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Bioassay-guided fractionation, phospholipase A2-inhibitory activity and structure elucidation of compounds from leaves of Schumanniophyton magnificum
Pharmaceutical Biology ( IF 3.8 ) Pub Date : 2020-01-01 , DOI: 10.1080/13880209.2020.1839510
Parker Elijah Joshua 1 , Chizoba Joy Anosike 1 , Rita Onyekachukwu Asomadu 1 , Daniel Emmanuel Ekpo 1 , Emmanuel Nnaemeka Uhuo 2 , Okwesili Fred Chiletugo Nwodo 1, 3
Affiliation  

Abstract Context Schumanniophyton magnificum Harms (Rubiaceae) is used traditionally in Nigeria for the treatment of snake bites. Snake venom contains phospholipase A2 (PLA2) which plays a key role in causing inflammation and pain. Objective To assess the anti-inflammatory effect of the methanol extract of Schumanniophyton magnificum (MESM) leaves through the inhibition of PLA2 and investigate the compounds responsible for the effect. Materials and methods PLA2-inhibitory activity of MESM was assessed at concentrations of 0.1–0.8 mg/mL using human red blood cells as substrate. Prednisolone was used as the standard control. MESM was subsequently partitioned using n-hexane, dichloromethane, ethyl acetate and aqueous-methanol (90:10 v/v), after which PLA2-inhibitory activity of the partitions was determined. The best partition was subjected to chromatographic techniques and the fractions obtained were assessed for PLA2 inhibition at 0.4 mg/mL. Compounds in the most active fraction were determined using Fourier-transform infrared spectroscopy (FTIR) and gas chromatography-mass spectrometry (GC-MS). Results MESM significantly inhibited PLA2 activity at 0.8 mg/mL (44.253%) compared to prednisolone (35.207%). n-Hexane partition (SMP1) proved more active with inhibition of 55.870% observed at 0.1 mg/mL. Fraction 1 (SMF1) showed the highest PLA2-inhibitory activity of 58.117%. FTIR studies revealed the presence of some functional groups in SMF1, and GC-MS confirmed the presence of 9 compounds which are first reported in this plant. Hexadecanoic acid, ethyl ester was identified as the major compound (24.906%). Discussion and conclusions The PLA2-inhibitory activity of MESM suggests that its compounds may be explored further in monitoring anti-inflammatory genes affected by the venoms.

中文翻译:

生物测定引导的分级分离、磷脂酶 A2 抑制活性和来自大树植物叶片的化合物的结构解析

摘要背景 Schumanniophyton magnificum Harms(茜草科)在尼日利亚传统上用于治疗蛇咬伤。蛇毒含有磷脂酶 A2 (PLA2),它在引起炎症和疼痛方面起着关键作用。目的通过抑制 PLA2 来评估大紫杉 (MESM) 叶甲醇提取物的抗炎作用,并研究负责该作用的化合物。材料和方法 MESM 的 PLA2 抑制活性在 0.1–0.8 mg/mL 的浓度下使用人红细胞作为底物进行评估。泼尼松龙用作标准对照。MESM 随后使用正己烷、二氯甲烷、乙酸乙酯和甲醇水溶液 (90:10 v/v) 进行分配,之后确定了分配的 PLA2 抑制活性。对最佳分配进行色谱分析,并评估所得级分的 PLA2 抑制作用,浓度为 0.4 mg/mL。使用傅立叶变换红外光谱 (FTIR) 和气相色谱-质谱 (GC-MS) 测定最活跃部分中的化合物。结果与泼尼松龙 (35.207%) 相比,MESM 在 0.8 mg/mL (44.253%) 时显着抑制了 PLA2 活性。正己烷分配 (SMP1) 证明更活跃,在 0.1 mg/mL 时观察到抑制率为 55.870%。部分 1 (SMF1) 显示最高的 PLA2 抑制活性为 58.117%。FTIR 研究显示 SMF1 中存在一些官能团,GC-MS 证实存在 9 种化合物,这些化合物在该植物中首次报道。十六烷酸乙酯被确定为主要化合物 (24.906%)。
更新日期:2020-01-01
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