Shandong Academy of Pharmaceutical Science, Jinan 250101, China.
School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.
Mar Drugs. 2017 Sep 20;15(9):294. doi: 10.3390/md15090294.
The hard-shelled mussel () has been used as Chinese traditional medicine for thousands of years; however, to date the ingredients responsible for the various beneficial health outcomes attributed to are still unclear. An α-d-Glucan, called MP-A, was isolated from , and observed to exert anti-inflammatory activity in THP-1 human macrophage cells. Specifically, we showed that MP-A treatment inhibited the production of inflammatory markers, including TNF-α, NO, and PGE2, inducible NOS (iNOS), and cyclooxygenase-2 (COX-2), in LPS-activated THP-1 cells. It was also shown to enhance phagocytosis in the analyzed cells, but to severely inhibit the phosphorylation of mitogen-activated protein kinases (MAPKs) and the nuclear translocation of NF-κB P65. Finally, MP-A was found to exhibit a high binding affinity for the cell surface receptor TLR4, but a low affinity for TLR2 and dectin-1, via surface plasmon resonance (SPR) analysis. The study indicates that MP-A suppresses LPS-induced TNF-α, NO and PEG2 production via TLR4/NF-κB/MAPK pathway inhibition, and suggests that MP-A may be a promising therapeutic candidate for diseases associated with TNF-α, NO, and/or PEG2 overproduction.
贻贝（）已被用作中药几千年；然而，迄今为止，归因于 的各种有益健康结果的成分仍不清楚。一种名为 MP-A 的α-d-葡聚糖从贻贝中分离出来，并观察到它在 THP-1 人巨噬细胞中具有抗炎活性。具体而言，我们表明，MP-A 处理抑制了 LPS 激活的 THP-1 细胞中炎症标志物 TNF-α、NO 和 PGE2、诱导型一氧化氮合酶（iNOS）和环氧化酶-2（COX-2）的产生。它还显示出增强在分析的细胞中的吞噬作用，但严重抑制丝裂原活化蛋白激酶（MAPK）的磷酸化和 NF-κB P65 的核易位。最后，通过表面等离子体共振（SPR）分析发现，MP-A 对细胞表面受体 TLR4 具有高结合亲和力，但对 TLR2 和 dectin-1 的亲和力较低。该研究表明，MP-A 通过 TLR4/NF-κB/MAPK 途径抑制抑制 LPS 诱导的 TNF-α、NO 和 PEG2 的产生，并且表明 MP-A 可能是与 TNF-α、NO 和/或 PEG2 过度产生相关的疾病的有前途的治疗候选物。
