Naglah Ahmed M, Almehizia Abdulrahman A, Al-Omar Mohamed A, Al-Wasidi Asma S, Mohamed Mayada H, Alsobeai Sanad M, Hassan Ashraf S, Aboulthana Wael M
Drug Exploration and Development Chair (DEDC), Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Department of Chemistry, College of Science, Princess Nourah Bint Abdulrahman University, Riyadh 11671, Saudi Arabia.
Pharmaceutics. 2025 Mar 31;17(4):446. doi: 10.3390/pharmaceutics17040446.
The current research was designed to quantify the active phyto-constituents and investigate the in vitro biological efficiency of different garden cress ( Linn.) seed extracts against chronic diseases as well as the in vivo toxicities that may be induced in mice upon the administration of each extract at both studied therapeutic doses. : The in vitro biological efficiency of different extracts, such as methanolic, aqueous, acetone, and ethyl acetate extracts, was assessed. The inhibition percentage (%) and the median inhibitory concentration (IC) values of different extracts were estimated against acetylcholinesterase enzyme, diabetes mellitus (α-amylase and α-glucosidase enzymes), and inflammation (cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2), and 5-lipoxygenase (5-LOX) enzymes). Additionally, the median inhibitory concentration (IC) values of different L. sativum extracts against HepG-2, Caco-2, and A549 cells were assessed using 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Moreover, the toxicities that might be induced in mice at hematological (using an automatic blood analyzer) and biochemical levels were evaluated. It was found that the methanolic extract possessed the highest in vitro biological activities compared to the other studied extracts. The inhibition percentage values of the methanolic extract were 51.34, 54.35, 44.10, 43.48, and 40.78% against acetylcholinesterase, α-amylase, α-glucosidase, protein denaturation, and proteinase enzymes, respectively. The methanolic extract also exhibited an inhibitory effect against the COX-1 (55.05%), COX-2 (57.30%), and 5-LOX (50.15%) enzymes. Additionally, the methanolic extract possesses the highest cytotoxic activity against HepG-2, Caco-2, and A549 cells, with IC values of 52.27, 40.73, and 37.95 μg/mL, respectively. The median lethal doses (LD) showed that the methanolic extract was safer when administered orally, followed by aqueous and acetone, then ethyl acetate extract. It was found that methanolic, aqueous, and acetone extracts showed no alterations when administered orally at two studied doses (1/10 and 1/20 of LD) compared to the control. : This study concluded that the methanolic extract possessed the highest in vitro biological activities and was safer than the other studied extracts, followed by aqueous, acetone, and then ethyl acetate extract. In the future, the in vivo biological efficacy of the methanolic extract will be evaluated, as well as an elucidation of its mechanism against chronic diseases.
当前的研究旨在量化活性植物成分，研究不同独行菜（Linn.）种子提取物对慢性疾病的体外生物功效，以及在两个研究治疗剂量下给小鼠施用每种提取物后可能诱导的体内毒性。评估了不同提取物（如甲醇提取物、水提取物、丙酮提取物和乙酸乙酯提取物）的体外生物功效。估计了不同提取物对乙酰胆碱酯酶、糖尿病（α-淀粉酶和α-葡萄糖苷酶）和炎症（环氧化酶-1（COX-1）、环氧化酶-2（COX-2）和5-脂氧合酶（5-LOX））的抑制百分比（%）和半数抑制浓度（IC）值。此外，使用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐（MTT）法评估了不同独行菜提取物对HepG-2、Caco-2和A549细胞的半数抑制浓度（IC）值。此外，还评估了在血液学（使用自动血液分析仪）和生化水平上给小鼠施用提取物可能诱导的毒性。结果发现，与其他研究提取物相比，甲醇提取物具有最高的体外生物活性。甲醇提取物对乙酰胆碱酯酶、α-淀粉酶、α-葡萄糖苷酶、蛋白质变性和蛋白酶的抑制百分比值分别为51.34%、54.35%、44.10%、43.48%和40.78%。甲醇提取物对COX-1（55.05%）、COX-2（57.30%）和5-LOX（50.15%）酶也表现出抑制作用。此外，甲醇提取物对HepG-2、Caco-2和A549细胞具有最高的细胞毒性活性，IC值分别为52.27、40.73和37.95μg/mL。半数致死剂量（LD）表明，口服甲醇提取物时更安全，其次是水提取物和丙酮提取物，然后是乙酸乙酯提取物。结果发现，与对照组相比，甲醇提取物、水提取物和丙酮提取物在两个研究剂量（LD的1/10和LD的1/20）下口服时没有变化。本研究得出结论，甲醇提取物具有最高的体外生物活性，比其他研究提取物更安全，其次是水提取物、丙酮提取物，然后是乙酸乙酯提取物。未来，将评估甲醇提取物的体内生物功效，并阐明其对抗慢性疾病的机制。
