Department of Pharmacognosy, Faculty of Pharmacy, "Victor Babeş" University of Medicine and Pharmacy, 2, Eftimie Murgu Sq., Timişoara 300041, Romania.
Department of Organic Chemistry, Martin-Luther University Halle-Wittenberg, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany.
Int J Mol Sci. 2019 Jun 10;20(11):2828. doi: 10.3390/ijms20112828.
Maslinic acid is a pentacyclic triterpene with a plethora of biological activities, including anti-inflammatory, antioxidant, antimicrobial, cardioprotective, and antitumor effects. New derivatives with improved properties and broad-spectrum activity can be obtained following structural changes of the compound. The present study was aimed to characterize a benzylamide derivative of maslinic acid-benzyl (2α, 3β) 2,3-diacetoxy-olean12-en-28-amide (EM2)-with respect to the anti-angiogenic and anti-inflammatory effects in two in vivo experimental models. Consequently, the compound showed good tolerability and lack of irritation in the chorioallantoic membrane assay with no impairment of the normal angiogenic process during the tested stages of development. In the acute ear inflammation murine model, application of EM2 induced a mild anti-inflammatory effect that was potentiated by the association with zinc chloride (ZnCl). A decrease in dermal thickness of mice ears was observed when EM2 and ZnCl were applied separately or in combination. Moreover, hyalinization of the dermis appeared only when EM2 was associated with ZnCl, strongly suggesting the role of their combination in wound healing.
马粟酸是一种五环三萜,具有多种生物学活性,包括抗炎、抗氧化、抗菌、心脏保护和抗肿瘤作用。通过对化合物进行结构改变,可以得到具有改善的性质和广谱活性的新衍生物。本研究旨在对马粟酸苄基酰胺衍生物-苄基(2α,3β)2,3-二乙酰氧基-齐墩 12-烯-28-酰胺(EM2)进行表征,以研究其在两种体内实验模型中的抗血管生成和抗炎作用。因此,该化合物在鸡胚尿囊膜试验中表现出良好的耐受性和无刺激性,在测试的发育阶段不会损害正常的血管生成过程。在急性耳炎症的小鼠模型中,EM2 的应用诱导了轻度的抗炎作用,而与氯化锌(ZnCl)联合使用时则增强了这种作用。当 EM2 和 ZnCl 单独或联合使用时,可观察到小鼠耳部皮肤厚度的减少。此外,当 EM2 与 ZnCl 联合使用时,真皮出现玻璃样变性,强烈提示它们联合应用于伤口愈合。