In Vitro Antiproliferative Activity and Phytochemicals Screening of Extracts of the Freshwater Microalgae, Chlorochromonas danica

Constant mutations of SARS-CoV-2 from 2019 to the present commences potential dilemma to the efficacy of developed COVID-19 antiviral drugs. In this current report, series of 3-phenyl(alkylamino)methyl-4-hydroxycoumarin was identified as compounds of drug-likeliness that, through molecular docking simulations, also demonstrated favourable binding to different sites of the SARS-CoV-2 RBD/hACE2 complex. This was achieved by varying the chain of the alkyl length and the substituent of the phenyl moiety. The subjected 3-phenyl(alkylamino)methyl-4-hydroxycoumarin compounds were successfully synthesized by a catalyst-free multicomponent condensation reaction of 4-hydroxycoumarin, p-substituted benzaldehyde, and linear alkyl amines in dichloromethane (DCM) at 22 °C. The crude products were achieved in a moderate (40–50 %) to a very good (80–90 %) yield with excellent purity without the need for chemical purification verified by nuclear magnetic resonance (NMR) spectroscopy. The simple method to produce 3-phenyl(alkylamino)methyl-4-hydroxycoumarin and the preliminary docking results present an opportunity for advancement in drug discovery. 

https://onlinelibrary.wiley.com/doi/pdfdirect/10.1002/slct.202300519

Extending the Library of 4‐Hydroxycoumarin Derivatives with Potential Pharmacological Activity by a Catalyst‐Free and Purification‐Free Method

In advanced biotechnology, the utilization of enzymes to achieve new or modified compounds with antibacterial, fungicidal, and anti-cancer specifications is crucial. Mushroom lactases are a hopeful biocatalyst for the synthesis and modification of different compounds. They are an accessible and inexpensive enzyme for the preparation of reaction objects and have recently received attention. Laccase purification was performed from basidiomycete Lentinus strigosus ( LS) in several stages: Stage 1. On ion-exchange chromatography on TEAE Servacell 23 (400 ml), two distinctly separated laccase activity peaks were observed, eluted from the carrier at 0.21 and 0.27 M NaCl. In order to reduce the loss of enzymes, all fractions with laccase activity were collected, concentrated, and desalted using an ultrafiltration cell (Amicon, United States) with a UM-10 membrane. Stage 2. The resulting preparation with laccase activity was applied to a Q-Sepharose column (60 ml). Two well-separated peaks with laccase activity were obtained during the elution: laccase I (0.12 M NaCl) and laccase II (0.2 M NaCl). Stage 3. In the course of further purification of both enzymes, carried out on anion-exchange carrier Resource Q (6 ml), a broken gradient was used: 0 - 10%, 10 - 20%, and 20 - 100% with 1M NaCl. Stage 4. Both laccase I and laccase II, obtained after Resource Q, were desalted, concentrated to 1 ml each, and applied to a Superdex 75 gel filtration column. As a result, two laccases were obtained in a homogeneous form. lacase II Etapa no purificação adicional enzimas, realizada I obtidas após Recurso concentradas aplicadas

Testing for the ability to modify antibiotics of Panus tigrinus 8/18 Lentinus strigosus 1566 laccase

In advanced biotechnology, the utilization of enzymes to achieve new or modified compounds with antibacterial, fungicidal, and anti-cancer specifications is crucial. Mushroom lactases are a hopeful biocatalyst for the synthesis and modification of different compounds. They are an accessible and inexpensive enzyme for the preparation of reaction objects and have recently received attention. Laccase purification was performed from basidiomycete Lentinus strigosus (LS) in several stages: Stage 1. On ion-exchange chromatography on TEAE Servacell 23 (400 ml), two distinctly separated laccase activity peaks were observed, eluted from the carrier at 0.21 and 0.27 M NaCl. In order to reduce the loss of enzymes, all fractions with laccase activity were collected, concentrated, and desalted using an ultrafiltration cell (Amicon, United States) with a UM-10 membrane. Stage 2. The resulting preparation with laccase activity was applied to a Q-Sepharose column (60 ml). Two well-separated peaks with laccase activity were obtained during the elution: laccase I (0.12 M NaCl) and laccase II (0.2 M NaCl). Stage 3. In the course of further purification of both enzymes, carried out on anion-exchange carrier Resource Q (6 ml), a broken gradient was used: 0 - 10%, 10 - 20%, and 20 - 100% with 1M NaCl. Stage 4. Both laccase I and laccase II, obtained after Resource Q, were desalted, concentrated to 1 ml each, and applied to a Superdex 75 gel filtration column. As a result, two laccases were obtained in a homogeneous form.

Testing for the ability to modify antibiotics of Panus tigrinus 8/18 Lentinus strigosus 1566 laccase.

In vitro and in silico antibacterial evaluation of coumarin derivatives against MDR strains of Staphylococcus aureus and Escherichia coli.

The 4-Hydroxycoumarin derivatives are known to show a broad spectrum of pharmacological applications. In this paper we are reporting the synthesis of a new series of 4-Hydroxycoumarin derivatives synthesized through Knovenegal condensation; they were characterized by using UV-Vis, FT-IR, NMR spectroscopies. The synthesized compounds were evaluated for antibacterial activity against Staphylococcus aureus and Salmonella typhimurium strains. The compounds (2), (3) and (8) showed favorable antibacterial activity with zone of inhibitions 26.5± 0.84, 26.0 ± 0.56 and 26.0 ± 0.26 against Staphylococcus aureus (Gram-positive) respectively. However, the compounds (5) and (9) were found more active with 19.5 ± 0.59 and 19.5 ± 0.32 zone of inhibitions against Salmonella typhimurium (Gram-negative). Whereas, in urease inhibition assay, none of the synthesized derivatives showed significant anti-urease activity; although, in carbonic anhydrase-II inhibition assay, the compound (2) and (6) showed enzyme inhibition activity with IC50 values 263±0.3 and 456±0.1, respectively.

/pdf/enzyme-inhibition-and-antibacterial-potential-of-4-1bky56gqin.pdf

Enzyme inhibition and antibacterial potential of 4-Hydroxycoumarin derivatives

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Enzyme inhibition and antibacterial potential of 4-Hydroxycoumarin derivatives