四氢原小檗碱型季铵化合物的合成及其某些参数的测定

以中草药有效成分原小檗碱类生物碱为先导物进行结构修饰,将原小檗碱用四氢硼钾还原成四氢原小檗碱,与卤代烃直接反应合成了24个四氢原小檗碱型季铵化合物。并测定了部分化合物对α_1受体的亲和力,HPLC反相C_(18)柱保留因子k。化合物的α_1受体亲和力随保留因子k及N-取代侧链的疏水参数π值的增大而增强。IC_(50),k及π之间高度相关。     

拟豪猪刺中的季铵生物碱

拟豪猪刺(Berberis soulieana schneid)系小檗科小檗属植物,分布于甘、陕、川、鄂等省。民间有用根及茎皮作黄连代用品,具有抗菌消炎作用。《中药志》仅用薄层色谱定性分析检查出小檗碱,巴马亭和小檗胺。本文从其根的酸水提取部分用硅胶柱色谱分离得B_3,B_4和B_5三个季铵生物碱。小檗碱:R_1R_2=—CH_2—巴马亭:R_1=R_2=—CH_3 药根碱:R_1=—H,R_2=—CH_3 三个化合物具有相似的紫外吸收,λ_(max)~(MeOH) 224,263,247和430nm、λ_(min)~(MeOH) 246,300和377nm,为2、3、9、10—四氧基取代的原小檗碱型骨架特     

手性对氯苄基四氢小檗碱的合成

目的:合成和分离对氯苄基四氢小檗碱的四个异构体,寻找优良的抗心律失常活性新药.方法:以小檗碱为原料进行还原制备四氢小檗碱,并用(-)/( )二对甲苯甲酰酒石酸对其拆分得到(-)S、( )R四氢小檗碱,然后每一单一异构体再进行季铵化,分别得到两个非对映异构体,最后进行柱层析分离制得对氯苄基四氢小檗碱(CPU-86017)的四个光学异构体.结果和结论:四个光学异构体经IR、1HNMR、13CNMR、MS、元素分析及在参考有关文献的基础上确证了其结构和构型.     

7-乙基吲哚的合成

以具心血管活性的四氢小檗碱类生物碱为先导物,结合某些钾通道阻滞剂的结构特征,设计并合成了14个未见文献报道的四氢小檗碱季铵化合物     

小檗碱体内药代动力学及药理活性研究进展

小檗碱是黄连、黄柏等中药材的主要活性成分之一,属于单苄异喹啉类季铵型生物碱,具有抗菌、消炎、抗心律失常、降血脂、降血糖以及抗肿瘤等多种药理活性。但小檗碱的口服生物利用度低,存在原形成分体内暴露水平与药效不相关的问题,提示小檗碱进入体内后可能产生了其他一些具有活性的代谢产物。因此,该文围绕小檗碱体内药物代谢、药物动力学及药理活性研究进展进行综述,有助于对小檗碱体内物质基础及药理活性有一概貌性的了解。     

N-(4-氯苄基)-2,3-亚甲二氧基-9-乙酰氧基-10-甲氧基-7,8,13,13a-四氢-8H-二苯骈[a,g]喹嗪氯化物的结构研究

N- (4-氯苄基 ) - 2 ,3 -亚甲二氧基 - 9-乙酰氧基 -1 0 -甲氧基 - 7,8,1 3 ,1 3 a-四氢 - 8H-二苯骈 [a,g]喹嗪氯化物 (ZH )是以小檗碱为先导物进行热解、酯化、还原、季铵化所得的原小檗碱类衍生物 ,初步药理试验表明此类化合物对乌头碱诱发的心律失常有一定的预防作用。本文通过 IR、MS、HRMS,特别是NMR谱 (包括1HNMR、13 CNMR、 COSY及HETCOR谱 ) ,对其结构进行了研究 ,结合四氢小檗碱核磁共振谱[1-3 ] ,确证了 ZH 的结构 ,并对其核磁共振信号进行了归属。1　仪　器1HNMR、13 CNMR、 COSY、 HETCOR谱用Bruker AM…     

