单剂量和多剂量巴洛沙星片在健康人体内的药动学特征

目的研究巴洛沙星片在10名健康志愿者体内的药动学特征。方法5名男性、5名女性健康志愿者单剂量和多剂量口服巴洛沙星片100 mg,采用Waters OASISTMHLB固相萃取小柱提取样品,反相高效液相色谱法测定血药浓度。结果主要药动学参数:单剂量为女t1/2(7．26±2．02)h、ρmax(1 229．93±419．98)μg·L-1、AUC0→48(10 031．56±2 856．78)μg·h·L-1;男t1/2(10．21±1．93)h、ρmax(989．37±219．62)μg·L-1、AUC0→48(9 783．05±879．95)μg·h·L-1。多剂量为女t1/2(8．53±1．84)h,ρav (690．28±150．0)μg·L-1,AUCss(8 283．30±1 800．08)μg·h·L-1,DF(1．68±0．68);男t1/2(8．72±1．23)h、ρav(784．74±82．62)μg·L-1、AUCss(9 416．93±991．41)μg·h·L-1、DF(1．19±0．15)。结论用DAS 2．0软件进行房室模型拟合,巴洛沙星体内过程符合一级消除二室模型,每次100mg,bid连续5 d,可达到稳定有效血药浓度。     

丹红注射液联合瑞舒伐他汀对冠心病合并高脂血症患者MFG-E8、Klotho蛋白表达及血脂水平的影响

目的 探究丹红注射液联合瑞舒伐他汀对老年冠心病合并高脂血症患者血清乳脂肪球表皮生长因子-8(MFG-E8)、Klotho蛋白表达及血脂水平的影响.方法 选取冠心病合并高脂血症老年患者86例,根据就诊顺序编号,以随机数字表法分为观察组与对照组,各43例.对照组予以瑞舒伐他汀治疗,观察组予以瑞舒伐他汀+丹红注射液治疗,两组均连续治疗4周.观察统计两组治疗效果、不良反应情况,并比较治疗前后两组血清MFG-E8、Klotho蛋白表达、炎性因子[超敏C反应蛋白(Hs-CRP)、肿瘤坏死因子-α(TNF-α)、白细胞介素-6(IL-6)]及血脂[低密度脂蛋白胆固醇(LDL-C)、三酰甘油(TG)、总胆固醇(TC)、高密度脂蛋白胆固醇(HDL-C)]水平.结果 (1)两组治疗后血脂相关指标水平均较治疗前改善,且观察组LDL-C(3.25±0.70)mmol·L-1、TG(1.70±0.99)mmol·L-1、TC(4.85±0.98)mmol·L-1均低于对照组(3.89±0.92)mmol·L-1、(2.45±1.05)mmol·L-1、(5.56±1.19)mmol·L-1,差异有统计学意义(P<0.05);(2)两组治疗后炎性因子水平均较治疗前改善,且观察组Hs-CRP(4.12±0.94)mg·L-1、TNF-α(0.39±0.25)μg·L-1、IL-6(9.15±2.48)ng·L-1均低于对照组(8.52±2.31)mg·L-1、(0.68±0.34)μg·L-1、(14.32±2.95)ng·L-1,差异有统计学意义(P<0.05);(3)两组治疗后Klotho、MFG-E8蛋白表达水平均较治疗前升高,且观察组Klotho蛋白表达水平(43.25±1.74)ng·L-1、MFG-E8蛋白表达水平(512.38±19.58)mg·L-1均高于对照组(34.85±1.87)ng·L-1、(325.47±12.94)mg·L-1,差异有统计学意义(P<.05);(4)观察组治疗总有效率95.35％(41/43)高于对照组74.42％(32/43),差异有统计学意义(P<0.05);观察组不良反应率20.93％(9/43)与对照组16.28％(7/43)相比,差异无统计学意义(P>0.05).结论 对冠心病合并高脂血症老年患者予以瑞舒伐他汀联合丹红注射液治疗,可有效降低血清Klotho、MFG-E8蛋白表达、血清炎性因子及调节血脂水平,疗效较为显著,且安全性较高.     

