Optimization parameters for the production of dimer of epicatechin from an endophytic fungus Curvularia australiensis FC2AP using response surface methodology (RSM).

The search for natural therapeutic agents has intensified due to their potential to treat various diseases. Bioactive secondary metabolites from endophytes offer high therapeutic profiles and can be mass-produced after optimizing medium parameters and purification. This investigation aimed to maximize crude pigmented secondary metabolite (CPSM) production from Curvularia australiensis FC2AP by optimizing fermentation conditions statistically. The endophytic fungus produced a maximum yield of 8.81 UL/g from biomass using Sabouraud's Dextrose Broth. After screening essential factors, the Plackett-Burman design was used for factorial optimization, and the Box Behnken design was employed to investigate three significant factors. The final CPSM yield was 12.3 UL/g, approximately 4-fold higher than the preliminary growth medium. Chromatographic purification using a gradient solvent system resulted in six fractions, with the fourth fraction demonstrating the highest bioactivity profile. Structural characterization confirmed this fraction to be a dimer of epicatechin, which has anti-cancer properties, as confirmed through in vivo studies on Sprague Dawley rats. This is the first report of a epicatechin dimer produced from C. australiensis.

Promoting Spatial Charge Transfer of ZrO2 Nanoparticles: Embedded on Layered MoS2/g-C3N4 Nanocomposites for Visible-Light-Induced Photocatalytic Removal of Tetracycline.

Photocatalytic degradation is a sustainable technique for reducing the environmental hazards created by the overuse of antibiotics in the food and pharmaceutical industries. Herein, a layer of MoS2/g-C3N4 nanocomposite is introduced to zirconium oxide (ZrO2) nanoparticles to form a "particle-embedded-layered" structure. Thus, a narrow band gap (2.8 eV) starts developing, deliberated as a core photodegradation component. Under optimization, a high photocatalytic activity of 20 mg/L TC at pH 3 with ZrO2@MoS2/g-C3N4 nanocomposite was achieved with 94.8% photocatalytic degradation in 90 min. A photocatalytic degradation rate constant of 0.0230 min-1 is determined, which is 2.3 times greater than the rate constant for bare ZrO2 NPs. The superior photocatalytic activity of ZrO2@MoS2/g-C3N4 is due to the dual charge-transfer channel between the MoS2/g-C3N4 and ZrO2 nanoparticles, which promotes the formation of photogenerated e-/h+ pairs. Charge recombination produces many free electron-hole pairs, which aid photocatalyst reactions by producing superoxide and hydroxyl radicals via electron-hole pair generation. The possible mechanistic routes for TC were investigated in-depth, as pointed out by the liquid chromatography-mass spectrometry (LC-MS) investigation. Overall, this work shows that photocatalysis is a feasible sorbent approach for environmental antibiotic wastewater treatment.

Inhibition of New Delhi Metallo-ß-Lactamase 1 (NDM-1) Producing Escherichia coli IR-6 by Selected Plant Extracts and Their Synergistic Actions with Antibiotics.

Improper use of antibiotics has led to a great concern in the development of pathogenic microbial resistance. New Delhi metallo-ß-lactamase 1 (NDM-1) producing bacteria are resistant to most of the ß-lactam antibiotics, and so far, no new compounds have been clinically tested against these bacteria. In this study, ethanol extracts from the leaves of 240 medicinal plant species were screened for antibacterial activity against an NDM-1 Escherichia coli strain. The extracts that showed antibacterial activity were then tested for minimum inhibitory concentrations (MICs) and zones of inhibition. The extract from Combretum albidum G. Don, Hibiscus acetosella Welw. ex Hiern, Hibiscus cannabinus L., Hibiscus furcatus Willd., Punica granatum L., and Tamarindus indica L. showed bactericidal activity between 5 and 15 mg/ml and the MIC was between 2.56 and 5.12 mg/ml. All six plant extracts inhibited activity of the NDM-1 enzyme in vitro, and the IC50 value ranged between 0.50 and 1.2 ng/µl. Disruption of bacterial cell wall integrity by the plant extracts was clearly visible with scanning electron microscopy. Increases in membrane permeability caused 79.4-89.7% bacterial cell deaths as investigated by fluorescence-activated cell sorting. All the plant extracts showed synergistic effects when combined with colistin [fractional inhibitory concentration (ΣFIC) = 0.125-0.375], meropenem (ΣFIC = 0.09-0.313), and tetracycline (ΣFIC = 0.125-0.313). Thus, the plant extracts can be fractionated for the identification of active compounds, which could be used as new antibacterial compounds for the development of drugs against NDM-1 E. coli in addition to their use in combination therapy.