苦参碱滴丸抗心律失常作用的实验研究

目的探讨苦参碱滴丸是否具有与片剂心律宁相同的抗心律失常作用。方法将大鼠随机分为 4组 :对照组 ,苦参碱滴丸 9粒 /kg组 ,苦参碱滴丸 18粒 /kg组 (苦参碱含量 10mg/粒 ) ,心律宁 5片 /kg组 (苦参碱含量10 0mg/片 )。给大鼠一次灌胃给药后 4 0min ,腹腔注射乌拉坦 1g/kg麻醉动物 ,连续观察Ⅱ导联心电图 ,由股静脉以 1.2 5 μg/min恒速输入乌头碱生理盐水 ,分别记录每只大鼠心律失常出现时间和诱发室性期前收缩、室性心动过速、心室颤动和心脏停搏的乌头碱用量。结果苦参碱滴丸 2个剂量组和心律宁片组与对照组比较 ,大鼠心律失常出现时间明显延长 (P <0 .0 5 ,P <0 .0 1) ,诱发大鼠心律失常的乌头碱用量明显增加 (P <0 .0 5 ,P <0 .0 1)。结论苦参碱滴丸对乌头碱诱发大鼠心律失常有明显预防作用 ,且较片剂用量小 ,起效快。     

小檗碱抑制D-半乳糖致大鼠蛋白糖基化的实验研究

目的:采用D-半乳糖诱导大鼠糖基化模型,观察小檗碱(Berberine,Ber)对蛋白糖基化反应的抑制作用。方法:D-半乳糖(150mg/kg,i.p.)给药8周,诱导糖基化模型大鼠,并于第2周开始给予小檗碱高(30mg/kg)、中(150mg/kg)、低(75mg/kg)剂量处理6周。测定红细胞醛糖还原酶活性、糖化血红蛋白含量和血清果糖胺、晚期糖基化终末产物含量。结果:小檗碱高、中剂量明显降低D-半乳糖引起的模型大鼠血糖升高(P<0.01,P<0.05),降低红细胞醛糖还原酶的活性,并显著抑制糖基化产物的形成(P<0.01,P<0.05)。结论:小檗碱对D-半乳糖诱致的大鼠糖基化反应具有明显的抑制作用。     

5-苯基-3-吡唑烷酮类化合物的抗惊厥作用

[目的 ]研究 13个 5 苯基 3 吡唑烷酮类衍生物化合物的抗惊厥作用 .[方法 ]采用最大电惊厥法测定抗惊厥活性 ,并以苯巴比妥钠及丙戊酸钠作对照 .[结果 ]化合物 (0 1)～ (0 5)中化合物 (0 5)具有较好的抗癫痫作用 ,其ED5 0 为 46 65mg/kg ;化合物 (0 6)～ (10 )无取代基的活性最低 ;化合物 (11)～(13 )是 3类化合物中抗癫痫活性最好的化合物 ,其中化合物 (13 )的ED5 0 为 10 0 7mg/kg .[结论 ] 5 苯基 3 吡唑烷酮类衍生物均具有较好的抗癫痫作用     

N—酰化／磺酰化四氢异喹啉化合物的合成

为寻找Ⅲ类抗心律失常药物,以钾通道阻滞剂分子中常见的酰胺和磺酰胺结构取代具钾通道阻滞活性和抗心律失常作用的氯化苄基四氢巴马汀(BTHP)分子中的季铵结构,设计合成了25个N-酰化或磺酰化的四氢异喹啉化合物(Ⅲ_(1～25)),其中23个化合物未见文献报道。这些化合物可视为BTHP的开环衍生物,结构均由元素分析、红外、核磁和质谱确证。     

APPLICATION OF LORNOXICAM TO PATIENT-CONTROLLED ANALGESIA IN PATIENTS UNDERGOING ABDOMINAL SURGERIES

FOR anesthesiologis s ,treatingpostoperativepainhas alwaysbeen a problem.Althoughopioidshave been provedtobe effective,theirsideeffectscouldnotbeignored.With thedevelopmentofscienceand pharmacology,many drugs with aspectsof satisfactoryanalgesicefficacyand couldbe welltoleratedby patientshave been developed.And lornoxicamisone of them, which isa non-steroidalanti-inflammatorydrug (NSAID ), with analgesic, anti-infl-ammatory,andantipyreticproperties.Itseliminationhalf-time(3 to 5 hours) isle…     

Acupuncture Treatment of Vomiting

CASE HISTORY A female patient, 46 years old, head of the foreign affairs department of a certain university in Beijing, paid her first visit on October 9, 2006, with the chief complaint of vomiting for one month. She got vomiting after meals in early September. Before that, she had discomfortable sensation in the stomach due to angry with others, but she didn't pay much attention. Later, it developed into vomiting after eating. After the vomiting, the discomfort would be relieved, but with slight hypodynamia. She was once diagnosed as having 'neurogenic vomiting'. Having taken some western and Chinese drugs, the above symptoms were a little bit improved, but she would have nausea upon eating and with regurgitation. Because of the fear for vomiting, she did not dare to have food intake, with body weight reduction of 6 kilos in one month.     

