阿胶强骨口服液联合骨化三醇治疗老年骨质疏松的临床研究

目的 探讨阿胶强骨口服液联合骨化三醇胶丸治疗老年骨质疏松的临床疗效。方法 选取2019年3月—2021年3月在安康市人民医院就诊治疗的128例老年骨质疏松患者,根据随机数字法将128例老年骨质疏松患者分为对照组（n=64）和治疗组（n=64）。对照组口服骨化三醇胶丸,1粒/次,2次/d。治疗组在对照组的基础上口服阿胶强骨口服液,10 mL/次,3次/d。两组患者均连续服用药物3个月。观察两组的临床疗效,比较两组临床症状好转时间、骨代谢指标和骨密度的变化。结果 治疗后,治疗组患者总有效率是98.44%,显著高于对照组的84.38%（P<0.05）。治疗组患者腰酸背痛好转时间、骨骼疼痛好转时间、下肢无力好转时间、肌肉痉挛好转时间均显著短于对照组（P<0.05）。治疗后,两组Ⅰ型胶原羧基端交联肽（CTX）、血清Ⅰ型胶原氨基端前肽（P1NP）均显著降低,但25-羟基维生素D[25（OH） D]、骨钙素（BGP）升高（P<0.05）;治疗后,治疗组骨代谢指标改善优于对照组（P<0.05）。治疗后,两组患者股骨颈骨骨密度、腰椎骨骨密度、股骨大转子骨密度均较治疗前显著升高（P<0.05）;治疗后,治疗组骨密度改善优于对照组（P<0.05）。结论 阿胶强骨口服液联合骨化三醇胶丸治疗老年骨质疏松临床疗效显著,能有效改善骨密度,增强骨代谢功能,值得临床推广应用。     

骨松宝颗粒联合硫酸氨基葡萄糖治疗膝骨关节炎的临床研究

目的 探讨骨松宝颗粒联合硫酸氨基葡萄糖治疗膝骨关节炎的临床疗效。方法 纳入2019年10月—2020年2月于南阳市第二人民医院骨科门诊及住院治疗的86例膝骨关节炎患者作为研究对象,按照随机数表法将患者分为对照组和观察组,每组各43例。对照组患者口服硫酸氨基葡萄糖胶囊,2粒/次,3次/d。观察组在对照组治疗的基础上口服骨松宝颗粒,1袋/次,3次/d。两组各治疗6周。观察两组患者的临床疗效,同时比较两组治疗前后的视觉模拟评分（VAS）、Lysholm评分、血清炎症因子及骨代谢指标水平。结果 治疗后,观察组总有效率为95.34%,显著高于对照组的79.07%,差异具有统计学意义（P<0.05）。治疗后,两组VAS评分显著降低,而Lysholm评分显著升高,同组治疗前后比较差异具有统计学意义（P<0.05）;治疗后,观察组VAS评分显著低于对照组,而Lysholm评分高于对照组,差异均具有统计学意义（P<0.05）。治疗后,两组肿瘤坏死因子-α（TNF-α）、白细胞介素-1β（IL-1β）、白细胞介素-6（IL-6）水平较显著降低（P<0.05）,且治疗后,观察组TNF-α、IL-1β、IL-6水平显著低于对照组,差异均具有统计学意义（P<0.05）。治疗后,两组抗酒石酸盐酸性磷酸酶异构体5b（TRACP-5b）水平显著降低,而骨钙素（BGP）和骨特异性碱性磷酸酶（BALP）水平显著升高,同组治疗前后比较差异具有统计学意义（P<0.05）;治疗后,观察组TRACP-5b水平显著低于对照组,而BGP和BALP水平显著高于对照组,两组比较差异具有统计学意义（P<0.05）。结论 骨松宝颗粒联合硫酸氨基葡萄糖治疗膝骨关节炎的临床疗效较好且安全性高,能明显改善膝关节疼痛症状及关节功能,可能机制与其能显著降低机体炎症因子水平及改善骨代谢有关。     

