Excretion of three alkaloids from Simiao Pills in urine, feces, and bile between normal and type 2 diabetic rats / 中国中药杂志

This study investigated the differences in excretion kinetics of three alkaloids and their four metabolites from Simiao Pills in normal and type 2 diabetic rats. The diabetes model was established in rats by injection of streptozotocin, and the alkaloids in urine, feces, and bile of normal and diabetic rats were detected by LC-MS/MS to explore the effect of diabetes on alkaloid excretion of Simiao Pills. The results showed that 72 h after intragastric administration of the extract of Simiao Pills, feces were the main excretion route of alkaloids from Simiao Pills. The total excretion rates of magnoflorine and berberine in normal rats were 4.87% and 56.54%, which decreased to 2.35% and 35.53% in diabetic rats, which had statistical significance(P<0.05). The total excretion rates of phellodendrine, magnoflorine, and berberine in the urine of diabetic rats decreased significantly, which were 53.57%, 60.84%, and 52.78% of those in normal rats, respectively. After 12 h of intragastric administration, the excretion rate of berberine in the bile of diabetic rats increased significantly, which was 253.33% of that of normal rats. In the condition of diabetes, the excretion rate of berberine metabolite, thalifendine significantly decreased in urine and feces, but significantly increased in bile. The total excretion rates of jateorrhizine and palmatine in the urine increased significantly, and t_(1/2) and K_e changed significantly. The results showed that diabetes affected the in vivo process of alkaloids from Simiao Pills, reducing their excretion in the form of prototype drug, affecting the biotransformation of berberine, and ultimately increasing the exposure of alkaloids in vivo, which would be conducive to the hypoglycemic effect of alkaloids. This study provides references for the clinical application and drug development of Simiao Pills in diabetes.

Correlation between deleted in liver cancer-1 expression and clinicopathological parameters of human pituitary adenoma / 中华神经医学杂志

Objective To determine the expression level of deleted in liver cancer-1 (DLC-1)gene in human pituitary tumors, and assess the correlation between DLC-1 expression and clinicopathological parameters in these tumors. Methods DLC-1 and Ki-67 protein expressions were analyzed by immunohistochemistry and DLC-1 mRNA expression by quantitative RT-PCR in 84 pituitary adcnomas and 6 normal human adenohypophyses. Results Immunohistochemical results suggested that DLC-1 expression decreased and Ki-67 expression increased in the pituitary adenomas; Pearson correlation analysis showed that they were negatively correlated (r=-0.764,P=0.001).RT-PCR indicated that DLC-1 mRNA expression decreased in the pituitary adenomas; significantly decreased DLC-1 expression in invasive pituitary adenomas was noted as compared with that in non-invasive ones (P＜0.05). Conclusion Down-regulation of DLC-1 expression may contribute to the tumorigenesis of pituitary adenomas and DLC-1 can be the new target of molecular therapy.

Expression of leptin in pituitary adenomas and its clinical significance / 中华神经医学杂志

Objective To detect the expression of leptin in pituitary adenomas and investigate the association of leptin expression with the invasiveness and proliferation of pituitary adenomas. Methods Sixty-one surgical specimens of pituitary adenomas and the clinical data of the cases were obtained from the Department of Nenrosurgery, Changzheng Hospital between February and October in 2007. Immunohistochemical staining was used to detect the expressions of leptin and Ki-67 in the pituitary adenomas to investigate the role of leptin in the occurrence and development of the tumor. Results The overall leptin positivity rate in these pituitary adenomas was 34.4%, significantly lower than that in normal pituitary tissues (P<0.05). The Ki-67 index and diameter of the leptin-positive pituitary adenomas were significantly lower than those of leptin-negative tumors (P<0.05). The leptin expression rate was significantly lower in invasive pituitary adenomas than in non-invasive adenomas (P<0.05). Conlusions Compared with normal pituitary tissues, pituitary adenomas have reduced leptin expression, which is significantly correlated to Ki-67 index, tumor invasiveness and diameter but not to the patients' age or gender.