Purification of gastroprotective triterpenoids from the stem bark of Amphipterygium adstringens;: Role of prostaglandins, sulfhydryls, nitric oxide and capsaicin-sensitive neurons

Purification of gastroprotective triterpenoids from the stem bark of Amphipterygium adstringens;: Role of prostaglandins, sulfhydryls, nitric oxide and capsaicin-sensitive neurons
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DOI:
10.1055/s-2003-45098
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发表时间:
2003-10-01
期刊:
影响因子:
2.7
通讯作者:
Navarrete, A
Navarrete, A
中科院分区:
医学3区
文献类型:
--
作者:
Arrieta, J;Benitez, J;Navarrete, A

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在这项研究中,从活性二氯甲烷馏分中纯化了三种生物活性化合物,这些化合物负责 Amphepterygium adstringens 的胃保护特性。这些化合物是 3α-羟基乳香二烯酸、β-谷甾醇和 3-表齐墩果酸。后者是最活跃的化合物(胃保护作用为 88.8%),其次是 3α-羟基乳香二烯酸和 β-谷甾醇(胃保护作用分别为 69.8% 和 42.5%)。生甲酚作为阳性对照,显示出88.4%的胃保护作用。乳香二烯酸也从活性部分中分离出来,但它不能抑制乙醇引起的胃损伤。甲醇提取物的胃保护作用被 I-NAME 预处理完全抑制,并通过吲哚美辛和 N-乙基马来酰亚胺预处理减弱。这些结果表明,内源性一氧化氮在束线菌甲醇提取物对乙醇引起的胃粘膜损伤的胃保护中起重要作用,并且前列腺素和内源性巯基也有部分参与。仅用 N-乙基马来酰亚胺预处理即可减弱 3α-羟基乳香二烯酸的作用,表明内源性硫氢基(硫醇)参与其胃保护机制。辣椒素敏感的传入神经元不参与甲醇提取物或 3α-羟基乳香二烯酸的胃保护作用。
In this investigation three bioactive compounds, responsible for the gastroprotective property of Amphipterygium adstringens, were purified from an active dichloromethane fraction. These compounds were 3alpha-hydroxymasticadienonic acid, beta-sitosterol and 3-epi-oleanolic acid. The latter was the most active compound (88.8% of gastroprotection) followed by 3alpha-hydroxymasticadienoic acid and beta-sitosterol (69.8 and 42.5% of gastroprotection, respectively). Carbenoxolone was used as positive control and it showed 88.4% of gastroprotection. Masticadienonic acid was also isolated from the active fraction, but it was unable to inhibit the ethanol-induced gastric lesions. The gastroprotection of the methanol extract was completely inhibited by the pretreatment with I-NAME and attenuated by pretreatment with indomethacin and N-ethylmaleimide. These results suggest that endogenous nitric oxide plays an important role in the gastroprotection of A. adstringens methanol extract on ethanol-induced gastric mucosal lesions and that there is partial participation by prostaglandins and endogenous sulfhydryls. The effect of 3alpha-hydroxymasticadienonic acid was attenuated only by pretreatment with N-ethylmaleimide, indicating that endogenous sulfhydryls (thiols) participate in its gastroprotective mechanism. Capsaicin-sensitive afferent neurons do not participate in the gastroprotection of either the methanol extract or 3alpha-hydroxymasticadienoic acid.