INTRODUCTION:

Cholic acid, a main bile acid, is a biosurfactant involved in the digestion of dietary lipids .It is commercially available at low cost. Furthermore, it has an unusual molecular structure with some special characteristics, such as the facial amphiphilicity. The carboxylic acid and three hydroxylic groups can act as synthesis handles. For these reasons cholic acid is a suitable building block for new functional molecules.

Cholic acid, a natural biodetergent has been reported to exhibited antibacterial^11-14, antiviral⁵, antifungal⁴, antimalarial¹⁰ , antitubercular¹⁰, anticancer⁹, spermicidal^{2, 3} , antiallergic ^6,7,8 etc. Since cholic acid is a suitable building block for new molecules or in other words, it is a lead compound for the development of various compounds, therefore, it is thought worthwhile to select it for the above research work.

The antimicrobial activity of metal chelates was found to be in the order¹:

Cd II>Ni II >Mn II >Cu II >Zn II >Co II >Fe II

Cholic acid is one of the lead molecule for preparing organometallic complexes and their complexes were found to have more active antifungal activity because of synergistic effect of cholic acid as well as metal ions.

EXPERIMENTAL:

This method was carried out to estimate the effect of test compound on the growth of tumor cells. The human breast cancer cells lines (MCF-7) were employed. The human breast cancer cell line (MCF-7) and mammary cancer cell line (EVSA-7), were co-incubated with the test compounds at 1 µg/mL doses for 96 hrs and the cell growth count was measured by MTT assay¹⁵. The basic principle involved in this assay depends upon the reduction of tetrazoleum salt. The yellow colored tetrazoleum MTT, [3-(4, 5-dimethylthiazol-2-yl)-2, 5,-diphenyltetrazoleumbromide] is reduced by metabolically active cells in part by the action of dehydrogenase enzymes to generate reducing equivalents such as NADH and NADPH. The resulting intra cellular purple colour zones were solubilized and quantified by spectrophotometer method. The MTT was dissolved in PBS (Phosphate Buffer Saline) at a concentration of 5 mg/ml. Then 50 µL of the MTT solution was added to each well of the 96 well culture plates, containing the 100 µL culture along with test compound and incubated at 37oC for 4 hrs. The medium was then removed carefully without disturbing the purple colored crystals. Then, 50 mL of dimethylsulfoxide (DMSO) was added to each well and mixed thoroughly to dissolve the crystals. The plates were then read on ELISA plate reader at a wavelength of 570 nm. The readings were presented as optical density/cell count.

RESULT AND DISCUSSION:

This activity was carried out to estimate the effect of test compound on the growth of tumor cells. The human breast cancer cell line (MCF-7) and mammary cancer cell line (EVSA-7) were employed. Their results are summarized in Table 1 respectively. All compounds except BSN-I and CDN-XII exhibits good result against human breast cancer cells lines (MCF-7) and all compounds except BSN-I show good results against mammary cancer cell line (EVSA-7).

Table-1: Anticancer Activity of Organometallic Complexes of Cholic Acid

Compound Code	Cell No.×10⁴(EVSA-7)	Cell No.×10⁴ (MCF-7)
BSN-I	11.74±1.22	12.34±1.05
CN-II	9.17±0.87	8.22±0.42
ZA-III	9.69±0.92	8.28±0.46
MCL-IV	9.69±0.92	9.17±0.87
NA-V	9.25±0.86	9.66±0.90
MA-VI	9.66±0.90	9.34±0.65
CCL-VII	9.34±0.65	9.17±0.87
AN-VIII	9.89±0.85	9.67±0.92
LA-IX	8.22±0.42	9.25±0.86
CON-X	9.69±0.92	9.34±0.65
BN-XI	8.28±0.46	9.89±0.85
CDN-XII	10.68±1.08	11.69±1.02
CUA-XIII	9.17±0.90	9.17±0.90
CUS-XIV	8.79±0.52	9.17±0.87
CA	9.66±0.90	9.89±0.85
Positive control	10.23±1.03	10.21±1.01
Negative control	42.24±4.22	40.26±3.23

Positive control=17β estradiol

Negative control =Culture medium only

CONCLUSION:

All the organometallic complexes of cholic acid except BSN-I exhibited more anticancer activity than standard i.e 17β estradiol due to synergistic effect of cholic acid as well as metal ions.

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Received on 03.04.2011 Modified on 05.04.2011

Asian J. Research Chem. 4(5): May, 2011; Page 695-696