scholarly journals Improved Antibacterial Activity of Water-Soluble Nanoformulated Kaempferol and Combretastatin Polyphenolic Compounds

2021 ◽  
Vol 2021 ◽  
pp. 1-12
Author(s):  
Y. Santhosh Kumar ◽  
Langeswaran Kulanthaivel ◽  
G. S. Hikku ◽  
R. Saravanan ◽  
Thangavelu Lakshmi ◽  
...  

Kaempferol and combretastatin are polyphenolic compounds derived from plant sources which are known for their antibacterial activity. However, owing to their large size and water insolubility, their antibacterial activity is limited. In this context, the present study focused on the nanoformulation of kaempferol (NF-k) and combretastatin (NF-c) and their influence on water solubility and antibacterial properties. The NF-k and NF-c were prepared using the solvent evaporation method and were thoroughly characterized for evaluating the morphology, molecular vibrations, size, etc. Based on the results, it is observed that the pristine forms of kaempferol and combretastatin drugs get nanoformulated and completely soluble in water. Using particle size analyzer, the particle sizes of NF-k and NF-c were estimated as 334 nm and 260 nm, respectively, which are very fine compared to pristine kaempferol and combretastatin (5193 nm and 1217 nm, respectively). The molecular vibrations that exist in NF-k and NF-c were confirmed by the Fourier transform infrared spectra, where the nanoformulated drug showed lower intensities than the pristine form of kaempferol and combretastatin. The drug release kinetics of the nanoformulated drugs were carried out using the dialysis membrane method and were compared with their pristine forms. Owing to the size effect, the NF-k and NF-c release up to 50% of the drug in a sustained manner till 50 h showing twofold higher concentration than the control where it released 25%. The antibacterial activity was assessed by measuring the optical density at 600 nm using UV-vis spectrophotometer and displayed significant activity against gram-positive Staphylococcus aureus strain. The mechanisms behind the antibacterial activity of NF-k and NF-c were discussed in detail. The activation of ATP-dependent efflux pump system and the blockage of porin channels could be the cause for the bactericidal activity. Our understanding of efflux pumps and their role in antibacterial activity is still in its early stages. No studies have been performed to date using nanoformulations of kaempferol and combretastatin to investigate their roles. This complicates the determination of the exact mechanisms acting against bacterial growth when using nanoformulation drugs. Our increasing knowledge of water-soluble nanoformulation drugs and their roles in reduced bacterial activity will pave the way to developing effective treatments in the future.

Polymers ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 1140
Author(s):  
Silvana Alfei ◽  
Gabriella Piatti ◽  
Debora Caviglia ◽  
Anna Maria Schito

The growing resistance of bacteria to current chemotherapy is a global concern that urgently requires new and effective antimicrobial agents, aimed at curing untreatable infection, reducing unacceptable healthcare costs and human mortality. Cationic polymers, that mimic antimicrobial cationic peptides, represent promising broad-spectrum agents, being less susceptible to develop resistance than low molecular weight antibiotics. We, thus, designed, and herein report, the synthesis and physicochemical characterization of a water-soluble cationic copolymer (P5), obtained by copolymerizing the laboratory-made monomer 4-ammoniumbuthylstyrene hydrochloride with di-methyl-acrylamide as uncharged diluent. The antibacterial activity of P5 was assessed against several multi-drug-resistant clinical isolates of both Gram-positive and Gram-negative species. Except for strains characterized by modifications of the membrane charge, most of the tested isolates were sensible to the new molecule. P5 showed remarkable antibacterial activity against several isolates of genera Enterococcus, Staphylococcus, Pseudomonas, Klebsiella, and against Escherichia coli, Acinetobacter baumannii and Stenotrophomonas maltophilia, displaying a minimum MIC value of 3.15 µM. In time-killing and turbidimetric studies, P5 displayed a rapid non-lytic bactericidal activity. Due to its water-solubility and wide bactericidal spectrum, P5 could represent a promising novel agent capable of overcoming severe infections sustained by bacteria resistant the presently available antibiotics.


