Macrolide Antibiotics

Beauvericin is a cyclohexapeptide Fusarium toxin with insecticidal, antibacterial, anticancer, antiviral and cytotoxic activities. Beauvericin causes cellular genotoxicity by producing DNA breaks, chromosomal aberrations and micronuclei, and inhibits the PI3K/AKT pathway to induce apoptosis, thereby inhibiting the growth of HCC. In addition, Beauvericin affects immune function by inhibiting lymphocyte proliferation and interfering with the differentiation process of human monocytes into macrophages.

Josamycin (EN-141) is an orally active macrolide antibiotic exhibiting antimicrobial activity against a wide spectrum of pathogens, such as bacteria. The dissociation constant K_d from ribosome for Josamycin is 5.5 nM.

Avermectin B1 (Abamectin) is a mixture of two similar segments of avermectin. Avermectin B1 is an orally anti-infection agent, which can be used in the research of parasitic worms, insect pests, agriculture and animal husbandry. Avermectin B1 can also induce the production of ROS and induces cytotoxicity, apoptosis and autophagy.

Borrelidin (Treponemycin) is a bacterial and eukaryal threonyl-tRNA synthetase inhibitor which is a nitrile-containing macrolide antibiotic isolated from Streptomyces rochei. Borrelidin is an inhibitor of Cdc28/Cln2 of the budding yeast, with an IC₅₀ of 24 μM. Borrelidin is a potent angiogenesis inhibitor, with an IC₅₀ of 0.8 nM. Borrelidin induces apoptosis in the tube-forming cells. Borrelidin has strong antimalarial activities, with IC₅₀s of 1.9 nM and 1.8 nM against K1 and FCR3 strains of Plasmodium falciparum, respectively.

Zearalanone is a reductive metabolite of Zearalenone (HY-103447). Zearalanone binds to serum albumin across multiple species. Zearalanone enhances the binding affinity of Warfarin (HY-B0687) to serum albumin.

Lagosin (Fungichromin) is a polyene macrolide antibiotic. Lagosin has demonstrated broad-spectrum antifungal activity and is impervious to agent resistance.

Nemadectin (CL-287088), an orally active broad-spectrum endectocide, is highly efficacious against natural infections of all the major canine gastrointestinal helminthes. Anthelmintic activity.

Virginiamycin M1 (Pristinamycin IIA; Ostreogrycin A), produced by?Streptomyces virginiae, is an polyunsaturated macrocyclic lactone antibiotic and acts as a component of Virginiamycin (HY-112665). Virginiamycin M1 alone is against Staphylococcus aureus with a MIC of 0.25 μg/mL.

Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with K_is of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties.

Leucomycin (Kitasamycin) is an orally active macrolide antibiotic produced by Streptomyces kitasatoensis. Leucomycin has broad-spectrum antibacterial activities against gram-positive and gram-negative bacteria, mycoplasma, leptospira, spirochaetes, rickettsiae and some larger viruses.

Tacrolimus (Standard) (FK506 (Standard); Fujimycin (Standard); FR900506 (Standard)) is the analytical standard of Tacrolimus (HY-13756). This product is intended for research and analytical applications. Tacrolimus (FK506), a molecular glue, a macrocyclic lactone, 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.

Pristinamycin IA (Mikamycin B) is a cycle-peptidic macrolactone antibiotic. Pristinamycin IA is a substrate of P-glycoprotein and inhibits its function. Pristinamycin IA is active against StaphyloEoccus and Srreptococcus.

Oligomycin B is an antibiotic that acts as a non-selective inhibitor of ATP Synthase. Oligomycin B increases mitochondrial membrane potential. Oligomycin B induces apoptosis and necrosis. Oligomycin B impairs the motility of Plasmopara viticola zoospores and induces their lysis. Oligomycin B inhibits Magnaporthe oryzae (wheat blast fungus) and suppresses the development of wheat blast. Oligomycin B reduces hyphal growth and spore germination of Botrytis cinerea, and protects Arabidopsis thaliana against Botrytis cinerea infection. Oligomycin B exacerbates cytotoxic brain edema in rats with cerebral cortical contusion, increases intracranial pressure and brain water content, and aggravates mitochondrial damage in these rats. Oligomycin B is used in studies related to grape downy mildew, traumatic brain injury, wheat blast, and gray mold.

Tylosin tartrate is a macrolide antibiotic found naturally as a fermentation product of Streptomyces fradiae. Tylosin tartrate exerts potent antimicrobial activity against Gram-positive bacteria. Tylosin tartrate is widely used as a feed additive for promoting animal growth. Tylosin tartrate is used for veterinary purposes against bacterial dysentery and respiratory diseases in poultry, pigs and cattle.

Venturicidin A (Aabomycin A1) is a natural product derived from Streptomyces, possessing antifungal, anti-Trypanosoma brucei, anti-Leishmania donovani, and ATP synthase inhibitory activities. Venturicidin A acts as an antibiotic adjuvant, promoting the uptake of aminoglycoside antibiotics and enhancing bactericidal efficacy. Venturicidin A inhibits ATP synthesis by blocking proton translocation through the F_O subunit. In bloodstream-form Trypanosoma brucei, Venturicidin A causes collapse of the mitochondrial membrane potential; in fungi, it disrupts cell membrane integrity, induces leakage of cytoplasmic contents, elevates ROS levels, and downregulates the expression of fungal pathogenicity-related genes. Venturicidin A exhibits antifungal activity against Botrytis cinerea. Venturicidin A is used in research on bacterial infections, trypanosome/leishmania infections, and gray mold disease.

Beta-Zearalenol is an mycotoxin produced by Fusarium spp, which causes apoptosis and oxidative stress in mammalian reproductive cells. Beta-Zearalenol is the derivative of zearalenone (ZEA) which can conjugate with glucuronic acid.

Virginiamycin S1 (Virginiamycin S) is a streptogramin class B antibiotic. Virginiamycin S1 binds to the bacterial 50S ribosome, occupies the region near the P-site, induces tRNA misreading/stalling, inhibits peptide chain elongation, and exhibits synergistic activity against Gram-positive bacteria when used in combination with Virginiamycin M1 (HY-N6686). Virginiamycin S1 can be used in the research of Gram-positive bacterial infections.

Bafilomycin C1 is a macrolide antibiotic isolated from Streptomyces sp. Bafilomycin C1 is a potent, specific and reversible inhibitor of vacuolar-type H⁺-ATPases (V-ATPases). Bafilomycin C1 inhibits growth of gram-positive bacteria and fungi. Bafilomycin C1 induces cell apoptosis and can be used for the study of hepatocellular carcinoma (HCC).

Nonactin is a macrotetrolide antibiotic and mitochondrial uncoupler with antibacterial, insecticidal, and acaricidal activities. Nonactin acts as an ionophore for monovalent cations, including K⁺, and NH₄⁺, and it can also inhibit the surface expression of endogenous HSP60. In addition, Nonactin can induce apoptosis in β-catenin mutant tumor cells and has anti-tumor activity.

Erythromycin thiocyanate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin thiocyanate binds 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^[1][2]. Erythromycin thiocyanate also exhibits antitumor and neuroprotective effect in different fields of research^[3][4].