Displaying publications 61 - 80 of 98 in total

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  1. Hibiscus cannabinus L. (kenaf) studies: Nutritional composition, phytochemistry, pharmacology, and potential applications
    Sim YY, Nyam KL
    Food Chem, 2021 May 15;344:128582.
    PMID: 33199120 DOI: 10.1016/j.foodchem.2020.128582
    The electronic database was searched up to July 2020, using keywords, kenaf and roselle, chemical constituents of kenaf and roselle, therapeutic uses of kenaf and roselle. Journals, books and conference proceedings were also searched. Investigations of pharmacological activities of kenaf revealed that this edible plant exhibits a broad range of therapeutic potential including antioxidant, antimicrobial, antityrosinase, anticancer, antihyperlipidemia, antiulcer, anti-inflammatory, and hepatoprotective activities. Kenaf also showed versatile utility as a functional ingredient in food, folk medicine, and animal nutritions, as well as in nanotechnology processes. The exploitation of underexploited kenaf by-products can be a significant part of waste management from an economic and environmental point of view. In addition, kenaf showed comparable nutritional, phytochemical, and pharmacological properties with Hibiscus sabdariffa (Roselle). This review has important implications for further investigations and applications of kenaf in food and pharmaceuticals industry.
    Matched MeSH terms: Anti-Infective Agents/chemistry
  2. The biological activities of the spiderworts (Tradescantia)
    Tan JBL, Kwan YM
    Food Chem, 2020 Jul 01;317:126411.
    PMID: 32087517 DOI: 10.1016/j.foodchem.2020.126411
    Widely used throughout the world as traditional medicine for treating a variety of diseases ranging from cancer to microbial infections, members of the Tradescantia genus show promise as sources of desirable bioactive compounds. The bioactivity of several noteworthy species has been well-documented in scientific literature, but with nearly seventy-five species, there remains much to explore in this genus. This review aims to discuss all the bioactivity-related studies of Tradescantia plants and the compounds discovered, including their anticancer, antimicrobial, antioxidant, and antidiabetic activities. Gaps in knowledge will also be identified for future research opportunities.
    Matched MeSH terms: Anti-Infective Agents/chemistry
  3. Black sea cucumber (Holothuria atra Jaeger, 1833) rescues Pseudomonas aeruginosa-infected Caenorhabditis elegans via reduction of pathogen virulence factors and enhancement of host immunity
    Lee WT, Tan BK, Eng SA, Yuen GC, Chan KL, Sim YK, et al.
    Food Funct, 2019 Sep 01;10(9):5759-5767.
    PMID: 31453615 DOI: 10.1039/c9fo01357a
    A strategy to circumvent the problem of multidrug resistant pathogens is the discovery of anti-infectives targeting bacterial virulence or host immunity. Black sea cucumber (Holothuria atra) is a tropical sea cucumber species traditionally consumed as a remedy for many ailments. There is a paucity of knowledge on the anti-infective capacity of H. atra and the underlying mechanisms involved. The objective of this study is to utilize the Caenorhabditis elegans-P. aeruginosa infection model to elucidate the anti-infective properties of H. atra. A bioactive H. atra extract and subsequently its fraction were shown to have the capability of promoting the survival of C. elegans during a customarily lethal P. aeruginosa infection. The same entities also attenuate the production of elastase, protease, pyocyanin and biofilm in P. aeruginosa. The treatment of infected transgenic lys-7::GFP worms with this H. atra fraction restores the repressed expression of the defense enzyme lys-7, indicating an improved host immunity. QTOF-LCMS analysis revealed the presence of aspidospermatidine, an indole alkaloid, and inosine in this fraction. Collectively, our findings show that H. atra possesses anti-infective properties against P. aeruginosa infection, by inhibiting pathogen virulence and, eventually, reinstating host lys-7 expression.
    Matched MeSH terms: Anti-Infective Agents/chemistry
  4. Potential targets by pentacyclic triterpenoids from Callicarpa farinosa against methicillin-resistant and sensitive Staphylococcus aureus
    Chung PY, Chung LY, Navaratnam P
    Fitoterapia, 2014 Apr;94:48-54.
