Penicacids E-G, three new mycophenolic acid derivatives from the marine-derived fungus Penicillium parvum HDN17-478.

Three new mycophenolic acid derivatives, penicacids E-G (1-3), together with three known analogues, mycophenolic acid (4), 4'-hydroxy-mycophenolic acid (5) and mycophenolic methyl ester (6), were isolated from a marine-derived fungus Penicillium parvum HDN17-478 from a South China Sea marine sediment sample. The structures of compounds 1-3 were elucidated by HRMS, NMR, and Mosher's method. Among them, compounds 1 and 2 were the first examples of mycophenolic acid analogs with a double bond at C-3'/C-4' position. The cytotoxicity of 1-6 was evaluated against the HCT-116, BEL-7402, MGC-803, SH-SY5Y, HO-8910 and HL-60 cell lines, and compounds 4 and 6 showed potent cytotoxicity with IC50 values ranging from 1.69 to 12.98 µmol·L-1.

Study on the mechanism of anti-MIRI action of total flavones of Fructus Chorspondiatis by PET/CT imaging.

BACKGROUND: To investigate anti myocardial ischemia/reperfusion injury (MIRI) action of total flavones of Fructus Chorspondiatis (TFFC) in rats by 13N-ammonia micro PET/CT imaging, etc. METHODS: Male Sprague-Dawley rats were randomly divided into 6 groups. Micro PET/CT imaging was performed before and after modeling to calculate the volume (VOI) and SUVmean of myocardial ischemic area. The oxidative stress index [(superoxide dismutase (SOD), malondialdehyde (MDA)] and the marker enzymes [creatine kinase (CK), lactate dehydrogenase (LDH)] of myocardial injury were detected. The pathological changes of myocardial were observed via HE staining. A MIRI model of rat cardiomyocytes in vitro was established, the damage and apoptosis of myocardial cells in each group were observed, and the apoptosis rate of cardiomyocytes was detected. RESULTS: The imaging viscosities of the imaging agents were observed at 24 and 48 h in each group. The VOI of 24 h imaging was (6.33±2.02), (6.01±1.56) and (3.32±0.86) mm3, respectively. The VOI of 48 h imaging was (3.31±1.33), (2.61±1.01) and (1.32±0.58) mm3. The 72 h imaging medium and high dose group recovered, while the low dose group still saw sparseness with (1.26±0.68) mm3 VOI. The ischemic (SUVmean) gradually increased with time. Metabolism gradually recovered (F=121.82, 450.82, 435.75, P<0.05). The three doses of TFFC can eliminate free radicals and reduce the damage of myocardial injury. Amongst them, the high-dose group had a better effect on SOD, and the middle-dose group had a better effect on MDA and LDH. The low-dose group affected CK, and a significant difference was observed compared with the control group (P<0.05). After administration, the morphology of myocardial cells in each dose group was improved to some extent. Nuclear pyknosis, rupture, the apoptosis rate, etc. were significantly reduced, the number of cells increased. The high dose group showed the most obvious improvement. CONCLUSIONS: The PET/CT imaging method can detect non-invasive, in vivo and dynamic MIRI, and can accurately evaluate the protective effect of traditional Mongolian medicine TFFC on MIRI. The Anti-MIRI of TFFC can scavenge free radicals, reduce oxidative stress damage, inhibit apoptosis, affect the activity of related enzymes.

Fusaricates H-K and fusolanones A-B from a mangrove endophytic fungus Fusarium solani HDN15-410.

Seven compounds including four undescribed fusaric acid derivatives, namely fusaricates H-K, and two undescribed γ-pyrone derivatives, named fusolanones A-B, as well as a known compound fusaric acid, were isolated from a mangrove endophytic fungus Fusarium solani. Fusaricates H-K represent the first cases of fusaric acid butanediol esters and are diastereoisomers. Their structures including absolute configurations were elucidated based on NMR, MS, chemical synthesis, chiral HPLC analysis and ECD calculations. The antibacterial activity of all undescribed compounds were tested and fusolanone B showed the best activity with MIC value 6.25 µg/mL on Vibrio parahaemolyticus.

α-Pyrone derivatives with cyto-protective activity from two Takla Makan desert soil derived actinomycete Nocardiopsis strains recovered in seawater based medium.

In this paper, we described the discovery of two Nocardiopsis strains HDN154-146 and HDN154-168 from Takla Makan desert soil samples using seawater based medium. Chemical investigation of these two strains led to the discovery of eight new α-pyrone derivatives named nocahypyrones A-H (1-8), together with one known analogue germicidin G (9). The structures of these compounds, including absolute configurations, were elucidated by extensive NMR, MS, and CD analyses. Compounds 1-9 were tested for their cyto-protective activities and for the first time we found α-pyrones 5 and 8 exhibited capabilities to induce expression of phase II detoxifying enzymes.

Current and emerging options for taxol production.

Paclitaxel (trademark "Taxol") is a plant-derived isoprenoid natural product that exhibits potent anticancer activity. Taxol was originally isolated from the Pacific yew tree in 1967 and triggered an intense scientific and engineering venture to provide the compound reliably to cancer patients. The choices available for production include synthetic and biosynthetic routes (and combinations thereof). This chapter focuses on the currently utilized and emerging biosynthetic options for Taxol production. A particular emphasis is placed on the biosynthetic production hosts including macroscopic and unicellular plant species and more recent attempts to elucidate, transfer, and reconstitute the Taxol pathway within technically advanced microbial hosts. In so doing, we provide the reader with relevant background related to Taxol and more general information related to producing valuable, but structurally complex, natural products through biosynthetic strategies.