19,20-Epoxycytochalasin D is a fungal metabolite that has been found in the endophytic fungus Nemania sp. UM10M. It is active against the chloroquine-sensitive and -resistant strains of P. falciparum (MIC = 0.4 ng ml for both) without inducing cytotoxicity in Vero cells. It is cytotoxic to BT-549, LLC-PK11, and P388 cells (IC50s = 7.84, 8.4, and 0.16 µM, respectively) but not SK-MEL, KB, or SKOV3 cells up to a concentration of 10 µM.
CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50= 46 nM) and STAT3 activation.1It binds to STAT3 (Kd= 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM, respectively). It reduces tumor growth in B16 F10 mouse melanoma and HepG2 mouse xenograft models when administered at doses of 100 and 10 mg kg, respectively. 1.Huang, R., Jing, X., Huang, X., et al.Bifunctional naphthoquinone aromatic amide-oxime derivatives exert combined immunotherapeutic and antitumor effects through simultaneous targeting of indoleamine-2,3-dioxygenase and signal transducer and activator of transcription 3J. Med. Chem.63(4)1544-1563(2020)
Anhydroepiophiobolin A is a sesterterpenoid fungal metabolite that has been found in B. oryzae. It is cytotoxic to HepG2 and K562 cells (IC50s = 47.1 and 35.6 μM, respectively) as well as A549, SKOV3, SK-MEL-2, XF498, and HCT15 cells (IC50s = 1.6-1.9 μg/ml). Anhydroepiophiobolin A is phytotoxic to S. viridis and D. erucoides in a leaf puncture assay.
(+)-Macrosphelide A is a fungal metabolite originally isolated from Microsphaeropsis. It inhibits adhesion of HL-60 human leukemia cells to human umbilical vein endothelial cells (HUVECs) in a concentration-dependent manner. It also inhibits the growth of SKOV3 ovarian cancer cells in a concentration-dependent manner. (+)-Macrosphelide A inhibits the growth of Gram-positive bacteria, including B. subtilis, M. luteus, B. thuringiensis, and S. aureus (MICs = 143, 143, 57, and 57 μg/ml, respectively), but not Gram-negative bacteria or fungi.
IDO1-IN-7, a potent and selective indoleamine-2,3-dioxygenase-1 (IDO1) inhibitor, exhibits high potency with an IC 50 of 6.1 nM in the cellular assay (SKOV3). Apart from its inhibitory properties, IDO1-IN-7 also demonstrates immunomodulatory effects, contributing to its potential applications in cancer research.