Enzyme inhibitors

It is a halogen-containing thiourea derivative synthesized from 1,3-thiazole. It inhibits biofilm formation in wild type and methicillin-resistant strains of staphylococcus epidermidis.

It is a thiourea derivative synthesized from 1,3-thiazole. It inhibits biofilm formation in wild type and methicillin-resistant strains of staphylococcus epidermidis.

Territrem B is a mycotoxin originally isolated from Aspergillus terreus that irreversibly inhibits acetylcholinesterase (AChE).

It is an antibiotic produced by several species of streptoverticillium. It is a potent indirect inhibitor of phospholipase A2 by specifically sequestering phosphatidylethanolamine (PE). It has antiviral activity against herpes simplex virus type 1 KOS strain infection in Vero cells. It is also an immunopotentiator.

Viridicatol is a fungal metabolite found in various Penicillium species as well as Phoma. It suppresses the expression of COX-2 and inducible nitric oxide synthase (iNOS) and inhibits production of nitric oxide and prostaglandin E2 (PGE2) in LPS-stimulated RAW 264.7 and BV2 cells.

Cyclo(L-Trp-L-Trp) is a cyclic dipeptide with antibacterial activity. It inhibits the growth of 41 out of 49 strains of multidrug resistant A. baumannii as well as B. subtilis, M. luteus, S. aureus, S. cerevisiae, A. niger and C. albicans. It has been used as a substrate for indole prenyltransferases in the synthesis of mono- and diprenylated indolines.

Fosmidomycin is an antimalarial and antibiotic originally isolated from culture broths of bacteria of the genus Streptomyces and has been used as an inhibitor of DOXP reductoisomerase, a key enzyme in the non-mevalonate pathway of isoprenoid biosynthesis.

Vibralactone D is isolated from Boreostereum vibrans and exhibits weak inhibitory effect against isozymes of 11beta-hydroxysteroid dehydrogenases (HSD).

Cyclo(L-Ala-L-Pro) is a cyclodipeptide found in Phellinus igniarius. Cyclo(L-Ala-L-Pro) exhibits an inhibitory effect on Aflatoxin Production of Aspergillus flavus.

The 50 ppm acetonitrile solution of Alternariol monomethyl ether, shows activities as a cholinesterase inhibitor as well as an anti-fungal agent, could be commonly used as a standard solution. It is an alternaria mycotoxin and genotoxin, which can inhibit the activity of DNA-topoisomerases.

Flavoglaucin is a natural compound isolated from marine fungus Eurotium sp. SF-5989. Flavoglaucin exhibits significant inhibitory effect on PTP1B with IC50 value of 13.4 micrometer. Flavoglaucin shows good binding affinity for human opioid or cannabinoid receptors. Flavoglaucin has anti-inflammatory effect, which inhibits inflammatory mediators via the induction of heme oxygenase-1 in lipopolysaccharide-stimulated RAW264.7 macrophages. Flavoglaucin exhibits significant radical scavenging activity against 1,1-diphenyl-2-picrylhydrazyl (DPPH) with the IC50 value of 11.3 microM.

Icaritin is unable to promote proliferation, migration and tube-like structure formation by human umbilical vein endothelial cells (HUVECs) in vitro. Icaritin potently inhibited proliferation of K562 cells (IC50 was 8 μM) and primary CML cells (IC50 was 13.4 μM for CML-CP and 18 μM for CML-BC), induced CML cells apoptosis and promoted the erythroid differentiation of K562 cells with time-dependent manner. Furthermore, Icaritin was able to suppress the growth of primary CD34+ leukemia cells (CML) and Imatinib-resistant cells, and to induce apoptosis. Icaritin strongly inhibited the growth of breast cancer MDA-MB-453 and MCF7 cells. At concentrations of 2-3 μM, icaritin induced cell cycle arrest at the G(2)/M phase accompanied by a down-regulation of the expression levels of the G(2)/M regulatory proteins such as cyclinB, cdc2 and cdc25C. Icaritin at concentrations of 4-5 μM, however, induced apoptotic cell death characterized by the accumulation of the annexin V- and propidium iodide-positive cells, cleavage of poly ADP-ribose polymerase (PARP) and down-regulation of the Bcl-2 expression. In mouse leukemia model, Icaritin could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells as effective as Imatinib without suppression of bone marrow. Icaritin could up-regulate phospho-JNK or phospho-C-Jun and down-regulate phospho-ERK, phospho-P-38, Jak-2, phospho-Stat3 and phospho-Akt expression with dose- or time-dependent manner.

Oxytetracycline EP Impurity A is an impurity of Oxytetracycline, which is a broad-spectrum tetracycline antibiotic used for the treatment of various infectious diseases, like anthrax, Chlamydia, cholera, typhus, relapsing fever, malaria, plaque, syphilis, respiratory infection, streptococcal infection, and acne.

A simple macrocyclic dilactone produced by a number of species of pathogenic fungi, including byssochlamys, stenphyllum, alternaria and drechslera. It exhibits antibacterial, herbicidal and anthelmintic properties. It is a weak inhibitor of propyl endopeptidases and can inhibit seed germination.

It is produced by the strain of Streptomyces. Stauprimide is an enhancer of embryonic stem cell differentiation into endoderm. It inhibits nuclear translocation of NME2.

Questinol is obtained from the cultures of the fungus Talaromyces stipitatus KUFA 0207. It can inhibit the production of NO, PGE2 and pro-inflammatory cytokines, including TNF-α, IL-1β and IL-6. It displays anti-inflammatory effect in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. It also shows remarkable anti-obesity activity.

Malformin C is a fungal cyclic pentapeptide with antibacterial and anticancer activities. Study shows that Malformin C inhibits cell growth in Colon 38 and HCT 116 cells in a dose-dependent manner with IC50 of 0.27±0.07μM and 0.18±0.023μM, respectively.

Miconazole nitrate is an imidazole antifungal agent that blocks ergosterol biosynthesis. It is commonly used as a topical drug for skin infections. It promotes the differentiation of mature oligodendrocytes from progenitor cells.

It is an NMDA receptor agonist produced by the breakdown of amino acids after the death of an organism. It is a polyamine plant growth regulator affecting the synthesis of macromolecules and the development of root systems in plants.

Nalidixic acid is a synthetic 1,8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum. It is an inhibitor of bacterial DNA polymerase (DNA gyrase) and avian myeloblastoma virus reverse transcriptase.