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两种不同山竹分离物的生物活性比较。

Comparison of the biological activity of two different isolates from mangosteen.

作者信息

Moongkarndi Primchanien, Jaisupa Nattapon, Samer Jutima, Kosem Nuttavut, Konlata Julaporn, Rodpai Ekkarat, Pongpan Narongchai

机构信息

Department of Microbiology, Faculty of Pharmacy, Mahidol University, Bangkok, Thailand.

出版信息

J Pharm Pharmacol. 2014 Aug;66(8):1171-9. doi: 10.1111/jphp.12239. Epub 2014 Mar 19.

Abstract

OBJECTIVE

Mangosteen has been used in traditional medicine for treatment of many diseases. Recent studies have reported the active constituents isolated from this plant. In this study, purified α-mangostin, a major component and partially purified water-soluble fraction found in fruit pericarps, was carefully isolated, and their biological activity was compared, i.e. antioxidative activity and cytotoxic effect in breast cancer cells: SKBR3.

METHODS

Antioxidative activity was determined using the 1,1-diphenyl-2-picrylhydrazyl radicals (DPPH) assay and reactive oxygen species (ROS) assay, whereas the cytotoxic effect was evaluated by the MTT assay and morphological changes by fluorescence staining.

KEY FINDING

The DPPH scavenging capacities of α-mangostin and water-soluble extract were obtained, the IC50 at 183.95 and 54.57 μg/ml, respectively. Meanwhile, the intracellular ROS level was significantly decreased after treatment with α-mangostin and water-soluble extraction at 20 and 200 μg/ml, respectively. α-mangostin exhibited the cytotoxicity at ED50 8.21 μg/ml, while the water-soluble extract was non-toxic to cells at ED50 higher than 160 μg/ml. Both constituents showed antioxidative activity by chemical assay and in cells, but α-mangostin expressed strong cytotoxicity and showed apoptotic bodies.

CONCLUSION

The different isolated constituents would be further studied for future possible use as chemotherapy in cancer and chemoprevention in Alzheimer's disease.

摘要

目的

山竹在传统医学中用于治疗多种疾病。最近的研究报道了从该植物中分离出的活性成分。在本研究中,仔细分离了纯化的α-倒捻子素(一种主要成分,存在于水果果皮中的部分纯化的水溶性组分),并比较了它们的生物活性,即抗氧化活性和对乳腺癌细胞SKBR3的细胞毒性作用。

方法

使用1,1-二苯基-2-苦基肼自由基(DPPH)测定法和活性氧(ROS)测定法测定抗氧化活性,而通过MTT测定法评估细胞毒性作用,并通过荧光染色观察形态变化。

主要发现

获得了α-倒捻子素和水溶性提取物的DPPH清除能力,IC50分别为183.95和54.57μg/ml。同时,分别用20和200μg/ml的α-倒捻子素和水溶性提取物处理后,细胞内ROS水平显著降低。α-倒捻子素在ED50为8.21μg/ml时表现出细胞毒性,而水溶性提取物在ED50高于160μg/ml时对细胞无毒。两种成分通过化学测定法和在细胞中均表现出抗氧化活性,但α-倒捻子素表现出较强的细胞毒性并出现凋亡小体。

结论

对于这些不同的分离成分,未来有必要进一步研究其在癌症化疗和阿尔茨海默病化学预防中的潜在用途。

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