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《台东荚蒾乙酸乙酯提取物的抗炎和镇痛活性》

The anti-inflammatory and analgesic activities of the ethyl acetate extract of Viburnum taitoense Hayata.

机构信息

School of Pharmaceutical Science, Guangxi Medical University, Nanning, 530021, China.

Guangxi Institute of Chinese Medicine and Pharmaceutical Science, Nanning, 530022, China.

出版信息

J Ethnopharmacol. 2021 Apr 6;269:113742. doi: 10.1016/j.jep.2020.113742. Epub 2020 Dec 24.

DOI:10.1016/j.jep.2020.113742
PMID:33359186
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Viburnum taitoense Hayata has been used as folk medicine by the minority people in Southwestern China for a long history, especially in Guangxi Zhuang Autonomous Region. The minority in Guangxi including Zhuang, Miao and Yao people use the ethanol extract of V. taitoense Hayata to treat the fracture, kill the pain of rheumatism because of its definite therapeutic effects.

AIM OF THE STUDY

So far, the scientific investigation of V. taitoense Hayata is done very little. Here, we first prepared the ethyl acetate extract of V. taitoense (EEVt), secondly measured the contents of phenols, flavonoids, and terpenoids in EEVt, and thirdly, the anti-inflammatory and analgesic activities of EEVt were investigated by invitro model of RAW 264.7 cells and invivo models of inflammation and pain in rats and mice.

MATERIALS AND METHODS

The contents of phenols, flavonoids, and terpenoids in EEVt were determined by UV spectrophotometry, respectively. The anti-inflammatory effect of EEVt (5, 25, 50, 100, and 200 μg/mL) in vitro was tested by determining its inhibitory effect on the nitric oxide production of RAW264.7 cells activated by lipopolysaccharide (LPS). The anti-inflammatory and analgesic effects of EEVt in vivo were investigated in the following experimental rats and mice models: carrageenan-induced paw edema, corton-oil-induced ear edema, acetic acid writhing test, and formalin pain test.

RESULTS

The contents of total phenolic, total flavonoids, and total triterpenoids in V. taitoense were measured to be 3.46 ± 0.04%, 2.38 ± 0.04%, and 14.96 ± 0.17%, respectively. In vitro test showed that EEVt at different tested dosages (5, 25, 50, 100, and 200 μg/mL) had no significant toxicity to RAW264.7 macrophages. At dosages of 37.5 and 75 μg/mL of EEVt significant inhibitory (p < 0.001) on the productions of nitric oxide (NO). High dosage (200 μg/mL) of EEVt displayed highly significant inhibitory (p < 0.001) on the productions of proinflammatory cytokines IL-6, IL-1β, and TNF-α from the LPS-induced RAW264.7 macrophages. EEVt showed obvious anti-inflammatory activity at different time points after carrageenan injection (p < 0.05) in vivo test, and its anti-inflammatory activity reached the strongest 4 h. Similarly, through the ear swelling test, EEVt (200 mg/kg) showed significant (p < 0.05) anti-inflammatory activity. Besides, formalin and acetic acid writhing experiments also showed that EEVt has significant (p < 0.05) analgesic activity.

CONCLUSION

EEVt was confirmed to be definite anti-inflammatory and analgesic effects, and the phytochemicals of EEVt was disclosed to be rich in triterpenoids, which was worthy to be further investigated.

摘要

民族药理学相关性

薇甘菊(Viburnum taitoense Hayata)在西南少数民族地区作为民间药物已有很长的历史,尤其是在广西壮族自治区。广西的少数民族,包括壮族、苗族和瑶族,都使用薇甘菊(Viburnum taitoense Hayata)的乙醇提取物来治疗骨折和风湿疼痛,因为它有明确的治疗效果。

研究目的

到目前为止,对薇甘菊(Viburnum taitoense Hayata)的科学研究很少。在这里,我们首先制备了薇甘菊(Viburnum taitoense Hayata)的乙酸乙酯提取物(EEVt),其次测量了 EEVt 中酚类、类黄酮和萜类化合物的含量,第三,通过 RAW 264.7 细胞的体外模型和大鼠和小鼠的炎症和疼痛体内模型研究了 EEVt 的抗炎和镇痛活性。

材料和方法

采用紫外分光光度法分别测定 EEVt 中酚类、类黄酮和萜类化合物的含量。通过测定 LPS 激活的 RAW264.7 细胞中一氧化氮(NO)的产生抑制作用,体外测试 EEVt(5、25、50、100 和 200μg/ml)的抗炎作用。采用角叉菜胶致足肿胀、角叉菜胶致耳肿胀、醋酸扭体试验和福尔马林疼痛试验,研究 EEVt 在以下实验大鼠和小鼠模型中的抗炎和镇痛作用。

结果

薇甘菊中总酚、总黄酮和总三萜的含量分别为 3.46±0.04%、2.38±0.04%和 14.96±0.17%。体外试验表明,不同剂量(5、25、50、100 和 200μg/ml)的 EEVt 对 RAW264.7 巨噬细胞无明显毒性。在 37.5 和 75μg/ml 的 EEVt 剂量下,对一氧化氮(NO)的产生有显著抑制作用(p<0.001)。高剂量(200μg/ml)的 EEVt 对 LPS 诱导的 RAW264.7 巨噬细胞产生的促炎细胞因子 IL-6、IL-1β和 TNF-α有高度显著抑制作用(p<0.001)。在体内试验中,不同时间点给予 EEVt(200mg/kg)后,均显示出明显的抗炎活性(p<0.05),其抗炎活性在 4 小时达到最强。同样,通过耳肿胀试验,EEVt(200mg/kg)也显示出显著的抗炎活性(p<0.05)。此外,福尔马林和醋酸扭体实验也表明,EEVt 具有显著的镇痛活性(p<0.05)。

结论

EEVt 被证实具有明确的抗炎和镇痛作用,其植物化学物质富含三萜类化合物,值得进一步研究。

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