Studies on flavonoids from Derris eriocarpa / 中国中药杂志

Derris eriocarpa, a traditional Chinese medicine belonging to the family of Leguminosae, is widely distributed mainly over Yunnan, Guangxi and Guizhou of China. Modern pharmacological researches on this herb showed that it had extensive bioactivities, such as promoting urination, removing dampness and cough and reducing inspissated mucus and other biological activities. The extensive studies on the chemical constituents of this plant have resulted in the isolation of triterpenoids, steroids, fatty acid and others, but the flavone compounds haven't reported before. In our further research on the ethyl acetate of this plant, nine flavone compounds were obtained by column chromatography on silica gel, Sephadex LH-20, semi-prep HPLC, polyamide column chromatography and recrystallization for separation and purification. The structures were determined on the basis of extensive spectroscopic analysis, including MS, NMR experiments and comparison with spectroscopic data in the literature, respectively, as diosmetin (1), 3, 3'-di-O-methylquercetin (2), afromosin (3), 6, 3'-dihydroxy-7, 4'-dimethoxyisoflavone (4), odoratin (5), 7, 3'-dihydroxy-8, 4'-dimethoxyisoflavone (6), 6, 4'-dihydroxy-7, 3'-dimethoxyisoflavone (7), 5, 7, 4'-trihydroxy-3, 3', 5'-trimethoxyflavone (8), and alpinumisoflavone (9). All these compounds were isolated from Derris eriocarpa How for the first time. And the in vitro assays showed that compound 2 possessed moderate inhibitory activity against human cancer cells K562 and HEL.

The expression and significance of CD151 in pituitary adenomas / 中国应用生理学杂志

<p><b>OBJECTIVE</b>To investigate the expression and significance of CD151 in pituitary adenomas.</p><p><b>METHODS</b>Thirty-six pituitary adenomas were collected immediately after surgery together with five normal pituitary tissue. Real time-PCR, Western blot and immunohistochemistry analysis were performed to detect the expression of CD151 mRNA and protein in thirty-six pituitary adenomases and five normal pituitary tissues.</p><p><b>RESULTS</b>The expression of CD151 in all pituitary adenomases was observed to be significantly higher than that in normal pituitary tissues by Western blot, real time PCR, and immunohistochemistry analysis (P < 0.01). The expression levels of protein and mRNA in invasive pituitary adenomas were much higher than those in non-invasive pituitary adenomas (P < 0.01).</p><p><b>CONCLUSION</b>The results suggested that the expression of CD151 was closely correlated with malignant degree of pituitary adenomas, which indicated the expression of CD151 was intimately correlated with occurrence and development of pituitary adenomas. Detecting CD151 might be a vital index to predict prognosis of pituitary adenomas.</p>

PDK1 plays a critical role in regulating cardiac function in mice and human / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>PDK1 is an essential protein kinase that plays a critical role in mammalian development. Mouse lacking PDK1 leads to multiple abnormalities and embryonic lethality at E9.5. To elucidate the role of PDK1 in the heart, we investigated the cardiac phenotype of mice that lack PDK1 in the heart in different growth periods and the alteration of PDK1 signaling in human failing heart.</p><p><b>METHODS</b>We employed Cre/loxP system to generate PDK1(flox/flox): α-MHC-Cre mice, which specifically deleted PDK1 in cardiac muscle at birth, and tamoxifen-inducible heart-specific PDK1 knockout mice (PDK1(flox/flox):MerCreMer mice), in which PDK1 was deleted in myocardium in response to the treatment with tamoxifen. Transmural myocardial tissues from human failing hearts and normal hearts were sampled from the left ventricular apex to analyze the activity of PDK1/Akt signaling pathways by Western blotting.</p><p><b>RESULTS</b>PDK1(flox/flox): α-MHC-Cre mice died of heart failure at 5 and 10 weeks old. PDK1(flox/flox) -MerCreMer mice died of heart failure from 5 to 21 weeks after the initiation of tamoxifen treatment at 8 weeks old. We found that expression levels of PDK1 in human failing heart tissues were significantly decreased compared with control hearts.</p><p><b>CONCLUSION</b>Our results suggest that PDK1 signaling network takes part in regulating cardiac viability and function in mice, and may be also involved in human heart failure disease.</p>

Human bone marrow stromal cells facilitate the cord blood CD34+ cells ex vivo expansion and short-term engraftment in NOD/SCID mice / 中华血液学杂志