2021 ◽  
Vol 01 ◽  
Author(s):  
Vivek Ahluwalia ◽  
Nusrat Iqbal ◽  
Samsul Alam ◽  
Vinod Kumar ◽  
Lalitesh K. Thakur ◽  
...  

: New molecules of natural origin with antibacterial properties are urgently required to control the antibiotic resistance. Worldwide, antibiotic resistance is key threats due to non-judicious and incongruous use of antibiotics. Researchers are focusing on identifying molecules from plant biodiversity that could have both antioxidant and antibacterial properties in one molecule. Much importance on natural antibacterial compounds has been given to the polyphenolic compounds from food commodities. The roles of dietary habits in disease prevention have been credited to presence of polyphenols with antioxidant properties. Polyphenols are secondary metabolites with manifold vital roles including antibacterial activity. Numerous mechanisms like bacterial membrane destruction, destruction of virulence factors, inhibition of the enzymes activity and toxins had been reported for antibacterial activity. Also, hydroxyl, alkyl and acetate moiety on aromatic nucleus influences both antioxidant and antibacterial activity. In this review, details are summarized concerning the antibacterial properties of the key polyphenolic compounds with antioxidant properties.


Marine Drugs ◽  
2019 ◽  
Vol 17 (1) ◽  
pp. 43 ◽  
Author(s):  
Ruilian Li ◽  
Xianghua Yuan ◽  
Jinhua Wei ◽  
Xiafei Zhang ◽  
Gong Cheng ◽  
...  

Microbial biofilms are considerably more resistant to antibiotics than planktonic cells. It has been reported that chitosan coupling with the aminoglycoside antibiotic streptomycin dramatically disrupted biofilms of several Gram-positive bacteria. This finding suggested the application of the covalent conjugate of antimicrobial natural polysaccharides and antibiotics on anti-infection therapy. However, the underlying molecular mechanism of the chitosan-streptomycin conjugate (CS-Strep) remains unclear and the poor water-solubility of the conjugate might restrict its applications for anti-infection therapy. In this study, we conjugated streptomycin with water-soluble chitosan oligosaccharides (COS). Unlike CS-Strep, the COS-streptomycin conjugate (COS-Strep) barely affected biofilms of tested Gram-positive bacteria. However, COS-Strep efficiently eradicated established biofilms of the Gram-negative pathogen Pseudomonas aeruginosa. This activity of COS-Strep was influenced by the degree of polymerization of chitosan oligosaccharide. The increased susceptibility of P. aeruginosa biofilms to antibiotics after conjugating might be related to the following: Suppression of the activation of MexX-MexY drug efflux pump system induced by streptomycin treatment; and down-regulation of the biosynthesis of biofilm exopolysaccharides. Thus, this work indicated that covalently linking antibiotics to chitosan oligosaccharides was a possible approach for the development of antimicrobial drugs against biofilm-related infections.


2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
Adel S. Al-Zubairi ◽  
Ahmad Bustamam Abdul ◽  
Siddig Ibrahim Abdelwahab ◽  
Chew Yuan Peng ◽  
Syam Mohan ◽  
...  

The use of evidence-based complementary and alternative medicine is increasing rapidly.Eleucine indica(EI) is traditionally used in ailments associated with liver and kidneys. The therapeutic benefit of the medicinal plants is often attributed to their antioxidant properties. Therefore, the aim of this study was to screen the hexane, dicholoromethane, ethyl acetate (EA) and methanol extracts (MeTH) of EI for their antioxidant, antibacterial and anti-cancer effects using total phenolic contents (TPCs) and DPPH, disc diffusion method and MTT cytotoxicity assays, respectively. The MeTH was showed to have the highest TPC and scavenging activity (77.7%) on DPPH assay, followed by EA (64.5%), hexane (47.19%) and DCM (40.83%) extracts, whereas the MeTH showed no inhibitory effect on all tested bacteria strains. However, the EA extract exhibited a broad spectrum antibacterial activity against all tested bacteria exceptBacillus subtilis, in which this bacterium was found to be resistant to all EI extracts. Meanwhile, hexane extract was demonstrated to have a remarkable antibacterial activity against methicillin resistantStaphylococcus aureus(MRSA) andPseudomonas aeruginosa, while the dicholoromethane extract did not exhibit significant activity againstP. aeruginosa. None of the extracts showed significant cytotoxic activity towards MCF-7, HT-29 and CEM-SS human cancer cell lines after 72 h incubation time (IC50> 30 μg/ml). These results demonstrate that the extract prepared from the EI possesses antioxidant activityin vitroin addition to antibacterial properties. Further investigations are needed to verify the antioxidant effectsin vitroandin vivo.


