Chemoenzymatic Synthesis of Complex Phenylpropanoid Derivatives by the Botrytis cinerea Secretome and Evaluation of Their Wnt Inhibition Activity

In this study, a series of complex phenylpropanoid derivatives were obtained by chemoenzymatic biotransformation of ferulic acid, caffeic acid, and a mixture of both acids using the enzymatic secretome of Botrytis cinerea. These substrates were incubated with fungal enzymes, and the reactions were monitored using state-of-the-art analytical methods. Under such conditions, a series of dimers, trimers, and tetramers were generated. The reactions were optimized and scaled up. The resulting mixtures were purified by high-resolution semi-preparative HPLC combined with dry load introduction. This approach generated a series of 23 phenylpropanoid derivatives, 11 of which are described here for the first time. These compounds are divided into 12 dimers, 9 trimers (including a completely new structural scaffold), and 2 tetramers. Elucidation of their structures was performed with classical spectroscopic methods such as NMR and HRESIMS analyses. The resulting compound series were analyzed for anti-Wnt activity in TNBC cells, with several derivatives demonstrating specific inhibition.

Sustainable phyto-fabrication of silver nanoparticles using Gmelina arborea exhibit antimicrobial and biofilm inhibition activity

Increase in bacterial resistance to commonly used antibiotics is a major public health concern generating interest in novel antibacterial treatments. Aim of this scientific endeavor was to find an alternative efficient antibacterial agent from non-conventional plant source for human health applications. We used an eco-friendly approach for phyto-fabrication of silver nanoparticles (AgNPs) by utilizing logging residue from timber trees Gmelina arborea (GA). GC–MS analysis of leaves, barks, flowers, fruits, and roots was conducted to determine the bioactive compounds. Biosynthesis, morphological and structural characterization of GA-AgNPs were undertaken by UV–Vis spectroscopy, scanning electron microscopy (SEM), energy-dispersive spectroscopy (EDX), transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FTIR) and X-ray diffractometer (XRD). GA-AgNPs were evaluated for antibacterial, antibiofilm, antioxidant, wound healing properties and their toxicity studies were carried out. Results identified the presence of terpenoids, sterols, aliphatic alcohols, aldehydes, and flavonoids in leaves, making leaf extract the ideal choice for phyto-fabrication of silver nanoparticles. The synthesis of GA-AgNPs was confirmed by dark brown colored colloidal solution and spectral absorption peak at 420 nm. Spherical, uniformly dispersed, crystalline GA-AgNPs were 34–40 nm in diameter and stable in solutions at room temperature. Functional groups attributed to the presence of flavonoids, terpenoids, and phenols that acted as reducing and capping agents. Antibacterial potency was confirmed against pathogenic bacteria Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus by disc diffusion assay, MIC and MBC assay, biofilm inhibition assay, electron-microscopy, cell staining and colony counting techniques. The results from zone of inhibition, number of ruptured cells and dead-cell-count analysis confirmed that GA-AgNPs were more effective than GA-extract and their bacteria inhibition activity level increased further when loaded on hydrogel as GA-AgNPs-PF127, making it a novel distinguishing feature. Antioxidant activity was confirmed by the free radical scavenging assays (DPPH and ABTS). Wound healing potential was confirmed by cell scratch assay in human dermal fibroblast cell lines. Cell-proliferation study in human chang liver cell lines and optical microscopic observations confirmed non-toxicity of GA-AgNPs at low doses. Our study concluded that biosynthesized GA-AgNPs had enhanced antibacterial, antibiofilm, antioxidant, and wound healing properties.

Synthesis, solid state self-assembly driven by antiparallel π⋯π stacking and {⋯H–C–C–F}2 dimer synthons, and in vitro acetyl cholinesterase inhibition activity of phenoxy pendant isatins

The phenoxy pendant isatins were observed to be highly potent inhibitors of acetylcholinesterase. In addition, the solid-state structure of a phenoxy pendant isatin showed an intriguing 1D-supramolecular self-assembled structure.

