克拉美辛——一种从克拉美里亚 Cytisoides 中分离得到的新型抗炎化合物。

Kramecyne--a new anti-inflammatory compound isolated from Krameria cytisoides.

机构信息

Departamento de Sistemas Biológicos, Universidad Autónoma Metropolitana-Xochimilco, Calzada del Hueso 1100, Col. Villa Quietud, Coyoacan C.P. 04960, D.F.A.P. 23-181, Mexico.

出版信息

Molecules. 2012 Feb 20;17(2):2049-57. doi: 10.3390/molecules17022049.

DOI:10.3390/molecules17022049

PMID:22349895

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6268713/

Abstract

In the present work we describe the structure and anti-inflammatory activity of a new compound, kramecyne, isolated from a methanol extract of Krameria cytisoides (Krameriaceae). The structure of kramecyne was determined by IR, NMR, MS, and elemental analysis, which indicated that the structure corresponded to a hexamer of cyclic peroxide monomers. This compound exhibited good anti-inflammatory activity in the 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema (51.8 ± 6.9% inhibition) and carrageenan-induced rat paw edema models at doses of 50 mg/kg. The compound significantly reduced edema to 63.1% after 1.0 h, and the effect was unchanged for 5 h. Kramecyne did not present acute toxicity, even at doses of 5,000 mg/kg.

摘要

在本工作中，我们描述了一种新化合物 kramecyne 的结构和抗炎活性，该化合物从 Krameria cytisoides（Krameriaceae）甲醇提取物中分离得到。通过 IR、NMR、MS 和元素分析确定了 kramecyne 的结构，表明其结构对应于环状过氧化物单体的六聚体。该化合物在 12-O-十四烷酰佛波醇-13-醋酸酯（TPA）诱导的小鼠耳肿胀（51.8±6.9%抑制）和角叉菜胶诱导的大鼠足肿胀模型中显示出良好的抗炎活性，剂量为 50mg/kg。该化合物在 1.0 小时后显著将肿胀减少至 63.1%，并且 5 小时内效果不变。即使剂量为 5000mg/kg，kramecyne 也没有表现出急性毒性。