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积雪草标准化提取物对基质金属蛋白酶、透明质酸酶和弹性蛋白酶的抑制作用。

Matrix metalloproteinase, hyaluronidase and elastase inhibitory potential of standardized extract of Centella asiatica.

机构信息

School of Natural Product Studies, Department of Pharmaceutical Technology, Jadavpur University, Kolkata, West Bengal, India.

出版信息

Pharm Biol. 2013 Sep;51(9):1182-7. doi: 10.3109/13880209.2013.782505. Epub 2013 Jun 13.

Abstract

CONTEXT

Centella asiatica (L.) Urban (Apiaceae), a valuable herb described in Ayurveda, is used in the indigenous system of medicine as a tonic to treat skin diseases.

OBJECTIVE

Centella asiatica methanol extract and its ethyl acetate, n-butanol and aqueous fraction, were subjected for the evaluation of skin care potential through the in vitro hyaluronidase, elastase and matrix metalloproteinase-1 (MMP-1) inhibitory assay.

MATERIALS AND METHODS

The C. asiatica plant was extracted with methanol and fractionated with ethyl acetate, n-butanol and water. The enzymatic activities were evaluated using ursolic acid and oleanolic acid as standards. Isolate molecule asiaticoside was quantified in the crude extract and fractions through high-performance liquid chromatography (HPLC) and structural was characterized by liquid chromatography-mass spectroscopy (LC-MS) and ¹H nuclear magnetic resonance (NMR). Isolated compound was also evaluated for in vitro enzyme assays.

RESULTS

Extract exhibited anti-hyaluronidase and anti-elastase activity with IC₅₀ of 19.27 ± 0.37 and 14.54 ± 0.39 µg/mL, respectively, as compared to ursolic acid. Centella asiatica n-butanol fraction (CAnB) and isolated compound showed significant hyaluronidase (IC₅₀ = 27.00 ± 0.43 and 18.63 ± 0.33 µg/mL) and elastase (IC₅₀ = 29.15 ± 0.31 and 19.45 ± 0.25 µg/mL) inhibitory activities, respectively, and also showed significant MMP-1 inhibition (p < 0.05 and p < 0.01).

DISCUSSION AND CONCLUSION

n-Butanol fraction was found to be most effective among the all fractions from which asiaticoside was isolated and further quantified by HPLC. This work concludes that the asiaticoside from C. asiatica may be a prospective agent for skin care.

摘要

背景

积雪草(Centella asiatica(L.)Urban)是一种在阿育吠陀中被描述的有价值的草药,在本土医学系统中被用作补品来治疗皮肤病。

目的

通过体外透明质酸酶、弹性蛋白酶和基质金属蛋白酶-1(MMP-1)抑制试验,对积雪草甲醇提取物及其乙酸乙酯、正丁醇和水部分进行皮肤护理潜力评价。

材料和方法

用甲醇提取积雪草植物,用乙酸乙酯、正丁醇和水进行部分分离。用熊果酸和齐墩果酸作为标准评估酶活性。通过高效液相色谱法(HPLC)对粗提物和各部分中的单体积雪草酸进行定量,并通过液相色谱-质谱(LC-MS)和 1H 核磁共振(NMR)对其结构进行表征。还对分离得到的化合物进行了体外酶试验评价。

结果

提取物对透明质酸酶和弹性蛋白酶表现出抑制活性,IC50 值分别为 19.27±0.37 和 14.54±0.39μg/mL,与熊果酸相比。与积雪草酸相比,积雪草正丁醇部分(CAnB)和分离得到的化合物对透明质酸酶(IC50 值分别为 27.00±0.43 和 18.63±0.33μg/mL)和弹性蛋白酶(IC50 值分别为 29.15±0.31 和 19.45±0.25μg/mL)具有显著的抑制活性,并且对 MMP-1 也具有显著的抑制作用(p<0.05 和 p<0.01)。

讨论与结论

在所研究的所有部分中,正丁醇部分是最有效的,并且通过 HPLC 对其中的积雪草酸进行了进一步定量。这项工作的结论是,积雪草中的积雪草酸可能是一种有前景的皮肤护理药物。

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