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柚皮素-磷脂复合物对大鼠的治疗潜力增强

Enhanced therapeutic potential of naringenin-phospholipid complex in rats.

作者信息

Maiti Kuntal, Mukherjee Kakali, Gantait Arunava, Saha Bishnu Pada, Mukherjee Pulok K

机构信息

School of Natural Product Studies, Department of Pharmaceutical Technology, Faculty of Engineering and Technology, Jadavpur University, Kolkata - 700 032, India.

出版信息

J Pharm Pharmacol. 2006 Sep;58(9):1227-33. doi: 10.1211/jpp.58.9.0009.

DOI:10.1211/jpp.58.9.0009
PMID:16945181
Abstract

Naringenin is a naturally occurring flavanone, possessing a variety of biological activity. Due to its rapid elimination, naringenin needs frequent administration to maintain an effective plasma concentration. We have evaluated the therapeutic potential of naringenin-phospholipid complex under oxidative stress conditions compared with free naringenin. Naringenin-phospholipid complex was prepared and assessed for antioxidant activity in carbon tetrachloride intoxicated rats at a dose level of 100 mg kg-1 (p.o.). Liver function tests were studied by assessing serum glutamate oxaloacetate transaminase, serum glutamate pyruvate transaminase, serum alkaline phosphatase and total bilirubin. Marker enzymes of liver, namely glutathione peroxidase, superoxide dismutase, catalase and thiobarbituric acid reactive substances, were measured to evaluate the antioxidant potential at the same dose level. The plasma concentration of naringenin was also measured. It was observed that the naringenin-phospholipid complex enhanced the antioxidant activity of the biomolecule and protected the liver significantly for a longer time as compared with free naringenin at the same dose level. Phospholipid complex of naringenin produced better antioxidant activity than the free compound with a prolonged duration of action, which may be helpful in reducing the fast elimination of the molecule from body.

摘要

柚皮素是一种天然存在的黄烷酮,具有多种生物活性。由于其快速消除,柚皮素需要频繁给药以维持有效的血浆浓度。我们评估了与游离柚皮素相比,柚皮素 - 磷脂复合物在氧化应激条件下的治疗潜力。制备了柚皮素 - 磷脂复合物,并以100 mg kg-1(口服)的剂量水平评估了其对四氯化碳中毒大鼠的抗氧化活性。通过评估血清谷氨酸草酰乙酸转氨酶、血清谷氨酸丙酮酸转氨酶、血清碱性磷酸酶和总胆红素来研究肝功能测试。在相同剂量水平下,测量肝脏的标记酶,即谷胱甘肽过氧化物酶、超氧化物歧化酶、过氧化氢酶和硫代巴比妥酸反应性物质,以评估抗氧化潜力。还测量了柚皮素的血浆浓度。观察到,与相同剂量水平的游离柚皮素相比,柚皮素 - 磷脂复合物增强了生物分子的抗氧化活性,并在更长时间内显著保护肝脏。柚皮素的磷脂复合物比游离化合物产生了更好的抗氧化活性,且作用持续时间延长,这可能有助于减少该分子从体内的快速消除。

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