National Research Center of Engineering & Technology for Utilization of Botanical Functional Ingredients, Hunan Agricultural University, Changsha, Hunan 410128, PR China.
Key Laboratory for Agro-Ecological Processes in Subtropical Region, and South-Central Experimental Station of Animal Nutrition and Feed Science in Ministry of Agriculture, Institute of Subtropical Agriculture, Chinese Academy of Sciences, Changsha, Hunan 410125, PR China.
Eur J Pharmacol. 2015 May 15;755:66-73. doi: 10.1016/j.ejphar.2015.03.002. Epub 2015 Mar 11.
To explore the regulatory mechanisms of magnolol and honokiol on calcium-activated potassium channels signaling pathway in Enterotoxigenic Escherichia coli (ETEC)-induced diarrhea mice, the concentrations of serum chloride ion (Cl(-)), sodium ion (Na(+)), potassium ion (K(+)) and calcium ion (Ca(2+)) were measured. Additionally, the mRNA expressions of calmodulin 1 (CaM), calcium/calmodulin-dependent protein kinase II alpha subunit (CaMKIIα) and beta subunit (CaMKIIβ), ryanodine receptor 1, inositol 1,4,5-trisphosphate receptors (IP3 receptors), protein kinases C (PKC), potassium intermediate/small conductance calcium-activated channels (SK) and potassium large conductance calcium-activated channels(BK)were determined. A diarrhea mouse model was established using ETEC suspensions (3.29×10(9)CFU/ml) at a dosage of 0.02ml/g live body weight (BW). Magnolol or honokiol was intragastrically administered at dosages of 100 (M100 or H100), 300 (M300 or H300) and 500 (M500 or H500) mg/kg BW according to a 3×3 factorial arrangement. Magnolol and honokiol increased the Cl(-) and K(+) concentrations, further, upregulated the CaM, BKα1 and BKβ3 mRNA levels but downregulated the IP3 receptors 1, PKC, SK1, SK2, SK3, SK4 and BKβ4 mRNA expressions. Magnolol and honokiol did not alter the CaMKIIα, CaMKIIβ, ryanodine receptor 1, IP3 receptor 2, IP3 receptor 3, BKβ1 and BKβ2 mRNA expressions. These results clarify that magnolol and honokiol, acting through Ca(2+) channel blockade, inhibit the activation of IP3 receptor 1 to regulate the IP3-Ca(2+) store release, activate CaM to inhibit SK channels, and effectively suppress PKC kinases to promote BKα1 and BKβ3 channels opening and BKβ4 channel closing, which modulates the intestinal ion secretion.
为了探讨厚朴酚和和厚朴酚对产肠毒素大肠埃希菌(ETEC)诱导腹泻小鼠钙激活钾通道信号通路的调节机制,测定了血清氯离子(Cl(-))、钠离子(Na(+))、钾离子(K(+))和钙离子(Ca(2+))的浓度。此外,还测定了钙调蛋白 1(CaM)、钙/钙调蛋白依赖性蛋白激酶 II 阿尔法亚基(CaMKIIα)和贝塔亚基(CaMKIIβ)、兰尼碱受体 1、三磷酸肌醇受体(IP3 受体)、蛋白激酶 C(PKC)、钾中间/小电导钙激活通道(SK)和钾大电导钙激活通道(BK)的 mRNA 表达。采用 ETEC 悬液(3.29×10(9)CFU/ml)以 0.02ml/g 活体重(BW)的剂量建立腹泻小鼠模型。根据 3×3 析因设计,厚朴酚或和厚朴酚以 100(M100 或 H100)、300(M300 或 H300)和 500(M500 或 H500)mg/kg BW 的剂量灌胃给药。厚朴酚和和厚朴酚增加了 Cl(-)和 K(+)浓度,进一步上调了 CaM、BKα1 和 BKβ3 mRNA 水平,但下调了 IP3 受体 1、PKC、SK1、SK2、SK3、SK4 和 BKβ4 mRNA 表达。厚朴酚和和厚朴酚不改变 CaMKIIα、CaMKIIβ、兰尼碱受体 1、IP3 受体 2、IP3 受体 3、BKβ1 和 BKβ2 mRNA 表达。这些结果表明,厚朴酚和和厚朴酚通过钙通道阻断作用,抑制 IP3 受体 1 的激活,调节 IP3-Ca(2+)库释放,激活 CaM 抑制 SK 通道,并有效抑制 PKC 激酶,促进 BKα1 和 BKβ3 通道开放和 BKβ4 通道关闭,从而调节肠道离子分泌。