anthracis

Dalbavancin (BI-397), a novel second-generation lipoglycopeptide antibiotic, possesses in vitro activity against a variety of Gram-positive pathogens including methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-resistant Staphylococcus epidermidis (MRSE),Dalbavancin inhibits Staphylococcus aureus and Bacillus anthracis with MIC90s of 0.06 μg/mL and 0.25 μg/mL, respectively

Coreoside B is isolated from coreoside and showed weak antimicrobial activity against S. aureus and B. anthracis.

Ciprofloxacin (Bay-09867) mainly targets bacterial DNA Gyrase (IC50=0.22-0.31 µM) and topoisomerase IV (IC50=0.3-1.9 µM). Ciprofloxacin is a highly active fluoroquinolone antibiotic.

GC-072 is a potent 4-oxoquinolizine antibiotic that selectively inhibits bacterial topoisomerase. It shows in vitro activity against both sensitive and resistant strains of B. pseudomallei, and it is also effective against other dangerous pathogens such as Burkholderia mallei, Bacillus anthracis, Yersinia pestis, and Francisella tularensis. In a murine model of melioidosis, oral administration of GC-072 demonstrated dose-dependent survival benefits, indicating its potential as a first-line oral treatment option for melioidosis.

Anthracimycin is an aminoacyl-tRNA synthetase inhibitor with demonstrated in vitro antibacterial activity against methicillin-resistant Staphylococcus aureus strains, Bacillus anthracis, and Mycobacterium tuberculosis. It can be utilized in studies of bacterial (Bacterial) infections.

Napyradiomycin A1is a fungal metabolite originally isolated fromC. rubraand has diverse biological activities.1,2It is active againstS. aureus,M. luteus,B. anthracis,C. bovis, andM. smegmatis(MICs = 1.56-12.5 μg/ml).1Napyradiomycin A1is an estrogen receptor antagonist (IC50= 4.2 μM in rat uterine homogenates).2It also inhibits mitochondrial NADH:ubiquinone oxidoreductase (complex I) and succinate:ubiquinone oxidoreductase (complex II) activities in bovine heart homogenates (IC50s = 20 and 9.7 μM, respectively).3 1.Shiomi, K., Iinuma, H., Hamada, M., et al.Novel antibiotics napyradiomycins. Production, isolation, physico-chemical properties and biological activityJ. Antibiot. (Tokyo)39(4)487-493(1986) 2.Hori, Y., Abe, Y., Shigematsu, N., et al.Napyradiomycins A and B1: Non-steroidal estrogen-receptor antagonists produced by a StreptomycesJ. Antibiot. (Tokyo)46(12)1890-1893(1993) 3.Yamamoto, K., Tashiro, E., Motohashi, K., et al.Napyradiomycin A1, an inhibitor of mitochondrial complexes I and IIJ. Antibiot. (Tokyo)65(4)211-214(2012)

Heliquinomycin is a bacterial metabolite originally isolated fromStreptomycesthat has diverse biological activities.1It is active against a variety of Gram-positive bacteria, including strains ofB. anthracis, B. subtilis, and methicillin-sensitive or -resistantS. aureus(MICs = <0.05-0.39 μg/ml). Heliquinomycin inhibits the activity of DNA helicase with a Kivalue of 6.8 μM. It reduces the growth of L1210 leukemia, B16 melanoma, and FS-3 fibrosarcoma cells (IC50s = 0.97, 0.89, and 0.83 μg/ml, respectively). 1.Chino, M., Nishikawa, K., Umekita, M., et al.Heliquinomycin, a new inhibitor of DNA helicase, produced by Streptomyces sp. MJ929-SF2 I. Taxonomy, production, isolation, physico-chemical properties and biological activitiesJ. Antibiot. (Tokyo)49(8)752-757(1996)

Carbazomycin C is a bacterial metabolite that has been found in Streptomyces and has diverse biological activities. It is active against S. aureus, B. anthracis, B. subtilis, and M. flavus, the fungi T. asteroides and T. mentagrophytes, and P. falciparum. It is also active against a panel of five plant pathogenic fungi. Carbazomycin C is cytotoxic to MCF-7, KB, and NCI H187 cells. It also inhibits 5-lipoxygenase (5-LO) activity in RBL-1 cell extracts.

