Yadav Vaishali, Chatterjee Shyam Sunder, Majeed Muhammed, Kumar Vikas
Neuropharmacology Research Laboratory, Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi, 221005, India.
Stettiner Straβe 1, Karlsruhe, Germany.
J Tradit Complement Med. 2015 Dec 11;6(4):413-423. doi: 10.1016/j.jtcme.2015.11.001. eCollection 2016 Oct.
To compare stress resistance increasing and analgesic activities of piperlongumine and a methanolic fruit extract (PLE).
Efficacies of a single and repeated daily oral doses (1-256 mg/kg/day) of PLE, piperlongumine, and 50 mg/kg/day doxycycline against foot shock stress triggered alteration in body weights and core temperatures, and of their 11 daily doses on antidepressants like activity in tail suspension test and on pentobarbital induced sedation in male mice were compared. In another experiment, analgesic activities of single and repeated daily 5 mg/kg oral doses of piperlongumine and PLE in mice hot plate test and in acetic acid induced writing tests were compared with those of aspirin and doxycycline.
After their single oral doses no effects of piperlongumine or PLE or doxycycline were observed in the footshock stress induced hyperthermia test or in hot plate test. However, significant effects of piperlongumine and PLE in both the tests were observed after their 5 or more daily doses. Both of them also dose dependently suppressed daily handling and repetitive testing triggered alterations in body weights and core temperatures. Their doxycycline like antidepressant activity in tail suspension test and aspirin like analgesic effects in acetic acid writhing test were observed after their 11 daily 5 mg/kg oral dose.
Piperlongumine is another bioactive secondary metabolite of and other plants of piper species with stress response suppressing, analgesic, and anti-inflammatory activities. Its bactericidal activities can also contribute to its therapeutically interesting bio-activity profile.
比较荜茇明碱和胡椒果实甲醇提取物（PLE）增强抗应激及镇痛的活性。
比较单次及每日重复口服剂量（1 - 256毫克/千克/天）的PLE、荜茇明碱以及50毫克/千克/天强力霉素对足部电击应激引发的体重和核心体温变化的影响，以及它们连续11天给药对雄性小鼠在悬尾试验中的抗抑郁样活性和戊巴比妥诱导的镇静作用的影响。在另一项实验中，将单次及每日重复口服5毫克/千克剂量的荜茇明碱和PLE在小鼠热板试验及醋酸诱导扭体试验中的镇痛活性与阿司匹林和强力霉素的进行比较。
单次口服给药后，在足部电击应激诱导的体温过高试验或热板试验中未观察到荜茇明碱、PLE或强力霉素的作用。然而，连续5天或更多天给药后，在两项试验中均观察到荜茇明碱和PLE有显著作用。它们还剂量依赖性地抑制了每日处理和重复测试引发的体重和核心体温变化。连续11天每日口服5毫克/千克剂量后，观察到它们在悬尾试验中有类似强力霉素的抗抑郁活性，在醋酸扭体试验中有类似阿司匹林的镇痛作用。
荜茇明碱是胡椒属及其他胡椒科植物的另一种具有应激反应抑制、镇痛和抗炎活性的生物活性次生代谢产物。其杀菌活性也有助于其具有治疗意义的生物活性谱。
