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. 2021 Jan 22;26(3):579. doi: 10.3390/molecules26030579.
(formerly ) is one of the major bacterial species responsible for acne vulgaris. Numerous bioactive compounds from Linn. var. Ser. have been isolated and examined for many years. In this study, we evaluated the suppressive effect of two cucurbitane-type triterpenoids, 5β,19-epoxycucurbita-6,23-dien-3β,19,25-triol (Kuguacin R; KR) and 3β,7β,25-trihydroxycucurbita-5,23-dien-19-al (TCD) on live -stimulated in vitro and in vivo inflammatory responses. Using human THP-1 monocytes, KR or TCD suppressed -induced production of interleukin (IL)-1β, IL-6 and IL-8 at least above 56% or 45%, as well as gene expression of these three pro-inflammatory cytokines. However, a significantly strong inhibitory effect on production and expression of tumor necrosis factor (TNF)-α was not observed. Both cucurbitanes inhibited s-induced activation of the myeloid differentiation primary response 88 (MyD88) (up to 62%) and mitogen-activated protein kinases (MAPK) (at least 36%). Furthermore, TCD suppressed the expression of pro-caspase-1 and cleaved caspase-1 (p10). In a separate study, KR or TCD decreased s-stimulated mouse ear edema by ear thickness (20% or 14%), and reduced IL-1β-expressing leukocytes and neutrophils in mouse ears. We demonstrated that KR and TCD are potential anti-inflammatory agents for modulating -induced inflammation in vitro and in vivo.
（以前）是引起寻常痤疮的主要细菌物种之一。多年来，从 Linn. var. Ser. 中分离并检查了许多生物活性化合物。在这项研究中，我们评估了两种葫芦烷型三萜，5β,19-环氧葫芦-6,23-二烯-3β,19,25-三醇（Kuguacin R；KR）和 3β,7β,25-三羟基葫芦-5,23-二烯-19-醛（TCD）对活刺激的体外和体内炎症反应的抑制作用。使用人 THP-1 单核细胞，KR 或 TCD 抑制至少 56%或 45%以上的 -诱导的白细胞介素 (IL)-1β、IL-6 和 IL-8 的产生，以及这三种促炎细胞因子的基因表达。然而，并没有观察到对肿瘤坏死因子 (TNF)-α 的产生和表达有明显的强抑制作用。两种葫芦烷都抑制了 s 诱导的髓样分化初级反应 88（MyD88）（高达 62%）和丝裂原活化蛋白激酶（MAPK）（至少 36%）的激活。此外，TCD 抑制了前半胱氨酸酶-1 和切割的半胱氨酸酶-1（p10）的表达。在另一项研究中，KR 或 TCD 减少了 s 刺激的小鼠耳肿胀（20%或 14%），并减少了小鼠耳中表达 IL-1β 的白细胞和中性粒细胞。我们证明 KR 和 TCD 是潜在的抗炎剂，可调节体外和体内的 -诱导炎症。
