Acridines
Intercalating Agents
Chlorobenzenes
Idoxuridine
Intercalation of proflavine and a platinum derivative of proflavine into double-helical Poly(A). (1/82)
The equilibria and kinetics of the interactions of proflavine (PR) and its platinum-containing derivative [PtCl(tmen)(2)HNC(13)H(7)(NHCH(2)CH(2))(2)](+) (PRPt) with double-stranded poly(A) have been investigated by spectrophotometry and Joule temperature-jump relaxation at ionic strength 0.1 M, 25 degrees C, and pH 5.2. Spectrophotometric measurements indicate that base-dye interactions are prevailing. T-jump experiments with polarized light showed that effects due to field-induced alignment could be neglected. Both of the investigated systems display two relaxation effects. The kinetic features of the reaction are discussed in terms of a two-step series mechanism in which a precursor complex DS(I) is formed in the fast step, which is then converted to a final complex in the slow step. The rate constants of the fast step are k(1) = (2.5 +/- 0.4) x 10(6) M(-1) s(-1), k(-1) = (2.4 +/- 0.1) x 10(3) s(-1) for poly(A)-PR and k(1) = (2.3 +/- 0.1) x 10(6) M(-1) s(-1), k(-1) = (1.6 +/- 0.2) x 10(3) s(-1) for poly(A)-PRPt. The rate constants for the slow step are k(2) = (4.5 +/- 0.5) x 10(2) s(-1), k(-2) = (1.7 +/- 0.1) x 10(2) s(-1) for poly(A)-PR and k(2) = 9.7 +/- 1.2 s(-1), k(-2) = 10.6 +/- 0.2 s(-1) for poly(A)-PRPt. Spectrophotometric measurements yield for the equilibrium constants and site size the values K = (4.5 +/- 0.1) x 10(3) M(-1), n = 1.3 +/- 0.5 for poly(A)-PR and K = (2.9 +/- 0.1) x 10(3) M(-1), n = 2.3 +/- 0.6 for poly(A)-PRPt. The values of k(1) are similar and lower than expected for diffusion-limited reactions. The values of k(-1) are similar as well. It is suggested that the formation of DS(I) involves only the proflavine residues in both systems. In contrast, the values of k(2) and k(-2) in poly(A)-PRPt are much lower than in poly(A)-PR. The results suggest that in the complex DS(II) of poly(A)-PRPt both proflavine and platinum residues are intercalated. In addition, a very slow process was detected and ascribed to the covalent binding of Pt(II) to the adenine. (+info)Low dielectric response in enzyme active site. (2/82)
The kinetics of charge transfer depend crucially on the dielectric reorganization of the medium. In enzymatic reactions that involve charge transfer, atomic dielectric response of the active site and of its surroundings determines the efficiency of the protein as a catalyst. We report direct spectroscopic measurements of the reorganization energy associated with the dielectric response in the active site of alpha-chymotrypsin. A chromophoric inhibitor of the enzyme is used as a spectroscopic probe. We find that water strongly affects the dielectric reorganization in the active site of the enzyme in solution. The reorganization energy of the protein matrix in the vicinity of the active site is similar to that of low-polarity solvents. Surprisingly, water exhibits an anomalously high dielectric response that cannot be described in terms of the dielectric continuum theory. As a result, sequestering the active site from the aqueous environment inside low-dielectric enzyme body dramatically reduces the dielectric reorganization. This reduction is particularly important for controlling the rate of enzymatic reactions. (+info)Specific binding of Hoechst 33258 to site 1 thymidylate synthase mRNA. (3/82)
The translational initiator codon in thymidylate synthetase (TS) mRNA is located in a stem-loop structure with a CC bubble. TS is an important target for anticancer drugs. Aminoglycoside antibiotics have been shown to specifically bind to TS mRNA site 1 constructs and, furthermore, specific binding requires the non-duplex CC bubble region. It is shown here that DNA intercalating agents and DNA minor groove-binding drugs also bind to a TS mRNA site 1 construct. This binding is competitive with aminoglycosides, suggesting that the binding sites overlap. Hoechst 33258 binds with a dissociation constant of 60 nM, a value significantly lower than the approximately 1 microM values found for aminoglycosides. Footprinting and direct binding studies show that the CC bubble is important for binding of the Hoechst compound. However, the exact structure of the bubble is unimportant. Interestingly, mutations in regions adjacent to the bulge also affect binding. These studies point to the important role of non-duplex RNA structures in binding of the DNA minor groove binder Hoechst 33258. (+info)Ozonation of mutagenic and carcinogenic polyaromatic amines and polyaromatic hydrocarbons in water. (4/82)
The Salmonella-microsome assay for mutagenesis was used to determine the effect of ozone on the mutagenesis of selected carcinogens and mutagens in water. Short periods of ozonation were shown to completely inactivate the mutagenicity of several polyaromatic amine mutagens including acriflavine, proflavine, and beta-naphthylamine. Selected polyaromatic hydrocarbons were also sensitive to ozonation. Kinetic studies revealed that the mutagenicity of benzo(a)pyrene, 3-methylcholanthrene, and 7,12-dimethylbenz(a)anthracene was destroyed after short periods of ozonation. To correlate loss of mutagenicity with loss of carcinogenicity, two polyaromatic hydrocarbons were treated with ozone, extracted from water with hexane, and tested for carcinogenicity in mice. When 7,12-dimethyl-benz(a)anthracene and 3-methyl-cholanthrene were treated with ozone, there was a substantial reduction in carcinogenicity compared to control groups treated with oxygen alone. However, a small number of tumors developed in the group of animals receiving a hexane extract of ozonated 7,12-dimethylbenz(a)anthracene. This activity may be due to breakdown products of 7,12-dimethylbenz(a)anthracene that are not mutagenic. (+info)Comparison of the treatment of herpes genitalis in men with proflavine photoinactivation, idoxuridine ointment, and normal saline. (5/82)