    PMID: 24508863 DOI: 10.1016/j.fitote.2014.01.026
    The evolution of antibiotic resistance in Staphylococcus aureus showed that there is no long-lasting remedy against this pathogen. The limited number of antibacterial classes and the common occurrence of cross-resistance within and between classes reinforce the urgent need to discover new compounds targeting novel cellular functions not yet targeted by currently used drugs. One of the experimental approaches used to discover novel antibacterials and their in vitro targets is natural product screening. Three known pentacyclic triterpenoids were isolated for the first time from the bark of Callicarpa farinosa Roxb. (Verbenaceae) and identified as α-amyrin [3β-hydroxy-urs-12-en-3-ol], betulinic acid [3β-hydroxy-20(29)-lupaene-28-oic acid], and betulinaldehyde [3β-hydroxy-20(29)-lupen-28-al]. These compounds exhibited antimicrobial activities against reference and clinical strains of methicillin-resistant (MRSA) and methicillin-sensitive S. aureus (MSSA), with minimum inhibitory concentration (MIC) ranging from 2 to 512 μg/mL. From the genome-wide transcriptomic analysis to elucidate the antimicrobial effects of these compounds, multiple novel cellular targets in cell division, two-component system, ABC transporters, fatty acid biosynthesis, peptidoglycan biosynthesis, aminoacyl-tRNA synthetases, ribosomes and β-lactam resistance pathways are affected, resulting in destabilization of the bacterial cell membrane, halt in protein synthesis, and inhibition of cell growth that eventually lead to cell death. The novel targets in these essential pathways could be further explored in the development of therapeutic compounds for the treatment of S. aureus infections and help mitigate resistance development due to target alterations.
    Matched MeSH terms: Anti-Infective Agents/chemistry
  5. Antimicrobial effects of Caulerpa sertularioides extract on foodborne diarrhea-caused bacteria
    Darah I, Tong WY, Nor-Afifah S, Nurul-Aili Z, Lim SH
    Eur Rev Med Pharmacol Sci, 2014;18(2):171-8.
    PMID: 24488904
    Caulerpa (C.) sertularioides has many therapeutic uses in the practice of traditional medicine in Malaysia. Crude methanolic, diethyl ether extract, ethyl acetate extract and butanolic extract from C. sertularioides were subjected to antimicrobial screening including the three Gram-positive and three Gram-negative diarrhea-caused bacteria.
    Matched MeSH terms: Anti-Infective Agents/chemistry
  6. Carboxymethyl cellulose wafers containing antimicrobials: a modern drug delivery system for wound infections
    Ng SF, Jumaat N
    Eur J Pharm Sci, 2014 Jan 23;51:173-9.
    PMID: 24076463 DOI: 10.1016/j.ejps.2013.09.015
    Lyophilised wafers have been shown to have potential as a modern dressing for mucosal wound healing. The wafer absorbs wound exudates and transforms into a gel, thus providing a moist environment which is essential for wound healing. The objective of this study was to develop a carboxymethyl cellulose wafer containing antimicrobials to promote wound healing and treat wound infection. The pre-formulation studies began with four polymers, sodium carboxymethyl cellulose (NaCMC), methylcellulose (MC), sodium alginate and xanthan gum, but only NaCMC and MC were chosen for further investigation. The wafers were characterised by physical assessments, solvent loss, microscopic examination, swelling and hydration properties, drug content uniformity, drug release and efficacy of antimicrobials. Three of the antimicrobials, neomycin trisulphate salt hydrate, sulphacetamide sodium and silver nitrate, were selected as model drugs. Among the formulations, NaCMC wafer containing neomycin trisulphate exhibited the most desirable wound dressing characteristics (i.e., flexibility, sponginess, uniform wafer texture, high content drug uniformity) with the highest in vitro drug release and the greatest inhibition against both Gram positive and Gram negative bacteria. In conclusion, we successfully developed a NaCMC lyophilised wafer containing antimicrobials, and this formulation has potential for use in mucosal wounds infected with bacteria.
