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对小细胞肺癌细胞系的细胞毒性活性以及从 Benjakul 的乙醇提取物中分离出的六种化合物的色谱指纹图谱

Cytotoxic activity against small cell lung cancer cell line and chromatographic fingerprinting of six isolated compounds from the ethanolic extract of Benjakul.

作者信息

Rattarom Ruchilak, Sakpakdeejaroen Intouch, Hansakul Pintusorn, Itharat Arunporn

出版信息

J Med Assoc Thai. 2014 Aug;97 Suppl 8:S70-5.

Abstract

BACKGROUND

Benjakul, a Thai traditional herbal preparation, comnprises five plants: Piper chaba, Piper sarmentosum, Piper interruptum, Plumbago indica, and Zingiber officinale. It has widely been used to treat cancer patients in folk medicine in Thailand. Benjakul extract, and its isolated compounds should be investigated for cytotoxic activity and analysis isolated compounds from chemical fingerprinting.

OBJECTIVE

To study cytotoxicity ofBenjakul extract and its isolatedpure compounds against human small cell lung cancer cell line (NCI-HI 688) and in normal human lungfibroblast cell line (MRC-5) and analysis the content ofisolated compounds for quality control of Benjakul extract.

MATERIAL AND METHOD

Bioassay-guided fractionation was used for isolated active compounds from ethanolic extract of Benjakul. Cytotoxic activity was carried using the SRB assay. HPLC method was applied to analyze six isolated compound contentfrom Benjakul extract.

RESULTS

The ethanolic extract ofBenjakul showed cytotoxicity against NCI-H1688 with IC50 value = 36.15±4.35 μg/ml. Hexane fraction as semi-separation by VLC showed the best cytotoxic activity (21.1 7±7.42 μg/ml). Six isolated compounds were identified as myristicin, plumbagin, methyl piperate, 6-shogaol, 6-gingerol and piperine. Plumbagin exhibited the highest cytotoxic activity and 6-shogaol was the second most effective cytotoxic constituent (IC50 values = 1.41±0.01 and 6.45±0.19 μg/ml, respectively). Piperine showed the highest content in both ofHPLC analysis and column chromatography separation.

CONCLUSION

Benjakul extract exhibited cytotoxicity against NCI-HI 688. Plumbagin and 6-shogaol are bioactive markers for cytotoxicity against this small cell lung cancer cell line. Chromatographic fingerprinting can be used to analyze six cytotoxic compounds isolatedfrom the ethanolic extract ofBenjakul.

摘要

背景

Benjakul是一种泰国传统草药制剂,由五种植物组成:长蒌叶胡椒、假蒌、间断胡椒、白花丹和姜。在泰国的民间医学中,它被广泛用于治疗癌症患者。应研究Benjakul提取物及其分离出的化合物的细胞毒性活性,并从化学指纹图谱中分析分离出的化合物。

目的

研究Benjakul提取物及其分离出的纯化合物对人小细胞肺癌细胞系(NCI-HI 688)和正常人肺成纤维细胞系(MRC-5)的细胞毒性,并分析分离出的化合物含量以控制Benjakul提取物的质量。

材料与方法

采用生物测定导向分馏法从Benjakul乙醇提取物中分离活性化合物。使用SRB法进行细胞毒性活性测定。采用HPLC法分析Benjakul提取物中六种分离出的化合物含量。

结果

Benjakul乙醇提取物对NCI-H1688显示出细胞毒性,IC50值 = 36.15±4.35 μg/ml。通过VLC进行半分离得到的己烷馏分显示出最佳的细胞毒性活性(21.17±7.42 μg/ml)。六种分离出的化合物被鉴定为肉豆蔻醚、白花丹素、胡椒酸甲酯、6-姜辣醇、6-姜酚和胡椒碱。白花丹素表现出最高的细胞毒性活性,6-姜辣醇是第二有效的细胞毒性成分(IC50值分别为1.41±0.01和6.45±0.19 μg/ml)。在HPLC分析和柱色谱分离中,胡椒碱的含量均最高。

结论

Benjakul提取物对NCI-HI 688显示出细胞毒性。白花丹素和6-姜辣醇是针对这种小细胞肺癌细胞系的细胞毒性生物活性标志物。色谱指纹图谱可用于分析从Benjakul乙醇提取物中分离出的六种细胞毒性化合物。

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