macrolide

Bafilomycin A1 belongs to the macrolide class of antibiotics and is a V-ATPase inhibitor (IC50=0.44 nM) that is specific and reversible. Bafilomycin A1 is an inhibitor of the late phase of autophagy, blocking the fusion of autophagosomes with lysosomes. Bafilomycin A1 also induces apoptosis.

Erythromycin (E-Mycin) is a Macrolide and Macrolide Antimicrobial. The physiologic effect of erythromycin is by means of Decreased Sebaceous Gland Activity.

Brefeldin A (Cyanein) belongs to the class of macrolide antibiotics and is an ATPase inhibitor (IC50=0.2 μM). Brefeldin A can induce tumor cell differentiation and apoptosis, and also possesses autophagy inhibitory activity.

Spiramycin (Rovamycin) is a macrolide antibiotic produced by Streptomyces ambofaciens. The drug is effective against gram-positive aerobic pathogens, N. gonorrhoeae, and staphylococci. It is used to treat infections caused by bacteria and Toxoplasma gondii.

Tacrolimus (Fujimycin) can bind FKBP12 to form a high-affinity complex (Ki: 0.2 nM) which inhibits the activity of the calcium/calmodulin-dependent protein phosphatase.

Midecamycin (Medecamycin A1), an acetoxy-substituted macrolide antibiotic, has effective on gram-positive and gram-negative bacteria acts by inhibiting bacterial protein synthesis.

Fidaxomicin (Tiacumicin B) is a semisynthetic macrolide antibiotic used to treat Clostridium difficile-associated diarrhea in adults. Fidaxomicin has minimal systemic absorption and has not been linked to serum enzyme elevations during therapy or to instances of clinically apparent, acute liver injury.

Roxithromycin (RU-28965) is a semi-synthetic derivative of the macrolide antibiotic erythromycin with antibacterial and anti-malarial activities.

Lankacidins is an antitumor antibiotic of the macrolide tetraenes family from Streptomyces.

17-hydroxy Venturicidin A is a macrolide fungal metabolite originally isolated from Streptomyces. It has antibiotic activity against M. luteus, B. subtilis, and S. aureus and antifungal activity against V. dahlia, Fusarium, and C. tropicalis in a disc assay.

Mycaminosyltylonolide is a macrolide antibiotic that is tylonolide having a beta-D-mycaminosyl residue attached at position 5. Mycaminosyltylonolide is a potent antibiotic with antibacterial activity and inhibits luciferase synthesis.

Borrelidin (Treponemycin) is a bacterial and eukaryal threonyl-tRNA synthetase inhibitor. It is a macrolide antibiotic isolated from Streptomyces rochei.

Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a CNS)permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein (Kis: 8.07 nM and 0.45 nM).

Venturicidin A is a macrolide antibiotic.

Bafilomycin B1, a macrolide antibiotic isolated from Streptomyces sp, acts as an inhibitor of K+-dependent ATPase of E. coli. It also inhibits Gram-positive bacteria and fungi.

Pladienolide B is a potent spliceosome inhibitor, a macrolide isolated from Streptomyces obtusususus Mer-12, which targets the SF3B1 subunit of the spliceosome.Pladienolide B exerts its antitumor effects by inhibiting pre-mRNA splicing and inducing necrosis.Pladienolide B possesses antitumor activity and can be used to study leukemia and lymphoid tumors. Pladienolide B has antitumor activity and can be used to study leukemia and lymphoid tumors.

Josamycin (EN-141) is a macrolide antibiotic exhibiting antimicrobial activity. The dissociation constant Kd from ribosome for Josamycin is 5.5 nM.

Leucomycin (Turimycin) is a macrolide antibiotic.

Erythromycin thiocyanate acts by binding to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid .Erythromycin thiocyanate

Ascomycin (Immunomycin)(Immunomycin, FR-900520, FK520) is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties.

Filipin complex is a 28-membered cyclopentene macrolide antifungal antibiotic produced by a mixture of S. filipinensis, S. avermitilis, and S. miharaensis that inhibits the entry of PRRSV viruses into cells.

