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1.
Int J Mol Sci ; 24(8)2023 Apr 21.
Article in English | MEDLINE | ID: mdl-37108827

ABSTRACT

Sustained interest in the use of renewable resources for the production of medical materials has stimulated research on bacterial cellulose (BC) and nanocomposites based on it. New Ag-containing nanocomposites were obtained by modifying various forms of BC with Ag nanoparticles prepared by metal-vapor synthesis (MVS). Bacterial cellulose was obtained in the form of films (BCF) and spherical BC beads (SBCB) by the Gluconacetobacter hansenii GH-1/2008 strain under static and dynamic conditions. The Ag nanoparticles synthesized in 2-propanol were incorporated into the polymer matrix using metal-containing organosol. MVS is based on the interaction of extremely reactive atomic metals formed by evaporation in vacuum at a pressure of 10-2 Pa with organic substances during their co-condensation on the cooled walls of a reaction vessel. The composition, structure, and electronic state of the metal in the materials were characterized by transmission and scanning electron microscopy (TEM, SEM), powder X-ray diffraction (XRD), small-angle X-ray scattering (SAXS) and X-ray photoelectron spectroscopy (XPS). Since antimicrobial activity is largely determined by the surface composition, much attention was paid to studying its properties by XPS, a surface-sensitive method, at a sampling depth about 10 nm. C 1s and O 1s spectra were analyzed self-consistently. XPS C 1s spectra of the original and Ag-containing celluloses showed an increase in the intensity of the C-C/C-H groups in the latter, which are associated with carbon shell surrounding metal in Ag nanoparticles (Ag NPs). The size effect observed in Ag 3d spectra evidenced on a large proportion of silver nanoparticles with a size of less than 3 nm in the near-surface region. Ag NPs in the BC films and spherical beads were mainly in the zerovalent state. BC-based nanocomposites with Ag nanoparticles exhibited antimicrobial activity against Bacillus subtilis, Staphylococcus aureus, Escherichia coli bacteria and Candida albicans and Aspergillus niger fungi. It was found that AgNPs/SBCB nanocomposites are more active than Ag NPs/BCF samples, especially against Candida albicans and Aspergillus niger fungi. These results increase the possibility of their medical application.


Subject(s)
Anti-Infective Agents , Metal Nanoparticles , Silver/pharmacology , Silver/chemistry , Metal Nanoparticles/chemistry , Cellulose/chemistry , Scattering, Small Angle , X-Ray Diffraction , Anti-Infective Agents/chemistry , Bacteria , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Microbial Sensitivity Tests , Spectroscopy, Fourier Transform Infrared
2.
Chem Biodivers ; 18(5): e2001050, 2021 May.
Article in English | MEDLINE | ID: mdl-33719150

ABSTRACT

Scaevola spinescens is endemic to Australia and has traditionally been used by Aboriginal and Torres Strait Islander communities to treat a variety of conditions including colds, flu, fever, stomach pain, urinary disorders, sores, tinea, leprosy, and cancer. Extracts prepared from S. spinescens are non-toxic and have been linked with various medicinal properties including antiviral, antibacterial, anti-inflammatory, and anticancer activities. These studies support the ethnopharmacological use of S. spinescens by Indigenous peoples of Australia and highlight the need for further investigations on the plant for potential use in pharmaceutical and food applications. This review provides a comprehensive, up-to-date review of the literature on S. spinescens focusing on the traditional use, medicinal properties, phytochemicals, and factors that affect their composition during pre-treatment and extraction, as well as providing a framework for future studies of the plant.


Subject(s)
Anti-Infective Agents/pharmacology , Anti-Inflammatory Agents/pharmacology , Antineoplastic Agents, Phytogenic/pharmacology , Magnoliopsida/chemistry , Phytochemicals/pharmacology , Anti-Infective Agents/chemistry , Anti-Infective Agents/isolation & purification , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/isolation & purification , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/isolation & purification , Australia , Ethnopharmacology , Phytochemicals/chemistry , Phytochemicals/isolation & purification
4.
Nucleic Acids Res ; 46(D1): D413-D418, 2018 01 04.
Article in English | MEDLINE | ID: mdl-29106651

