Enzyme inhibitors

Used as a plant growth regulator and controller. It suppresses somatic embryo formation and postembryonic shoot/root development in eleutherococcus senticosus.

Chevalone C is a meroterpenoid fungal metabolite originally isolated from E. chevalieri. It is active against M. tuberculosis H37Ra (MIC = 6.3 μg/ml) and is cytotoxic to BC1 human breast cancer cells (IC50 = 8.7 μg/ml). Chevalone C inhibits the growth of multidrug-resistant isolates of E. coli, S. aureus and E. faecium in a disc diffusion assay when used at a concentration of 15 μg/disc. It also induces cell death in HCT116 colorectal carcinoma cells.

Kumbicin C is a bis-indolyl benzenoid fungal metabolite produced by A. kumbius FRR6049. Kumbicin C was found to inhibit the growth of mouse myeloma cells (IC50 = 0.74 μg/mL) and the Gram-positive bacterium Bacillus subtilis (MIC = 1.6 μg/mL).

Asperphenamate is a fungal secondary metabolite isolated from Aspergillus flavipes. Asperphenamate has been found in a broad range of Pencillium and Aspergillus species and even in plants, as a product of endophytic fungi. Asperphenamate has weak antitumor activity. It inhibits proliferation of T47D and MDA-MB-231 breast and HL-60 leukemia cancer cell lines (IC50s = 92.3, 96.5, and 97.9 μM, respectively) and inhibits yeast α-glucosidase activity (IC50 = 8.3 μM). Asperphenamate is also used to synthesize N-Benzoyl-O-(N'-(1-benzyloxycarbonyl-4-piperidiylcarbonyl)-D-phenylalanyl)-D-phenylalaninol (BBP), an asperphenamate derivative that inhibits human breast carcinoma MCF-7 cell growth.

Pachybasin is an anthraquinone fungal metabolite isolated from Trichoderma harzianum. It regulates the increase in the number of Trichoderma mycoparasitic coils via cAMP signaling. It inhibits the growth of E. coli, S. aureus, B. subtilis, M. luteus bacteria, C. albicans, S. cerevisiae, A. niger, A. flavus and F. oxysporum fungi.

O-Methylviridicatin is a metabolite produced by several species of Penicillium. It blocks TNF-alpha activation of the HIV LTR in the Hela-based system, with an IC50 of 5 mM, and inhibits virus production in the OM-10.1 cell line, a model of chronic infection responsive to induction by TNF-alpha, with an IC50 of 2.5 mM.

It is produced by the strain of Streptomyces sp. NK26588. Iromycin A is a bacterial pyridone metabolite that acts as a nitric oxide synthase (NOS) inhibitor with selectivity for NOS III (endothelial NOS) over NOS I (neuronal NOS).

Chrodrimanin B is a meroterpenoid fungal metabolite that has been found in Talaromyces species. It has insecticidal activity against third instar silkworm larvae (LD50 = 10 μg/g of diet) and selectively inhibits the silkworm GABA receptor RDL (IC50 = 1.13 nM) over human α1β2γ2 subunit-containing GABA receptors (IC50 = 1.48 μM).

Sartorypyrone A is a meroditerpene metabolite produced by Neosartorya fungal species, displaying antibacterial and antibiofilm activities. It shows inhibitory effects against various Gram-positive bacteria. It also suppresses the growth of MCF-7 breast, NCI-H460 lung and A375-C5 melanoma cancer cell lines.

Lariatin A is an antimycobacterial lasso peptide isolated from Rhodococcus jostii. Lariains A has inhibitory effect on the growth of Mycobacterium smegmatis with MIC value of 3.13 mg/ml in agar dilution method.

Indole-3-carbinol is an inhibitor of cell growth via suppressing incorporation of [3H]thymidine, triggering G1 cell cycle arrest and downregulation of cyclin-dependent kinase 6 (CDK6) expression. It exhibits anticancer activity by inhibition of NF-κB and Akt signaling pathways. Nutritional supplement in health care products.

5-Fluorocytosine, a fluorinated pyrimidine analogue, is a synthetic antifungal medication.

Sulfamonomethoxine, a sulfonamide derivative, is an antibacterial agent commonly used as a veterinary drug. It is also an enzyme inhibitor used to address hyperpyrexia.

Malonyl-CoA decarboxylase (MCD) is found from bacteria to humans, which has important roles in regulating fatty acid metabolism and food intake. CBM 301940 is a potent malonyl-CoA decarboxylase (MCD) inhibitor with IC50 of 23 nM. It suppresses malonyl-CoA degradation and fatty acid oxidation in isolated rat hearts, leading to secondary increase in glucose oxidation.

Unguinol is a metabolite of the fungi Aspergillus unguis and Aspergillus nidulans. It has been found to be an active growth promotant in animals, in particular, monogastric animals such as chickens. It is an inhibitor of pyruvate phosphate dikinase (PPDK).

Pyrazinamide is a pyrazine that is used therapeutically as an antitubercular agent. It is a prodrug that stops the growth of Mycobacterium tuberculosis. It is thought to inhibit the enzyme fatty acid synthase (FAS) I, which is required by the bacterium to synthesise fatty acids although this has been discounted. It binds to the ribosomal protein S1 (RpsA) and inhibits trans-translation.

Sulfamethazine is a sulfonamide antibacterial agent that competitively inhibits dihydrospteric acid synthase, blocks the synthesis of folic acid and inhibits growth and proliferation. It can be used to treat pasteurosis, mastitis, urinary tract infections caused by sensitive bacteria in livestock, and can also be used for swine atrophic rhinitis, streptococcal disease, swine toxoplasmosis and coccidiosis.

A beta-lactamase inhibitor. It can irreversibly inactivate beta-lactamase enzymes of beta-lactam resistant microbes preventing them from breaking down beta-lactam antibiotics.

Fumitremorgin C, isolated from Aspergillus fumigatus, is a potent and specific inhibitor of the breast cancer resistance protein (BCRP/ABCG2) multidrug transporter. It reverses multidrug resistance mediated by BCRP and increases cytotoxicity of several anticancer agents in vitro.

Hydroxyurea is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase.