title: Three new pigment protein tyrosine phosphatases inhibitors from the insect parasite fungus Cordyceps gracilioides: terreusinone A, pinophilin C and cryptosporioptide A.
abstract: Three new pigment compounds--terreusinone A (1), pinophilin C (2) and cryptosporioptide A (3)-were isolated from a solid culture of Cordyceps gracilioides. The structures of these compounds were determined by extensive spectroscopic analysis including HRESIMS, 1D- and 2D-NMR. The structure of terreusinone A (1) was further confirmed by single-crystal X-ray crystallographic diffraction analysis. In an in vitro activity assay, 1, 2 and 3 exhibited high inhibitory activity against PTP1B, SHP2, CDC25B, LAR and SHP1. Terreusinone A (1) inhibited PTP1B, SHP2, CDC25B, LAR and SHP1 enzyme with IC50 values 12.5, >50, 4.1, 10.6, 5.6 µg/mL, respectively; pinophilin C (2) with IC50 values 6.8, 8.0, 4.5, 4.7, 3.4 µg/mL, respectively; and cryptosporioptide A (3) with IC50 values 7.3, 5.7, 7.6, >50, 4.9 µg/mL, respectively.
authors: College of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, China. weipeiyao_218@163.com.
authors: Pei-Yao
authors: PY
authors: Wei
authors: College of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, China. liulinxia.hi@163.com.
authors: Lin-Xia
authors: LX
authors: Liu
authors: College of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, China. liuting61800@163.com.
authors: Ting
authors: T
authors: Liu
authors: College of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, China. hyperchuan@aliyun.com.
authors: Chuan
authors: C
authors: Chen
authors: College of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, China. duqiangluo@163.com.|Biotechnology Center of Hebei Province, Hebei University, Baoding 071002, China. duqiangluo@163.com.
authors: Du-Qiang
authors: DQ
authors: Luo
authors: Biotechnology Center of Hebei Province, Hebei University, Baoding 071002, China. shibaozhong111@163.com.
authors: Bao-Zhong
authors: BZ
authors: Shi
mesh_terms: D000179:Acrylates / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D000818:Animals; D001517:Coleoptera / Q000382:microbiology*; D032661:Cordyceps / Q000737:chemistry*; D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D015394:Molecular Structure; D010860:Pigments, Biological / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D061065:Polyketides / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors*
chemical_list: D000179:Acrylates; D004791:Enzyme Inhibitors; D010860:Pigments, Biological; D061065:Polyketides; C000594269:cryptosporioptide A; C000604244:pinophilin C; C000604242:terreusinone A; D017027:Protein Tyrosine Phosphatases; C036658:acrylic acid