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评价从孟加拉药用植物金毛狗脊中分离得到的派屈蛇麻烷、二十四烷和多种类黄酮的细胞毒性活性。

Evaluation of cytotoxic activity of patriscabratine, tetracosane and various flavonoids isolated from the Bangladeshi medicinal plant Acrostichum aureum.

机构信息

School of Pharmacy, Griffith University, Gold Coast campus, Queensland, Australia.

出版信息

Pharm Biol. 2012 Oct;50(10):1276-80. doi: 10.3109/13880209.2012.673628. Epub 2012 Aug 20.

DOI:10.3109/13880209.2012.673628
PMID:22906240
Abstract

CONTEXT

Acrostichum aureumL. (Pteridaceae), a mangrove fern, has been used as a Bangladeshi traditional medicine for a variety of diseases including peptic ulcer.

OBJECTIVE

Isolation and structural elucidation of cytotoxic secondary metabolites from the methanol extract of the aerial parts of A. aureum.

MATERIALS AND METHODS

Compounds were isolated using HPLC. The compound structures were elucidated by 1D and 2D NMR, MS and other spectroscopic methods using published data. The compounds were tested for their cytotoxic activity against healthy and cancer cells using the MTT assay. Active compounds were further evaluated for apoptosis-and necrosis-inducing potential against gastric cancer cells (AGS) using the FITC Annexin V apoptosis assay.

RESULTS AND DISCUSSION

Seven known compounds, patriscabratine, tetracosane and 5 flavonoids (quercetin-3-O-β-d-glucoside, quercetin-3-O-β-d-glucosyl-(6→1)-α-l-rhamnoside, quercetin-3-O-α-l-rhamnoside, quercetin-3-O-α-l-rhamnosyl-7-O-β-d-glucoside and kaempferol) were isolated. Patriscabratine was found moderately cytotoxic against AGS, MDA-MB-231 and MCF-7 cells with IC(50) values ranging from 69.8 to 197.3 μM. Tetracosane showed some cytotoxic activity against AGS, MDA-MB-231, HT-29 and NIH 3T3 cells with IC(50) values ranging from 128.7 to >250 μM. Patriscabratine and tetracosane displayed an apoptotic effect (10%) on AGS cells within 24 h which was increased (20%) after 48 h, and was comparable to, if not greater, than the positive control, cycloheximide.

CONCLUSION

Except for quercetin-3-O-β-d-glucoside and kaempferol; compounds were isolated for the first time from this plant and evaluated for their cytotoxic activity. The results highlight the potential of this plant as a source of bioactive compounds and provide a rationale for its traditional use in peptic ulcer treatment.

摘要

背景

金毛狗蕨(凤尾蕨科)是一种红树林蕨类植物,已被用作孟加拉传统药物,用于治疗各种疾病,包括消化性溃疡。

目的

从金毛狗蕨地上部分甲醇提取物中分离具有细胞毒性的次生代谢产物,并对其结构进行鉴定。

材料与方法

采用高效液相色谱法进行化合物分离。通过 1D 和 2D NMR、MS 及其他光谱方法并结合文献数据对化合物结构进行解析。采用 MTT 法测定化合物对正常细胞和癌细胞的细胞毒性。采用 FITC Annexin V 凋亡检测法,进一步评价活性化合物对胃癌细胞(AGS)的促凋亡和促坏死作用。

结果与讨论

从金毛狗蕨中分离得到 7 个已知化合物,分别为:原小檗碱、二十四烷和 5 种黄酮类化合物(槲皮素-3-O-β-d-葡萄糖苷、槲皮素-3-O-β-d-葡萄糖基-(6→1)-α-l-鼠李糖苷、槲皮素-3-O-α-l-鼠李糖苷、槲皮素-3-O-α-l-鼠李糖基-7-O-β-d-葡萄糖苷和山奈酚)。原小檗碱对 AGS、MDA-MB-231 和 MCF-7 细胞具有中等细胞毒性,IC50 值范围为 69.8-197.3 μM。二十四烷对 AGS、MDA-MB-231、HT-29 和 NIH 3T3 细胞具有一定的细胞毒性,IC50 值范围为 128.7->250 μM。原小檗碱和二十四烷在 24 h 内对 AGS 细胞表现出凋亡作用(10%),48 h 后增加至(20%),与阳性对照环磷酰胺相当,如果不比环磷酰胺更强。

结论

除槲皮素-3-O-β-d-葡萄糖苷和山奈酚外,本研究首次从该植物中分离出这些化合物,并对其细胞毒性进行了评价。结果表明,该植物具有作为生物活性化合物来源的潜力,为其在消化性溃疡治疗中的传统应用提供了依据。

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