复方缓释胶囊中氯苯那敏的人体药物代谢动力学及生物等效性研究

目的研究美敏伪麻缓释胶囊和盐酸伪麻黄碱缓释胶囊中氯苯那敏在健康人体内的药物代谢动力学过程和生物等效性。方法本试验采用双周期自身随机交叉试验设计。21名受试者分为2组,先后口服2种复方缓释胶囊,2次用药间隔14 d,采用HPLC-MS/MS测定。结果试验药物和参比药物中氯苯那敏的Cmax为(5.05±1.39)ng·m L-1和(5.41±1.45)ng·m L-1;tmax为(4.50±1.89)h和(4.25±1.55)h;AUC0~t为(136.50±47.52)h·ng·m L-1和(145.40±46.28)h·ng·m L-1;AUC0~inf为(160.85±63.80)h·ng·m L-1和(168.72±56.26)h·ng·m L-1;t1/2为(23.26±6.91)h和(22.68±6.41)h;相对生物利用度F0~t和F0~inf分别为(93.2±19.0)%和(93.5±18.4)%。Cmax、AUC0~t、AUC0~inf比值的90%可信区间分别为87.07%~99.28%、85.95%~101.04%和86.64%~101.18%。结论美敏伪麻缓释胶囊和盐酸伪麻黄碱缓释胶囊中的氯苯那敏在中国健康男性受试者体内具有生物等效性。     

脂必泰胶囊与阿托伐他汀钙对老年血脂异常患者血脂和炎症因子的影响

目的：观察脂必泰胶囊与阿托伐他汀钙对老年血脂异常患者血脂和炎症因子的影响。方法选择老年血脂异常患者64例,随机分为对照组和治疗组,每组32例。对照组患者睡前口服阿托伐他汀钙片10 mg·d-1,治疗组患者在对照组基础上加服脂必泰胶囊(每次240 mg,bid)。均治疗6周。分别于治疗前后检测两组患者血清总胆固醇( TC)、三酰甘油( TG)、低密度脂蛋白胆固醇( LDL-C)、高密度脂蛋白胆固醇( HDL-C)、肿瘤坏死因子-α( TNF-α)和白细胞介素-6(IL-6)水平。结果与对照组治疗后比较,治疗组患者血清TC[(5.18±0.57) mmol·L-1比(5.73±0.65)mmol·L-1]、TG[(1.52±0.43) mmol·L-1比(1.86±0.48)mmol·L-1]、LDL-C[(3.36±0.48) mmol·L-1比(3.85±0.53)mmol·L-1]、TNF-α[(5.37±2.21) ng·L-1比(7.63±2.59)ng·L-1]和IL-6[(12.27±2.75) ng·L-1比(15.63±2.92)ng·L-1]水平均显著降低(均P<0.01),HDL-C[(1.26±0.25) mmol·L-1比(1.13±0.23)mmol·L-1]水平显著升高(P<0.05)。结论脂必泰胶囊联合阿托伐他汀钙治疗老年血脂异常,不仅有调脂作用,还具有降低患者血清TNF-α和IL-6水平、抑制炎症反应作用。     

芍药苷对胶原诱导型关节炎大鼠下丘脑-垂体-肾上腺轴的影响

目的探讨芍药苷治疗胶原诱导型关节炎(CIA)是否与调节下丘脑-垂体-肾上腺(HPA)轴有关。方法 Wistar大鼠右足趾皮内注射牛Ⅱ型胶原(CⅡ)和弗氏完全佐剂制备CIA大鼠模型,7 d后大鼠背部和尾根部皮下注射CⅡ加强免疫1次。初次免疫后第14天ig给予地塞米松2 mg.kg-1或芍药苷25,50和100 mg.kg-1,每天1次,连续28 d。初次免疫后第14,21,28,35和42天观察CIA大鼠的足爪肿胀度和关节炎指数的变化。给药结束后第2天大鼠摘眼球取血,放射免疫法检测血浆促肾上腺皮质激素释放激素(CRH)、促肾上腺皮质激素(ACTH)和皮质酮(CS)含量;制备血清,用ELISA法检测白细胞介素4(IL-4)、干扰素γ(IFN-γ)、IL-1β、肿瘤坏死因子α(TNF-α)和抗CⅡ抗体含量。结果与正常对照组相比,模型对照组大鼠关节红肿,关节炎指数升高(P<0.01),血中CRH、CS、抗CⅡ抗体、IFN-γ、IL-1β和TNF-α水平明显升高(P<0.01),IL-4水平下降(P<0.01),ACTH无明显改变。ig给予芍药苷50和100 mg.kg-1可抑制CIA大鼠关节肿胀,降低关节炎指数(P<0.05),在第42天关节炎指数由模型对照组的6.4±0.7降至5.6±0.5和5.4±0.7(P<0.05);使模型对照组血清IFN-γ由(21.3±2.5)ng.L-1降至16.6±1.3和(16.1±1.9)ng.L-1(P<0.01),IL-1β由(37.3±4.2)ng.L-1降至32.1±2.9和(31.2±4.1)ng.L-1(P<0.01),TNF-α由(53.9±7.9)ng.L-1降至39.4±6.8和(31.3±6.1)ng.L-1(P<0.01),抗CⅡ抗体由(2.13±0.32)ng.L-1降至1.35±0.58和(1.10±0.42)ng.L-1(P<0.01),IL-4由(26.6±3.0)ng.L-1升至41.9±3.1和(49.1±4.2)ng.L-1(P<0.01);能使血浆CRH的水平由模型对照组的(2.3±0.5)μg.L-1升高至4.9±1.0和(5.3±1.1)μg.L-1(P<0.01),CS由(33±10)μg.L-1升高至47±9和(51±13)μg.L-1(P<0.01),ACTH水平亦有明显升高(P<0.01)。结论芍药苷治疗CIA可能与调节PHA轴有关。     