Dalbavancin hydrochloride (MDL-63397 hydrochloride) is a semi-synthetic lipopeptide antibiotic that inhibits bacterial cell wall synthesis and exhibits potent bactericidal activity against Gram-positive bacteria. The MIC90 values of dalbavancin hydrochloride against Staphylococcus aureus and Bacillus anthracis are 0.06 μg/mL and 0.25 μg/mL, respectively.

Obiltoxaximab is a monoclonal antibody targeting the free protective antigen (PA) of Bacillus anthracis, used for the treatment of inhalational anthrax caused by Bacillus anthracis.

Raxibacumab (ABthrax) is a humanized antibody targeting the protective antigen of Bacillus anthracis, with anti-infective activity, blocking the interaction of anthrax protective antigen with its receptor. It is used in studies of anthrax disease prevention.

CaLL, an antimicrobial peptide, exhibits antibacterial activity against B. anthracis, including both its vegetative form, and B. cepacia, with minimum inhibitory concentrations (MICs) of 7.8, 31.3, and 31.3 μg/mL, respectively [1].

P1 is a broad-spectrum antimicrobial peptide effective against both Gram-positive and Gram-negative bacteria, including B. anthracis spores and Carbapenem-resistant strains of A. baumannii and K. pneumoniae [1].

(±)-Decursinol (3',4'-dihydro-3'-hydroxy-Xanthyletin) is a natural product from Angelica gigas.

2'(3')-O-Anthraniloyladenosine-5'-O-triphosphate (2'-ANT-ATP) and its isomer 3'-ANT-ATP are fluorescent derivatives of ATP that spontaneously isomerize. Emitting a maximum light of 428 nm when excited at 330 nm in water, 2'(3')-ANT-ATP specifically inhibits several types of adenylyl cyclase (AC) including mammalian AC1, AC2, and AC5 with inhibition constants (Kis) of 130, 640, and 120 nM, respectively. It also inhibits Bordetella pertussis AC toxin CyaA with Kis of 1.3 µM (in the presence of manganese) and 20 µM (in the presence of magnesium), Bacillus anthracis AC toxin edema factor with Kis of 0.44 µM (with manganese) and 5.15 µM (with magnesium), and Escherichia coli recombinase A (RecA) with a Ki of 6.3 µM.

2'(3')-O-Anthraniloylguanosine-5'-O-triphosphate (2'-ANT-GTP) and 3'-ANT-GTP are fluorescent derivatives of GTP that exhibit spontaneous isomerization. 2'(3')-ANT-GTP features an emission peak at 428 nm when excited at 330 nm in aqueous conditions. It functions as an inhibitor of several adenylyl cyclases, notably mammalian adenylyl cyclase 1 (AC1; Ki = 10 nM with manganese), inhibits B. anthracis adenylyl cyclase toxin edema factor (Kis = 4.1 and 13 µM with manganese and magnesium, respectively), and B. pertussis adenylyl cyclase toxin CyaA (Ki = 29 µM with manganese).

Bactobolin A, a microbial metabolite initially derived from Pseudomonas, exhibits both antibiotic and anticancer properties. It demonstrates activity against various bacteria including S. aureus, S. epidermidis, S. faecalis, B. anthracis, B. subtilis, E. coli, S. typhi, and S. dysenteriae, with minimum inhibitory concentrations (MICs) ranging from 0.1 to 12.5 µg/ml. Additionally, in vivo studies show that bactobolin A enhances survival rates at doses of 0.25 to 4 mg/kg in an L1210 murine leukemia model.

Clazamycin A, a microbial metabolite and antibiotic derived from Streptomyces, exhibits efficacy against several bacteria, namely S. aureus, B. anthracis, B. subtilis, E. coli, and P. aeruginosa, with minimum inhibitory concentrations (MICs) of 100, 6.25, 100, 50, and 25 µg/ml, respectively.

Antibiofilm agent-9 (Compound 4), a derivative of pyrrolnitrin, exhibits antimicrobial activity. It inhibits Bacillus anthracis with a Minimum Inhibitory Concentration (MIC) of 0.031 μg/mL. The compound demonstrates significant antibiofilm activity, achieving an inhibition rate of 84% after 24 hours at a concentration of 8.0 μg/mL. Additionally, Antibiofilm agent-9 shows favorable pharmacokinetic properties in mouse models.