In tropical Southeast Asia, is the most economically important tree and the largest genus in the Dipterocarpaceae family. It comprises about 150-200 species, of which majority are distributed in Malaysia, with others found in Sumatra and Borneo (Kalimantan) in Indonesia. Research on the chemical constituents of plants has been ongoing for many years.
View Article and Find Full Text PDFBackground: Breast cancer is one of the main causes of death in women. is an Indonesian herbal plant that can be used as an anti-cancer. However, herbal medicines have low bioavailability, which affects their bioactivity.
View Article and Find Full Text PDFα-glucosidase is an enzyme that catalyzes the release of α-glucose molecules through hydrolysis reactions. Regulation of this enzyme can increase sugar levels in type-2 diabetes mellitus (DM) patients. Pyranocoumarin derivatives have been identified as α-glucosidase inhibitors.
View Article and Find Full Text PDFIn the first phytochemical investigation of specialized metabolites from the stem bark of , which is used in different traditional medicines, including those of Myanmar and China, five lignans (-) and three coumarins (-) were isolated by semipreparative HPLC separations and identified mainly by 1D and 2D NMR spectral analysis. The radical scavenging activity of isolated compounds was tested using the DPPH method. Noteworthy, most lignans exhibited antiradical effects comparable to vitamin C and gallic acid.
View Article and Find Full Text PDFWe report a natural product compound isolated from known as 3,4,3'-tri--methylellagic acid (T-EA) as a candidate drug for cancer treatment. The characterization of the isolated T-EA compound was carried out using various spectroscopic methods. The evaluation showcased the inhibition activity of T-EA towards the T47D and HeLa cell lines with EC values of 55.
View Article and Find Full Text PDFRSC Adv
July 2022
The human estrogenic enzyme 17beta-hydroxysteroid dehydrogenase type-1 (HSD17B1) provides biosynthesis regulation of active estrogen in stimulating the development of breast cancer through cell proliferation. The β-sitosterol is classified as a steroid compound and is actually a type of triterpenoid compound that has a similar structure to a steroid. This similarity provides a great opportunity for the inhibitor candidate to bind to the HDS17B1 enzyme because of the template similarity on the active site.
View Article and Find Full Text PDFAn investigation has been carried out on natural products from dolabellane derivatives to understand their potential in inhibiting the SARS-CoV-2 main protease (3CL) using an approach. Inhibition of the 3CL enzyme is a promising target in stopping the replication of the SARS-CoV-2 virus through inhibition of the subsite binding pocket. The redocking process aims to determine the 3CL active sites.
View Article and Find Full Text PDFA combination of molecular docking and molecular dynamics simulation (250 ns) has been carried out to study the interaction of stilbenoid trimer compounds with the SIRT1 enzyme as the target protein. SIRT1 expression regulates cellular stress responses that lead to the development of cancer. Redocking showed a good native ligand pose with an RMSD value of 1.
View Article and Find Full Text PDFViruses cause widely transmitted diseases resulting in pandemic conditions. Currently, the world is being hit by the Covid-19 pandemic caused by the SAR-CoV-2 infection. Countries in the world are competing to develop antivirals to overcome this problem.
View Article and Find Full Text PDFThe bluish-purple petals of Chinese bellflower, (kikyo in Japanese), contain platyconin () as the major anthocyanin. Platyconin () is a polyacylated anthocyanin with two caffeoyl residues at the 7-position, and its color is stable in a diluted, weakly acidic aqueous solutions. HPLC analysis of the fresh petal extract showed the presence of several minor pigments.
View Article and Find Full Text PDFA combination of computational techniques has been carried out to predict the binding of nordentatin derivatives based on pyranocoumarin semi-synthesis with the target protein from the expression of the PDE4B gene. The inhibition of the cAMP pathway is the main target of anti-cancer drugs, which is responsible for uncontrolled cell division in cancer. Modeling was done using a combination of semi-empirical methods and the density functional theory (PM3-DFT/6-31G*/B3LYP) to obtain the optimal structure of a small ligand that could be modeled.
View Article and Find Full Text PDFFive compounds (-), including three coumarins (-) and two alkaloids (,) were isolated during the first investigation of the stem bark of (L.) Corrêa. collected in Myanmar.
View Article and Find Full Text PDFAn amendment to this paper has been published and can be accessed via a link at the top of the paper.
View Article and Find Full Text PDFA new pyrano coumarin, identified as excavatin A () together with two known compounds nordentatin () and binorpocitrin () was isolated from the 95% EtOH extract of . All structures were elucidated by using spectroscopy methods such as extensive NMR and HR-FAB-MS spectrometry. All the isolated compounds were tested on antidiabetes activity by using α-glucosidase inhibition assay and the antioxidant activity by DPPH assay.
