基于“因毒为能”思想的有毒中药常山毒效转化知识图谱可视化分析

目的 基于“因毒为能”思想,分析常山抗疟活性成分常山碱及其衍生物的知识图谱,为其毒效转化提供理论依据。方法 对中国知网与Web of Science数据库1993年1月1日至2023年10月18日核心集检索,导出相关中英文文献,使用CiteSpace、VOSviewer、Excel软件对中英文文献的发文量、作者、发文机构、国家、被引频次、关键词等进行分析。结果 共纳入文献235篇,其中中文137篇,英文98篇。常山碱及常山酮相关文献的年发文量呈现稳步增长趋势,共有18个国家对常山碱及常山酮进行了相关研究,其中研究最多的国家是中国,其次是以色列、美国、日本。中文发文量最多的机构为中国农业科学院兰州畜牧与兽药研究所兽用药物创制重点实验室（11篇）,英文发文量最多的机构为Volcani Institute of Agricultural Research(17篇)。被引频次前10次的中英文文献研究方向为常山碱及常山酮的药理活性、合成等。结论 常山碱及其衍生物的研究呈现上升趋势,中英文关键词共现、聚类显示常山碱及常山酮药理活性、毒性、结构修饰是目前的研究热点。对常山碱及其衍生物的抗疟机制、致吐...     

疟疾防治药物的研究——ⅩⅢ.3-取代氨基喹唑酮-4衍生物的合成

我国在2000年以前即用常山治疟,其主要有效成分常山乙碱(Ⅰ)具有用量小、效价高、无抗药性的特点,但因有严重的呕吐副反应和杀灭原虫不彻底的缺点,故不能广泛使用。     

鸡骨常山根中三个新吲(口朶)生物碱的分离和鉴定

从云南产鸡骨常山(Alstonia yunnanensis妇Diels)根中又分离得9个吲哚生物碱和一个非碱成分。根据理化性质和UV、IR、NMR及MS等光谱数据,推断三个新碱是去乙酰匹克林拉三甲氧基苯甲酸酯(deacetylpicraline 3,4,5-trimethoxybenzoate Ⅵ),17-乙酰蛇根精(17-acetylsarpagine Ⅺ)和16-差向蛇根精(16-episarpagine Ⅻ)。六个为已知碱。     

百蕊草生物碱成分的分离与鉴定

目的 研究百蕊草中的生物碱成分.方法 应用多种色谱手段进行分离纯化,通过IR、MS、HR-MS、NMR、2D-NMR技术鉴定化合物结构.结果 从百蕊草总生物碱部位分离得到3个化合物,分别鉴定为N-甲基金雀花碱(1)、白金雀儿碱(2)和槐果碱(3).结论 化合物N-甲基金雀花碱、白金雀儿碱、槐果碱均为首次从该植物中分离得到.     

弯喙乌头的化学成分研究

从弯喙乌头(Aconitum campylorrhynchum)中分离出一个微量新生物碱,经光谱和化学方法证明为8-乙酰嘟啦碱-(8-acetytdolaconine,Ⅰ),同时分离得到2个已知生物碱;即嘟啦碱(Ⅱ)和aconosine,(Ⅲ),后者是该植物的主要生物碱成分,在非生物碱部分还分离得到β-谷甾醇,棕榈酸和香豆酸。     

鸡骨常山根中三个新吲(口朶)生物碱的分离和鉴定

从云南产鸡骨常山(Alstonia yunnanensis Diels)根中又分离得9个吲哚生物碱和一个非碱成分。根据理化性质和UV、IR、NMR及MS等光谱数据,推断三个新碱是去乙酰匹克林拉三甲氧基苯甲酸酯(deacetylpicraline 3,4,5-trimethoxybenzoate Ⅵ),17-乙酰蛇根精(17-acetylsarpagine Ⅺ)和16-差向蛇根精(16-episarpagine Ⅻ)。六个为已知碱。     

抗癌植物药的开发研究——Ⅲ 城口唐松草的抗癌活性成分研究

从毛茛科城口唐松草(Thalictrum fargesii Fr.ex Fin.et Gagnep)根中首次分离得到两种具有抗癌活性的生物碱,分别鉴定为唐松草新碱(Thalidasine Ⅰ)和香唐松草碱(Thalifoetidine Ⅱ)。     

