金乌香冲剂中槟榔碱定量方法研究

对金乌香冲剂中槟榔碱进行了酸性染料比色法定量方法研究，结果表明在pH=5．0时，槟榔碱可与溴甲酚绿生成稳定呈色离子对，在槟榔碱浓度范围1．65μg／mL～10．4μg／mL内线性关系良好，r=0．9992，平均回收率99．7％，RSD=2．1％（n=5）。     

Effect of benactyzine and arecoline on the45Ca uptake by rat brain nerve endings

The effect of the central cholinolytic benactyzine and the cholinomimetic arecoline on the uptake of⁴⁵Ca by rat brain synaptosomes was studied in vitro. Benactyzine was shown to cause biphasic changes (a decrease followed by an increase) in the intensity of uptake of the isotope, whereas arecoline led to a rapid initial increase in⁴⁵Ca uptake. Benactyzine was shown to depress the effect of arecoline and depolarization on uptake of the isotope. It is concluded that the increase in⁴⁵Ca uptake through the action of arecoline is connected with activation of Nachannels. Benactyzine, on the other hand, reduces the permeability of the these channels for⁴⁵Ca and activates the Ca-channels proper.(Presented by Academician of the Academy of Medical Sciences of the USSR S. S. Golikov.) Translated from Byulleten' Éksperimental'noi Biologii i Meditsiny, Vol. 86, No. 9, pp. 301–304, September, 1978.     

环氧合酶-2在口腔黏膜下纤维性变癌变过程中作用研究

目的 探讨环氧合酶-2（COX-2）在口腔黏膜下纤维性变（OSF）癌变组织中的表达，观察槟榔碱对人口腔角质形成细胞（KC）COX-2表达的影响。方法 应用免疫组化SP法检测15例OSF癌变组织，30例OSF组织，10例正常口腔黏膜中COX-2蛋白表达，Western-blot法检测不同浓度槟榔碱（30、60、90ug／mL）对KCCOX-2蛋白表达的影响。结果 COX-2在正常黏膜组织中无明显表达，在OSF组织及OSF癌变组织中阳性表达率分别是36．7％（11／30）、80．0％（12／15），且癌变组织中表达强度明显高于OSF组织（P〈0．05）；槟榔碱呈剂量依赖性增加KCCOX-2蛋白表达，不同浓度槟榔碱组均高于空白对照组（P〈0.05）。结论 COX-2在OSF癌变组织中表达异常增高，槟榔碱能增加KCCOX-2表达，COX-2过度表达可能在OSF癌变过程中起一定作用。     

槟榔碱对血管内皮细胞增殖活动影响的实验研究

目的：观察槟榔碱对血管内皮细胞（endothelial cell,EC）增殖活动的影响。方法：采用MTT法检测槟榔碱干预后的EC存活率。结果：30～120μg/ml槟榔碱抑制EC的增殖,并呈浓度和时间依赖效应（P〈0.05）,60μg/ml槟榔碱干预EC24h细胞数量减少,120μg/ml槟榔碱干预EC72h细胞存活率达到最低（p〈0.05）。结论：一定浓度范围的槟榔碱可抑制EC的增殖。     

槟榔碱对小鼠酒精急性中枢抑制作用的影响

目的:探讨非选择性毒蕈碱受体(M受体)激动剂—槟榔碱,对小鼠酒精急性中枢抑制作用的影响。方法:测定小鼠的自主活动,观察槟榔碱对酒精诱导的小鼠低活动性的影响。建立酒精诱导小鼠翻正反射消失(loss of therighting reflex,LORR)的模型,观察槟榔碱对LORR潜伏期和持续时间的影响。结果:酒精(1.0、2.0、3.0 g.kg-1)和槟榔碱(0.25、0.51、.0 mg.kg-1)均可剂量依赖性地抑制小鼠的自主活动,但槟榔碱对酒精诱导的小鼠低活动性无影响。槟榔碱(0.25、0.5、1.0 mg.kg-1)对酒精诱导小鼠LORR的潜伏期无影响,但可显著缩短LORR的持续时间。结论:槟榔碱可以拮抗酒精诱导小鼠LORR的药理作用,提示槟榔碱可能具有一定的醒酒作用。     

槟榔不同工艺处理品中3种生物碱的含量比较

目的:建立测定槟榔中槟榔碱、槟榔次碱、去甲基槟榔次碱的HPLC-DAD方法,并比较不同处理工艺对3种生物碱含量的影响.方法:采用Partisil 10 SCX阳离子色谱柱(4.6 mm ×250 mm,10 μm),流动相乙腈-0.5％磷酸(三乙胺试液调pH 3.8)(50∶50),流速1 mL· min-1,检测波长215 nm,柱温25℃.考察不同烘烤时间和不同煮沸时间条件下,槟榔皮、核中3种生物碱含量的变化.结果:生物碱的含量随烘烤或者煎煮时间的延长而降低,在不同工艺条件下降低程度不同,100℃烘烤8h后生物碱的损失率约50％,煮沸0.5h后损失率高达80％,说明煎煮对槟榔皮、核中生物碱含量的影响较烘烤要大.结论:所建立的HPLC-DAD方法适用于槟榔生物碱的定量分析,为开发槟榔药食两用的安全剂量标准提供实验依据.     

Heat shock protein 27 expression in areca quid chewing-associated oral squamous cell carcinomas

Oral Diseases (2012) 18 , 713–719 Objectives: Heat shock protein (HSP) 27 is a low‐molecular‐weight protein that functions as a molecular chaperone and plays a cytoprotective role through its antioxidant activity during cell stress. Areca quid chewing is associated with the high incidence of oral squamous cell carcinomas (OSCCs) in Taiwan. The aim of this study was to compare heat shock protein 27 (HSP27) expression in OSCCs and the normal oral tissues. Methods: Forty‐eight OSCCs from areca quid chewers and ten normal oral tissue biopsy samples without areca quid chewing were analyzed by immunohistochemistry for HSP27. The normal human oral keratinocytes (HOKs) were challenged with arecoline, the major alkaloid of areca nut, by Western blot for HSP27. Furthermore, epigallocatechin‐3 gallate (EGCG), glutathione precursor N‐acetyl‐l ‐cysteine (NAC), cyclooxygenase‐2 inhibitor NS‐398, HSP inhibitor quercetin, extracellular signal‐regulated protein kinase (ERK) inhibitor PD98059, and p38 inhibitor SB203580 were added to find the possible regulatory mechanisms. Results: Heat shock protein 27 exhibited higher expression in OSCCs than normal specimens (P < 0.05). Arecoline was found to elevate HSP27 expression in a dose‐ and time‐dependent manner (P < 0.05). The additions of pharmacological agents were found to inhibit arecoline‐induced HSP27 expression (P < 0.05). Conclusions: Heat shock protein 27 expression is significantly elevated in areca quid chewing‐associated OSCCs. Arecoline‐induced HSP27 expression was downregulated by EGCG, NS398, NAC, quercetin, PD98059, and SB203580.