Synthesis and antitumor activity evaluation of lamiridosin A derivatives.

A series of lamiridosin A derivatives were synthesized through simple procedures. Their antitumor activities were evaluated against EC9706, MGC803, and B16 cell lines in vitro. Several compounds showed potent antitumor activity, especially compound 10, with IC50 value of 2.36 µmol/L against MGC803 cell lines, is more potent than marketed positive drug 5-fluorouridine (5-FU).

[Chemical Constituents from Melissa officinalis Leaves].

OBJECTIVE: To investigate the chemical constituents of Melissa officinalis leaves. METHODS: The chemical constituents were separated by silica gel column chromatography and their structures were determined by spectroscopic experiments. RESULTS: 13 compounds were isolated and identified as protocatechuyl aldehyde(1), serratagenic acid(2), vanillin(3), 2α,3ß-dihydroxy-urs-12-en-28-oic acid(4), ursolic acid(5), oleanolic acid(6), daucosterol(7),2α,3ß,23,29-tetrahydroxyolean-12-en-28-oic acid-29-O-ß-D-gluco- pyranoside(8), luteolin(9) rosmarinic acid(10), luteolin-7-O-ß-D-glucoside (11), ß-stitosterol(12) and palmitic acid(13). CONCLUSION: Compounds 1 ~ 8 are separated from this plant for the first time and compounds 1-4 and 8 are isolated from this genus for the first time.

[Chemical constituents from Punica granatum flowers].

OBJECTIVE: To investigate the chemical constituents in the flowers of Punica granatum. METHODS: The chemical constituents were separated by silica gel column chromatography and their structures were determined by spectroscopic experiments. RESULTS: As a result, twelve compounds were isolated and identified as oleanolic acid (1), ursolic acid (2), palmitic acid (3), tricin (4), catechin (5), rutin (6), apigenin (7), apigenin-7-O-glucoside (8), 2S, 3S, 4S-trihydroxypentanoic acid (9), gallic acid (10), beta-stitosterol (11), and daucosterol (12). CONCLUSION: Compounds 3, 4, 7, 8 and 9 are separated from this plant for the first time, and compounds 3, 4 and 9 are isolated from this genus for the first time.

(4Z)-4-[(Cyclo-propyl-amino)(phen-yl)methyl-ene]-3-methyl-1-phenyl-1H-pyrazol-5(4H)-one.

In the title compound, C(20)H(19)N(3)O, the dihedral angles formed by the pyrazolone ring with the two phenyl rings are 64.27 (6) and 17.00 (6)°. The mol-ecular structure is stabilized by intra-molecular N-H⋯O and C-H⋯O hydrogen bonds. In the crystal, the mol-ecules are linked into chains along the b axis by inter-molecular C-H⋯O hydrogen bonds.

4-[(Z)-Allyl-amino-(phen-yl)methyl-ene]-3-methyl-1-phenyl-1H-pyrazol-5(4H)-one.

The title compound, C(20)H(19)N(3)O, exists in a keto-enamine tautomeric form. The pyrazolone ring makes dihedral angles of 20.52 (10) and 77.73 (5)° with the two phenyl rings and an intra-molecular N-H⋯O hydrogen bond occurs. A weak inter-molecular C-H⋯O hydrogen bond is observed in the crystal structure. The allyl group is disordered over two positions, with site-occupancy factors of 0.533 (5) and 0.467 (5).

[Relationship between soluble intercellular adhesion molecule-1 and severe pneumonia].

