Regenerative marine waste towards CaCO3 nanoformulation for Alzheimer's therapy.

Alzheimer's disorder (AD) is associated with behavioural and cognitive destruction with due respect to the neurological degeneration. Conventional therapeutic approach for treatment of AD using neuroprotective drugs suffered certain limitations such as poor solubility, insufficient bioavailability, adverse side effects at higher dose and ineffective permeability on blood brain barrier (BBB). Development of nanomaterial based drug delivery system helped to overcome these barriers. Hence the present work focused on encapsulating neuroprotective drug citronellyl acetate within CaCO3 nanoparticles to develop neuroprotective CaCO3 nanoformulation (CA@CaCO3 NFs). CaCO3 was derived from marine conch shell waste, while the neuroprotective drug citronellyl acetate was scrutinized by in-silico high throughput screening. In-vitro findings revealed that CA@CaCO3 nanoformulation exhibited enhanced free radical scavenging activity of 92% (IC50 value - 29.27 ± 2.6 µg/ml), AChE inhibition of 95% (IC50 value - 25.6292 ± 1.5 µg/ml) at its maximum dose (100 µg/ml). CA@CaCO3 NFs attenuated the aggregation of ß-amyloid peptide (Aß) and also disaggregated the preformed mature plaques the major risk factor for AD. Overall, the present study reveals that CaCO3 nanoformulations exhibits potent neuroprotective potential when compared to the CaCO3 nanoparticles alone and citronellyl acetate alone due to the sustained drug release and synergistic effect of CaCO3 nanoparticles and citronellyl acetate depicting the fact that CaCO3 can act as promising drug delivery system for treatment of neurodegenerative and CNS related disorders.

Development of siderophore-based rhizobacterial consortium for the mitigation of biotic and abiotic environmental stresses in tomatoes: An in vitro and in planta approach.

AIM: Tomato-associated plant-growth-promoting rhizosphere bacteria were screened for effective antagonistic activity against the fungal vascular wilt pathogens; tolerance to heavy metals; and enhancing the bioavailability of iron for tomato plants through in vitro and in vivo approaches. METHODS AND RESULTS: Among the 121 rhizobacteria screened for siderophores, 25 isolates were observed to be siderophore producers and out of these, seven isolates chelate copper and iron thus exhibiting in vitro antagonism against the virulent strains of Fusarium oxysporum f. sp. lycopersici MTCC10270 (Fol), Fusarium equiseti MFol and Sarocladium sp. SWL isolated from infected tomatoes. Pseudomonas stutzeri KRP8 was identified to be the most potent strain among the siderophore producers and its siderophores were chemically characterized by mass spectra as metal bound and metal-free forms. Upon bio-inoculation of fortified bacterial consortium (siderozote) into the rhizosphere of vermiculite pot cultured tomatoes supplied with varying concentrations of iron and copper ions, we observed in planta growth improvements, antagonism, enhancement of bioavailability of iron and heavy metal tolerance using Inductively Coupled Plasma-Optical Emission Spectrometry. CONCLUSION AND SIGNIFICANCE OF THE STUDY: Our rhizobacterial consortium provides an opportunity for soil reclamation through an ecofriendly method for a heavy metal-free agricultural landscape.

One-pot fabrication of multifunctional catechin@ZIF-L nanocomposite: Assessment of antibiofilm, larvicidal and photocatalytic activities.

Zeolitic imidazole framework (ZIF) is an emerging class of metal organic frameworks exhibiting unique features such as crystalline nature with tunable pore size, large surface area and biocompatible nature. Exceptional thermal and chemical stabilities of ZIF-L make it a suitable candidate for biomedical applications. The present study has focused on the single step fabrication of catechin encapsulated ZIF-L and evaluation of its antibiofilm efficiency, larvicidal activity and dye degradation ability. The as- prepared CA@ZIF-L nanocomposite was characterized by spectroscopic and microscopic techniques. The results revealed that the CA@ZIF-L showed significant toxicity against mosquito larvae in a dose dependent manner with the IC50 63.43±1.25 µg/mL. CA@ZIF-L showed dose dependent reduction of biofilm formation in both ATCC and clinical MRSA strains. In addition, CA@ZIF-L exhibited excellent photocatalytic activity with around 92% degradation of methylene blue under direct sunlight. Overall, the present work highlights the possibility of employing the multifunctional CA@ZIF-L nanocomposite as a suitable material for biomedical and photocatalytic applications.

