Icariside D2, isolated from Annona glabra fruit, inhibits angiotensin-converting enzyme. Icariside D2 shows significant cytotoxic activity on the HL-60 cell line with the IC50 value of 9.0 ± 1.0 μM. Icariside D2 induces apoptosis [1][2].
Tuberculosis inhibitor 12 (compound 12) is an oxadiazole derivative and an inhibitor of Mycobacterium tuberculosis. The inhibition rates of Tuberculosis inhibitor 12 (20 μM) on 7H9-Tw-OADC and 7H9-Tw-OADC reached 82% and 78% respectively[1].
Anguizole is a small molecule inhibitor of HCV replication and alters NS4B's subcellular distribution.IC50 Value: Target: HCV
Alamethicin, isolated from Trichoderma viride, is a channel-forming peptide antibiotic and induces voltage-gated conductance in model and cell membranes[1][2].
Antibacterial agent 72 displays the antibacterial activities by targeting the bacterial membrane.
4-Epianhydrotetracycline hydrochloride is a degradation product of the antibiotic tetracycline. 4-Epianhydrotetracycline hydrochloride is active against Pseudomonas, Agrobacterium, Moraxella, Bacillus, and E. coli (MIC50s = 0.75-16 mg/L).
A potent non-nucleoside RSV L-protein polymerase inhibitor with IC50 of 89 nM; shows anti-RSV activity with IC50 of 57.6 nM and 47.8 nM for RSV A2 and RSV B-EST, respectively; shows weak cytotoxicity (CC50=600 nM).
Synthalin A sulfate is a biguanylated diamine with antibacterial and hypoglycemic properties. Synthalin A sulfate against S. aureus with a MIC of 64 μg/mL[1].
5,7-Dihydroxychromone, the extract of Cudrania tricuspidata, activates Nrf2/ARE signal and exerts neuroprotective effects against 6-hydroxydopamine (6-OHDA)-induced oxidative stress and apoptosis. 5,7-Dihydroxychromone inhibits the expression of activated caspase-3 and caspase-9 and cleaved PARP in 6-OHDA-induced SH-SY5Y cells[1].
DL-Pyroglutamic acid (CAE) as an inactivator of hepatitis B surface, inactivates vaccinia virus, herpes simplex virus, and influenza virus except poliovirus. DL-Pyroglutamic acid is also a possible inhibitor of GABA transaminase, increases GABA amount with antiepileptic action[1][2].
Fluensulfone is a new nematicide for chemical control of plant parasitic nematodes.
Methisazone (Marboran) is an antiviral agent that works by inhibiting mRNA and protein synthesis. Methisazone is also a SARS-CoV-2 (COVID-19) inhibitor. Methisazone is mainly used in pox viruses[1].
Cephalotin (Cephalotin) is a beta-lactam antibiotic, inhibits class C β-lactamase AmpC, with an Ki of 0.32 µM[1].
Metioprim is a competitive inhibitor of bacterial Dihydrofolate reductase (DHFR). Metioprim has inhibitory activity against anaerobic bacteria. Metioprim shows synergistic activity in combination with DDS (HY-B0688) against E. coli. and various mycobacteria[1][2].
Nosiheptide (Multhiomycin), a thiopeptide antibiotic produced by Streptomyces actuosus, inhibits bacterial protein synthesis and bears a unique indole side ring system and regiospecific hydroxyl groups on the characteristic macrocyclic core. Nosiheptide has been widely used as a feed additive for animal growth[1][2].
BPH-1086 (compound 10) is an IspH inhibitor, IspH domain fused with ribosomal protein S1 (RPS1) can bind to mRNA or form part of the bacterial ribosome[1][2].
Lomefloxacin(SC47111A) is a fluoroquinolone antibiotic.Target: AntibacterialLomefloxacin is a bactericidal fluoroquinolone agent with activity against a wide range of gram-negative and gram-positive organisms. The bactericidal action of lomefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited [1].
Arterolane is an antimalarial agent, with IC50 of both 1.1 nM against P. falciparum Ro73 and W2, respectively.
HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC50 of 13.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitory activity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC50 of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS[1].
1-Hydroxy-2-butanone is a natural compound isolated from Bomboo Juice with antitubercular activity[1].
Daptomycin is a lipopeptide antibiotic with rapid in vitro bactericidal activity against gram-positive organisms.
Miconazole-d2 is the deuterium labeled Miconazole[1]. Miconazole (R18134) is an imidazole antifungal agent. Miconazole also has antibacterial effects[2][3].
Daphnin is one of the major coumarin bioactive components with antibacterial activity. Daphnin is isolated from the whole herb of Daphne odora (Thunb.), which is a folk medicine in China for the relief of fever[1][2].
MtTMPK-IN-4 (compound 2), a para-piperidine, is a potent mycobacterium tuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 of 6.1 μM. MtTMPK-IN-4 is a potent tyrosinase inhibitor. MtTMPK-IN-4 is a potent antibacterial agent[1][2].
Cyclo(L-Phe-L-Pro), isolated from Pseudomonas fluorescens and Pseudomonas alcaligenes cell-free culture supernatants is an antifungal cyclic dipeptide[1]. Cyclo(L-Phe-L-Pro) inhibits IFN-β production by interfering with retinoic-acid-inducible gene-I (RIG-I) activation[2]. Cyclo(L-Phe-L-Pro) exhibits free-radical scavenging activity with the IC50 of 24 µM in the DPPH assay[3].
Surfactin is a potent cyclic lipopeptide biosurfactants that mediates flux of mono-and divalent cations, such as calcium, across lipid bilayer membranes. Surfactin can act as an antimicrobial adjuvant with anti-bacterial, anti-fungal, antimycoplasma and hemolytic effects[1][2]. Surfactin also has antiviral activity against a variety of enveloped viruses[3].
Triclosan-methyl is a transformation product of triclosan. Triclosan is a bactericide in personal care products such as toothpaste, shampoos, and soaps. Triclosan is also a stabilizing agent in a multitude of detergents and cosmetics[1].
Bronopol is an antimicrobial, with low mammalian toxicity (at in-use levels) and high activity against bacteria (especially the troublesome Gram-negative species).
Eriobofuran is an antifungal agent can be isolated from Sorbus aucuparia[1][2].