Ma Shuli, Zhang Dawei, Lou Hongxiang, Sun Longru, Ji Jianbo
Department of Natural Products Chemistry, Key Lab of Chemical Biology (MOE), School of Pharmaceutical Sciences, Shandong University, Jinan 250012, PR China.
Department of Vascular Surgery, Affiliated Hospital of Shandong University of Traditional Chinese Medicine, Jinan 250014, PR China.
J Ethnopharmacol. 2016 Jul 21;188:193-9. doi: 10.1016/j.jep.2016.05.018. Epub 2016 May 10.
Salvia miltiorrhiza var. alba roots are used as the Chinese traditional medicine Danshen for the treatment of cardiovascular diseases in local clinical practice. Tanshinones are the major effective constituents of S. miltiorrhiza var. alba roots, but only tanshinone IIA, tanshinone I, cryptotanshinone, and 15,16-dihydrotanshinone have been investigated for their anti-inflammatory activities.
Eleven known compounds were isolated from S. miltiorrhiza var. alba roots, and the structures of all compounds were elucidated by spectroscopic analysis and comparisons with reported data. Immune anti-inflammatory activities were assessed by the ability to inhibit the production of tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and interleukin (IL)-8 using enzyme-linked immunosorbent assay. Quantitative real-time polymerase chain reaction (qRT-PCR) was also used to compare the inhibitory effects of the compounds on TNF-α, IL-1β, and IL-8 mRNA expression with that of tanshinone IIA in lipopolysaccharide-stimulated THP-1 macrophages.
All tanshinones, except for compound 5, significantly inhibited the mRNA and protein expression of TNF-α, IL-1β, and IL-8, and their anti-inflammatory activities were stronger than that of tanshinone IIA. Compound 9 (5μM) showed the highest inhibitory effects for TNF-α, IL-1β, and IL-8, at 56.3%, 67.6%, and 51.7%, respectively.
Ten of the 11 tanshinones were shown to have anti-inflammatory properties superior to those of TSIIA, and which significantly inhibited the expression of TNF-α, IL-1β, and IL-8. The present results provided a referential basis for explaining the use of S. miltiorrhiza var. alba root as a Chinese folk medicine for treating cardiovascular diseases associated with inflammation, and show the importance of trace constituents of this herb.
白花丹参根在当地临床实践中被用作治疗心血管疾病的中药丹参。丹参酮是白花丹参根的主要有效成分,但仅对丹参酮IIA、丹参酮I、隐丹参酮和15,16 - 二氢丹参酮的抗炎活性进行了研究。
从白花丹参根中分离出11种已知化合物,通过光谱分析并与报道数据进行比较确定了所有化合物的结构。采用酶联免疫吸附测定法,通过抑制肿瘤坏死因子(TNF)-α、白细胞介素(IL)-1β和白细胞介素(IL)-8产生的能力来评估免疫抗炎活性。还使用定量实时聚合酶链反应(qRT-PCR)比较这些化合物对脂多糖刺激的THP-1巨噬细胞中TNF-α、IL-1β和IL-8 mRNA表达的抑制作用与丹参酮IIA的抑制作用。
除化合物5外,所有丹参酮均显著抑制TNF-α、IL-1β和IL-8的mRNA和蛋白表达,且它们的抗炎活性均强于丹参酮IIA。化合物9(5μM)对TNF-α、IL-1β和IL-8的抑制作用最高,分别为56.3%、67.6%和51.7%。
11种丹参酮中的10种显示出优于丹参酮IIA的抗炎特性,并显著抑制TNF-α、IL-1β和IL-8的表达。本研究结果为解释白花丹参根作为治疗与炎症相关心血管疾病的民间草药的用途提供了参考依据,并显示了该草药微量成分的重要性。