ABSTRACT

Available genomic data for pathogens has created new opportunities for drug discovery and development to fight them, including new resistant and multiresistant strains. In particular structural data must be integrated with both, gene information and experimental results. In this sense, there is a lack of an online resource that allows genome wide-based data consolidation from diverse sources together with thorough bioinformatic analysis that allows easy filtering and scoring for fast target selection for drug discovery. Here, we present Target-Pathogen database (http://target.sbg.qb.fcen.uba.ar/patho), designed and developed as an online resource that allows the integration and weighting of protein information such as: function, metabolic role, off-targeting, structural properties including druggability, essentiality and omic experiments, to facilitate the identification and prioritization of candidate drug targets in pathogens. We include in the database 10 genomes of some of the most relevant microorganisms for human health (Mycobacterium tuberculosis, Mycobacterium leprae, Klebsiella pneumoniae, Plasmodium vivax, Toxoplasma gondii, Leishmania major, Wolbachia bancrofti, Trypanosoma brucei, Shigella dysenteriae and Schistosoma Smanosoni) and show its applicability. New genomes can be uploaded upon request.


Subject(s)
Anti-Infective Agents/chemistry , Computational Biology/methods , Databases, Factual , Genome, Bacterial , Genome, Fungal , Genome, Helminth , Genome, Protozoan , Amino Acid Sequence , Anti-Infective Agents/pharmacology , Binding Sites , Communicable Diseases/drug therapy , Drug Discovery , Humans , Internet , Metabolic Networks and Pathways/drug effects , Metabolic Networks and Pathways/genetics , Models, Molecular , Molecular Targeted Therapy , Protein Binding , Protein Conformation, alpha-Helical , Protein Conformation, beta-Strand , Protein Interaction Domains and Motifs , Sequence Alignment , Sequence Homology, Amino Acid , Software
5.
Phytother Res ; 27(6): 791-801, 2013 Jun.
Article in English | MEDLINE | ID: mdl-22887725

ABSTRACT

The root of Hemidesmus indicus R. Br., commonly known as Indian Sarsaparilla, is used traditionally to treat a wide variety of illnesses including rheumatism, leprosy, impotence, urinary tract and skin infections. The anticancer, antioxidant, anti-inflammatory, antipyretic, analgesic, antimicrobial, antidiabetic, hepatoprotective, cardioprotective, renoprotective, neuroprotective and immunomodulatory properties of H. indicus have been investigated in numerous in vivo and in vitro studies. Among these, the antioxidant and antimicrobial activity was well documented. This review details the phytochemistry and therapeutic applications of H. indicus root.


Subject(s)
Hemidesmus/chemistry , Plant Extracts/pharmacology , Animals , Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Antioxidants/chemistry , Antioxidants/pharmacology , Cells, Cultured , Humans , Phytotherapy , Plant Extracts/chemistry , Plant Roots/chemistry
6.
Int J Nanomedicine ; 7: 5175-82, 2012.
Article in English | MEDLINE | ID: mdl-23055729

ABSTRACT

BACKGROUND: Dapsone is described as being active against Mycobacterium leprae, hence its role in the treatment of leprosy and related pathologies. Despite its therapeutic potential, the low solubility of dapsone in water results in low bioavailability and high microbial resistance. Nanoemulsions are pharmaceutical delivery systems derived from micellar solutions with a good capacity for improving absorption. The aim of this work was to develop and compare the permeability of a series of dapsone nanoemulsions in Caco-2 cell culture against that of effective permeability in the human body simulated using Gastroplus™ software. METHODS AND RESULTS: The release profiles of the dapsone nanoemulsions using different combinations of surfactants and cosolvent showed a higher dissolution rate in simulated gastric and enteric fluid than did the dispersed dapsone powder. The drug release kinetics were consistent with a Higuchi model. CONCLUSION: This comparison of dapsone permeability in Caco-2 cells with effective permeability in the human body simulated by Gastroplus showed a good correlation and indicates potential improvement in the biodisponibility of dapsone using this new system.


