一步合成3-酮一△4,6甾体化合物

目的 研究用3-羟基-△5甾体化合物为原料合成3-酮-△4,6甾体化合物.方法 利用溴、溴化锂和助催化剂吡啶方法同时进行氧化脱氢.结果 得到目标化合物,精品收率达60%以上.结论 用该法收率高,成本低且一步合成.     

(S)-2-吡咯烷-α,α-二取代甲醇的合成

目的:合成一组具有重要用途的光学活性β-氨基醇. 方法:以手性天然产物L-脯氨酸为原料经酯化、氨基保护、格氏反应和催化氢解等四步反应合成四种光学活性的β-氨基醇. 结果:从原料L-脯氨酸到目标分子,四步总产率46%. 产物的1H NMR和元素分析结果与结构和元素组成相符. 结论:该方法原料价廉易得,反应条件温和,操作简便,产率高. 为合成手性β-氨基醇类化合物提供了一条有效途径.     

雌甾-3-甲氧基-2，5（10）-二烯-17-酮的合成研究

目的：研究雌甾-3-甲氧基-2,5（10）-二烯-17-酮（B）的最佳合成工艺。方法：以雌甾-3-甲氧基-2,5（10）-二烯-17-醇（A）为原料,分别运用沃氏氧化、活性二氧化锰和Collins试剂为氧化剂对其进行氧化反应,以得到标题化合物,并比较三种合成方法。结果与讨论：在以雌甾-3-甲氧基-2,5（10）-二烯-17-醇（A）为原料合成标题化合物的方法中,以沃氏氧化为最佳。     

手性氨基醇的研究进展

手性识别是自然界的一个重要现象，通过立体选择合成手性分子是当今有机合成中的一个重要部分，也是目前迅速发展的研究领域之一。不对称催化，一般指利用合理设计的金属络合物，来精确地区分左、右手两种进攻方式，从而产生高度对映的化合物。在手性金属络合物的设计中，配体的选择是很重要的，往往直接影响到手性识别的效果。手陛氨基醇分子中具有良好的配位能力的N原子及O原子，可与多种元素形成络合物，而且手性氨基醇的来源丰富，制备也较简单，甚至有些天然化合物（如麻黄碱）本身就是氨基醇，只要对其稍加修饰，即可成为优越的配体或催化剂。故在不对称催化中是一类优秀配体或催化剂。     

苦毒烷型萜类化合物及其生物活性的研究进展

苦豆烷型萜类化合物是一类独特的天然产物，具有高度密集的多环结构和连续的手性中心。苦毒烷型萜类化合物具有倍半萜、降二萜和倍半萜生物碱的骨架类型，是中药的主要功效成分之一，主要分布在苦皮桐科、兰科、防己科、叶下珠科和马桑科等中药民族药中。例如石斛、马桑、木奶果等均富含苦毒烷型萜类化合物。该类化合物具有6,5-双环骨架的母核，通常发生氧化和骨架重排，从而产生结构多样的衍生物， 例如具有络合或桥连γ-内酯的苦毒烷型类倍半萜和具有螺γ-内酯的苦毒烷型类降二萜。部分苦毒烷型类分子具有高度复杂的四环或五环环系结构，多达12个手性中心。苦毒烷型类化合物不仅用于治疗神经系统、癌症和免疫系统疾病，而且是神经系统疾病研究的工具分子，因此备受关注。近年来，大量具有显著生物活性的苦毒烷型类化合物不断被报道。迄今为止，已经有文献对苦毒烷型类生物碱和苦毒烷型类倍半萜的合成进行了综述，该文主要详细总结了天然苦毒烷型萜类化合物的结构。同时，对该类分子的分布和生物活性也进行概述。     

一个新颖的人参皂苷元衍生物及其抗HL-60肿瘤细胞活性

目的 研究人参皂苷元衍生物及其抗HL-60肿瘤细胞活性。 方法 利用Smith降解处理人参总皂苷,采用硅胶柱色谱、制备型高效液相色谱技术分离、纯化人参皂苷元等产物。通过波谱数据分析产物结构。采用MTT法测试产物抗HL-60肿瘤细胞活性。 结果 分离鉴定了原人参二醇(PD)、原人参三醇(PT)和24,25-烯-3β,6α-二羟基-12,20-(1′-羟基)双氧乙基-达玛烷(1),化合物1为新化合物命名为1′-羟基双氧乙基原人参三醇。 结论 化合物1为新型人参皂苷元衍生物,其抑制HL-60细胞增殖的作用强于PD和PT。     

一个新颖的人参皂苷元衍生物及其抗肿瘤活性（英文）

目的 研究人参皂苷元衍生物及其抗肿瘤活性.方法 通过Smith降解法水解人参皂苷Rg1和Rb1, 采用硅胶柱层析分离和纯化水解得到的产物, 通过NMR的数据分析鉴定产物的结构.结果 分离得到20 (S) -原人参三醇、20 (S) -原人参二醇、1, -羟基双氧乙基原人参三醇 (1) , 1, -羟基双氧乙基原人参二醇 (2) .结论 smith降解法能得到人参皂苷元衍生物, 化合物 (2) 为新颖的人参皂苷元衍生物, 其能抑制细胞周期分裂蛋白25B, 具有抗肿瘤的活性.     