Anticancer, antimicrobial and photocatalytic activities of green synthesized magnesium oxide nanoparticles (MgONPs) using aqueous extract of Sargassum wightii.

A rapid and ecofriendly fabrication of metal oxide nanoparticles using biogenic sources is the current trend being used to replace the toxic chemical method. The present study was carried out to synthesize magnesium oxide nanoparticles (MgONPs) using the marine brown algae Sargassum wighitii as the reducing and capping agent. The as-prepared MgONPs were characterized by spectroscopic and microscopic analyses. UV-visible spectrum of the MgONPs showed a sharp absorption peak at 322 nm. X- ray diffraction analysis illustrated that the MgONPs were crystalline in nature with a face-centered cubic structure. Presence of magnesium and oxygen were further confirmed by EDX profile. FTIR analysis showed the presence of functional groups specific for sulfated polysaccharides, which might be responsible for the synthesis of MgONPs. Zeta potential and dynamic light scattering analysis illustrated that the MgONPs were highly stable at 19.8 mV with an average size of 68.06 nm. MgONPs showed potent antibacterial activity and antifungal activities against human pathogens. Photocatalytic activity of MgONPs was witnessed by the quick degradation of the organic dye methylene blue on exposure to both sunlight and UV irradiation. MgONPs showed significant cytotoxicity against the lung cancer cell lines A549 in a dose dependent manner with the IC50 value of 37.5 ±â€¯0.34 µg/ml. Safety evaluation using peripheral blood mononuclear cells (PBMCs) illustrated the MgONPs to be non-toxic in nature. Overall, the results concluded that the MgONPs generated using marine algae have exhibited scope for multifaceted biological applications.

Antioxidant and Cholinesterase Inhibitory Activities of Ethyl Acetate Extract of Terminalia chebula: Cell-free In vitro and In silico Studies.

BACKGROUND: Alzheimer's disease (AD) is a progressive neurodegenerative disorder clinically characterized by memory loss and impaired cognitive function. Cholinergic enzyme deficiency and oxidative stress are the two major factors implicated in the pathogenesis of AD. The symptomatic treatment, as of now, is the use of cholinesterase inhibitors toward cholinergic "downturn." Therefore, there is a search for compounds that will be useful in focused therapies. There has been suggestion that Terminalia chebula fruit would be a potential source. OBJECTIVE: To assess the anticholinesterase and antioxidant activities of T. chebula fruit which is widely practiced in the Ayurvedic medicines for memory enhancement. MATERIALS AND METHODS: Ethyl acetate extract of T. chebula fruit (TCEA) was subjected to phytochemical investigation of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities and cell-free antioxidant activity. TCEA was further subjected to gas chromatography-mass spectrum (GC-MS) analysis. The bioactive compounds were analyzed for molecular docking with AChE and BuChE proteins. RESULTS: TCEA exhibited potent AChE and BuChE inhibitory activities comparable to the standard drug donepezil. In vitro cell-free antioxidant assays demonstrated that TCEA possesses excellent free radical scavenging activity, reducing power, and potent metal-chelating activity. Total polyphenolic content of TCEA was 596.75 ± 0.35 µg gallic acid equivalents/mg of extract, which correlates with the antioxidant activity of TCEA. Molecular docking of compounds expounded in GC-MS analysis for AChE and BuChE enzyme activities revealed that methyl N-(N-benzyloxycarbonyl-beta-l-aspartyl)-beta-d-glucosaminide as the most potent compound with good predicted activities. CONCLUSION: Overall, the results revealed that the bioactive molecule methyl N-(N-benzyloxycarbonyl-beta-l-aspartyl)-beta-d-glucosaminide present in TCEA is a potential depressant for the treatment of AD and related neurodegenerative disorders. SUMMARY: The present study was carried out to assess the neuroprotective effect of Terminalia chebula fruit and its phytoconstituent. Phytochemical analysis of fruit ethyl acetate extract of T. chebula (TCEA) showed the presence of alkaloid, cardiac glycoside, and tannin. TCEA showed potent acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities when compared to standard drug donepezil. Results of in vitro antioxidant assays revealed excellent free radical scavenging activity, reducing power, and potent metal-chelating activity. Gas chromatography-mass spectrum analysis illustrated the presence of 22 active compounds, among which methyl N-(N-benzyloxycarbonyl-beta-l-aspartyl)-beta-d-glucosaminide exhibited potent AChE and BuChE inhibition analyzed through in silico studies. Abbreviations used: AD: Alzheimer's disease; TCEA: Ethyl acetate extract of Terminalia chebula; GC-MS: Gas chromatography-mass spectrum; ROS: Reactive oxygen species; RNS: Reactive nitrogen species; AChE: Acetylcholinesterase; BuChE: Butyrylcholinesterase; NFT: Neurofibrillary tangles; Aµ: µ-amyloid; NSAIDS: Nonsteroidal anti-inflammatory drugs; FDA: Food and Drug Administration; RT: Room temperature; HCl: Hydrochloric acid; ATCI: Acetylthiocholine iodide; BTCI: Butyrylthiocholine iodide; BHT: Butylated hydroxytoluene; DPPH: 2,2-diphenyl-1-picrylhydrazyl; TCA: Trichloroacetic acid; GAE: Gallic acid equivalent; NICT: National Institute of Information and Communications Technology; 3D: Three-dimensional; PDB: Protein data bank; OPLS: Optimized potentials for liquid simulations; XP: Extra precision; SD: Standard deviation; ANOVA: Analysis of variance; EDTA: Ethylenediaminetetraacetic acid.

