PHARMACOLOGICAL AND ANTIMICROBIAL STUDIES OF SCHIFF is BASE COMPLEXES.

Synopsis of the Project Report of UGC Sponsored Minor Research Project

 

Principal Investigator

Dr. V M. Pai,

Associate  Professor in Chemistry, 

Dr. A.V.BALIGA COLLEGE OF ARTS AND SCIENCE,

KUMTA – 581 343,

 

F.No: MRP(S)-234 /08-09/KAKA087/UGC- SWRO

Date : 30-03-2009

 

Project Title

PHARMACOLOGICAL AND ANTIMICROBIAL STUDIES OF SCHIFF is BASE COMPLEXES.

The co ordination compounds were found to exhibit a wide range of pharmacological and antimicrobial properties. This has been documented in the literature. The Schiff bases in particular possess antimicrobial, antifungal activities. Some of them even possess anticancer properties. In the Schiff bases the metal complexes are found to possess greater pharmacological and antimicrobial activities. In this context the metal complexes of the Sciff bases were prepared and studied.

The hydrozones form a class of Schiff bases which show antibacterial properties. Hence Oxaloanilic acid hydrozones and substituted hydrazones were selected as ligands. The Copper, Cobalt and Nickel were selected as metals as the complexes of these metal were found to be active.

Thus Oxalonilic acid hydrozones were condensed with Copper, Cobalt and Nickel salts to prepare the complexes.

The complexes were characterized by elemental analyses, conductance measurements, magnetic moment measurements, infra red spectra and electronic spectra. The complexes were found to have 1:2 metal : ligand stichiometry.

Antimicrobail and Pharmacological Activities of ligands and complexes:

It was well established the biological activity of the organic molecules is enhanced by complexation. This can be attributed to the fact that anti-bacterial and antifungal agents exert these toxic effects on microorganisms through chelation. This has been shown by many workers. Mohan et al have screened the metal complexes obtained by condensation of 3 and 3/ substituted salicyaldehydes with benzylhydrazones. Fe(II), Ni(II), Co(II), Zn(II) and Pt(IV) complexes were found to be active against P388 lumphocyatic leukemia in mice. 

The Cu(II), Co(II) and Ni(II) complexes with hydrazones were tested for antibacterial activity. The bacterias used for screening were Sallomonella typhhi, Bascillus substilis, Streptococus aureus and Vibro cholera. The tests were made by the cup plate method at Biogenics, Hubli. The zone of inhibition was measured by millimeters.

It is observed in all complexes that the complexes were found to have greater antimicrobial activity than the respective ligands. However none of the complexes were found to have very large antibacterial activity so that they can be studied extensively.

The antifungal evalution was done using fungi Aspergillus niger and Candida albacans. The zone of inhibition of the ligands and their corresponding complexes were measured. It was found that the antifungal activity of ligands enhances with complexes. Among the complexes th copper complexes were found to have greater antifungal activity than corresponding Cobal and Nickel complexes.

The antioxidant properties of the representative complexes were studied at various concentrations. The values obtained indicated that the complexes under study do not possess sufficient anti-oxidant properties to be considered for the further studies.

The ligands and complexes were studied for Hyaluronidase inhibition activity.

*The assay was performed according to methods suggested by Ling et al (2003) and Sigma Protocol.

* The assay medium consisting of 3-5 U Hyauronidase (from Sigma – Aldrich, Bangalore) in 100 microlitre, 200 mM Sodium Phosphate buffer pH 7.0 with 77 mM Sodium Chloride, 0.01% BSA was preincubated with different concentrations of the test compound (in Dimethyl sulfoxide) for 15 minutes at 37oC.  

* The assay was commnesed by adding 100 micro litre hyaluronic acid, (0.03% in 300 mM sodium phosphate, pH 5.35 ) to the incubation mixture and incubated for a further 45 minutes at 37oC.

*The undigested hyaluronic acid was precipitated with 1 ml acid albumin solution made up of 0.1% bovine serum albumin in 24 mM sodium acetate and 79 mM acetic acid (pH 3.75)

*After standing at room temperature for 10 minutes the absorbance of the reaction mixture was measured at 600 nm.

* The absorbance in the absence of enzyme was used as the reference value for the maximum inhibition.

* The inhibitory activity of test compound was calculated as the percentage ration of the absorbance in the presence of test compound verses absorbance in the absence of enzyme. *The enzyme activity was checked by control experiment run simultaneously in which the enzyme was prencubated in 5 micro litre DMSO instead and followed by the assay procedures described above.

* Compounds were tested in a range on 10 micro gram to 100 micro gram in the reaction mixture.

* Indomethacin was used as reference standard.

The results obtained suggests the complexes possess moderate hyaluronidase inhibition activity.

The said work is done by me with my co worker Dr. G. T. Kuchind. Since the methods required the help of sophisticated instruments which were only available at University. Biological and Pharmacological procedures were very long and time consuming, the time allotted was not enough to submit the report in time. The delay may be excused.

The aim was to study the biological and pharmacological activity and if the complexes Since coplexes does not show remarkable antimicrobial and pharmacological properties, the findings can just be used as addition to the knowledge. Thus aim of the project according to me achieved.

 


 

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