Background/objectives: The blood-brain barrier (BBB) significantly limits the treatment of central nervous system disorders, such as schizophrenia, by restricting drug delivery to the brain. This study explores the potential of intranasal clozapine-loaded lipid nanocapsules (IN LNCs) as a targeted and effective delivery system to the brain.
Methods: LNCs were prepared using the phase inversion technique and characterized in terms of size, zeta potential, entrapment efficiency (EE%), and in vitro drug release.
Chem Biol Interact
April 2024
Cell division, differentiation, and controlled cell death are all regulated by phosphorylation, a key biological function. This mechanism is controlled by a variety of enzymes, with cyclin-dependent kinases (CDKs) being particularly important in phosphorylating proteins at serine and threonine sites. CDKs, which contain 20 unique components, serve an important role in regulating vital physiological functions such as cell cycle progression and gene transcription.
View Article and Find Full Text PDFDiabetic cardiomyopathy, a multifaceted complication of diabetes mellitus, remains a major challenge in clinical management due to its intricate pathophysiology. Emerging evidence underscores the pivotal role of autophagy dysregulation in the progression of diabetic cardiomyopathy, providing a novel avenue for therapeutic intervention. Noncoding RNAs (ncRNAs), a diverse class of regulatory molecules, have recently emerged as promising candidates for targeted therapeutic strategies.
View Article and Find Full Text PDFTumorigenesis exemplifies the complex process of neoplasm origination, which is characterised by somatic genetic alterations and abnormal cellular growth. This multidimensional phenomenon transforms previously dormant cells into malignant equivalents, resulting in uncontrollable proliferation and clonal expansion. Various elements, including random mutations, harmful environmental substances, and genetic predispositions, influence tumorigenesis's aetiology.
View Article and Find Full Text PDFMEG3, a significant long non-coding RNA (lncRNA), substantially functions in diverse biological processes, particularly breast cancer (BC) development. Within the imprinting DLK-MEG3 region on human chromosomal region 14q32.3, MEG3 spans 35 kb and encompasses ten exons.
View Article and Find Full Text PDFBroccoli, var. italica, has recently gained considerable attention due to its remarkable nutritional composition and numerous health benefits. In this review, the nutritional aspects of broccoli are examined, highlighting its rich nutrient content and essential bioactive compounds.
View Article and Find Full Text PDFA series of novel macroacyclic Schiff base ligands and their Cu (II) complexes were synthesised via reacting dicarbonyls of varying chain lengths with -methyl dithiocarbazate (SMDTC) and -benzyl dithiocarbazate (SBDTC) followed by coordination with Cu (II) ions. X-ray crystal structures were obtained for compound , an SBDTC-diacetyl analogue, and , an SMDTC-hexanedione Cu (II) complex. Anticancer evaluation of the compounds showed that , an SMDTC-glyoxal complex, demonstrated the highest cytotoxic activity against MCF-7 and MDA-MB-231 breast cancer cells with IC values of 1.
View Article and Find Full Text PDFAmikacin sulfate-loaded dextran sulfate sodium nanoparticles were formulated, lyophilized (LADNP), and then analyzed. The LADNP had a -20.9 ± 8.
View Article and Find Full Text PDFEthnopharmacological Relevance: Artemisia sieberi Besser is a medicinal herb that has been traditionally used across the Middle East for the treatment of cancer. Further pharmacological studies on its extracts revealed that they possess cytotoxic activity against certain cancer cells, however, there were no studies conducted on the anticancer potential of Artemisia sieberi essential oil (ASEO).
Aim Of The Study: To evaluate the anticancer potential of ASEO, elucidate the oil's mode of action for the first time and investigate its chemical composition.
belongs to the family Resedaceae. It is widely spread in Saudi Arabia and other countries in Southwest Asia. is extensively used in traditional medicine as an anti-inflammatory and antibacterial agent, in addition to being a vital source of food for certain desert animal species.
View Article and Find Full Text PDFWe report microwave synthesis of seven unique pyrimidine anchored derivatives (-) incorporating multifunctional amino derivatives along with their anticancer activity and their activity against COVID-19 in silico. - were characterized by different analytical and spectroscopic techniques. Cytotoxic activity of - was tested against HCT116 and MCF7 cell lines, whereby exhibited highest anticancer activity on HCT116 and MCF7 with EC values of 89.
View Article and Find Full Text PDFThe emergence of multidrug-resistant bacteria and fungi requires the development of antibiotics and antifungal agents. This review identified natural products isolated from Asian angiosperms with antibacterial and/or antifungal activities and analyzed their distribution, molecular weights, solubility, and modes of action. All data in this review were compiled from Google Scholar, PubMed, Science Direct, Web of Science, ChemSpider, PubChem, and a library search from 1979 to 2022.