Anticancer activity of Moringa oleifera mediated silver nanoparticles on human cervical carcinoma cells by apoptosis induction.

Silver nanomaterial plays a crucial role in the growing field of nanotechnology as there is an increasing commercial demand for silver nanoparticles (AgNPs) owing to their wide biological applications. The present investigation aims at developing anti-cancerous colloidal silver using Moringa olifera stem bark extract. Electron and atomic force microscopic images were taken to analyze the surface morphology of the synthesized AgNPs. The effects of synthesized AgNPs were tested against human cervical carcinoma cells (HeLa) and cell morphology was further evaluated using 4,6-diamidino-2-phenylindole (DAPI) staining. The efficiency of green synthesized AgNPs was studied with the help of fluorescence activated cell sorting (FACS) and was shown to induce apoptosis through reactive oxygen species (ROS) generation in HeLa cells.

Ethylenediamine: an effective reagent for deacetylation of natural products.

The use of ethylenediamine in methanol is described for the selective cleavage of the acetate group in nimbin (1) to 6-deacetyl nimbin (1a) under microwave irradiation. This method enables to deacetylate without affecting other functional groups such as α,ß-unsaturated ketone, ester, ether, etc. in certain tetranortriterpenoids and other acetate-containing natural compounds.

In vitro antifungal activity of indirubin isolated from a South Indian ethnomedicinal plant Wrightia tinctoria R. Br.

ETHNOPHARMACOLOGICAL RELEVANCE: Acalypha indica, Cassia alata, Lawsonia inermis, Punica granatum, Thespesia populnea and Wrightia tinctoria are folklore medicines extensively used in the treatment of ringworm infections and skin related diseases in Tamil Nadu, India. AIM: The present study was designed to investigate the in vitro antifungal activity of certain medicinal plants and the pure compound indirubin isolated from Wrightia tinctoria. MATERIALS AND METHODS: The hexane, chloroform, methanol and ethanol extracts of six different plants were investigated against dermatophytes, non-dermatophytes and yeasts. Chloroform extract of Wrightia tinctoria leaf was fractionated using column chromatography and the major compound was identified using spectroscopic techniques. Antifungal activity was studied by spore germination test using agar dilution method. The minimum inhibitory concentration (MIC) was determined using broth microdilution method. RESULTS: Wrightia tinctoria showed promising activity against dermatophytic and non-dermatophytic fungi. Leaf chloroform extract showed activity at 0.5 mg/ml against Trichophyton rubrum, Epidermophyton floccosum, Aspergillus niger and Scopulariopsis brevicaulis. The major compound, identified as indirubin, exhibited activity against dermatophytes such as Epidermophyton floccosum (MIC=6.25 µg/ml); Trichophyton rubrum and Trichophyton tonsurans (MIC=25 µg/ml); Trichophyton mentagrophytes and Trichophyton simii (MIC=50 µg/ml). It was also active against non-dermatophytes (Aspergillus niger, Candida albicans and Cryptococcus sp.) within a MIC range of 0.75-25 µg/ml. CONCLUSION: The indole compound indirubin from Wrightia tinctoria showed antifungal activity and may be useful in the treatment of dermatophytosis.

Isolation, characterization and antioxidative effect of phyllanthin against CCl4-induced toxicity in HepG2 cell line.

The present study was an attempt to investigate the hepatoprotective and antioxidative property of Phyllanthus amarus (P. amarus) extract and phyllanthin. Phyllanthin, one of the active lignin present in this plant species was isolated from the aerial parts, by silica gel column chromatography employing gradient elution with hexane-ethyl acetate solvent mixture. It was obtained in high yields (1.23%), compared to reported procedures and the purity was ascertained by HPTLC and reversed-phase HPLC analysis. Characterization of phyllanthin was done by mp, UV-Visible spectrophotometry, elemental analysis, FT-IR, 1H NMR, 13C NMR and mass spectral analysis. Free radical scavenging activity of P. amarus extract and phyllanthin was also examined using DPPH assay. The protective effect of P. amarus extract and phyllanthin was studied on CCl4-induced toxicity in human hepatoma HepG2 cell line. The results indicated that CCl4 treatment caused a significant decrease in cell viability. In addition, the toxin treatment initiated lipid peroxidation (LPO), caused leakage of enzymes like alanine transaminase (ALT) and lactate dehydrogenase (LDH) with a significant decrease in glutathione (GSH) levels. It was observed that phyllanthin effectively alleviated the changes induced by CCl4 in a concentration-dependent manner, with much smaller strengths as compared to P. amarus extract.