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ORIGINAL RESEARCH ARTICLE

Polygoni Cuspidati Radix Inhibits the Activation of Syk Kinase in Mast Cells for Antiallergic Activity

Beong Ou Lim^*, Jun Ho Lee, Na Young Ko, Se Hwan Mun, Jie Wan Kim, Do Kyun Kim, Ju Dong Kim, Bo Kyung Kim, Hyung Sik Kim, Erk Her, Hoi Young Lee and Wahn Soo Choi^,1

^* College of Biomedical & Health Science, Konkuk University, Chungju 380-701, Korea; Department of Immunology and Physiology, College of Medicine, Konkuk University, Chungju 380-701, Korea; College of Pharmacy, Pusan National University, Busan 609-735, Korea; and College of Medicine, Konyang University, Nonsan 320-711, Korea

To whom requests for reprints should be addressed at ¹ 322 Danwol-dong, Chungju, Chungbuk-do 380–701, Republic of Korea. E-mail: wahnchoi{at}kku.ac.kr

The antiallergic activity of Polygoni cuspidati radix (PR) and the mechanism of action by which it functions were investigated in this study. The extract of PR exhibited potent inhibitory activity in mast cells; its IC₅₀ values were 62 ± 2.1 µg/ml for RBL-2H3 mast cells and 46 ± 3.2 µg/m for bone marrow–derived mast cells by antigen stimulation, and it also suppressed the expression of tumor necrosis factor- and interleukin-4 in RBL-2H3 cells. According to the in vivo animal allergy model, it inhibited a local allergic reaction, passive cutaneous anaphylaxis, in a dose-dependent manner. With regard to its mechanism of action, PR inhibited the activating phosphorylation of Syk, a key signaling protein for the activation of mast cells. It also suppressed Akt and the mitogen-activated protein kinases ERK1/2, p38, and JNK, which are critical for the production of various inflammatory cytokines in mast cells. The results of the study indicate that the antiallergic activity of PR is mediated through the inhibition of histamine release and allergic cytokine production by the inhibition of Syk activating phosphorylation in mast cells.

Key Words: Polygoni cuspidati radix • anti-allergic activity • mast cells • Syk kinase

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