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1.
Biomed Res Int ; 2021: 4303902, 2021.
Article in English | MEDLINE | ID: mdl-34646883

ABSTRACT

The wound healing process is essential to reform the damaged tissue and prevent its invasion by pathogens. The present study aims at evaluating the antibacterial and therapeutic properties of the Capsicum annuum L. (Solanaceae) extract against infected wound in a rat model with its mechanisms of antibacterial action. The fruit extract was prepared by maceration in methanol. The broth microdilution method was used to investigate the antibacterial activity of the methanol extract of C. annuum fruits. The therapeutic effect of the extract gel was performed on an excision wound infected with Staphylococcus aureus using a rat model. The total phenol, flavonoid, and tannin contents as well as the antibacterial mechanisms of action of the extract were determined using spectrophotometric methods. The C. annuum fruit extract showed antibacterial properties which can be linked to its total phenolic, flavonoid, and tannin contents. The antibacterial activity is due to the inhibition of the biofilm formation, ATPases/H+ proton pump, and dehydrogenase activity as well as the alteration of the bacterial cell membrane through the leakage of nucleic acids, reducing sugars and proteins. The extract gel showed a significant (p < 0.05) increase in the percentage of wound closure and eradicated S. aureus at the infection site. The extract gel was nonirritating to the skin and slightly irritating to the eyes and should be used with caution. Overall, the findings of the present study support the traditional use of the studied plant in the treatment of wounds and infectious diseases associated with the tested bacteria.


Subject(s)
Anti-Bacterial Agents/therapeutic use , Capsicum/chemistry , Plant Extracts/therapeutic use , Wound Infection/drug therapy , Adenosine Triphosphatases/metabolism , Animals , Anti-Bacterial Agents/pharmacology , Bacteria/drug effects , Bacteria/enzymology , Biofilms/drug effects , Cell Membrane Permeability/drug effects , Disease Models, Animal , Electron Transport/drug effects , Eye/drug effects , Flavonoids/analysis , Fruit/chemistry , L-Lactate Dehydrogenase/metabolism , Male , Methanol/chemistry , Microbial Sensitivity Tests , Phenols/analysis , Plant Extracts/pharmacology , Proton Pumps/metabolism , Rats, Wistar , Skin/drug effects , Sugars/analysis , Tannins/analysis , Wound Infection/microbiology
2.
Acta Chim Slov ; 67(1): 203-211, 2020 Mar.
Article in English | MEDLINE | ID: mdl-33558912

ABSTRACT

A novel bismuth(III) complex with 2-amino-3-carbomethoxy-4,5,6,7-tetrahydrobenzo[b]thiophene (ACTT) as a ligand have been synthesized. The novel complex was characterized on the basis of its IR, NMR, elemental analysis and MS spectral data. It was found that the ligand behaves as a monodentate chelating agent and bonds to the metal ion through the nitrogen atom of the amino group to form the [BiIII(ACTT)6]Cl3 complex. The new complex compound displayed significant antimicrobial activity (MIC = 8-32 µg/mL) against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Shigella flexneri, Candida albicans, Candida tropicalis and Cryptococcus neoformans.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Coordination Complexes/pharmacology , Thiophenes/pharmacology , Anti-Bacterial Agents/chemical synthesis , Antifungal Agents/chemical synthesis , Bacteria/drug effects , Bismuth/chemistry , Candida albicans/drug effects , Candida tropicalis/drug effects , Coordination Complexes/chemical synthesis , Ligands , Microbial Sensitivity Tests , Thiophenes/chemical synthesis
3.
BMC Complement Altern Med ; 18(1): 252, 2018 Sep 15.
Article in English | MEDLINE | ID: mdl-30219066

