Nannoni Giulia, Volterrani Giulia, Mattarocci Alessandro, AlÌ Alessandro, Bertona Marco, Emanuele Enzo
LaBiotre Srl, Tavarnelle Val di Pesa, Florence, Italy.
2E Science, Robbio, Pavia, Italy.
Cent Eur J Immunol. 2020;45(2):125-129. doi: 10.5114/ceji.2020.97899. Epub 2020 Jul 27.
Bacterial lipopolysaccharide (LPS) initiates several major cellular responses that play a crucial role in the pathogenesis of inflammation, including activation of neutrophils and production of prostaglandin E2 (PGE2) by cyclooxygenase-2 (COX-2).
Recent years have witnessed a growing interest in natural compounds as promising alternatives to synthetic COX-2 inhibitors. In this study, we sought to investigate the effect of a proprietary herbal extract from Lippia citriodora and Plantago lanceolata, titred in verbascoside (≥ 5%) and aucubin (≥ 2%), against LPS-stimulated expressions of COX-2 in human neutrophils using both reverse transcription-polymerase chain reaction (RT-PCR) and a PGE2 immunoassay.
Our main results indicated that: 1. The proprietary herbal extract titred in verbascoside and aucubin is not significantly cytotoxic as shown by the MTT assay; 2. The extract does not significantly inhibit COX-1, whereas it is able to suppress LPS-elicited COX-2 hyperexpression at the mRNA level in human neutrophils; and 3. The effect of the extract at 5% concentration was comparable to that elicited celecoxib 1%, although, in terms of absolute and relative reduction of COX-2 mRNA expression and production of PGE2 in human neutrophils, the drug significantly outperformed the extract.
In general, these results suggest that the proprietary herbal extract titred in verbascoside and aucubin is safe and may possess significant anti-inflammatory and analgesic effects by acting as a specific COX-2 inhibitor. Further studies are required to confirm the clinical efficacy of the extract.
细菌脂多糖(LPS)引发多种主要细胞反应,这些反应在炎症发病机制中起关键作用,包括中性粒细胞的激活以及环氧化酶-2(COX-2)介导的前列腺素E2(PGE2)的产生。
近年来,天然化合物作为合成COX-2抑制剂的有前景的替代物,受到越来越多的关注。在本研究中,我们试图研究一种来自柠檬马鞭草和窄叶车前草的专利草药提取物(其毛蕊花糖苷含量≥5%,桃叶珊瑚苷含量≥2%)对LPS刺激的人中性粒细胞中COX-2表达的影响,采用逆转录聚合酶链反应(RT-PCR)和PGE2免疫测定法。
我们的主要结果表明:1. MTT试验显示,含毛蕊花糖苷和桃叶珊瑚苷的专利草药提取物无明显细胞毒性;2. 该提取物对COX-1无明显抑制作用,但能够在mRNA水平抑制LPS诱导的人中性粒细胞中COX-2的过度表达;3. 5%浓度的提取物的效果与1%塞来昔布相当,不过,就人中性粒细胞中COX-2 mRNA表达的绝对和相对降低以及PGE2的产生而言,该药物的效果明显优于提取物。
总体而言,这些结果表明,含毛蕊花糖苷和桃叶珊瑚苷的专利草药提取物是安全的,并且可能通过作为一种特异性COX-2抑制剂而具有显著的抗炎和镇痛作用。需要进一步研究来证实该提取物的临床疗效。