芪骨胶囊联合重组特立帕肽治疗骨质疏松症的临床研究

目的 观察芪骨胶囊联合注射用重组特立帕肽治疗骨质疏松症的临床疗效。方法 选取2020年1月—2021年3月南阳医学高等专科学校第一附属医院收治的111例骨质疏松症患者，根据治疗方案的不同将所有患者分为对照组（54例）和治疗组（57例）。对照组患者大腿或腹部皮下注射注射用重组特立帕肽，20μg/次，1次/d。治疗组患者在对照组的基础上口服芪骨胶囊，3粒/次，3次/d。28d为1个疗程，共治疗6个疗程。观察两组的临床疗效，比较两组的不同部位骨密度、骨吸收和骨形成指标。结果 治疗后，治疗组的总有效率为94.74%，高于对照组患者的总有效率77.78%，组间比较差异显著（P<0.05）。治疗后，两组腰椎L_2～4、股骨颈、桡骨远端1/3处的骨密度均较治疗前升高（P<0.05），且治疗后治疗组的腰椎L_2～4、股骨颈、桡骨远端1/3处的骨密度高于对照组（P<0.05）。治疗后，两组血清Ⅰ型原胶原C-端前肽（PICP）、骨特异性碱性磷酸酶（BALP）、骨钙素（BGP）水平均较治疗前升高（P<0.05），且治疗后，治疗组的血清PICP、BALP、BGP水平高于对照组（P<0.05）。治疗后，两组血清抗酒石酸酸性磷酸酶（TRACP）、Ⅰ型胶原C-末端肽交联（S-CTX）水平均较治疗前下降（P<0.05），且治疗后治疗组的血清TRACP、S-CTX水平低于对照组（P<0.05）。结论 芪骨胶囊联合注射用重组特立帕肽治疗骨质疏松症具有较好的临床疗效，可有效改善机体骨密度，调节血清PICP、BALP、BGP、TRACP、S-CTX水平。     

唑来膦酸联合阿法骨化醇治疗骨质疏松症的效果及其对骨转换、骨代谢功能的影响

目的 研究唑来膦酸联合阿法骨化醇治疗骨质疏松症的效果及其对骨转换、骨代谢功能的影响。方法 选择2015年1月—2017年12月在濮阳市中原油田濮东医院进行诊治的95例骨质疏松症患者,随机分为两组。对照组口服阿法骨化醇治疗,0.5 μg/次,1次/d。观察组联合静脉滴注唑来膦酸,5 mL唑来膦酸溶于100 mL生理盐水中以恒定的速度进行静脉滴注。两组均治疗12个月。比较两组的临床治疗效果,检测两组骨转换指标、骨代谢指标,并统计两组不良反应情况。结果 观察组的有效率为91.48%,显著高于对照组的72.92%（P<0.05）。两组治疗后的Ⅰ型胶原交联C-末端肽（CTX-1）均显著降低（P<0.05）,骨钙素（OC）显著升高（P<0.05）,且观察组较对照组变化更为显著（P<0.05）。两组治疗后的血清碱性磷酸酶、甲状旁腺素以及骨特异碱性磷酸酶等骨代谢指标均显著降低（P<0.05）,且观察组较对照组降低地更为显著（P<0.05）。观察组的不良反应发生率为6.38%,与对照组的4.17%相比无明显差异（P<0.05）。结论 唑来膦酸联合阿法骨化醇治疗骨质疏松症的效果明显优于单独使用阿法骨化醇,可以有效改善患者的骨转换和骨代谢状态,具有较高的临床参考价值。     

