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1.
Antimicorbial activities of a series of metal derivatives of some sulfa drugs were examined. Such metal derivatives showed higher antimicorbial activity than the parent sulfa drugs, and among the metals, gold derivatives are seen to be the most effective. 相似文献
2.
Karen Bush Joan S. Freudenberger Dorothy S. Slusarchyk R. B. Sykes E. Meyers 《Cellular and molecular life sciences : CMLS》1982,38(4):436-437
Summary Growth ofCandida albicans can be inhibited by sulfa drugs which prevent biosynthesis of folic acid. The dihydrofolate reductase (E.C. 1.5.1.3) inhibitors aminopterin and methotrexate also exhibit anticandidal activity, but trimethoprim does not. Kinetic evaluations withC. albicans dihydrofolate reductase indicate that methotrexate and aminopterin are tight-binding inhibitors whereas trimethoprim binds poorly. 相似文献
3.
With the rapid rise in the emergence of bacterial strains resistant to multiple classes of antimicrobial agents, there is
an urgent need to develop novel antimicrobial therapies to combat these pathogens. Cationic host defence peptides (HDPs) and
synthetic derivatives termed innate defence regulators (IDRs) represent a promising alternative approach in the treatment
of microbial-related diseases. Cationic HDPs (also termed antimicrobial peptides) have emerged from their origins as nature’s
antibiotics and are widely distributed in organisms from insects to plants to mammals and non-mammalian vertebrates. Although
their original and primary function was proposed to be direct antimicrobial activity against bacteria, fungi, parasites and/or
viruses, cationic HDPs are becoming increasingly recognized as multifunctional mediators, with both antimicrobial activity
and diverse immunomodulatory properties. Here we provide an overview of the antimicrobial and immunomodulatory activities
of cationic HDPs, and discuss their potential application as beneficial therapeutics in overcoming infectious diseases. 相似文献
4.
Cathelicidins - a family of multifunctional antimicrobial peptides 总被引:12,自引:0,他引:12
One component of host defence at mucosal surfaces are epithelial-derived antimicrobial peptides. Cathelicidins are one family of antimicrobial peptides characterized by conserved pro-peptide sequences that have been identified in several mammalian species. LL-37/hCAP-18 is the only cathelicidin found in humans and is expressed in inflammatory and epithelial cells. Besides their direct antimicrobial function, cathelicidins have multiple roles as mediators of inflammation influencing diverse processes such as cell proliferation and migration, immune modulation, wound healing, angiogenesis and the release of cytokines and histamine. Finally, cathelicidin antimicrobial peptides qualify as prototypes of innovative drugs that may be used to treat infection and/or modulate the immune response. This review provides an overview of antimicrobial peptides of the cathelicidin family, the structures of their genes and peptides and their biological functions. 相似文献
5.
A. Delitheos S. Kefalas T. Kokkinou D. Varonos 《Cellular and molecular life sciences : CMLS》1982,38(11):1346-1348
Summary Several drugs of various pharmacological classes were tested for antimicrobial activity by the agar diffusion technique and minimal inhibitory concentration (MIC) estimation. Among them diclofenac sodium, haloperidol, meclastine fumarate, chlorpromazine, chlorimipramine and promethazine were the more active. 相似文献
6.
Summary Araplysillins-I and-II, two novel dibromotyrosine derivatives, were isolated fromPsammaplysilla arabica and their structure was elucidated by spectroscopic methods. They proved to be inhibitors of Na+/K+ ATPase and to have antimicrobial activity. 相似文献
7.
The eye and its associated tissues including the lacrimal system and lids have evolved several defence mechanisms to prevent
microbial invasion. Included among this armory are several host-defence peptides. These multifunctional molecules are being
studied not only for their endogenous antimicrobial properties but also for their potential therapeutic effects. Here the
current knowledge of host-defence peptide expression in the eye will be summarised. The role of these peptides in eye disease
will be discussed with the primary focus being on infectious keratitis, inflammatory conditions including dry eye and wound
healing. Finally the potential of using host-defence peptides and their mimetics/derivatives for the treatment and prevention
of eye diseases is addressed. 相似文献
8.
J. W. Faigle H. Stierlin H. Mory T. Winkler H. -P. Kriemler 《Cellular and molecular life sciences : CMLS》1985,41(4):476-478
Summary Indoxyl derivatives were detected as minor products among the urinary metabolites of two trial drugs, a benzodiazepine (GP 55 129) and a benzophenone (CGP 11 952). Their structures were elucidated by NMR and mass spectroscopy. Presumably, metabolites containing potential aldehyde functions react spontaneously with endogenous indoxyl. Such derivatives have not hitherto been encountered in drug metabolism. 相似文献
9.
