Symbiotic Fungi Alter the Acquisition of Phosphorus in through Regulating Root Architecture, Plant Phosphate Transporter Gene Expressions and Soil Phosphatase Activities.

Plant roots can be colonized by many symbiotic fungi, whereas it is unclear whether and how symbiotic fungi including arbuscular mycorrhizal fungi and endophytic fungi promote phosphorus (P) uptake in plants. The objective of the present study was to analyze the effect of inoculation with a culturable endophytic fungus (), three arbuscular mycorrhizal fungi (, , and ), and mixture of . , .

Design, synthesis and biological evaluation of dipeptides as novel non-covalent 20S proteasome inhibitors.

Based on the interaction modes of the natural 20S proteasome inhibitors , we have previously discovered a dipeptide . To explore the SAR around compound , we designed and synthesized a series of dipeptides () with a fragment-based strategy. Among them, nine compounds showed significant inhibitory activities against the chymotrypsin-like activity of human 20S proteasome with IC values at the submicromolar level, which were comparable or even superior to the parent compound .

[Design, synthesis and biological evaluation of oxadiazole derivatives as xanthine oxidase inhibitors].

Xanthine oxidase (XO) is an important target for the treatment of hyperuricemia and gout. Based on the two known non-purine xanthine oxidase inhibitors, febuxostat and topiroxostat, 14 oxadiazole derivatives have been designed and synthesized. These compounds have been evaluated against XO and five of them exhibited significant inhibitory activities at the concentrations below 10 μmol·L(-1).

NPRL-Z-1, as a new topoisomerase II poison, induces cell apoptosis and ROS generation in human renal carcinoma cells.

NPRL-Z-1 is a 4β-[(4"-benzamido)-amino]-4'-O-demethyl-epipodophyllotoxin derivative. Previous reports have shown that NPRL-Z-1 possesses anticancer activity. Here NPRL-Z-1 displayed cytotoxic effects against four human cancer cell lines (HCT 116, A549, ACHN, and A498) and exhibited potent activity in A498 human renal carcinoma cells, with an IC50 value of 2.

[SAR of benzoyl sulfathiazole derivatives as PTP1B inhibitors].

Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. We have previously identified the benzoyl sulfathiazole derivative II as a non-competitive PTP1B inhibitor with in vivo insulin sensitizing effects. Preliminary SAR study on this compound series has been carried out herein, and thirteen new compounds have been designed and synthesized.

Effect of Ren meridian acupoints moxibustion on light propagation along the pericardium meridian at human wrist.

Objective: To explore the relationship between acupoints and meridians.

Methods: Researches were performed on 45 healthy people under the same conditions. The diffuse light intensity of the Pericardium meridian and its surrounding areas were measured before and after warming moxibustion on three acupoints [Shimen (RN5), Qihai (RN6), and Yinjiao (RN7)] of Ren meridian below umbilicus in the same way.

Spectroscopic studies on bilirubin aggregate at liquid/liquid interface.

Bilirubin (BR) aggregating at liquid/liquid interface was firstly detected by Fourier transform infrared (FTIR) imaging/spectroscopy combining with ultraviolet-visible (UV/Vis) absorption spectra. In the UV/Vis absorption spectra of BR aggregate, a new shoulder appeared at 474 nm, and BR absorption maximum underwent red shift from 450 nm to a longer wavelength at 497 nm, which indicates that BR aggregate was formed at the interface. Meanwhile, the BR molecule structure changed or conformation torsion, that is, the increase in orbit overlap or dihedral angle and the enhancement of exciton coupling.

Synthesis and evaluation of novel podophyllotoxin analogs.

Because prior studies have shown inconsistency between structure-activity relationships for podophyllotoxin derivatives as topoisomerase II inhibitors and cytotoxic agents, eight novel podophyllotoxin analogs were synthesized to further explore the effects of structural variations on both A and D rings on activity. The new compounds contain a 4,5-dimethoxy substituted A ring and opened D-ring variants and were prepared by appropriate functional and stereochemical operations at the methylenedioxy group, C7, C8, and C8'. Four compounds (15, 18, 21 and 22) demonstrated noticeable inhibitory activity against A549, DU145, KB and KBvin tumor cells, and the most active compound 18 showed IC(50) values less than 10 μg/mL.

[Design, synthesis and evaluation of malonic acid-based PTP1B inhibitors].

Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. Phosphotyrosine (pTyr) is the substrate for PTP1B dephosphorylation. Malonic acid moiety was used herein as a mimic of the phosphate group in pTyr, and novel malonic acid derivatives 1-7 were designed, synthesized and evaluated as PTP1B inhibitors.

Induction of cell cycle arrest by GL331 via triggering an ATM-dependent DNA damage response in HepG2 cells.

GL331, a topoisomerase II inhibitor, has been found to trigger DNA damage response (DDR) to induce cell cycle arrest. However, the underlying mechanism has not yet been fully understood. This study investigated the molecular mechanism involved in the GL331-induced cell cycle arrest via DDR in human hepatocellular carcinoma HepG2 cells.

[Design, synthesis and evaluation of novel 2H-1, 4-benzodiazepine-2-ones as inhibitors of HIV-1 transcription].

HIV-1 trans-activator of transcription (Tat) plays a critical role in HIV-1 transcription. Based on the beta-turn motif present in HIV-1 Tat, a series of novel benzodiazepine analogs were designed as beta-turn mimetics and prepared from p-chloro-nitrobenzene/2-phenylacetonitrile, p-toluidine/benzoyl chloride, or (Z)-7-nitro-5-phenyl-1H-benzo[e][1, 4]diazepin-2(3H)-one (nitrazepam) through different synthetic routes. Preliminary biological evaluation indicated that compound 30 exhibited inhibitory activity on HIV-1 tat-mediated LTR transcription with EC50 of 25.

PTP1B inhibitor improves both insulin resistance and lipid abnormalities in vivo and in vitro.

PTP1B is a negative regulator of insulin signaling pathway. This study investigated the effects of compound CCF06240, a PTP1B inhibitor, on insulin sensitivity and lipid metabolic abnormalities in vivo and in vitro, respectively. The insulin resistant IRM mouse model was induced by HFD.