Abstract:
Curcumin is a wonder molecule as it is used for prevention and cure of multiple diseases such as cancer, diabetes, inflammation, cataract, rheumatoid arthritis, HIV etc., However, it has not been possible so far to assign a definite drug profile because of low bioavailability, fast metabolism, poor adsorption, low solubility and lack of targeted delivery. Several bioconjugate of curcumin with amino acids and nucleotides have been prepared so far to overcome these limitations. In the present study the two new conjugates of curcumin have been synthesized by esterifying its phenolic group functions with nicotinic acid (vitamin B3) and its isomer picolinic acid viz. 1,7-bis (4-O-nicotinoyl-3-methoxyphenyl)-1, 6-heptadiene-3, 5-dione (2) and 1, 7-bis (4-O-picolinoyl-3-methoxyphenyl)-1, 6-heptadiene-3, 5-dione (4). These bioconjugate were evaluated for antibacterial activity against medically important gram positive cocci (Entercoccus faecium) and gram negative bacilli (Klebsiella pneumoniae, Escherichia coli and Pseudomonas aeruginosa). Antibacterial activity was performed by microdilution broth susceptibility method in vitro. Results demonstrated that both bioconjugates possess high antibiotic potential as evidenced by enhanced antibacterial activity in comparison to pure curcumin. On the basis of results it may concluded that lipophilic nature of these conjugates enhances the cellular uptake and may be better option for medicinal and pharmacological applications.
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