Lima Milena da Silva, Evangelista Afrânio Ferreira, Santos Gisele Graça Leite Dos, Ribeiro Ivone Maria, Tomassini Therezinha Coelho Barbosa, Pereira Soares Milena Botelho, Villarreal Cristiane Flora
Faculdade de Farmácia, Universidade Federal da Bahia , CEP 40170-290, Salvador, BA, Brazil.
J Nat Prod. 2014 Nov 26;77(11):2397-403. doi: 10.1021/np5003093. Epub 2014 Nov 14.
Pain is the most common reason a patient sees a physician. Nevertheless, the use of typical painkillers is not completely effective in controlling all pain syndromes; therefore further attempts have been made to develop improved analgesic drugs. The present study was undertaken to evaluate the antinociceptive properties of physalins B (1), D (2), F (3), and G (4) isolated from Physalis angulata in inflammatory and centrally mediated pain tests in mice. Systemic pretreatment with 1-4 produced dose-related antinociceptive effects on the writhing and formalin tests, traditional screening tools for the assessment of analgesic drugs. On the other hand, only 3 inhibited inflammatory parameters such as hyperalgesia, edema, and local production of TNF-α following induction with complete Freund's adjuvant. Treatment with 1, 3, and 4 produced an antinociceptive effect on the tail flick test, suggesting a centrally mediated antinociception. Reinforcing this idea, 2-4 enhanced the mice latency reaction time during the hot plate test. Mice treated with physalins did not demonstrate motor performance alterations. These results suggest that 1-4 present antinociceptive properties associated with central, but not anti-inflammatory, events and indicate a new pharmacological property of physalins.
疼痛是患者就医最常见的原因。然而，使用典型的止痛药并不能完全有效地控制所有疼痛综合征；因此，人们进一步尝试研发更有效的镇痛药。本研究旨在评估从酸浆中分离出的酸浆苦素B（1）、D（2）、F（3）和G（4）在小鼠炎症性疼痛和中枢介导性疼痛试验中的抗伤害感受特性。用1 - 4进行全身预处理对扭体试验和福尔马林试验产生了剂量相关的抗伤害感受作用，这两种试验是评估镇痛药的传统筛选工具。另一方面，只有3能抑制完全弗氏佐剂诱导后的炎症参数，如痛觉过敏、水肿和肿瘤坏死因子-α的局部产生。用1、3和4处理对甩尾试验产生了抗伤害感受作用，表明是中枢介导的抗伤害感受。进一步支持这一观点的是，2 - 4延长了小鼠在热板试验中的潜伏期反应时间。用酸浆苦素处理的小鼠未表现出运动性能改变。这些结果表明，1 - 4具有与中枢相关而非抗炎相关的抗伤害感受特性，并表明了酸浆苦素的一种新的药理学特性。