Uji Aktivitas Ekstrak Daun Dan Akar Singawalang (Petiveria alliaceae) Terhadap Penghambatan Tirosinase

Tyrosinase is an enzyme that plays a role in the formation of skin pigments from a person because it is involved in the process of melanogenesis. Tyrosinase plays a very important role in the skin depigmentation process, there are several attempts to inhibit the skin depigmentation process, one of which is by inhibiting tyrosinase. Research on the leaves and roots of singawalang (Petiveria alliacea) was conducted to determine the potential as a tyrosinase inhibitor. Leaves and root extracts of singawalang were macerated with ethanol, then tested for identification of secondary metabolites. Singawalang leaves extract contains alkaloids, tannins and terpenoids while singawalang root extract contains alkaloids, flavonoids, tannins and terpenoids. Tyrosinase inhibitory activity used the microplate reader ELISA technique at a wavelength of 492 nm. Tests were carried out on kojic acid as a comparison and L-DOPA as a substrate. The results of the tyrosinase inhibition activity test for the extracts of singawalang leaves, singawalang roots and kojic acid, IC50 were 9.817 mg / mL, 4.987 mg / mL and 0.092 mg / mL, respectively.

In-vitro antidiabetic activity of methanolic extract of leaves and fruits of Pouteria campechiana (Kunth) Baehni

Introduction and Aim: Herbal medicine have been used to treat several ailments since decades. Pouteria campechiana (Kunth) Baehni belongs to the family Sapotaceae which is widely found around the world. In folk medicine, various parts of P. campechiana is used to treat various illness. Inhibition of alpha-amylase and alpha-glucosidase enzymes can be an important strategy in management of postprandial blood glucose level in non-insulin dependent diabetic patient. Hence, present study focused to evaluate the in vitro antidiabetic activity of leaf and fruit methanolic extract of Pouteria campechiana (Kunth) Baehni. Materials and Methods: Methanolic extract of P. campechiana leaf (PCL) and fruit (PCF) was screened by biochemical assay such as ?-amylase inhibition activity by CNPG3 method (2-chloro-p-nitrophenyl-?-D-maltotrioside) and ?- glucosidase inhibition activity and in vitro cellular assay such as glucose uptake assay in 3T3-L1 cell line. Results: Methanolic extract of P. campechiana leaf and fruit showed inhibition of ??Amylase and ??Glucosidase enzymes. The methanolic extract of P. campechiana leaf and fruit at varying concentrations (?g/ml), did not exhibit cytotoxicity against 3T3-L1 cell line after 24 hours of incubation. The test compounds PCL and PCF induced the uptake of 2?(N?(7?Nitrobenz?2?oxa?1,3?diazol?4?yl) Amino) ? 2?Deoxyglucose (2-NBDG) in 3T3L1 cells. PCF and PCL both showed almost similar activity of standard drug, Metformin at higher concentrations. Conclusion: Based on the results, it can be concluded that methanolic leaf and fruit extract of P. campechiana possess antidiabetic activity.

Saccharobisindole, Neoasterric Methyl Ester, and 7-Chloro-4(1H)-quinolone: Three New Compounds Isolated from the Marine Bacterium Saccharomonospora sp.

Analysis of the chemical components from the culture broth of the marine bacterium Saccharomonospora sp. CNQ-490 has yielded three novel compounds: saccharobisindole (1), neoasterric methyl ester (2), and 7-chloro-4(1H)-quinolone (3), in addition to acremonidine E (4), pinselin (5), penicitrinon A (6), and penicitrinon E (7). The chemical structures of the three novel compounds were elucidated by the interpretation of 1D, 2D nuclear magnetic resonance (NMR), and high-resolution mass spectrometry (HRMS) data. Compound 2 generated weak inhibition activity against Bacillus subtilis KCTC2441 and Staphylococcus aureus KCTC1927 at concentrations of 32 μg/mL and 64 μg/mL, respectively, whereas compounds 1 and 3 did not have any observable effects. In addition, compound 2 displayed weak anti-quorum sensing (QS) effects against S. aureus KCTC1927 and Micrococcus luteus SCO560.

Evaluation of in-vitro Anti-Inflammatory Activity of Gallic Acid

Gallic acid's anti-inflammatory effect was studied at various concentrations, including 50,100,150,200, and 250 ug/ml. Gallic acid's anti-inflammatory effect was assessed using two in-vitro assays: proteinase inhibition and albumin denaturation. The greatest proteinase inhibition activity of 52.83 percent was achieved at a concentration of 250ug/ml, according to the results. It also revealed that at 250ug/ml, the maximum percentage inhibition in albumin denaturation was 74.79 percent. Gallic acid's antiproteinase and albumin denaturation activities both increase with increasing concentrations, according to this research. Keywords: Gallic acid, Anti-Inflammatory, In-Vitro Assays, Albumin Denaturation, Proteinase activity.