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Host-parasite co-metabolic activation of antitrypanosomal aminomethyl-benzoxaboroles.

Recent development of benzoxaborole-based chemistry gave rise to a collection of compounds with great potential in targeting diverse infectious diseases, including human African Trypanosomiasis (HAT), a devastating neglected tropical disease. However, further medicinal development is largely restricted by a lack of insight into mechanism of action (MoA) in pathogenic kinetoplastids. We adopted a multidisciplinary approach, combining a high-throughput forward genetic screen with functional group focused chemical biological, structural biology and biochemical analyses, to tackle the complex MoAs

Антимикробный спектр деятельности и механизм действий линейных альфа-гелипических Пептидов, вдохновляемых креветочными антилиполисахаридами.

Креветочные антилипополизакхаридные факторы (АФО) образуют многофункциональное и разнообразное семейство противомикробных защитных пептидов (АМП), состоящих из seven Члены (группы А-G), которые различаются по своей первичной структуре и биохимическим свойствам. Это амфипатические пептиды с two Сохраненные остатки цистейна стабилизируют центральный β-волокн, который, как считается, является основным районом их биологической деятельности. В этом исследовании мы синтезировали three Линейные (без цистейна) пептиды, основанные на аминокислотной последовательности центральных β-волокн недавно иденти

Immunomodulatory effect of Arabinosylated lipoarabinomannan restrict the progression of visceral leishmaniasis through NOD2 inflammatory pathway: Functional regulation of T cell subsets.

NOD like receptors (NLR) are essential pathogen associated molecular pattern receptors of cytoplasmic origin. During several intracellular parasitic infections NLR played vital role for host protective immune response against the pathogen. Amongst various classes of NLR, NOD1 and NOD2 had been extensively studied and were found to be the most active member of the NLR family. Therefore, we wanted to study the role of NOD1/NOD2 during Leishmania donovani infection and the mechanism behind the utilization of this pathway as a therapeutic approach. Using the infected model of macrophage and BALB/c

Low-dose benznidazole treatment results in parasite clearance and attenuates heart inflammatory reaction in an experimental model of infection with a highly virulent Trypanosoma cruzi strain.

Chagas disease, caused by Trypanosoma cruzi, is the main cause of dilated cardiomyopathy in the Americas. Antiparasitic treatment mostly relies on benznidazole (Bzl) due to Nifurtimox shortage or unavailability. Both induce adverse drug effects (ADE) of varied severity in many patients, leading to treatment discontinuation or abandonment. Since dosage may influence ADE, we aimed to assess Bzl efficacy in terms of parasiticidal and anti-inflammatory activity, using doses lower than those previously reported. BALB/c mice infected with the T. cruzi RA strain were treated with different doses of B

Inhibition of myotoxic activity of Bothrops asper myotoxin II by the anti-trypanosomal drug suramin.

Suramin, a synthetic polysulfonated compound, developed initially for the treatment of African trypanosomiasis and onchocerciasis, is currently used for the treatment of several medically relevant disorders. Suramin, heparin, and other polyanions inhibit the myotoxic activity of Lys49 phospholipase A2 analogues both in vitro and in vivo, and are thus of potential importance as therapeutic agents in the treatment of viperid snake bites. Due to its conformational flexibility around the single bonds that link the central phenyl rings to the secondary amide backbone, the symmetrical suramin molecu

Antiparasitic activities of two sesquiterpenic lactones isolated from Acanthospermum hispidum D.C.

ETHNOPHARMACOLOGICAL RELEVANCE: Aerial parts of Acanthospermum hispidum D.C. are often used by traditional healers in Benin for various diseases and especially for malaria. AIM OF THE STUDY: To identify active compounds from extracts of Acanthospermum hispidum D.CV. leaves previously shown to possess antimalarial properties and analyse in vivo activity and toxicity of crude extracts. MATERIALS AND METHODS: Compounds were isolated from aerial part of Acanthospermum hispidum D.C. and structurally elucidated using extensive spectroscopic analysis. Antiplasmodial activity was evaluated in vitro

Imipramine exploits histone deacetylase 11 to increase the IL-12/IL-10 ratio in macrophages infected with antimony-resistant Leishmania donovani and clears organ parasites in experimental infection.

The efflux of antimony through multidrug resistance protein (MDR)-1 is the key factor in the failure of metalloid treatment in kala-azar patients infected with antimony-resistant Leishmania donovani (Sb(R)LD). Previously we showed that MDR-1 upregulation in Sb(R)LD infection is IL-10-dependent. Imipramine, a drug in use for the treatment of depression and nocturnal enuresis in children, inhibits IL-10 production from Sb(R)LD-infected macrophages (Sb(R)LD-Mϕs) and favors accumulation of surrogates of antimonials. It inhibits IL-10-driven nuclear translocation of c-Fos/c-Jun, critical for enhanc

Множество миеломных клеточных липидов повышают целевость и эффективность нанолипосомных формул In Vitro.

Множественная миелома (MM) — рак крови, характеризующийся накоплением аномальных плазменных клеток в костном мозге (BM). Неопластическое расширение постепенно нарушает нормальное производство клеток крови, вытесняя здоровые кровеносные клетки. Болезнь характеризуется неизмеримо дифференцированными клетками В, которые выделяют антитела как часть адаптивной иммунной реакции. Одной из серьезных угроз, с которой сталкивается терапия малых молекул наркотиков для MM, является отсутствие селективной наркодиагностики, что в конечном счете приводит к недостаточному накоплению лекарств для целевых клето

Genus Sophora: a comprehensive review on secondary chemical metabolites and their biological aspects from past achievements to future perspectives.

Sophora is deemed as one of the most remarkable genera of Fabaceae, and the third largest family of flowering plants. The genus Sophora comprises approximately 52 species, 19 varieties, and 7 forms that are widely distributed in Asia and mildly in Africa. Sophora species are recognized to be substantial sources of broad spectrum biopertinent secondary metabolites namely flavonoids, isoflavonoids, chalcones, chromones, pterocarpans, coumarins, benzofuran derivatives, sterols, saponins (mainly triterpene glycosides), oligostilbenes, and mainly alkaloids. Meanwhile, extracts and isolated compoun

Homoharringtonine: updated insights into its efficacy in hematological malignancies, diverse cancers and other biomedical applications.

HHT has emerged as a notable compound in the realm of cancer treatment, particularly for hematological malignancies. Its multifaceted pharmacological properties extend beyond traditional applications, warranting an extensive review of its mechanisms and efficacy. This review aims to synthesize comprehensive insights into the efficacy of HHT in treating hematological malignancies, diverse cancers, and other biomedical applications. It focuses on elucidating the molecular mechanisms, therapeutic potential, and broader applications of HHT. A comprehensive search for peer-reviewed papers was condu

Совпадение в полном тексте источника
… Plant alkaloids, such as HHT, are increasingly recognized as potent trypanocidal agents. Research indicates that pretreatment with such alkaloids significantly inhibits the growth and protein biosynthesis of these parasites in both a concentration- and time-dependent manner. …

Abstracts from the World Congress of Cardiology/Brazilian Congress of Cardiology 2022

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