骨疏康颗粒联合雷洛昔芬治疗绝经后骨质疏松症的临床研究

目的 探讨骨疏康颗粒联合盐酸雷洛昔芬片治疗绝经后骨质疏松症的临床疗效。方法 选取2021年1月—2022年12月在漯河市郾城区中医院就诊的120例骨质疏松症患者,按照随机数字表法将120例患者分为对照组和治疗组,每组各60例。对照组患者口服盐酸雷洛昔芬片,1片/次,1次/d。治疗组患者在对照组治疗的基础上餐后温水冲服骨疏康颗粒,1袋/次,3次/d。两组患者连续治疗3个月。观察两组的临床疗效,比较两组自觉疼痛程度、股骨近端、桡尺骨的骨密度和血清骨钙素（BGP）、Ⅰ型胶原C末端肽（CTX-1）、Ⅰ型前胶原氨基末端肽（PINP）、转化生长因子-β₁（TGF-β₁）、白细胞介素-6（IL-6）、胰岛素样生长因子1（IGF-1）水平。结果 治疗后,治疗组患者的总有效率95.00%比对照组的83.33%更高（P＜0.05）。治疗后,两组数字疼痛强度量表（NRS）评分明显降低（P＜0.05）,且治疗组患者NRS评分较对照组更低（P＜0.05）。治疗后,治疗组股骨近端、桡尺骨的骨密度明显高于治疗前（P＜0.05）,且治疗组股骨近端、桡尺骨的骨密度明显高于对照组（P＜0.05）。治疗后,两组的血清BGP、CTX-1水平低于治疗前,血清PINP水平高于治疗前（P＜0.05）;治疗组的血清BGP、CTX-1水平低于对照组,血清PINP水平高于对照组（P＜0.05）。治疗后,两组的血清TGF-β₁、IL-6水平低于治疗前,血清IGF-1水平高于治疗前（P＜0.05）;治疗后,治疗组的血清TGF-β₁、IL-6水平低于对照组,血清IGF-1水平高于对照组,差异有统计学意义（P＜0.05）。结论 骨疏康颗粒联合盐酸雷洛昔芬片可提高骨质疏松症的疗效,有助于降低患者疼痛程度,提高骨密度,改善骨代谢水平,且安全性良好。     

骨康胶囊联合氨基葡萄糖治疗胫骨平台骨折的临床研究

目的 探讨骨康胶囊联合氨基葡萄糖胶囊治疗胫骨平台骨折的临床疗效。方法 选取2019年2月—2021年1月在广西北海市第二人民医院就诊的80例胫骨平台骨折患者作为研究对象,按照治疗方法将80例患者分为对照组和观察组,各包括40例。对照组口服氨基葡萄糖胶囊,0.75 g/次,2次/d。观察组在对照组的基础上口服骨康胶囊,1.6 g/次,3次/d。两组连续治疗6个月。观察两组的临床疗效、骨折愈合时间和完全负重时间,同时比较两组治疗前后的血清中β-胶原降解产物（β-CTX）、骨钙素（BGP）、骨特异性碱性磷酸酶（BALP）的水平,以及视觉模拟评分法（VAS）、Lysholm功能量表评分情况。结果 治疗后,观察组的总有效率为92.50%,对照组为75.00%,组间比较有明显差异（P<0.05）。治疗后,两组β-CTX、BGP、BALP水平均显著升高（P<0.05）;治疗后,观察组的β-CTX、BGP、BALP水平显著高于对照组,差异有统计学意义（P<0.05）。治疗后,两组VAS评分显著降低,Lysholm评分明显升高（P<0.05）;且治疗后,观察组VAS评分显著低于对照组,Lysholm评分高于对照组（P<0.05）。治疗后,观察组的骨折愈合时间、完全负重时间均短于对照组,差异有统计学意义（P<0.05）。结论 骨康胶囊联合氨基葡萄糖胶囊可促进胫骨平台骨折术后的骨折愈合,改善膝关节功能,减轻疼痛程度,可能与调节骨代谢指标有关,具有良好临床意义。     