36 male patients with genital infection by HSV confirmed by culture were each allocated to one of three treatment groups: (1) Proflavine photoinactivation, (2) 0.5 per cent. idoxuridine ointment (IDU), (3) Normal saline. They were assessed objectively at each attendance by measurement of the lesions with an operating microscope fitted with a measuring grid in one eyepiece. Material for culture for HSV was taken at each visit; the presence of symptoms (pain, discomfort, and irritation) was noted. The areas of lesions in the proflavine photoinactivation group remained larger significantly longer than in the other groups, the healing time was slower, and HSV could be isolated for longer. It is concluded that proflavine photoinactivation is of no greater value than 0.5 per cent. IDU or normal saline in the treatment of genital infection by HSV in the male. (+info)Effect of DNA delay mutations of bacteriophage T4 on genetic recombination. (6/82)
Studies have been made of the effect of the DNA delay mutations of bacteriophage T4 on growth and genetic recombination in a number of Escherichia coli hosts. DNA delay mutations in genes 39, 52, 58 (61), and 60 result in abnormally high recombination frequencies. These high recombination frequencies are discussed in the context of other observations. (+info)Intrinsic and extrinsic light responses of Salmonella typhimurium and Escherichia coli. (7/82)
Exposure to intense light in the region between 390 and 530 nm has been shown to have three effects on the motility of Salmonella typhimurium and Escherichia coli. Short pulses of light initiate continuous tumbling. Longer exposures to light induce smooth swimming, and prolonged exposures induced paralysis. The tumbling response is intimately connected with the chemical gradient-sensing apparatus of the bacterium and can be overcome by strong temporal gradients of attractant. Some mutants of S. typhimurium which are defective in the tumble-generating mechanism for chemotaxis are also unable to tumble in intense light. This intrinsic light effect can be mimicked by the addition of external dyes (the classical photodynamic effect), but it can be shown that the two phenomena are distinct. The extrinsic (photodynamic) effect can be inhibited by histidine or by anaerobic conditions, whereas the intrinsic effect is not. The observation that the extrinsic effect can also produce the three types of light responses listed above suggests a common pathway after an intial event on either an endogenous or an externally added photoreceptor. (+info)Effect of acriflavin on the kinetoplast of Leishmania tarentolae. Mode of action and physiological correlates of the loss of kinetoplast DNA. (8/82)
The loss of kinetoplast DNA in Leishmania tarentolae, which occurs in the presence of low concentrations of acriflavin, was found to be a result of selective inhibition of replication of this DNA. Nuclear DNA synthesis was relatively unaffected and cell and kinetoplast division proceeded normally for several generations. An approximately equal distribution of parental kinetoplast DNA between daughter kinetoplasts resulted in a decrease in the average amount of DNA per kinetoplast. The final disappearance of the stainable kinetoplast DNA occurred at a cell division in which all the remaining visible kinetoplast DNA was retained by one of the daughter cells. The selective inhibition of kinetoplast DNA synthesis was caused by a selective localization of acriflavin in the kinetoplast. The apparent intracellular localization of dye and the extent of uptake at a low dye concentration could be manipulated, respectively, by varying the hemin (or protoporphyrin IX) concentration in the medium and by adding red blood cell extract (or hemoglobin). Hemin and protoporphyrin IX were found to form a complex with acriflavin. During growth in acriflavin, cells exhibited an increasing impairment of colony-forming ability and rate of respiration. No change in the electrophoretic pattern of total cell soluble proteins was apparent. The data fit the working hypothesis that the loss of kinetoplast DNA leads to a respiratory defect which then leads to a decrease in biosynthetic reactions and eventual cell death. A possible use of the selective localization of acriflavin in the kinetoplast to photooxidize selectively the kinetoplast DNA is suggested. (+info)Proflavine is an antimicrobial agent, specifically a type of dye known as an acridine dye. It is used primarily as a topical antiseptic and disinfectant. Proflavine works by intercalating into DNA, which disrupts the structure of the DNA molecule and prevents bacterial replication.