OBJECTIVE: It has been reported that soluble intercellular adhesion molecule-1 (sICAM-1) participates in many immune and inflammatory reactions. Its expression and role in severe pneumonia has not fully been understood. This study aimed to investigate the changes of sICAM-1 expression in severe pneumonia and the relationship between sICAM-1 and severe pneumonia in children. METHODS: Serum sICAM-1 levels were determined by the double antibody sand using ELISA in 50 children with severe pneumonia and 56 children with mild pneumonia. Fifty-two healthy children served as control group. RESULTS: Serum sICAM-1 levels in children with severe pneumonia (402.36 +/- 31.24 mu g/L) were remarkably higher than those in the mild pneumonia group (278.86 +/- 36.24 mu g/L) at the acute stage and higher than in the control group (180.74 +/- 21.46 mu g/L) (P < 0.01). Serum sICAM-1 levels in children with severe pneumonia decreased significantly at the recovery stage (198.56 +/- 12.63 mu g/L) (P < 0.01), which were not statistically different from those in the mild pneumonia group at the recovery stage and the control group. There were no significant differences in serum sICAM-1 levels among the severe pneumonia subgroups caused by different pathogens (bacteria, virus or Mycoplasma) at the acute stage. Serum sICAM-1 levels at the acute stage in children with severe pneumonia who were treated successfully were not significantly different from those in patients whose symptoms were partly improved. CONCLUSIONS: sICAM-1 might be involved in the inflammation course of severe pneumonia. It can severe as a marker of the diagnosis and the severity evaluation of severe pneumonia.

Pore-scale lattice Boltzmann simulation of flow and mass transfer in bioreactor with an immobilized granule for biohydrogen production.

The photo bioreaction combined with flow and mass transfer is simulated with pore-scale lattice Boltzmann (LB) method, which is the scenario of a bioreactor filled with a porous granule immobilized photosynthetic bacteria cells for hydrogen production. The quartet structure generation set (QSGS) is used to generate porous structure of the immobilized granule. The effects of porosity of the immobilized granule on flow and concentration fields as well as the hydrogen production performance are investigated. Higher porosity facilitates the substrate solution smoothly flowing through the porous granule with increasing velocity, and thus results in higher product concentration inside the immobilized granule. Additionally, the substrate consumption efficiency increases, while hydrogen yield slightly decreases with increasing porosity, and they tend to stable for the porosity larger than 0.5. Furthermore, the LB numerical results have a good agreement with the experimental results. It is demonstrated that the pore-scale LB simulation method coupling with QSGS is available to simulate the photo hydrogen production in the bioreactor with porous immobilized granules.

Two new dammarane-type glycosides from Phlomis umbrosa.

Two new dammarane-type glycosides, phlomisumbroside A (1) and phlomisumbroside B (2), together with 15 known compounds (3-17) were isolated from the leaves of Phlomis umbrosa Turcz. Their structures were established by the spectroscopic methods including 2D NMR techniques.

Purification and studies on characteristics of cholinesterases from Daphnia magna.

Due to their significant value in both economy and ecology, Daphnia had long been employed to investigate in vivo response of cholinesterase (ChE) in anticholinesterase exposures, whereas the type constitution and property of the enzyme remained unclear. A type of ChE was purified from Daphnia magna using a three-step procedure, i.e., Triton X-100 extraction, ammonium sulfate precipitation, and diethylaminoethyl (DEAE)-Sepharose™-Fast-Flow chromatography. According to sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE), molecular mass of the purified ChE was estimated to be 84 kDa. Based on substrate studies, the purified enzyme preferred butyrylthiocholine iodide (BTCh) [with maximum velocity (Vmax)/Michaelis constant (Km)=8.428 L/(min·mg protein)] to acetylthiocholine iodide (ATCh) [with Vmax/Km=5.346 L/(min·mg protein)] as its substrate. Activity of the purified enzyme was suppressed by high concentrations of either ATCh or BTCh. Inhibitor studies showed that the purified enzyme was more sensitive towards inhibition by tetraisopropylpyrophosphoramide (iso-OMPA) than by 1,5-bis(4-allyldimethylammoniumphenyl) pentan-3-one dibromide (BW284C51). Result of the study suggested that the purified ChE was more like a type of pseudocholinesterase, and it also suggested that Daphnia magna contained multiple types of ChE in their bodies.