Background: Leishmaniasis is a complex protozoan disease comprises a wide range of clinical manifestations that is usually divided into visceral leishmaniasis, cutaneous leishmaniasis, and muco-cutaneous leishmaniasis depending on leishmania parasite strains and host's immune system responses. Most of the drugs produced for the treatment of leishmanial, from the first used (Glucantime and pentostam) to the lately accepted (miltefosine), are toxic, resistance issues and poorly tolerated. The purpose of this In Silico and In vitro study is evaluating the effectiveness of some novel experimental biurets and Glucantime against Leishmania tropica promastigotes.
Materials and methods: In general, eight experimental biuret compounds and glucantime (reference drug) were docked into the active sites of L. tropica pteridine reductase 1, using AutoDock 4.3 software which was modeled by homology modeling programs. promastigote stages of L. tropica (MHOM/IR/02/Mash10) were transferred to RPMI-1640medium, supplemented with 10% FCS and antibiotics then grown at 25±2°C. We used MTT assay to find viability of L. tropica promastigotes at wide range concentrations of biuret compounds and the achieved results were explicated as 50 and 90 percent of inhibitory concentration (IC50 and IC90). All experiments were performed in triplicate.
Results: In Silico Procedure shown that from the eight selected experimental biurets, four ligands showed highly active on PTR1. K8 and K3 were the most active against L. tropica promastigote with IC50s of 1.23 μM and 3.1 μM after 72 h respectively .The K6 showed less toxicity with IC50 more than 60μM. Glucantime displayed less growth inhibition with IC50 of 45.65μM.
Conclusion: In silico consequences in present st...
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...rated the most antileishmanial activity against Leishmania tropica (MHOM/IR/02/Mash10) promastigotes in vitro with IC50s of 14.67 µM and 17.21 µM after 48 h 3.1 µM and 1.23 µM after 72h respectively and is thinkable in comparison with miltefosin with IC50 of 11 µM against this leishmania strain by using MTT assay evaluation after 48 h of incubation that was performed by Khademvatan et al previously . Replacement of the phenyl, benzo[d]thiazol-2-ylthiopropyl with 2-methylquinoline-4-yl (compounds K1 and K6) reduced the activity. In this report, the results demonstrated that with an increase in concentration of biurets or glucantime, the promastigote killing and inhibitory effect on the growth of Leishmania tropica promastigotes will be increased and the optical density (OD) that has a direct correlatation with the number of viable promastigotes will be decreased.
Prodigiosin can formulate into a biopigment, henceforth contribute to the production of important medicinal materials. It is a highly desirable molecule, as of its characteristic traits being; antibacterial, antimycotic, antimalarial, antitumour and also immunosuppressant. (Prad...
The cationic surfactant molecules obtained from Mannich bases possess excellent fungicidal property along with good biocidal property against Gram-positive
Plenty of fungal problems exist, including athlete’s foot, jock itch, ringworm, and onychomycosis (fungal infection beneath nails). However, many antifungal drugs exist as well, such as Lamisil, which is the most effective. Using the molecule terbinafine hydrochloride, it puts holes in the cell membranes of fungal cells, and can destroy fungi. Despite this, Lamisil has many problems such as harmful side effects, and a high cost, and can therefore be vastly improved. Some of Lamisil’s competitors, such as Tinactin, offer a similar medication for a cheaper price, and other analogs of the drug could prove to be safer and even more effective. For now though, Lamisil, the 87th best selling prescription drug in the world, is the best antifungal medication1.
Rogers, D. H.; Morris, J. C.; Roden, F. S.; Frey, B.; King, G. R.; Russkamp, F. W.; Bell, R. A.; Mander, L. N. Pure Appl. Chem., 1996, 68, 515.
Subissi et. al (2010), stated that the mechanism of action of ciclopirox is varied from other topical anti fungal that act through ergosterol inhibition. This unique and the level mechanism of action has give a very low potential for the resistance development in pathogenic fungi.
...Coauthor, ChemBioChem 2006, 7, 1-10; b) A. Author, B. Coauthor, Angew. Chem. 2006, 118, 1-5; Angew. Chem. Int. Ed. 2006, 45, 1-5.))
