Department of Pharmacognosy, Faculty of Pharmacy, University of Ibadan, Ibadan, Nigeria; H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Science (ICCBS), University of Karachi, Karachi 75270, Pakistan.
Department of Pharmacognosy, Faculty of Pharmacy, University of Ibadan, Ibadan, Nigeria.
Steroids. 2020 Jul;159:108636. doi: 10.1016/j.steroids.2020.108636. Epub 2020 Mar 9.
Sphenocentrum jollyanum seeds (MeOH extract and n butanol fraction) exhibited urease inhibitory activity (IC 40.0 ± 0.92, 28.6 ± 0.41). The Ethyl acetate (EtOAc) fraction gave significant antacid activity with an increase in the baseline pH value of 1.2 to 1.61 ± 0.00 and 1.53 ± 0.00 at 50 and 100 mg, respectively, compared to the antacid activity of sodium bicarbonate (1.53 ± 0.00, 1.47 ± 0.00). Five known ecdysteroid compounds isolated from S. jollyanum ethyl acetate and n butanol fractions are Pinnatasterone (1), Polypodine B (2), 20-hydroxyecdysone (3), 20, 26-dihydroxyecdysone, (4) and Atrotosterone A (5). The compounds' structures were determined using extensive 1D and 2D NMR experiments, and the molecular mass for each of the compounds was confirmed by FAB-MS. Compounds 1-5 were evaluated for their urease inhibitory and antacid activities. Fractions were active in comparison with the standard drug acetohydroxamic acid, and sodium bicarbonate, respectively. Compounds 2, 3 and 1 showed significant urease inhibitory activity (IC 7.0 ± 0.56, 13.8 ± 0.49 and 14.1 ± 0.59), respectively. The activity of compounds 4 and 5 were moderate compared to that of acetohydroxamic acid (IC value 20.3 ± 0.43). Very few compounds have been isolated from this plant despite the numerous biological activities reported for it. The antacid and urease inhibitory activities of this plant and isolated compounds are described for the first time.
醉果种子（甲醇提取物和正丁醇部分）表现出抑制脲酶的活性（IC50 为 0.0 ± 0.92，28.6 ± 0.41）。乙酸乙酯（EtOAc）部分具有显著的抗酸活性，与抗酸活性相比，基线 pH 值分别从 1.2 增加到 1.61 ± 0.00 和 1.53 ± 0.00 在 50 和 100mg 时，分别为碳酸氢钠（1.53 ± 0.00，1.47 ± 0.00）。从醉果乙酸乙酯和正丁醇部分中分离得到的 5 种已知的蜕皮甾体化合物为 Pinnatasterone（1）、Polypodine B（2）、20-羟基蜕皮酮（3）、20,26-二羟基蜕皮酮（4）和 Atrotosterone A（5）。这些化合物的结构是通过广泛的 1D 和 2D NMR 实验确定的，每个化合物的分子量都是通过 FAB-MS 确认的。对化合物 1-5 进行了抑制脲酶和抗酸活性的评价。与标准药物乙酰氧肟酸和碳酸氢钠相比，各部分均具有活性。化合物 2、3 和 1 表现出显著的抑制脲酶活性（IC50 分别为 13.8 ± 0.49、14.1 ± 0.59 和 7.0 ± 0.56）。与乙酰氧肟酸（IC 值 20.3 ± 0.43）相比，化合物 4 和 5 的活性适中。尽管该植物具有多种生物活性，但从中分离出的化合物却很少。首次描述了该植物及其分离化合物的抗酸和抑制脲酶的活性。