2017 ◽  
Vol 2017 ◽  
pp. 1-11 ◽  
Author(s):  
Erika Adomavičiūtė ◽  
Solveiga Pupkevičiūtė ◽  
Vaida Juškaitė ◽  
Modestas Žilius ◽  
Sigitas Stanys ◽  
...  

An electrospun hydrophilic non-water-soluble biocompatible polylactic acid (PLA) nonwoven material was used as a delivery system for propolis ethanolic extract (PEE) and silver nanoparticles (AgNPs) that are known for their established antiseptic and antimicrobial activity. Combination of PEE and AgNPs in a single product should provide efficient antimicrobial protection and improved wound healing. Evaluations of PEE and AgNPs on morphology of electrospun materials, release kinetics of AgNPs and phenolic compounds, antibacterial properties, and cytotoxicity of electrospun PLA materials were performed. The presence of PEE or/and AgNPs resulted in denser mats formed by thicker PLA fibers. The average diameter of PLA microfibers was 168±29 nm. The average diameter of microfibers increased to 318±40 and 370±30 nm when 10 wt% and 20 wt% ethanol were added, respectively. Addition of 10 wt% or 20 wt% PEE increased the diameter to 282±25 and 371±25 nm, respectively. Suspension of AgNPs also caused the formation of thicker microfibers with 254±25 nm diameter. Electrospun PLA microfibers with PEE maintained viability of HaCaT cells. Testing of antimicrobial activity confirmed the ability of AgNPs containing PLA electrospun materials to inhibit the growth of microorganisms.


Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3947 ◽  
Author(s):  
Focsan ◽  
Polyakov ◽  
Kispert

Carotenoids are natural dyes and antioxidants widely used in food processing and in therapeutic formulations. However, their practical application is restricted by their high sensitivity to external factors such as heat, light, oxygen, metal ions and processing conditions, as well as by extremely low water solubility. Various approaches have been developed to overcome these problems. In particular, it was demonstrated that application of supramolecular complexes of “host-guest” type with water-soluble nanoparticles allows minimizing the abovementioned disadvantages. From this point of view, nanoencapsulation of carotenoids is an effective strategy to improve their stability during storage and food processing. Also, nanoencapsulation enhances bioavailability of carotenoids via modulating their release kinetics from the delivery system, influencing the solubility and absorption. In the present paper, we present the state of the art of carotenoid nanoencapsulation and summarize the data obtained during last five years on preparation, analysis and reactivity of carotenoids encapsulated into various nanoparticles. The possible mechanisms of carotenoids bioavailability enhancement by multifunctional delivery systems are also discussed.


2019 ◽  
Vol 34 (8) ◽  
pp. 1052-1058
Author(s):  
Héctor A Lobato-Aguilar ◽  
Gabriel Lizama-Uc ◽  
Jorge A Uribe-Calderon ◽  
Juan Cauich-Rodriguez ◽  
Nayeli Rodriguez-Fuentes ◽  
...  

Organoclays were prepared by means of cation-exchange reactions using different concentrations of chlorhexidine diacetate and two different types of clays: montmorillonite and palygorskite. The antibacterial activity against Escherichia coli was evaluated by means of disk diffusion tests as well as through bacterial growth inhibition (monitored by optical density measurements) in Luria broth media. Results indicate that modified palygorskites showed a greater antibacterial activity than those exhibited by modified montmorillonite, as latter only displayed antibacterial properties at the highest chlorhexidine diacetate loading. Modeling of chlorhexidine release was also performed and the models best described the drug release phenomena depended on the type of clay; being the Higuchi model and Korsemeyer–Peppas model for montmorillonite, whereas the zero-order model and Korsemeyer–Peppas model for palygorskite.


