鲟鱼软骨肽活性评价及软膏剂制备

Evaluation of the activity of sturgeon cartilage peptides and preparation of ointments

鲟鱼软骨因为富含硫酸软骨素和蛋白质等生物活性物质而具有广阔的应用前景。本研究进行了鲟鱼软骨肽在NIH/3T3和C2C12细胞中的安全性评价,研究结果表明,相比空白对照,鲟鱼软骨肽不会引起NIH/3T3、C2C12细胞的凋亡和坏死,为鲟鱼软骨肽的经皮给药递送提供体外实验依据。进一步评价鲟鱼软骨肽对2′-联氨-双-3-乙基苯并噻唑啉-6-磺酸(ABTS)、二苯基苦基苯肼(DPPH)自由基的清除活性,发现鲟鱼软骨肽具有较好的抗氧化活性。本研究制备得到了一种稳定性好、皮肤刺激性小、鲟鱼软骨肽含量为7%的鲟鱼软骨肽软膏,并分析了其在小鼠皮肤上的透皮吸收能力(本实验获得中国医学科学院药物研究所动物伦理委员会批准,批准号:00007684)。结果发现,鲟鱼软骨肽软膏12 h累积释放量达到92%。本研究进一步分析了鲟鱼软骨肽软膏抑制二甲苯致炎后小鼠耳肿胀的能力,相比于基质组和对照组,鲟鱼软骨肽软膏具有显著抗炎活性。综上,本研究发现鲟鱼软骨肽具有良好的安全性和抗氧化活性,制备的鲟鱼软骨肽软膏为鲟鱼软骨肽的进一步应用及经皮给药递送研究提供实验依据。

Sturgeon cartilage has a wide range of applications as it is rich in biologically active substances such as chondroitin sulphate and protein.In this study,the safety evaluation of sturgeon cartilage peptide in NIH/3T3 and C2C12 cells was conducted,and the results showed that sturgeon cartilage peptide did not induce apoptosis and necrosis in NIH/3T3 and C2C12 cells compared to the blank control,which provides an in vitro experimental basis for the transdermal drug delivery of sturgeon cartilage peptide.Further evaluation of the scavenging activity of sturgeon cartilage peptides against the 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)(ABTS)and 2,2-diphenyl-1-picrylhydrazyl(DPPH)free radicals showed that sturgeon cartilage peptides have strong antioxidant activity.A stable sturgeon cartilage peptide ointment containing 7%sturgeon cartilage peptide was prepared and analysed for its transdermal absorption in mouse skin.This experiment was approved by the Animal Ethics Committee of the Institute of Materia Medica,Chinese Academy of Medical Sciences(approval number:00007684).It was found that the 12-hour cumulative release of sturgeon cartilage peptide ointment reached 92%.In this study,we further analyzed the ability of sturgeon cartilage peptide ointment to inhibit ear swelling in mice after xylene-induced inflammation.The sturgeon cartilage peptide ointment showed significant anti-inflammatory activity compared to the matrix group and the control group.In conclusion,the present study clearly demonstrated that sturgeon cartilage peptide has good safety and antioxidant activity,and the prepared sturgeon cartilage peptide ointment provides an experimental basis for further application of sturgeon cartilage peptide as well as the study of transdermal drug delivery.