ABSTRACT

BACKGROUND: The search for new antimicrobials should take into account drug resistance phenomenon. Medicinal plants are known as sources of potent antimicrobial compounds including flavonoids. The objective of this investigation was to evaluate the antimicrobial activities of flavonoid glycosides from Graptophyllum grandulosum, as well as to determine their mechanism of antibacterial action using lysis, leakage and osmotic stress assays. METHODS: The plant extracts were prepared by maceration in organic solvents. Column chromatography of the n-butanol extract followed by purification of different fractions led to the isolation of five flavonoid glycosides. The antimicrobial activities of extracts/compounds were evaluated using the broth microdilution method. The bacteriolytic activity was evaluated using the time-kill kinetic method. The effect of extracts on the red blood cells and bacterial cell membrane was determined by spectrophotometric methods. RESULTS: Chrysoeriol-7-O-ß-D-xyloside (1), luteolin-7-O-ß-D-apiofuranosyl-(1 → 2)-ß-D-xylopyranoside (2), chrysoeriol-7-O-ß-D-apiofuranosyl-(1 → 2)-ß-D-xylopyranoside (3), chrysoeriol-7-O-α-L-rhamnopyranosyl-(1 → 6)-ß-D-(4"-hydrogeno sulfate) glucopyranoside (4) and isorhamnetin-3-O-α-L-rhamnopyranosyl-(1 → 6)-ß-D-glucopyranoside (5) were isolated from G. grandulosum and showed different degrees of antimicrobial activities. Their antibacterial activities against multi-drug-resistant Vibrio cholerae strains were in some cases equal to, or higher than those of ciprofloxacin used as reference antibiotic. The antibacterial activities of flavonoid glycosides and chloramphenicol increased under osmotic stress (5% NaCl) whereas that of vancomycin decreased under this condition. V. cholerae suspension treated with flavonoid glycosides, showed a significant increase in the optical density at 260 nm, suggesting that nucleic acids were lost through a damaged cytoplasmic membrane. A decrease in the optical density of V. cholerae NB2 suspension treated with the isolated compounds was observed, indicating the lysis of bacterial cells. The tested samples were non-toxic to normal cells highlighting their good selectivity index. CONCLUSIONS: The results of the present study indicate that the purified flavonoids from G. glandulosum possess antimicrobial activities. Their mode of antibacterial activity is due to cell lysis and disruption of the cytoplasmic membrane upon membrane permeability.


Subject(s)
Acanthaceae/chemistry , Anti-Bacterial Agents/pharmacology , Flavonoids/pharmacology , Glycosides/pharmacology , Plant Extracts/pharmacology , Animals , Anti-Bacterial Agents/chemistry , Bacteria/drug effects , Cell Membrane/drug effects , Erythrocytes , Flavonoids/chemistry , Glycosides/chemistry , Hemolysis/drug effects , Microbial Sensitivity Tests , Plant Extracts/chemistry , Rats
4.
BMC Complement Altern Med ; 18(1): 159, 2018 May 16.
Article in English | MEDLINE | ID: mdl-29769064

ABSTRACT

BACKGROUND: Antimicrobial resistance is a serious threat against humankind and the search for new therapeutics is needed. This study aims to investigate the antimicrobial and antioxidant activities of ethanol extracts and compounds isolated from Dissotis senegambiensis and Amphiblemma monticola, two Cameroonian Melastomataceae species traditionally used for the treatment of fever, malaria and infectious diseases. METHODS: The plant extracts were prepared by maceration in ethanol. Standard chromatographic and spectroscopic methods were used to isolate and identify fourteen compounds from the two plant species [1-6 (from D. senegambiensis), 3, 4 and 7-14 (from A. monticola)]. A two-fold serial micro-dilution method was used to determine the minimum inhibitory concentration (MIC) against four bacterial strains including two resistant bacterial strains, methicillin resistant S. aureus (MRSA3) and methicillin resistant S. aureus (MRSA4) and three yeast strains. RESULTS: The fractionation of EtOH extracts afforded fourteen compounds belonging to triterpenoid and phenolic derivatives. The ethanol extracts, compounds 3, 5-8, 10 and the mixture of 10 + 12 were active against all the tested bacterial and fungal species. Compound 7 (MIC = 16-32 µg/mL) and 10 (MIC = 8-16 µg/mL) displayed the largest antibacterial and antifungal activities, respectively. Compounds 7, 10 and the mixture of 10 + 12 showed prominent antibacterial activity against methicillin- resistant S. aureus (MRSA) which is in some cases equal to that of ciprofloxacin used as reference antibacterial drug. Compound 8 also showed high radical-scavenging activities and ferric reducing power when compared with vitamin C and butylated hydroxytoluene used as reference antioxidants. The tested samples were non-toxic to normal cells highlighting their good selectivity. CONCLUSIONS: The result of this investigation reveals the potential of D. senegambiensis and A. monticola as well as the most active compounds in the search for new antimicrobial and antioxidant agents. So, further investigations are needed.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antioxidants/pharmacology , Melastomataceae/chemistry , Plant Extracts/pharmacology , Animals , Anti-Bacterial Agents/chemistry , Antioxidants/chemistry , Biphenyl Compounds , Cameroon , Erythrocytes , Hemolysis/drug effects , Methicillin-Resistant Staphylococcus aureus/drug effects , Phenols/chemistry , Phenols/pharmacology , Picrates , Plant Extracts/chemistry , Plant Extracts/toxicity , Rats , Triterpenes/chemistry , Triterpenes/pharmacology
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