恒古骨伤愈合剂联合注射用骨肽治疗胫骨平台骨折的临床研究

目的 分析恒古骨伤愈合剂联合注射用骨肽治疗胫骨平台骨折的临床研究。方法 选取2019年6月—2022年6月郑州市第七人民医院治疗的143例胫骨平台骨折患者,按照随机数字表法将患者分为对照组（72例）和治疗组（71例）。对照组患者在手术后静脉滴注注射用骨肽,100 mg注射用骨肽加入0.9%氯化钠注射液250 mL中,1次/d。治疗组在对照组的治疗基础上口服恒古骨伤愈合剂,25 mL/次,隔日用药一次。两组治疗时间为1个月。观察两组的临床疗效,比较临床症状改善时间、血清创伤指标和骨代谢指标。结果 治疗后,治疗组患者膝关节恢复优良率是90.14%,显著高于对照组的76.39%（P＜0.05）。治疗后,治疗组患者疼痛消失时间、下床活动时间、骨折愈合时间均显著短于对照组（P＜0.05）。治疗后,两组患者白细胞介素-10（IL-10）、白细胞介素-1（IL-1）和C反应蛋白（CRP）均较治疗前增加（P＜0.05）,且治疗后治疗组IL-10、IL-1和CRP明显低于对照组（P＜0.05）。治疗后,两组骨保护素（OPG）、骨形态发生蛋白2（BMP-2）水平均较治疗前显著升高,而Ⅰ型胶原羧基末端肽（CTX-Ⅰ）水平均显著下降（P＜0.05）;治疗后,治疗组患者骨代谢指标改善优于对照组（P＜0.05）。水平。结论 恒古骨伤愈合剂联合注射用骨肽治疗胫骨平台骨折具有较好的临床疗效,有助于更快改善临床症状,减轻炎症反应,改善骨代谢水平,促进膝关节功能恢复。     

骨松宝颗粒联合骨化三醇治疗老年骨质疏松性股骨粗隆间骨折的临床研究

目的 探讨骨松宝颗粒联合骨化三醇胶丸治疗老年骨质疏松性股骨粗隆间骨折的临床疗效。方法 选取2018年7月-2019年12月新乡医学院第一附属医院收治的82例老年骨质疏松性股骨粗隆间骨折患者，按照随机数字表法将82例患者分为对照组和治疗组，每组各41例。对照组口服骨化三醇胶丸，0.25μg/次，3次/d。治疗组患者在对照组治疗的基础上温水冲服骨松宝颗粒，5 g/次，2次/d。两组患者连续治疗6个月。观察两组的临床疗效，比较两组的视觉模拟评分法（VAS）评分、髋关节功能（Harris）评分、骨密度和血清抗酒石酸酸性磷酸酶5b（TRACP-5b）、胰岛素样生长因子Ⅰ（IGF-Ⅰ）、骨钙素（OC）水平。结果 治疗后，治疗组患者的总有效率比对照组高（95.12%vs 80.49%），差异有统计学意义（P<0.05）。治疗后，两组的VAS评分显著降低，Harris评分显著升高（P<0.05）；且治疗组的VAS评分低于对照组，Harris评分高于对照组（P<0.05）。治疗后，两组的腰椎骨密度明显升高（P<0.05），且治疗组升高的更明显（P<0.05）。治疗后，两组的TRACP-5b水平显著降低，IGF-Ⅰ、OC水平显著升高，差异有统计学意义（P<0.05）；且治疗后治疗组的TRACP-5b水平比对照组低，IGF-Ⅰ、OC水平比对照组高，差异有统计学意义（P<0.05）。结论 骨松宝颗粒联合骨化三醇胶丸治疗老年骨质疏松性股骨粗隆间骨折具有较好的临床疗效，可减轻疼痛程度，改善骨密度，调节血清骨代谢指标。     

