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Helicobacter pylori (H. pylori) has occupied a significant place among infectious pathogens and it has been documented as a leading challenge due to its higher resistance to the commonly used drugs...

Effective and precise eradication of Helicobacter pylori (H. pylori) is the most promising approach to avoid H. pylori-related gastrointestinal disorders. The present study was conducted to demonstrate the efficacy of the co-delivery of hesperidin (Hesp) and clarithromycin (CLR) in nanostructured lipid carriers (NLCs) against H. pylori. We have produced a new delivery system by combining bioflavonoid Hesp and CLR NLCs to address the failure in single antibiotic therapies. Briefly, a blend of solid lipid, liquid lipid, and surfactant was used. Homogeneous NLCs with all the formulations showed a nano size and surface-negative charge and presented high in vitro stability and slow release of the drug even after 24 h. Bioimaging studies by scanning electron microscopy, transmission electron microscopy, and imaging flow cytometry indicated that NLCs interacted with the membrane by adhering to the outer cell membrane and disrupted the membrane that resulted in the leakage of cytoplasmic contents. The prepared NLCs provide sustained and controlled drug release that can be used to increase the rate of H. pylori eradication.

A new abietane diterpene namely plectrabarbene (2), together with two known compounds: sugiol (1) and 11,14-dihydroxy-8,11,13-abietatrien-7-one (3) have been isolated from the aerial parts of Plectranthus barbatus Andr. (Labiatae). The structures of these compounds were determined by various spectral techniques (e.g., UV, IR, NMR, and FAB) and by comparison with the literature data. A molecular docking study of the isolated diterpenes (1&ndash, 3) was performed with AChE to gain an insight into their AChE inhibition mechanism. The results of docking experiments revealed that the all tested compounds showed binding affinity at the active site of AchE in comparison to donepezil.

Fungal endophytes are considered promising sources of new bioactive natural products. In this study, a Mucor sp. has been isolated as an endophyte from the medicinal plant Centaurea stoebe. Through bioactivity-guided fractionation, the isolation of the new bioactive terezine E in addition to the previously reported 14-hydroxyterezine D was carried out. The isolated compounds were fully characterised by HRESIMS and 1D and 2D NMR analyses. Both compounds exhibited potent antiproliferative activity against K-562 and HUVEC cell lines and antifungal efficacy against the tested fungal strains.

Two new compounds calothphenone (1) and 6-methoxy kaempferol 3-O-(6″-E-p-coumaroyl)-β- d-glucopyranoside (6-methoxy tiliroside) (2) along with six known compounds viz gallic acid (3), methyl gallate (4), kaempferol 3-O-(6″-E-p-coumaroyl)-β-d-glucopyranoside (tiliroside) (5), castalagin (6), kaempferol (7) and quercetin (8) were isolated from the ethyl acetate fraction (EAF) of 80% aqueous methanol extract of Calothamnus quadrifidus aerial parts. Their structure was established based on different chemical and spectroscopic techniques (1H-/13C-NMR and 2D NMR). Antioxidant activity for EAF and compounds 1, 2 and 5 was evaluated using DPPH, superoxide radical and nitric oxide (NO) inhibition methods. EAF exhibited strong activity to inhibit DPPH, superoxide and NO radicals. Moreover, all tested compounds demonstrated a close high ability to inhibit superoxide and NO radicals in comparison to ascorbic acid, but they exerted lower activity towards DPPH radical.

Methanolic extracts of edible plants and seaweeds were tested for their inhibitory activity against Jack bean urease. Quercetin-4'-O-beta-D-glucopyranoside was isolated from Allium cepa as a urease inhibitor with an IC(50) value of 190 microM-. Quercetin and two quercetin glycosides, avicularin and guaijaverin, were isolated from Psidium guajava as urease inhibitors with respective IC(50) values of 80 microM-, 140 microM-, and 120 microM-.