Indoxyl derivatives were detected as minor products among the urinary metabolites of two trial drugs, a benzodiazepine (GP 55 129) and a benzophenone (CGP 11 952). Their structures were elucidated by NMR and mass spectroscopy. Presumably, metabolites containing potential aldehyde functions react spontaneously with endogenous indoxyl. Such derivatives have not hitherto been encountered in drug metabolism. 相似文献
10.
Proline-rich antimicrobial peptides are a group of cationic host defense peptides of vertebrates and invertebrates characterized
by a high content of proline residues, often associated with arginine residues in repeated motifs. Those isolated from some
mammalian and insect species, although not evolutionarily related, use a similar mechanism to selectively kill Gram-negative
bacteria, with a low toxicity to animals. Unlike other types of antimicrobial peptides, their mode of action does not involve
the lysis of bacterial membranes but entails penetration into susceptible cells, where they then act intracellularly. Some
aspects of the transport system and cytoplasmic targets have been elucidated. These features make them attractive both as
anti-infective lead compounds and as a new class of potential cell-penetrating peptides capable of internalising membrane-impermeant
drugs into both bacterial and eukaryotic cells 相似文献
11.
Mangoni ML 《Cellular and molecular life sciences : CMLS》2011,68(13):2157-2159
Primitive innate defense mechanisms in the form of gene-encoded antimicrobial peptides are now considered as potential candidates
for the development of new therapeutics. They are well known for their function as the first protective barrier of all organisms
against microbial infections. In addition, emerging studies reveal that they assist in modulating the host immune system.
The biological properties of these host-defense peptides, their role in human health, their cell selectivity and related molecular
mechanisms are discussed in this multi-author review along with the strategies to transform them or their peptidomimetics
into clinically usable drugs. 相似文献
12.
P. Zatta 《Cellular and molecular life sciences : CMLS》1976,32(6):693-694
Summary Mono- and oligosaccharide derivatives of dolichol phosphate can be hydrolyzed by heavy metal, preferably Zn++ at 100°C or 65°C. The reactions follow first order kinetics. The reaction proceeds through hydrolysis of the sugar phosphate bond.This work was supported by GB No. 38335. 相似文献
13.
Victor Van Puyenbroeck Kurt Vermeire 《Cellular and molecular life sciences : CMLS》2018,75(9):1541-1558
Proteins routed to the secretory pathway start their journey by being transported across biological membranes, such as the endoplasmic reticulum. The essential nature of this protein translocation process has led to the evolution of several factors that specifically target the translocon and block translocation. In this review, various translocation pathways are discussed together with known inhibitors of translocation. Properties of signal peptide-specific systems are highlighted for the development of new therapeutic and antimicrobial applications, as compounds can target signal peptides from either host cells or pathogens and thereby selectively prevent translocation of those specific proteins. Broad inhibition of translocation is also an interesting target for the development of new anticancer drugs because cancer cells heavily depend on efficient protein translocation into the endoplasmic reticulum to support their fast growth. 相似文献
14.
Amy A. Baxter Fung T. Lay Ivan K. H. Poon Marc Kvansakul Mark D. Hulett 《Cellular and molecular life sciences : CMLS》2017,74(20):3809-3825
There is an ongoing need for effective and targeted cancer treatments that can overcome the detrimental side effects presented by current treatment options. One class of novel anticancer molecules with therapeutic potential currently under investigation are cationic antimicrobial peptides (CAPs). CAPs are small innate immunity peptides found ubiquitously throughout nature that are typically membrane-active against a wide range of pathogenic microbes. A number of CAPs can also target mammalian cells and often display selective activity towards tumor cells, making them attractive candidates as novel anticancer agents warranting further investigation. This current and comprehensive review describes key examples of naturally occurring membrane-targeting CAPs and their modified derivatives that have demonstrated anticancer activity, across multiple species of origin and structural subfamilies. In addition, we address recent advances made in the field and the ongoing challenges faced in translating experimental findings into clinically relevant treatments. 相似文献
15.
B Croizat F Berthelot B Ferrandes P Eymard C Sahuquillo 《Comptes rendus des séances de l'Académie des sciences. Série D, Sciences naturelles》1979,289(16):1283-1286
We describe the induction of neuroblastoma morphological differentiation by 1 methyl cyclohexane carboxylic acid (CCA) and by some C1 derivatives of CCA. This induction proceeds in a medium which allows, in the absence of inducer, a normal growth of neuroblastoma cells and contains 7.5% fetal Calf serum. In order to establish a clear-dose response relationship and to compare the relative potencies of different drugs, the morphological changes were assessed by examining "long neurite-bearing cells". 相似文献
16.
