Volume 74, Issue 1-2

Microbial transformations of isoxanthohumol ( 1 ), a beer prenylated flavonoid, by 51 fungi were investigated. Many of the tested fungi cultures were capable of effective transformation of 1 . Mucor hiemalis and Fusarium oxysporum converted isoxanthohumol ( 1 ) into isoxanthohumol 7- O -β- d -glucopyranoside ( 3 ) and (2 R )-2″-(2″′-hydroxyisopropyl)-dihydrofurano[2″,3″:7,8]-4″,5-hydroxy-5-methoxyflavanone ( 4 ), respectively. No product was obtained in the transformation of 1 by Absidia glauca conducted in a phosphate buffer. In the same medium, Beauveria bassiana converted isoxanthohumol ( 1 ) to isoxanthohumol 7- O -β- d -4″′- O -methylglucopyranoside ( 2 ).

Rhizopus microsporus var. oligosporus is a fungus that belongs to the Mucoraceae family that is used for the preparation of some soy-fermented foods. Microbial biotransformation of progesterone by R. microsporus var. oligosporus afforded some monohydroxylated and dihydroxylated metabolites. The main product was purified using chromatographic methods and identified as 11α-hydroxyprogesterone on the basis of its spectroscopic features. Time course studies by high-performance thin-layer chromatography demonstrated that this fungi efficiently hydroxylated progesterone at the 11α-position for 3 days with a yield of 76.48%, but beyond this time, the microorganism transformed 11α-hydroxyprogesterone into dihydroxylated metabolites. 11α-Hydroxyprogesterone is widely used as a precursor in the synthesis of hydrocortisone and other steroidal anti-inflammatory agents.

The current study was conducted to evaluate the antimicrobial, antioxidant, antileishmanial and cytotoxic potential of designed derivatives of 1,1′-(1,3-phenylenebis(methylene))bis(3-alkyl/aryl-1H-benzimidazol-3-ium) salts. The antibacterial potential of the test compounds was investigated against Staphylococcus aureus, Pseudomonas aeruginosa and two methicillin-resistant S. aureus (MRSA) strains (MRSA10, MRSA11), where compound 6 showed the best results. For brine shrimp lethality bioassay (BSLB), compound 6 again showed up to 100% mortality at 200 μg/mL and 56.7% mortality at 6.25 μg/mL. Antileishmanial assay was performed against Leishmania tropica at 20 μg/mL dosage, where 6 showed the most promising activity with 16.26% survival (83.74% mortality; IC 50 =14.63 μg/mL). The anticancer potential of the selected benzimidazole derivatives was evaluated against two selected cell lines (human colorectal cancer, HCT-116 and breast adenocarcinoma, MCF-7) using sulforhodamine B (SRB) assay. Compound 6 was found to be the most effective cytotoxic compound with 75% inhibition of HCT-116 proliferation at 1 mg/mL concentration. Succinctly, 6 exhibited impressive pharmacological potential that might be attributed to its higher lipophilic character owing to the longer N-substituted alkyl chains when compared to the other test compounds.

Previous studies show that certain physical and chemical properties of chemical compounds are closely related with their molecular structure. As a theoretical basis, it provides a new way of thinking by analyzing the molecular structure of the compounds to understand their physical and chemical properties. The molecular topological indices are numerical invariants of a molecular graph and are useful to predict their bioactivity. Among these topological indices, the eccentric-connectivity index has a prominent place, because of its high degree of predictability of pharmaceutical properties. In this article, we compute the closed formulae of eccentric-connectivity–based indices and its corresponding polynomial for water-soluble perylenediimides-cored polyglycerol dendrimers. Furthermore, the edge version of eccentric-connectivity index for a new class of dendrimers is determined. The conclusions we obtained in this article illustrate the promising application prospects in the field of bioinformatics and nanomaterial engineering.

Dendrimers are large and complex molecules with very well defined chemical structures. More importantly, dendrimers are highly branched organic macromolecules with successive layers or generations of branch units surrounding a central core. Topological indices are numbers associated with molecular graphs for the purpose of allowing quantitative structure-activity relationships. These topological indices correlate certain physico-chemical properties such as the boiling point, stability, strain energy, and others, of chemical compounds. In this article, we determine hyper-Zagreb index, first multiple Zagreb index, second multiple Zagreb index, and Zagreb polynomials for hetrofunctional dendrimers, triangular benzenoids, and nanocones.

The study’s objective was to investigate the volatile compounds, assess the total phenolic content and phenolic acids profile, determine the antioxidant capacity and evaluate the anthocyanin and flavonoid contents in stinging nettle ( Urtica dioica L.), tansy ( Tanacetum vulgare L.), bladder campion (Silene vulgaris (Moench) Garcke) and rosehip fruit ( Rosa canina L. cv. Plovdiv 1). The total phenolic content ranged from 0.55±0.00 to 47.39±0.41 mg GAE/g dw, total flavonoids ranged from 0.45±0.02 to 17.27±0.45 mg QЕ/g dw and the total anthocyanins ranged from 0.94±0.23 to 58.11±2.85 mg/L. The results demonstrated that the selected research plants show auspiciously useful properties in fields like pharmacy, food preparation, cosmetics, etc. Furthermore, the most promising extraction methods in terms of bioactivity are decoction and tincture ( U. dioica; T. vulgare; S. vulgaris ) and tincture ( R. canina ). The current study could be regarded as a first detailed investigation of the biological activity and phytochemical composition of R. canina L. cv. Plovdiv 1.

A strain of Bacillus methylotrophicus was isolated from a soil sample collected in Aswan eastern desert, which is known for its extremely arid climate. After fermentation of the strain in liquid culture and subsequent extraction, a bioassay-guided isolation procedure yielded five compounds: 2-benzyl-4 H -pyran-4-one, named bacillopyrone ( 1 ), pyrophen ( 2 ), macrolactin A ( 3 ) and the cyclopeptides malformin A1 ( 4 ), and bacillopeptin A ( 5 ). The structures were determined by interpretation of nuclear magnetic resonance (NMR) spectroscopy and high resolution mass spectrometry (HR-MS) data. This is the first report on the isolation of compounds 1 and 2 from Bacillus species; compound 1 was reported previously as synthetic product. Bacillopyrone ( 1 ) exhibited moderate activity against the Gram-negative Chromobacterium violaceum with minimum inhibitory concentration 266.6 μg/mL, while macrolactin A ( 3 ) and malformin A1 ( 4 ) inhibited Staphylococcus aureus (minimum inhibitory concentrations 13.3 and 133.3 μg/mL, respectively).