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番石榴叶印度传统医学方剂中多酚类代谢产物分析及其化学预防活性评价。

Metabolite profiling of polyphenols in a Terminalia chebula Retzius ayurvedic decoction and evaluation of its chemopreventive activity.

机构信息

Dipartimento di Scienze della Vita, Università degli Studi di Modena e Reggio Emilia, via G. Campi, 183-41125 Modena, Italy.

出版信息

J Ethnopharmacol. 2013 May 20;147(2):277-85. doi: 10.1016/j.jep.2013.02.025. Epub 2013 Mar 15.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

The decoction of Terminalia chebula fruit is an ayurvedic remedy whose prolonged oral administration is prized as a generic intestinal and hepatic detoxifying agent. Its administration is suggested also under the perspective of a reduced risk of cancer, metabolic and cardiovascular diseases.

AIM OF THE STUDY

To evaluate the phytochemical profile and the chemopreventive potential of Terminalia chebula fruit decoction prepared according to the ayurvedic decoction recipe.

MATERIALS AND METHODS

The quali- and quantitative metabolite profiling of polyphenols was obtained using HPLC-UV/DAD and HPLC-ESI-MS. The crude decoction and purified compounds were tested for their capability to interact with the EphA2-ephrin-A1 system and for their antimutagenic properties against dietary and environmental mutagens (AA, 2-NF, NaN3, and heterocyclic amines IQ, MeIQ, MeIQx, Glu-P1, Glu-P2,) in the Ames-Salmonella/microsome assay, with and without enzymatic induction.

RESULTS

The decoction was found to contain 3,4,6-tri-O-galloyl-d-glucose (55.87 mg/g), chebulic acid (54.03 mg/g), β-punicalagin (41.25mg/g), corilagin (40.31 mg/g), α-punicalagin (35.55 mg/g), chebulagic acid (29.09 mg/g), gallic acid (27.96 mg/g) 1,3,4,6-tri-O-galloyl-β-d-glucose (24.25mg/g) chebulinic acid (20.23 mg/g), 1,2,3,4,6-penta-O-galloyl-d-glucose (13.53 mg/g), ellagic acid (8.00 mg/g), 1,6-di-O-galloyl-d-glucose (4.16 mg/g). An inhibitory effect was recorded in both Salmonella typhimurium TA98 and TA100 strains against the mutagenic activity of heterocyclic amines (22-61%), promutagen AA (91-97%) and directly acting mutagen 2-NF (52%) with but not against NaN3 (7%). Galloyl derivatives allowed an inhibition of mutagenicity induced by MeIQ above 80% at 0.01 mol/plate. Both decoction and purified compounds were able to modulate the EphA2-ephrinA1 system, suggesting a potential multiple chemopreventive mechanism.

CONCLUSIONS

The traditional ayurvedic decoction of Terminalia chebula may harbour a potential as a safe and low-cost chemopreventive agent at the intestinal level, if administered according to the ayurvedic specifications. Moreover, its recourse may enhance the presence of some polyphenolic constituents.

摘要

民族药理学相关性

诃子果实的煎剂是一种阿育吠陀疗法,长期口服被视为一种通用的肠道和肝脏解毒剂。从降低癌症、代谢和心血管疾病风险的角度来看,也建议使用这种药物。

研究目的

评估根据阿育吠陀煎药配方制备的诃子果实煎剂的植物化学成分谱和化学预防潜力。

材料和方法

采用 HPLC-UV/DAD 和 HPLC-ESI-MS 获得多酚的定性和定量代谢产物分析。粗煎剂和纯化化合物均经过 EphA2-ephrin-A1 系统相互作用能力测试和抗饮食和环境诱变剂(AA、2-NF、NaN3 和杂环胺 IQ、MeIQ、MeIQx、Glu-P1、Glu-P2)的致突变性测试,在艾姆斯沙门氏菌/微粒体试验中,进行和不进行酶诱导。

结果

该煎剂被发现含有 3,4,6-三-O-没食子酰基-d-葡萄糖(55.87mg/g)、诃子酸(54.03mg/g)、β-鞣花酸(41.25mg/g)、柯里拉京(40.31mg/g)、α-鞣花酸(35.55mg/g)、诃子酸(29.09mg/g)、没食子酸(27.96mg/g)、1,3,4,6-四-O-没食子酰基-β-d-葡萄糖(24.25mg/g)、诃子鞣宁酸(20.23mg/g)、1,2,3,4,6-五-O-没食子酰基-d-葡萄糖(13.53mg/g)、鞣花酸(8.00mg/g)、1,6-二-O-没食子酰基-d-葡萄糖(4.16mg/g)。该煎剂对沙门氏菌 typhimurium TA98 和 TA100 菌株的致突变活性具有抑制作用,对杂环胺(22-61%)、促突变剂 AA(91-97%)和直接作用诱变剂 2-NF(52%)具有抑制作用,但对 NaN3(7%)没有抑制作用。没食子酰基衍生物在 0.01mol/板时可抑制 MeIQ 诱导的突变性超过 80%。煎剂和纯化化合物均能调节 EphA2-ephrinA1 系统,提示其具有潜在的多种化学预防机制。

结论

如果按照阿育吠陀的规范进行使用,传统的诃子果实阿育吠陀煎剂可能具有作为肠道水平安全、低成本化学预防剂的潜力。此外,其应用可能会增加一些多酚成分的含量。

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