Pharmacy Department, Honghui Hospital, Xi'an Jiaotong University, Shaanxi Province, 710054, China.
Department of Pharmacology, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Paud Road, Pune, 411038, India.
Regul Toxicol Pharmacol. 2019 Jul;105:77-85. doi: 10.1016/j.yrtph.2019.04.001. Epub 2019 Apr 13.
Citrus sinensis contains glycoside hesperetin-7-rhamnoglucoside (hesperidin) which harbor an array of therapeutic potentials including antioxidant, anticancer, and anti-inflammatory. However, a systematic examination of safety is needed before its utilization. Hence, the present investigation is aimed to evaluate acute and sub-chronic toxicity of hesperidin isolated from the citrus fruit. Hesperidin (73%) was isolated from a methanolic extract of dried peel of the citrus fruit, characterized using FTIR, and standardized by HPLC. Its acute oral toxicity (AOT) and sub-chronic toxicity studies were carried out in Sprague-Dawley rats. Hesperidin (5000 mg/kg) showed 10% mortality in AOT. In sub-chronic toxicity study, hesperidin (250 and 500 mg/kg) did not induce any abnormalities in body weight, food consumption, clinical signs, ophthalmological and neurological observations, urine analysis, hematology, clinical chemistry, organ weights, and gross pathology. However, hesperidin (1000 mg/kg) showed significant (p < 0.05) alterations in body and organ weights, hematology, clinical chemistry, and tissue histopathology. To conclude, hesperidin has median lethal dose (LD) of 4837.5 mg/kg, and Low Observed Adverse Effect Level (LOAEL) at 1000 mg/kg for both male and female Sprague-Dawley rats. Thus, hesperidin isolated from citrus fruit showed a good safety profile in animal study.
甜橙含有糖苷橙皮苷-7-鼠李糖苷（柚皮苷），具有抗氧化、抗癌和抗炎等多种治疗潜力。然而，在其应用之前，需要对其安全性进行系统检查。因此，本研究旨在评估从柑橘类水果中分离得到的柚皮苷的急性和亚慢性毒性。柚皮苷（73%）从柑橘类水果干皮的甲醇提取物中分离出来，采用傅里叶变换红外光谱（FTIR）进行表征，并通过高效液相色谱法（HPLC）进行标准化。对其进行了急性口服毒性（AOT）和亚慢性毒性研究。AOT 中，柚皮苷（5000mg/kg）导致 10%的死亡率。在亚慢性毒性研究中，柚皮苷（250 和 500mg/kg）未引起体重、食物消耗、临床症状、眼科和神经观察、尿液分析、血液学、临床化学、器官重量和大体病理学的任何异常。然而，柚皮苷（1000mg/kg）在体重和器官重量、血液学、临床化学和组织组织病理学方面表现出显著（p<0.05）改变。综上所述，柚皮苷的半数致死剂量（LD）为 4837.5mg/kg，对雄性和雌性斯普拉格-道利大鼠的低观察不良效应水平（LOAEL）为 1000mg/kg。因此，从柑橘类水果中分离得到的柚皮苷在动物研究中表现出良好的安全性。