View Article and Find Full Text PDFThe COVID-19 era has prompted several researchers to search for a linkage between COVID-19 and its associated neurological manifestation. Toll-like receptor 4 (TLR-4) acts as one such connecting link. spike protein of SARS-CoV-2 can bind either to ACE-2 receptors or to TLR-4 receptors, leading to aggregation of α-synuclein and neurodegeneration via the activation of various cascades in neurons.
View Article and Find Full Text PDFThis study was done to evaluate the anticancer potential of (Forssk.) Sch.Bip.
View Article and Find Full Text PDFThe aim of this a pioneering research is to investigate linear alkylbenzenes (LABs) as biomarkers of sewage pollution in sediments collected from four rivers and estuaries of the south and east of Peninsular Malaysia. The sediment samples went through soxhlet extraction, two-step column chromatography purification, fractionation and gas chromatography-mass spectrometry (GC-MS) analysis. Principal component analysis (PCA) with multivariate linear regression (MLR) was used as well for source apportionment of LABs.
View Article and Find Full Text PDFCardamonin is a polyphenolic natural product that has been shown to possess cytotoxic activity against a variety of cancer cell lines. We previously reported the semi-synthesis of a novel Cu (II)-cardamonin complex () that demonstrated potent antitumour activity. In this study, we further investigated the bioactivity of against MDA-MB-468 and PANC-1 cancer cells in an attempt to discover an effective treatment for triple-negative breast cancer (TNBC) and pancreatic cancer, respectively.
View Article and Find Full Text PDF(L.) Mansf. is an edible herb that is commonly used in the cuisine of several Asian countries.
View Article and Find Full Text PDFCardamonin is a natural chalcone that has been shown to exhibit high anticancer activity. In an attempt to discover analogues of cardamonin with enhanced anticancer activity, 19 analogues were synthesized and tested against A549 and HK1 cell lines. Results of the MTS cell viability assay showed that several derivatives possessed cytotoxic activities that were several-fold more potent than cardamonin.
View Article and Find Full Text PDFActa Crystallogr E Crystallogr Commun
February 2015
The title compound, C17H18N2O2S2, synthesized via a condensation reaction between S-benzyl di-thio-carbazate and 3,4-di-meth-oxy-benzaldehyde, crystallized with two independent mol-ecules (A and B) in the asymmetric unit. Both mol-ecules have an L-shape but differ in the orientation of the benzyl ring with respect to the 3,4-di-meth-oxy-benzyl-idine ring, this dihedral angle is 65.59 (8)° in mol-ecule A and 73.
View Article and Find Full Text PDFActa Crystallogr Sect E Struct Rep Online
December 2013
The title compound, C33H42O4 [systematic name: (1S,5S,7R)-3-benzoyl-4-hy-droxy-8,8-dimethyl-1,5,7-tris-(3-methyl-but-2--enyl)bi-cyclo-[3.3.1]nona-3-ene-2,9-dione], has a central bi-cyclo-[3.
View Article and Find Full Text PDFBioinorg Chem Appl
December 2013
Two bidentate Schiff base ligands having nitrogen sulphur donor sequence were derived from the condensation of S-benzyldithiocarbazate (SBDTC) with 2-chloroacetophenone and 4-chloroacetophenone to give S-benzyl- β -N-(2-chlorophenyl)methylenedithiocarbazate (NS2) and S-benzyl- β -N-(4-chlorophenyl)methylenedithiocarbazate (NS4) isomers. Each of the ligands was then chelated with Cd(2+), Zn(2+), Cu(2+), and Ni(2+). The compounds were characterized via IR spectroscopy and melting point while the structure of NS4 was revealed via X-ray crystallography.
View Article and Find Full Text PDFActa Crystallogr Sect E Struct Rep Online
June 2013
The title compound, [Ni(C13H11N4S2)2], was obtained by the reaction of S-2-picolyldi-thio-carbazate and pyridine-2-carbaldehyde with nickel(II) acetate. The Ni(II) atom is located on a twofold rotation axis and is bonded to four N atoms at distances of 2.037 (8) and 2.
View Article and Find Full Text PDFActa Crystallogr Sect E Struct Rep Online
February 2013
The title compound, C(12)H(16)N(2)S(3), was obtained by the condensation reaction of S-benzyl dithio-carbazate and 3-mercaptobutan-2-one. The phenyl ring and thiol (SH) group are approximately perpendicular [S-C-C-C and N-C-C-S torsion angles = 67.8 (3) and 116.
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