Search

Three novel members of angucycline family named N05WA963A (1), B (2) and D (4), together with a new anthracycline named N05WA963C (3) were isolated from the culture broth of Streptomyces sp. N05WA963. The structures were elucidated on the basis of comprehensive spectral data analysis. All four compounds have shown antiproliferative effects on a panel of cancer cell lines such as SW620, K-562, MDA-MB-231, YES-4, T-98 and U251SP.

The shape of dendrimer amphiphiles has an unexpected effect on their self-assembly. A series of diaminobutane poly(propylenimine) generation 3 dendrimer (DAB-dendr-(NH(2))(16)) amphiphiles has been synthesized, bearing an average of five (PD5), three (PD3) and one (PD1) palmitoyl group(s) per dendrimer molecule. Additionally DAB-dendr-(NH(2))(16) was derivatized with a layer of poly(ethylene glycol) (PEG, degree of polymerization = 12) groups and conjugated to an average of 1 palmitoyl group at the PEG end (PPD1). A final amphiphile resulted from the conjugation of DAB-dendr-(NH(2))(16) with 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-succinimidylpropionate (DSPE-PEG(3400)-SPA), i.e.: DPD5 (with 4 DSPE-PEG arms). The critical micellar concentration in aqueous media followed the trend: DPD5

Dihydroorotate Dehydrogenase (DHODH) catalyzes the rate-limiting step in pyrimidine biosynthesis, and its inhibitors have been developed as drugs for treatment of immune diseases. We studied new DHODH inhibitors from microbial metabolites.We established a rapid and effective high throughput screening method for screening DHODH inhibitors from microbial metabolites. The active compounds were isolated from the candidate strain by column chromatography and preparative HPLC.We picked out F01WB-1315 strain as candidate from 4560 fungal strains. We isolated two active compounds F01WB-1315A and B, with IC50 of 0.07 microg/mL and 0.51 microg/mL, respectively. F01WB-1315B could completely inhibit the spleen lymphocytes proliferation stimulated by ConA in vitro, but F01WB-1315A only had 31.62% inhibitory activity. F01WB-1315A, B were identified to be Ascofuranone and Ascochlorin by their physicochemical properties, MS, 13C-NMR and 1H-NMR analysis.F01WB-1315A and B are two strong specific DHODH inhibitors and show moderate inhibitory activity against spleen lymphocytes proliferation.

In order to screen the active constituents of Vaccinium vitis-idaea L., the compounds absorbed into the rat blood after oral administration of ethanol extract of the stems and leaves of V. vitis-idaea (EEV) have been analyzed. Two compounds were detected in the plasma and identified as arbutin and fraxin, which are originally existed in the crude drug. Furthermore, the pharmacological effects of the two compounds involving EEV for curing acute and chronic respiratory tract infection were tested. The results showed that both arbutin and fraxin have the anti-inflammatory, anti-coughing and phlegm-removing effects. Therefore, it was ascertained that the arbutin and fraxin would be the main active constituents of V. vitis-idaea L.