Laboratoire de Pharmacologie, Pharmacocinétique et Pharmacie Clinique, Faculté des Sciences Pharmaceutiques et Biologiques, Université de Lille 2, Lille, France.
Pharm Biol. 2010 Feb;48(2):128-33. doi: 10.3109/13880200903051609.
The ability of Alchornea cordifolia (Schum. and Thonn.) Müll. Arg. (Euphorbiaceae) leaves to inhibit human neutrophil elastase (HNE) and superoxide anion (O(2)(-)) activities was evaluated on aqueous and ethyl acetate extracts as they allow for a targeted extraction of polyphenols. The direct effect of A. cordifolia extracts on HNE and O(2)(-) was assessed in an acellular system. Results showed that extracts scavenge HNE and O(2)(-) in a dose-dependent manner. Better activity was exhibited by the ethyl acetate extract with lower IC(50) (2.2 and 4. 1 mg/L for HNE and O(2)(-), respectively) than for the aqueous extract. Cellular systems including isolated human polymorphonuclear neutrophils (PMN) were investigated to assess the effect of extracts on PMN metabolism. PMN were stimulated with 4beta-phorbol-12-myristate-13-acetate (PMA), calcium ionophore (CaI), or N-formyl-methionyl-leucine-phenylalanine (fMLP), each stimulant having its own stimulation pathway. From the IC(50) obtained, it can be concluded that A. cordifolia reduces HNE and O(2)(*-) liberation. Furthermore it was demonstrated that A. cordifolia extracts have no cytotoxic activity on PMN by measuring release of the cytosolic enzyme lactate dehydrogenase. As the ethyl acetate extract offers a higher rate of total phenols than the aqueous extract as well as better scavenging activity, it can be supposed that polyphenols, which are well known for their potent antioxidant and antielastase activity, are implicated in the activity of the plant. Phenolic substances such as quercetin, myricetin-3-glucopyranoside, myricetin-3-rhamnopyranoside, and proanthocyanidin A2 were identified in the ethyl acetate extract. In conclusion, the study provides proof of ethnomedical claims and partly explains the mechanisms of the anti-inflammatory action of A. cordifolia leaves.
阿尔克恩拉 Cordifolia(舒。和 Thonn。)Müll.Arg。(大戟科)叶抑制人中性粒细胞弹性蛋白酶(HNE)和超氧阴离子(O(2)(-))的能力进行了评估，因为它们允许多酚的靶向提取。A. Cordifolia 提取物对 HNE 和 O(2)(-)的直接影响在非细胞系统中进行了评估。结果表明，提取物以剂量依赖的方式清除 HNE 和 O(2)(-)。具有较低 IC(50)的乙酸乙酯提取物表现出更好的活性(分别为 HNE 和 O(2)(-)的 2.2 和 4.1mg/L)，而水提取物则不然。包括分离的人多形核白细胞(PMN)在内的细胞系统被用来评估提取物对 PMN 代谢的影响。PMN 用 4β-佛波醇-12-肉豆蔻酸-13-醋酸盐(PMA)、钙离子载体(CaI)或 N-甲酰基-甲硫氨酸-亮氨酸-苯丙氨酸(fMLP)刺激，每种刺激物都有自己的刺激途径。从获得的 IC(50)可以得出结论，A. Cordifolia 减少 HNE 和 O(2)(*-)的释放。此外，通过测量细胞溶质酶乳酸脱氢酶的释放来证明 A. Cordifolia 提取物对 PMN 没有细胞毒性。由于乙酸乙酯提取物提供了比水提取物更高的总酚含量以及更好的清除活性，可以假定多酚，由于其强大的抗氧化和抗弹性酶活性而闻名，参与了植物的活性。在乙酸乙酯提取物中鉴定出了槲皮素、杨梅素-3-葡萄糖苷、杨梅素-3-鼠李糖苷和原花青素 A2 等酚类物质。总之，该研究提供了对民族医学主张的证明，并部分解释了 A. Cordifolia 叶抗炎作用的机制。