    Matched MeSH terms: Anti-Infective Agents/chemistry*
  7. Medicinal uses, phytochemistry and pharmacology of family Sterculiaceae: a review
    Al Muqarrabun LM, Ahmat N
    Eur J Med Chem, 2015 Mar 6;92:514-30.
    PMID: 25599949 DOI: 10.1016/j.ejmech.2015.01.026
    The family Sterculiaceae is one of the most important families among flowering plants. Many of its members demonstrate medicinal properties and have been used for the treatment of various ailments and wounds. A wide range of compounds including alkaloids, phenyl propanoids, flavonoids, terpenoids and other types of compounds including hydrocarbons, sugars, quinones, phenolic acids, lactones, lignans, amine and amides have been isolated from several species in this family. Few studies have reported that some extracts and single compounds isolated from this family exhibited several biological activities, such as antimicrobial, anti-inflammatory, antioxidant and cytotoxic activities. The present review is an effort to provide information about the traditional uses, phytochemistry and pharmacology of species from family Sterculiaceae, and to uncover the gaps and potentials requiring further research opportunities regarding the chemistry and pharmacy of this family.
    Matched MeSH terms: Anti-Infective Agents/chemistry
  8. Click chemistry approach: regioselective one-pot synthesis of some new 8-trifluoromethylquinoline based 1,2,3-triazoles as potent antimicrobial agents
    Garudachari B, Isloor AM, Satyanarayana MN, Fun HK, Hegde G
    Eur J Med Chem, 2014 Mar 3;74:324-32.
    PMID: 24486415 DOI: 10.1016/j.ejmech.2014.01.008
    Three series of 8-trifluoromethylquinoline based 1,2,3-triazoles derivatives (5a-c, 6a-d and 7a-c) were synthesized by multi-step reactions by click chemistry approach. Synthesized compounds were characterized by spectral studies and X-ray analysis. The final compounds were screened for their in-vitro antimicrobial activity by well plate method (zone of inhibition). Compounds 5c, 6b, 8b, 11 and 12 were found to be active against tested microbial strains. The results are summarized in Tables 5 and 6.
    Matched MeSH terms: Anti-Infective Agents/chemistry
  9. Synthesis and antimicrobial properties of some new thiazolyl coumarin derivatives
    Arshad A, Osman H, Bagley MC, Lam CK, Mohamad S, Zahariluddin AS
    Eur J Med Chem, 2011 Sep;46(9):3788-94.
    PMID: 21712145 DOI: 10.1016/j.ejmech.2011.05.044
    Two novel series of hydrazinyl thiazolyl coumarin derivatives have been synthesized and fully characterized by IR, (1)H NMR, (13)C NMR, elemental analysis and mass spectral data. The structures of some compounds were further confirmed by X-ray crystallography. All of these derivatives, 10a-d and 15a-h, were screened in vitro for antimicrobial activity against various bacteria species including Mycobacterium tuberculosis and Candida albicans. The compounds 10c, 10d and 15e exhibited very good activities against all of the tested microbial strains.
    Matched MeSH terms: Anti-Infective Agents/chemistry
  10. Hybrid molecules based on 1,3,5-triazine as potential therapeutics: A focused review
    Prasher P, Sharma M, Aljabali AAA, Gupta G, Negi P, Kapoor DN, et al.
    Drug Dev Res, 2020 11;81(7):837-858.
    PMID: 32579723 DOI: 10.1002/ddr.21704
    Majority of the representative drugs customarily interact with multiple targets manifesting unintended side effects. In addition, drug resistance and over expression of the cellular efflux-pumps render certain classes of drugs ineffective. With only a few innovative formulations in development, it is necessary to identify pharmacophores and novel strategies for creating new drugs. The conjugation of dissimilar pharmacophoric moieties to design hybrid molecules with an attractive therapeutic profile is an emerging paradigm in the contemporary drug development regime. The recent decade witnessed the remarkable biological potential of 1,3,5-triazine framework in the development of various chemotherapeutics. The appending of the 1,3,5-triazine nucleus to biologically relevant moieties has delivered exciting results. The present review focuses on 1,3,5-triazine based hybrid molecules in the development of pharmaceuticals.