Gamithromycin (ML-1709460) is a macrolide compound with antibacterial activity.

Concanamycin C, a natural macrolide antibiotic, was initially isolated from Streptomyces and identified as an inhibitor of T-cell proliferation in response to concanavalin A (1,2). It exhibits cytotoxicity to fungi, including yeasts, by inhibiting vacuolar-type ATPases (3,4).

Spinosyn A is a polyketide-derived macrolide produced by Saccharopolyspora spinosa and is an active ingredient in several commercial insecticides.

4-Pentynoic acid (Propargylacetic acid) has been used in reactions with 1-bromo-1-alkynes in the presence of a Pd catalyst yields biologically active ynenol lactones. It also is used in a synthesis of a cytotoxic macrolide by ring-closing metathesis of a bis acetylene.

Erythromycin ethylsuccinate (EES) is a macrolide antibiotic, produced by Streptomyces erythreus.

Azithromycin hydrate (CP-62993 dihydrate) is a semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.

Nargenicin is a macrolide antibiotic that selectively inhibits the growth of S. aureus, methicilin resistant S. aureus (MRSA), and M. luteus (MICs = 0.6, 0.3, and 2.5 μg/ml, respectively) over a panel of 11 Gram-positive and Gram-negative bacteria (MICs = >80 μg/ml). [1] It dose-dependently inhibits S. aureus DnaE in the presence of DNase I-activated DNA and E. coli DnaE when used at concentrations of 0.00001-0.1 and 0.01-100 μg/mL, respectively. [2] In murine BV-2 microglial cells, nargenicin (1 μM) inhibits cytokine expression and nitric oxide production induced by LPS.[3] Nargenicin (200 μM), when used in combination with 1,25-dihydroxyvitamin D3 or all-trans retinoic acid , reduces cell proliferation by 37-47% and increases cell differentiation by 82-85% in HL-60 human myeloid leukemia cells.[4]

Phanerosporic acid is a fungal secondary metabolite originally isolated from P. chrysosporum that has antibacterial activity against B. cereus, B. subtilis, and E. coli and antifungal activity against S. cerevisiae, A. niger, O. ulmi, U. maydis, C. cucmerinum, C. cladosporioides, and B. cinerea.1 It has been used in the synthesis of macrolide derivatives.References1. Arnone, A., Assante, G., Nasini, G., et al. Phanerosporic acid, a β-resorcylate obtained from Phanerochaete chrysosporium. Phytochemistry 28(10), 2803-2806 (1989). Phanerosporic acid is a fungal secondary metabolite originally isolated from P. chrysosporum that has antibacterial activity against B. cereus, B. subtilis, and E. coli and antifungal activity against S. cerevisiae, A. niger, O. ulmi, U. maydis, C. cucmerinum, C. cladosporioides, and B. cinerea.1 It has been used in the synthesis of macrolide derivatives. References1. Arnone, A., Assante, G., Nasini, G., et al. Phanerosporic acid, a β-resorcylate obtained from Phanerochaete chrysosporium. Phytochemistry 28(10), 2803-2806 (1989).

Tylosin (Tylosine) is a macrolide antibiotic obtained from cultures of Streptomyces fradiae. The drug is effective against many microorganisms in animals but not in humans.

Tylosin tartrate, a macrolide antibiotic, is approved for the control of mycoplasmosis in poultry.

Tacrolimus monohydrate (LCP-Tacro) is a macrolide from the culture broth of a strain of Streptomyces tsukubaensis, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties. It prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro and has strong immunosuppressive activity in vivo.

Dirithromycin (LY237216) is a macrolide glycopeptide antibiotic. It is used to treat many different types of bacterial infections, such as bronchitis, pneumonia, tonsillitis, and even skin infections.

Kitasamycin tartrate, a macrolide antibiotic produced by Streptomyces kitasatoensis, has a wide spectrum of antimicrobial activity.