s. pneumoniae

Ethylhydrocupreine hydrochloride (Optochin hydrochloride) 是奎宁的一种衍生物，具有抗菌作用，可抑制肺炎链球菌的活性。Ethylhydrocupreine hydrochloride 具有抗疟活性，对 Plasmodium falciparum 的IC50为 25.75 nM。Ethylhydrocupreine hydrochloride 是Gallus gallus2 受体 (ggTas2r1，ggTas2r2和ggTas2r7) 激动剂。

Cefuroxime (Cephuroxime) 是一种具有口服活性的第二代头孢菌素类抗生素，具有抗菌活性，抑制革兰氏阳性菌和革兰氏阴性菌，可用于研究软组织感染。

Blasticidin S HCl 是从 Streptomyces griseochromogenes 中分离的肽基核苷类抗生素 (antibiotic)，主要通过干扰核糖体中肽键的形成从而抑制原核细胞和真核细胞蛋白的合成。

LB 11058 是一种新型的注射用头孢菌素，含有 C-3 吡啶基取代的乙烯基硫化物及 C-7 的2-氨基-5-氯-1,3-噻唑基团。该化合物对肺炎链球菌具有极高的活性，并对β-溶血性链球菌也展示出了相似的高效作用。LB 11058 对S. aureus的抑制模式类似，所有分离株均在该模式下被抑制。

Solithromycin (OP-1068) 是口服可生物利用的抗菌剂，抑制肺炎链球菌、葡萄球菌、金黄色葡萄球菌和流感嗜血杆菌的细胞活力、蛋白质合成和生长速率， IC50 值分别为 7.5 ng mL、40 ng mL 和 125 ng mL。它可与核糖体的大 50S 亚基结合抑制蛋白质生物合成。

Leucomycin a5 is a metabolite from the leucomycin complex, which was originally isolated from S. kitasatoensis. It is active against a variety of Gram-positive and Gram-negative bacteria (MICs = 0.04-0.8 µg ml) but not against K. pneumoniae, S. typhimuriu

(+)-δ-Cadinene 是一种从G. hirsutum 中发现的倍半萜，具有抗菌、杀虫、抗癌和抗增殖活性。 它对肺炎双球菌的MIC 值为31.25 μg ml，对 A. stephensi、A. aegypti 和 C. quinquefasciatust 三龄幼虫的LC50s 值分别8.23、9. 2和3。(+)-δ-Cadinene（10、50 和 100 μM）可诱导 OVCAR-3 人类卵巢癌细胞凋亡并抑制其增殖。

(-)-Viriditoxin is a mycotoxin originally isolated from A. viridinutans that has antibacterial and antiproliferative activity. It is active against methicillin-sensitive and -resistant S. aureus (MSSA and MRSA, respectively), tetracycline-sensitive and -resistant Staphylococcus, vancomycin-sensitive and -resistant Enterococcus, and penicillin-sensitive and -resistant S. pneumoniae (MICs = 2-32 μg/ml). (-)-Viriditoxin is also active against fish pathogens, including S. iniae and S. parauberis (MICs = 0.16-0.21 μg/ml). It inhibits polymerization and the GTPase activity of E. coli FtsZ, a tubulin-like GTPase involved in bacterial cell division (IC50s = 8.2 and 7 μg/ml, respectively). (-)-Viriditoxin inhibits proliferation of human DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5.36, 0.63, and 7.6 μM, respectively) . It is also toxic to mice (LD50 = 2.8 mg/kg, i.p.).

10'-Desmethoxystreptonigrin is an antibiotic originally isolated from Streptomyces and a derivative of the antibiotic streptonigrin. It is active against a variety of bacteria, including S. aureus, S. faecalis, E. coli, K. pneumoniae, and P. vulgaris (MICs = 0.4, 1.6, 3.1, 3.1 and 0.4 μg/ml, respectively). 10'-Desmethoxystreptonigrin is cytotoxic to HCT116 colon and A2780 ovarian cancer cells (IC50s = 0.004 and 0.001 μg/ml, respectively), as well as HCT116 cells resistant to etoposide and teniposide and cisplatin-resistant A2780 cells (IC50s = 0.003, 0.001, and 0.01 μg/ml, respectively). 10'-Desmethoxystreptonigrin is also an inhibitor of p21ras farnesylation (IC50 = 21 nM).

Deethylindanomycin is a polyether antibiotic that has been found in S. setonii. It is active against a variety of Gram-positive bacteria, including various strains of S. aureus and Streptococcus, as well as one strain of S. pneumoniae (MICs = 4, 4, and 2 μg ml, respectively). It is also active against coccidia in vitro, inhibiting E. tenella development, but is inactive against E. tenella infection in chicks when administered at a dose of 200 μg g in the diet. Deethylindanomycin acts as an ionophore in lipid bilayer membranes and is more selective for potassium ions than calcium, magnesium, and sodium ions. It induces histamine release from rodent mast cells and human basophils in vitro in a calcium-dependent manner.