雷公藤生物碱的分离鉴定

我们从雷公藤（ＴｒｉｐｔｅｒｙｇｉｕｍＷｉｌｆｏｒｄｉｉＨｏｏｋ．ｆ．）中按常法分离得到总碱后经ＨＰＬＣ分析出现８个峰，经硅胶柱层析及硅胶ＲＰ－１８反相中压柱层析分离得到５个生物碱，由化学方法和光谱分析证明为雷公藤吉碱（Ｗｉｌｆｏｒｇｉｎｅ２０）．雷公藤次碱（Ｗｉｌｆｏｒｉｎｅ２１），雷公藤春碱（Ｗｉｌｆｏｒｔｒｉｎｅ２２），雷公藤碱戊（Ｗｉｌｆｏｒｉｄｉｎｅ２３），呋喃南蛇碱（Ｃｅｌａｆｕｒｉｎｅ１６）。ＨＰＬＣ分析指出含量最高为雷公藤吉碱，其次为呋喃南蛇碱。     

抗癌植物药的开发研究Ⅲ 城口唐松草的抗癌活性成分研究

从毛莨科城口唐松草（Thalictrum fargcsii Fr.ex Fin.etGagnep)根中首次分离得到两种具有抗癌活性的生物碱。分别鉴定为唐松草新碱（ThalidasineⅠ）和香唐松草碱（ThalifoetidineⅡ）。     

轮环藤中生物碱成分的研究

目的 研究轮环藤根中的生物碱成分.方法 采用多种色谱手段分离纯化,并通过波谱技术及理化性质鉴定化合物结构.结果 从轮环藤根中分离得到8个生物碱成分,分别鉴定为异粒枝碱(Ⅰ)、轮环藤碱(Ⅱ)、海岛轮环藤碱(Ⅲ)、海岛轮环藤酚碱(Ⅳ)、racemosinine B(Ⅴ)、木兰碱(Ⅵ)、α-cyclanoline(Ⅶ)和steponine(Ⅷ).结论 化合物Ⅳ～Ⅷ均为首次从轮环藤中分离得到.     

不同职业入伍的新兵社会状况及心理素质的研究

目的 研究不同职业入伍新兵的社会状况和心理素质特点.方法 整群抽取某部2630名集训新兵进行社会状况分析,并应用症状自评量表(SCL-90)、艾森克成人个性问卷(EPQ)、自我和谐量表(SCCS)、简易应对方式问卷(CSQ)、社会支持量表(SSRS)进行心理调查.结果 收回有效问卷2599份,城镇入伍、双亲家庭、高中以上文化、主动入伍、要求进步的新兵中入伍前职业是学生者较多;农村入伍、单亲家庭、初中以下文化、被动入伍的新兵中其他职业入伍者较多(P<0.05).SCL-90:学生新兵强迫、人际关系敏感、抑郁、焦虑、敌对、精神病性因子得分低于其他职业新兵(P<0.05,P<0.01);EPQ:学生新兵内外向因子得分高于其他职业新兵,而神经质和精神质得分低于其他职业新兵(P<0.01);SCCS:学生新兵自我不和谐、自我刻板性因子得分低于其他职业新兵,而自我灵活性得分高于其他职业新兵(P<0.01);CSQ:学生新兵积极应对得分高于其他职业新兵(P<0.01);学生新兵SSRS各因子得分均高于其他职业新兵(P<0.01).结论 学生新兵心理素质较好,可塑性强,入伍前职业是影响新兵心理素质的重要因素之一;新兵入伍后应结合入伍动机、目的、家庭状况,从自我和谐、积极应对、主动寻求支持等方面加强新兵的个性塑造.     

“民工潮”现象的社会学研究

民工潮是在我国经济和社会改革深化的过程发展起来的农民和农村人口的临时性的机械迁移,是我国农村乃至整个社会新的社会分层和社会流动机制运行引发的一个社会经济现象.从另一种视觉来看,民工潮包含的两个社会流动过程涨潮(农民从农村向城市流动)是一个下降的社会流动过程,而落潮(民工回乡)是一个向上的社会流动过程.民工潮是增强我国农村和城市社会经济发展活力的重要因素,对我国城乡的稳定发展也有特殊的积极意义.对民工潮的疏导是长期性工作,除了要促进区域经济的平衡发展和乡镇经济发展,让农业剩余劳动力尽量就近转移外,政府的服务工作和农村教育事业的发展也意义重大.     

