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Phyto constituent-Centered Byproducts and Nanomedicines as Leishmanicidal Scavengers
Published in Mahfoozur Rahman, Sarwar Beg, Mazin A. Zamzami, Hani Choudhry, Aftab Ahmad, Khalid S. Alharbi, Biomarkers as Targeted Herbal Drug Discovery, 2022
Sabya Sachi Das, P. R. P. Verma, Sandeep Kumar Singh
The drugs comprising antimony (pentavalent antimonials) as a principal component are primarily the drugs of choice as anti-leishmanial drugs (ALD) for first line cure of Leishmaniasis where confrontation has not been stated (Singh et al., 2006). These comprise of the generic sodium stibogluconate (pentostam, Figure 5.3), the branded meglumine antimoniate, which is been in practice for over five decades. Unfortunately, the Leishmania protozoal parasites have been progressively developed the resistance to these pentavalent antimonial drugs and hence this raised a question for their usage in disease-endemic extents (Maltezou, 2010). Since, these antimonials are directed intravenously (I.V) or intramuscularly (I.M), they are not suitable for patients. They are also concomitant with adverse reactions, which include biochemical pancreatitis, elevation in serum aminotransferases level, and electro-cardiographic oddities (Polonio and Efferth, 2010).
New Chemical Scaffolds to Selectively Target the Trypanothione Metabolism
Published in Venkatesan Jayaprakash, Daniele Castagnolo, Yusuf Özkay, Medicinal Chemistry of Neglected and Tropical Diseases, 2019
Pentavalent antimonials are prodrugs that become active upon reduction to trivalent antimony in the cell. Cunningham and Fairlamb demonstrated that antimonials interfere with the trypanothione metabolism by inhibiting the enzymatic activity of TR (Cunningham et al. 1995).
Modern Pharmacognostic Investigation of Harmal
Published in Ephraim Shmaya Lansky, Shifra Lansky, Helena Maaria Paavilainen, Harmal, 2017
Ephraim Shmaya Lansky, Shifra Lansky, Helena Maaria Paavilainen
A companion Iranian look at harmal and Leishmania major (Mirzaei et al. 2007) similarly went in vitro to explore its therapeutic power relative to the pentavalent antimonial. They grew the promastigote form of L. major, which is the flagellated stage that lives in sandflies, as opposed to the nonmotile, a-flagellate amastigote stage, which nevertheless expertly establishes itself in mammals (Kima 2007). Mirzaei et al. (2007) and they showed a model to measure inhibition of L. major promastigotes. Though their standard P. harmala extract prepared according to the method of Manske and Holmes (1952) was effective against the parasite in a manner comparable to that of the antimonial, it was so at approximately 100 times the antimonial dose. Overall, however, the harmal was adjudged to possess comparable action to the trivalent Sb compound, albeit at a higher dose. This differential in dose (IC 50) is to be expected whenever a crude drug is compared to a pure compound.
Spiro heterocycles bearing piperidine moiety as potential scaffold for antileishmanial activity: synthesis, biological evaluation, and in silico studies
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Mounir A. A. Mohamed, Asmaa M. Kadry, Salma A. Bekhit, Mohammed A. S. Abourehab, Kikuko Amagase, Tamer M. Ibrahim, Ahmed M. M. El-Saghier, Adnan A. Bekhit
Leishmaniasis is a complex disease that is caused by more than 20 species of Leishmania and correlated to several clinical manifestations ranging from simple skin lesions around the bite site to fatal visceral forms1,2. More than one billion people are at risk of leishmaniasis in endemic areas3,4. Based on literature data, there is no effective and safe treatment for leishmaniasis for further developments. About 50 years ago pentavalent antimonials used as first-line drugs for the treatment of leishmaniasis diseases despite of high toxicity1,2. Besides, existing approved drugs for leishmania can cause various sever adverse effects like gastro-intestinal disturbance, hepatic and renal dysfunction, especially, co-infections of immunocompromised patients with leishmaniasis, e.g. HIV-leishmania co-infection, are fatal1,2.
Evaluating the effect of oral clarithromycin on acute cutaneous leishmaniasis lesions compared with systemic glucantime
Published in Journal of Dermatological Treatment, 2022
Naghmeh Zabolinejad, Pouran Layegh, Zahra Abbasi Shaye, Maryam Salehi, Somayeh Ghanizadeh
The pentavalent antimonial drug has been the most common treatment for leishmaniasis for many years. However, resistance to this drug is on a rise, and there has been a great tendency toward the use of new anti-leishmaniasis treatments over the past few years, which are not only suitable for the treatment of the disease, but also are easy to use and available and have fewer complications (18,19). Since CL is a self-limiting disease and the aim of treatment is to control the spread of the disease in endemic areas and reduce scarring, it is logical to apply drugs with a greater effect, fewer complications, and easier use. Due to the structural similarity of azithromycin and clarithromycin and the therapeutic effects of clarithromycin on intracellular organisms, and the proven anti-leishmanial effects of azithromycin, clarithromycin could also be considered as an anti-leishmaniasis treatment.
The effect of pentavalent antimonial compounds used in the treatment of cutaneous leishmaniasis on hemogram and biochemical parameters
Published in Cutaneous and Ocular Toxicology, 2019
Isa An, Mehmet Harman, Mustafa Esen, Hakim Çelik
Pentavalent antimonials is the most commonly used approach in the treatment of CL, since it produces the most effective results in most of the cases with low rate of recurrence and cosmetically good results in general. Pentavalent antimonials have been the cornerstone of anti-leishmanial treatment since the 1940s. The mechanisms of action of the pentavalent antimonials are not fully known, but they are thought to inhibit ATP synthesis of the parasite. There are two pentavalent antimonials which are therapeutically equivalent. These are meglumine antimonate (MA) and sodium stibogluconate (SSG)2,3,5. These compounds may cause side effects such as muscle and joint pain, fatigue, loss of appetite, nausea, abdominal pain, headache, skin rash and nonspecific ST changes in electrocardiography. Increase in pancreatic enzymes, elevation of transaminases, bone marrow suppression and acute renal failure have also been reported in the literature2,6–9.