<p><b>OBJECTIVE</b>To explore the potential of human bone marrow stromal cells (MSCs) as the feeding-layer to promote ex vivo expansion of cord blood CD34+ cells and engraftment of the expanded cells in NOD/SCID mice.</p><p><b>METHODS</b>Human MSCs were routinely isolated and cultured. MSCs at passage 3 were used as feeding-layer for the expansion of cord blood CD34+ cell in the presence of thrombopoietin (TPO), flt3/flk2 ligand (FL), stem cell factor (SCF) and granulocyte-colony stimulating factor (G-CSF). The engraftment potential between unexpanded and expanded cord blood cells transplanted into NOD/SCID mice was compared.</p><p><b>RESULTS</b>The total nucleated cells (TNC), CD34 cells and colony forming units (CFUs) in the MSC feeding culture were increased by 111.6-, 19.3- and 58-fold after 1 week expansion and 532.8-, 41.3- and 563.5- fold increased after 2 weeks expansion respectively as compared with that in non MSC feeding culture. In transplant experiment, the percentage of human CD45+ cells (45.3% -59.1%) in bone marrow of recipient mice transplanted with the MSC feeding expanded cells was the highest in all the groups at six weeks after transplantation.</p><p><b>CONCLUSION</b>Human MSCs enhance CB CD34+ cells in vitro expansion and their capacity of short-term engraftment in NOD/SCID mice.</p>

Study on skin toxicology and penetration enhancement of skin absorption of volatile oil extracted from tender branchers of Camellia oleifera / 中国中药杂志

<p><b>OBJECTIVE</b>To study the toxicity on skin and penetration effect of volatile oil from tender branchers of Camellia oleifera on nitrendipine, baicalin, nimesulide for percutaneous obsorption.</p><p><b>METHOD</b>Acute skin toxicity, irritation and allergy on rats were tested, and mouse skin in vitro was applied for studying the effects of different concentrations of volatile oil in nitrendipine, baicalin, nimesulide on drug permeation.</p><p><b>RESULT</b>Different dosage volatile oil had no acute toxicity, irritation or hypersensitive effects. Compared to azone, more powerful enhancement effects of volatile oil at different concentration on nitrendipine, baicalin, nimesulide were very obvious.</p><p><b>CONCLUSION</b>This paper firstly reported the results of experiment about the toxicity to skin and penetr-ation effect of volatile oil from tender branches of C. oleifera.</p>

Structure-activity relationships of salicylic acid and its analogs in the inhibitory action on beta-lactamase / 药学学报

<p><b>AIM</b>Nineteen compounds related to salicylic acid were evaluated for their in vitro activity of inhibiting beta-lactamase isolated from a resistant strain of Pseudomonas aeruginosa, and their structure-activity relationships were examined.</p><p><b>METHODS</b>Nitrocefin method was used.</p><p><b>RESULTS</b>The 50% inhibitory concentration (IC50) of salicylic acid inhibiting beta-lactamase was 22 mmol x L(-1); four analogs had IC50 lower than that of salicylic acid; fifteen analogs had IC50 higher than that of salicylic acid.</p><p><b>CONCLUSION</b>Examination of the structure-activity relationships of the compounds revealed that carboxyl group and adjoining hydroxyl group were active group, and replacement of adjoining hydroxyl by carboxyl increased activity nearly 4-fold. Moreover, addition of a sulfonic group at C-5 and nitro group at C-3, 5 of benzenoic ring of salicylic acid resulted in a 2-fold to 3-fold increase in activity, addition of a amino group at C-5 of benzenoic ring of salicylic acid decreased activity, add addition of -Cl or -F at C-2,4 position of benzenoic ring of benzoic acid did not show activity.</p>

Study on amelioration of aminoguanidine on diabetic neuropathy and its mechanism / 中国药理学通报

Aim: To determine whether aminoguanidine increases the motor neve conduction velocity of db/db mice and why. Mothods: Motor neve conduction velocity was assayed by Powerlab/8s multipurpose physiological recorder. Advanced glycosylation end products of db/db mice kidney were determined by fluorometer. Results Motor neve conduction velocity of 6 months db/db mice treated with Aminoguanidine for 5 months increased significantly. Conclusion: Aminoguanidine can prevent the decrease of the motor neve conduction velocity of db/db mouse by decreasing the advanced glycosylation end products.