Aporphine Alkaloids of Ocotea brenesii

The aporphine alkaloids (+)-isocorydine, (-)-3-hydroxynuciferine, and 3-hydroxy-6a,7-dehydronuciferine were isolated from the alkaloid fraction of an ethanol extract of the leaves of Ocotea brenesii Standley. Although (+)-isocorydine has been isolated from extracts of several Ocotea species previously, this is the first reported isolation of (-)-3-hydroxynuciferine and 3-hydroxy-6a,7-dehydronuciferine from this genus. Finally, to our knowledge, this is the first reported isolation of (-)-3-hydroxynuciferine from nature, although the compound was previously synthesized from nuciferine. In addition, it is only the second reported isolation of 3-hydroxy-6a,7-dehydronuciferine from a higher plant.     

Do Sources of Cigarettes Among Adolescents Vary by Age Over Time?

Trends in sources of cigarettes among adolescents were assessed using data from a teen cohort (2000–2006). Five sources—bought from store, got from other teen, stole from others, bought from others, and got from an adult—were measured over time by age. The most common source among all ages was other teens. Fewer teens bought cigarettes from stores, with a downward trend for all ages. Among all ages there was an upward trend in stealing, with younger teens more likely to steal cigarettes. In addition to targeting cigarette sales, interventions are needed to target other youth cigarette sources.     

A quantitative ultrastructural comparison of macrophages from rats exposed to smoke derived from conventional tobacco and a tobacco substitute

Using an image analysing computer a variety of ultrastructural features from micrographs of alveolar macrophages have been quantified.Macrophages from rats exposed to smoke from conventional tobacco cigarettes, for 6 months, revealed statistically significant changes when compared to controls. The macrophages were larger, rounded with fewer pseudopodia and contained increased numbers of inclusions.There were no statistically significant changes in macrophages from rats exposed to smoke from a tobacco substitute.     

REDUCED RESPONSES TO NORADRENALINE OF ISOLATED DIGITAL ARTERIES FROM HYPERTENSIVES

1. Strips of digital arteries obtained post-mortem from thirteen hypertensives have been compared with those from thirteen normotensives. 2. The strips from hypertensives and from males had a significantly greater response to 80 mmol/1 KCl, but this was due to the increased cross-sectional areas of the strips from hypertensives and from males. 3. The maximum responses to noradrenaline and serotonin, but not the pED₅₀ values, were significantly smaller in the strips from the hypertensives than in those from the normotensives, but there were no differences between the strips from hypertensives and normotensives in either the maximum response or pED₅₀ values to angiotensin or barium chloride. 4. It is concluded that these results suggest a decreased number of α-receptors are present in human hypertensive vascular smooth muscle and this is a sequel either of the increased pressure itself, or of increased exposure in vivo of the blood vessels from hypertensives to noradrenaline.     

Direct and indirect acquisition of syringes from syringe exchange programmes in Baltimore, Maryland, USA

Syringe exchange programmes (SEPs) are a fundamental source of sterile syringes and other health services for injection drug users (IDUs). However, various obstacles prevent many individuals from obtaining syringes from this source. As a result, some IDUs acquire syringes from “secondary exchangers”. The current study assessed the acquisition of syringes from the Baltimore City Needle Exchange Program (BNEP) as well as factors associated with obtaining syringes from the BNEP. Participants were asked to identify the colour of the cap of the most recently obtained syringe (red or grey cap suggested BNEP origins). In addition, support and risk network variables were examined. Although 38% reported using a syringe with a grey or red cap, only 7% reported that the BNEP was their primary source of syringes. Multivariate analyses showed that reporting the most recent syringe cap as red or grey was associated with obtaining syringes from the BNEP, obtaining syringes from a spouse, obtaining syringes from friends/neighbours, and number of drug users in their network. Based on these findings, encouraging secondary exchange is an effective method of providing injectors with syringes.     

Ribonucleotide reductase isolated from human cells: Heterogeneity among the sources

The amount of ammonium sulfate required to precipitate the ribonucleotide reductase activities derived from histocytic lymphoma cells obtained from patients or from KB or Connaughton cultured human cells is different than for reductase activity derived from Molt-4F and HeLa-S3 cells. The reductase activity of Molt-4F cells sedimented in a sucrose density gradient at a faster rate than the enzyme activity from KB cells; CDP and ADP reductase activity from either source co-sedimented. Enzymes from both cell lines sedimented at a faster rate in the presence of CDP and ATP than in the absence of these compounds, with CDP and ADP reductase still co-sedimenting. In addition, the enzymes obtained from the two sources have different stabilities at 37°. Hydroxyurea, 1-formylisoquinoline thiosemicarbazone (IQ-1), 1,10-phenanthroline and potassium chloride inhibit the enzyme activity derived from either Molt-4F or KB cells. However, a difference in the ratio of CDP to ADP reductase activity in Molt-4F and KB cells and a difference between the sensitivities of the CDP and the ADP reductase activities from the same cell line to various concentrations of inhibitors was observed.     

