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Hemisynthesis and evaluation of pharmacological activities of carvacrolderivatives

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Title Hemisynthesis and evaluation of pharmacological activities of carvacrolderivatives
 
Creator Jaafari, Abdeslam
Lekchiri, Souad
Tilaoui, Mounir
Oukerrou, Moulay Ali
Rakib, El Mostapha
Mouse, Hassan Ait
 
Subject Antibacterial
Carvacrol
Cytotoxicity
Hemi-synthesis
NMR analysis
 
Description 537-542
Hemi-synthesis, a process widely used in pharmacological research, consists of a modification in the chemical structure
of a natural product in order to improve its activity and/or to reduce its side effects. Two carvacrol-derivatives (P1 and P2)
have been synthetized using reactions of alkylation by binding alkan groups at the hydroxyl group of carvacrol. NMR
analysis was performed for synthetized derivatives to confirm the success of the reactions. Then, cytotoxic activity, against
two tumour cell lines (P-815 and MCF-7), and antibacterial activity of carvacrol, P1 and P2 were performed. Cytotoxicity
was measured using the colourimetric methyl tetrazolium test (MTT) and antimicrobial activity was measured using the
diffusion technique on solid media and the determination of CMI on liquid media. Our results show that chemical
modifications made on carvacrol have no effect on its antitumor activity. However, an important decrease of its antibacterial
activity was observed, especially for P1. Our results suggest that hydroxyl group at this position of the molecule may be
responsible for carvacrol antibacterial activity, while the other parts of the molecule may be responsible for its antitumor
activity. On the other hand, introduced modifications may affect mechanism of action of the molecules as well as its
pharmacokinetics properties.
 
Date 2023-02-01T09:22:56Z
2023-02-01T09:22:56Z
2023-02
 
Type Article
 
Identifier 0976-0512 (Online); 0976-0504 (Print)
http://nopr.niscpr.res.in/handle/123456789/61318
https://doi.org/10.56042/ijnpr.v13i4.33049
 
Language en
 
Relation A61K 36/00
A61P 31/00
A61P 31/04
A61P 35/00
 
Publisher NIScPR-CSIR,India
 
Source IJNPR Vol.13(4) [December 2022]