慢性心力衰竭患者6 min步行试验与血清脑利钠肽水平的临床研究

目的 :通过对慢性心力衰竭患者的 6min步行试验 (6MWT)的距离和血清脑利钠肽 (BNP)水平的观察 ,探讨 6MWT和BNP水平对心力衰竭患者心脏功能评估的临床意义。方法 :测量 5 1例慢性心力衰竭患者 (心衰组 )的 6MWT距离和酶联免疫吸附法检测血清BNP 32浓度。并以 30例健康成人为对照组。结果 :心衰组的 6MWT距离 380 .3± 12 1.7m明显低于对照组 5 46 .8± 12 8.5m (P <0 .0 1)。心衰组BNP水平 75 8.3± 2 89.5ng·L-1明显高于对照组10 9.3± 37.6ng·L-1(P <0 .0 1)。NYHA心功能Ⅱ级的 6MWT距离 4 2 5 .0± 10 5 .8m明显低于Ⅲ级335 .6± 12 6 .1m (P <0 .0 1)。NYHAⅡ级的BNP水平 6 38.5± 2 2 4 .5ng·L-1明显高于Ⅲ级 878.0±334.0ng·L-1(P <0 .0 1)。 6MWT距离 <30 0、30 0～374 .9、375～ 4 49.9和 <4 5 0m患者的BNP水平分别为 988.9± 2 0 2 .6、76 8.6± 2 17.4、6 5 7.5± 185 .0和5 0 6 .9± 198.4ng·L-1(P <0 .0 1) ;6MWT的距离与BNP水平呈负相关 (r =- 0 .75 2 ,P <0 .0 1)。结论 :6MWT和BNP水平测定对慢性心力衰竭患者的心脏功能评估具有重要临床意义。     

米格列奈钙片单、多次给药人体药代动力学研究

目的研究米格列奈钙片在健康人体单、多次给药的药代动力学。方法40名健康志愿者,随机平均分为4组（男女各半）,单次给药分别口服米格列奈钙片5、10、20mg,多次给药10mg,q8h×7d。按试验方案采血,高效液相色谱-质谱联用法测定血浆中米格列奈浓度,DAS2．0软件计算药代动力学参数。结果健康受试者单次给药5、10、20mg主要药代动力学参数分别为：tmax（0．27±0．10）、（0．39±0．39）和（0．34±0．16）h;Cmax（697．114-168．83）、（1293．56±293．59）和（1716．43±276．29）μg·h-1·L-1;t1／28（2．44±2．32）、（1．32±0．45）和（2．38±2．22）h;AUC0-1（797．8±149．0）、（1545．1±240．5）和（2474．7±624．6）μg·h-·L-。多剂量给药10mg达稳态后,主要药代动力学参数为tmax（0．27±0．07）;Cmax（1149．99±297．61）μg·h-1·L-1;t1／2β（1．40±0．33）h;AUC0-1（1236．84-327．6）μg·h-1·L-1;Cmin（5．68±2．32）μg·h-1·L-1;AUCss（1236．78±327．64）μg·h-1·L-1;Cav（154．60±40．96）μg·h-1·L-1;Dr（7．45±0．68）;蓄积因子R（O．93±0．30）。结论米格列奈钙片口服给药5—20mg剂量范围内,体内过程呈线性;10mg,q8h连续多次7d,血药浓度d4已达稳态,体内无蓄积;且男女性别间体内过程也未见显著性差别。     

