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

In-vitro antibacterial activity and cytotoxicity of selected medicinal plant extracts from Penang Island Malaysia on metronidazole-resistant-Helicobacter pylori and some pathogenic bacteria.

researchHelicobacter pylori is the major agent in the etiology of chronic active gastritis, duodenal and gastric ulcers and has been linked to gastric carcinoma. The increasing antibiotic resistance of this organism and other bacteria has led to increased treatment failures, especially in therapies involving commonly used antibiotics. Malaysia has an unexplored potential of medicinal plants. This study evaluates the in-vitro antimicrobial activity of 32 selected medicinal plants used in Malaysian traditional medicine for gastrointestinal disorders and wounds. Extracts were tested against H. pylori by disc diffusion and agar dilution methods. Toxicity of the most potent extracts was also investigated. Organic solvent extracts of Derris trifoliata Lour. selectively inhibited H. pylori, and thus was further studied. Petroleum ether (PE), chloroform (CHL) and methanol (MET) extracts were tested against 13 other bacterial isolates representing eight genera. Petroleum ether and chloroform extracts showed strong activity against metronidazole-resistant clinical isolates of H. pylori with MIC90 and MIC50 ranging from 1- 4mg/l. All extracts of D. trifoliata produced higher inhibition zone diameters against H. pylori than for other bacteria. Toxicity tests showed Lc50 of PE, CHL and MET extracts on Artemia salina Leach as 1.14, 1.1, and 54.9mg/l respectively. Chemical analysis revealed the presence of fatty acids, steroids, triterpenoids, alkaloids, phenols, and phenyl propanoids, tannin, and mucilage in the extracts. Derris trifoliata shows potential as a source of selective anti-H. pylori agent

Antioxidants in aqueous extract of Myristica fragrans (Houtt.) suppress mitosis and cyclophosphamide-induced chromosomal aberrations in Allium cepa L. cells

In this study, freeze-dried water extract from the leaves of Myristica fragrans (Houtt.) was tested for mutagenic and antimutagenic potentials using the Allium cepa assay. Freeze-dried water extract alone and its combination with cyclophosphamide (CP) (50 mg/kg) were separately dissolved in tap water at 500, 1000, 2000, and 4000 mg/kg. Onions (A. cepa) were suspended in the solutions and controls for 48 h in the dark. Root tips were prepared for microscopic evaluation. 2,2-Diphenyl-1-picrylhydrazyl (DPPH) free radicals’ scavenging power of the extract was tested using butylated hydroxyanisole (BHA) and butylated hydroxytoluene (BHT) as standards. Water extract of Myristica fragrans scavenged free radicals better than BHA, but worse than BHT. The extract alone, as well as in combination with CP suppressed cell division, and induced chromosomal aberrations that were insignificantly different from the negative control (P≤0.05). However, cytotoxic and mutagenic actions of CP were considerably suppressed. The observed effects on cell division and chromosomes of A. cepa may be principally connected to the antioxidant properties of the extract. The obtained results suggest mitodepressive and antimutagenic potentials of water extract of the leaves of M. fragrans as desirable properties of a promising anticancer agent