Cytotoxicity And Cell Death Mechanisms Against Cancer Cell Lines Elicited By The Extracts Of Physalis Minima L.

the aims of this study were to determine cytotoxicity of some medicinal herbs and to investigate cell death mechanism elicited by the most potent extract as well as its fractions. Tujuan kajian ini ialah untuk menentukan sitotoksisiti beberapa tumbuhan ubatan dan untuk menyelidiki mekanisma kematian sel yang dielisitkan oleh ekstrak yang paling poten dan fraksiny

Cytotoxic Activities of Physalis minima L. Chloroform Extract on Human Lung Adenocarcinoma NCI-H23 Cell Lines by Induction of Apoptosis

Physalis minima L. is reputed for having anticancer property. In this study, the chloroform extract of this plant exhibited remarkable cytotoxic activities on NCI-H23 (human lung adenocarcinoma) cell line at dose- and time-dependent manners (after 24, 48 and 72 h of incubation). Analysis of cell-death mechanism demonstrated that the extract exerted apoptotic programed cell death in NCI-H23 cells with typical DNA fragmentation, which is a biochemical hallmark of apoptosis. Morphological observation using transmission electron microscope (TEM) also displayed apoptotic characteristics in the treated cells, including clumping and margination of chromatins, followed by convolution of the nuclear and budding of the cells to produce membrane-bound apoptotic bodies. Different stages of apoptotic programed cell death as well as phosphatidylserine externalization were confirmed using annexin V and propidium iodide staining. Furthermore, acute exposure to the extract produced a significant regulation of c-myc, caspase-3 and p53 mRNA expression in this cell line. Due to its apoptotic effect on NCI-H23 cells, it is strongly suggested that the extract could be further developed as an anticancer drug

Bioprospecting medicinal plants for antioxidant components

AbstractObjectiveTo evaluate antioxidant activities of seven medicinal plant species and their fractions, and to identify their phenolic compounds.MethodsTwo extractions were processed and further fractionated by column chromatography to evaluate the concentration that inhibit 50% of 2,2′-azinobis (3-ethylbenzothiazoline-6-suslfonic acid, 1,1-diphenyl-2-picryl-hydrazyl radicals, and their ferric reducing antioxidant power. The identification of the fractions of phenolic compounds was done by ultra performance liquid chromatography.ResultsThe aqueous-acetone extracts of Feretia apodanthera and Ozoroa insignis exhibited the highest antioxidant potentials comparable to those of the standard quercetin. Their subsequently silica gel column fractionation showed three most active fractions from which the major constituents quercetin, myricetin, kampferol, rutin and isoquercetin were identified.ConclusionsThese plant species have potent antioxidant profiles and polyphenol compounds that may help to manage with radical related disease and aging

Benzofuranyl Esters: Synthesis, Crystal Structure Determination, Antimicrobial and Antioxidant Activities

A series of five new 2‐(1‐benzofuran‐2‐yl)‐2‐oxoethyl 4-(un/substituted)benzoates 4(a–e), with the general formula of C8H5O(C=O)CH2O(C=O)C6H4X, X = H, Cl, CH3, OCH3 or NO2, was synthesized in high purity and good yield under mild conditions. The synthesized products 4(a–e) were characterized by FTIR, 1H-, 13C- and 1H-13C HMQC NMR spectroscopic analysis and their 3D structures were confirmed by single-crystal X-ray diffraction studies. These compounds were screened for their antimicrobial and antioxidant activities. The tested compounds showed antimicrobial ability in the order of 4b < 4a < 4c < 4d < 4e and the highest potency with minimum inhibition concentration (MIC) value of 125 μg/mL was observed for 4e. The results of antioxidant activities revealed the highest activity for compound 4e (32.62% ± 1.34%) in diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, 4d (31.01% ± 4.35%) in ferric reducing antioxidant power (FRAP) assay and 4a (27.11% ± 1.06%) in metal chelating (MC) activity

Interleukin-6 Induces the down regulation of human peroxisome proliferator activated receptor alpha via the MAPK-induced STAT pathway in human hepatocytes

IL-6 plays a crucial role in the development of acute phase response. One of the important regulators of IL-6-activated APR is peroxisome proliferator activated receptor alpha (PPA

In vitro antibacterial effect of the leaf extract of Murraya koenigii on cell membrane destruction against pathogenic bacteria and phenolic compounds identification

Introduction: Different parts of Murraya koenigii are traditionally used for treating various infections. Multidrug-resistant bacteria is considered one of the most significant threats to public health and urgent attention is needed to address this pressing problem. The aim of this study was to examine the antibacterial effect of the leaves and stems of the plant to identify and screen for phenolic compounds and to explore whether the potent plant extract had a destructive effect on the cell membrane. Materials and methods: Leaf and stem extracts extracts (hexane, chloroform, ethyl acetate and methanol) of the plant were screened using micro broth dilution methods. Nine strains of bacteria were used in this study. The identification of phenolic compounds was performed using UPLC, and the membrane destruction was observed using SEM. Results: The ethyl acetate extract of the leaves gave the lowest MIC value (15.63 μg/mL) against S. aureus, E. coli 0157:H7. V. alginolyticus, V. parahaemolyticus and Y. enterocolitica. Among the tested compounds, the least MIC value of 31.25 μg/ml was observed from myricetin and quercetin against Y. enterocolitica (ATCC 23715). The two major peaks matched with quercetin and myricetin aglycons at the retention time of 3.853 and 4.160 min and two myricetin and quercetin derivatives at the retention time of 4.162 and 4.406. The alteration of the cellular morphology of the bacteria which comprises alteration in their arrangement, rigidity and destruction of the membrane was observed after treatment with plant extract. Conclusions: The findings of this research establish the efficacy of ethyl acetate leaf extract of this plant in treating diseases associated with pathogenic bacteri

Tyrosinase inhibition potency of phthalimide derivatives: crystal structure, hirshfeld surface analysis and molecular docking studies

A new series of seven 2-((pyridinylamino)methyl)isoindoline-1,3-dione derivatives were synthesized under mild condition and characterized by spectroscopy analysis. The crystal structures of these derivatives were further determined using single crystal X-ray diffraction technique. All derivatives adopt a V-shape conformation. The dihedral angle between phthalimide and pyridine rings increases as the torsion angle C1–N1–C9–N2 between phthalimide ring and methylene group increases. The torsion angles and molecular conformations are comparable to those related structures from the Cambridge Structural Database (CSD). Furthermore, the intermolecular interactions of all studied crystal structures were quantified and analyzed using Hirshfeld surface (HS) analysis. The quantitative data on the percentage contributions of overall interactions in all compounds are calculated by the two-dimensional (2D) fingerprint plots from the HS analysis. These compounds were evaluated for their antioxidant and antityrosinase properties. Noteworthy, 2-(((6-methoxypyridin-3-yl)amino)methyl)isoindoline-1,3-dione (compound g) exhibited higher tyrosinase inhibitory activity (EC50=753 μg/mL) than the positive control ‘arbutin’ (EC50=403 μg/mL). The inhibitory effect of compound g was further confirmed by computational molecular docking studies and the result revealed the 6-methoxypyridin-3-yl substituent has a better binding affinity toward tyrosinase