    Matched MeSH terms: Anti-Infective Agents/chemistry
  11. Transdermal anti-inflammatory activity of bilayer film containing olive compound hydroxytyrosol: physical assessment, in vivo dermal safety and efficacy study in Freund's adjuvant-induced arthritic rat model
    Ng SF, Tan LS, Buang F
    Drug Dev Ind Pharm, 2017 Jan;43(1):108-119.
    PMID: 27588411 DOI: 10.1080/03639045.2016.1224893
    Previous studies have shown that hydroxytyrosol (HT) can be a potential alternative therapeutic agent for the treatment of rheumatoid arthritis (RA). However, HT is extensively metabolized following oral administration, which leads to formulating HT in a topical vehicle to prolong drug action as well as to provide a localized effect. Hidrox-6 is a freeze-dried powder derived from fresh olives and contains a high amount of HT (∼3%) and other polyphenols. Alginate bilayer films containing 5% and 10% Hidrox-6 were formulated. The films were characterized with respect to their physical, morphology, rheological properties; drug content uniformity; and in vitro drug release. Acute dermal irritancy tests and a skin sensitization study were carried out in rats. An efficacy study of the bilayer films for RA was conducted using Freund's adjuvant-induced polyarthritis rats. Animal data showed that the bilayer film formulations did not cause skin irritancy. The efficacy in vivo results showed that the Hidrox-6 bilayer films lowered the arthritic scores, paw and ankle circumference, serum IL-6 level and cumulative histological scores compared with those measured for controls. The topical Hidrox-6 bilayer films improve synovitis and inflammatory symptoms in RA and can be a potential alternative to oral RA therapy.
    Matched MeSH terms: Anti-Infective Agents/chemistry
  12. Fulltext Isolation and characterization of cyclo-(tryptophanyl-prolyl) and chloramphenicol from Streptomyces sp. SUK 25 with antimethicillin-resistant Staphylococcus aureus activity
    Alshaibani MM, Jalil J, Sidik NM, Edrada-Ebel R, Zin NM
    Drug Des Devel Ther, 2016;10:1817-27.
    PMID: 27330275 DOI: 10.2147/DDDT.S101212
    BACKGROUND: Zingiber spectabile, commonly known as Beehive Ginger, is used as an ethnobotanical plant in many countries as an appetizer or to treat stomachache, toothache, muscle sprain, and as a cure for swelling, sores and cuts. This is the first report of isolation of Streptomyces strain from the root of this plant. Strain Universiti Kebangsaan 25 (SUK 25) has a very high activity to produce secondary metabolites against methicillin-resistant Staphylococcus aureus (MRSA), which is associated with high morbidity and mortality rates due to acquired multidrug resistance genes and causes medication failure in some clinical cases worldwide. Phylogenetic analysis based on the 16S ribosomal RNA gene sequence exhibited that the most closely related strain was Streptomyces omiyaensis NBRC 13449T (99.0% similarity).

    AIM: This study was conducted to carry out the extraction, identification, and biological evaluation of active metabolites isolated from SUK 25 against three MRSA strains, namely, MRSA ATCC 43300, MRSA ATCC 33591, and MRSA ATCC 49476.

    MATERIALS AND METHODS: The production of secondary metabolites by this strain was optimized through Thronton's media. Isolation, purification, and identification of the bioactive compounds were carried out using reversed-phase high-performance liquid chromatography, high-resolution mass spectrometry, Fourier transform infrared, and one-dimensional and two-dimensional nuclear magnetic resonance.

    RESULTS: During screening procedure, SUK 25 exhibited good antimicrobial potential against several strains of MRSA. The best biological activity was shown from fraction number VII and its subfractions F2 and F3 with minimum inhibitory concentration values at 16 µg/mL and 8 µg/mL, respectively. These two subfractions were identified as diketopiperazine cyclo-(tryptophanyl-prolyl) and chloramphenicol.

    CONCLUSION: On the basis of obtained results, SUK 25 isolated from Z. spectabile can be regarded as a new valuable source to produce secondary metabolites against bacteria, especially MRSA.

    Matched MeSH terms: Anti-Infective Agents/chemistry
  13. Fulltext Berberine nanoparticles with enhanced in vitro bioavailability: characterization and antimicrobial activity
    Sahibzada MUK, Sadiq A, Faidah HS, Khurram M, Amin MU, Haseeb A, et al.
