Int J Biol Macromol
February 2024
Tyrosinase is a key enzyme in enzymatic browning, causing quality losses in food through the oxidation process. Thus, the discovery of an effective and natural tyrosinase inhibitor via green technology is of great interest to the global food market due to food security and climate change issues. In this study, Syzygium aqueum (S.
View Article and Find Full Text PDFThe emergence of resistance to pathogenic bacteria has resulted from the misuse of antibiotics used in wound treatment. Therefore, nanomaterial-based agents can be used to overcome these limitations. In this study, polycaprolactone (PCL)/gelatin/graphene oxide electrospun nanofibers (PGO) are functionalized via plasma treatment with the monomeric groups diallylamine (PGO-M1), acrylic acid (PGO-M2), and -butyl acrylate (PGO-M3) to enhance the action against bacteria cells.
View Article and Find Full Text PDFEncephaloceles are the type of dysraphism in which a skull defect allows for herniation of meninges, with or without the inclusion of neural tissue, and are commonly associated with agenesis of the corpus callosum. Encephaloceles are classified as frontal, occipital, or parietal, with parietal cephaloceles, or vertex cephaloceles (VC), being the least common. Despite this, VCs present as the most common cause of a midline scalp mass, displaying complex venous and neural malformations commonly referred to as the "tip of the iceberg.
View Article and Find Full Text PDFEach year there are an estimated 1.7 million adults in the United States that develop sepsis and nearly 16% of these adult patients die because of this disease process. Sepsis, however, can impact patients of all ages.
View Article and Find Full Text PDFVascular anomalies are present in the posterior circulation. In the case of this stroke patient, the posterior cerebral artery (PCA) was shown to have a fetal origin. A fetal PCA is classified as either a partial or complete fetal PCA, which can be determined by the presence of a remnant or absence of P1, the PCA segment directly arising from the terminal of the basilar artery.
View Article and Find Full Text PDFWidespread resistance of to current artemisinin-based combination therapies necessitate the discovery of new medicines. Pharmacophoric hybridization has become an alternative for drug resistance that lowers the risk of drug-drug adverse interactions. In this study, we synthesized a new series of hybrids by covalently linking the scaffolds of pyrano[2,3-c]pyrazole with 4-aminoquinoline via an ethyl linker.
View Article and Find Full Text PDFJ Recept Signal Transduct Res
August 2022
Non-steroidal anti-inflammatory drugs (NSAIDs) are widely prescribed to treat inflammatory-related diseases, pain and fever. However, the prolong use of traditional NSAIDs leads to undesirable side effects such as gastric, ulceration, and renal toxicity due to lack of selectivity toward respective targets for COX-2, 5-LOX, and PDE4B. Thus, targeting multiple sites can reduce these adverse effects of the drugs and increase its potency.
View Article and Find Full Text PDFVanilloid (4-hydroxy-3-methoxyphenyl benzenoid) containing foods are reported to possess many biological activities including anti-inflammatory properties. Homodimerisation of the Toll-like receptor-4 (TLR-4)/Myeloid differentiation factor 2 (MD-2) complex results in life-threatening complications in inflammatory disorders. In this study, we report activity of vanilloids in inhibition of TLR-4/MD-2 homodimersization and their molecular interactions with the receptor.
View Article and Find Full Text PDFIn this study, a series of 20 structurally similar vanilloids (Vn) were tested for their antiproliferative effects against 12 human cancer cells: human breast (MCF-7 and MDA-MB-231), cervical (HeLa), ovarian (Caov-3), lung (A549), liver (HepG2), colorectal (HT-29 and HCT116), nasopharyngeal (CNE-1 and HK-1), and leukemic (K562 and CEM-SS) cancer cells. Among all the tested vanilloids, Vn16 (6-shogaol) exhibited the most potent cytotoxic effects against human colorectal cancer cells (HT-29). The apoptotic induction effects exhibited by Vn16 on HT-29 cells were confirmed using dual staining fluorescence microscopy and enzyme-linked immunosorbent assay.
View Article and Find Full Text PDFBiomed Res Int
December 2015
28 new pyrrolidine types of compounds as analogues for natural polyhydroxy alkaloids of codonopsinine were evaluated for their anti-MRSA activity using MIC and MBC value determination assay against a panel of S. aureus isolates. One pyrrolidine compound, MFM 501, exhibited good inhibitory activity with MIC value of 15.
View Article and Find Full Text PDFThis study was carried out to determine the antinociceptive activity of a novel synthetic oxopyrrolidine-based compound, (2R,3R,4S)-ethyl 4-hydroxy-1,2-dimethyl-5-oxopyrrolidine-3-carboxylate (ASH21374), and to elucidate the involvement of the opioid, vanilloid, glutamate, and nitric oxide - cyclic guanosine monophosphate (NO/cGMP) systems in modulating the observed antinociception. ASH21374, in the doses of 2, 10, and 100 mg/kg body mass, was administered orally to mice 60 mins prior to exposure to various antinociceptive assays. From the results obtained, ASH21374 exhibited significant (P < 0.
View Article and Find Full Text PDFBackground: With a higher throughput and lower cost in sequencing, second generation sequencing technology has immense potential for translation into clinical practice and in the realization of pharmacogenomics based patient care. The systematic analysis of whole genome sequences to assess patient to patient variability in pharmacokinetics and pharmacodynamics responses towards drugs would be the next step in future medicine in line with the vision of personalizing medicine.
Methods: Genomic DNA obtained from a 55 years old, self-declared healthy, anonymous male of Malay descent was sequenced.
