Neuropharmacology Research Laboratory, Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi, India.
Stettiner Straße 1, Karlsruhe, Germany.
J Tradit Complement Med. 2014 Dec 19;5(1):42-50. doi: 10.1016/j.jtcme.2014.10.002. eCollection 2015 Jan.
Andrographolide is a major bioactive secondary plant metabolite isolated Andrographis paniculata (Burm. F.) Wall. Ex. Nees. ( chuān xīn lián), a well-known traditionally used medicinal herb. The aim of the study was to pharmacologically evaluate the beneficial effect of andrographolide on stress-induced thermoregulatory and other physiological responses in mice. A stress-induced hyperthermia test was conducted in mice. The test agents were orally administered once daily for 11 consecutive days, and treatment effects on body weight changes, basal rectal temperature, and foot-shock-triggered hyperthermic responses were quantified on Day 1, Day 5, Day 7, and Day 10 of the experiments. Pentobarbital-induced hypnosis was quantified on the 11(th) day of treatment. Observations made during a pilot dose finding experiment revealed that, like A. paniculata extracts, pure andrographolide also possess adaptogenic properties. Observed dose-dependent efficacies of 3 mg/kg/d, 10 mg/kg/d, and 30 mg/kg/d andrographolide in the pilot experiment were reconfirmed by conducting two further analogous experiments using separate groups of either male or female mice. In these confirmatory experiments, efficacies of andrographolide were compared with that of 5 mg/kg/d oral doses of the standard anxiolytic diazepam. Significantly reduced body weights and elevated core temperatures of the three vehicle-treated control groups observed on the 5(th) day and subsequent observational days were completely absent even in the groups treated with the lowest andrographolide dose (3 mg/kg/d) or diazepam (5 mg/kg/d). Benzodiazepine-like potentiation of pentobarbital hypnosis was observed in andrographolide-treated animals. These observations reveal that andrographolide is functionally a diazepam-like desensitizer of biological mechanisms, and processes involved in stress trigger thermoregulatory and other physiological responses.
穿心莲是一种主要的生物活性植物次生代谢产物,从穿心莲(Burm. F.)Wall。前。 Nees.(川新莲)中分离出来,穿心莲是一种众所周知的传统药用植物。本研究的目的是从药理学上评价穿心莲内酯对小鼠应激诱导的体温调节和其他生理反应的有益作用。在小鼠中进行应激诱导的发热试验。试验药物每天口服一次,连续 11 天,在试验的第 1、5、7 和 10 天,对体重变化、基础直肠温度和电击诱发的发热反应进行定量,并在第 11 天进行戊巴比妥诱导的催眠作用定量。在探索性剂量发现试验中观察到,与穿心莲提取物一样,纯穿心莲内酯也具有适应原性。在探索性试验中,3mg/kg/d、10mg/kg/d 和 30mg/kg/d 的穿心莲内酯表现出剂量依赖性的疗效,这一结果在使用单独的雄性或雌性小鼠进行的另外两个类似试验中得到了证实。在这两个验证试验中,穿心莲内酯的疗效与 5mg/kg/d 口服剂量的标准抗焦虑药地西泮进行了比较。在第 5 天和随后的观察日,三个载体处理的对照组的体重显著减轻,核心体温升高,这种情况在接受最低剂量的穿心莲内酯(3mg/kg/d)或地西泮(5mg/kg/d)治疗的组中完全不存在。在接受穿心莲内酯治疗的动物中观察到苯二氮䓬类药物增强戊巴比妥催眠作用。这些观察结果表明,穿心莲内酯在功能上是一种苯二氮䓬类药物,可使生物机制脱敏,参与应激触发的体温调节和其他生理反应的过程。