Bacillinaphthin A: A New Naphthohydroquinone from the Endophyte Bacillus subtilis NPROOT3.

The present study explores the endophyte associated with the halophyte Salicornia brachiata for uncovering new biologically important compounds. Thus, HPLC-PDA guided chemical investigation of the ethyl acetate extract of the Bacillus subtilis NPROOT3 led to the isolation of a new compound named bacillinaphthin A (1) along with previously known rubinaphthin A (2). The structure of 2 was determined by a comparison of HR-ESI-MS, 1 H and 13 C nuclear magnetic resonances (NMR) with those of reported data, whereas the structure of new compound 1 was elucidated by interpretation of 1D- and 2D-NMR and MS data. Bacillinaphthin (1) and rubinaphthin (2) feature 1,4-dihydroxy-2-naphthoic acid derivatives which have been isolated herein for the first time from the genus Bacillus. Bacillinaphthin (1) is a new congener of 2 with an additional succinic acid side chain attached to the sugar moiety. Production of succinoglycan compounds was reported to regulate symbiosis, hence the isolation of 1 exhibits an example of chemical ecology between the halophyte and its endophyte. In silico tools were used to assess the bioactive potential of both isolated molecules.

Microbial melanin: Recent advances in biosynthesis, extraction, characterization, and applications.

Melanin is a common name for a group of biopolymers with the dominance of potential applications in medical sciences, cosmeceutical, bioremediation, and bioelectronic applications. The broad distribution of these pigments suggests their role to combat abiotic and biotic stresses in diverse life forms. Biosynthesis of melanin in fungi and bacteria occurs by oxidative polymerization of phenolic compounds predominantly by two pathways, 1,8-dihydroxynaphthalene [DHN] or 3,4-dihydroxyphenylalanine [DOPA], resulting in different kinds of melanin, i.e., eumelanin, pheomelanin, allomelanin, pyomelanin, and neuromelanin. The enzymes responsible for melanin synthesis belong mainly to tyrosinase, laccase, and polyketide synthase families. Studies have shown that manipulating culture parameters, combined with recombinant technology, can increase melanin yield for large-scale production. Despite significant efforts, its low solubility has limited the development of extraction procedures, and heterogeneous structural complexity has impaired structural elucidation, restricting effective exploitation of their biotechnological potential. Innumerable studies have been performed on melanin pigments from different taxa of life in order to advance the knowledge about melanin pigments for their efficient utilization in diverse applications. These studies prompted an urgent need for a comprehensive review on melanin pigments isolated from microorganisms, so that such review encompassing biosynthesis, bioproduction, characterization, and potential applications would help researchers from diverse background to understand the importance of microbial melanins and to utilize the information from the review for planning studies on melanin. With this aim in mind, the present report compares conventional and modern ideas for environment-friendly extraction procedures for melanin. Furthermore, the characteristic parameters to differentiate between eumelanin and pheomelanin are also mentioned, followed by their biotechnological applications forming the basis of industrial utilization. There lies a massive scope of work to circumvent the bottlenecks in their isolation and structural elucidation methodologies.

Biodiversity and antimicrobial potential of bacterial endophytes from halophyte Salicornia brachiata.

Extreme natural habitats like halophytes, marsh land, and marine environment are suitable arena for chemical ecology between plants and microbes having environmental impact. Endophytes are an ecofriendly option for the promotion of plant growth and to serve as sustainable resource of novel bioactive natural products. The present study, focusing on biodiversity of bacterial endophytes from Salicornia brachiata, led to isolation of around 336 bacterial endophytes. Phylogenetic analysis of 63 endophytes revealed 13 genera with 27 different species, belonging to 3 major groups: Firmicutes, Proteobacteria, and Actinobacteria. 30% endophytic isolates belonging to various genera demonstrated broad-spectrum antibacterial and antifungal activities against a panel of human, plant, and aquatic infectious agents. An endophytic isolate Bacillus amyloliquefaciens 5NPA-1, exhibited strong in-vitro antibacterial activity against human pathogen Staphylococcus aureus and phytopathogen Xanthomonas campestris. Investigation through LC-MS/MS-based molecular networking and bioactivity-guided purification led to the identification of three bioactive compounds belonging to lipopeptide class based on 1H-, 13C-NMR and MS analysis. To our knowledge, this is the first report studying bacterial endophytic biodiversity of Salicornia brachiata and the isolation of bioactive compounds from its endophyte. Overall, the present study provides insights into the diversity of endophytes associated with the plants from the extreme environment as a rich source of metabolites with remarkable agricultural applications and therapeutic properties.

Development of Sustained Release Oseltamivir Phosphate Dry Powder Inhaler: In-Vitro Characterization and In-Vivo Toxicological Studies.

BACKGROUND: Oseltamivir Phosphate (OP) is an ethyl ester prodrug prescribed for the treatment of influenza virus infection. Current marketed formulations of OP have been observed to be supplemented with an adverse effect during post-marketing surveillance. These prerequisites are sufficed by developing a sustained release Dry Powder for Inhalation (DPI). OBJECTIVE: The objective of the present study was to develop OP-DPI by an innovative formulation approach comprising of Immediate (IR) and Sustained (SR) Release portions. METHODS: DPI formulation comprising IR and SR portions were prepared by spray drying technique using Hydroxy Propyl Methyl Cellulose (HPMC) as the rate-controlling polymer for SR portion. The spray-dried product was further characterized for various pharmaco-technical, in-vitro and in-vivo parameters. RESULTS: OP-DPI showed a burst release of 49% within 15 min further sustaining the drug release up to 9 hrs. The in-vitro aerodynamic performance of OP-DPI showed maximum deposition at stage 3 and Fine Particle Dose (FPD) of 1.08 mg indicating deposition in the upper respiratory tract. Solid-state characterization by DSC and XRD indicated the partial amorphization of OP due to spray drying. In-vivo toxicological examination revealed no sign of inflammation, indicating the safety of the developed formulation. Accelerated stability study as per ICH guidelines displayed no significant change in the solid-state characterization and drug-related performance of OP-DPI. CONCLUSION: Prepared novel and scalable OP-DPI may have the potential to overcome the problems associated with existing marketed dosage forms of OP. Further, localized drug delivery of the antiviral drug through the pulmonary route might be clinically beneficial in controlling the viral proliferation.