Department of Pharmacy, University of Napoli Federico II, Via D. Montesano 49, 80131 Naples, Italy.
Level 1 Medical Director Anaesthesia and Resuscitation A. U. O. Luigi Vanvitelli, Via Santa Maria di Costantinopoli, 80138 Naples, Italy.
Molecules. 2024 Jan 25;29(3):586. doi: 10.3390/molecules29030586.
Excess cortisol release is associated with numerous health concerns, including psychiatric issues (i.e., anxiety, insomnia, and depression) and nonpsychiatric issues (i.e., osteoporosis). The aim of this study was to assess the in vitro inhibition of cortisol release, bioaccessibility, and bioavailability exerted by a chemically characterized L. extract (SLE). The treatment of H295R cells with SLE at increasing, noncytotoxic, concentrations (5-30 ng/mL) showed significant inhibition of cortisol release ranging from 58 to 91%. The in vitro simulated gastric, duodenal, and gastroduodenal digestions, induced statistically significant reductions ( < 0.0001) in the bioactive polyphenolic compounds that most represented SLE. Bioavailability studies on duodenal digested SLE, using Caco-2 cells grown on transwell inserts and a parallel artificial membrane permeability assay, indicated oroxylin A glucuronide and oroxylin A were the only bioactive compounds able to cross the Caco-2 cell membrane and the artificial lipid membrane, respectively. The results suggest possible applications of SLE as a food supplement ingredient against cortisol-mediated stress response and the use of gastroresistant oral dosage forms to partially prevent the degradation of SLE bioactive compounds. In vivo studies and clinical trials remain necessary to draw a conclusion on the efficacy and tolerability of this plant extract.
皮质醇释放过多与许多健康问题有关，包括精神问题（如焦虑、失眠和抑郁）和非精神问题（如骨质疏松症）。本研究旨在评估一种经过化学表征的 L.提取物（SLE）对皮质醇释放的体外抑制、生物利用度和生物可及性。用 SLE 在非细胞毒性浓度（5-30ng/mL）处理 H295R 细胞，显示出对皮质醇释放的显著抑制作用，范围为 58%至 91%。体外模拟胃、十二指肠和胃十二指肠消化，诱导统计学上显著降低（<0.0001）了最能代表 SLE 的生物活性多酚化合物。使用在 Transwell 插入物上生长的 Caco-2 细胞和平行人工膜渗透率测定法对十二指肠消化 SLE 进行的生物利用度研究表明，橙皮苷葡萄糖醛酸和橙皮苷是唯一能够穿过 Caco-2 细胞膜和人工脂质膜的生物活性化合物。结果表明，SLE 可能作为一种食品补充剂成分，用于对抗皮质醇介导的应激反应，并使用胃耐型口服剂型部分防止 SLE 生物活性化合物的降解。需要进行体内研究和临床试验，以得出关于这种植物提取物的功效和耐受性的结论。
