Quinine Sulphate Microparticles as Treatment for Leishmaniasis.

Conclusion: Overall, quinine sulphate microparticles had better pharmacokinetic profile and showed higher efficacy against Leishmania donovani parasites in vivo. Thus, quinine sulphate microparticles have the potential, especially, in treating visceral leishmaniasis. PMID: 32411255 [PubMed]
Source: Journal of Tropical Medicine - Category: Tropical Medicine Tags: J Trop Med Source Type: research

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de;o P. de de Sousa In low-income populations, neglected diseases are the principal cause of mortality. Of these, leishmaniasis and malaria, being parasitic, protozoan infections, affect millions of people worldwide and are creating a public health problem. The present work evaluates the leishmanicidal and antiplasmodial action of a series of twelve p-coumaric acid derivatives. Of the tested derivatives, eight presented antiparasitic activities 1–3, 8–12. The hexyl p-coumarate derivative (9) (4.14 ± 0.55 μg/mL; selectivity index (SI) = 2.72) showed the highest leishmanicidal potenc...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research
CONCLUSIONS Our results showed that 8-oxoG clearance in L. braziliensis is important to avoid misincorporation during DNA replication after oxidative stress generated by H2O2. PMID: 32638832 [PubMed - in process]
Source: Memorias do Instituto Oswaldo Cruz - Category: Infectious Diseases Authors: Tags: Mem Inst Oswaldo Cruz Source Type: research
by No élie Douanne, George Dong, Mélanie Douanne, Martin Olivier, Christopher Fernandez-Prada Leishmaniasis constitutes the 9th largest disease burden among all infectious diseases. Control of this disease is based on a short list of chemotherapeutic agents headed by pentavalent antimonials, followed by miltefosine and amphotericin B; drugs that are far from ideal due to host toxicity, elevated cost, limited access, and high rates of drug resistance. Knowing that the composition of extracellular vesicles (EVs) can vary according to the state of their parental cell, we hypothesized that EVs released by drug-r...
Source: PLoS Neglected Tropical Diseases - Category: Tropical Medicine Authors: Source Type: research
In conclusion, NLCs may have promising potential as carrier for topical treatment of various conditions of skin and mucosa. PMID: 32632542 [PubMed - in process]
Source: AAPS PharmSciTech - Category: Drugs & Pharmacology Authors: Tags: AAPS PharmSciTech Source Type: research
AbstractLeishmaniasis is a serious global challenge with neither efficacious prophylactic vaccine nor effective and safe therapeutic measures. Cathelicidins, members of antimicrobial peptides family, are small proteins of innate immunity system, which represent a protective barrier against a number of potential pathogens in living organisms. The murine cathelicidin or cathelin-related antimicrobial peptide (CRAMP) is expressed by a variety of cells or tissues, and highly resembles to human cathelicidin (LL-37). It is naturally expressed at a low concentration in adolescent age, but extensively increases during cutaneous in...
Source: Journal of Parasitic Diseases - Category: Parasitology Source Type: research
CONCLUSION: The results suggest that the incorporation into NPs potentiated the therapeutic effect of thiourea 1, most likely by improving the selective delivery of the drug to the phagocytic cells that are targeted for infection by L. amazonensis. This work reinforces the importance of nanotechnology in the acquisition of new therapeutic alternatives for oral treatments. PMID: 32621717 [PubMed - as supplied by publisher]
Source: Current Drug Delivery - Category: Drugs & Pharmacology Authors: Tags: Curr Drug Deliv Source Type: research
In this study, we have synthesized 25 2-methoxy-6,6-dimethyl-6H-benzo[c]chromen analogues of 1 and its co-metabolite pulchral (5a), by semi-synthetic procedures starting from the natural product pulchrol (1) itself. All 27 compounds, including the two natural products 1 and 5a, were subsequently assayed in vitro for antiparasitic activity against Trypanozoma cruzi, Leishmania brasiliensis and Leishmania amazoniensis. In addition, the cytotoxicity in RAW cells was assayed, and a selectivity index (SI) for each compound and each parasite was calculated. Several compounds are more potent or equi-potent compared with the posit...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research
, Sousa VRF Abstract Visceral leishmaniasis (VL) is an infectious disease caused by the protozoan parasite Leishmania (Leishmania) infantum, an intracytoplasmic parasite that affects humans and other species of domestic and wild mammals. In Brazil, the treatment of canine visceral leishmaniasis (CVL) with miltefosine has been implemented since 2016, and the reports on the clinical and immunological conditions of treated dogs are scarce. Thus, this study aimed to assess and monitor the clinical, laboratory, and immunological condition of dogs with CVL before (D0) and after (D29) using three pharmacotherapeutic prot...
Source: Experimental Parasitology - Category: Parasitology Authors: Tags: Exp Parasitol Source Type: research
by Jeziel D. Damasceno, Jo ão Reis-Cunha, Kathryn Crouch, Dario Beraldi, Craig Lapsley, Luiz R. O. Tosi, Daniella Bartholomeu, Richard McCulloch Homologous recombination (HR) has an intimate relationship with genome replication, both during repair of DNA lesions that might prevent DNA synthesis and in tackling stalls to the replication fork. Recent studies led us to ask if HR might have a more central role in replicating the genome ofLeishmania, a eukaryotic parasite. Conflicting evidence has emerged regarding whether or not HR genes are essential, and genome-wide mapping has provided evidence for an unorthodox org...
Source: PLoS Genetics - Category: Genetics & Stem Cells Authors: Source Type: research
Conclusion: The selection performed does not suggest rapid development of resistance against aminopyrazoles in the field. Karyotype changes may confer elevated levels of resistance, but these do not seem to be stable in the vertebrate and invertebrate hosts. MDR/MRP efflux pumps are not likely to significantly impact the activity of the aminopyrazole leads. PMID: 32601168 [PubMed - as supplied by publisher]
Source: Antimicrobial Agents and Chemotherapy - Category: Microbiology Authors: Tags: Antimicrob Agents Chemother Source Type: research
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