Bioactive brominated oxindole alkaloids from the Red Sea sponge Callyspongia siphonella

In the present study, LC-HRESIMS-assisted dereplication along with bioactivity-guided isolation led to targeting two brominated oxindole alkaloids (compounds 1 and 2) which probably play a key role in the previously reported antibacterial, antibiofilm, and cytotoxicity of Callyspongia siphonella crude extracts. Both metabolites showed potent antibacterial activity against Gram-positive bacteria, Staphylococcus aureus (minimum inhibitory concentration (MIC) = 8 and 4 µg/mL) and Bacillus subtilis (MIC = 16 and 4 µg/mL), respectively. Furthermore, they displayed moderate biofilm inhibitory activity in Pseudomonas aeruginosa (49.32% and 41.76% inhibition, respectively), and moderate in vitro antitrypanosomal activity (13.47 and 10.27 µM, respectively). In addition, they revealed a strong cytotoxic effect toward different human cancer cell lines, supposedly through induction of necrosis. This study sheds light on the possible role of these metabolites (compounds 1 and 2) in keeping fouling organisms away from the sponge outer surface, and the possible applications of these defensive molecules in the development of new anti-infective agents

Pharmacological Efficacy of Ginseng against Respiratory Tract Infections

Respiratory tract infections are underestimated, as they are mild and generally not incapacitating. In clinical medicine, however, these infections are considered a prevalent problem. By 2030, the third most comprehensive reason for death worldwide will be chronic obstructive pulmonary disease (COPD), according to the World Health Organization. The current arsenal of anti-inflammatory drugs shows little or no benefits against COPD. For thousands of years, herbal drugs have been used to cure numerous illnesses; they exhibit promising results and enhance physical performance. Ginseng is one such herbal medicine, known to alleviate pro-inflammatory chemokines and cytokines (IL-2, IL-4, IFN-γ, TNF-α, IL-5, IL-6, IL-8) formed by macrophages and epithelial cells. Furthermore, the mechanisms of action of ginsenoside are still not fully understood. Various clinical trials of ginseng have exhibited a reduction of repeated colds and the flu. In this review, ginseng’s structural features, the pathogenicity of microbial infections, and the immunomodulatory, antiviral, and anti-bacterial effects of ginseng were discussed. The focus was on the latest animal studies and human clinical trials that corroborate ginseng’s role as a therapy for treating respiratory tract infections. The article concluded with future directions and significant challenges. This review would be a valuable addition to the knowledge base for researchers in understanding the promising role of ginseng in treating respiratory tract infections. Further analysis needs to be re-focused on clinical trials to study ginseng’s efficacy and safety in treating pathogenic infections and in determining ginseng-drug interactions

Bioactive glucitol-core containing gallotannins and other phytochemicals from silver maple (acer saccharinum) leaves

In the course of our group\u27s investigation of members of the maple (Acer) genus, a series of glucitol-core containing gallotannins (GCGs) were isolated and identified (by NMR and HREISMS). Among higher plants, only certain maple species are known to produce GCGs, compounds with potential nutraceutical and cosmetic applications due to their reported antioxidant, antidiabetic, anti-α-glucosidase, anti-glycation, anticancer, and skin health promoting effects. Herein, we sought to investigate whether the previously un-investigated silver maple (Acer saccharinum) species was also a source of GCGs. Nine phenolic compounds, including six GCGs, were identified (by HPLC-DAD analyses using previously isolated standards) as ginnalins A-C (1-3), maplexins B, D, and F (4-6), methyl syringate (7), methyl gallate (8), and 3-methoxy-4-hydroxyphenol-1-β-D-(6-galloyl)-glucopyranoside (9). In addition, one sesquiterpenoid, namely, pubineroid A (10), was isolated and identified (by NMR)

Intravenous Nanocarrier for Improved Efficacy of Quercetin and Curcumin against Breast Cancer Cells: Development and Comparison of Single and Dual Drug–Loaded Formulations Using Hemolysis, Cytotoxicity and Cellular Uptake Studies

