Mallick Md Nasar, Singh Mhaveer, Parveen Rabea, Khan Washim, Ahmad Sayeed, Zeeshan Najm Mohammad, Husain Syed Akhtar
Bioactive Natural Product Laboratory, Department of Pharmacognosy and Phytochemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi 110062, India ; Human Genetics Laboratory, Department of Bioscience, Jamia Millia Islamia, New Delhi 110025, India.
Bioactive Natural Product Laboratory, Department of Pharmacognosy and Phytochemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi 110062, India.
Biomed Res Int. 2015;2015:513875. doi: 10.1155/2015/513875. Epub 2015 Oct 18.
Hydroalcoholic extract of Picrorhiza kurroa and its fractions were subjected to in vitro screening for cytotoxicity; further best active fraction (BAF) obtained was tested against Ehrlich ascites carcinoma (EAC) model in Balb/c mice after its quality control analysis.
Cytotoxicities of all the fractions and mother extract of P. kurroa were determined, using MTT assay on breast cancer (MCF-7, MDA-MB 231) and cervical cancer (HeLa, SiHa) cell lines. Metabolic fingerprinting was developed using HPTLC with quantification of biomarkers (cucurbitacins B and E; betulinic acid; picrosides 1 and 2; and apocynin) in BAF. The EAC tumor-bearing mice were used for in vivo anticancer activity after oral administration (50 mg Kg(-1)) for 10 days.
Cytotoxicity assay of mother extract and its fractions over breast cancer and cervix cancer cell lines showed that dichloromethane (DCM) fraction was most cytotoxic (IC50 36.0-51.0 µg mL(-1) at 72 h). Oral administration of DCM fraction showed significant reduction in tumor regression parameters, viable tumor cell count and restoration of hematological parameters may be due to presence of cucurbitacins B and E; betulinic acid; picrosides 1 and 2; and apocynin, as compared to the untreated mice of the control group.
The DCM fraction of P. kurroa displayed potent anticancer activity and can be further explored for the development of a potential candidate for cancer therapy.
对胡黄连水醇提取物及其各馏分进行体外细胞毒性筛选;对获得的最佳活性馏分(BAF)进行质量控制分析后,在Balb/c小鼠的艾氏腹水癌(EAC)模型上进行测试。
使用MTT法对乳腺癌(MCF-7、MDA-MB 231)和宫颈癌(HeLa、SiHa)细胞系测定胡黄连所有馏分和母提取物的细胞毒性。采用高效薄层层析法(HPTLC)对BAF中的生物标志物(葫芦素B和E、桦木酸、胡黄连苷1和2以及白杨素)进行定量,建立代谢指纹图谱。将荷EAC肿瘤的小鼠口服给药(50 mg Kg(-1))10天后用于体内抗癌活性研究。
母提取物及其馏分对乳腺癌和宫颈癌细胞系的细胞毒性试验表明,二氯甲烷(DCM)馏分的细胞毒性最强(72小时时IC50为36.0 - 51.0 µg mL(-1))。与对照组未处理的小鼠相比,口服DCM馏分可使肿瘤消退参数、存活肿瘤细胞计数显著降低,并使血液学参数恢复,这可能归因于其中存在葫芦素B和E、桦木酸、胡黄连苷1和2以及白杨素。
胡黄连的DCM馏分具有强大的抗癌活性,可进一步探索开发一种潜在的癌症治疗候选药物。