Extraction, Characterization, and Evaluation of the Cytotoxic Activity of Piperine in Its Isolated form and in Combination with Chemotherapeutics against Gastric Cancer

Molecules, Год журнала: 2023, Номер 28(14), С. 5587 - 5587

Опубликована: Июль 22, 2023

Gastric cancer is one of the most frequent types neoplasms worldwide, usually presenting as aggressive and difficult-to-manage tumors. The search for new structures with anticancer potential encompasses a vast research field in which natural products arise promising alternatives. In this scenario, piperine, an alkaloid Piper species, has received attention due to its biological activity, including attributes. present work proposes three heating-independent, reliable, low-cost, selective methods obtaining piperine from nigrum L. (Black pepper). Electronic (SEM) optical microscopies, X-ray diffraction, nuclear magnetic resonance spectroscopies (13C 1H NMR), (UV–Vis, photoluminescence, FTIR) confirm obtention crystals. MTT assay reveals that samples exhibit good cytotoxic activity against primary metastasis models gastric cell lines Brazilian Amazon. showed cytotoxicity on evaluated models, revealing higher effectiveness cells bearing degree aggressiveness. Moreover, investigated crystals demonstrated ability act enhancer when combined traditional chemotherapeutics (5-FU GEM), allowing drugs achieve same effect employing lower concentrations. These results establish molecule therapy investigations cancer, both isolated form or bioenhancer.

Язык: Английский

---

Bioprospecting of Natural Compounds for Industrial and Medical Applications

Опубликована: Июнь 25, 2021

Bioprospecting is the investigation of biodiversity to search new resources commercial value. The bioprospecting program includes scientific and economic activities that explore genes, organisms, species in diverse habitats ecosystem while safeguarding conservation, traditional knowledge, growth local communities. natural products obtained from have contributed immensely medicinal agricultural fields recently bioremediation, biomimetic engineering, aquaculture, nanotechnology fields. These include pharmaceuticals, industrial chemicals, metabolic pathways, behaviors, materials. They are used as such product development or may be physical blueprints designs leads. Since involves worldwide activities, ethical legal issues also addressed prevent biopiracy other malpractices. In this chapter, we will discuss about bioprospecting, rational processes, their drawbacks, approaches advance utility agricultural, medical,

Язык: Английский

---

Comparison of In Vitro Approaches to Assess the Antibacterial Effects of Nanomaterials

Journal of Functional Biomaterials, Год журнала: 2022, Номер 13(4), С. 255 - 255

Опубликована: Ноя. 19, 2022

The antibacterial properties of nanomaterials (NMs) can be exploited in a range consumer products (e.g., wound dressings, food packaging, textiles, medicines). There is also interest the exploitation NMs as treatments for infectious diseases to help combat antibiotic resistance. Whilst activity has been assessed vitro and vivo numerous studies, methodology used very varied. Indeed, while approaches are available assess effect vitro, they have not yet systematically their suitability sensitivity testing NMs. It therefore timely consider what assays should prioritised screen majority existing studies focused on investigating effects exhibited by silver (Ag) employed limited assays. We compared copper oxide (CuO) Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis at various concentrations (12.5–200 µg/mL) using battery tests (well disc diffusion, plate counts—time-kill method, optical density measurement—OD, Alamar Blue live/dead viability assays, quantitative polymerase chain reaction). CuO were most toxic B. E. P. aeruginosa was least sensitive strain. All detected NMs; however, varied sensitivity, time, cost, technical difficulty requirement specialized equipment. In future, we suggest that combination provide robust assessment particular, recommend time-kill OD due greater sensitivity. standard operating protocols developed so harmonised approach.

Язык: Английский

---

Discovery of furopyridine-based compounds as novel inhibitors of Janus kinase 2: In silico and in vitro studies

International Journal of Biological Macromolecules, Год журнала: 2024, Номер 260, С. 129308 - 129308

Опубликована: Янв. 11, 2024

Язык: Английский

---

Cassia alata L.: A Study of Antifungal Activity against Malassezia furfur, Identification of Major Compounds, and Molecular Docking to Lanosterol 14-Alpha Demethylase

Pharmaceuticals, Год журнала: 2024, Номер 17(3), С. 380 - 380

Опубликована: Март 16, 2024

Empirically, in Indonesia, the leaves of Cassia alata L. (candle bush or ketepeng cina) have been used as a topical antifungal agent. Malassezia furfur is natural microorganism found human body. It among factors contributing to conditions such pityriasis versicolor, common, benign, superficial fungal infection skin that closely associated with seborrheic dermatitis and dandruff. This study aimed explore C. leaves, starting from determining activity against M. identification major compounds ethyl acetate n-hexane fractions, then we carried out molecular docking fraction lanosterol 14-alpha demethylase. The method was disc diffusion technique test activity, LC-MS/MS for compound identification, homology modeling through Swiss Models docking. fractions extract showed concentration-dependent furfur. LCMS/MS analysis revealed five fractions. demonstrated highest binding affinity stearidonic acid at −7.2 kcal/mol. can be concluded furfur, supported by both vitro silico studies.