美替诺龙醋酸酯的合成

目的　由 17β 乙酰氧基 5α雄甾 1 烯 3 酮 (1)经 5步反应合成蛋白同化激素美替诺龙醋酸酯 (17β 乙酰氧基 1 甲基 5α雄甾 1 烯 3 酮 ,6 )。方法　 17β 乙酰氧基 5α雄甾 1 烯 3 酮 (1)在酸的存在下与NBS反应 ,得2 β 溴 1α ,17β 二羟基 5α 雄甾烷 3 酮 17 醋酸酯 (2 ) ,化合物 (2 )用H2 /活性镍催化氢解 ,得 1α ,17β 二羟基 5α 雄甾烷 3 酮 17 醋酸酯 (3) ,然后在对甲苯磺酸的催化下化合物 (3)与甲醇作用 ,得 3,3 二甲氧基 5α 雄甾烷 1α ,17β 二醇 17 醋酸酯 (4 )。化合物 (4 )经铬酐 硫酸氧化 ,得 17β 乙酰氧基 3,3 二甲氧基 5α 雄甾烷 1 酮 (5 ) ,再经格氏反应和乙酰化反应 ,制得 17β 乙酰氧基 1 甲基 5α 雄甾 1 烯 3 酮 (美替诺龙醋酸酯 ,6 )。由化合物 1到 6的总收率为 48.7%。结果　此法以较高收率合成了美替诺龙醋酸酯。结论　该合成法有适用于工业化生产的前景     

酶促立体有择反应条件优化的初探

具光学活性的内型－三环〔５，２，１，０２，６〕癸－８－烯－３，５－二醇－５－乙酸酯是合成光学活性天然产物的很有用的手性合成子。采用正交试验优选出目标化合物最佳合成条件后，按作者设计的条件进行实验，获得了（＋）内型－三环〔５，２，１，０２，６〕癸－８－烯－３，５－二醇－５－乙酸酯。其（＋）对映体过量百分率（％ｅ．ｅ）＞９８．３％，产率８１％。提示本文报道的优化条件对该酶促反应是适合的。     

4-烯-3-酮甾体化合物17β,19位羟基的Jones试剂氧化反应研究

Jones试剂(26.72 g铬酐溶于含有23 ml浓硫酸的水溶液中,用水稀释到100 ml)可将仲醇氧化为酮,伯醇氧化为羧酸。作者在用Jones试剂氧化化合物(1c)以获得化合物(2b)时,意外地发现主产物是化合物(2c)。鉴于这一异常反应的出现,我们对具有4-烯-3~-酮结构的甾体化合物17β,19位羟基Jones试剂氧化产物作了研究。 用Jones试剂氧化化合物(1a)或(1b),分别得到     

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…     

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.     

猪肺磷脂注射液联合经鼻持续气道正压通气对呼吸衰竭早产儿的临床疗效及肌酸激酶同工酶活性的影响

目的 探讨猪肺磷脂注射液联合经鼻持续气道正压通气(NCPAP)对呼吸衰竭早产儿的临床疗效及肌酸激酶同工酶活性(CK-MB)的影响.方法 选取呼吸衰竭早产儿80例,分为观察组和对照组各40例.对照组采用NCPAP给氧治疗,观察组给予NCPAP给氧联合猪肺磷脂气管内给药.观察两组患儿治疗前及治疗12h、24 h后PaO2、PaCO2、血氧饱和度(SaO2)、pH的变化情况,检测治疗前及治疗5d后血清CK-MB水平;评估两组患儿的临床治疗效果.结果 两组患儿PaO2、PaCO2、SaO2、pH比较,差异均有统计学意义(P＜0.05),其中观察组治疗后的PaO2、SaO2、pH均高于对照组,PaCO2则低于对照组.两组的PaO2、SaO2、pH均随观察时间延长而升高(P＜0.05),PaCO2均随观察时间的延长而降低(P＜0.05).观察组治疗有效率为87.5％,显著高于对照组的70.0％ (P ＜0.05).治疗5d后两组患儿血清CK-MB水平均较前降低(P＜0.05),且观察组明显低于对照组(P＜0.05).结论 猪肺磷脂注射液气管内给药联合NCPAP可以显著降低呼吸衰竭早产儿CK-MB的含量,提高治疗有效率,起到很好的呼吸循环支持作用.     

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.     

Survey and practice of reporting quality of randomized controlled clinical trials on traditional Chinese medicine

Evidence obtained from randomized controlled trials （RCTs） has been generally accepted as the gold standard in the evaluation of clinical effectiveness. Readers need to understand the trial design, implementation, results, analysis and interpretation, so as to fully Jnderstand the results of RCTs. Thus, the investigators of RCTs have to report these items in a complete, accurate and clear manner. Since 1998, we have conducted several evaluations on the reporting quality of RCTs published in Chinese journals on traditional Chinese medicine （TCM） and results have shown that there is an urgent need for higher quality RCTs on TCM.