Plants traditionally used in age-related brain disorders (dementia): an ethanopharmacological survey.

CONTEXT: Epidemiological studies have shown that despite mortality due to communicable diseases, poverty and human conflicts, the incidence of dementia increases in the developing world in tandem with the ageing population. Although some FDA approved drugs are available for the treatment of dementia, the outcomes are often unsatisfactory. In traditional practices of medicine, numerous plants have been used to treat cognitive disorders, including neurodegenerative diseases such as Alzheimer's disease (AD) and other memory-related disorders. In western medicine most of the drugs used for the treatment of neurodegenerative disorders are derived from plant sources. OBJECTIVE: This article reviews plants and their active constituents that have been used for their reputed cognitive-enhancing and antidementia effects. METHODS: A literature survey in Science Direct, Pubmed, and Google Scholar was performed to gather information regarding drug discovery from plants sources for the treatment of congnitive disorders and dementia. RESULTS: More than forty herbal remedies were identified with cholinesterase inhibitory, anti-inflammatory, or antioxidant activities. Bioactive compounds include alkaloids, flavonoids, steroids, saponins, terpenoids, and essential oils. About eleven herbal plants with multipotent activity against AD are discussed. CONCLUSION: Literature surveys show that most of the research has been conducted on herbal remedies effect on cholinesterase inhibitory and antioxidant activities. Studies regarding the effect of herbal drugs on ß-secretase inhibitory activity and antiaggregation property are lacking. This review provides leads for identifying potential new drugs from plant sources for the treatment of neurodegenerative disorders.

Cholinesterase inhibitors from Sargassum and Gracilaria gracilis: seaweeds inhabiting South Indian coastal areas (Hare Island, Gulf of Mannar).

Dementia is a chronic progressive mental disorder, which adversely affects memory, thinking, comprehension, calculation and language. Some of the commonest forms of dementia are Alzheimer's disease, Parkinsonism, Dementia with Lewy Bodies and Myasthenia gravis. All these disorders are related to abnormalities in the central cholinergic system, which shows a decline in acetylcholine level. Cholinesterase (ChE) inhibitors are one of the novel strategies used for the symptomatic treatment of neurological disorders like dementia. In the course of screening new ChE inhibitors from marine sources, about 11 seaweeds, which have wide pharmaceutical applications, were collected from Hare Island, Gulf of Mannar, Tamilnadu, India. Methanolic extracts of the seaweeds were assessed for ChE inhibitory activity under in vitro conditions. Kinetic parameters IC(50), K(i) and V(max) were also analysed. The results showed that 3/11 seaweeds showed 50% inhibition for both ChEs (using acetylthiocholine iodide and butyrylthiocholine iodide as substrate) at concentrations of 2 mg mL(-1) (Gracilaria gracilis, Sargassum, Cladophora fasicularis for ChE with acetylthiocholine iodide as substrate and Gracilaria gracilis, Gracilaria edulis, Sargassum for ChE with butyrylthiocholine iodide as substrate) and 4/11 showed no inhibitory activity. Inhibitory activity of seaweed extracts was compared with standard drug donepezil. Enzyme kinetic analysis showed that algal extracts exhibited mixed type inhibition (partially non-competitive inhibition).