Departamento de Farmacia, División de Ciencias Naturales y Exactas, Universidad de Guanajuato, Guanajuato, Mexico.
Departamento de Farmacia, División de Ciencias Naturales y Exactas, Universidad de Guanajuato, Guanajuato, Mexico.
J Ethnopharmacol. 2018 Oct 5;224:314-322. doi: 10.1016/j.jep.2018.06.016. Epub 2018 Jun 18.
Eysenhardtia polystachya is used for the empirical treatment of cancer, infections, diarrhea, inflammation, and pain. This study identified, using GC-MS, the main chemical components in an ethanol extract of E. polystachya branches and leaves (EPE) and tested its cytotoxic, antimicrobial, anti-diarrheal, anti-inflammatory, and antinociceptive effects. The in vitro and in vivo toxicity of EPE was evaluated using the comet assay in human peripheral blood mononuclear cells (PBMC) and the acute toxicity test in mice, respectively. The cytotoxic and the antimicrobial effects were performed using the MTT assay and the minimum inhibitory concentration (MIC) test, respectively. The levels of pro-inflammatory mediators in LPS-stimulated macrophages were measured to evaluate the in vitro anti-inflammatory effects of EPE. The antidiarrheal (castor oil test, small intestine transit, and castor oil-induced enteropooling), and anti-inflammatory activities (TPA and carrageenan) of EPE were also performed. The antinociceptive actions of EPE were carried out with the following tests: acetic acid, formalin, and hot plate. The hypnotic and locomotor effects were analyzed using pentobarbital and a rotarod system, respectively. The main component in EPE was D-pinitol (26.93%). The antidiarrheal and antinociceptive effects of D-pinitol were also evaluated. EPE showed low in vitro toxicity (DNA damage in PBMC at concentrations higher than 200 µg/ml), and low in vivo toxicity (LD > 2000 mg/kg i.p. and p.o.). Furthermore, EPE lacked cytotoxic activity (IC > 300 µg/ml) on human cancer cells, but showed good antimicrobial effects in E. coli (MIC=1.56 µg/ml) and S. aureus (MIC = 0.78 µg/ml). In multi-drug resistant microorganisms, EPE showed MIC> 100 µg/ml. EPE exerted in vitro anti-inflammatory effects, mainly, by the decrease in the production of HO (IC = 43.9 ± 3.8 µg/ml), and IL-6 (73.3 ± 6.9 µg/ml). EPE (ED =7.5 ± 0.9 mg/kg) and D-pinitol (ED = 0.1 ± 0.03 mg/kg) showed antidiarrheal activity, and antinociceptive effects in the acetic acid test with ED = 117 ± 14.5 mg/kg for EPE and 33 ± 3.2 mg/kg for D-pinitol. EPE showed also antinociceptive activity in the phase 2 of the formalin test (ED = 48.9 ± 3.9 mg/kg), without inducing hypnotic effects or altering the locomotor activity in mice. The results here presented corroborate the folk medicinal use of Eysenhardtia polystachya in the treatment of infections, diarrhea, inflammation, and pain. D-pinitol, the main metabolite of EPE, showed antinociceptive and antidiarrheal effects with similar potency compared to standard drugs.
梁王茶被用于癌症、感染、腹泻、炎症和疼痛的经验性治疗。本研究采用 GC-MS 法鉴定了梁王茶枝叶乙醇提取物（EPE）中的主要化学成分，并测试了其细胞毒性、抗菌、抗腹泻、抗炎和镇痛作用。EPE 的体外和体内毒性分别用人外周血单核细胞（PBMC）彗星试验和小鼠急性毒性试验进行评估。采用 MTT 法和最低抑菌浓度（MIC）试验分别进行细胞毒性和抗菌作用检测。通过 LPS 刺激的巨噬细胞中促炎介质的水平来评估 EPE 的体外抗炎作用。还进行了 EPE 的抗腹泻（蓖麻油试验、小肠转运和蓖麻油诱导的肠液积聚）和抗炎（TPA 和角叉菜胶）作用。采用醋酸、福尔马林和热板试验进行 EPE 的镇痛作用。采用戊巴比妥和转棒系统分别分析催眠和运动作用。EPE 的主要成分是 D-松醇（26.93%）。还评估了 D-松醇的抗腹泻和镇痛作用。EPE 表现出低体外毒性（DNA 损伤在浓度高于 200 µg/ml 的 PBMC 中）和低体内毒性（腹腔注射 LD > 2000 mg/kg 和口服 LD > 2000 mg/kg）。此外，EPE 对人癌细胞无细胞毒性活性（IC > 300 µg/ml），但对大肠杆菌（MIC = 1.56 µg/ml）和金黄色葡萄球菌（MIC = 0.78 µg/ml）具有良好的抗菌作用。在多药耐药微生物中，EPE 的 MIC > 100 µg/ml。EPE 表现出体外抗炎作用，主要通过降低 HO（IC = 43.9 ± 3.8 µg/ml）和 IL-6（73.3 ± 6.9 µg/ml）的产生来实现。EPE（ED = 7.5 ± 0.9 mg/kg）和 D-松醇（ED = 0.1 ± 0.03 mg/kg）表现出抗腹泻作用，在醋酸试验中具有镇痛作用，EPE 的 ED 为 117 ± 14.5 mg/kg，D-松醇的 ED 为 33 ± 3.2 mg/kg。EPE 还在福马林试验的第二阶段表现出镇痛作用（ED = 48.9 ± 3.9 mg/kg），没有诱导催眠作用或改变小鼠的运动活动。这里呈现的结果证实了梁王茶在治疗感染、腹泻、炎症和疼痛方面的民间药用用途。EPE 的主要代谢物 D-松醇表现出与标准药物相当的镇痛和抗腹泻作用。
