Mission impossible for cellular internalization: When porphyrin alliance with UiO-66-NH2 MOF gives the cell lines a ride.

Is it possible to accelerate cell internalization by hybridization of nanomaterials? Herein we support the realization of using metal-organic frameworks (MOFs) with the assistance of rigid porphyrin structure (H2TMP) aimed at drug loading, drug release, relative cell viability, and targeted in vitro drug delivery. There are several MOFs, i.e., UiO-66-NH2 (125 ± 12.5 nm), UiO-66-NH2 @H2TMP (160 ± 14 nm), UiO-66-NH2 @H2TMP@DOX, and UiO-66-NH2 @H2TMP@DOX@RO were synthesized and characterized applying HEK-293, HT-29, MCF-7, and MCF-10A cell lines. MTT investigations proved a significantly higher relative cell viability for H2TMP-aided leaf-extract-coated nanocarriers (above 62 % relative cell viability). Furthermore, the rigid H2TMP structure improved drug loading capacity by 24 % through an enhanced hydrogen bond, van der Waals, and π-π interactions. The in vitro targeted drug delivery experiments were conducted on HT-29 and MCF-7 cell lines. First, nanocarriers were treated with HT-29 cells, where UiO-66-NH2 @H2TMP@DOX@RO appeared as the best nanocarrier. Then, the selected nanocarrier was extracted from the HT-29 cell line and treated with the MCF-7 cell line. For the first time, the DOX remained inside the UiO-66-NH2 @H2TMP@DOX@RO after successful delivery to the HT-29 cell lines was observed on the MCF-7 cell line, and the second targeted drug delivery was performed. The results of this survey can enlighten the future ahead of cell internalization in MOF-based hybrid nanostructures.

Identification of sustainable trypsin active-site inhibitors from Nigrospora sphaerica strain AVA-1.

Trypsin is a protein-digesting enzyme that is essential for the growth and regeneration of bone, muscle, cartilage, skin, and blood. The trypsin inhibitors have various role in diseases such as inflammation, Alzheimer's disease, pancreatitis, rheumatoid arthritis, cancer prognosis, metastasis and so forth. From 10 endophytic fungi isolated, we were able to screen only one strain with the required activity. The fungus with activity was obtained as an endophyte from Dendrophthoe falcata and was later identified as Nigrospora sphaerica. The activity was checked by enzyme assays using trypsin. The fungus was fermented and the metabolites were extracted and further purified by bioassay-guided chromatographic methods and the compound isolated was identified using gas chromatography-mass spectrometry. The compound was identified as quercetin. Docking studies were employed to study the interaction. The absorption, distribution, metabolism, and excretion analysis showed satisfactory results and the compound has no AMES and hepatotoxicity. This study reveals the ability of N. sphaerica to produce bioactive compound quercetin has been identified as a potential candidate for trypsin inhibition. The present communication describes the first report claiming that N. sphaerica strain AVA-1 can produce quercetin and it can be considered as a sustainable source of trypsin active-site inhibitors.

Natural carbon-based quantum dots and their applications in drug delivery: A review.

Natural carbon based quantum dots (NCDs) are an emerging class of nanomaterials in the carbon family. NCDs have gained immense acclamation among researchers because of their abundance, eco-friendly nature, aqueous solubility, the diverse functionality and biocompatibility when compared to other conventional carbon quantum dots (CDs).The presence of different functional groups on the surface of NCDs such as thiol, carboxyl, hydroxyl, etc., provides improved quantum yield, physicochemical and optical properties which promote bioimaging, sensing, and drug delivery. This review provides comprehensive knowledge about NCDs for drug delivery applications by outlining the source and rationale behind NCDs, different routes of synthesis of NCDs and the merits of adopting each method. Detailed information regarding the mechanism behind the optical properties, toxicological profile including biosafety and biodistribution of NCDs that are favourable for drug delivery are discussed. The drug delivery applications of NCDs particularly as sensing and real-time tracing probe, antimicrobial, anticancer, neurodegenerative agents are reviewed. The clinical aspects of NCDs are also reviewed as an initiative to strengthen the case of NCDs as potent drug delivery agents.

Preparation, characterization and antimicrobial activity of polyvinyl alcohol/gum arabic/chitosan composite films incorporated with black pepper essential oil and ginger essential oil.

Natural materials have attracted increasing attention in wound dressing and food packaging process, which could overcome the serious environmental issues caused by conventional synthetic materials. Essential oils (EOs) such as black pepper essential oil (BPEO) and ginger essential oil (GEO) have extensively been reported for their nutritional and biomedical properties. In this study, biocomposite films based on polyvinyl alcohol (PVA), gum arabic (GA) and chitosan (CS) incorporated with BPEO and GEO were fabricated by solvent casting method. FTIR, XRD, SEM and DSC were performed with mechanical and antimicrobial properties of PVA/GA/CS films with and without BPEO and GEO. The BPEO-PVA/GA/CS film showed heterogeneous rough surface with cavities containing entrapment of BPEO droplets, whereas, the GEO-PVA/GA/CS film showed heterogeneous rough surface with coarseness due to the incorporation of respective EOs. The BPEO and GEO incorporated PVA/GA/CS films were considerable resistant to breakage and flexible with improved heat stability. The BPEO and GEO incorporated PVA/GA/CS films were significantly inhibited the growth of Bacillus cereus, Staphylococcus aureus, Escherichia coli and Salmonella typhimurium. The obtained results have demonstrated that both BPEO and GEO incorporated PVA/GA/CS films are promising alternatives to wound dressing and food packaging materials.