Subject(s)
Dapsone/administration & dosage , Dapsone/pharmacokinetics , Models, Biological , Models, Chemical , Nanocapsules/chemistry , Administration, Oral , Anti-Infective Agents/administration & dosage , Anti-Infective Agents/chemistry , Biological Availability , Caco-2 Cells , Computer Simulation , Dapsone/chemistry , Diffusion , Emulsions/chemistry , Humans , Nanocapsules/ultrastructure , Particle Size , Permeability
7.
Pharm Biol ; 48(9): 1007-11, 2010 Sep.
Article in English | MEDLINE | ID: mdl-20731552

ABSTRACT

CONTEXT: The roots of Plumbago zeylanica Linn. (Plumbaginaceae) are reputed to have a wide spectrum of therapeutic properties in the Ayurvedic system of medicine. They are useful in curing many ailments such as skin diseases, diarrhea, plague and leprosy. OBJECTIVE: The study was aimed at isolating, separating and evaluating the antimicrobial properties of compounds such as neoisoshinanolone and 1-epineo-isoshinanolone from the roots of P. zeylanica. MATERIALS AND METHODS: The crude petroleum ether extract of roots of P. zeylanica was subjected to repeated chromatographic techniques to separate compounds 2 and 3 along with plumbagin. Structure elucidation was carried out using nuclear magnetic resonance (NMR), infra red (IR) and mass spectroscopy. The serial dilution method was used to test antimicrobial activities and their minimum inhibitory concentration (MIC) expressed in microg/mL. RESULTS: 1-Epineo-isoshinanolone is more active with a MIC of 12.5-25 microg/mL whereas neoisoshinanolone has recorded a MIC of 50-100 microg/mL. The activities are compared with plumbagin (0.78-3.13 microg/mL) and standards streptomycin for bacteria and nystatin for fungi. DISCUSSION: Earlier researchers have established the presence of plumbagin in the roots of P. zeylanica and its antimicrobial activities. The structure elucidation of two more biologically active biogenetic precursors along with their activities in the root extracts has been established for the first time in the present study. CONCLUSION: The root extract of P. zeylanica possesses good antimicrobial activity, which suggests its therapeutic use in the Ayurvedic system of medicine to cure skin diseases.


Subject(s)
Anti-Infective Agents/pharmacology , Drug Discovery , Plant Roots/chemistry , Plumbaginaceae/chemistry , Tetrahydronaphthalenes/pharmacology , Anti-Infective Agents/chemistry , Anti-Infective Agents/isolation & purification , Fungi/drug effects , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effects , Isomerism , Magnetic Resonance Spectroscopy , Mass Spectrometry , Medicine, Ayurvedic , Microbial Sensitivity Tests , Molecular Structure , Naphthoquinones/chemistry , Naphthoquinones/isolation & purification , Naphthoquinones/pharmacology , Plant Extracts/chemistry , Spectrophotometry, Infrared , Tetrahydronaphthalenes/chemistry , Tetrahydronaphthalenes/isolation & purification , Transition Temperature
8.
Dermatol Clin ; 28(3): 599-610, 2010 Jul.
Article in English | MEDLINE | ID: mdl-20510768

ABSTRACT

After synthesis of dapsone (4,4' diaminodiphenylsulfone) in 1908, the compound was known exclusively in chemistry. Following the epoch-making discovery of the antimicrobial potential for sulfonamides emerged, the sulfone class was included in the medical armamentarium. The therapeutic role of sulfones related to both pathogen-caused diseases and chronic inflammatory dermatoses has led to extensive use in dermatology. At present dapsone is the only sulfone congener available for clinical practice. The sulfone is used in rifampin-based multiple-drug regiments to treat multibacillary and paucibacillary leprosy and to treat Pneumocystis jiroveci pneumonia and prevent toxoplasmosis in individuals with AIDS. In dermatology, dapsone is the preferred drug for treating dermatitis herpetiformis (Duhring's disease) and is useful in the management of a broad range of chronic inflammatory entities, especially autoimmune bullous disorders. With proper administration and monitoring, the sulfone should be considered a useful and safe agent.


