Akram Muhammad, Syed Ahmed Shah, Kim Kyeong-A, Lee Jong Soo, Chang Sun-Young, Kim Chul Young, Bae Ok-Nam
College of Pharmacy Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, Republic of Korea.
CL Institute Korea (CLIK), Ansan, Republic of Korea; Department of Chemistry, Ajou University, Suwon, Republic of Korea.
J Ethnopharmacol. 2015 Nov 4;174:322-30. doi: 10.1016/j.jep.2015.08.028. Epub 2015 Aug 28.
Salvia plebeia R. Br. (SP) has been widely used as a traditional folk medicine for the treatment of infectious diseases and pain. An anti-inflammatory potential of SP has remains largely unknown.
We tried to elucidate the principle mechanism and the active ingredients underlying the anti-inflammatory activities of SP.
We investigated the protective activities of SP methanolic extract (SPME) and seven representative ingredients against inflammation. Quantitative analysis using HPLC-DAD-ESI/MS was conducted to determine the relative amounts of these seven active ingredients in SPME. Both in vitro murine macrophages and in vivo mouse models were employed to elucidate SP- and active ingredient-mediated anti-inflammatory effects.
SPME significantly reduced inflammatory processes both in vivo in a TPA-induced ear edema model and in vitro in lipopolysaccharide (LPS)-activated macrophages. SPME decreased the release of nitric oxide (NO) and prostaglandin E2 (PGE2) and expression of inducible nitric oxide synthase (iNOS). Seven active components (luteoloside (C1), nepitrin (C2), homoplantagenin (C3), luteolin (C4), nepetin (C5), hispidulin (C6), and eupatorin (C7)) of SPME were analyzed and their relative concentrations were determined, demonstrating that C2, C3, C5 and C6 were present in higher amounts than were C1, C4, and C7. These major compounds inhibited NO and PGE2 production, and iNOS and COX-II protein expression through heme oxygenase-1 (HO-1) induction via activation of nuclear factor erythroid 2-related factor2 (Nrf2).
Our data demonstrate that SPME possesses potent in vitro and in vivo anti-inflammatory activities. Nepetin and hispidulin, and their glycosides are the major active compounds in SPME, and their effects are mediated by Nrf2/HO-1 signaling. Taken together, we propose that SPME and its active ingredients may serve as novel therapeutic candidates for diseases associated with excessive inflammation.
荔枝草（Salvia plebeia R. Br.，SP）作为一种传统民间药物，已被广泛用于治疗传染病和疼痛。其抗炎潜力在很大程度上仍不为人知。
我们试图阐明荔枝草抗炎活性的主要机制和活性成分。
我们研究了荔枝草甲醇提取物（SPME）和七种代表性成分的抗炎保护活性。采用HPLC-DAD-ESI/MS进行定量分析，以确定这七种活性成分在SPME中的相对含量。利用体外小鼠巨噬细胞和体内小鼠模型来阐明SP及活性成分介导的抗炎作用。
在体内TPA诱导的耳部水肿模型和体外脂多糖（LPS）激活的巨噬细胞中，SPME均显著减轻了炎症过程。SPME减少了一氧化氮（NO）和前列腺素E2（PGE2）的释放以及诱导型一氧化氮合酶（iNOS）的表达。分析了SPME的七种活性成分（木犀草苷（C1）、尼泊尔黄酮苷（C2）、高车前苷元（C3）、木犀草素（C4）、尼泊尔黄酮（C5）、滨蓟黄素（C6）和泽兰黄素（C7））并确定了它们的相对浓度，结果表明C2、C3、C5和C6的含量高于C1、C4和C7。这些主要化合物通过激活核因子红细胞2相关因子2（Nrf2）诱导血红素加氧酶-1（HO-1），从而抑制NO和PGE2的产生以及iNOS和COX-II蛋白的表达。
我们的数据表明，SPME在体外和体内均具有强大的抗炎活性。尼泊尔黄酮和滨蓟黄素及其糖苷是SPME中的主要活性化合物，它们的作用是由Nrf2/HO-1信号介导的。综上所述，我们认为SPME及其活性成分可能成为与过度炎症相关疾病的新型治疗候选药物。