仙灵骨葆胶囊联合阿仑膦酸钠对骨质疏松症患者的骨代谢及骨转换指标的影响

目的 探讨仙灵骨葆胶囊联合阿仑膦酸钠对骨质疏松症患者骨代谢及骨转换指标的影响。方法 选取2015年9月—2018年9月西宁市第一人民医院92例骨质疏松症患者作为研究对象,按照随机数字法将患者分为对照组和观察组,每组各46例。对照组患者口服阿仑膦酸钠片,10 mg/次,1次/d。观察组在对照组的基础上口服仙灵骨葆胶囊,2粒/次,3次/d,两组均持续治疗3个月。观察两组患者的临床疗效,同时比较两组治疗前后的骨代谢、骨转换指标及腰椎L_2-4和股骨颈骨密度。结果 治疗后,观察组总有效率为93.48%,对照组总有效率为78.26%,两组总有效率比较差异具有统计学意义（P<0.05）。治疗后,两组患者骨源性碱性磷酸酶（BAP）、骨钙素（BGP）和碱性磷酸酶（ALP）水平均显著升高,24 h尿钙（U-Ca）水平显著降低（P<0.05）,且观察组骨代谢各指标水平显著优于对照组（P<0.05）。治疗后,两组患者的核因子κB受体活化因子配基（RANKL）及Ⅰ型胶原交联C-末端肽（CTX-1）水平均显著降低,骨保护素（OPG）水平显著升高（P<0.05）,且观察组各骨转换指标水平显著优于对照组（P<0.05）。两组治疗后腰椎L_2-4和股骨颈骨密度均显著增加（P<0.05）,且观察组腰椎L_2-4和股骨颈骨密度显著高于对照组（P<0.05）。结论 仙灵骨葆胶囊联合阿仑膦酸钠可有效改善患者的骨代谢、骨转换指标及骨密度水平,疗效确切,在骨质疏松症患者治疗中具有较高的应用价值。     

金骨莲胶囊联合右旋酮洛芬氨丁三醇治疗风湿痹阻型类风湿关节炎的临床研究

目的 探讨金骨莲胶囊联合右旋酮洛芬氨丁三醇片治疗风湿痹阻型类风湿关节炎的疗效。方法 选取2022年1月—2022年12月山西医科大学附属运城市中心医院收治的类风湿关节炎患者100例,根据治疗方案不同将患者分为对照组（50例）和治疗组（50例）。对照组患者口服右旋酮洛芬氨丁三醇片,12.5 mg/次,3次/d。治疗组在对照组基础上口服金骨莲胶囊,5粒/次,3次/d。两组患者均持续治疗4周。观察两组患者临床疗效,比较治疗前后两组患者中医证候积分、肿胀关节数、压痛关节数,及红细胞沉降率（ESR）、肿瘤坏死因子-α（TNF-α）和白细胞介素-6（IL-6）水平。结果 治疗后,治疗组总有效率显著优于对照组（98.00% vs 86.00%,P＜0.05）。治疗后,两组患者中医证候积分、肿胀关节数、压痛关节数及ESR、TNF-α、IL-6水平比治疗前显著降低（P＜0.05）,且治疗组明显低于对照组（P＜0.05）。结论 金骨莲胶囊联合右旋酮洛芬氨丁三醇片治疗风湿痹阻型类风湿关节炎疗效及安全性均较高,能有效降低患者炎性水平,减轻关节疼痛及改善中医证候。     

Synthesis and evaluation of 2,6-piperidinedione derivatives as potentially novel compounds with analgesic and other CNS activities

New 2,6-piperidinediones 2_a–g and 4_a–d were prepared by initial condensation of aromatic aldehydes or cycloalkanones with cyanoacetamide to give α-cyanocinnamides l_a–g or cycloalkylidenes 3_a,b which underwent Michae1 addition with ethyl cyanoacetate or diethylmalonate. Compounds 4_a–d were alkylated by various alkyl halides to produce the N-alkylated 2,6-piperidinedione derivatives 5_a–m. Some new selected compounds 2_a–c,f, 4_a–d & 5_e,h,j were pharmacologically evaluated for potential anticonvulsant, sedative and analgesic activities. These compounds exhibited significant anticonvulsant and analgesic effects after a single I.P. administration 100 mg/kg b.wt. . On the other hand all the investigated compounds induced hypnotic activity and prolonged the phenobarbital sodium- induced sleep as compared with the control group and the most potent compound was found to be 2_f.     

