具有6-O-取代肉桂基部分的东莨菪苷-梓醇衍生物的抗炎活性比较
Anti-Inflammatory Activity Comparison among Scropoliosides-Catalpol Derivatives with 6-O-Substituted Cinnamyl Moieties.
作者信息
Zhu Tiantian, Zhang Liuqiang, Ling Shuang, Qian Fei, Li Yiming, Xu Jin-Wen
机构信息
Murad Research Institute for Modernized Chinese Medicine, Shanghai University of Traditional Chinese Medicine.
School of Pharmacy, Shanghai University of Traditional Chinese Medicine.
出版信息
Molecules. 2015 Nov 3;20(11):19823-36. doi: 10.3390/molecules201119659.
We have previously shown that scropolioside B has higher anti-inflammatory activity than catalpol does after the inhibition of nuclear factor (NF)-κB activity and IL-1β expression, maturation, and secretion. Various scropoliosides were extracted, isolated, and purified from Scrophularia dentata Royle ex Benth. We then compared their anti-inflammatory activities against LPS-induced NF-κB activity, cytokines mRNA expression, IL-1β secretion, and cyclooxygenase-2 activity. The inhibitory effects of the scropoliosides varied depending on whether the 6-O-substituted cinnamyl moiety was linked to C'' 2-OH, C''3-OH, or C''4-OH, and on the number of moieties linked, which is closely related to the enhancement of antiinflammatory activity. Among these compounds, scropolioside B had the strongest antiinflammatory effects.
我们之前已经表明，在抑制核因子（NF）-κB活性以及白细胞介素-1β（IL-1β）的表达、成熟和分泌后，东莨菪苷B比梓醇具有更高的抗炎活性。从玄参（Scrophularia dentata Royle ex Benth.）中提取、分离并纯化了多种东莨菪苷。然后，我们比较了它们对脂多糖（LPS）诱导的NF-κB活性、细胞因子mRNA表达、IL-1β分泌以及环氧合酶-2活性的抗炎活性。东莨菪苷的抑制作用因6-O-取代肉桂酰基部分与C''2-OH、C''3-OH还是C''4-OH相连，以及相连部分的数量而异，这与抗炎活性的增强密切相关。在这些化合物中，东莨菪苷B具有最强的抗炎作用。
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