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%.

Flumequine-13C3is intended for use as an internal standard for the quantification of flumequine by GC- or LC-MS. Flumequine is a fluoroquinolone antibiotic.1It is active againstS. aureus, S. pyogenes, B. subtilis, E. coli, P. aeruginosa, S. faecalis, andK. pneumoniae(MICs = 1-100 μg ml). Flumequine is also active against field isolates of B. hyodysenteriae (MICs = 6.25-200 μg ml).2It inhibits DNA gyrase, disrupting supercoiling of bacterial DNA to block transcription and replication.3In vivo, flumequine (50 mg kg) increases survival in rat models ofP. vulgaris-induced urinary tract infection andP. mirabilis-induced prostatitis.1Formulations containing flumequine have been used in the treatment of urinary tract infections in veterinary medicine. 1.Rohlfing, S.R., Gerster, J.R., and Kvam, D.C.Bioevaluation of the antibacterial flumequine for urinary tract useAntimicrob. Agents Chemother.10(1)20-24(1976) 2.Aller-Morán, L.M., Martínez-Lobo, F.J., Rubio, P., et al.Evaluation of the in vitro activity of flumequine against field isolates of Brachyspira hyodysenteriaeRes. Vet. Sci.10351-53(2015) 3.Smith, J.T.The mode of action of 4-quinolones and possible mechanisms of resistanceJ. Antimicrob. Chemother.18 (Suppl. D)21-29(1986)

Desacetylcefotaxime is an active metabolite of the cephalosporin antibiotic cefotaxime .1It is active against 60 clinical isolates derived from patients with meningitis, includingH. influenzae,S. pneumoniae,S. agalactiae, andN. meningitidis(MIC90s = 0.008-0.12 μg/ml). 1.Jones, R.N.Cefotaxime and desacetylcefotaxime antimicrobial interactions. The clinical relevance of enhanced activity: A reviewDiagn. Microbiol. Infect. Dis.22(1-2)19-33(1995)

Desotamide is a cyclic hexapeptide antibiotic originally isolated from Streptomyces. It is active against S. aureus, S. pneumoniae, and methicillin-resistant S. epidermidis (MRSE; MICs = 16, 12.5, and 32 μg ml, respectively).

Quinaldopeptin is a quinomycin antibiotic. It is active against a variety of bacteria, including S. pyogenes, S. aureus, C. perfringens, S. faecalis, E. coli, and K. pneumoniae (MICs = 0.2, 0.4, 0.8, 1.6, 3.1 and 6.3 μg ml, respectively). It is cytotoxic to B16 F10 and Moser cells (IC50s = 0.0008 and 0.04 μg ml, respectively) and increases survival in a P388 leukemia mouse model. Quinaldopeptin is a bis-intercalator depsipeptide (NPBID) that binds to and intercalates into DNA (Kd = 32 nM).

Terpendole I is a fungal metabolite that has been found in A. yamanashiensis.1 It is a weak inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 145 μM) and is active against the bacteria B. cereus and B. subtilis (MICs = 100 μg/ml for both) but not S. aureus, P. aeruginosa, or K. pneumoniae (MICs = >200 μg/ml for all) or the fungus C. albicans (MIC = 200 μg/ml).1,2 It is cytotoxic to HeLa cells with an IC50 value of 52.6 μM.3 |1. Tomoda, H., Tabata, N., Yang, D.-J., et al. Terpendoles, novel ACAT inhibitors produced by Albophoma yamanashiensis. III. Production, isolation and structure elucidation of new components. J. Antibiot. (Tokyo) 48(8), 793-804 (1995).|2. Zhao, J.-C., Wang, Y.-L., Zhang, T.-Y., et al. Indole diterpenoids from the endophytic fungus Drechmeria sp. as natural antimicrobial agents. Phytochemistry 148, 21-28 (2018).|3. Nagumo, Y., Motoyama, T., Hayashi, T., et al. Structure-activity relationships of terpendole E and its natural derivatives. ChemistrySelect 2(4), 1533-1536 (2017).

Leoidin is a depsidone originally isolated from L. gangaleoides that has antibacterial and enzyme inhibitory activities.1,2,3 It is active against the bacteria E. faecalis, H. influenzae, M. catarrhalis, S. aureus, and S. pneumoniae (MICs = 8, 32, 1, 128, and 64 μg ml, respectively).2 Leoidin inhibits phenylalanyl-tRNA synthetase (PheRS) isolated from P. aeruginosa (IC50 = 42 μM). It also inhibits organic anion-transporting polypeptide 1B1 (OATP1B1) and OATP1B3 with Ki values of 0.08 and 1.84 μM, respectively, in CHO cells expressing the human transporters.3

Cefazolin-13C2,15N is intended for use as an internal standard for the quantification of cefazolin by GC- or LC-MS. Cefazolin is a broad-spectrum cephalosporin antibiotic that is active in vitro against various Gram-positive and Gram-negative bacteria (MICs = 0.2-12.5 μg ml). It also inhibits the growth of clinical isolates of S. aureus, E. coli, P. mirabilis, and K. pneumoniae (MICs = 0.1-25 μg ml). In vivo, cefazolin protects against S. aureus, E. coli, and P. mirabilis infection in mice (ED50s = <0.09-1.78, 0.44-3.63, and 2.31-5.2 mg animal, respectively). Formulations containing cefazolin have been used to treat a variety of bacterial infections.