EFFECT OF POLICOSANOL SUCCESSIVE DOSE INCREASES ON PLATELET AGGREGATION IN HEALTHY VOLUNTEERS

Policosanol is a cholesterol-lowering drug with hypocholesterolemic effects demonstrated in experimental models, healthy volunteers and type II hypercholesterolemic patients. In addition, antiplatelet effects of policosanol have been shown in experimental models and healthy volunteers. The effect of successively increasing doses of policosanol on platelet aggregation was investigated in a randomized, placebo-controlled, double-blind study conducted in 37 healthy volunteers. The volunteers were on a placebo-baseline period (two tablets per day) for 7 days and thereafter they received randomly, under double-blind conditions, placebo or policosanol (10mgday⁻¹) for 7 days. After this period dosage was doubled to 20mgday⁻¹for the next 7 days and then again doubled to 40mgday⁻¹, while the control group received placebo tablets all the time. Platelet aggregation as well as coagulation time was measured at baseline and after each dosing step. Results showed that antiplatelet effects of policosanol were successfully enhanced throughout the study, thus suggesting a dose-dependent relationship. No significant effect was reached during the first dosing period, but significant reductions of epinephrine and ADP-induced platelet aggregation were observed after the second one. Finally, a significant inhibition of platelet aggregation induced by all the agonists was observed at the last dosing step. Coagulation time remained unchanged during the trial.     

鼻渊净胶囊的HPLC指纹图谱研究

目的 建立鼻渊净胶囊的高效液相色谱（HPLC）指纹图谱。方法 采用Agilent SB-C₁₈（4.6 mm×250 mm,5 μm）色谱柱,乙腈-水为流动相、以1.0 ml/min流速行梯度洗脱,检测波长210 nm,柱温30 ℃,洗脱时间为80 min。采用中药色谱指纹图谱相似度评价系统（2004A版）对检测出色谱进行指纹图谱相似度评价。结果 建立了鼻渊净胶囊的HPLC指纹图谱,确定了20个共有峰,15个峰归属到各药材,其中5个峰确认了化学成分;10批样品的指纹图谱的整体相似度与对照图谱比较,均在90%以上。结论 所建立的鼻渊净胶囊指纹图谱有助于从整体上控制该制剂的质量。     

NEURAMIDE STIMULATES ADRENOCORTICOTROPIN BUT NOT PROLACTIN RELEASE FROM RAT PITUITARY

Neuramide (NMD), a substance found in crude preparations of porcine stomach extract, is a viral inhibitor that also has putative immunostimulatory effects. The effects of NMD on stress-hormone (ACTH and prolactin—PRL) release were assessed inin vivoandin vitrostudies. In the former, blood levels of corticosterone and PRL were measured in NMD-treated male rats.In vitroexperiments were performed to evaluate the effects of NMD and three of its fractions (obtained with high performance liquid chromatography) on ACTH and PRL release from perfused rat pituitary slices. NMD increased plasma corticosterone levelsin vivoand produced dose-dependent increases inin vitropituitary release of ACTH. No effects on PRL secretion were observedin vivoorin vitro. The stimulatory effects on ACTH release were caused by the NMD fraction with a molecular weight of >5000<10000Da.     

Investigation of the prevalence of tetQ, tetX and tetX1 genes in Bacteroides strains with elevated tigecycline minimum inhibitory concentrations

In this study, the antibiotic susceptibilities to tigecycline and tetracycline of 35 selected Bacteroides fragilis group strains were determined by Etest, and the presence of tetQ, tetX, tetX1 and ermF genes was investigated by polymerase chain reaction (PCR). tetQ was detected in all 12 B. fragilis group isolates (100%) exhibiting elevated tigecycline minimum inhibitory concentrations (MICs) (≥8 μg/mL) as well as the 8 strains (100%) with a tigecycline MIC of 4 μg/mL, whilst tetX and tetX1 were present in 15% and 75% of these strains, respectively. All of these strains were fully resistant to tetracycline (MIC ≥ 16 μg/mL). On the other hand, amongst the group of strains with tigecycline MICs < 4 μg/mL (15 isolates), tetQ, tetX and tetX1 were found less frequently (73.3%, 13.3% and 46.7%, respectively). All but two strains harbouring the tetQ gene in this group were non-susceptible to tetracycline, with a MIC > 4 μg/mL. These data suggest that in most cases tigecycline overcomes the tetracycline resistance mechanisms frequently observed in Bacteroides strains. However, the presence of tetX and tetX1 genes in some of the strains exhibiting elevated MICs for tigecycline draws attention to the possible development and spread of resistance to this antibiotic agent amongst Bacteroides strains. The common occurrence of ermF, tetX, tetX1 and tetQ genes together predicted the presence of the CTnDOT-like Bacteroides conjugative transposon in this collection of Bacteroides strains.     

INDIRECT PARASYMPATHOMIMETIC ACTIVITY OF THE CLASS III ANTIARRHYTHMIC SUBSTANCE / -SOTALOLIN VITRO: REVERSIBLE INHIBITION OF CHOLINESTERASE ISOENZYMES FROM BLOOD AND THE HUMAN CENTRAL NERVOUS SYSTEM

Inhibitory effects of the class III antiarrhythmic compound / -sotalol on acetylcholinesterase (AChE; EC 3.1.1.7) isoenzymes of both erythrocytes and the human caudate nucleus and on serum cholinesterase (ChE; EC 3.1.1.8) were studiedin vitrousing a spectrophotometric kinetic assay with acetylthiocholine (ASCh) as substrate. Sotalol concentrations in the assays varied from 0.32 to 3.2m . All isoenzymes studied were inhibited by / -sotalol in a reversible and concentration-dependent manner. Double reciprocal plots of the reaction velocity against varying ASCh concentrations revealed that / -sotalol reduced substrate affinity (apparent Michaelis constant, KM, increased) of serum ChE, but did not change the enzyme's maximal rate of ASCh hydrolysis (V_max). Thus, / -sotalol inhibition of serum ChE was of the competitive type (rate constant for reversible competitive inhibition: K_i=0.51m ). In contrast, / sotalol reduced the maximal reaction velocity of the AChE isoenzyme from the central nervous system (caudate nucleus), but had no influence on substrate affinity of the enzyme (K_Mwith ASCh unchanged) indicating purely non-competitive inhibition kinetics (rate constant of reversible non-competitive inhibition: K_i′=0.44m ). / -sotalol inhibition of erythrocyte AChE was of mixed competitive/non-competitive type (K_i=0.31m , K_i′=0.49m ). Non-competitive / -sotalol inhibition of caudate nucleus AChE and the non-competitive component of erythrocyte AChE inhibition cannot be overcome by increased concentrations of the cholinergic transmitter acetylcholine (ACh). Peak / -sotalol plasma levels as described in the literature for both humans (15μ ) and experimental animals (dogs: 18μ ; rats: 260μ ) as well as maximal myocardial concentrations of the substance (dogs: 46μ ; rats: 478μ ) are in the range of about 2% to 100% of the sotalol inhibition rate constants determined in the present paper for cholinesterase isoenzymesin vitro. Thus, / -sotalol inhibition of ACh hydrolysisin vivomay contribute to both the well known antiarrhythmic potential and proarrhythmic side effects of the compound.     