    Drug Des Devel Ther, 2018;12:303-312.
    PMID: 29491706 DOI: 10.2147/DDDT.S156123
    BACKGROUND: Berberine is an isoquinoline alkaloid widely used in Ayurveda and traditional Chinese medicine to treat illnesses such as hypertension and inflammatory conditions, and as an anticancer and hepato-protective agent. Berberine has low oral bioavailability due to poor aqueous solubility and insufficient dissolution rate, which can reduce the efficacy of drugs taken orally. In this study, evaporative precipitation of nanosuspension (EPN) and anti-solvent precipitation with a syringe pump (APSP) were used to address the problems of solubility, dissolution rate and bioavailability of berberine.

    METHODS: Semi-crystalline nanoparticles (NPs) of 90-110 nm diameter for APSP and 65-75 nm diameter for EPN were prepared and then characterized using differential scanning calorimetry (DSC) and X-ray powder diffractometry (XRD). Thereafter, drug content solubility and dissolution studies were undertaken. Berberine and its NPs were evaluated for their antibacterial activity.

    RESULTS: The results indicate that the NPs have significantly increased solubility and dissolution rate due to conversion of the crystalline structure to a semi-crystalline form.

    CONCLUSION: Berberine NPs produced by both APSP and EPN methods have shown promising activities against Gram-positive and Gram-negative bacteria, and yeasts, with NPs prepared through the EPN method showing superior results compared to those made with the APSP method and the unprocessed drug.

    Matched MeSH terms: Anti-Infective Agents/chemistry
  14. Temperature-mediated absorption of phenylmercuric nitrate on polyethylene and polypropylene containers in chloramphenicol eye drops
    Charoo N, Chiew M, Tay A, Lian L
    Cutan Ocul Toxicol, 2014 Sep;33(3):242-6.
    PMID: 24147942 DOI: 10.3109/15569527.2013.837058
    The aim of this work was to find the effect of temperature and manufacturing source of phenylmercuric nitrate (PMN) on PMN absorption on low-density polyethylene (LDPE) and polypropylene containers in chloramphenicol eye drops. Two factorial experiments were designed to study the effect of temperature on PMN assay in chloramphenicol eye drops stored in LDPE and prepared from two different PMN sources. PMN source had no effect on PMN assay at 2-8 °C, however at stress conditions (30 °C/75%RH) for 3 weeks, the effect of PMN source on PMN assay was found significant (p 
    Matched MeSH terms: Anti-Infective Agents/chemistry*
  15. Imidazo[1,2-a]pyridine Scaffold as Prospective Therapeutic Agents
    Deep A, Bhatia RK, Kaur R, Kumar S, Jain UK, Singh H, et al.
    Curr Top Med Chem, 2017;17(2):238-250.
    PMID: 27237332
    Imidazo[1,2-a]pyridine is one of the most potential bicyclic 5-6 heterocyclic rings that is recognized as a "drug prejudice" scaffold due to its broad range of applications in medicinal chemistry such as anticancer, antimycobacterial, antileishmanial, anticonvulsant, antimicrobial, antiviral, antidiabetic, proton pump inhibitor, insecticidal activities. This scaffold has also been represented in various marketed preparations such as zolimidine, zolpidem, alpidem. Therefore, several attempts were made to carry out the structural modifications of this scaffold to discover and develop novel therapeutic agents. This review provides a valuable insight into the research findings of wide range of derivatives of imidazo[1,2-a]pyridine scaffold leading to promising heterocyclic compounds which could be explored further for the synthesis of new derivatives as well as construction of potential drug-like chemical libraries for biological screening in search of new therapeutic agents.
    Matched MeSH terms: Anti-Infective Agents/chemistry
  16. Calixarene: A Versatile Material for Drug Design and Applications
    Hussain MA, Ashraf MU, Muhammad G, Tahir MN, Bukhari SNA
    Curr Pharm Des, 2017;23(16):2377-2388.
