Publications by authors named "Rui Krause"

Herein, we investigated the phytochemical composition and antibacterial activities of the organic layers from biosynthesized silver nanoparticles (AgNPs). AgNPs were synthesized using and extracts. UV-vis absorption in the 400-450 nm range indicated surface plasmonic resonance peak of AgNPs.

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  • Triple-negative breast cancer (TNBC) lacks key hormone receptors, leading to high recurrence and mortality, creating a strong demand for better treatment options.
  • Innovative strategies like nanoparticles are being researched for TNBC treatment, offering unique properties that enhance drug delivery and targeting.
  • The manuscript reviews the latest advancements in nanomaterials, including liposomes and gold nanoparticles, highlighting their potential as effective anticancer agents and in improving drug delivery systems for TNBC.
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Malaria is one of the most devastating diseases across the globe, particularly in low-income countries in Sub-Saharan Africa. The increasing incidence of malaria morbidity is mainly due to the shortcomings of preventative measures such as the lack of vaccines and inappropriate control over the parasite vector. Additionally, high mortality rates arise from therapeutic failures due to poor patient adherence and drug resistance development.

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Na-l-Thyroxine (Na-l-Thy) is a frequently prescribed synthetic hormone for hypothyroidism treatment. Despite its efficacy, its hydrophobic nature poses a challenge for achieving optimal bioavailability. To address this, researchers explored various delivery methods, including micro-formulations and nano-formulations, for precise and prolonged release of hydrophobic and hydrophilic drugs.

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  • DC is a medicinal plant from the Fabaceae family, used for various health issues like stomach problems, malaria, and breast milk stimulation.
  • Column chromatography of the plant's stem bark led to the isolation of eight chemical compounds, with their structures analyzed using NMR, IR, and MS techniques.
  • Testing showed that most compounds had low toxicity in breast cancer and non-cancerous cell lines, but one compound, (3)-3-acetoxyolean-12-en-28-oic acid, was more toxic to hormone receptor-positive breast cancer cells than to non-cancerous cells.
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Ethnopharmacological Relevance: In recent times the decriminalisation of cannabis globally has increased its use as an alternative medication. Where it has been used in modern medicinal practises since the 1800s, there is limited scientific investigation to understand the biological activities of this plant.

Aim Of The Study: Dipeptidyl peptidase IV (DPP-IV) plays a key role in regulating glucose homeostasis, and inhibition of this enzyme has been used as a therapeutic approach to treat type 2 diabetes.

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A novel class of bioactive complexes (1-3) [M(L)(bpy)], where, L = 2-(4-morpholinobenzylideneamino)phenol, bpy = 2,2'-bipyridine, M = Mn (1), Co (2) or Ni (3), were assigned to octahedral geometry based on analytical and spectral measurements. Gel electrophoresis showed that complex (2) demonstrated significant DNA cleavage activity compared to the other complexes under the action of oxidation agent (HO). The DNA binding constant properties measured by various techniques were in the following sequence: (2) > (3) > (1) > (), which suggests that the complexes might intercalate DNA, a possibility that is also supported by their biothermodynamic characteristics.

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A carboxylic acid, an aldehyde, and an isonitrile were combined in a single step (Passerini reaction) under mechanochemical activation to produce several α-acyloxycarboxamide derivatives in high to excellent yields within 15 min of milling. Mechanochemistry, when combined with the diversity provided by multicomponent reactions, enables the efficient synthesis of the target compounds, with great atom economy, shorter reaction times, and experimental simplicity. The method allows for the rapid production of a vast library of complex compounds from a limited number of substrates.

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Spirocyclic scaffolds are found in many pharmacologically active natural and synthetic compounds. From time to time, efforts have been made to develop new or better processes for the synthesis of spirocyclic compounds. Spiro [Indole-pyrrolidine] Derivatives are readily synthesized in high to excellent yields by the Michael condensation of 3-dicyanomethylene-2H-indol-2-ones (produced via the Knoevenagel condensation of indole-2,3-dione with malononitrile) with isothiocyanate derivatives under aqueous and mechanochemical conditions.

