MOE Key Laboratory of Protein Sciences, Laboratory of Molecular Pharmacology and Pharmaceutical Sciences, School of Life Sciences, Tsinghua University, Beijing, 100084, China.
School of Pharmacology and Pharmaceutical Sciences, Tsinghua University, Beijing, 100084, China.
Chin J Integr Med. 2019 Jun;25(6):454-461. doi: 10.1007/s11655-017-2952-4. Epub 2017 Aug 9.
To explore the anti-nociceptive effect of patchouli alcohol (PA), the essential oil isolated from Pogostemon cablin (Blanco) Bent, and determine the mechanism in molecular levels.
The acetic acid-induced writhing test and formalin-induced plantar injection test in mice were employed to confirm the effect in vivo. Intracellular calcium ion was imaged to verify PA on mu-opioid receptor (MOR). Cyclooxygenase 2 (COX2) and MOR of mouse brain were expressed for determination of PA's target. Cellular experiments were carried out to find out COX2 and MOR expression induced by PA.
PA significantly reduced latency period of visceral pain and writhing induced by acetic acid saline solution (P<0.01) and allodynia after intra-plantar formalin (P<0.01) in mice. PA also up-regulated COX2 mRNA and protein (P<0.05) with a down-regulation of MOR (P<0.05) both in in vivo and in vitro experiments, which devote to the analgesic effect of PA. A decrease in the intracellular calcium level (P<0.05) induced by PA may play an important role in its anti-nociceptive effect. PA showed the characters of enhancing the MOR expression and reducing the intracellular calcium ion similar to opioid effect.
Both COX2 and MOR are involved in the mechanism of PA's anti-nociceptive effect, and the up-regulation of the receptor expression and the inhibition of intracellular calcium are a new perspective to PA's effect on MOR.
探索来自广藿香（ Pogostemon cablin （ Blanco ） Bent ）的精油对醇的抗伤害作用，并在分子水平上确定其机制。
采用醋酸诱导扭体试验和福尔马林诱导足底注射试验，在体内证实其作用。通过细胞内钙离子成像来验证对μ-阿片受体（ MOR ）的影响。表达小鼠脑内环氧化酶 2 （ COX2 ）和 MOR ，以确定 PA 的作用靶点。通过细胞实验，找出 PA 诱导的 COX2 和 MOR 表达。
PA 可显著延长醋酸盐水诱导的内脏疼痛潜伏期和扭体反应潜伏期（ P<0.01 ），并减少足底福尔马林注射引起的痛觉过敏（ P<0.01 ）。在体内和体外实验中， PA 还上调了 COX2 mRNA 和蛋白（ P<0.05 ），下调了 MOR （ P<0.05 ），这有助于解释 PA 的镇痛作用。 PA 诱导的细胞内钙离子水平降低（ P<0.05 ）可能在其镇痛作用中发挥重要作用。 PA 表现出增强 MOR 表达和减少细胞内钙离子的特性，类似于阿片类药物的作用。
COX2 和 MOR 均参与了 PA 抗伤害作用的机制，上调受体表达和抑制细胞内钙离子可能是 PA 对 MOR 作用的新视角。