The aim of this study was to investigate the in vitro cellular activity of novel spiroisoxazoline type compounds against normal and cancer cell lines from lung tissue (Hs888Lu), neuron-phenotypic cells (SH-SY5Y), neuroblastoma (SH-SY5Y), human histiocytic lymphoma (U937), lung cancer (A549), and leukaemia (HL-60). Our bioassay program revealed that the spiroisoxazoline type compounds show cytotoxicity only in lymphoma cell lines, which is in contrast with the pyrrolidine precursor of these spiroisoxazoline compounds, where significant cytotoxicity is seen in all normal and cancer cell lines. These data suggest a tumour-specific mechanism of action.
View Article and Find Full Text PDFColloids Surf B Biointerfaces
October 2009
Two novel glycolipids have been synthesized and their phase behaviour studied. They have been characterized using FT-IR, FAB and 13C NMR and 1H NMR to ensure the purity of novel glycolipids. The two glycolipids are distinguished based on the head group of glycolipids (monosaccharide/glucose and disaccharide/maltose).
View Article and Find Full Text PDFActa Crystallogr Sect E Struct Rep Online
October 2009
In the title compound, C(23)H(28)N(2)O(5), the 4,5-dihydro-isoxazole ring adopts a slight envelope conformation and the dioxolane ring is in a twisted conformation. The mol-ecular structure, in the vicinity of the benzyl group, may be influenced by an intra-molecular C-H⋯O hydrogen bond which generates an S(7) ring motif. In the crystal structure, mol-ecules are linked via weak inter-molecular C-H⋯O hydrogen bonds, forming extended chains along the b axis.
View Article and Find Full Text PDFActa Crystallogr Sect E Struct Rep Online
October 2009
In the title compound, C(18)H(20)N(2)O(5), the pyrrolidine ring adopts an envelope conformation with the C atom bonded to the methyl groups as the flap. The dihydro-isoxazole ring is essentially planar (r.m.
View Article and Find Full Text PDFPhytochemical studies on the leaves and trunk bark of Garcinia cantleyana yielded five caged-xanthonoids including one tetra- and four tri-prenylated xanthones, cantleyanone A (1), 7-hydroxyforbesione (2) and cantleyanones B-D (4-6), as well as a simple xanthone, 4-(1,1-dimethylprop-2-enyl)-1,3,5,8-tetrahydroxyxanthone (3). Eight other known compounds, deoxygaudichaudione A, gaudichaudione H, friedelin, garbogiol, macranthol, glutin-5-en-3beta-ol, and a mixture of sitosterol and stigmasterol were also isolated. Their structures were elucidated by means of spectroscopic data and comparison of their NMR data with literature values.
View Article and Find Full Text PDFThe plant Andrographis paniculata found throughout Southeast Asia contains Andrographolide 1, a diterpenoid lactone, which has antitumour activities against in vitro and in vivo breast cancer models. In the present study, we report on the synthesis of andrographolide derivatives, 3,19-isopropylideneandrographolide (2), 14-acetyl-3,19-isopropylideneandrographolide (3) and 14-acetylandrographolide (4), and their in vitro antitumour activities against a 2-cell line panel consisting of MCF-7 (breast cancer cell line) and HCT-116 (colon cancer cell line). Compounds 2 and 4 were also screened at the US National Cancer Institute (NCI) for their activities against a panel of 60 human cancer cell lines derived from nine cancer types.
View Article and Find Full Text PDFAndrographolide 1, a diterpenoid lactone of the plant Andrographis paniculata, known to possess antitumour activity in in vitro and in vivo breast cancer models was subjected to semisynthesis leading to the preparation of a number of novel compounds. These compounds exhibited in vitro antitumour activity with moderate to excellent growth inhibition against MCF-7 (breast) and HCT-116 (colon) cancer cells. Compounds 3,19-(2-chlorobenzylidene)andrographolide(5), 3,19-(3-chlorobenzylidene)andrographolide(6), 3,19-(3-fluorobenzylidene) andrographolide(7), 3,19-(4-fluorobenzylidene)andrographolide(8), 3,19-(2-fluorobenzylidene)andrographolide(10), 3,19-(2-chloro-5-nitrobenzylidene)andrographolide (21), 3,19-(4-chlorobenzylidene)andrographolide(30) and 3,19-(2-chloro-4-fluorobenzylidene) andrographolide(31) were also screened against 60 NCI (National Cancer Institute, USA) human tumour cell lines derived from nine cancer cell types.
View Article and Find Full Text PDFFour new furanoanthraquinones, 2-hydroxymethyl-3,4-[2'-(1-hydroxy-1-methylethyl)-dihydrofurano]-8-hydroxyanthraquinone, 2-hydroxymethyl-3,4-[1'-hydroxy-2'-(1-hydroxy-1-methylethyl)-dihydrofurano]-8-hydroxyanthraquinone, 2-hydroxymethyl-3,4-[2'-1-hydroxy-1-methylethyl)-dihydrofurano]anthraquinone and 2-methyl-3,4-[2'-(1-hydroxy-1-methylethyl)-dihydrofurano] anthraquinone or capitellataquinone A-D and four known anthraquinones, rubiadin, anthragallol 2-methyl ether, alizarin 1-methyl ether and digiferruginol, together with scopoletin were isolated from the stems of Hedyotis capitellata Wall (Rubiaceae). Lucidin-3-O-beta-glucoside was isolated from the roots of the plant. Characterization of the new compounds was carried out by extensive NMR studies using FGCOSY, FGHMQC, FGHMBC and DEPT-135 in addition to other spectroscopic methods.
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