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A new simple, efficient, and environmentally friendly protocol is presented for the catalytic synthesis of α-acyloxycarboxamides using -formamides as a carbonyl precursor under aqua and mechanochemical conditions. Immobilized sulfuric acid on silica gel was employed for the synthesis of desired products, the reaction of benzoic acid, 1-napthylisocyanide and various heterocyclic -formamides. After a careful optimization of the reaction conditions, the desired Passerini products were obtained in high to excellent yields in short reaction times (10-30 min) at room temperature.

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Novel constructed bioactive mixed-ligand complexes () [Cu(L)(phen)] and () [Zn(L)(phen)] {where, L = 2-(4-morpholinobenzylideneamino)phenol), phen = 1,10-phenanthroline} have been structurally analysed by various analytical and spectroscopic techniques, including, magnetic moments, thermogravimetric analysis, and X-ray crystallography. Various analytical and spectral measurements assigned showed that all complexes appear to have an octahedral geometry. Agar gel electrophoresis's output demonstrated that the Cu(II) complex () had efficient deoxyribonucleic cleavage and complex () demonstrated the partial cleavage accomplished with an oxidation agent, which generates spreadable OH through the Fenton type mechanism.

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A new class of pharmacologically active mixed-ligand complexes (-) [M(L) (bpy)], where  = 2-(4-morpholinobenzylideneamino)phenol), bpy = 2,2'-bipyridine, M = Cu (), and Zn (), were assigned an octahedral geometry by analytical and spectral measurements. Gel electrophoresis showed that complex () demonstrated the complete DNA cleavage mediated by HO. The overall DNA-binding constants observed from UV-vis, fluorometric, hydrodynamic, and electrochemical titrations were in the following sequence: () > () > (), which suggests that the complexes might intercalate DNA, a possibility that is further supported by the biothermodynamic characteristics.

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  • - A new, efficient method for making isocyanides involves dehydrating formamides using phosphorus oxychloride and triethylamine as a solvent at low temperatures (0 °C) and takes less than 5 minutes.
  • - This protocol results in high yields of pure isocyanides and allows for quick access to various functionalized versions.
  • - The approach is safer, generates less waste, and is more environmentally friendly compared to older methods of synthesizing isocyanides.
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The application of immobilized sulfuric acid on silica gel (HSO-SiO) as an efficient and easily reusable solid catalyst was explored in the synthesis of novel α-acyloxycarboxamide derivatives via a Passerini reaction of benzoic acid, aldehyde/ketone, and isocyanides. The Passerini adducts were obtained in high to excellent yields within 10 min in aqueous media under catalytic conditions. The key advantages of the process include a short reaction time, high yields, the catalyst's low cost, and the catalyst's reusability.

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The aim of this study was to identify bioactive secondary metabolites from with potential inhibitory effects against HIV and phytochemical study of root barks resulted in the identification of three new biflavonoids (-), along with four known ones (-). Compound (Gerontoisoflavone A) was a single flavonoid present in the rootbark of the plant and was used as a reference. Compound (IC = 0.

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  • Over the last century, the average age for puberty has been declining, potentially due to food additives impacting health and early sexual maturation.
  • A study tested the effects of the food dye tartrazine on immature female Wistar rats, looking at parameters like vaginal opening and reproductive organ weight after 40 days of administration.
  • Results showed that the highest dose of tartrazine led to earlier vaginal opening and increased levels of reproductive hormones, suggesting a significant disruption in the normal puberty process and linking it to the rise in early puberty in girls consuming processed foods.
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The biological activities of dehydrocostus lactone and its analogues are suggested to be mediated by the lactone ring and α,β-methylene-γ-lactone. However, few studies exist on the structure-activity relationship of 13-amino derivatives of dehydrocostus latone. In this study new 13-amino derivatives of dehydrocostus lactone DHLC (1-4) were synthesized through Michael addition reactions, and were screened against three different breast cancer cell lines, namely hormone receptor positive breast cancer (MCF-7), triple-negative breast cancer (HCC70), and non-tumorigenic mammary epithelial (MCF-12A) cell lines.

