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蒲桃叶成分的镇痛活性:一种来自乙酸乙酯可溶部分的二氢山奈酚鼠李糖苷。

Analgesic activity of Eugenia jambolana leave constituent: a dikaempferol rhamnopyranoside from ethyl acetate soluble fraction.

作者信息

Lingaraju Madhu Cholenahalli, Anand Shikha, Balaganur Venkanna, Kumari Rashmi Rekha, More Amar Sunil, Kumar Dinesh, Bhadoria Brijesh Kumar, Tandan Surendra Kumar

机构信息

Division of Pharmacology and Toxicology, Indian Veterinary Research Institute , Izatnagar, Uttar Pradesh , India and.

出版信息

Pharm Biol. 2014 Aug;52(8):1069-78. doi: 10.3109/13880209.2014.885060.

DOI:10.3109/13880209.2014.885060
PMID:25017653
Abstract

CONTEXT

Eugenia jambolana Lam. (Myrtaceae) is a medicinal plant used in folk medicine for the treatment of diabetes, inflammation, and pain.

OBJECTIVE

We investigated the antinociceptive effect of kaempferol-7-O-α-l-rhamnopyranoside]- 4'-O-4'-[kaempferol-7-O-α-l-rhamnopyranoside (EJ-01), isolated from the E. jambolana leaves.

MATERIALS AND METHODS

EJ-01 (3, 10, and 30 mg kg(-1), orally) was assessed for peripheral (formalin-nociception and acetic acid-writhing) and central (hot plate and tail flick test) analgesic activity in mice and the in vitro anti-inflammatory activity (25, 50, and 100 µg mL(-1)) in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells.

RESULTS AND DISCUSSION

EJ-01 (10 and 30 mg kg(-1)) significantly inhibited mean writhing counts (37.74 and 36.83) in acetic acid writhing and paw licking time (55.16 and 45.66 s) in the late phase of the formalin test as compared with the respective control (60.66 and 104.33 s). EJ-01 did not show analgesic activity in central pain models. Significant reduction in the tumor necrosis factor (TNF)-α (295.48, 51.20, and 49.47 pg mL(-1)) and interleukin (IL)-1β (59.38, 20.08, and 15.46 pg mL(-1)) levels were observed in EJ-01-treated medium (25, 50, and 100 µg mL(-1)) as compared with vehicle-treated control values (788.67 and 161.77 pg mL(-1)), respectively. Significant reduction in total nitrite plus nitrate (NOx) levels (70.80 nmol) was observed in the EJ-01-treated medium (100 µg mL(-1)) as compared with the vehicle-treated value (110.41 nmol).

CONCLUSION

EJ-01 is a valuable analgesic constituent of E. jambolana leaves and this study supports the pharmacological basis for the use of this plant in traditional medicine for curing inflammatory pain.

摘要

背景

毛叶枣(使君子科)是一种药用植物,在民间医学中用于治疗糖尿病、炎症和疼痛。

目的

我们研究了从毛叶枣叶中分离出的山奈酚 -7-O-α-L-鼠李吡喃糖苷]-4'-O-4'-[山奈酚-7-O-α-L-鼠李吡喃糖苷(EJ-01)的抗伤害感受作用。

材料与方法

评估EJ-01(3、10和30 mg kg⁻¹,口服)对小鼠外周(福尔马林致痛和醋酸扭体)和中枢(热板和甩尾试验)镇痛活性以及在脂多糖(LPS)刺激的RAW 264.7细胞中的体外抗炎活性(25、50和100 μg mL⁻¹)。

结果与讨论

与各自的对照组(60.66和104.33秒)相比,EJ-01(10和30 mg kg⁻¹)在醋酸扭体试验中显著抑制平均扭体次数(37.74和36.83),在福尔马林试验后期显著抑制爪舔时间(55.16和45.66秒)。EJ-01在中枢性疼痛模型中未显示镇痛活性。与溶剂处理的对照值(788.67和161.77 pg mL⁻¹)相比,在EJ-01处理的培养基(25、50和100 μg mL⁻¹)中观察到肿瘤坏死因子(TNF)-α(295.48、51.20和49.47 pg mL⁻¹)和白细胞介素(IL)-1β(59.38、20.08和15.46 pg mL⁻¹)水平显著降低。与溶剂处理值(110.41 nmol)相比,在EJ-01处理的培养基(100 μg mL⁻¹)中观察到总亚硝酸盐加硝酸盐(NOx)水平显著降低(70.80 nmol)。

结论

EJ-01是毛叶枣叶中一种有价值的镇痛成分,本研究支持了该植物在传统医学中用于治疗炎性疼痛的药理学基础。

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