(-)-Mycousnine is a microbial metabolite and derivative of usnic acid originally isolated fromM. nawaethat has antibacterial and antifungal activities.1,2It is active against the Gram-positive bacteriaB. subtilis,K. rhizophila, andS. aureus(MICs = 4, 8, and 4 g ml, respectively) but not the Gram-negative bacteriaE. coli,S. typhimurium, andK. pneumoniae(MICs = >128 g ml for all).2(-)-Mycousnine is also active against the fungiT. mentagrophytes,T. rubrum, andC. albicans(MICs = 25, 25, and 100 μg ml, respectively).1 1.Sassa, T., and Igarashi, M.Structures of (-)-mycousnine, (+)-isomycousnine and (+)-oxymycousnine, new usnic acid derivatives from phytopathogenic Mycosphaerella nawaeAgric. BioI. Chem.54(9)2231-2237(1990) 2.Lee, J., Lee, J., Kim, G.J., et al.Mycousfurans A and B, antibacterial usnic acid congeners from the fungus Mycosphaerella sp., isolated from a marine sedimentMar. Drugs17(7)422(2019)

Dihydronovobiocin is a coumarin antibiotic and derivative of novobiocin .1It is active against the bacteriaS. aureus,S. haemolyticus,D. pneumoniae,S. typhosa,K. pneumoniae, andP. multocida(MICs = 0.6, 2, 0.6, 10, 10, and 3 μg/ml, respectively).2Dihydronovobiocin inhibits DNA gyrase subunit B with an IC50value of 64.5 nM.3 1.Berger, J., and Batcho, A.D.Coumarin - glycoside antibioticsJ. Chromatogr. Lib.15101-158(1978) 2.Hoeksema, H.Dihydronovobiocin and derivatives thereof3,175,9441-9(1965) 3.Gevi, M., and Domenici, E.A scintillation proximity assay amenable for screening and characterization of DNA gyrase B subunit inhibitorsAnal. Biochem.300(1)34-39(2002)

Desacetyl cefapirin is an active metabolite of the cephalosporin antibiotic cefapirin .1 Desacetyl cefapirin is active against E. coli, K. pneumoniae, P. mirabilis, and S. aureus with MIC values of 120, 24, 34, and 0.42 μg ml, respectively.References1. Jones, R.N., and Packer, R.R. Cefotaxime, cephalothin, and cephapirin: Antimicrobial activity and synergy studies of cephalosporins with significant in vivo desacetyl metabolite concentrations. Diagn. Microbiol. Infect. Dis. 2(1), 65-68 (1984). Desacetyl cefapirin is an active metabolite of the cephalosporin antibiotic cefapirin .1 Desacetyl cefapirin is active against E. coli, K. pneumoniae, P. mirabilis, and S. aureus with MIC values of 120, 24, 34, and 0.42 μg ml, respectively. References1. Jones, R.N., and Packer, R.R. Cefotaxime, cephalothin, and cephapirin: Antimicrobial activity and synergy studies of cephalosporins with significant in vivo desacetyl metabolite concentrations. Diagn. Microbiol. Infect. Dis. 2(1), 65-68 (1984).

Neohydroxyaspergillic acid is a fungal metabolite produced by A. sclerotiorum that has antibiotic and antifungal activities. It inhibits the growth of P. aeruginosa, M. smegmatis, S. aureus, E. coli, K. pneumoniae, B. mycoides, and B. subtilis bacteria (MICs = 125-500 μg/ml). Neohydroxyaspergillic acid also inhibits the growth of G. convolute, S. consortiale, P. blakesleeanus, C. globosum, and T. mentagrophytes (MICs = 175-700 μg/ml) but not A. niger, P. notatum, M. verrucaria, or S. cerevisiae fungi.

Phenelfamycin E is an antibiotic originally isolated from Streptomyces. It is active against β-hemolytic Streptoccus, S. pneumoniae, C. difficile, C. perfringens, and P. magnus128 μg/ml). Phenelfamycin E (4-64 mg/kg) increases survival in a mouse model of lethal S. pyogenes infection in a dose-dependent manner. Dietary administration of phenelfamycin E increases body weight in chickens.

Corynecin I is a chloramphenicol-like antibiotic originally isolated from Corynebacterium. It is active against Gram-positive and Gram-negative bacteria with MIC values of 5.2-83 μg ml for S. sonnei, P. vulgaris, K. pneumoniae, and S. aureus among others.