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在丹参中,酚酸具有抵抗淀粉样β诱导的细胞毒性的保护作用,而丹参酮则作为乙酰胆碱酯酶抑制剂发挥作用。

In Salvia miltiorrhiza, phenolic acids possess protective properties against amyloid β-induced cytotoxicity, and tanshinones act as acetylcholinesterase inhibitors.

机构信息

New Medicine R&D Center, Disha Pharmaceutical Group, Weihai 264205, PR China.

出版信息

Environ Toxicol Pharmacol. 2011 May;31(3):443-52. doi: 10.1016/j.etap.2011.02.006. Epub 2011 Feb 26.

DOI:10.1016/j.etap.2011.02.006
PMID:21787715
Abstract

Radix Salvia miltiorrhiza (RSM), a traditional Chinese medicinal herb, has been alleged to possess therapeutic effects against senile dementia, also known as Alzheimer's disease (AD). However, the effects of the major components in RSM on cytotoxicity induced by amyloid-β peptide (Aβ) and on acetylcholinesterase activity have not been studied in depth to date. In this report, the effects of RSM aqueous/ethanol extracts, total polyphenols, total tanshinones and 3 phenolic compounds against toxicity mediated by Aβ(25-35) were tested with PC-12 cells. The results showed that Aβ(25-35)-induced cytotoxicity was revised by RSM aqueous/ethanol extracts and total polyphenols and that danshensu and salvianolic acid B could protect PC-12 cells by blocking Aβ(25-35)-induced Ca(2+)-intake, lactate dehydrogenase release, cell viability decrease and apoptosis. In addition, the activities of RSM extracts and relevant constituents in their inhibition of acetylcholinesterase were investigated using rat brain homogenates as an enzyme resource. Galanthamine hydrobromide, an accepted acetylcholinesterase inhibitor, was employed as a positive control agent. Our preliminary studies demonstrated that RSM ethanol extract, total tanshinones, tanshinone I and dihydrotanshinone I had remarkable inhibition effects on acetylcholinesterase in vitro. These findings suggest that both tanshinones and polyphenols in RSM are the active constituents responsible for the beneficial effects of this herb in AD treatment.

摘要

丹参(Radix Salvia miltiorrhiza,RSM),一种传统的中草药,据称对老年痴呆症(AD)也有治疗作用。然而,到目前为止,RSM 中的主要成分对淀粉样β肽(Aβ)诱导的细胞毒性和乙酰胆碱酯酶活性的影响尚未进行深入研究。在本报告中,用 PC-12 细胞测试了 RSM 水/乙醇提取物、总多酚、总丹参酮和 3 种酚类化合物对 Aβ(25-35)介导的毒性的影响。结果表明,RSM 水/乙醇提取物和总多酚可纠正 Aβ(25-35)诱导的细胞毒性,丹酚酸 B 和丹参素可通过阻断 Aβ(25-35)诱导的 Ca(2+)摄取、乳酸脱氢酶释放、细胞活力下降和凋亡来保护 PC-12 细胞。此外,还使用大鼠脑匀浆作为酶源研究了 RSM 提取物及其相关成分对乙酰胆碱酯酶活性的抑制作用。氢溴酸加兰他敏作为公认的乙酰胆碱酯酶抑制剂,被用作阳性对照剂。我们的初步研究表明,RSM 乙醇提取物、总丹参酮、丹参酮 I 和二氢丹参酮 I 对体外乙酰胆碱酯酶具有显著的抑制作用。这些发现表明,RSM 中的丹参酮和多酚都是该草药对 AD 治疗有益作用的活性成分。

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