    PMID: 27779081 DOI: 10.2174/1381612822666160928143328
    The therapy of various diseases by the drugs entrapped in calixarene derivatives is gaining attraction of researchers nowadays. Calixarenes are macrocyclic nano-baskets which belong to cavitands class of host-guest chemistry. They are the marvelous hosts with distinct hydrophobic three dimensional cavities to entrap and encapsulate biologically active guest drugs. Calixarene and its derivatives develop inclusion complexes with various types of drugs and vitamins for their sustained/targeted release. Calixarene and its derivatives are used as carriers for anti-cancer, anti-convulsant, anti-hypertensive, anthelmentic, anti-inflammatory, antimicrobial and antipsychotic drugs. They are the important biocompatible receptors to improve solubility, chemical reactivity and decrease cytotoxicity of poorly soluble drugs in supramolecular chemistry. This review focuses on the calixarene and its derivatives as the state-of-the-art in host-guest interactions for important drugs. We have also critically evaluated calixarenes for the development of prodrugs.
    Matched MeSH terms: Anti-Infective Agents/chemistry
  17. Are There Any Other Compounds Isolated From Dermacoccus spp at All?
    AlMatar M, Eldeeb M, Makky EA, Köksal F, Var I, Kayar B
    Curr Microbiol, 2017 Jan;74(1):132-144.
    PMID: 27785553 DOI: 10.1007/s00284-016-1152-3
    Microbial-derived natural products have functional and structural diversity and complexity. For several decades, they have provided the basic foundation for most drugs available to modern medicine. Microbial-derived natural products have wide-ranging applications, especially as chemotherapeutics for various diseases and disorders. By exploring distinct microorganisms in different environments, small novel bioactive molecules with unique functionalities and biological or biomedical significance can be identified. Aquatic environments, such as oceans or seas, are considered to be sources of abundant novel bioactive compounds. Studies on marine microorganisms have revealed that several bioactive compounds extracted from marine algae and invertebrates are eventually generated by their associated bacteria. These findings have prompted intense research interest in discovering novel compounds from marine microorganisms. Natural products derived from Dermacoccus exhibit antibacterial, antitumor, antifungal, antioxidant, antiviral, antiparasitic, and eventually immunosuppressive bioactivities. In this review, we discussed the diversity of secondary metabolites generated by genus Dermacoccus with respect to their chemical structure, biological activity, and origin. This brief review highlights and showcases the pivotal importance of Dermacoccus-derived natural products and sheds light on the potential venues of discovery of new bioactive compounds from marine microorganisms.
    Matched MeSH terms: Anti-Infective Agents/chemistry
  18. Green synthesis of graphene-silver nanocomposites and its application as a potent marine antifouling agent
    Yee MS, Khiew PS, Chiu WS, Tan YF, Kok YY, Leong CO
    Colloids Surf B Biointerfaces, 2016 Dec 01;148:392-401.
    PMID: 27639489 DOI: 10.1016/j.colsurfb.2016.09.011
    Fouling of marine surfaces has been a perpetual problem ever since the days of the early sailors. The tenacious attachment of seaweed and invertebrates to man-made surfaces, notably on ship hulls, has incurred undesirable economic losses. Graphene receives great attention in the materials world for its unique combination of physical and chemical properties. Herein, we present a novel 2-step synthesis method of graphene-silver nanocomposites which bypasses the formation of graphene oxide (GO), and produces silver nanoparticles supported on graphene sheets through a mild hydrothermal reduction process. The graphene-Ag (GAg) nanocomposite combines the antimicrobial property of silver nanoparticles and the unique structure of graphene as a support material, with potent marine antifouling properties. The GAg nanocomposite was composed of micron-scaled graphene flakes with clusters of silver nanoparticles. The silver nanoparticles were estimated to be between 72 and 86nm (SEM observations) while the crystallite size of the silver nanoparticles (AgNPs) was estimated between 1 and 5nm. The nanocomposite also exhibited the SERS effect. GAg was able to inhibit Halomonas pacifica, a model biofilm-causing microbe, from forming biofilms with as little as 1.3wt.% loading of Ag. All GAg samples displayed significant biofilm inhibition property, with the sample recording the highest Ag loading (4.9wt.% Ag) associated with a biofilm inhibition of 99.6%. Moreover, GAg displayed antiproliferative effects on marine microalgae, Dunaliella tertiolecta and Isochrysis sp. and inhibited the growth of the organisms by more than 80% after 96h. The marine antifouling properties of GAg were a synergy of the biocidal AgNPs anchored on the stable yet flexible graphene sheets, providing maximum active contact surface areas to the target organisms.
