Cho Yong-Hun, Kim Na-Hyung, Khan Imran, Yu Jae Myo, Jung Hyun Gug, Kim Han Hyuk, Jang Jae Yoon, Kim Hyeon Jeong, Kim Dong-In, Kwak Jae-Hoon, Kang Sun Chul, An Bong Jeun
Dept. of Cosmeceutical Science, DaeguHanny Univ, Gyeongsan, 712-715, Korea.
Dept. of Oriental Pharmacy, Wonkwang Uni, Iksan-city, Jeonbuk 570-749, Republic of Korea.
J Food Sci. 2016 Oct;81(10):C2447-C2456. doi: 10.1111/1750-3841.13497. Epub 2016 Sep 20.
Diospyros kaki (DK) contains an abundance of flavonoids and has been used in folk medicine in Korea for centuries. Here, we report for the first time the anti-inflammatory activities of Quercetin (QCT) and Quercetin 3-O-β-("2"-galloyl)-glucopyranoside (Q32G) isolated from DK. We have determine the no cytotoxicity of Q32G and QCT against RAW 264.7 cells up to concentration of 50 μM. QCT and Q32G demonstrated potent anti-inflammatory activities by reducing expression of nitric oxide (NO), tumor necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6 inducible NO synthase (iNOS), cyclooxygenase (COX)-2, and mitogen-activated protein kinase (MAPKs) in mouse RAW 264.7 macrophages activated with lipopolysaccharide (LPS). Both QCT or Q32G could decrease cellular protein levels of COX-2 and iNOS as well as secreted protein levels of NO, PGE , and cytokines (TNF-α, IL-1β, and IL-6) in culture medium of LPS-stimulated RAW 264.7 macrophages. Immunoblot analysis showed that QCT and Q32G suppressed LPS-induced MAP kinase pathway proteins p-p38, ERK, and JNK. This study revealed that QCT and Q32G have anti-inflammatory potential, however Q32G possess comparable activity as that of QCT and could be use as adjuvant to treat inflammatory diseases.
柿(DK)含有丰富的黄酮类化合物,在韩国民间医学中已使用了几个世纪。在此,我们首次报道了从DK中分离出的槲皮素(QCT)和槲皮素3 - O-β-(“2”-没食子酰基)-吡喃葡萄糖苷(Q32G)的抗炎活性。我们已确定在浓度高达50μM时,Q32G和QCT对RAW 264.7细胞无细胞毒性。QCT和Q32G通过降低用脂多糖(LPS)激活的小鼠RAW 264.7巨噬细胞中一氧化氮(NO)、肿瘤坏死因子(TNF)-α、白细胞介素(IL)-1β、IL - 6、诱导型一氧化氮合酶(iNOS)、环氧化酶(COX)-2和丝裂原活化蛋白激酶(MAPKs)的表达,表现出强大的抗炎活性。QCT或Q32G均可降低LPS刺激的RAW 264.7巨噬细胞培养基中COX - 2和iNOS的细胞蛋白水平以及NO、前列腺素E和细胞因子(TNF - α、IL - 1β和IL - 6)的分泌蛋白水平。免疫印迹分析表明,QCT和Q32G抑制LPS诱导的MAP激酶途径蛋白p - p38、ERK和JNK。本研究表明,QCT和Q32G具有抗炎潜力,然而Q32G具有与QCT相当的活性,可作为治疗炎症性疾病的佐剂。