Tryptophan is an essential amino acid deficient in cereals, especially maize. However, maize ( L.) is the main source of protein in some developing countries in Africa and Latin America.
View Article and Find Full Text PDFFive new series of pyrrolo-fused heterocycles were designed through a scaffold hybridization strategy as analogs of the well-known microtubule inhibitor phenstatin. Compounds were synthesized using the 1,3-dipolar cycloaddition of cycloimmonium N-ylides to ethyl propiolate as a key step. Selected compounds were then evaluated for anticancer activity and ability to inhibit tubulin polymerization in vitro.
View Article and Find Full Text PDFWe report here an energy-efficient and straight synthesis of two new classes of derivatized fluorescent azatetracycles under ultrasound (US) irradiation. A first class of azatetracyclic compounds was synthesized by heterogeneous catalytic bromination of the α-keto substituent attached to the pyrrole moiety of the tetracyclic cycloadducts, while for the second, one class was synthesized by nucleophilic substitution of the bromide with the azide group. Comparative with conventional thermal heating (TH) under US irradiation, both types of reactions occur with substantially higher yields, shortened reaction time (from days to hours), lesser energy consumed, easier workup of the reaction, and smaller amounts of solvent required (at least three to five-fold less compared to TH), which make these reactions to be considered as energy efficient.
View Article and Find Full Text PDFAggregation of amyloid-β peptides (Aβ) is a hallmark of Alzheimer's disease (AD), which is affecting an increasing number of people. Hence, there is an urgent need to develop new pharmaceutical treatments which could be used to prevent the AD symptomatology. Activity-dependent neuroprotective protein (ADNP) was found to be deficient in AD, whereas NAP, an 8-amino-acid peptide (NAPVSIPQ) derived from ADNP, was shown to enhance cognitive function.
View Article and Find Full Text PDFThis communication reports a novel synthesis route for the preparation of monofunctionalized -cyclodextrin in a single stage. The approach involves only the in-situ protection of secondary hydroxyl groups as an excellent alternative to the classical procedure involving a series of five steps of protection and deprotection of hydroxyl groups (both primary and secondary ones) belonging to -cyclodextrin.
View Article and Find Full Text PDFA potential microtubule destabilising series of new indolizine derivatives was synthesised and tested for their anticancer activity against a panel of 60 human cancer cell lines. Compounds , , , and showed a broad spectrum of growth inhibitory activity against cancer cell lines representing leukaemia, melanoma and cancer of lung, colon, central nervous system, ovary, kidney, breast, and prostate. Among them, compound was distinguishable by its excellent cytostatic activity, showing GI values in the range of 10-100 nM on 43 cell lines.
View Article and Find Full Text PDFEur J Mass Spectrom (Chichester)
April 2020
NAP (NAPVSIPQ) is a small peptide derived from the activity-dependent neuroprotective protein (ADNP), which provides neuroprotection against amyloid-β peptide toxicity associated with Alzheimer disease. Several metal ions are able to promote the formation of amyloid-β peptide oligomers and protofibrils in human brain tissue. Although the relationship between metal ions and amyloid-β peptide peptides is extensively investigated, that with the NAP peptide is less understood.
View Article and Find Full Text PDFEur J Mass Spectrom (Chichester)
August 2017
The NAP peptide (H(2)N-(1)NAPVSIPQ(8)-CONH(2)) is a truncated version of the activity-dependent neuroprotective protein. Its neuroprotective activities consist of the inhibition of Aβ(25-35) and Aβ(1-40) fibrillogenesis as well as protection against Aβ-induced neurotoxicity and prevention of microtubule disruption associated with Alzheimer's disease. Therefore, we synthesized NAP and its mutant peptide with the sequence: H(2)N-(1)NAPVCIPQ(8)-COOH (NAPCOH), by replacing serine S(5) with cysteine C(5).
View Article and Find Full Text PDFThe need for a simple and accurate method for protein estimation in alcoholic extracts led to the reexamination of the optimum conditions of a colorimetric assay based on the biuret reaction. Sonication time and the other experimental parameters were optimized after kinetics study on the extraction of either zein or total proteins. Zein extraction and purity were investigated by (1)H and (13)C NMR spectroscopy, SDS-PAGE electrophoresis, and UV-visible spectrophotometry (UV-vis).
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