Temporins, anti-infective peptides with expanding properties 总被引:2,自引:1,他引:1
Mangoni ML 《Cellular and molecular life sciences : CMLS》2006,63(9):1060-1069
Antimicrobial peptides are effector molecules of the innate immune response of all pluricellular organisms, providing them
with first-line defence against pathogens. Amphibian skin secretions represent one of the richest natural sources for such
peptide antibiotics, and temporins, a large family of antimicrobial peptides from frog skin, are among the smallest ones found
in nature to date. Their functional role and modes of action have been described, along with their interesting and unique
properties. These properties make temporins good molecules for an in-depth understanding of host defence peptides in general.
Furthermore, they are attractive templates for the future design of new therapeutics against infectious diseases with new
modes of action, urgently needed due to the increasing resistance of microorganisms to the available drugs.
Received 8 November 2005; received after revision 19 December 2005; accepted 18 January 2006 相似文献
17.
Due to the rapid emergence of resistant microbes to the currently available antibiotics, cationic antimicrobial peptides have
attracted considerable interest as a possible new generation of anti-infective compounds. However, low cost development for
therapeutic or industrial purposes requires, among other properties, that the peptides will be small and with simple structure.
Therefore, considerable research has been devoted to optimizing peptide length combined with a simple design. This review
focuses on the similarities and differences in the mode of action and target cell specificity of two families of small peptides:
the naturally occurring temporins from the skin of amphibia and the engineered ultrashort lipopeptides. We will also discuss
the finding that acylation of cationic peptides results in molecules with a more potent spectrum of activity and a higher
resistance to proteolytic degradation. Conjugation of fatty acids to linear native peptide sequences is a powerful strategy
to engineer novel successful anti-infective drugs. 相似文献
18.
(S)-9-(2,3-dihydroxypropyl) adenine (DHPA), D-eritadenine and some other open-chain nucleoside analogues, which exhibit adverse biological effects in microorganisms, plants and animals, cause pronounced inhibition of intestinal phosphatases in the hemipteran insect Pyrrhocoris apterus. The rate of p-nitrophenylphosphate hydrolysis by homogenates from intestinal epithelium and Malpighian tubules was inhibited up to 94% by 2-10 millimolar concentrations of these drugs. This effect is stronger than that of sodium fluoride, which is recognized as a common inhibitor of phosphatase. We conclude that inhibition of phosphatase activity in the digestive and excretory organs may be responsible for the previously reported massive excretion of phosphorylated derivatives of the nucleoside analogues after their oral administration to insects. 相似文献
19.
E. Schraufstätter 《Cellular and molecular life sciences : CMLS》1948,4(12):484-486
Summary Chalcone, flavanone, flavone, and its derivatives had a certain bacteriostatic effect onSt. aureus. Flavonol has no activity and morin, a derivative of flavonol, showed only a weak inhibition of the bacterial growth.Cystein did not have any antagonistic effect.Extracts of drugs, which contain natural flavanones, flavones, isoflavones and flavonols, are more or less bacteriostatic. 相似文献
20.
The short proline-rich antibacterial peptide family 总被引:16,自引:0,他引:16
Otvos L 《Cellular and molecular life sciences : CMLS》2002,59(7):1138-1150
From the many peptide families that are induced upon bacterial infection and can be isolated from all classes of animals,
the short, proline-rich antibacterial peptides enjoy particular interest. These molecules were shown to inactivate an intracellular
biopolymer in bacteria without destroying or remaining attached to the bacterial cell membrane, and as such emerged as viable
candidates for the treatment of mammalian infections. These peptides were originally isolated from insects, they kill mostly
Gram-negative bacteria with high efficiency and they show structural similarities with longer insect- and mammal-derived antimicrobial
peptides. However, while the distant relatives appear to carry multiple functional domains, apidaecin, drosocin, formaecin
and pyrrhocoricin consist of only minimal determinants needed to penetrate across the cell membrane and bind to the target
biopolymer. These peptides appear to inhibit metabolic processes, such as protein synthesis or chaperone-assisted protein
folding. Pyrrhocoricin derivatives protect mice from experimental infections in vivo, suggesting the utility of modified analogs
in the clinical setting. Sequence variations of the target protein at the peptide-binding site may allow the development of
new peptide variants that kill currently unresponsive strains or species.
Received 12 December 2001; received after revision 11 February 2002; accepted 19 February 2002 相似文献