Dehydrothyrsiferol Against Cutaneous Leishmaniasis: Treatment Outcome in a Murine Model.

One of the most important steps in preclinical drug discovery is to demonstrate the in vivo efficacy of potential leishmanicidal compounds and good characteristics at the level of parasite killing prior to initiating human clinical trials. This paper describes the use of dehydrothyrsiferol (DT), isolated from the red alga , in a pharmaceutical form supported on Sepigel, and the in vivo efficacy against a mouse model of cutaneous leishmaniasis. Studying the ultrastructural effect of DT was also carried out to verify the suspected damage at the cellular level and determine the severity of damages produced in the homeostasis of promastigotes.

Unexpected Genetic Diversity of Nostocales (Cyanobacteria) Isolated from the Phyllosphere of the Laurel Forests in the Canary Islands (Spain).

A total of 96 strains of Nostocales (Cyanobacteria) were established from the phyllosphere of the laurel forests in the Canary Islands (Spain) and the Azores (Portugal) using enrichment media lacking combined nitrogen. The strains were characterized by light microscopy and SSU rRNA gene comparisons. Morphologically, most strains belonged to two different morphotypes, termed "-type" and "-type".

Bioassay-Guided Fractionation Networking for Discovery of Biofungicides from Cultivated .

Considering the detrimental impacts of the current pesticides on the biotic components of the biosphere, the development of novel pesticides is vital. Plant-derived biopesticides have emerged as popular alternatives to create a safer and more sustainable agriculture model. This study aims to validate the previous bioguided fractionation of endemic Canary Islands sage, , as a potential source of botanical pesticides using a cultivation process.

Fungal lectins show differential antiproliferative activity against cancer cell lines.

Glycosylation patterns represent an important signature of cancer cells that can be decoded by glycan-binding proteins, i.e., lectins.

Accessing Promising Passerini Adducts in Anticancer Drug Design.

The 3-component Passerini reaction (3CPR), discovered little more than 100 years ago, has been demonstrated in the last few decades to be a valuable tool for accessing structural diversity and complexity, essential topics to consider in drug discovery programs. Focusing on accessing a fine-tuned family of α-acyloxyamide-oxindole hybrids, we underline herein our latest insights regarding the use of this mild reaction approach to obtain promising anticancer agents. Cheap and commercially available isatin was used as starting material.

Biochemistry and Future Perspectives of Antibiotic Resistance: An Eye on Active Natural Products.

Antibiotic resistance poses a serious threat to the current healthcare system, negatively impacting the effectiveness of many antimicrobial treatments. The situation is exacerbated by the widespread overuse and abuse of available antibiotics, accelerating the evolution of resistance. Thus, there is an urgent need for novel approaches to therapy to overcome established resistance mechanisms.

Chemical Composition, Enantiomeric Distribution, and Physical Properties of the Fruit Essential Oil from (Reynel) Rutaceae from Ecuador.

The essential oil was obtained by steam distillation, using a Clevenger apparatus, from the pericarp of the fruit of from Ecuador. The qualitative and quantitative analyses were performed by gas chromatography coupled with mass spectrometry (GC-MS) and flame ionization detection (GC-FID) on two capillary columns with non-polar DB-5ms and a polar HP-INNOWax stationary phase. Thirty-three components were identified, accounting for 99.

1,1'-Diarylethylene as a Key Additive for the Visible Light Synthesis of Bioactive Dihydrobenzo[]phenanthridine Compounds.

This study introduces a straightforward synthetic approach for generating 7,8-dihydrobenzo[]phenanthridine analogs through visible-light-induced cyclization, showing promise as antitumor agents. Unexpectedly, the incorporation of 1,1'-diarylethylene as an additive significantly boosts yield. Through mechanistic investigations, we uncover its crucial role as a trap for the methyl radical formed after the N-O bond cleavage of acetyl oxime, promoting intramolecular cyclization of a nitrogen-centered imine radical.

Synthesis, Biological Activity, and Molecular-Docking Studies of New Brassinosteroid Analogs.

