Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Department of Medicinal Plants and Natural Products, National Organization of Drug Control and Research, Giza, Egypt.
PLoS One. 2021 Aug 6;16(8):e0255904. doi: 10.1371/journal.pone.0255904. eCollection 2021.
Root and bark of Limonium axillare (Forssk) Kuntze are used as antidiabetic remedies in parts of East Africa, but this activity has never been fully investigated. To validate its ethnobotanical use, we compared the chemical and pharmacological profiles of the ethanolic extracts of L. axillare root (REE) and aerial parts (AEE). Administration of REE (500 mg kg-1) reduced streptozotocin-induced hyperglycemia by 44%, restored serum insulin levels, reestablished Glut2 and Glut4 expression and ameliorated pancreatic tissue damage in diabetic rats. In vitro studies revealed a strong radical scavenging effect, α-glucosidase, and α-amylase inhibition activity of REE at IC50 at 25.2, 44.8 and 89.1μg/mL, respectively. HPLC analysis identified ten phenolic compounds in REE with umbelliferone as the major constituents at 10 ± 0.081 mg/g of extract. Additionally, six compounds were isolated from REE including, β-sitosterol-3-palmitate, β-sitosterol, myricetin and gallic acids with two new tetrahydrofuran monoterpenes; 2-isopropyl- 3,4,4, trimethyl-tetrahydrofuran (3), and 2-isopropyl-4-methyl-tetrahydrofuran-3,4 dicarboxylic acid (4), the latter was revealed by molecular docking to be a good ligand to glycerol-3-phosphate dehydrogenase a key enzyme in glycolysis.
肋柱花的根和树皮在东非部分地区被用作抗糖尿病药物，但这种活性从未得到充分研究。为了验证其民族植物学用途，我们比较了肋柱花根（REE）和地上部分（AEE）的乙醇提取物的化学和药理学特征。REE（500mg/kg）给药可使链脲佐菌素诱导的高血糖降低 44%，恢复血清胰岛素水平，重建 Glut2 和 Glut4 表达，并改善糖尿病大鼠的胰腺组织损伤。体外研究表明，REE 具有很强的自由基清除作用、α-葡萄糖苷酶和α-淀粉酶抑制活性，IC50 分别为 25.2、44.8 和 89.1μg/mL。HPLC 分析鉴定出 REE 中的十种酚类化合物，其中茴芹内酯为主要成分，含量为 10±0.081mg/g 提取物。此外，从 REE 中分离出六种化合物，包括β-谷甾醇-3-棕榈酸酯、β-谷甾醇、杨梅素和没食子酸，其中两种新的四氢呋喃单萜；2-异丙基-3,4,4-三甲基-四氢呋喃（3）和 2-异丙基-4-甲基-四氢呋喃-3,4-二羧酸（4），后者通过分子对接显示出是甘油-3-磷酸脱氢酶（糖酵解中的关键酶）的良好配体。
