Department of Pharmacology and Toxicology, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna, Nigeria; Institute of Pharmacology and Toxicology, Faculty of Medicine, Otto-von-Guericke University, Leipziger Str. 44, 39120 Magdeburg, Germany; Department of Pharmacology and Toxicology, National Institute for Pharmaceutical Research and Development, P. M. B. 21, Abuja, Nigeria.
Institute of Pharmacology and Toxicology, Faculty of Medicine, Otto-von-Guericke University, Leipziger Str. 44, 39120 Magdeburg, Germany.
J Ethnopharmacol. 2016 May 26;184:101-6. doi: 10.1016/j.jep.2016.03.003. Epub 2016 Mar 3.
Extracts of the stem bark of Ficus platyphylla (FP) have been used in traditional the Nigerian medicine to treat psychoses, depression, epilepsy, pain and inflammation. Previous studies have revealed the analgesic and anti-inflammatory effects of FP in different assays including acetic acid-induced writhing, formalin-induced nociception, and albumin-induced oedema.
PURPOSE/METHODS: In this study, we assessed the effects of the standardised extract of FP on hot plate nociceptive threshold and vocalisation threshold in response to electrical stimulation of the tail root in order to confirm its acclaimed analgesic properties. We also investigated the molecular mechanisms underlying these effects, with the focus on opiate receptor binding and the key enzymes of eicosanoid biosynthesis, namely cyclooxygenase (COX) and 5-lipoxygenase (5-LO).
FP (i) increased the hot plate nociceptive threshold and vocalisation threshold. The increase in hot plate nociceptive threshold was detectable over a period of 30min whereas the increase in vocalisation threshold persisted over a period of 90min. (ii) FP showed an affinity for µ opiate receptors but not for δ or κ opiate receptors, and (iii) FP inhibited the activities of COX-2 and 5-LO but not of COX-1.
We provided evidence supporting the use of FP in Nigerian folk medicine for the treatment of different types of pain, and identified opioid and non-opioid targets. It is interesting to note that the dual inhibition of COX-2 and 5-LO appears favourable in terms of both efficacy and side effect profile.
榕属植物的茎皮提取物（FP）在尼日利亚传统医学中被用于治疗精神病、抑郁症、癫痫、疼痛和炎症。先前的研究表明，FP 在不同的测定中具有镇痛和抗炎作用，包括乙酸诱导的扭体、福尔马林诱导的伤害感受和白蛋白诱导的水肿。
目的/方法：在这项研究中，我们评估了 FP 标准化提取物对热板伤害感受阈值和电刺激尾根引起的发声阈值的影响，以确认其公认的镇痛特性。我们还研究了这些作用的分子机制，重点是阿片受体结合和花生四烯酸生物合成的关键酶，即环加氧酶（COX）和 5-脂氧合酶（5-LO）。
FP（i）增加了热板伤害感受阈值和发声阈值。热板伤害感受阈值的增加可在 30 分钟内检测到，而发声阈值的增加可持续 90 分钟。（ii）FP 显示出对 µ 阿片受体的亲和力，但对 δ 或 κ 阿片受体没有亲和力，（iii）FP 抑制 COX-2 和 5-LO 的活性，但不抑制 COX-1 的活性。
我们提供了证据支持 FP 在尼日利亚民间医学中用于治疗不同类型的疼痛，并确定了阿片类和非阿片类靶点。有趣的是，COX-2 和 5-LO 的双重抑制在疗效和副作用方面似乎都有利。
