Antioxidative 2H-chromenyls attenuate pro-inflammatory 5-lipoxygenase and carbolytic enzymes: Prospective bioactive agents from Babylonidae gastropod mollusk Babylonia spirata.,Journal of Food Biochemistry

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Antioxidative 2H-chromenyls attenuate pro-inflammatory 5-lipoxygenase and carbolytic enzymes: Prospective bioactive agents from Babylonidae gastropod mollusk Babylonia spirata.
Journal of Food Biochemistry ( IF 3.5 ) Pub Date : 2020-04-16 , DOI: 10.1111/jfbc.13196
Kajal Chakraborty ₁ , Soumya Salas _{1,

2,

3}

Affiliation

Oxygenated heterocycles are emerging as valuable pharmacophores involved in the prophylaxis and treatment of several diseases elicited by the reactive oxygen species. Bioassay‐led chromatographic fractionation of the organic extract of the gastropod mollusk Babylonia spirata (family Babylonidae) yielded two unprecedented 2H‐chromenyl derivatives characterized as 2‐(butyryloxy)‐5‐hydroxy‐hexahydro‐2H‐chromene‐3‐methyl carboxylate (1) and (3‐hydroxy‐hexahydro‐2H‐chromen‐2‐yl)methyl pentanoate (2). The chromenyl derivative (1) registered significantly greater attenuation potential against pro‐inflammatory 5‐lipoxygenase (IC₅₀ ~ 2.02 mM) than those exhibited by the compound (2) (IC₅₀ 2.76 mM) and the non‐steroidal anti‐inflammatory drug ibuprofen (IC₅₀ 4.36 mM, p < .05). The compound (1) exhibited comparable antioxidant activity (IC₅₀ 1.47–1.72 mM) with standard antioxidative agent α‐tocopherol (IC₅₀ 1.4–1.7 mM). Inhibitory potential of chromenyl derivative (1) toward α‐glucosidase (IC₅₀ 1.18 mM) and α‐amylase (IC₅₀ 0.92 mM) was greater than those displayed by 2 (IC₅₀ 1.16–1.56 mM). Structure–activity relationships revealed that bioactivities of the compounds were determined by the electronic factors and hydrophilic–lipophilic balance.

中文翻译：

抗氧化的2H色基减弱了促炎性5-脂氧合酶和糖分解酶：来自巴比伦腹足纲软体动物巴比伦螺旋藻的预期生物活性剂。

含氧杂环化合物正逐渐成为有价值的药效团，参与预防和治疗由活性氧引起的几种疾病。腹足软体动物的有机提取物的生物活性测定为主导的色谱分离巴比伦尼亚spirata（家庭Babylonidae），得到2个前所未有2 ħ表征为2-（丁酰氧基）-chromenyl衍生物-5-羟基六氢-2- ħ色烯-3-羧酸甲酯（1）和（3-羟基-六氢-2 H-铬-2-基）戊酸甲酯（2）。色烯衍生物（1）对促炎性5-脂氧合酶的衰减潜力明显更大（IC ₅₀ 比化合物（2）（IC ₅₀ 2.76 mM）和非甾体抗炎药布洛芬（IC ₅₀ 4.36 mM，p <.05）所显示的浓度高约2.02 mM 。的化合物（1）显示出相当的抗氧化活性（IC ₅₀ 1.47-1.72毫摩尔）与标准抗氧化剂α生育酚（IC ₅₀ 1.4-1.7毫米）。色烯衍生物（1）对α-葡萄糖苷酶（IC ₅₀ 1.18 mM）和α-淀粉酶（IC ₅₀ 0.92 mM）的抑制潜力大于2（IC ₅₀1.16–1.56 mM）。结构-活性关系表明，化合物的生物活性由电子因素和亲水-亲脂平衡决定。

更新日期：2020-04-16

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