Sodium artelinate: A potential antimalarial

1161-116

Polyhydroxy alkaloids from plants: NMR shielding behaviour^†

483-496Polyhydroxy alkaloids comprise a relatively small group of less than 49 members, consisting of five and six membered monocyclic and fused bicyclic ring systems. The majority of them show a general property as glycosidase inhibitors. The NMR shielding data for the polyhydroxy compounds are tabulated and critical spectral features are discussed briefly

New triglycerides from antimicrobial extracts of <i>Nepeta hindostana</i> weed

542-550Three new triglycerides (21, 22 and 23) along with several known fatty compounds: palmitic acid (1), oleic acid (2), linoleic acid (3), palmitic acid methyl ester (4), oleic acid methyl ester (5), alkane: tetracosane (6), alkenes: docos-1-ene (7), 1,3,3-trimethyl-cyclo-prop-1-ene (8), triglycerides: glycerol-1,2,3-triolein (14), glycerol-1,2,3-tripalmitin (10), glycerol-1,3-dipalmitate-2-oleate (11), glycerol-2,3-dioleo-1-palmitate (12), glycerol-1,2-dipalmito-3-oleate (13), steroids: lupeone (15), stigmasterol (16), β-sitosterol (17), monoterpenoid: linalool (9), triterpenoids: oleanonic acid (18), oleanolic acid (19), and ursolic acid (20) have been isolated from the hexane, ethyl acetate and methanol extracts of the aerial part of N. hindostana. Their structures have been elucidated on the basis of spectroscopic techniques including 1D, 2D NMR and MS. The hexane, ethyl acetate and methanol extracts have shown good antimicrobial activity

Anti-Helicobacter Pylori Potential of Artemisinin and Its Derivatives

The antimalarial drug artemisinin from Artemisia annua demonstrated remarkably strong activity against Helicobacter pylori, the pathogen responsible for peptic ulcer diseases. In an effort to develop a novel antimicrobial chemotherapeutic agent containing such a sesquiterpene lactone endoperoxide, a series of analogues (2 natural and 15 semisynthetic molecules), including eight newly synthesized compounds, were investigated against clinical and standard strains of H. pylori. The antimicrobial spectrum against 10 H. pylori strains and a few other bacterial and fungal strains indicated specificity against the ulcer causing organism. Of five promising molecules, a newly synthesized ether derivative �-artecyclopropylmether was found to be the most potent compound, which exhibited MIC range, MIC90, and minimum bactericidal concentration range values of 0.25 to 1.0 �g/ml, 1.0 �g/ml, and 1 to 16 �g/ml, respectively, against both resistant and sensitive strains of H. pylori. The molecule demonstrated strong bactericidal kinetics with extensive morphological degeneration, retained functional efficacy at stomach acidic pH unlike clarithromycin, did not elicit drug resistance unlike metronidazole, and imparted sensitivity to resistant strains. It is not cytotoxic and exhibits in vivo potentiality to reduce the H. pylori burden in a chronic infection model. Thus, �-artecyclopropylmether could be a lead candidate for anti-H. pylori therapeutics. Since the recurrence of gastroduodenal ulcers is believed to be mainly due to antibiotic resistance of the commensal organism H. pylori, development of a candidate drug from this finding is warrante