Cytotoxic activities of five compounds with high polarity in BT-474 breast cancer cell line by NRU and MTT assays

Nobiletin (NOB) is one of the polymethoxyflavones mainly found in citrus fruits. Aromatase or cytochrome P450 (CYP19) enzyme catalyzes the last and rate-limiting step in estrogen biosynthesis. This study was carried out to investigate the effect of NOB on the activity and expression of aromatase, and to compare this property with letrozole (LET) as aromatase inhibitor in the MCF-7 breast cancer cell line. Cell viability was assessed with 3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide (MTT) assays. Aromatase enzyme activity based on the conversion of androgenic substrate testosterone into 17β-estradiol was determined. CYP19 gene expression was measured by quantitative real-time PCR. MTT assays demonstrated that NOB at a concentration of 100 μmol/L decreased cell viability in a time-dependent manner (P < 0.05). NOB significantly inhibited aromatase at the concentration of 0.1 μmol/L (P = 0.013), whereas other concentrations had no effect. Treatment with 10 μmol/L and 1 μmol/L of NOB for 48 h significantly increased (P = 0.001) and decreased (P = 0.02) relative aromatase expression, respectively. The combination of LET and NOB had no effect on aromatase. This study showed for the first time that NOB decreases the activity and expression of aromatase at low concentrations in MCF-7 breast cancer cells.

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Cytotoxicity of Buah Merah (Pandanus conoideus Lamk.) Extract on Breast Cancer Cell Line (T47D)

Indonesian Journal of Biotechnology ◽

10.22146/ijbiotech.8636 ◽

2015 ◽

Vol 19 (1) ◽

pp. 71 ◽

Cited By ~ 1

Author(s):

Tri R. Nuringtyas ◽

Yoga Pratama ◽

G. Galih ◽

Subagus Wahyuono ◽

Sukarti Moeljopawiro

Keyword(s):

Breast Cancer ◽

Cell Line ◽

Cancer Cell ◽

Breast Cancer Cell ◽

Breast Cancer Cell Line ◽

Cancer Cell Line ◽

Cytotoxic Activities ◽

Active Compounds ◽

Ic50 Value ◽

Bioassay Guided Fractionation

Buah Merah (Pandanus conoideus Lamk.) has been extensively used to treat various diseases includingcancer. There are many varieties of buah merah and there was no scientifi c study comparing cytotoxicity ofdifferent varieties. The objective of this study was to investigate the cytotoxicity of three varieties of buah merahknown as Barugum, Maler and Yanggiru on breast cancer cell line (T47D). All samples were collected fromPapua, Indonesia. Each sample was extracted consecutively using three solvents chloroform, methanol andwater resulted to nine crude extracts. The cytotoxic activities were determined using MTT assay. The crudeextract showed the lowest IC50 was selected for further bioassay-guided fractionation. Fractionation was doneusing vacuum liquid chromatography coupled with preparative TLC to fi nd the active compounds. Severaldetection reagents were applied to TLC for identifi cation of the class of the potent compounds. The resultshowed that the potent extracts was obtained from Barugum methanol extract followed by Maler chloroformextract with IC50 value of 132.83 μg/ml and 139.72 μg/ml, respectively. All Yanggiru extracts did not showactivity. The bioassay-guided fractionation of Barugum and Maler extracts showed that the most potent fractioneluted by a mixture of hexane:ethyl acetate (75:25), was in Maler variety with IC50 value of 25,7 μg/ml, fourtimes higher than the most potent fraction of Barugum with IC50 value of 104,61 μg/ml. TLC analysis of themost potent fraction showed that the active compounds was class of terpene. Result of this study supportedthe utilization of buah merah Maler variety for breast cancer treatment.

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