Foods ◽  
2019 ◽  
Vol 8 (4) ◽  
pp. 132 ◽  
Author(s):  
Chang Ha Park ◽  
Ye Eun Park ◽  
Hyeon Ji Yeo ◽  
Se Won Chun ◽  
Thanislas Bastin Baskar ◽  
...  

The discovery of a new species exhibiting more effective antibacterial properties is necessary because of the demand on Lavandula species, which continues to increase in a variety of industries. Lavandula pubescens might be a good alternative, as it exhibits strong antibacterial activity. In this study, the chemical composition of the essential oils from different organs (flowers, leaves, stems, and roots) of L. pubescens was identified using gas chromatography-mass spectrometry. Furthermore, the antimicrobial activities of different solvent extracts (methanol, ethanol, diethyl ether, hexane, and ethyl acetate) and different organ (flower, leaf, stem, and root) extracts of L. pubescens were evaluated. Only the ethyl acetate extracts of L. pubescens exhibited antibacterial activity against all bacterial strains tested, including Staphylococcus haemolyticus, Escherichia coli (KF 918342), Aeromonas hydrophila (KCTC 12487), E. coli (ATCC 35150), Cronobacter sakazakii (ATCC 29544), and Aeromonas salmonicida (KACC 15136). In particular, the extracts exhibited significant activity against S. haemolyticus. Ethyl acetate extract of the leaf exhibited the best activity against all bacterial strains. This study provides valuable information on the chemical compositions in essential oils and antimicrobial properties of L. pubescens.


2019 ◽  
Author(s):  
Jenna Franke ◽  
Benjamin Raliski ◽  
Steven Boggess ◽  
Divya Natesan ◽  
Evan Koretsky ◽  
...  

Fluorophores based on the BODIPY scaffold are prized for their tunable excitation and emission profiles, mild syntheses, and biological compatibility. Improving the water-solubility of BODIPY dyes remains an outstanding challenge. The development of water-soluble BODIPY dyes usually involves direct modification of the BODIPY fluorophore core with ionizable groups or substitution at the boron center. While these strategies are effective for the generation of water-soluble fluorophores, they are challenging to implement when developing BODIPY-based indicators: direct modification of BODIPY core can disrupt the electronics of the dye, complicating the design of functional indicators; and substitution at the boron center often renders the resultant BODIPY incompatible with the chemical transformations required to generate fluorescent sensors. In this study, we show that BODIPYs bearing a sulfonated aromatic group at the meso position provide a general solution for water-soluble BODIPYs. We outline the route to a suite of 5 new sulfonated BODIPYs with 2,6-disubstitution patterns spanning a range of electron-donating and -withdrawing propensities. To highlight the utility of these new, sulfonated BODIPYs, we further functionalize them to access 13 new, BODIPY-based voltage-sensitive fluorophores. The most sensitive of these BODIPY VF dyes displays a 48% ΔF/F per 100 mV in mammalian cells. Two additional BODIPY VFs show good voltage sensitivity (≥24% ΔF/F) and excellent brightness in cells. These compounds can report on action potential dynamics in both mammalian neurons and human stem cell-derived cardiomyocytes. Accessing a range of substituents in the context of a water soluble BODIPY fluorophore provides opportunities to tune the electronic properties of water-soluble BODIPY dyes for functional indicators.


2017 ◽  
Vol 23 (3) ◽  
pp. 467-480 ◽  
Author(s):  
Satyanarayan Pattnaik ◽  
Kamla Pathak

Background: Improvement of oral bioavailability through enhancement of dissolution for poorly soluble drugs has been a very promising approach. Recently, mesoporous silica based molecular sieves have demonstrated excellent properties to enhance the dissolution velocity of poorly water-soluble drugs. Description: Current research in this area is focused on investigating the factors influencing the drug release from these carriers, the kinetics of drug release and manufacturing approaches to scale-up production for commercial manufacture. Conclusion: This comprehensive review provides an overview of different methods adopted for synthesis of mesoporous materials, influence of processing factors on properties of these materials and drug loading methods. The drug release kinetics from mesoporous silica systems, the manufacturability and stability of these formulations are reviewed. Finally, the safety and biocompatibility issues related to these silica based materials are discussed.


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