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鳄嘴花的细胞毒性和细胞色素P450抑制活性。

Cytotoxicity and cytochrome P450 inhibitory activities of Clinacanthus nutans.

作者信息

Quah Suk Yen, Chin Jin Han, Akowuah Gabriel Akyirem, Khalivulla Shaik Ibrahim, Yeong Siew Wei, Sabu Mandumpal Chacko

出版信息

Drug Metab Pers Ther. 2017 Mar 1;32(1):59-65. doi: 10.1515/dmpt-2016-0034.

DOI:10.1515/dmpt-2016-0034
PMID:28253196
Abstract

BACKGROUND

Clinacanthus nutans Lindau (family: Acanthaceae), also known as "Sabah Snake Grass" or "Belalai Gajah" in Malaysia, has been widely used by Malaysians due to its anticancer property. However, the anticancer activity of C. nutans leaves extract and its safe use need to be further investigated. The objectives of the present study were to evaluate the cytotoxic effects of methanol leaves extract of C. nutans in various human cancer cell lines and to evaluate the in vitro effect of C. nutans leaves on the activity of CYP3A4 and CYP2E1 in human liver microsomes.

METHODS

The cytotoxic effects of methanol extract of C. nutans leaves in various cancer cell lines (Hep-G2, A549, HT-29, MDA-MB-231, MCF-7, and CRL 1739) and normal cells (3T3) were determined using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cell proliferation assay. The activities of CYP3A4 and CYP2E1 were determined using simple spectrophotometric methods.

RESULTS

Results obtained showed that the methanol extract of C. nutans leaves exhibited the highest cytotoxic effect against Hep-G2 cell lines (liver cancer) (IC50=13.33 μg/mL), followed by breast cancer oestrogen negative (MDA-MB-231) (IC50 of 18.67 μg/mL). Methanol leaves extract of C. nutans showed significant inhibition (p<0.05) in CYP3A4 and CYP2E1 activity in human liver microsomes.

CONCLUSIONS

In conclusion, methanol leaves extract of C. nutans exhibited the highest cytotoxic activity against liver cancer cells (Hep-G2). There is a possibility that herb-drug interaction could occur with C. nutans through inhibitory effects on CYP3A4. Additionally, inhibition of C. nutans on CYP2E1 could show anti-carcinogenesis effects in human liver microsomes.

摘要

背景

鳄嘴花(Clinacanthus nutans Lindau,爵床科),在马来西亚也被称为“沙巴蛇草”或“马来接骨木”,因其抗癌特性而被马来西亚人广泛使用。然而,鳄嘴花叶提取物的抗癌活性及其安全使用仍需进一步研究。本研究的目的是评估鳄嘴花甲醇叶提取物对多种人类癌细胞系的细胞毒性作用,并评估鳄嘴花叶对人肝微粒体中CYP3A4和CYP2E1活性的体外影响。

方法

使用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐(MTT)细胞增殖试验测定鳄嘴花甲醇叶提取物对多种癌细胞系(Hep-G2、A549、HT-29、MDA-MB-231、MCF-7和CRL 1739)和正常细胞(3T3)的细胞毒性作用。使用简单的分光光度法测定CYP3A4和CYP2E1的活性。

结果

所得结果表明,鳄嘴花甲醇叶提取物对肝癌细胞系(Hep-G2)表现出最高的细胞毒性作用(IC50 = 13.33 μg/mL),其次是雌激素阴性乳腺癌(MDA-MB-231)(IC50为18.67 μg/mL)。鳄嘴花甲醇叶提取物对人肝微粒体中CYP3A4和CYP2E1活性表现出显著抑制作用(p<0.05)。

结论

总之,鳄嘴花甲醇叶提取物对肝癌细胞(Hep-G2)表现出最高的细胞毒性活性。鳄嘴花有可能通过对CYP3A4的抑制作用而发生草药-药物相互作用。此外,鳄嘴花对CYP2E1的抑制作用可能在人肝微粒体中显示出抗癌作用。

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