Porphyromonas gingivalis has been identified as one of the major periodontal pathogens. Activity-directed fractionation and purification processes were employed to identify bioactive compounds from bitter melon leaf. Ethanolic extract of bitter melon leaf was separated into five subfractions by open column chromatography. Subfraction-5-3 significantly inhibited P. gingivalis-induced interleukin (IL)-8 and IL-6 productions in human monocytic THP-1 cells and then was subjected to separation and purification by using different chromatographic methods. Consequently, 5β,19-epoxycucurbita-6,23(E),25(26)-triene-3β,19(R)-diol (charantadiol A) was identified and isolated from the subfraction-5-3. Charantadiol A effectively reduced P. gingivalis-induced IL-6 and IL-8 productions and triggered receptors expressed on myeloid cells (TREM)-1 mRNA level of THP-1 cells. In a separate study, charantadiol A significantly suppressed P. gingivalis-stimulated IL-6 and tumor necrosis factor-α mRNA levels in gingival tissues of mice, confirming the inhibitory effect against P. gingivalis-induced periodontal inflammation. Thus, charantadiol A is a potential anti-inflammatory agent for modulating P. gingivalis-induced inflammation.

中文翻译：

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从野生苦瓜叶中分离出的 Charantadiol A 对热灭活牙龈卟啉单胞菌刺激的 THP-1 单核细胞和牙周炎小鼠模型的抗炎作用


牙龈卟啉单胞菌已被确定为主要的牙周病原菌之一。采用活性导向的分馏和纯化过程来鉴定苦瓜叶中的生物活性化合物。通过开柱色谱将苦瓜叶的乙醇提取物分离成五个亚级分。 Subfraction-5-3显着抑制牙龈卟啉单胞菌诱导的人单核细胞THP-1细胞中白细胞介素(IL)-8和IL-6的产生，然后使用不同的色谱方法进行分离和纯化。因此，从亚组分-5-3中鉴定并分离出5β,19-环氧葫芦-6,23(E),25(26)-三烯-3β,19(R)-二醇（苦菜二醇A）。 Charantadiol A 有效降低牙龈卟啉单胞菌诱导的 IL-6 和 IL-8 产生，并触发 THP-1 细胞的骨髓细胞 (TREM)-1 mRNA 水平上表达的受体。在另一项研究中，charantadiol A 显着抑制小鼠牙龈组织中牙龈卟啉单胞菌刺激的 IL-6 和肿瘤坏死因子-α mRNA 水平，证实了对牙龈卟啉单胞菌诱导的牙周炎症的抑制作用。因此，charantadiol A是调节牙龈卟啉单胞菌诱导的炎症的潜在抗炎剂。