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麻叶荨麻地上部分的乙醇提取物的化学成分、药理作用和毒性。

Chemical characterization, pharmacological effects, and toxicity of an ethanol extract of Celtis pallida Torr. (Cannabaceae) aerial parts.

机构信息

Department of Pharmacy, Division of Natural and Exact Sciences, University Guanajuato, Noria Alta sin número, C.P. 36040 Guanajuato, Gto., Mexico.

School of Chemical Sciences, Autonomous University of San Luis Potosí, San Luis Potosí, Mexico.

出版信息

J Ethnopharmacol. 2018 Jun 12;219:126-132. doi: 10.1016/j.jep.2018.03.014. Epub 2018 Mar 12.

DOI:10.1016/j.jep.2018.03.014
PMID:29545209
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Celtis pallida Torr (Cannabaceae) is employed as a folk medicine for the treatment of inflammation, pain, skin infections, and diarrhea, among other diseases.

AIM OF THE STUDY

The purpose of this work was to assess the chemical composition, the in vitro and in vivo toxicity, the antimicrobial, anti-inflammatory, antidiarrheal, antinociceptive, locomotor, and sedative effects of an ethanolic extract obtained from Celtis pallida aerial parts (CPE).

MATERIALS AND METHODS

The composition of CPE was carried out by GC-MS. The in vitro and in vivo toxic activity of CPE was estimated with the comet assay (10-1000 µg/ml) for 5 h in peripheral blood mononuclear cells, and the acute toxicity test (500-5000 mg/kg p.o.), for 14 days, respectively. The antimicrobial effect of CPE was evaluated using the minimum inhibitory concentration (MIC) assay, whereas the antidiarrheal activity (10-200 mg/kg p.o.) was calculated using the castor oil test. The antinociceptive effects of CPE (50-200 mg/kg p.o.) were estimated with the acetic acid and formalin tests, as well as the hot plate test. The sedative and locomotor activities of CPE (50-200 mg/kg p.o.) were assessed with the pentobarbital-induced sleeping time test and the rotarod test, respectively.

RESULTS

The main compound found in CPE was the triterpene ursolic acid (22% of the extract). CPE at concentrations of 100 µg/ml or higher induced genotoxicity in vitro and showed low in vivo toxicity (LD > 5000 mg/kg p.o.). Additionally, CPE lacked (MIC > 400 µg/ml) antimicrobial activity but exerts antinociceptive (ED = 12.5 ± 1.5 mg/kg) and antidiarrheal effects (ED = 2.8 mg/kg), without inducing sedative effects or altering the locomotor activity. The antinociceptive activity of CPE suggests the participation of adrenoceptors, as well as the nitric oxide/cyclic guanosine monophosphate (cGMP) pathway.

CONCLUSION

C. pallida exerts its antinociceptive effects probably mediated by the nitric oxide/cyclic guanosine monophosphate (cGMP) pathway.

摘要

民族药理学相关性

朴树(大麻科)被用作民间药物,用于治疗炎症、疼痛、皮肤感染和腹泻等疾病。

研究目的

本工作的目的是评估从朴树地上部分获得的乙醇提取物(CPE)的化学成分、体外和体内毒性、抗菌、抗炎、抗腹泻、镇痛、运动和镇静作用。

材料和方法

通过 GC-MS 进行 CPE 的成分分析。通过外周血单个核细胞中的彗星试验(10-1000μg/ml)评估 CPE 的体外和体内毒性活性,5 小时;通过急性毒性试验(500-5000mg/kg p.o.),14 天。通过最低抑菌浓度(MIC)测定评估 CPE 的抗菌作用,而通过蓖麻油试验计算抗腹泻作用(10-200mg/kg p.o.)。通过醋酸和福尔马林试验以及热板试验评估 CPE 的镇痛作用(50-200mg/kg p.o.)。通过戊巴比妥钠诱导的睡眠时间试验和转棒试验分别评估 CPE 的镇静和运动活性(50-200mg/kg p.o.)。

结果

CPE 中的主要化合物是三萜熊果酸(占提取物的 22%)。CPE 在 100μg/ml 或更高浓度下诱导体外遗传毒性,体内毒性低(LD > 5000mg/kg p.o.)。此外,CPE 缺乏抗菌活性(MIC > 400μg/ml),但具有镇痛(ED = 12.5±1.5mg/kg)和抗腹泻作用(ED = 2.8mg/kg),不引起镇静作用或改变运动活性。CPE 的镇痛作用提示参与肾上腺素能受体以及一氧化氮/环鸟苷酸(cGMP)途径。

结论

朴树可能通过一氧化氮/环鸟苷酸(cGMP)途径发挥其镇痛作用。

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