Hydroxyalkyne-Bithiophene Derivatives: Synthesis and Antileishmanial Activity.

Leishmaniasis is one of the most important neglected tropical diseases, prevalent in underdeveloped or developing countries, and new pharmacological agents for this disease are urgently needed. In this study, thiophene derivatives based on the natural product 5'-methyl-(5-[4-acetoxy-1-butynyl])-2,2'-bithiophene were synthesized and evaluated against promastigote forms of Leishmania amazonensis. The bithiophene BT-1 was the most potent and selective synthetic compound toward the parasites, exhibiting IC of 23.

Beyond phototoxicity: The dark side of new methylene blue on mitochondrial and cellular bioenergetics.

New methylene blue (NMB) is a phenothiazine dye with recognized photodynamic properties. This study evaluated both light-dependent and intrinsic (light-independent) effects of NMB on mitochondrial function, hepatic metabolism, and cell viability using three models: isolated rat liver mitochondria, ex vivo perfused rat liver, and HepG2 cells. In isolated mitochondria, NMB uncoupled oxidative phosphorylation, decreasing the respiratory control (RC) and ADP/O ratios, even without irradiation.

Morin as a Modulator of Hepatic Glucose Fluxes: A Balance Between Antihyperglycemic Potential and Mitochondrial Toxicity.

This study evaluated the acute effects of morin on gluconeogenesis and glycogenolysis, key metabolic pathways that maintain glycemia, in perfused rat livers. It also assessed the acute effects of morin on mitochondrial energy metabolism and toxicity in hepatic cancer cells (HepG2) and renal epithelial cells (VERO), alongside its impact on the activity of key enzymes. Liver perfusion experiments assessed glucose fluxes, oxygen consumption, adenine nucleotide levels, and enzyme activities.

Strategy for the Construction of SARS-CoV-2 S and N Recombinant Proteins and Their Immunogenicity Evaluation.

This study reports the construction, expression, and purification of synthetic SARS-CoV-2 spike (S) and nucleoprotein (N) containing immunodominant epitopes. The pET28aS_epit construct included epitopes 287-317, 402, 507, 524-598, and 601-640, while the pET28aN_epit construct included residues 42-62, 153-172, and 355-401. Commercial sequences of both proteins were used as controls.

In vitro biofilm formation and virulence of Paracoccidioides lutzii (LDR2) in a Galleria mellonella larval model.

Paracoccidioidomycosis (PCM) is a systemic mycosis caused by the thermodimorphic fungi Paracoccidioides brasiliensis and the newly identified species P. lutzii. This study investigated in vitro biofilm formation by P.

Efficacy of benznidazole delivery during Chagas disease nanotherapy is dependent on the nanocarrier morphology.

The causative agent of Chagas disease, the protozoan Trypanosoma cruzi, is an obligate intracellular parasite that is typically treated with daily oral administration of Benznidazole (BNZ), a parasiticidal pro-drug with considerable side effects. Previously, we effectively targeted intracellular parasites using ∼100 nm diameter BNZ-loaded poly(ethylene glycol)-b-poly(propylene sulfide) (PEG-b-PPS) vesicular nanocarriers (a.k.

photochemoprotective potential of emulsion containing the ethyl acetate fraction from (Myrtaceae).

This work aimed to study the chemical composition and evaluate the photochemoprotective potential of an emulsion containing bioactive plant material obtained from Sobral leaves. The ethyl acetate fraction (EAF) was selected for its high content of total phenolics and high antioxidant capacity. Chemical analysis using 1D/2D nuclear magnetic resonance spectroscopy identified three ursane-type pentacyclic triterpenoids - corosolic acid (1), 3-O-α-L-arabinopyranosyl-pomolic acid (2), and pomolic acid (3) - and one phenolic acid, gallic acid (4).

Synergistic Antibacterial Interaction of Geraniol and Biogenic Silver Nanoparticles on Methicillin-Resistant .

Since ancient times, plants have been used in folk medicine to treat different diseases. Plants offer exceptional chemical diversity with a wide range of biological activities, and have therefore been the most promising sources for the discovery and development of drugs, including antimicrobial agents. This study reports the antibacterial effect of geraniol (GER), alone and in combination with biogenic silver nanoparticles (bioAgNPs), produced using the aqueous extract of bark, against planktonic and sessile cells of methicillin-resistant (MRSA), one of the main opportunistic and potentially fatal human pathogens.

