灌木海桑表现出抗氧化和细胞毒性活性，通过诱导细胞凋亡和 G2/M 细胞周期阻滞。
Dillenia suffruticosa exhibited antioxidant and cytotoxic activity through induction of apoptosis and G2/M cell cycle arrest.
机构信息
Laboratory of Molecular Biomedicine, Institute of Bioscience, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia.
出版信息
J Ethnopharmacol. 2013 Mar 27;146(2):525-35. doi: 10.1016/j.jep.2013.01.017. Epub 2013 Jan 23.
ETHNOPHARMACOLOGICAL RELEVANCE
Dillenia suffruticosa (Family: Dilleniaceae) locally known as Simpoh air has been reported to be used traditionally to treat cancerous growth. Therefore, the present study was attempted to investigate the antioxidant and cytotoxic properties of different parts (root, flower, fruit and leaf) of D. suffruticosa extracts.
METHODS AND MATERIALS
In this study, direct solvent extraction (aqueous and methanol) from different parts of D. suffruticosa (root, flower, fruit and leaf) were carried out. Antioxidant activities of D. suffruticosa extract were determined by using DPPH, ABTS FRAP and β-carotene bleaching assays. Cytotoxicity and cell cycle arrest of the active extract were determined using MTT assay and flow cytometer, respectively. Sequential solvent extraction (hexane, DCM, EtOAc, and MeOH) were also carried out in root of D. suffruticosa to further evaluate the antioxidant and cytotoxic activity of the different solvent extracts.
RESULTS
Methanol (MeOH) root extract showed the highest TPC, antioxidant and cytotoxic activities (especially towards HeLa) compared to others (P<0.05). Based on the results, sequential solvent extraction (hexane, DCM, EtOAc and MeOH) was carried out in the roots of D. suffruticosa. MeOH extract exhibited the highest antioxidant activities among others and significantly correlated (P<0.05) with TPC, suggesting the important contribution of phenolic compounds to its antioxidant activity. On the other hand, the DCM and EtOAc exhibited higher cytotoxic activity to selected cancer cells (HeLa, MCF-7, MDA-MB-231, A549 and HT29) compared to others. In short, there is no established correlation between antioxidant and cytotoxic activities of D. suffruticosa extracts indicating that an agent with high antioxidant activities will not necessarily possesses good cytotoxic activities in return. Qualitative phytochemical screening of D. suffruticosa extracts suggested the presence of saponins, triterpenes, sterols, and polyphenolic compounds which are believed to contribute to the cytotoxic activities.
CONCLUSION
It is suggested that the cytotoxicity of the active extracts in HeLa was due to the induction of apoptosis and cell cycle arrest at G2/M.
民族药理学相关性
本地称为 Simpoh air 的杜茎山（杜茎山科）已被报道传统上用于治疗癌性生长。因此，本研究试图研究杜茎山不同部位（根、花、果和叶）提取物的抗氧化和细胞毒性特性。
方法和材料
在这项研究中，直接溶剂提取（水和甲醇）来自杜茎山的不同部位（根、花、果和叶）。通过 DPPH、ABTS FRAP 和β-胡萝卜素漂白测定法测定杜茎山提取物的抗氧化活性。使用 MTT 测定法和流式细胞仪分别测定活性提取物的细胞毒性和细胞周期停滞。还对杜茎山的根进行了连续溶剂提取（己烷、DCM、EtOAc 和 MeOH），以进一步评估不同溶剂提取物的抗氧化和细胞毒性活性。
结果
与其他部位（P<0.05）相比，甲醇（MeOH）根提取物表现出最高的总酚含量、抗氧化和细胞毒性活性（尤其是对 HeLa）。基于这些结果，对杜茎山的根进行了连续溶剂提取（己烷、DCM、EtOAc 和 MeOH）。MeOH 提取物在其他提取物中表现出最高的抗氧化活性，与 TPC 显著相关（P<0.05），表明酚类化合物对其抗氧化活性的重要贡献。另一方面，DCM 和 EtOAc 对选定的癌细胞（HeLa、MCF-7、MDA-MB-231、A549 和 HT29）的细胞毒性高于其他提取物。简而言之，杜茎山提取物的抗氧化和细胞毒性活性之间没有建立明确的相关性，这表明具有高抗氧化活性的药物不一定会反过来具有良好的细胞毒性活性。杜茎山提取物的定性植物化学筛选表明存在皂苷、三萜、甾体和多酚化合物，这些化合物被认为有助于细胞毒性。
结论
建议活性提取物在 HeLa 中的细胞毒性是由于诱导细胞凋亡和细胞周期停滞在 G2/M 期。
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