Antimicrobial, Antitumor and Side Effects Assessment of a Newly Synthesized Tamoxifen Analog.
Animals
Anti-Bacterial Agents
/ adverse effects
Antineoplastic Agents
/ adverse effects
Body Weight
/ drug effects
Cell Proliferation
/ drug effects
Cell Survival
/ drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Escherichia coli
/ drug effects
Humans
Listeria monocytogenes
/ drug effects
MCF-7 Cells
Mice
Microbial Sensitivity Tests
Molecular Structure
Staphylococcus aureus
/ drug effects
Structure-Activity Relationship
Tamoxifen
/ analogs & derivatives
1;1-bis[4-(3-dimethylaminopropoxy)phenyl]-2-phenyl-but-1-ene dihydrochloride
Antimicrobial
activity
Antitumor
Mice
Tamoxifen citrate
Toxicity
Journal
Current topics in medicinal chemistry
ISSN: 1873-4294
Titre abrégé: Curr Top Med Chem
Pays: United Arab Emirates
ID NLM: 101119673
Informations de publication
Date de publication:
2020
2020
Historique:
received:
28
06
2020
revised:
20
07
2020
accepted:
20
07
2020
pubmed:
21
8
2020
medline:
1
7
2021
entrez:
21
8
2020
Statut:
ppublish
Résumé
Tamoxifen citrate is a very prevalent drug marketed under several trade names like Apo-Tamox, Nolvadex, Tamec, Tamizam, and Tamoplex. This molecule is approved by the FDA for breast cancer treatment. Some studies have shown that tamoxifen has anti-tuberculosis and antiparasitic activities. Like any drug, tamoxifen possesses side effects, more or less dangerous. Basically, this work is a comparative study that aims to: primarily compare the antimicrobial and antitumor activities of tamoxifen and a newly synthesized tamoxifen analog; and to determine the molecule with lesser side effects. Three groups of mice were injected with tamoxifen citrate and compound 2(1,1-bis[4-(3- dimethylaminopropoxy)phenyl]-2-phenyl-but-1-ene dihydrochloride) at doses corresponding to C1 (1/10), C2 (1/50), and C3 (1/100) to compound 2 lethal dose (LD50 = 75 mg/kg) administered to adult mice. A group of noninjected mice served as a study control. Experimental results suggest that compound 2 has better antitumor and antimicrobial activity than tamoxifen citrate besides its lower toxicity effects. The results obtained from the present study confirmed the antitumor and antimicrobial effect of tamoxifen citrate and its hematological side effects. Compound 2 seems to be more effective than tamoxifen citrate for antitumor and antimicrobial treatment while having less hematological side effects and less disruption of the blood biochemical parameters. These findings encourage us to perform further studies on compound 2 and test it for other therapeutic uses for which tamoxifen was found effective.
Sections du résumé
BACKGROUND
Tamoxifen citrate is a very prevalent drug marketed under several trade names like Apo-Tamox, Nolvadex, Tamec, Tamizam, and Tamoplex. This molecule is approved by the FDA for breast cancer treatment. Some studies have shown that tamoxifen has anti-tuberculosis and antiparasitic activities. Like any drug, tamoxifen possesses side effects, more or less dangerous.
AIMS
Basically, this work is a comparative study that aims to: primarily compare the antimicrobial and antitumor activities of tamoxifen and a newly synthesized tamoxifen analog; and to determine the molecule with lesser side effects.
METHODS
Three groups of mice were injected with tamoxifen citrate and compound 2(1,1-bis[4-(3- dimethylaminopropoxy)phenyl]-2-phenyl-but-1-ene dihydrochloride) at doses corresponding to C1 (1/10), C2 (1/50), and C3 (1/100) to compound 2 lethal dose (LD50 = 75 mg/kg) administered to adult mice. A group of noninjected mice served as a study control.
RESULTS
Experimental results suggest that compound 2 has better antitumor and antimicrobial activity than tamoxifen citrate besides its lower toxicity effects.
CONCLUSION
The results obtained from the present study confirmed the antitumor and antimicrobial effect of tamoxifen citrate and its hematological side effects. Compound 2 seems to be more effective than tamoxifen citrate for antitumor and antimicrobial treatment while having less hematological side effects and less disruption of the blood biochemical parameters. These findings encourage us to perform further studies on compound 2 and test it for other therapeutic uses for which tamoxifen was found effective.
Identifiants
pubmed: 32814527
pii: CTMC-EPUB-109301
doi: 10.2174/1568026620666200819145526
doi:
Substances chimiques
Anti-Bacterial Agents
0
Antineoplastic Agents
0
Tamoxifen
094ZI81Y45
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
2281-2288Informations de copyright
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