AMELIORIATION OF CHEMICALLY-INDUCED HEPATOCYTE INJURY BY CYCLOSPORINE A

Cyclosporine A, beside its current applications, possesses potential hepatoprotective effects. This study was directed to investigate the effect of Cyclosporine A pretreatment on hepatic injury due to carbon tetrachloride (CCl₄) and -galactosamine. Rats were injected by two successive doses of Cyclosporine A (5mgkg⁻¹day⁻¹). Six hours after the second dose, 1mlkg⁻¹of CCl₄was administered i.p. Effects associated with Cyclosporine A pretreatment were examined by using isolated hepatocytes and hepatocytes that were immobilized and continuously perfused. -Galactosamine (5m ) was added directly to the perfusion medium. After isolation, hepatocytes were examined histologically by light and electron microscopy, immobilized and perfused for further metabolic functional activity evaluation. Cyclosporine A pretreatmentin vivoproduced hepatoameliorative effects of various degrees which were statistically significant as manifested by: (1) an increased trypan blue exclusion after CCl₄; (2) an improved ureagenesis after CCl₄; (3) a reduction in the lipid droplets accumulation in the cytoplasm produced by CCl₄administration; (4) well preserved cytoplasmic organelles as mitochondria, endoplasmic reticulum ER, nuclear chromatin structures that were altered by CCl₄; and (5) an increased hepatocytes survival in the agarose gel matrix, reduction of LD leakage and improvement of ureagenesis after -galactosamine addition to the perfusion medium. The beneficial effect of Cyclosporine A pretreatment in modifying hepatotoxicity of chemical insults merits further studies.     

栝楼不同药用部位质量控制的研究进展

瓜蒌子、瓜蒌皮、瓜蒌、天花粉来源于栝楼的不同药用部位,4味药材均为常用的大宗药材,现行版《中国药典》对其制定的质量标准过于简单,无法科学合理地控制其质量。本文对瓜蒌子、瓜蒌皮、瓜蒌、天花粉安全性和有效组分的研究进行综述,明确了相关研究存在的问题并针对问题提出建议,为科学全面的药材及饮片标准的制定提供参考依据。     

喙果黑面神化学成分研究

目的研究大戟科植物喙果黑面神(Breynia rostrata Merr.)的化学成分。方法利用硅胶、凝胶等色谱技术分离纯化化学成分,根据化合物的理化性质和光谱数据进行结构鉴定。结果从喙果黑面神的正丁醇萃取部分分离得到4个化合物,分别鉴定为6-O-甲基丙酰基-α-D-吡喃葡糖(6-O-methylpropanoyl-α-D-glucopyranose,1);4″-苯酚基-6-O-甲基丙酰基-β-D-吡喃葡糖苷(4″-phenolic-6-O-methylpropanoyl-β-D-glucopyranoside,2);1-O-没食子酰基-β-D-吡喃葡糖苷(1-O-galloyl-β-D-glucopyranoside,3);熊果苷(arbutin,4)。结论化合物1和2为新化合物,3和4均为首次从该种植物分离得到。     

EFFECTS OF 2-GUANIDINE-4-METHYLQUINAZOLINE ON GASTRIC ACID SECRETION IN RATS

In this study 2-guanidine-4-methylquinazoline (2-GMQ) appeared to decrease basal and stimulated gastric acid secretion, while structurally related compounds as dimethyl- biguanide, cyanoguanidine and 2-cyanoamino-4-methylpyrymidine did not. Thus, there is an antisecretory effect when the biguanide group is associated with a lipophilic structure. The antisecretive effects exerted by 2-GMQ are associated with anti H₂-histamine activity.The anti H₂-histamine nature of the effects of 2-GMQ was confirmed by the capacity of this compound of depressing the chronotropic activity of the isolated guinea pig auricle increased by histamine, as well as relaxant activity in rat uterus contracted by histamine, since both preparations are rich in H₂-histamine receptors.