Qiu Baoguo''''s Experience in Treating Consumptive Syndromes after Radio-Chemotherapies

Radiotherapy and chemotherapy are the important modern medical therapies for malignant tumors,yet they can also bring about serious local and systemic toxic side reactions so to decrease the patient;'s life quality,manifested by a series of consumptive symptoms.Having engaged in the combined work of Chinese and western medicine for nearly 50 years,the research fellow Qiu Baoguo in Henan Provincial Academy of TCM has developed his unique views on the TCM study of consumptive syndromes.The author of this essay had once the fortune tO follow Dr.Qiu in clinic,and specially would like to introduce in the following Dr.Qiu's experience in treating consumptive syndromes after radio-chemotherapies for patients with malignant tumor.     

Insomnia Due to Deficiency of Both the Heart and Spleen Treated by Acupuncture-Moxibustion and Chinese Tuina

OBJECTIVE: To observe therapeutic effects of the comprehensive therapy of acupuncture-moxibustion and Chinese Tuina for treatment of insomnia due to deficiency of both the heart and spleen. METHODS: 92 cases were divided randomly into the treatment group (treated by acupuncture-moxibustion and Chinese Tuina) and the control group (treated by acupuncture-moxibustion). RESULTS: The therapeutic effect of the treatment group was obviously superior to that of the control group (the CHI2 test showed P < 0.01). CONCLUSIONS: The comprehensive therapy of acupuncture-moxibustion and Chinese Tuina can give marked therapeutic effects for treatment of insomnia due to deficiency of both the heart and spleen.     

Analysis of CK-19,PDX-1,Nestin,Ngn3 in different donor islet purity in rats

Objective: To investigate if there are the CK-19, PDX-1, Nestin, Ngn3 positive cells in the donor islets of different purity in rats. Methods: Thirty male adult SD rats were randomly divided into 3 groups. Islets were isolated using digestion by ductal injection of collagenase. Group Ⅰ (n=10): Separating cell preparations were not purified, Group Ⅱ(n=10): Islet sediment was purified with 25% Ficoll400 ,Group Ⅲ (n=10): Islet sediment was purified with 25% and 11% Ficoll-400. The levels of protein of CK-19, PDX-1, Nestin and Ngn3 were detected by immunohistochemistry and the mRNA of CK-19, PDX-1, Nestin, Ngn3 was amplified by RT-PCR. Results: After two different purification methods applied, three islet preparations of different purities were obtained. The difference of islet purity was significant among various groups (P＜0.05). Compared with group Ⅱ and group Ⅲ,the protein and mRNA of CK-19, PDX-1, Nestin,Ngn3 were both higher in group Ⅰ; group Ⅲ was poorly expressed. Conclusions: The three different islet purity donor islet have different CK-19, PDX-1, Nestin, Ngn3 positive cells within them, indicating that there are some islet stem cells in the purified donor islet.     

Dr.Zhang Ren''''s Experience in the Acupuncture Treatment of Different Diseases with the Same Therapeutic Principle

Dr.Zhang Ren,the chief physician,is the chairman of Shanghai Acupuncture and Moxibustion Association.Having been engaged in medicine for about 40 years,he is experienced in treating various intractable diseases.In his long years of clinical practice,he advocates taking the TCM differentiation as the basis to seek for the acupuncture method for treatment of modern intractable diseases.The author of this essay had the fortune to follow Dr.Zhang in study.The following is a summary of Dr.Zhang's experience in the acupuncture treatment for different intractable diseases with the same therapeutic principle.     

Luo Lingjie''''s Experience in Treating Chronic Nephropathy

In treating chronic nephropathy,Luo Lingjie,a chief physician,pays attention to regulating the balance between yin and yang,treating infection if present,and removing pathogenic factors.He prescribes gentle drugs and uses carefully strongly warming-tonifying ones,emphasizes the importance of persuading the patient to persist in treatment with medication and nurse one's health for recuperation,and is good at combined use of TCM and western medicine therapy and brings the merits of various therapies into full play,with obvious theraoeutic effects.     

Acupuncture Combined with Spinal Tui Na for Treatment of Primary Dysmenorrhea in 30 Cases

Objective: To observe the therapeutic effects in acupunture treatment of primary dysmenorrhea combined with spinal Tui Na, and study its mechanism. Methods: Thirty cases of the treatment group were treated by acupuncture combined with spinal Tui Na, and thirty cases in the control group were treated by routine acupuncture. Results: The total effective rate was 93.3% in the treatment group, and 73.3% in the control group, with a significant difference between the two groups (P<0.05). Conclusions: Acupuncture combined with spinal Tui Na has good prospects for treatment of primary dysmenorrhea.