Estimating safe human exposure levels for lunar dust using benchmark dose modeling of data from inhalation studies in rats

Abstract

The pulmonary toxicity of airborne lunar dust was assessed in rats exposed by nose-only inhalation to 0, 2.1, 6.8, 20.8 and 60.6?mg/m3 of respirable size lunar dust. Rats were exposed for 6?h/d, 5?d/week, for 4 weeks (120?h). Biomarkers of toxicity were assessed in bronchial alveolar lavage fluid (BALF) collected at 1?d, 1 week, 4 weeks or 13 weeks post-exposure for a total of 76 endpoints. Benchmark dose (BMD) analysis was conducted on endpoints that appeared to be sensitive to dose. The number of endpoints that met criteria for modeling was 30. This number was composed of 13 endpoints that produced data suitable for parametric analysis and 17 that produced non-normal data. Mean BMD values determined from models generated from non-normal data were lower but not significantly different from the mean BMD of models derived from normally distributed data. Thus BMDs ranged from a minimum of 10.4 (using the average BMD from all 30 modeled endpoints) to a maximum of 16.6 (using the average BMD from the most restricted set of models). This range of BMDs yields safe exposure estimate (SEE) values of 0.6 and 0.9?mg/m3, respectively, when BMDs are extrapolated to humans, using a species factor of 3 and extrapolated from a 1-month exposure to an anticipated 6-month lunar surface exposure. This estimate is very similar to a no-observable-adverse-effect-level (NOAEL) determined from the same studies (0.4?mg/m3) and a SEE derived from a study of rats that were intratracheally instilled with lunar dusts (0.5–1.0?mg/m3).     

One-year follow-up after multimodal inpatient treatment for cocaine and methamphetamine dependecies

Of a randomly selected sample of 214 patients treated with aversion therapy for cocaine dependence in four chemical dependency units operated by Schick Shadel Hospitals, 156 were followed up 12 to 20 months posttreatment (average 15.2 months). Significant other validation was obtained in 33%. Total abstinence from cocaine for the group overall was 53% at one year post treatment, and current abstinence of at least 6 months at follow-up was 68.6%. Those treating with aversion for cocaine alone had a one-year abstinence of 39% and a current abstinence of 62.4%. Those treating with aversion for alcohol and cocaine had a one-year total abstinence from cocaine of 69% and a current abstinence of 76%. Those treating with aversion for cocaine and marijuana had a one-year total abstinence from cocaine of 50% and a current abstinence of 65%. Those treating with aversion for alcohol, cocaine, and marijuana had a one-year total abstinence from cocaine of 73% and a current abstinence of 73%. One-year total abstinence from alcohol was 54% for those receiving aversion for both alcohol and cocaine and 77% for those receiving aversion for alcohol, cocaine, and marijuana. Current abstinence from alcohol at follow-up was 68% and 81%, respectively. One-year total abstinence from marijuana was 42% for those treating with aversion for cocaine One-year total abstinence from marijuana was 42% for those treating with aversion for cocaine and marijuana and 64% for those treating with aversion for alcohol, cocaine, and marijuana. Current abstinence at follow-up from marijuana was 61% and 81%, respectively. The use of aversion therapy for both alcohol and cocaine in alcoholics who were also using cocaine was associated with higher total abstinence rates (88% vs. 55%) from cocaine when compared with alcoholics who used cocaine but received no aversion as part of their program. The conclusion is tentative since the follow-up rate in this study was lower than that of the previous study (64% vs. 84%). Being around other users accounted for 49% of relapse situations. Family/Work stress was associated with relapse in 33% of cases and unpleasant feelings in 24% of cases. The use of both reinforcement treatments and the use of support following treatment were associated with improved abstinence rates from cocaine. Those patients who reported losing all urges for cocaine after treatment had a total abstinence from cocaine of 90%, those who reported losing all the uncontrollable urges had a total abstinence of 64%, and those who reported still having the urge reported only 33% total abstinence from cocaine.