那格列奈对初诊2型糖尿病患者炎性反应状态的影响

目的探讨那格列奈治疗初诊2型糖尿病对患者炎性反应状态的影响。方法回顾性分析采用那格列奈治疗的74例初诊2型糖尿病患者的临床资料,观察患者治疗前、治疗后的空腹血糖（FBG）、餐后0．5h血糖（0．5hPG）、餐后1h血糖（1hPG）、餐后2h血糖（2hPG）、空腹胰岛素（FINS）、餐后0．5h胰岛素（0．5biNS）、餐后1h胰岛素（1bINS）、餐后2h胰岛素（2hlNS）、白细胞介素-2（IL-2）及C反应蛋白（CRP）水平变化情况。结果治疗后,患者的FBG、0．5hPG、1hPG、2hPG、FINS、0．5hlNS、1hlNS、2bINS、IL-2及CRP分别为（8．0±1．5）mmol／L、（12．0±1．8）mmol／L、（10．2±1．3）mmol／L、（10．5±1．2）mmol／L、（168．2±11．5）pmol／L、（213．5±23．5）pmol／L、（197．0±21．5）pmol／L、（189．5±12．0）pmol／L、（14．0±1．5）斗g／／L、（13．5±1．5）mg／L,较治疗前的（10．5±1．0）mmol／L、（14．5±1．5）mmol／L、（12．5±1．4）rnmol／L、（11．6±2．0）mmol／L、（180．7±12．0）pmol／L、（229．8±26．0）pmol／L、（218．5±23．0）pmol／L、（197．0±14．5）pmol／L、（12．5±2．0）彬L、（22．8±2．0）mg／L均明显下降（t=11．9293、9．1785、10．3561、4．1115、6．4696、4．0009、5．8744、3．4279、5．2307、32．0006,均P〈0．05）,治疗过程中无严重不良反应发生。结论那格列奈治疗初诊2型糖尿病能够明显改善患者的炎性反应状态,且治疗过程中无严重不良反应。‘     

尼索地平口腔崩解片和普通片在健康人体的生物等效性

目的研究尼索地平口腔崩解片和普通片在健康志愿者体内的生物等效性。方法 20例男性健康志愿者,随机交叉口服尼索地平口腔崩解片10 mg和普通片10 mg,间隔7 d。用高效液相色谱串联质谱法测定血浆中尼索地平的血药浓度,计算主要药动学参数。结果尼索地平口腔崩解片和普通片中尼索地平的tmax分别为(1.50±0.40)h和(1.43±0.49)h,ρmax分别为(1 252.5±918.6)ng·L-1和(1 240.6±757.7)ng·L-1,t1/2分别为(8.07±2.00)h和(8.77±2.46)h,AUC0-t分别为(5 505.3±3 398.3)ng·h·L-1和(4 781.1±2 102.8)ng·h·L-1,AUC0-∞分别为(6 053.0±3 603.8)ng·h·L-1和(5 413.6±2 388.3)ng·h·L-1。以AUC0-t计算,尼索地平口腔崩解片的相对生物利用度为(113.1±31.3)%。两种片剂的药动学参数均无显著差异(P>0.05)。结论尼索地平口腔崩解片和普通片在健康人体内具有生物等效性。     

前列地尔治疗肝硬化失代偿期合并肝肾综合征的疗效观察

目的　观察前列地尔对肝硬化失代偿期合并肝肾综合征的临床疗效。方法　6 8例患者随机分为两组,都给予常规保肝、对症支持治疗,治疗组加用前列地尔10 μg静脉滴注,疗程2周;治疗期间观察患者的一般情况、2 4h尿量,每周复查肝功、肾功。结果　两组患者治疗后肝功能较治疗前均有所改善,治疗组的改善更为显著,血清总胆红素由132 5±5 7 8μmol·L-1降至6 3. 7±30 . 4 μmol·L-1,丙氨酸氨基转移酶由16. 8 2±5 9 .3IU·L-1降至74 . 8±2 .7 2IU·L-1(P <0 . 0 5 ) ;治疗组治疗后肾功明显改善,血肌苷由16 6 3±5 8 2 μmol·L-1降至10 2 .1±2 9. 5 μmol·L-1,尿素氮由2 0 . 6±7 3mmol·L-1降至6 . 4±3 .1mmol·L-1,2 4h尿量由4 2 .7 4±112 . 6ml增加到16 32 . 8±2 2. 8 5ml(P <0 . 0 5 ) ,而对照组肾功、尿量无改善(P >0 . 0 5 )。结论　前列地尔治疗肝硬化失代偿期合并肝肾综合征效果良好,不良反应少,临床可推广应用。     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Pharmacological treatment of COVID-19: an opinion paper

The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.