Duramycin is a cyclic peptide lantibiotic derived from Streptomyces cinnamoneuma. Duramycin interacts with phosphatidylethanolamine (PE) and has antibacterial, antiviral effects. Duramycin stimulates chloride secretion in airway epithelium and has the potential for cystic fibrosis treatment.
Sucrose octasulfate (SOS), a component of the gastrointestinal protectant sucralfate, is an alkaline aluminum-sucrose complex that inhibits peptic hydrolysis and raises gastric pH, protecting esophageal epithelium against acid injury. It can bind to exosite II of thrombin (KD = ~1.4 μM) and inhibit its catalytic activity (IC50 = 4.5 μM) and, as such, has been used as a surrogate for heparin. Furthermore, SOS has been shown to inhibit tumor growth in mouse melanoma and lung carcinoma models by preventing fibroblast growth factor 2 (FGF-2) binding to endothelial cells and also by removing any pre-bound FGF-2 from these cells (IC50 = ~2 μg/ml).
11-cisRetinol is an isomer of vitamin A . It is formed from vitamin A,viaatrans-retinyl ester intermediate, by the enzyme RPE65 in the retinal pigment epithelium and then converted to 11-cis retinal as part of the visual cycle.1,211-cisRetinol is an agonist of salamander and human red rod opsins expressed in COS cells and an inverse agonist of salamander red cone opsin, as well as human red and green cone opsins expressed in COS cells.3It promotes pigment formation in cone, but not rod, photoreceptors. 1.Rando, R.R.The biochemistry of the visual cycleChem. Rev.101(7)1881-1896(2001) 2.Guignard, T.J.P., Jin, M., Pequignot, M.O., et al.FATP1 inhibits 11-cis retinol formation via interaction with the visual cycle retinoid isomerase RPE65 and lecithin: Retinol acyltransferaseJ. Biol. Chem.285(24)18759-18768(2010) 3.Ala-Laurila, P., Cornwall, M.C., Crouch, R.K., et al.The action of 11-cis-retinol on cone opsins and intact cone photoreceptorsJ. Biol. Chem.284(24)16492-16500(2009)
LL-37 is a cationic and α-helical antimicrobial peptide expressed in human bone marrow, testis, granulocytes, and gingival epithelium and is upregulated in psoriatic lesions. It inhibits growth of Gram-positive E. coli D21 and Gram-negative B. megatarium in a concentration-dependent manner and LL-37 expression is induced in A549 epithelial cells, alveolar macrophages, neutrophils, and monocyte-derived macrophages following M. tuberculosis infection. LL-37 binds sheep erythrocytes coated with S. minnesota Re-LPS and induces agglutination with a minimal agglutinating concentration (MAC) of 12.1 μg/ml. It is a chemoattractant for, and can induce calcium mobilization in, human monocytes, neutrophils, and T cells that naturally express formyl peptide receptor-like 1 (FPRL1) and FPRL1-transfected HEK293 cells. LL-37 (10-15 μM) pretreatment of dengue virus type 2 (DENV-2) reduces its infectivity as well as levels of viral genomic RNA and NS1 antigen. In vivo, LL-37 inhibits cecal ligation and puncture-induced caspase-1 activation and pyroptosis of peritoneal macrophages, reduces levels of the inflammatory cytokines IL-1β, IL-6, and TNF-α, and improves survival in polybacterial septic mice.
Piriprost is a leukotriene inhibitor attenuates the smoke-induced increase in alveolar-capillary barrier permeability and decrease in plasminogen activator activity and causes a swelling of type I alveolar epithelium.
Y27632 is a selective ROCK inhibitor, which inhibits ET-1-induced increases in natriuretic peptide production, cell size, protein synthesis, and myofibrillar organization. Y27632 prevents dimethylnitrosamine-induced hepatic fibrosis in rats, increases apoptosis and disrupts the actin cortical mat in embryonic avian corneal epithelium, affects initial heart myofibrillogenesis in cultured chick blastoderm, promotes the proliferation and cell cycle progression of cultured astrocyte from spinal cord.