Department of Biotechnology and Pharmaceutical Technology, Yuanpei University of Medical Technology, Hsinchu 300, Taiwan.
Department of Human Development and Family Studies, National Taiwan Normal University, Taipei 106, Taiwan.
Molecules. 2020 Sep 18;25(18):4277. doi: 10.3390/molecules25184277.
(formerly ) is a key pathogen involved in the development and progression of acne inflammation. The numerous bioactive properties of wild bitter melon (WBM) leaf extract and their medicinal applications have been recognized for many years. In this study, we examined the suppressive effect of a methanolic extract (ME) of WBM leaf and fractionated components thereof on live -induced in vitro and in vivo inflammation. Following methanol extraction of WBM leaves, we confirmed anti-inflammatory properties of ME in -treated human THP-1 monocyte and mouse ear edema models. Using a bioassay-monitored isolation approach and a combination of liquid-liquid extraction and column chromatography, the ME was then separated into -hexane, ethyl acetate, -butanol and water-soluble fractions. The hexane fraction exerted the most potent anti-inflammatory effect, suppressing -induced interleukin-8 (IL-8) production by 36%. The ethanol-soluble fraction (ESF), which was separated from the -hexane fraction, significantly inhibited s-induced activation of mitogen-activated protein kinase (MAPK)-mediated cellular IL-8 production. Similarly, the ESF protected against s-stimulated mouse ear swelling, as measured by ear thickness (20%) and biopsy weight (23%). Twenty-four compounds in the ESF were identified using gas chromatograph-mass spectrum (GC/MS) analysis. Using co-cultures of and THP-1 cells, β-ionone, a compound of the ESF, reduced the production of IL-1β and IL-8 up to 40% and 18%, respectively. β-ionone also reduced epidermal microabscess, neutrophilic infiltration and IL-1β expression in mouse ear. We also found evidence of the presence of anti-inflammatory substances in an unfractionated phenolic extract of WBM leaf, and demonstrated that the ESF is a potential anti-inflammatory agent for modulating in vitro and in vivo -induced inflammatory responses.
（以前）是痤疮炎症发展和进展的关键病原体。多年来，野生苦瓜（WBM）叶提取物的许多生物活性特性及其药用应用已得到认可。在这项研究中，我们研究了 WBM 叶甲醇提取物及其分馏成分对活诱导的体外和体内炎症的抑制作用。在 WBM 叶甲醇提取后，我们证实了 ME 在脂多糖（LPS）处理的人 THP-1 单核细胞和小鼠耳水肿模型中的抗炎特性。使用生物测定监测的分离方法以及液-液萃取和柱层析的组合，将 ME 分离成正己烷、乙酸乙酯、正丁醇和水溶性馏分。正己烷馏分表现出最强的抗炎作用，抑制 LPS 诱导的白细胞介素-8（IL-8）产生 36%。从正己烷馏分中分离出的乙醇可溶部分（ESF）显著抑制 s 诱导的丝裂原激活蛋白激酶（MAPK）介导的细胞 IL-8 产生的激活。同样，ESF 可防止 s 刺激的小鼠耳肿胀，如耳厚度（20%）和活检重量（23%）所示。使用气相色谱-质谱（GC/MS）分析鉴定了 ESF 中的 24 种化合物。使用和 THP-1 细胞的共培养物，ESF 中的β-紫罗兰酮化合物将 IL-1β和 IL-8 的产生分别降低了 40%和 18%。β-紫罗兰酮还减少了小鼠耳中的表皮微脓肿、嗜中性粒细胞浸润和 IL-1β表达。我们还在 WBM 叶的未分馏酚提取物中发现了具有抗炎作用的物质的证据，并证明 ESF 是一种潜在的抗炎剂，可调节体外和体内 LPS 诱导的炎症反应。