View Article and Find Full Text PDFThe small red bean, Vigna angularis, is primarily used to produce the "an-paste" component of Japanese sweets. Through the manufacturing process, the red seed-coat pigment is transferred to the colorless "an-particles", imparting a purple color. However, the major pigment in the seed coat has not yet been identified, although it is historically presumed to be an anthocyanin.
View Article and Find Full Text PDFHuman sirtuin 1 (hSIRT1) is a NAD -dependent deacetylase that regulates several cellular processes. Unlike resveratrol, natural polymeric phenolic compounds isolated from Vitaceae are mostly hSIRT1 inhibitors. The resveratrol tetramer, (+)-hopeaphenol ((+)-HP), and its geometric isomer, (-)-isohopeaphenol ((-)-iHP), were tested for inhibitory effects on purified hSIRT1 using a fluorescent derivative of peptide substrate p53-AMC (Fluor de Lys) and a cofactor NAD .
View Article and Find Full Text PDFThe rise of bleeding and bleeding complications caused by oral anticoagulant use are serious problems nowadays. Strategies that block the initiation step in blood coagulation involving activated factor VII-tissue factor (fVIIa-TF) have been considered. This study explores toxic K-139, from Lake Kasumigaura, Ibaraki, Japan, as a promising cyanobacterium for isolation of fVIIa-sTF inhibitors.
View Article and Find Full Text PDFTwo new sterols 1 and 2 and five known ones 3 - 7 were isolated for the first time from the fruiting bodies of Cortinarius glaucopus. Their structures were established by 1- and 2D-NMR spectra and HR-FABS-MS. The relative configuration of 1 was firmly determined by comparison of the observed H- H couplings and NOESY correlations, with those predicted for the computed geometries of the conformers.
View Article and Find Full Text PDFThe structure of the prespore-cell-promoting factor from Dictyostelium discoideum was determined to be 2-hydroxy-5-methyl-6-pentylbenzoquinone. The synthetic compound has prespore-cell-promoting activity similar to the natural one, with half-maximal induction at a concentration as low as 40 pM. It was also found that the factor induces aggregation in an aggregation-deficient mutant of a related species, Polysphodilium violaceum.
View Article and Find Full Text PDFA new pentacyclic triterpenoid, 3β,25-epoxy-3α,22β,23α-trihydroxy-olean-12-en-28-oic acid (1), together with seven known compounds, including five triterpenoids, β-amyrin (2), lantadene B (3), lantanilic acid (4), lantanolic acid (5) and ursolic acid (6) in addition to β-sitosterol (7) and benzoic acid (8) has been isolated from the leaves of Lantana montevidensis. Their chemical structures were elucidated by spectroscopic analysis and by comparison with the literature data and/or authentic samples. Compound 1 showed moderate to weak antibacterial activity against Staphylococcus aureus and Escherichia coli.
View Article and Find Full Text PDFThe use of medicinal plants with anti-diabetic properties continues because of the high cost of diabetes mellitus treatment. In the Bicol region of the Philippines, one local source is the leaves of Ficus pseudopalma Blanco (Philippine fig), which is utilized as an ingredient of their cuisine, and the decoction of its leaves is believed to have a blood-glucose lowering effect. The aim of this study was to evaluate the blood-glucose lowering effect of F.
View Article and Find Full Text PDFTwenty kinds of cyclic dipeptides containing l-leucine were synthesized, and their antioxidant activity against ·OH and O(2)(·-) was investigated. Compounds possessing polar amino acid residues, such as Asp, Cys, Glu, Lys, Pro, Ser, and Trp, exhibited higher antioxidant activity against ·OH than vitamin E. However, only cyclo(l-Cys-l-Leu) scavenged O(2)(·-).
View Article and Find Full Text PDFIn our previous report, rosmarinic acid (RA) was revealed to be an antidote active compound in Argusia argentea (family: Boraginaceae). The plant is locally used in Okinawa in Japan as an antidote for poisoning from snake venom, Trimeresurus flavoviridis (habu). This article presents mechanistic evidence of RA's neutralization of the hemorrhagic effects of snake venom.
View Article and Find Full Text PDFPreviously, we reported the structural requirements of the cinnamic acid relatives for inhibition of snake venom hemorrhagic action. In the present study, we examined the effect of benzenepolycarboxylic acids and substituted benzoic acids against Protobothropsflavoviridis venom-induced hemorrhage. Pyromellitic acid (1,2,4,5-benzenetetracarboxylic acid) was found to be a potent inhibitor of hemorrhage, with an IC(50) value of 0.
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