It's important to note that proflavine has been largely replaced by other more effective and safer antimicrobial agents in clinical practice. It is still used in some research settings and for certain specific applications, such as staining tissues for microscopic examination.
Proflavine should be used with caution, as it can cause skin irritation and may have harmful effects if ingested or absorbed through the skin. As with any medication, it should only be used under the guidance of a healthcare professional.
Acridines are a class of heterocyclic aromatic organic compounds that contain a nucleus of three fused benzene rings and a nitrogen atom. They have a wide range of applications, including in the development of chemotherapeutic agents for the treatment of cancer and antibacterial, antifungal, and antiparasitic drugs. Some acridines also exhibit fluorescent properties and are used in research and diagnostic applications.
In medicine, some acridine derivatives have been found to intercalate with DNA, disrupting its structure and function, which can lead to the death of cancer cells. For example, the acridine derivative proflavin has been used as an antiseptic and in the treatment of certain types of cancer. However, many acridines also have toxic side effects, limiting their clinical use.
It is important to note that while acridines have potential therapeutic uses, they should only be used under the supervision of a qualified healthcare professional, as they can cause harm if not used properly.
Intercalating agents are chemical substances that can be inserted between the stacked bases of DNA, creating a separation or "intercalation" of the base pairs. This property is often exploited in cancer chemotherapy, where intercalating agents like doxorubicin and daunorubicin are used to inhibit the replication and transcription of cancer cells by preventing the normal functioning of their DNA. However, these agents can also have toxic effects on normal cells, particularly those that divide rapidly, such as bone marrow and gut epithelial cells. Therefore, their use must be carefully monitored and balanced against their therapeutic benefits.
Chlorobenzenes are a group of chemical compounds that consist of a benzene ring (a cyclic structure with six carbon atoms in a hexagonal arrangement) substituted with one or more chlorine atoms. They have the general formula C6H5Clx, where x represents the number of chlorine atoms attached to the benzene ring.
Chlorobenzenes are widely used as industrial solvents, fumigants, and intermediates in the production of other chemicals. Some common examples of chlorobenzenes include monochlorobenzene (C6H5Cl), dichlorobenzenes (C6H4Cl2), trichlorobenzenes (C6H3Cl3), and tetrachlorobenzenes (C6H2Cl4).
Exposure to chlorobenzenes can occur through inhalation, skin contact, or ingestion. They are known to be toxic and can cause a range of health effects, including irritation of the eyes, skin, and respiratory tract, headaches, dizziness, nausea, and vomiting. Long-term exposure has been linked to liver and kidney damage, neurological effects, and an increased risk of cancer.
It is important to handle chlorobenzenes with care and follow appropriate safety precautions to minimize exposure. If you suspect that you have been exposed to chlorobenzenes, seek medical attention immediately.
'Diamines' are organic compounds containing two amino groups (-NH2) in their molecular structure. The term 'diamine' itself does not have a specific medical definition, but it is used in the context of chemistry and biochemistry.
Diamines can be classified based on the number of carbon atoms between the two amino groups. For example, ethylenediamine and propylenediamine are diamines with one and two methylene (-CH2-) groups, respectively.