Much work has been dedicated to the quest to determine the structure-activity relationship in synthetic brassinosteroid (BR) analogs. Recently, it has been reported that analogs with phenyl or benzoate groups in the alkyl chain present activities comparable to those shown by natural BRs, depending on the nature of the substituent in the aromatic ring. However, as it is well known that the activity depends on the structure of the whole molecule, in this work, we have synthesized a series of compounds with the same substituted benzoate in the alkyl chain and a hydroxyl group at C3.

Staurosporine as a Potential Treatment for Keratitis Using Mouse Cornea as an Ex Vivo Model.

is a ubiquitous genus of amoebae that can trigger a severe and progressive ocular disease known as Keratitis (AK). Furthermore, current treatment protocols are based on the combination of different compounds that are not fully effective. Therefore, an urgent need to find new compounds to treat infections is clear.

Exploring the Anticancer Potential of Phenolic -Triterpenes from Celastraceae Species.

To explore new compounds with antitumour activity, fifteen phenolic -tripterpenes isolated from Celastraceae species, , and , have been studied. Their chemical structures were elucidated through spectroscopic and spectrometric techniques, resulting in the identification of three novel chemical compounds. Evaluation on human tumour cell lines (A549 and SW1573, non-small cell lung; HBL-100 and T-47D, breast; HeLa, cervix, and WiDr, colon) revealed that three compounds, named 6-oxo-pristimerol, demethyl-zeylasteral, and zeylasteral, exhibited significant activity (GI ranging from 0.

Novel Coumarin-Steroid/Terpenoid Hybrids: In Vitro and In Silico Anticancer Studies.

We have synthesized a series of novel coumarin-steroid and triterpenoid hybrids and evaluated their potential anticancer activity through molecular docking calculations and in vitro antiproliferative assays. These hybrids, derived from estrone and oleanolic acid, were linked via hydrocarbon spacers of varying lengths. Molecular docking studies against human aromatase revealed strong interactions, particularly for compound 11d, which exhibited significant binding affinity (-12.

Novel tetrahydropyran-triazole hybrids with antiproliferative activity against human tumor cells.

A series of new hybrid compounds was prepared combining tetrahydropyran rings with different aromatic systems by means of a 1,2,3-triazole, using a building block strategy. The design of these structures was guided by Lead-Likeness and Molecular Analysis (LLAMA) software, adding modifications to our most potent scaffold (the tetrahydropyran ring) to generate promising "lead-like" candidates, which were subsequently compared against reported anticancer compounds. Our synthesized compounds demonstrated significant antiproliferative activity when compared with the standards cisplatin and 5-fluorouracil, across a panel of six different tumor cell lines.

Dual electro-/pH-responsive nanoparticle/hydrogel system for controlled delivery of anticancer peptide.

An electro-chemo-responsive carrier has been engineered for the controlled release of a highly hydrophilic anticancer peptide, CR(NMe)EKA (Cys-Arg- N-methyl-Glu-Lys-Ala). Remotely controlled on demand release of CR(NMe)EKA, loaded in electro-responsive poly(3,4-ethylenedioxythiophene) (PEDOT) nanoparticles, has been achieved by applying electrical stimuli consisting of constant positive (+0.50 V) or negative voltages (-0.

The Ugi4CR as effective tool to access promising anticancer isatin-based α-acetamide carboxamide oxindole hybrids.

Considering early-stage drug discovery programs, the Ugi four-component reaction is a valuable, flexible, and pivotal tool, facilitating the creation of two new amide bonds in a one-pot fashion to effectively yield the desired α-aminoacylamides. Here, we highlight the reputation of this reaction approach to access number and scaffold diversity of a library of isatin-based α-acetamide carboxamide oxindole hybrids, promising anticancer agents, in a mild and fast sustainable reaction process. The library was tested against six human solid tumor cell lines, among them, non-small cell lung carcinoma, cervical adenocarcinoma, breast cancer and colon adenocarcinoma.

