Phyto constituent-Centered Byproducts and Nanomedicines as Leishmanicidal Scavengers
Mahfoozur Rahman, Sarwar Beg, Mazin A. Zamzami, Hani Choudhry, Aftab Ahmad, Khalid S. Alharbi in Biomarkers as Targeted Herbal Drug Discovery, 2022
Tiuman et al. (2005) investigated the in vitro ALA of PTN, extracted from several parts of plant Tanacetum parthenium, against L. amazonensisparasite. Results showed the high potency of these compounds as leishmanicidal agents (IC50 0.37 μg/mL). Karioti et al. (2009) evaluated the in vitro antiprotozoal as well as leishmanicidal activity three irregulars, linear sesquiterpene and reported that all compounds exhibited potent trypanocidal and leishmanicidal activity. Moura do Carmo et al. (2012) examined the fabrication of EO found from leaves of Piper demeraranum and Piper duckeiby GC-MS. The main constituents found in P. demeraranum oil and P. duckei oil showed high potential of ALA (IC50 15-76 μg mL-1) against strains of L. amazonensis.Rottini et al. (2015) estimated the inhibitory effect of (—) α-bisabolol, in contradiction of the promastigotes and intracellular amastigotes phases of L. amazonensis, and their IC50 with effective concentration of 8.07 μg/mL (24 h) and 4.26 μg/mL (48 h) was recorded. Rodrigues et al. (2018) estimated the ALA of Copaifera spp. Oleoresins against L. amazonensis and L. infantum strains. Further, results showed that these novel compounds exhibited ALA against L. amazonensis (IC50= 62.5 μg/mL) and alongside L. infantum (IC50 = 65.9 μg/mL).
Antimicrobials during Pregnancy
“Bert” Bertis Britt Little in Drugs and Pregnancy, 2022
The two most common forms of vaginitis during pregnancy are fungal and protozoan. Pregnant women with vaginitis secondary to fungi, such as Candida species, can be treated with a variety of antifungal agents that are listed in Box 2.24. Women with trichomoniasis present an unusual therapeutic dilemma. Although there is no scientific evidence that metronidazole is either teratogenic or causes adverse effects in the embryo/fetus, the manufacturer has issued a stern warning regarding its use during the first trimester of pregnancy. Fortunately, many of the patients with trichomoniasis can be treated with antiprotozoal agents until they are past the first trimester and then treated with metronidazole—the only effective treatment for this protozoan infection.
Iodoquinol and Quinacrine
M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson in Kucers’ The Use of Antibiotics, 2017
Quinacrine, also known as mepacrine hydrochloride, was synthesized by scientists at Bayer in Germany in 1931. It was one of the first synthetic antimalarial substitutes for quinine but was later superseded by chloroquine because of the latter’s more favorable toxicity profile. During World War II, it was marketed as Mepacrine or Atabrine, and it has been used for malaria chemoprophylaxis. More recently, it has been used as an antiprotozoal agent because it has activity against G. lamblia as well as Plasmodium species. However, quinacrine is now rarely used to treat giardiasis because of the drug’s toxicity and the superiority of metronidazole for this indication (see Chapter 99, Metronidazole) (Upcroft and Upcroft, 2001). Quinacrine has also been used for the treatment of tapeworm, but it has been replaced for this indication by newer, less toxic agents. It is an acridine derivative that is both water and alcohol soluble, with the chemical formula C23H30ClN3O and a molecular weight of 400.0 g/mol; the chemical structure is shown in Figure 191.2.
Metabolomic profile, anti-trypanosomal potential and molecular docking studies of Thunbergia grandifolia
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Heba A. S. El-Nashar, Ahmed M. Sayed, Hany A. M. El-Sherief, Mostafa E. Rateb, Lina Akil, Ibrahim Khadra, Taghreed A. Majrashi, Sara T. Al-Rashood, Faizah A. Binjubair, Mahmoud A. El Hassab, Wagdy M. Eldehna, Usama Ramadan Abdelmohsen, Nada M. Mostafa
Trypanosomiasis or sleeping sickness is a protozoan disease that infects animals and humans transmitted by the bite of Glossina (tsetse) fly carrying Trypanosoma brucei1. Currently, trypanosomiasis affects more than 50 million cattle and 70 million people in sub-Saharan Africa2. The available current medicines record lack of efficiency, resistance, and toxicity, so there is an urgent need for the development of novel, safe, efficacious, cost-effective drugs with new mechanism of action3,4. In African countries where trypanosomiasis is prevalent, natural products (herbal extracts) have traditionally been utilised for centuries and are still extensively used to cure infections and other parasitic diseases5,6. Interestingly, about 30% of the world population has confidence in traditional therapies due to their wide availability and affordability7. Moreover, various drugs like quinine and artemisinin were established as plant-derived potential antiprotozoal agents8.
Controlled delivery of the antiprotozoal agent (tinidazole) from intravaginal polymer matrices for treatment of the sexually transmitted infection, trichomoniasis
Published in Pharmaceutical Development and Technology, 2019
Hevanshi Vidhushika Fernando, Li Li Chan, Nhung Dang, Diviya Santhanes, Hasini Banneheke, Sivalingam Nalliah, Allan G. A. Coombes
Microporous PCL matrices incorporating tinidazole may be prepared by rapidly cooling co-solutions of PCL and the drug, resulting in a maximum tinidazole loading of 3.9% (w/w). Gradual release of around 50% of the drug load occurred over 7 days in SVF with retained antiprotozoal activity of almost 50% at day 7 compared with 35% for equivalent concentrations of ‘non-formulated’ drug solutions. Based on in vitro measurements, the predicted in vivo concentrations of tinidazole produced over 7 days by a PCL matrix in the form of an IVR would exceed the MIC against the protozoan parasite T. vaginalis. These findings recommend investigations of IVRs produced from the matrix material to evaluate their flexural properties, insertion and retention characteristics and in vivo behaviour.
Thio- and selenosemicarbazones as antiprotozoal agents against Trypanosoma cruzi and Trichomonas vaginalis
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Alexandra Ibáñez-Escribano, Cristina Fonseca-Berzal, Mónica Martínez-Montiel, Manuel Álvarez-Márquez, María Gómez-Núñez, Manuel Lacueva-Arnedo, Teresa Espinosa-Buitrago, Tania Martín-Pérez, José Antonio Escario, Penélope Merino-Montiel, Sara Montiel-Smith, Alicia Gómez-Barrio, Óscar López, José G. Fernández-Bolaños
Management of diseases caused by pathogenic protozoa is not a simple task4. On the one hand, development of successful vaccines is a hitherto unachieved goal5; on the other hand, the chemotherapeutic arsenal available so far suffers from important drawbacks: most of them are old drugs that are developing chemoresistance6, and are endowed with severe side-effects7 and low efficiency8. Moreover, their high prices, and complex administration protocols make them unaffordable for underdeveloped countries9. Accordingly, the development of new antiprotozoal agents is a hot topic in current Medicinal Chemistry research10,11.
Related Knowledge Centers
- Entamoeba Histolytica
- Eukaryote
- Naegleria Fowleri
- Virus
- Infection
- Pathogen
- Anatomical Therapeutic Chemical Classification System
- Medication
- Protozoan Infection
- Paraphyly