Xinjiachalcone A is a natural product isolated from Glycyrrhiza inflata Batalin. Xinjiachalcone A shows both a low MIC and a strong bactericidal activity against H. pylori(MIC : 12.5 to 50 µM, seventeen H. pylori strains).
Actinopyrone A is a pyrone isolated from S. pactum with diverse biological activities. It has selective and potent antimicrobial activity against H. pylori (MIC = 0.1 ng mL) with no activity against other Gram-negative bacteria including E. coli, K. pneumoniae, P. aeruginosa, and B. fragilis. Actinopyrone A also mildly inhibits growth of Gram-positive bacteria and dermatophytes with MIC values ranging from <6.25 to 25 μg mL. Intravenous administration of actinopyrone A (30 μg kg) increases coronary blood flow in dogs by 196.2%.
cis-9,10-Methyleneoctadecanoic acid is a cyclopropane fatty acid that has been found in bacteria and the digestive gland of P. globosa. It is a component of S. aureus cell membranes and levels decrease upon treatment with carvacrol. cis-9,10-Methyleneoctadecanoic acid is secreted by H. pylori and enhances histamine- and dibutyryl cAMP-stimulated acid secretion in isolated guinea pig parietal cells. It also activates protein kinase C (PKC) in a calcium-dependent manner.
Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide inhibits H. pylori recombinant carbonic anhydrase (CA) and the human CA isoforms I, II, and V with Ki values of 218, 56, 35, and 21 nM, respectively.4,5 In mice, it has anticonvulsant activity against maximal electroshock seizure (MES) and pentylenetetrazole-induced maximal, but not minimal, seizures (ED50s = 19.6, 9.3, and >500 mg kg, respectively). Zonisamide (40 mg kg, p.o.) prevents MPTP-induced decreases in the levels of dopamine , but not homovanillic acid or dihydroxyphenyl acetic acid , and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy. |1. Masuda, Y., Ishizaki, M., and Shimizu, M. Zonisamide: Pharmacology and clinical efficacy in epilepsy. CNS Drug Rev. 4(4), 341-360 (1998).|2. Rock, D.M., Macdonald, R.L., and Taylor, C.P. Blockade of sustained repetitive action potentials in cultured spinal cord neurons by zonisamide (AD 810, CI 912), a novel anticonvulsant. Epilepsy Res. 3(2), 138-143 (1989).|3. Suzuki, S., Kawakami, K., Nishimura, S., et al. Zonisamide blocks T-type calcium channel in cultured neurons of rat cerebral cortex. Epilepsy Res. 12(1), 21-27 (1992).|4. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).|5. De Simone, G., Di Fiore, A., Menchise, V., et al. Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: Solution and X-ray crystallographic studies. Bioorg. Med. Chem. Lett. 15(9), 2315-2320 (2005).|6. Yabe, H., Choudhury, M.E., Kubo, M., et al. Zonisamide increases dopamine turnover in the striatum of mice and common marmosets treated with MPTP. J. Pharmacol. Sci. 110(1), 64-68 (2009).
6,8-Diprenylorobol possesses weaker anti-H. pylori activity, it may be a useful chemopreventive agent for peptic ulcer or gastric cancer in H. pylori-infected individuals.
9-Hydroxy-alpha-lapachone can highly inhibit the growth of H. pylori, it exhibits potent inhibitory activity against H. pylori Cystathionine gamma-synthase, with IC(50) values of 4.64 microM. It may have anti-inflammatory activity, it exhibits potent inhi
Dihydrolicoisoflavone A possesses weaker anti-H. pylori activity, it may be useful chemopreventive agents for peptic ulcer or gastric cancer in H. pylori-infected individuals.
Isojacareubin displays potent activity against H. pylori HP40 clinical isolate with MIC 23.9 uM, which is approximately two times greater than that of the standard drug amoxicillin. Isojacareubin is a potent inhibitor of protein kinase C (PKC), suppresses