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Moringa isothiocyanate-1 is bioaccessible and bioavailable as a stable unmodified compound
Phytochemistry Letters ( IF 1.7 ) Pub Date : 2020-05-23 , DOI: 10.1016/j.phytol.2020.05.001
Khea Wolff , Asha Jaja-Chimedza , Youjin Kim , Carrie Waterman , Alexander Poulev , Ilya Raskin , David Ribnicky

Moringa oleifera Lam. is a widely cultivated subtropical tree with a variety of documented medicinal properties. An ethanolic moringa seed extract (MSE) was shown to contain high concentrations of the stable moringa isothiocyanate-1 (MIC-1, 1). Compound 1 has anti-inflammatory and antidiabetic properties but has not been characterized metabolically. The objective of this study was to understand its bioaccessibility using a human intestinal model and bioavailability using serum from treated rats. Bioaccessibility of 1, using the TNO Intestinal Model (TIM-1), was determined to be 61% and 62% in the fasted and fed states respectively. Compound 1 from the serum of treated animals was measured directly without prior chemical or enzymatic digestion. Bioavailability and pharmacokinetic studies were conducted in Sprague-Dawley rats treated with 50 mg/kg of 1, either intravenously with pure 1, or orally gavaged with MSE or 1. Serum levels of 1 were 6 to 12 times higher in animals dosed intravenously than in animals dosed by gavage with a half-life of about 2 h. Serum levels of 1 dropped to zero between 8 and 24 h for all three treatments. These results suggest 1 remains largely unmodified during uptake, unlike other isothiocyanates, and has favorable bioaccessibility and bioavailability characteristics for a potential therapeutic agent.



中文翻译:

辣木异硫氰酸酯-1是可生物利用的,并且可作为稳定的未改性化合物生物利用

辣木林。是一种广泛种植的亚热带树,具有多种已记录的药用特性。乙醇辣木种子提取物(MSE)已显示含有高浓度的稳定辣木异硫氰酸酯1(MIC- 1,1)。化合物1具有抗炎和抗糖尿病的特性,但尚未在代谢上表征。这项研究的目的是了解使用人肠模型的生物可及性和使用治疗大鼠血清的生物可利用性。使用TNO肠模型(TIM-1)的1的生物可及性在禁食和进食状态下分别确定为61%和62%。化合物1无需事先进行化学或酶消化即可直接测定治疗动物血清中的血红素。在Sprague-Dawley大鼠中进行了生物利用度和药代动力学研究,以50 mg / kg的1剂量对纯净的1静脉内注射,或经MSE或1口服灌胃。静脉内给药的动物的血清水平为1,比管饲法给药的动物的半衰期约为2小时高6至12倍。在这三种治疗中,血清水平1在8至24小时之间均降至零。这些结果表明1 与其他异硫氰酸酯不同,其在吸收过程中仍保持很大程度上未改性,并且对于潜在的治疗剂具有良好的生物利用度和生物利用度特性。

更新日期:2020-05-23
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