Synthesis and antiprotozoal evaluation of novel Knoevenagel hydroxychloroquine derivatives.

Leishmaniasis and Chagas diseases affect millions of people, particularly in developing countries, with conventional treatments proving unsatisfactory due to increasing drug resistance and high toxicity. Therefore, there is an urgent need for new drugs to combat neglected tropical diseases (NTDs). In this study, we synthesized 15 new Knoevenagel adducts derived from hydroxychloroquine and evaluated their antiprotozoal activity against , , and .

Effect of glycerol diglycidyl ether crosslinker on pectin-starch blended pharmaceutical films.

Pharmaceutical films can show versatility and biocompatibility. Pectin and starch blends crosslinked with glycerol diglycidyl ether (GDE) can improve the physicochemical properties of films. This study aimed to develop films with pectin and starch crosslinked with GDE.

Syringic acid protective role: Combatting oxidative stress induced by UVB radiation in L-929 fibroblasts.

Neglecting proper skin care and repeated exposure to ultraviolet (UV) radiation can have serious consequences, including skin burns, photoaging and even the development of skin cancer. UV radiation-induced damage is mediated by highly unstable and reactive molecules, named reactive oxygen species (ROS). To counteract ROS, the skin has an endogenous antioxidant system.

Design of solid lipid nanoparticles for skin photoprotection through the topical delivery of caffeic acid-phthalimide.

Exposure of the skin to ultraviolet (UV) radiation is associated with many pathological conditions such as premature aging and skin cancer. Furthermore, members of Nicotinamide Adenine Dinucleotide Phosphate-oxidase (NADPH oxidase or NOX) enzyme family can produce UV-induced reactive oxygen species (ROS), even after cessation of radiation exposure. The caffeic acid-phthalimide (CF) compound is a potent antioxidant, which reduces the generation of ROS.

Polysaccharide-Stabilized Semisolid Emulsion with Vegetable Oils for Skin Wound Healing: Impact of Composition on Physicochemical and Biological Properties.

The demand for natural-based formulations in chronic wound care has increased, driven by the need for biocompatible, safe, and effective treatments. Natural polysaccharide-based emulsions enriched with vegetable oils present promising benefits for skin repair, offering structural support and protective barriers suitable for sensitive wound environments. This study aimed to develop and evaluate semisolid polysaccharide-based emulsions for wound healing, incorporating avocado () and blackcurrant () oils (AO and BO, respectively).

New Dichalcogenides Induce Oxidative Stress and Cell Death of Leishmania amazonensis.

Leishmaniasis are caused by protozoa of the genus Leishmania and affect millions of people worldwide. They are considered neglected diseases that primarily impact individuals in tropical and subtropical regions. The drugs currently available for treating this infection have limitations, such as high toxicity, adverse reactions, and a long therapeutic intervention period.

Unraveling the intrinsic and photodynamic effects of aluminum chloride phthalocyanine on bioenergetics and oxidative state in rat liver mitochondria.

Previous research has revealed that mitochondria are an important target for photodynamic therapy (PDT), which might be employed as a therapeutic approach for several malignancies, including hepatocellular carcinoma (HCC). In this study, we investigated both intrinsic toxicity and photodynamic effects of the photosensitizer (PS) aluminum chloride phthalocyanine (AlClPc) on mitochondrial functions. Several aspects of mitochondrial bioenergetics, structure, and oxidative state were investigated in the isolated mitochondria obtained from rat liver by differential centrifugation.

Hypericin-loaded in modified theranostic liposome nanoplatform: a preliminary in vivo study of targeting and diagnosis.

Modified theranostic liposomes were created by combining phospholipid 1,2-dipalmitoyl-sn-3-glycerol-phosphatidylcholine with two previously modified Pluronic copolymers covalently linked with spermine and folic acid to carry and stabilize the photosensitizer compound hypericin. After physicochemical characterization, the photocytotoxicity was evaluated against different cancer and healthy cells presenting a strong photodynamic effect. The formulation exhibited no photoactivity without illumination and without hypericin.