Malaria kills more people than any communicable disease except for tuberculosis. It is caused by four species of parasitic protozoa that infect human red blood cells. Four different types of these protozoa are known: protozoa falciparum, protozoa vivax, protozoa ovale, and protozoa malariae. Protozoa falciparum is the most lethal of the four and accounts for the majority of infections. Malaria parasites are not able to survive unless they have both a mosquito and human host, however the disease cannot be hosted by any kind of mosquito, only those of the genus "anopheles".
Compounding all of these solutions, the pharmaceutical industry needs to conduct extensive research on developing new antibiotics for various pathogenic bacteria by studying the bacterial structure. This will help scientists to formulate ways of counteracting the functions of the various constituents of bacteria.
Infectious diseases represent an important cause of morbidity and mortality among the general population, particularly in developing countries. Therefore, pharmaceutical companies have been motivated to develop new antimicrobial drugs in recent years, especially due to the constant emergence of microorganisms resistant to conventional antimicrobials (Silva et al., 2010).
In the movie Beetlejuice, the theme is that the afterlife is not really the end for us all; we live on a multiple level world between life and death, and need to respect the dead. The theme is idealistic and not applicable in real life to all people. Throughout the movie, Burton reveals his take on the living and life after death and the delicate interaction between the two. The character Otho, played by Glenn Shadix is key to Burton’s interpretation and scrutiny of the afterlife. Throughout the film Otho makes comments about the dead and even goes as far to steal The Handbook for the Recently Deceased. Otho comments on those who commit suicide and how they become civil servant s in the afterlife. Barbra and Adam Maitland, played by Geena Davis and Alec Baldwin are used as guides for the audience into the process of the afterlife and give a unique Ghost’s perspective on the process.
Malaria in humans is caused by four species of protozoa, sophisticated one-celled organisms, that can infect red blood cells. These four species are called Plasmodium falciparum, plasmodium vivax, plasmodium malariae, and plasmodium ovale. The worst cases are caused by the Plasmodium falciparum species, which is also the species with the most resistance to drugs. To contract malaria, a mosquito, but not just any mosquito must bite a human. The only type of mosquito that can infect humans with the malaria virus is the Anopheles mosquito. While there are...
Penicillin works by virtue of its beta-lactam ring that specifically binds to microbial enzymes in bacterial cell walls, and keeps the cell membrane structures from linking up. Eventually, if the bacterium keeps dividing, the cell membrane will become increasingly weaker and lyse. The beta-lactam ring is very simple in and of itself, but its ability to remain potent with several different functional groups attached to it makes it spectacular in its applications.
One of the greatest achievements in the 20th century was the invention and mass production of antibiotics. Antibiotics or antimicrobials are chemical drugs that are used to treat a variety of different infectious bacterial diseases by destroying or slowing the growth of the bacteria. Antibiotics are toxic to the target cell but do not harm the host. They are designed to attack various kinds of parasites, fungus, and bacteria. Contrary to popular belief antibiotics do not work against viruses like those that cause the common cold. Antibiotics are broken down into different classifications because antibiotics are selective killers, which mean that it has been manufactured to kill a certain malicious bacteria strain. Each antimicrobial differs from one another by their physical and chemical properties and by their antibacterial spectrum of activity. The different kinds of antibiotics fight off the infection in different ways. The different ways the antibiotic functions is by inhibiting the bacterial cell from metabolizing, by preventing the bacteria’s cell wall synthesizing, by creating a permeable membrane of the bacteria cell, or by suppressing nucleic acid transcription and replication. Most antibiotics today are semisynthetic, which means their natural derivative has been altered. Antibiotics have two distinct groups that was separated by their effect on bacteria. Bactericidal antimicrobials kills bacteria while bacteriostatic agents hinder the bacteria from growing or reproducing. They are also seperated depending on their activity sepectrum. Narrow antibiotics target a spesfic group of bacteria while a broad spectrum targets many different kinds of cells.
Lamisil is a medicine that tackles fungus of the skin, toenails and fingernails. A generic form of this is called Terbinafine. Nail fungus is a type of infection that is caused by certain types of fungi. When the fungus reaches the nail, this causes the nail bed to become thick, discolored and brittle. With the oral tablet, after Lamisil has entered the blood, the medicine then moves into the nails and skin. Then, the medicine either kills the fungi or acts to slow the growth.
V. Amarnath, D. C. Anthony, K. Amarnath, W. M. Valentine, L. A. Wetterau, D. G. J. Org. Chem. 1991, 56, p. 6924-6931.