Palladium nanoparticles for the synthesis of phenanthridinones and benzo[]chromenes C-H activation reaction.

In the present work, derivatives of phenanthridine-6(5)-ones and benzo[]chromenes were efficiently prepared through an intramolecular C-H bond functionalization reaction catalyzed by photochemically synthesized Pd-PVP nanoparticles. The heterocycles were obtained intramolecular arylation of the corresponding -methyl--aryl-2-halobenzamide or aryl-(2-halo)benzyl ethers using KCO as base in a mixture of HO : DMA as solvent without additives or ligands. High yields of the heterocyclic compounds were achieved (up to 95%) using a moderately low catalyst loading (1-5 mol%) under an air atmosphere at 100 °C.

Development and Evaluation of PEG-gelatin-based Microparticles to Enhance the Oral Delivery of Insulin.

Background: Diabetes mellitus is a global disease identified by hyperglycemia due to defects in insulin secretion, insulin action, or both.

Objective: The main objective of this research was to evaluate the ability of gelatinized Poly(ethylene glycol) (PEG) microparticles to be used as carriers for oral insulin delivery via double emulsion preparation.

Methods: Five different batches of the formulation consisting of gelatin:PEG were prepared as follows: 0:1 (W1), 1:0 (W2), 1:1 (W3), 1:3 (W4), and 3:1 (W5).

The time between Palaeolithic hearths.

Resolving the timescale of human activity in the Palaeolithic Age is one of the most challenging problems in prehistoric archaeology. The duration and frequency of hunter-gatherer camps reflect key aspects of social life and human-environment interactions. However, the time dimension of Palaeolithic contexts is generally inaccurately reconstructed because of the limitations of dating techniques, the impact of disturbing agents on sedimentary deposits and the palimpsest effect.

Click-chemistry mediated synthesis of OTBN-1,2,3-Triazole derivatives exhibiting STK33 inhibition with diverse anti-cancer activities.

There is a continuous and pressing need to establish new brain-penetrant bioactive compounds with anti-cancer properties. To this end, a new series of 4'-((4-substituted-4,5-dihydro-1H-1,2,3-triazol-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile (OTBN-1,2,3-triazole) derivatives were synthesized by click chemistry. The series of bioactive compounds were designed and synthesized from diverse alkynes and N-OTBN, using copper (II) acetate monohydrate in aqueous dimethylformamide at room temperature.

Ethanolic Extract from Fruits of , a Chilean Extremophile Plant. Assessment of Antioxidant Activity and In Vitro Cytotoxicity.

is a shrub with yellow flowers that reach up to two meters high, endemic of the Atacama Region in Chile. This species grows under special environmental conditions such as low altitude, arid areas, and directly sun-exposed habitats. In the present study, ethanolic extract was obtained from fruits of , and then partitioned in solvents of increasing polarity to obtain five fractions: hexane (HF), dichloromethane (DF), ethyl acetate (AF), and the residual water fraction (QF).

Antiproliferative and Antibacterial Activity of Polyporoid Fungi from Veracruz, Mexico.

Polyporoid fungi represent a vast source of bioactive compounds with potential pharmacological applications. The importance of polyporoid fungi in traditional Chinese medicine has led to an extensive use of some species of Ganoderma for promoting health and longevity because their consumption is associated with several bioactivities. Nevertheless, bioactivity of some other members of the Polyporaceae family has also been reported.

Advancements in steroidal Pt(II) & Pt(IV) derivatives for targeted chemotherapy (2000-2023).

One of the key strategies in chemotherapy involves crosslinking the DNA strands of cancer cells to impede their replication, with platinum (Pt) coordination compounds being a prominent class and cisplatin being its major representative. Steroidal ligands tethered to DNA interactive Pt core act as drug carriers for targeted therapy. While crosslinking of nuclear or mitochondrial DNA strands using coordination complexes has been studied for years, there remains a lack of comprehensive reviews addressing the advancements made in steroidal-Pt derivatives.