Enzyme inhibitors

It is produced by the strain of Fusarium aquaedeductuum WC-5228. It inhibits the binding activity of type B endothelin-1 (ETB) receptor with IC50 of 50 μmol/L. It has antibacterial activities against Gram-positive bacteria, including vancomycin-resistant Enterococcus faecium and methicillin-resistant Staphylococcus aureus.

It is produced by the strain of Streptomyces sp. MJ929-SF2. It has anti-DNA helicase activity with Ki value of 6.8 X 10-6 mol/L. It has strong anti-gram-positive bacteria (including MR-SA) activity (MIC is 0.05-0.39 μg/mL), but has no effect on gram-negative bacteria and fungi. It has anti-tumor activity on HeLa S3, L1210, IMC, B16 and FS-3 cells with IC50 (μg/mL) of 1.6, 0.97, 1.56, 0.88 and 0.83, respectively. Its acute toxicity is low, LD50 is 100 mg/kg (mouse, enterocoelia).

Diazaphilonic acid is produced by the strain of Talaramuces flavus PF1195. It has no antibacterial activity, but inhibits the ability of DNA amplification and telomerase.

Dibefurin is produced by the strain of AB16501-759. The inhibition of neurocalcitonin phosphatase was 16μg/mL, the inhibition of mixed lymphocyte reaction was 2.5 μg/mL, and the bioassay of lymphocytotoxicity was 33.0 μg/mL.

It is produced by the strain of Streptomyces lavendulae GC-148.

Diheteropeptin is produced by the strain of Diheterospora chlamydospora Q58044. It has similar activity to T ransforming growth factor-β, and inhibits the ability of Histone Deacet ylase.

Dihydrocompactin is produced by the strain of Penicillum citrinum (SANK 18767). It has inhibitory effect on HMG-COA.

Dihydromonacolin L is produced by the strain of Monascus ruber. The IC50 of HMG-CO reductase was 4.1 μmol/L.

Fluostatin A is produced by the strain of Streptomyces sp. TA-3391. It inhibits the ability of DPP-III, and with arginyl-arginine-2-naphthalene formamide as the substrate, the IC50 is 0.44μg/mL.

Fluostatin B is produced by the strain of Streptomyces sp. TA-3391. It inhibits the ability of DPP-III, and with arginyl-arginine-2-naphthalene formamide as the substrate, the IC50 is 24.0μg/mL.

Cis-Fumagillin methyl ester is originally isolated from Penicillum sp. F2757. It inhibits the MetAP2 and MetAPI with IC50 of 6.3nmol/L and <200nmol/L, respectively.

It is produced by the strain of Fusarium sambucinum. It inhibits (1,3)-β-glucan synthetase and has antifungal properties.

It is produced by the strain of Fusarium sambucinum. It inhibits (1,3)-β-glucan synthetase and has antifungal properties.

Fusidienol A is produced by the strain of Phoma spp. and Fusidium griseum. It is a Ras Farnesyl protein transferase inhibitor.

It is produced by the strain of Streptomyces toyocaensis. Gabaculine inhibits GABA aminotransferase by binding to the enzyme to form Schiff group firstly, and then aromatizing to form m-aminobenzoic acid derivatives.

A polar ring alcohol produced by the strain of Streptomycetes. Gabosine A has the ability of inhibiting Glyoxylase I.

A polar ring alcohol produced by the strain of Streptomycetes. Gabosine C has the ability of inhibiting Glyoxylase I.

It is produced by the strain of Westerdykella multispora F50733. It can inhibit the activity of leucinase A and the IC50 of leucinase A is 0.63 μmol/L.

It is produced by the strain of Beauvaria felina QN 22047. Gerfelin inhibited GGPP synthase activity with IC50 of 3.5 g/mL.

Isochromophilone III is produced by the strain of Pen. multicolor FO-3216 and FO-2328. It inhibited the ACAT of rat hepatocellular microsome and the B-16 melanoma cell with the IC50 (μmol/L) of 110 and 33.