Язык: Английский

---

Total Synthesis of Mycinolide IV and Path‐Scouting for Aldgamycin N

Angewandte Chemie International Edition, Год журнала: 2021, Номер 60(14), С. 7893 - 7899

Опубликована: Янв. 15, 2021

Abstract Proof‐of‐concept is provided that a large estate of 16‐membered macrolide antibiotics can be reached by “unified” approach. The key building block was formed on scale an asymmetric vinylogous Mukaiyama aldol reaction; its alkene terminus then converted either into the corresponding methyl ketone Wacker oxidation or chain‐extended aldehyde catalyst‐controlled branch‐selective hydroformylation. These transformations ultimately opened access to two structurally distinct series targets. Notable late‐stage maneuvers comprise rare example ruthenium‐catalyzed redox isomerization 1,3‐enyne‐5‐ol 1,3‐diene‐5‐one derivative, as well elaboration tertiary propargylic alcohol acyloin trans ‐hydrostannation/Chan‐Lam‐type coupling. Moreover, this case study illustrates underutilized possibility forging complex macrolactone rings transesterification under essentially neutral conditions.

Язык: Английский

---

Potential of supercritical fluid myrtle extracts as an active ingredient and co-preservative for cosmetic and topical pharmaceutical applications

Sustainable Chemistry and Pharmacy, Год журнала: 2022, Номер 28, С. 100739 - 100739

Опубликована: Июнь 11, 2022

This study investigated the applications of a myrtle extract obtained by supercritical fluid extraction (SFE), technique considered environmentally friendly, as possible antimicrobial ingredient in cosmetic and pharmaceutical formulations. The was at 230 bar 45 °C, for 2 h, with flow CO2 0.3 kg h−1. A cosolvent (ethanol) also used, 0.09 extracts thus were tested against seven Gram-positive bacteria one yeast using well diffusion broth dilution techniques. results showed that exhibits good antibacterial activity all strains studied is superior to most those conventional methods. Antifungal present but lesser extent. Cell viability studies carried out exposing HaCat cells range concentrations, from 0.1 μg/mL up 60 24 MTT assay. Salmonella mutagenicity assay applied evaluate antimutagenicity extract. suggest green solvent, CO2, safe could reduce genotoxic damage induced reactive oxygen species (ROSs).

Язык: Английский

---

Construction and characterization of two SARS‐CoV‐2 minigenome replicon systems

Journal of Medical Virology, Год журнала: 2022, Номер 94(6), С. 2438 - 2452

Опубликована: Фев. 9, 2022

The ongoing COVID-19 pandemic severely impacts global public health and economies. To facilitate research on severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virology antiviral discovery, a noninfectious viral replicon system operating under biosafety level containment is warranted. We report herein the construction characterization of two SARS-CoV-2 minigenome systems. First, we constructed IVT-CoV2-Rep complementary DNA template to generate messenger RNA (mRNA) with nanoluciferase (NLuc) reporter via in vitro transcription (IVT). mRNA transfection assay demonstrated rapid transient replication variety cell lines, which could be completely abolished by known inhibitors. Our data also suggest that phenotype not due host innate responses. In addition, have developed DNA-launched BAC-CoV2-Rep, supports in-cell as initial template. BAC-CoV2-Rep exhibited much stronger longer signal compared version. found portion NLuc was derived from spliced resistant treatment, especially during early phase after transfection. summary, established systems are suitable for basic research, hold promise stable line development further optimization.

Язык: Английский

---

Multifunctional nanoreactors with nutrient consumption and ROS generation capabilities for antibacterial and skin repair

Journal of Materials Chemistry B, Год журнала: 2022, Номер 10(42), С. 8664 - 8671

Опубликована: Янв. 1, 2022

Bacterial wound infection has brought a serious threat to human health and caused huge economic losses. Attempts develop biomaterials with excellent antibacterial effects are meaningful promote healing. Herein, we report multifunctional nanoreactor nutrient consumption reactive oxygen species (ROS) generation capabilities for skin repair. The was constructed by the encapsulation of glucose oxidase (GOx) into Cu2+-doped zeolite-based imidazole framework (ZIF-8) through one-pot synthesis method. not only consumes nutrients bacteria GOx-driven oxidation reaction, but also generates highly toxic hydroxyl radicals (˙OH) kill via Cu+-mediated Fenton-like reaction. Moreover, Zn2+ released from is capable exhibiting synergistic activity. In addition mediating reactions, Cu2+ promotes angiogenesis accelerate Thus, ability cut off supply starve bacteria, produce ROS healing, enabling it be promising treatment infection.

Язык: Английский

---

Overview on Strategies and Assays for Antibiotic Discovery

Pharmaceuticals, Год журнала: 2022, Номер 15(10), С. 1302 - 1302

Опубликована: Окт. 21, 2022

The increase in antibiotic resistance poses a major threat to global health. Actinomycetes, the Gram-positive bacteria of order Actinomycetales, are fertile producers bioactive secondary metabolites, including antibiotics. Nearly two-thirds antibiotics that used for treatment bacterial infections were originally isolated from actinomycetes strains belonging genus Streptomyces. This emphasizes importance discovery. However, identification new antimicrobial compound and exploration its mode action very challenging tasks. Therefore, different approaches enable “detection” an characterization mechanisms leading biological activity indispensable. Beyond bioinformatics tools facilitating biosynthetic gene clusters (BGCs), whole cell-screenings—in which cells exposed actinomycete-derived compounds—are common strategy applied at early stage drug development. More recently, target-based have been established. In this case, candidates tested interactions with usually validated targets. review focuses on bioactivity-based screening methods provides readers overview most relevant assays investigation action. Moreover, article includes examples successful application these suggestions improvement.

Язык: Английский

---