Synthesis of Keratin Nanoparticles Extracted from Human Hair through Hydrolysis with Concentrated Sulfuric Acid: Characterization and Cytotoxicity.

Human hair, composed primarily of keratin, represents a sustainable waste material suitable for various applications. Synthesizing keratin nanoparticles (KNPs) from human hair for biomedical uses is particularly attractive due to their biocompatibility. In this study, keratin was extracted from human hair using concentrated sulfuric acid as the hydrolysis agent for the first time.

Trichilia catigua against Helicobacter pylori: An in vitro, molecular and in silico approach.

Helicobacter pylori is a bacterium that is present in the stomach of about 50% of the global population and is associated with several gastric disorders, including cancer. Natural products with antimicrobial activity have been tested against H. pylori, among them Trichilia catigua (catuaba), which is widely distributed in Brazil.

Design, synthesis and identification of novel molecular hybrids based on naphthoquinone aromatic hydrazides as potential trypanocide and leishmanicidal agents.

In pursuit of potential agents to treat Chagas disease and leishmaniasis, we report the design, synthesis, and identification novel naphthoquinone hydrazide-based molecular hybrids. The compounds were subjected to in vitro trypanocide and leishmanicidal activities. N'-(1,4-Dioxo-1,4-dihydronaphthalen-2-yl)-3,5-dimethoxybenzohydrazide (13) showed the best performance against Trypanosoma cruzi (IC50 1.

Inclusion Complexes of (Lour.) Pers Essential Oil into β-Cyclodextrin: Preparation, Physicochemical Characterization, Cytotoxicity and Antifungal Activity.

The uses of natural compounds, such as essential oils (EOs), are limited due to their instability to light, oxygen and temperature, factors that affect their application. Therefore, improving stability becomes necessary. The objective of this study was to prepare inclusion complexes of essential oil (LCEO) with β-cyclodextrin (β-CD) using physical mixing (PM), kneading (KN) and co-precipitation (CP) methods and to evaluate the efficiency of the complexes and their physicochemical properties using ATR-FTIR, FT-Raman, DSC and TG.

Discovery of a new pyrido[2,3-]pyridazine-2,8-dione derivative as a potential anti-inflammatory agent through COX-1/COX-2 dual inhibition.

In this paper, we present the design and synthesis of a novel series of pyrido[2,3-]pyridazine-2,8-dione derivatives the annulation of the 2-pyridone pattern. The synthesized derivatives were evaluated for anti-inflammatory activity using an ear edema model. Compound 7c, which showed a greater inhibition of ear edema (82%), was further tested for its COX-1/COX-2 inhibitory activity.

Dithiothreitol reduces oxidative stress and necrosis caused by ultraviolet A radiation in L929 fibroblasts.

Ultraviolet A (UVA) radiation, present in sunlight, can induce cell redox imbalance leading to cellular damage and even cell death, compromising skin health. Here, we evaluated the in vitro antioxidant and photochemoprotective effect of dithiothreitol (DTT). DTT neutralized the free radicals 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH·), and superoxide anion (O) in in vitro assays, as well as the ferric ion (Fe) in the ferric reducing antioxidant power (FRAP) assay.

anticancer and antifungal properties of the essential oil from the leaves of kunth.

The essential oil from (EOLO) is employed in traditional medicine as it has both antimicrobial and anti-inflammatory properties. The current investigation first evaluated the EOLO's cytotoxic activity in tumour (SiHa and HT-29) and non-tumour (human lymphocyte) cells by MTT. The effect on ROS production was further evaluated in cancer cells by fluorimetry.

Berberine-fluconazole microparticle-based combination therapy to treat candidiasis infections.

Aim: This study aims to incorporate alginate microparticles containing berberine and fluconazole into two different types of pharmaceutical formulations, to subsequently evaluate the antifungal activity against Candida albicans.

Methods And Results: Alginate microparticles containing BBR (berberine) and FLU (fluconazole) were produced by the spray-drying technique, characterized and incorporated in two pharmaceutical formulations, a vaginal cream and artificial saliva. Broth microdilution, checkerboard, time-kill curve, and scanning electron microscopy were carried out to determine the antifungal effects of BBR and FLU against C.