In medicine, certain diamines may have biological significance. For instance, putrescine and cadaverine are polyamines that are produced during the decomposition of animal tissues and can be found in necrotic or infected tissues. These compounds have been implicated in various pathological processes, including inflammation, oxidative stress, and cancer progression.
It is important to note that while some diamines may have medical relevance, the term 'diamines' itself does not have a specific medical definition.
Idoxuridine is an antiviral medication used primarily for the treatment of herpes simplex virus (HSV) infections of the eye, such as keratitis or dendritic ulcers. It works by interfering with the DNA replication of the virus, thereby inhibiting its ability to multiply and spread.
Idoxuridine is available as an ophthalmic solution (eye drops) and is typically applied directly to the affected eye every 1-2 hours while awake, for up to 2 weeks. Common side effects include local irritation, stinging, or burning upon application. Prolonged use of idoxuridine may lead to bacterial resistance or corneal toxicity, so it is important to follow your healthcare provider's instructions carefully when using this medication.
It is essential to note that idoxuridine is not commonly used today due to the development of more effective and less toxic antiviral agents for HSV infections.
Acriflavine is an antiseptic and disinfectant substance that has been used in dermatology and veterinary medicine. Its chemical name is trypaflavine, and it is a mixture of basic dyes with the ability to interact with DNA, RNA, and proteins. Acriflavine has shown antibacterial, antifungal, and antiviral properties, although its use in human medicine has been limited due to its potential toxicity and staining effects on tissues. It is still used in some topical preparations for the treatment of skin conditions such as psoriasis and eczema.
Proflavine
Acriflavine
Acridine
Leonard Lerman
Intercalation (biochemistry)
Paramasivam Natarajan
Mutagenesis
Microscopy with UV surface excitation
Sharmila Anandasabapathy
Rev (HIV)
Pillararene
Triple dye
List of MeSH codes (D03)
Mutagen
List of drugs: Pro-Prz
IARC group 3
Proflavine - Wikipedia
Site du DCM - Université Grenoble Alpes - Proflavine derivatives as fluorescent imaging agents of amyloid deposits.
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Acridine orange2
- hototoxicity against one or more of the test organisms, but the established photosensitizing acridines proflavine and acridine orange were photobactericidal against all strains. (archive.org)
- The dihedral angle of the MB pairs, corresponding to a left-handed helix, is opposite to that with acridine orange and proflavine on DNA, indicating that the latter ligands bind to DNA in a different way. (ac.ir)
Antiseptic1
- Proflavine is an antiseptic dye used to stop the growth of certain bacteria at the site of the wound. (icmpharma.com)
Acriflavine1
- Proflavine, also called proflavin and diaminoacridine, is an acriflavine derivative, a disinfectant bacteriostatic against many gram-positive bacteria. (wikipedia.org)
Blue1
- Proflavine absorbs strongly in the blue region at 445 nm (in water at pH 7) with molar extinction coefficient of c. 40,000. (wikipedia.org)
Acridine5
- The mutants studied were acridine mutants, meaning they had been exposed to the potent mutagen proflavine, a bright yellow dye derived from the coal tar chemical acridine. (nih.gov)
- Proflavine is a synthetic acridine dye which early in this century was found to have bacteriostatic and bacteriocidal properties when administered topically. (nih.gov)
- Two acridine dyes, proflavine (PF, 2:8-diamino- acridine), and acridine orange (AO, 2:8-b¢sDimethylaminoacridine) were used. (nih.gov)
- Proflavine hemi sulphate is the hemi sulphate salt of proflavine, an acridine-based fluorescence contrast agent and disinfectant. (angrytails.com)
- Proflavine is an acridine-based fluorescence contrast agent and disinfectant. (angrytails.com)
HEMISULFATE2
- Proflavine hemisulfate is the hemisulfate salt of it. (angrytails.com)
- When proflavine hemisulfate is applied to the skin, it enters cells and "intercalates" into DNA. (angrytails.com)
Acriflavine derivative1
- Proflavine, also called proflavin and diaminoacridine, is an acriflavine derivative, a disinfectant bacteriostatic against many gram-positive bacteria. (wikipedia.org)
Monohydrochloride1
- A bioassay of the carcinogenicity of proflavine monohydrochloride hemihydrate was conducted using Fischer 344/CR rats and B6C3F1 mice. (nih.gov)
Agents1
- Proflavine derivatives as fluorescent imaging agents of amyloid deposits. (univ-grenoble-alpes.fr)