The present work highlights the suitability of an oil-based nanocarrier to deliver quercetin (Q) and curcumin (C) through the intravenous route for treatment of breast cancer. The nanoemulsion prepared by the modified emulsification-solvent evaporation method resulted in particle size (p ˃ 0.05) and demonstrated the biocompatibility of the nanoemulsion with human blood. In vitro cytotoxic potential of single and dual drug–loaded nanoemulsions were determined against breast cancer cells (MF-7). The IC50 value for QNE and CNE were found to be 40.2 ± 2.34 µM and 28.12 ± 2.07 µM, respectively. The IC50 value for QC-NE was 21.23 ± 2.16 µM and demonstrated the synergistic effect of both the drugs. The internalization of the drug inside MF-7 cells was detected by cellular uptake study. The cellular uptake of QNE and CNE was approximately 3.9-fold higher than free quercetin and curcumin (p < 0.0001). This strategically designed nanoemulsion appears to be a promising drug delivery system for the proficient primary preclinical development of quercetin and curcumin as therapeutic modalities for the treatment of breast cancer

Synthesis, Antimicrobial Screening, Homology Modeling, and Molecular Docking Studies of a New Series of Schiff Base Derivatives as Prospective Fungal Inhibitor Candidates

Twelve new Schiff base derivatives have been prepared by the condensation reaction of different amino substituted compounds (aniline, pyridin-2-amine, o-toluidine, 2-nitrobenzenamine, 4-aminophenol, and 3-aminopropanol) and substituted aldehydes such as nicotinaldehyde, o,m,p-nitrobenzaldehyde, and picolinaldehyde in ethanol using acetic acid as a catalyst. The envisaged structures of the all the synthesized ligands have been confirmed on the basis of their spectral analysis FT-IR, mass spectroscopy, 1H- and 13C-NMR. In vitro screening of their antibacterial and antifungal potential against Escherichia coli bacterium and Fusarium oxysporum f.sp albedinis (F.o.a) fungus, respectively, revealed that all the ligands showed no significant antibacterial activity, whereas most of them displayed good antifungal activity. Homology modeling and docking analysis were performed to explain the antifungal effect of the most and least active compound against two F.o.a fungus proteins

Bioprocessing of Agro-Industrial Waste for Maximization of Pectinase Production by a Novel Native Strain <i>Aspergillus cervinus</i> ARS2 Using Statistical Approach

The demand for microbial pectinase has increased due to its vast applications in different industries. The current study dealt with the synthesis of pectinase by a novel native strain Aspergillus cervinus ARS2 using agro-industrial waste. Comparative studies conducted on pectinase production by submerged fermentation (SmF) and solid-state fermentation (SSF) showed that pectinase activity was more increased in SSF (44.51 ± 1.33 IU/mL) than in SmF (40.60 ± 1.15 IU/mL) when using orange peel as a substrate. Using SSF, one-factor-at-a-time (OFAT) studies were conducted, considering different process variables such as inoculum size, initial pH, incubation time, moisture content, incubation temperature, and substrate particle size, all of which affected the pectinase activity. OFAT results showed the highest pectinase activity at an inoculum size of 106 spores/mL (43.11 ± 1.06 U/mL), an incubation time of 6 days (43.81 ± 1.21 U/mL), a moisture content of 100% (44.30 ± 1.69 U/mL), a substrate particle size of 1.7 mm (42.06 ± 1.20 U/mL), an incubation temperature of 37 °C (45.90 ± 1.33 U/mL), and an initial pH of 4 (43.31 ± 0.89 U/mL). The identified significant process variables were then optimized by response surface methodology (RSM)-central composite design (CCD). The results showed optimum pectinase activity of 107.14 ± 0.71 IU/mL for a substrate particle size of 2 mm, an incubation temperature of 31.5 °C, an initial pH of 4.9, and a moisture content of 107%, which was obtained from the Minitab optimizer. By using statistical optimization, the pectinase production from the isolated novel fungal strain A. cervinus ARS2 was increased 2.38-fold. Therefore, the A. cervinus ARS2 strain can be further explored for large-scale pectinase production which could meet the growing industrial demands