ABSTRACT
Phenylpropanoid glycoside compound 1, the natural anti-tumor compound isolated from the erial parts of Cirsium japonicum, was first totally synthesized using easily available materials in short, convenient route with overall yield of 13.9%.
Subject(s)
Antineoplastic Agents, Phytogenic/chemical synthesis , Antineoplastic Agents, Phytogenic/pharmacology , Cirsium/chemistry , Glycosides/chemistry , Glycosides/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Molecular Structure , Plant Extracts/chemistryABSTRACT
Anemarchalconyn (1) and anemarcoumarin A (2), the natural bioactive compounds isolated from the rhizomes of Anemarrhena asphodeloides Bunge (Liliaceae), were first totally synthesized using easily available materials in short, convenient routes with overall yields of 32 and 48%.
Subject(s)
Anemarrhena/chemistry , Coumarins/chemical synthesis , Phenols/chemical synthesis , Molecular Structure , Phenols/chemistry , Rhizome/chemistryABSTRACT
The present study aimed to clarify the effect of berberine on the chloride channels in human colorectal carcinoma cells (SW480). The whole-cell patch clamp technique was used to detect the Cl(-) current activated by berberine. The physiological and pharmacological characteristics of the current were clarified by changing the osmotic pressure of extracellular perfusate and applying chloride channel blockers. The results showed that, under isotonic conditions, the background current of SW480 cells was weak and stable. A large current was induced by perfusing the cells with the isotonic solution containing berberine (10 nmol/L), current density being (85.8 ± 4.6) pA/pF at +80 mV, (-71.9 ± 3.5) pA/pF at -80 mV, with a latency of (115.6 ± 21.7) s. The chloride current showed weak outward rectification and negligible time- and voltage-dependent inactivation. The reversal potential (-5.5 mV ± 1.2 mV) of the current was close to the calculated equilibrium potential for Cl(-) (ECl = -0.9 mV). Experiments under different osmotic pressures showed that the properties of hypotonicity-activated current recorded in SW480 cells were similar to those of the current induced by berberine, and hypertonic solutions suppressed the berberine-induced current by (98.6 ± 2.3)%. On the other hand, berberine-induced Cl(-) current was significantly inhibited by the chloride channel blockers NPPB (100 µmol/L) and tamoxifen (20 µmol/L), with the inhibition ratios of (83.1 ± 3.6)% and (95.6 ± 1.2)% respectively. These results suggest that berberine can activate the chloride channels that are sensitive to NPPB and tamoxifen, as well as the changes of cell volume in human colorectal carcinoma cells.
Subject(s)
Berberine/pharmacology , Chloride Channels/drug effects , Colorectal Neoplasms/metabolism , Cell Line, Tumor , Colorectal Neoplasms/pathology , Humans , Nitrobenzoates/pharmacology , Osmotic Pressure/drug effects , Patch-Clamp Techniques , Tamoxifen/pharmacologyABSTRACT
Cyanoimidation of aldehydes using cyanamide as a nitrogen source and using NBS as an oxidant was achieved in high yields without the addition of a catalyst. The method has several advantages, including mild conditions, simple workflow, and inexpensive reagents. The reaction proceeds in a one-pot manner, giving rise to the formation of intermolecular C-N and C-O bonds. Subsequently, the substituted N-cyanobenimidate products may also undergo a cyclization reaction to give l,2,4-triazole derivatives in high yields.
Subject(s)
Aldehydes/chemistry , Triazoles/chemical synthesis , Catalysis , Combinatorial Chemistry Techniques , Cyclization , Molecular Structure , Nitriles/chemistry , Oxidants/chemistry , Triazoles/chemistryABSTRACT
A new big pi-conjugated, symmetrical fluorene derivative, 9, 9-bis(2-ethylhexyl)-2,7-bis(2-(4-methoxy) benzene-2, 1-ethenyl) fluorene (abbreviated as MO-Flu-MO) was synthesized and characterized by elemental analysis, mass spectral, UV-Vis and IR spectral. Spectral characteristics of this compound, including linear absorption spectral and one-photon fluorescence spectral, were measured in acetonitrile, methylene chloride, tetrahydrofuran and hexane at room temperature. It was found that solvent effects have different influence on absorption spectral and fluorescence spectral, major reasons of such spectral behavior are discussed.
Subject(s)
Fluorenes/chemistry , Spectrum Analysis , Fluorenes/chemical synthesis , Fluorescence , Hexanes/chemistry , Methylene Chloride/chemistry , Models, Chemical , Molecular Structure , Solvents/chemistry , Spectrometry, Fluorescence , Spectrophotometry, Infrared , Spectrophotometry, UltravioletABSTRACT
OBJECTIVE: To investigate association of vitamin D receptor (VDR) gene polymorphisms with the susceptibility to chronic periodontitis (CP) of Han Nationality. METHODS: Buccal swabs from 166 patients with severe, moderate and mild CP respectively and 80 matched control individuals were collected. DNA was extracted from these buccal swabs using Chelex-100 method. VDR BsmI, ApaI, TaqI were tested with polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP). The distribution of the genotypes and allele frequencies in the patient and control groups were analyzed. RESULTS: The frequency of VDR ApaI allele A was significantly higher among patients with CP than controls. Frequencies of VDR ApaI allele A were significantly higher in severe CP patients than in moderate CP and mild CP respectively. There was no significant difference in the genotype distribution or the allele frequencies of VDR BsmI and TaqI between the controls and CP patients. CONCLUSIONS: These data indicate that VDR ApaI allele A may be related to the susceptibility to CP in Han Nationality.
Subject(s)
Chronic Periodontitis/genetics , Genetic Predisposition to Disease , Polymorphism, Genetic , Receptors, Calcitriol/genetics , Adult , Aged , Alleles , Asian People/genetics , Female , Gene Frequency , Humans , Male , Middle AgedABSTRACT
OBJECTIVE: To study the relationship between zeta chain level of peripheral blood T/NK cells and tumor progression in renal-cell carcinoma and bladder cancer and its clinical significance. METHODS: The peripheral blood mononuclcear cells in 58 patients with renal cell carcinoma, 22 patients with bladder cancer and 14 healthy blood donors were examined by flow cytometry with fluorescent anti-CD3 (for T cells), or anti-CD56 (for NK cells) and anti-zeta chain monoclonal antibodies. RESULTS: The zeta chain expression of T cell and NK cell in stage I, II and III renal-cell carcinoma decreased to 59.5%, 37.6%, 21.3% and 62.2%, 27.1%, 18.8% of the healthy control level, respectively. That in stage I, II and III bladder cancer decreased to 37.6%, 29.5%, 18.9% and 35.4%, 20.8%, 5.8% of the control level, respectively. T and NK cell zeta chain levels in 17.5% (14/80) of the patients were within the normal range. T/NK ratios of peripheral blood in stage III patients were remarkably lower than those of the healthy donor. CONCLUSION: Reduced T and NK zeta chain levels and T/NK ratio in the renal-cell carcinoma and bladder cancer are generally consistent with tumor progression. The patients with normal T and NK zeta chain level may be indicated for immunotherapy.