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A novel series of metal(II) complexes (1-5) [M(L)]{Where M = Cu (1), Co (2), Mn (3), Ni (4) and Zn (5)} constructed from 2-(4-morpholinobenzylideneamino)phenol Schiff base ligand (HL) in a 1:2 M ratio and the spectral and analytical results put forward square planar geometry. Spectro-electrochemical, hydrodynamic, gel electrophoresis, and DNA binding/cleavage results for all the compounds demonstrate that complex (1) had excellent DNA binding/cleavage properties compared to other compounds. The observation also suggests that test compounds could intercalate with DNA, and the biothermodynamic property more strongly supports the stabilizing of the double helix DNA with the complexes.

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A previously unreported gallocatechin glycoside, (2 ,3) 4'--methyl-gallocatechin-3--α-ʟ-rhamnopyranoside () and an unseparable mixture of two previously undescribed dihydromyricetin glycosides, (2 ,3) 4'--methyl-dihydromyricetin-3--α-ʟ-rhamnopyranoside () and (2 ,3) 4'--methyl-dihydromyricetin-3--α-ʟ-rhamnopyranoside () along with three known compounds were isolated from the -butanol soluble fraction of the stem bark of Oliv. Their structures were elucidated by detailed spectroscopic analyses, including H NMR, C NMR, H-H COSY, HSQC, HMBC, NOESY, HR-ESI-MS and chemical methods. The crude ethanol extract, the fractions, and some of the isolated compounds were screened for their antioxidant and antibacterial activities.

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Despite their incredible contribution to fighting viral infections, antiviral viral resistance is an increasing concern and often arises due to unfavorable physicochemical and biopharmaceutical properties. To address this kind of issue, lipid nanocapsules (LNC) are developed in this study, using efavirenz (EFV) as a drug model. EFV solubility was assessed in water, Labrafac Lipophile and medium chain triglycerides oil (MCT oil).

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In the search for convenient, green, and practical catalytic methods for the current interest in organic synthesis, a simple, green, and highly efficient protocol for -formylation of various amines was carried out in the presence of immobilized sulfuric acid on silica gel (HSO-SiO). All reactions were performed in refluxing triethyl orthoformate (65 °C). The product formamides were obtained with high-to-excellent yields within 4 min to 2 h.

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Microbial infections are leading causes of death and morbidity all over the world due to the development of the resistance to antibiotics by certain microorganisms. In this study, the chemical exploration of the ethanol (EtOH) extract of the aerial part of (Dracaenaceae) led to the isolation of one previously unreported chalcone derivative, i.e.

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Metallic nanoparticles (MNPs) produced by green synthesis using plant extracts have attracted huge interest in the scientific community due to their excellent antibacterial, antifungal and antibiofilm activities. To evaluate these pharmacological properties, several methods or protocols have been successfully developed and implemented. Although these protocols were mostly inspired by the guidelines from national and international regulatory bodies, they suffer from a glaring absence of standardization of the experimental conditions.

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Ethnopharmacological Relevance: Monsonia angustifolia is traditionally used to treat anthrax, heartburn, diarrhea, eye infections and hemorrhoids. Dodonaea angustifolia is frequently used as a treatment for dental pain, microbial infections and jungle fever. The two plant species were selected due to the presence of secondary metabolites such as coumarins, flavonoids, terpenoids, saponins and polyphenolics from the crude extracts, which exhibit pharmacological significance.

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Background: Euphorbia grandicornis is widely utilized in traditional medicine for the treatment of microbial infections including sexually transmitted diseases such as syphilis, gonorrhoea and for healing of wounds.

Objective: The aim of this work was to isolate and evaluate the antibacterial and anticancer activities of Euphorbia grandicornis chemical constituents.

Methods: Chemical constituents were isolated and identified using various spectroscopic techniques such as IR, MS, and NMR.

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