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刺五加茎皮中的齐墩果烷型三萜和皂苷对脂多糖刺激的骨髓来源树突状细胞产生促炎细胞因子的抑制作用。

Inhibitory effects of oleanane-type triterpenes and saponins from the stem bark of Kalopanax pictus on LPS-stimulated pro-inflammatory cytokine production in bone marrow-derived dendritic cells.

机构信息

College of Pharmacy, Chungnam National University, Daejeon, 305-764, Korea.

出版信息

Arch Pharm Res. 2013 Mar;36(3):327-34. doi: 10.1007/s12272-013-0031-8. Epub 2013 Feb 27.

DOI:10.1007/s12272-013-0031-8
PMID:23444041
Abstract

Kalopanax pictus (Araliaceae) is a deciduous tree distributed in Korea, Japan, and China. The stem bark of K. pictus has been functionally used as a traditional crude drug for the treatment of various inflammatory diseases. In the present study, we describe the inhibitory effects of oleanane-type triterpenes and saponins isolated from the stem bark of K. pictus on production of pro-inflammatory cytokines in LPS-stimulated bone marrow-derived dendritic cells. Of the compounds tested, 16,23,29-trihydroxy-3-oxo-olean-12-en-28-oic acid (1), 4,23,29-trihydroxy-3,4-seco-olean-12-en-3-oate-28-oic acid (2), 3β,6β,23-trihydroxyolean-12-en-28-oic acid 28-O-β-D-glucopyranoside (3), nipponogenin E (6), 3β,6β,23-trihydroxyolean-12-en-28-oic acid (7), and caulophyllogenin (19) significantly inhibited the production of IL-12 p40 and IL-6 with IC50 values ranging from 3.3 to 9.1 μM. Compounds 2, 3, 7, and 19 significantly suppressed the secretion of TNF-α with IC50 ranging from 8.8 to 20.0 μM. These data provide scientific support for the use of K. pictus stem bark and its triterpene and saponin components in the inhibition of pro-inflammatory cytokine secretion, including IL-12 p40, IL-6, and TNF-α, and for prevention and treatment of inflammatory diseases.

摘要

朝鲜白木(五加科)是一种落叶乔木,分布于韩国、日本和中国。朝鲜白木的茎皮作为一种传统的粗提物,具有治疗各种炎症性疾病的功能。在本研究中,我们描述了从朝鲜白木茎皮中分离得到的齐墩果烷型三萜和皂苷对脂多糖刺激的骨髓来源树突状细胞产生促炎细胞因子的抑制作用。在所测试的化合物中,16,23,29-三羟基-3-氧代-齐墩烷-12-烯-28-酸(1)、4,23,29-三羟基-3,4-裂环齐墩烷-12-烯-3-羧酸-28-酸(2)、3β,6β,23-三羟基齐墩烷-12-烯-28-酸 28-O-β-D-吡喃葡萄糖苷(3)、nipponogenin E(6)、3β,6β,23-三羟基齐墩烷-12-烯-28-酸(7)和长春质碱(19)显著抑制了 IL-12 p40 和 IL-6 的产生,IC50 值范围为 3.3 至 9.1 μM。化合物 2、3、7 和 19 显著抑制 TNF-α 的分泌,IC50 值范围为 8.8 至 20.0 μM。这些数据为朝鲜白木茎皮及其三萜和皂苷成分在抑制促炎细胞因子(包括 IL-12 p40、IL-6 和 TNF-α)分泌方面的应用提供了科学依据,可用于炎症性疾病的预防和治疗。

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