutinho, J. P.; Koketsu, M.; Krettli, A. U.
    The rapid spread of drug resistant malaria parasites has necessitated the search for novel antimalarials and chemosensitizers capable of reversing drug resistance in the parasites. A number of studies have revealed the resistance reversal activities of pregnane glycosides and the antimalarial activity of a pregnane glycoside obtained from Gongronema species. However, the pregnane (2) and pregnane glycosides (1, 3–4) isolated from Gongronema latifolium leaf have not been evaluated for these activities. This study was therefore carried out to evaluate the antiplasmodial and chloroquine resistance reversal activities of a pregnane and three pregnane glycosides isolated from G. latifolium leaf in vitro. The compounds were evaluated for their inhibitory activities against P. falciparum 3D7 (a chloroquine-sensitive strain) and P. falciparum W2 (a chloroquine-resistant clone) in vitro. The activities of chloroquine in separate combination with each of the compounds against P. falciparum W2 were also evaluated. Moreover, the interaction of the active compounds (1 and 4) with selected P. falciparum proteins (PfProteins) were evaluated in silico. The results revealed that only 1 and 4 were active against P. falciparum 3D7 and P. falciparum W2. Also, 2 and 3 did not exhibit chloroquine resistance reversal activity. Activity of chloroquine against P. falciparum W2 was potentiated by 1 by 3200% at concentrations higher than 0.625 μg/mL. Also, 1 and 4 demonstrated similar binding patterns and higher binding tendencies to the selected PfProteins compared to chloroquine. Thus, 1 (iloneoside) is an antimalarial pregnane glycoside which can potentiate the activity of chloroquine against multidrug resistant P. falciparum.
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    Iloneoside, an antimalarial pregnane glycoside isolated from Gongronema latifolium leaf, potentiates the activity of chloroquine against multidrug resistant Plasmodium falciparum
    (Elsevier, 2022-03) Adebayo, J. O.; Ceravolo, I. P.; Gyebi, G.A.; Olorundare, O. E.; Babatunde, A. S.; Penna-Coutinho, J. P.; Koketsu, M.; Krettli, A. U.
    The rapid spread of drug resistant malaria parasites has necessitated the search for novel antimalarials and chemosensitizers capable of reversing drug resistance in the parasites. A number of studies have revealed the resistance reversal activities of pregnane glycosides and the antimalarial activity of a pregnane glycoside obtained from Gongronema species. However, the pregnane (2) and pregnane glycosides (1, 3–4) isolated from Gongronema latifolium leaf have not been evaluated for these activities. This study was therefore carried out to evaluate the antiplasmodial and chloroquine resistance reversal activities of a pregnane and three pregnane glycosides isolated from G. latifolium leaf in vitro. The compounds were evaluated for their inhibitory activities against P. falciparum 3D7 (a chloroquine-sensitive strain) and P. falciparum W2 (a chloroquine-resistant clone) in vitro. The activities of chloroquine in separate combination with each of the compounds against P. falciparum W2 were also evaluated. Moreover, the interaction of the active compounds (1 and 4) with selected P. falciparum proteins (PfProteins) were evaluated in silico. The results revealed that only 1 and 4 were active against P. falciparum 3D7 and P. falciparum W2. Also, 2 and 3 did not exhibit chloroquine resistance reversal activity. Activity of chloroquine against P. falciparum W2 was potentiated by 1 by 3200% at concentrations higher than 0.625 μg/mL. Also, 1 and 4 demonstrated similar binding patterns and higher binding tendencies to the selected PfProteins compared to chloroquine. Thus, 1 (iloneoside) is an antimalarial pregnane glycoside which can potentiate the activity of chloroquine against multidrug resistant P. falciparum.
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    Iloneoside: a cytotoxic ditigloylated pregnane glycoside from the leaves of Gongronema latifolium Benth
    (2018) Gyebi, G. A.; Adebayo, J. O.; Olorundare, O. E.; Pardede, A.; Ninomiya, M.; Afolabi, S.O.; Koketsu, M
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    Metal Displacement Effects on Monoesterase Activity of Calf Intestinal Alkaline Phosphatase
    (Nigerian Society of Biochemistry and Molecular Biology, 2012) Igunnu, Adedoyin; Arise, R. O.; Adebayo, J. O.; Malomo, S. O.
    The mechanism of modulation of alkaline phosphatase activity by metal ions has not been fully elucidated. We investigated the time-dependent modulatory effects of Mg 2+ and Zn 2+ in promoting the hydrolysis of para-nitrophenyl phosphate (monoesterase reaction) by calf intestinal alkaline phosphatase (CIAP) and the effects of addition of the activating metal ions to the metal-inhibited enzyme. The CIAP was affected by changes in pre-incubation time in the presence of the two metal cofactors. Both Mg 2+ (0.1 – 0.25 mM) and Zn 2+ (0.1 – 5 mM) modulated Zn 2+ - and Mg 2+ - inhibited monoesterase activity of CIAP. The CIAP activity was inhibited when the enzyme was pre-incubated with 1 mM Ca 2+ . Further addition of Mg 2+ (0.1 – 2 mM) did not completely restore the activity though partly relieved the inhibition caused by Ca 2+ - pre-incubated enzyme. Again, addition of 2mM Zn 2+ to Ca 2+ - pre-incubated alkaline phosphatase completely restored the activity of the enzyme. This study suggests that Mg 2+ and Zn 2+ regulate the catalytic property of each other and modulate the inhibitory effect of Ca 2+ in alkaline phosphatase catalysis through a displacement effect. The modulation of Ca 2+ -inhibited CIAP activity by Mg 2+ and Zn 2+ may be explored in the treatment of disorders of bone mineralization especially those arising from inhibited alkaline phosphatase activity.