    Matched MeSH terms: Anti-Infective Agents/chemistry
  19. Nanoencapsulation, an efficient and promising approach to maximize wound healing efficacy of curcumin: A review of new trends and state-of-the-art
    Hussain Z, Thu HE, Ng SF, Khan S, Katas H
    Colloids Surf B Biointerfaces, 2017 Feb 01;150:223-241.
    PMID: 27918967 DOI: 10.1016/j.colsurfb.2016.11.036
    Wound healing is a multifarious and vibrant process of replacing devitalized and damaged cellular structures, leading to restoration of the skin's barrier function, re-establishment of tissue integrity, and maintenance of the internal homeostasis. Curcumin (CUR) and its analogs have gained widespread recognition due to their remarkable anti-inflammatory, anti-infective, anticancer, immunomodulatory, antioxidant, and wound healing activities. However, their pharmaceutical significance is limited due to inherent hydrophobic nature, poor water solubility, low bioavailability, chemical instability, rapid metabolism and short half-life. Owing to their pharmaceutical limitations, newer strategies have been attempted in recent years aiming to mitigate problems related to the effective delivery of curcumanoids and to improve their wound healing potential. These advanced strategies include nanovesicles, polymeric micelles, conventional liposomes and hyalurosomes, nanocomposite hydrogels, electrospun nanofibers, nanohybrid scaffolds, nanoconjugates, nanostructured lipid carriers (NLCs), nanoemulsion, nanodispersion, and polymeric nanoparticles (NPs). The superior wound healing activities achieved after nanoencapsulation of the CUR are attributed to its target-specific delivery, longer retention at the target site, avoiding premature degradation of the encapsulated cargo and the therapeutic superiority of the advanced delivery systems over the conventional delivery. We have critically reviewed the literature and summarize the convincing evidence which explore the pharmaceutical significance and therapeutic feasibility of the advanced delivery systems in improving wound healing activities of the CUR and its analogs.
    Matched MeSH terms: Anti-Infective Agents/chemistry
  20. Study of the antimicrobial activity of cyclic cation-based ionic liquids via experimental and group contribution QSAR model
    Ghanem OB, Shah SN, Lévêque JM, Mutalib MIA, El-Harbawi M, Khan AS, et al.
    Chemosphere, 2018 Mar;195:21-28.
    PMID: 29248749 DOI: 10.1016/j.chemosphere.2017.12.018
    Over the past decades, Ionic liquids (ILs) have gained considerable attention from the scientific community in reason of their versatility and performance in many fields. However, they nowadays remain mainly for laboratory scale use. The main barrier hampering their use in a larger scale is their questionable ecological toxicity. This study investigated the effect of hydrophobic and hydrophilic cyclic cation-based ILs against four pathogenic bacteria that infect humans. For that, cations, either of aromatic character (imidazolium or pyridinium) or of non-aromatic nature, (pyrrolidinium or piperidinium), were selected with different alkyl chain lengths and combined with both hydrophilic and hydrophobic anionic moieties. The results clearly demonstrated that introducing of hydrophobic anion namely bis((trifluoromethyl)sulfonyl)amide, [NTF2] and the elongation of the cations substitutions dramatically affect ILs toxicity behaviour. The established toxicity data [50% effective concentration (EC50)] along with similar endpoint collected from previous work against Aeromonas hydrophila were combined to developed quantitative structure-activity relationship (QSAR) model for toxicity prediction. The model was developed and validated in the light of Organization for Economic Co-operation and Development (OECD) guidelines strategy, producing good correlation coefficient R2 of 0.904 and small mean square error (MSE) of 0.095. The reliability of the QSAR model was further determined using k-fold cross validation.
    Matched MeSH terms: Anti-Infective Agents/chemistry*
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