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鸡蛋花（夹竹桃科）的抗增殖活性。

Antiproliferative activity of Vallaris glabra Kuntze (Apocynaceae).

作者信息

Wong Siu Kuin, Lim Yau Yan, Ling Sui Kiong, Chiang Chan Eric Wei

机构信息

School of Science, Monash University Sunway Campus, Bandar Sunway, 46150 Petaling Jaya, Selangor, Malaysia.

Natural Products Division, Forest Research Institute Malaysia, Kepong, 52109 Selangor, Malaysia.

出版信息

Pharmacogn Mag. 2014 Apr;10(Suppl 2):S232-9. doi: 10.4103/0973-1296.133238.

DOI:10.4103/0973-1296.133238
PMID:24991097
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4078344/
Abstract

BACKGROUND

Our earlier study on the antiproliferative (APF) activity of leaf extracts of ten Apocynaceae species showed that leaves of Vallaris glabra possessed strong and broad-spectrum properties.

MATERIALS AND METHODS

In this study, sequential extracts of leaves, flowers and stems, and fractions and isolated compounds from dichloromethane (DCM) leaf extract of V. glabra were assessed for APF activity using the sulphorhodamine B (SRB) assay. Apoptotic effect of MDA-MB-231 cancer cells treated with DCM leaf extract of V. glabra was studied using Hoechst 33342 dye and caspase colorimetry.

RESULTS

Both DCM extracts of leaves and flowers possessed broad-spectrum APF activity against HT-29, MCF-7, MDA-MB-231 and SKOV-3 cancer cells. From DCM leaf extract, stearic acid (SA) and ursolic acid (UA) were isolated by column chromatography, and identified by NMR and MS analyses. APF activity of SA from DCM leaf extract displayed weak inhibitory activity and scientific literature showed UA has anticancer properties against those cancer cells used in this study. MDA-MB-231 cancer cells treated with DCM leaf extract and stained with Hoechst 33342 dye provided evidence that the extract had an apoptotic effect on the cells. Caspase colorimetry showed that the apoptotic effect involved activation of caspase-8, -9 and -3, but not caspase-6.

CONCLUSION

The potential of V. glabra as a candidate species for anticancer drugs warrants further investigation.

摘要

背景

我们早期对十种夹竹桃科植物叶提取物的抗增殖（APF）活性研究表明，光叶瓦拉瑞亚的叶子具有强大且广谱的特性。

材料与方法

在本研究中，使用磺酰罗丹明B（SRB）测定法评估了光叶瓦拉瑞亚叶、花和茎的序贯提取物，以及二氯甲烷（DCM）叶提取物的馏分和分离化合物的APF活性。使用Hoechst 33342染料和半胱天冬酶比色法研究了用光叶瓦拉瑞亚DCM叶提取物处理的MDA - MB - 231癌细胞的凋亡作用。

结果

叶和花的DCM提取物对HT - 29、MCF - 7、MDA - MB - 231和SKOV - 3癌细胞均具有广谱APF活性。通过柱色谱从DCM叶提取物中分离出硬脂酸（SA）和熊果酸（UA），并通过NMR和MS分析进行鉴定。DCM叶提取物中SA的APF活性表现出较弱的抑制活性，科学文献表明UA对本研究中使用的那些癌细胞具有抗癌特性。用DCM叶提取物处理并用Hoechst 33342染料染色的MDA - MB - 231癌细胞提供了证据，表明该提取物对细胞具有凋亡作用。半胱天冬酶比色法表明凋亡作用涉及半胱天冬酶 - 8、 - 9和 - 3的激活，但不涉及半胱天冬酶 - 6。

结论

光叶瓦拉瑞亚作为抗癌药物候选物种的潜力值得进一步研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7927/4078344/7b6ba3da85d7/PM-10-232-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7927/4078344/6db1f646d215/PM-10-232-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7927/4078344/3be2c9eb0a6d/PM-10-232-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7927/4078344/7b6ba3da85d7/PM-10-232-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7927/4078344/6db1f646d215/PM-10-232-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7927/4078344/3be2c9eb0a6d/PM-10-232-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7927/4078344/7b6ba3da85d7/PM-10-232-g005.jpg

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本文引用的文献

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Ursolic acid from Oldenlandia diffusa induces apoptosis via activation of caspases and phosphorylation of glycogen synthase kinase 3 beta in SK-OV-3 ovarian cancer cells.熊果酸诱导 SK-OV-3 卵巢癌细胞凋亡与半胱氨酸天冬氨酸蛋白酶激活及糖原合成激酶 3β磷酸化有关
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Induction of apoptotic cell death by ursolic acid through mitochondrial death pathway and extrinsic death receptor pathway in MDA-MB-231 cells.
熊果酸通过线粒体死亡途径和外在死亡受体途径诱导 MDA-MB-231 细胞凋亡。
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