Cytarabine 5′-monophosphate (ara-CMP), an active metabolite of the nucleoside analog cytarabine formed by deoxycytidine kinase, is incorporated into DNA by DNA polymerase α, significantly slowing DNA synthesis. It inhibits nuclear and mitochondrial DNA replication in S. cerevisiae at 15 mM and improves survival in an L1210 murine leukemia model at 3.5-75.1 mg kg.
1-Undecanoyl-rac-glycerol is a monoacylglycerol that contains undecanoic acid at the sn-1 position. It completely inhibits the growth of the bacteria B. cereus, B. subtilis, M. luteus, E. faecalis, and S. aureus when used at concentrations ranging from 250 to 1,500 mg L.1 1-Undecanoyl-rac-glycerol (0.1 and 0.3 mg ml) also has antifungal activity against K. marxianus, S. cerevisiae, and C. maltosa.2
SCH 725674 is an antifungal macrolide originally isolated from Aspergillus. It inhibits the growth of S. cerevisiae and C. albicans in vitro (MICs = 8 and 32 μg ml, respectively).
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.
Burnettramic acid A is a fungal metabolite originally isolated fromA. burnettiithat has diverse biological activities.1It is active againstB. subtilis,S. aureus,C. albicans, andS. cerevisiae(IC50s = 2.3, 5.9, 0.5, and 0.2 μg ml, respectively). Burnettramic acid A is cytotoxic to NS-1 murine myeloma cells but not neonatal foreskin fibroblasts (IC50s = 13.8 and >100 μg ml, respectively). 1.Li, H., Gilchrist, C.L.M., Lacey, H.J., et al.Discovery and heterologous biosynthesis of the burnettramic acids: Rare PKS-NRPS-derived bolaamphiphilic pyrrolizidinediones from an Australian fungus, Aspergillus burnettiiOrg. Lett.21(5)1287-1291(2019)
Phanerosporic acid is a fungal secondary metabolite originally isolated from P. chrysosporum that has antibacterial activity against B. cereus, B. subtilis, and E. coli and antifungal activity against S. cerevisiae, A. niger, O. ulmi, U. maydis, C. cucmerinum, C. cladosporioides, and B. cinerea.1 It has been used in the synthesis of macrolide derivatives.References1. Arnone, A., Assante, G., Nasini, G., et al. Phanerosporic acid, a β-resorcylate obtained from Phanerochaete chrysosporium. Phytochemistry 28(10), 2803-2806 (1989). Phanerosporic acid is a fungal secondary metabolite originally isolated from P. chrysosporum that has antibacterial activity against B. cereus, B. subtilis, and E. coli and antifungal activity against S. cerevisiae, A. niger, O. ulmi, U. maydis, C. cucmerinum, C. cladosporioides, and B. cinerea.1 It has been used in the synthesis of macrolide derivatives. References1. Arnone, A., Assante, G., Nasini, G., et al. Phanerosporic acid, a β-resorcylate obtained from Phanerochaete chrysosporium. Phytochemistry 28(10), 2803-2806 (1989).
Sphinganine (d20:0) is a natural isomer of dihydro-D-erythro-sphinganine (sphinganine (d18:0); that is a precursor of ceramide and sphingosine as well as a substrate for sphingosine kinases, which generate sphingosine-1-phosphate (d18:1) . In S. cerevisiae, the amount of sphinganine (d20:0) increases 10.8-fold in response to heat stress, indicating it is involved in heat stress adaptation. Sphinganine levels increase significantly in response to certain mycotoxins, including fumonisins as well as in some cancers. Sphinganine can block protein kinase C activation in some cases but not others.
Blasticidin A is a bacterial metabolite originally isolated from S. resistomycificus strain 2A-327. It inhibits aflatoxin production by A. parasiticus without affecting fungal growth (IC50s = 0.25 and 1.6 μM, respectively). Blasticidin A also decreases ribosomal protein levels and inhibits protein synthesis in S. cerevisiae.
