A new benzamide derivative from rice fermentation of Streptomyces sp. CPCC 202950 / 中国中药杂志

Eight compounds were isolated from the rice fermentation of Streptomyces sp. CPCC 202950 by a combination of various chromatographic techniques including column chromatography over silica, Sephadex LH-20, flash C₁₈, and reversed-phase HPLC. Their structures were identified as 3-[(3'-amino-3'-oxoprop-1'-en-2'-yl)oxy]benzamide (1), m-hydroxybenzamide (2), leptosphaepin (3), 5-methyluracil (4), feruloylamide (5), p-hydroxyphenylacetoamide (6), vanillamide (7), cyclo (L-val-L-ala) (8). Among them, 1 was a new benzamide analogue, and 2 was a new natural product. In the preliminary assays, none of the compounds 1-8 exhibited obvious inhibition of HIV-1 protease activity, and toxic with the Hela, HepG2, and U2OS cells. (IC₅₀ > 10 μmol•L⁻¹).

Separation, purification and primary reverse cholesterol transport study of Cordyceps militaris polysaccharide / 中国中药杂志

The authors designed to separate, purify and determine the monosaccharide composition of the polysaccharide from Cordyceps militaris, and study its effect on reverse cholesterol transport in vivo by isotope tracing assay. Polysaccharides were separate and purify by ion exchange column Q-sepharose Fast Flow and size exclusion column Sephacryl S200HR; the molecular weight and monosaccharide composition of the polysaccharides were determined by high performance gel permeation chromatography and high performance liquid chromatography coming with pre-column derivation, respectively. Finally, three purified polysaccharides CMBW1, CMBW2 and CMYW1 were obtained, their total carbohydrate contents were 87%, 89%, 95%, respectively; their protein contents were 6.5%, 1.3%, 2.8%, respectively; their molecular weights were 772.1, 20.9, 13.2 kDa, respectively; CMBW1 was composed of mannose, glucosamine, rhamnose, glucuronic acid, glucose, galactose and arabinose with a molar ratio of 7.25: 0.17: 1.29: 0.23: 6.30: 11.08: 0.79; CMBW2 was composed of mannose, glucosamine, galactose and arabinose with a molar ratio of 2.40: 0.16: 2.92: 0.24; CMYW1 was composed of mannose, glucosamine, glucuronic acid and glucose with a molar ratio of 0.59: 0.57: 0.45: 25.61. Polysaccharide at 50 mg x kg(-1) could significantly improve the transport of 3H- cholesterol to blood and excretion from feces. All of the three purified polysaccharides CMBW1, CMBW2 and CMYW1 were heteropolysaccharide; and they could improve reverse cholesterol transport in vivo, the underlying mechanisms are being studied.

The relationship between the activation of ERK and the up-regulation of uPA in laryngeal squamous cell carcinoma / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#To study the relationship between the expression of extracellular signal-regulated kinase (ERK) and the expression of urokinase-type plasminogen activator (uPA) as well as its effect on the development of laryngeal squamous cell carcinoma (ISCC).@*METHOD@#Western blot was used to detect ERK1/2 protein expression, meanwhile, the change of ERK1/2 activity was examined to measure its efficiency of phosphate transferase in 40 LSCC. Immunohistochemistry was applied to detect uPA protein expression. The correlation of each factor with relevant clinical factor was statistically analyzed.@*RESULT@#Expression of ERK1/2 showed a positive linear correlation (P < 0.05). Neither ERK1 nor ERK2 expression was significantly related to T-grades, histological classes and cervical lymph node status. Neither T-grades, nor histological classes was significantly related to ERK1/2 activity or uPA protein expression. There was significant correlation between ERK1/2 activity and cervical lymph node status and between uPA protein expression and cervical lymph node status (P < 0.05). ERK1/2 protein expression was correlated with neither ERK1/2 activity nor uPA protein expression, but there was a significant positive linear association between ERK1/2 activity and uPA protein expression (P < 0.05).@*CONCLUSION@#Abnormal activation of ERK may play an important role in cervical lymph node metastasis of LSCC by up-regulation of uPA expression.