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青葙(苋科)抗癌原理的表征

Characterization of Anticancer Principles of Celosia argentea (Amaranthaceae).

作者信息

Rub Rukhsana A, Pati Manohar J, Siddiqui Areej A, Moghe Alpana S, Shaikh Nasreen N

机构信息

Department of Pharmacognosy, M.C.E. Society's Allana College of Pharmacy, Camp, Pune, Maharashtra, India.

Department of Pharmacognosy, MMM's College of Pharmacy, Pimpri, Maharashtra, India.

出版信息

Pharmacognosy Res. 2016 Apr-Jun;8(2):97-104. doi: 10.4103/0974-8490.172659.

DOI:10.4103/0974-8490.172659
PMID:27034599
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4780145/
Abstract

BACKGROUND

An Indian origin, Celosia argentea is a weed growing during rainy season traditionally claimed for treating several ailments. Early researches on C. argentea were focused on the anti-cancer screening of seeds, with few reports on aerial parts.

OBJECTIVE

To isolate and characterize bioactive compounds of aerial parts of C. argentea and evaluate their anticancer potential.

MATERIALS AND METHODS

The methanolic aerial part extract was fractionated on column chromatography using chloroform: methanol mixture. The fractions; 80:20 and 95:5 were purified on MCI-HP20 HPLC column. Chromatographically pure compounds were pooled, concentrated and characterized spectroscopically. The compounds were further screened for anti-oxidant and cytotoxic potential.

RESULTS

Isolated compounds were confirmed as: (1) Luteolin-7-O-glucoside and (2) phenolic, 1-(4-hydroxy-2-methoxybenzofuran-5-yl)-3-phenylpropane-1,3-dione. Both exhibited significant antioxidant potential with IC50 values of 20.80 and 21.30 μg/ml for 2,2-diphenyl-1-picrylhydrazyl assay (***P < 0.001) and significant Trolox equivalent antioxidant capacity (TEAC) values for 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (*P < 0.05) and ferric reducing antioxidant potential assay (****P < 0.0001). In 3(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazoliumbromide assay, Compound 1 and 2 showed potent cytotoxicity against SiHa, HCT, MCF-7 cancer cell lines at 20 μg/ml (****P < 0.0001) and 18 μg/ml (**P < 0.01), respectively, without affecting the normal Vero cells. Both compounds enabled maximum reduction in cell viability at 50 μg/ml against HT-29 (***P < 0.001) and MCF-7 cell lines (**P < 0.01) in try pan blue viability assay. Apoptosis occurred at concentrations of 47.33 ± 0.8 μg/ml and 56.28 ± 1.2 μg/ml for Compound 1 and 35.15 ± 0.4 μg/ml and 28.05 ± 0.3 μg/ml for Compound 2 for HT-29 and MCF-7 respectively.

CONCLUSION

A novel anticancer phenolic compound; (1-(4-hydroxy-2-methoxybenzofuran-5-yl)-3-phenylpropane-1,3-dione), isolated from aerial parts of C. argentea was a valuable finding of the research.

SUMMARY

The present study validated the potential of the plant C. argentea as an antioxidant, and anticancer remedy with two valuable isolations. Although one of them is a known compound: Luteolin 7-0 glycoside, the other isolated phenolic compound;-{1-(4-hydroxy-2-methoxybenzofuran-5-yl)-3-phenylpropane-1,3-dione}, is the first to be reported and thus can be considered as a valuable outcome of this research work.

摘要

背景

鸡冠花原产于印度,是一种在雨季生长的杂草,传统上认为它可治疗多种疾病。早期对鸡冠花的研究主要集中在种子的抗癌筛选上,关于地上部分的报道较少。

目的

分离并鉴定鸡冠花地上部分的生物活性化合物,并评估其抗癌潜力。

材料与方法

采用氯仿 - 甲醇混合液对甲醇提取的地上部分提取物进行柱色谱分离。将80:20和95:5的馏分在MCI - HP20高效液相色谱柱上纯化。将色谱纯的化合物合并、浓缩并进行光谱表征。进一步筛选这些化合物的抗氧化和细胞毒性潜力。

结果

分离得到的化合物经确认分别为:(1)木犀草素 - 7 - O - 葡萄糖苷和(2)酚类化合物1 - (4 - 羟基 - 2 - 甲氧基苯并呋喃 - 5 - 基) - 3 - 苯基丙烷 - 1,3 - 二酮。在2,2 - 二苯基 - 1 - 苦基肼测定中,二者均表现出显著的抗氧化潜力,IC50值分别为20.80和21.30 μg/ml(***P < 0.001);在2,2'- 联氮 - 双 - (3 - 乙基苯并噻唑啉 - 6 - 磺酸)测定中,二者具有显著的Trolox等效抗氧化能力(TEAC)值(*P < 0.05);在铁离子还原抗氧化能力测定中,二者也表现出显著的能力(****P < 0.0001)。在3 - (4,5 - 二甲基噻唑 - 2 - 基) - 2,5 - 二苯基溴化四氮唑测定中,化合物1和2分别在20 μg/ml(****P < 0.0001)和18 μg/ml(**P < 0.01)时对SiHa、HCT、MCF - 7癌细胞系显示出强大的细胞毒性,且不影响正常的Vero细胞。在台盼蓝细胞活力测定中,两种化合物在50 μg/ml时对HT - 29和MCF - 7细胞系均能使细胞活力最大程度降低(*P < 0.001和P < 0.01)。对于HT - 29和MCF - 7细胞系,化合物1在浓度为47.33 ± 0.8 μg/ml和56.28 ± 1.2 μg/ml时诱导凋亡,化合物2在浓度为35.15 ± 0.4 μg/ml和28.05 ± 0.3 μg/ml时诱导凋亡。

结论

从鸡冠花地上部分分离得到的一种新型抗癌酚类化合物1 - (

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