Salinas-Sánchez David Osvaldo, Jiménez-Ferrer Enrique, Sánchez-Sánchez Veronica, Zamilpa Alejandro, González-Cortazar Manasés, Tortoriello Jaime, Herrera-Ruiz Maribel
Biomedical Research Center of the South (IMSS), Argentina 1, Col. Centro, Xochitepec 62790, Morelos, Mexico.
Biodiversity and Conservation Research Center (UAEM), Av. Universidad 1001, Col. Chamilpa, Cuernavaca 62209, Morelos, Mexico.
Molecules. 2017 May 26;22(6):863. doi: 10.3390/molecules22060863.
The ethyl acetate extract (SsAcOEt) from , select fractions (F-6, F-12, F-13, F-14), and one isolated compound, were evaluated in 12--tetradecanoylphorbol 13-acetate (TPA) ear edema and kaolin/carrageenan (KC)-induced monoarthritis assays. SsEtOAc induced edema inhibition of 90% (2.0 mg/ear), fractions showed activity within a range of 67-89%. Due to the fact F-14 showed the highest effect, it was separated, yielding a proanthocyanidin-type called epicatechin-(4β → 8)-epicatechin-(4β → 8, 2β → O → 7) epicatechin (ETP). This compound (2.0 mg/ear) provoked 72% of edema inhibition (ED50 = 0.25 mg/ear, Emax = 52.9%). After 9 days of treatment, joint inflammation was decreasing, and on the last day, SsEtOAc (400 mg/kg), F-14 and ETP (10 mg/kg), SsEtOAc (200 mg/kg), methotrexate (MTX) 1.0 mg/kg and meloxicam (MEL) 1.5 mg/kg, produced an inhibition articulate edema of 94, 62, 36, 21, 80, and 54%, respectively. In the joint, pro-inflammatory molecules were elevated in animals without treatment (vehicle group, VEH). Treatments from induced a decrease in the concentration of interleukin (IL)-1β, IL-17, and IL-6, and SsEtOAc at a higher dose diminished tumor necrosis factor (TNF-α). IL-10 and IL-4 were fewer in the VEH group in comparison with healthy mice; the animals with treatments from induced an increment in the levels of these cytokines in joint and spleen.
对来自[具体来源未明确]的乙酸乙酯提取物（SsAcOEt）、选定馏分（F - 6、F - 12、F - 13、F - 14）以及一种分离出的化合物，进行了12 - 十四酰佛波醇 - 13 - 乙酸酯（TPA）耳部水肿和高岭土/角叉菜胶（KC）诱导的单关节炎试验评估。SsEtOAc在2.0毫克/耳剂量时诱导的水肿抑制率为90%，各馏分的活性在67 - 89%范围内。由于F - 14显示出最高效果，对其进行分离，得到一种原花青素类化合物，称为表儿茶素 - (4β → 8) - 表儿茶素 - (4β → 8, 2β → O → 7)表儿茶素（ETP）。该化合物（2.0毫克/耳）引起72%的水肿抑制（ED50 = 0.25毫克/耳，Emax = 52.9%）。治疗9天后，关节炎症逐渐减轻，在最后一天，SsEtOAc（400毫克/千克）、F - 14和ETP（10毫克/千克）、SsEtOAc（200毫克/千克）、甲氨蝶呤（MTX）1.0毫克/千克和美洛昔康（MEL）1.5毫克/千克分别产生了94%、62%、36%、21%、80%和54%的关节水肿抑制率。在关节中，未治疗的动物（载体组，VEH）体内促炎分子水平升高。[具体治疗组未明确]的治疗导致白细胞介素（IL）-1β、IL - 17和IL - 6浓度降低，高剂量的SsEtOAc使肿瘤坏死因子（TNF - α）减少。与健康小鼠相比，VEH组中的IL - 10和IL - 4较少；[具体治疗组未明确]的治疗动物在关节和脾脏中这些细胞因子水平升高。