Thielavin A is a fungal metabolite originally isolated from T. terricola that is related to thielavin B . Thielavin A inhibits COX, blocking both the conversion of arachidonic acid to prostaglandin H2 and the conversion of PGH2 to PGE2 . Thielavin A also inhibits glucose-6-phosphatase in rat liver microsomes (IC50 = 4.6 μM). It is a non-competitive inhibitor of α-glucosidase from S. cerevisiae (IC50 = 23.8 μM; Ki = 27.8 μM).
Linearmycin A is a polyene antibiotic that has been found inStreptomyces.1It is active against the bacteriaS. aureusandE. coli(MICs = 3.1 and 1.6 μg disc, respectively), the fungiS. cerevisiaeandC. albicans(MICs = 0.1 and 1.6 μg disc, respectively), and the plant pathogenic fungusA. nigerin disc assays (MIC = 0.2 μg disc). Linearmycin A induces lysis and degradation ofB. subtilisas a component ofStreptomycesMg1 extract.2 1.Sakuda, S., Guce-Bigol, U., Itoh, M., et al.Novel linear polyene antibiotics: LinearmycinsJ. Chem. Soc., Perkin Trans. 1182315-2319(1996) 2.Stubbendieck, R.M., and Straight, P.D.Escape from lethal bacterial competition through coupled activation of antibiotic resistance and a mobilized subpopulationPLoS Genet.11(12)e1005722(2015)
(–)-Voacangarine, an indole alkaloid isolated from V. africana, exhibits cytotoxicity towards various cell lines including HepG2, A375, MDA-MB-231, SH-SY5Y, and CT26 with IC50 values of 20 µg ml. Additionally, it demonstrates cytostatic effects on wild-type S. cerevisiae and is cytotoxic to Δrad3-e5 and Δrad6-1 mutant strains of S. cerevisiae, which have defects in DNA strand break repair and the mutagenic repair pathway, respectively.
Cyclin-dependent kinase 2 also known as cell division protein kinase 2. The protein encoded by this gene is a member of the cyclin-dependent kinase family of Ser Thr protein kinases. This protein kinase is highly similar to the gene products of S. cerevis
C18 Phytoceramide (t18:0 18:0) (Cer(t18:0 18:0)) is a bioactive sphingolipid found in S. cerevisiae, wheat grains, and the stratum corneum layer of mammalian epidermis. Cer(t18:0 18:0) is composed of a phytosphingosine backbone amine-linked to a C18 fatty acid chain. Cer(t18:0 18:0) has a role in regulation of apoptosis, cell differentiation, proliferation of smooth muscle cells, and inhibition of the mitochondrial respiratory chain. It also inhibits expression of the allergic cytokines IL-4, TNF-α, and transcription factors c-Jun and NF-κB in histone-stimulated murine skin tissue. Formulations containing cer(t18:0 18:0) have been used used in cosmetics as a skin protectants as they reduce water loss to prevent epidermal dehydration and irritation.
1,3-Dipalmitoleoyl-rac-glycerol is a diacylglycerol with palmitoleic acid at the sn-1 and sn-3 positions. It selectively inhibits α-glucosidase from S. cerevisiae over rat enzyme (IC50s = 4.45 and 9,326.5 μM, respectively). 1,3-Dipalmitoleoyl-rac-glycerol has been used in the formation of lipid bilayers to study the effects of membrane composition and the ionophore valinomycin on membrane potential.
C16 Phytoceramide (t18:0/16:0) is a phytoceramide, which is a family of sphingolipids found in the intestine, kidney, and extracellular spaces of the stratum corneum of the mammalian epidermis. C16 Phytoceramide (t18:0/16:0) is composed of a phytosphingosine backbone amine-linked to a C16 fatty acid chain. The levels of C16 phytoceramide (t18:0/16:0) increase following heat stress in S. cerevisiae. It has been used with other ceramides to create stratum corneum substitutes to study percutaneous penetration and psoriasis in vitro.