Subject(s)
Anti-Infective Agents/therapeutic use , Dapsone/therapeutic use , Skin Diseases/drug therapy , Therapies, Investigational , Adult , Anti-Infective Agents/adverse effects , Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Autoimmune Diseases/drug therapy , Child , Dapsone/adverse effects , Dapsone/chemistry , Dapsone/pharmacology , Humans , Hypersensitivity/etiology , Jaundice/chemically induced , Leprosy/drug therapy , Orphan Drug Production , Peripheral Nervous System Diseases/chemically induced , Pneumocystis carinii/drug effects , Pneumonia, Pneumocystis/drug therapy , Toxoplasmosis/drug therapy
9.
Eur J Med Chem ; 44(3): 1093-9, 2009 Mar.
Article in English | MEDLINE | ID: mdl-18657884

ABSTRACT

Several families of water soluble dendrimers were synthesized based on poly(propyleneoxide) amines (Jeffamines) (P(1)). P(1)-core and branched units were constructed from both methylacrylate and ethylenediamine (P(2)-P(9), and generations 0-3 with -NH(2), -COOH functionalities). They were characterized by elemental analysis (EA), gel permeation chromatography (GPC), FT-IR, (1)H, and (13)C NMR. The antimicrobial activities of only water soluble compounds (P(1), P(3), P(4), P(6), P(7) and P(9)) were evaluated using disk diffusion method in water as well as the minimal inhibitory concentration (MIC) dilution method against 9 bacteria. The obtained results from disk diffusion method are assessed in side-by-side comparison with those of Penicillin-g, Ampicillin, Cefotaxime, Vancomycin, Oflaxacin, and Tetracycline, well-known antibacterial agents. The results from dilution procedure are compared with Gentamycin as antibacterial and Nystatin as antifungal. The antifungal activities are reported on five yeast cultures namely, Candida albicans, Kluyveromyces fragilis, Rhodotorula rubra, Debaryomyces hansenii, and Hanseniaspora guilliermondii, and the results are referenced with Nystatin, Ketaconazole, and Clotrimazole, commercial antifungal agents. In most cases, the compounds show broad-spectrum (gram-positive and gram-negative bacteria) activities that are comparatively higher or equipotent to the antibiotic and antifungal agents in the comparison tests.


Subject(s)
Anti-Infective Agents/chemical synthesis , Anti-Infective Agents/pharmacology , Anti-Infective Agents/chemistry , Chromatography, Gel , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests , Solubility , Spectroscopy, Fourier Transform Infrared , Water/chemistry
10.
s.l; s.n; 2003. 10 p. graf.
Non-conventional in English | Sec. Est. Saúde SP, HANSEN, Hanseníase Leprosy, SESSP-ILSLACERVO, Sec. Est. Saúde SP | ID: biblio-1241159

ABSTRACT

Clofazimine, a water insoluble substituted iminophenazine derivative with anti-mycobacterial and anti-inflammatory activity, is recommended by the WHO for the treatment of leprosy. It is also active against disseminated Mycobacterium avium complex (MAC) disease in HIV-infected patients. Recently, we achieved a 4000-fold increase of clofazimine water solubility using a novel modified clofazimine-cyclodextrin complex synthesized and patented by our group [Wasserlösliche, Iminiophenazinderivate enthaltende pharmazeutische Zusammensetzungen, deren Herstellung und Verwendung, German Patent, DE19814814C2]. In this paper we examine the activity of this complex against MAC in human macrophages, and evaluate its cytotoxicity. MAC-infected macrophages were treated for 24h with free or complexed clofazimine. The in vitro minimum inhibitory concentrations of both free and complexed clofazimine were 0.1 microg/ml. Free and complexed clofazimine inhibited the growth of MAC inside macrophages to a similar extent, while modified cyclodextrin alone had no observable effects on MAC or macrophages. Complexed clofazimine was not toxic to cells at concentrations effective against MAC. The TD(50) of the modified cyclodextrin in THP-1 cell line was 297 microg/ml.


Subject(s)
Humans , Animals , Mice , Anti-Infective Agents/pharmacology , Anti-Infective Agents/chemistry , Anti-Infective Agents/toxicity , Clofazimine/pharmacology , Clofazimine/chemistry , Clofazimine/toxicity , Mycobacterium avium Complex , Cells, Cultured , Sterols/chemistry , Macrophages , Macrophages/microbiology , Microbial Sensitivity Tests , Succinic Acid/chemistry
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