Four new fluorenone alkaloids and one new dihydroazafluoranthene alkaloid from Caulophyllum robustum Maxim

Four new fluorenone alkaloids, caulophylline A-D (1-4), and one new dihydroazafluoranthene alkaloid, caulophylline E (5) were isolated from the roots of Caulophyllum robustum Maxim. Their structures were elucidated by spectroscopic analysis. Among the isolated alkaloids, Caulophylline E showed good scavenging effects against DPPH radical with IC₅₀ of 39 μM.     

四种沙漠植物生物碱含量的测定

用有机溶剂提取新疆南疆沙漠地区部分植物中的生物碱，结果显示：采集于十二团的权枝鸦葱中的生物碱含量较高，采集于阿拉尔市的碱蓬的生物碱含量较高，采集于岳普湖县的星花碱蓬的生物碱含量较高，采集于且末县的镰叶碱蓬的生物碱含量较高。于夏季采集的碱蓬其生物碱含量较于冬季时采集的高。从而初步得出：同种植物因生长地不同其生物碱含量不同，采集季节不同其生物碱含量也不同。     

不同生态区域中间香型烤烟生物碱含量及组分的比较

[目的]对比分析传统中间香型烤烟5个不同生态区域典型地点烟叶样品的生物碱含量及其组分差异,为烟叶生产种植的合理区划及改进烟叶质量提供参考.[方法]以传统中间香型烤烟5个生态区域的127份C3F烟叶样品为材料,分析比较其生物碱含量及组分的差异.[结果]5个生态区域以贵州中部山区烟叶中烟碱、降烟碱、麦斯明含量最高,分别达2.88％和0.68、0.0044 mg/g;秦巴山区烟叶中烟碱、降烟碱、麦斯明、新烟草碱含量最低,分别为2.24％和0.50、0.0032、0.76 mg/g.主要生物碱含量高低排序为烟碱＞新烟草碱＞降烟碱＞假木贼碱＞麦斯明.烟叶中烟碱占总生物碱的比例均高于93.00％,麦斯明占总生物碱的比例相对较稳定.相关分析结果表明,麦斯明与新烟草碱的相关程度为低度相关,麦斯明与降烟碱的相关程度及假木贼碱与新烟草碱的相关程度均达中度相关.[结论]5个生态区域烟叶生物碱含量存在明显差异,总生物碱和烟碱含量从高到低依次为贵州中部山区＞武陵山区＞东北产区＞山东产区＞秦巴山区,其中烟碱占总生物碱的比例均高于93.00％.     

苦豆子总碱防治菜青虫及对蔬菜品质的影响

试验结果表明,苦豆子总碱500~1000倍液对菜青虫的防治效果较好,药后3d的杀虫效果达78.4%~81.1%;在喷施苦豆子总碱500~3000倍液1、4、7、10d后均未检出其在蔬菜中的残留;喷施苦豆子总碱后蔬菜叶绿素的含量显著增加,亚硝酸盐和维生素C的含量明显下降。     

苦参愈伤组织的诱导及苦参总碱含量的检测

为了探索苦参愈伤组织培养的适宜条件和选择苦参总碱含量高的愈伤组织,用不同的消毒方法和不同的激素配比对苦参的子叶、叶片、地上茎和地下茎进行离体培养,诱导愈伤组织;并对外植体以及分别诱导出的愈伤组织进行苦参总碱的检测。结果表明,对苦参的外植体采用自来水冲洗30 min,75%酒精处理30 s,4%NaClO、滴加一滴tween-20,消毒5min就能取得较好的消毒效果;不同外植体以MS培养基为基本培养基加1.0 mg/L 2,4-D和1.5~2.5 mg/L NAA的条件下,均能高效率的诱导出愈伤,且生长较好;初步认为子叶和地下茎的愈伤组织中苦参总碱含量较高,适合选择子叶或地下茎的愈伤组织进一步进行筛选高产细胞系。     

Discovery and Evaluation of Thiazinoquinones as Anti-Protozoal Agents

Pure compound screening has identified the dioxothiazino-quinoline-quinone ascidian metabolite ascidiathiazone A (2) to be a moderate growth inhibitor of Trypanosoma brucei rhodesiense (IC₅₀ 3.1 μM) and Plasmodium falciparum (K1 dual drug resistant strain) (IC₅₀ 3.3 μM) while exhibiting low levels of cytotoxicity (L6, IC₅₀ 167 μM). A series of C-7 amide and Δ²⁽³⁾ analogues were prepared that explored the influence of lipophilicity and oxidation state on observed anti-protozoal activity and selectivity. Little variation in anti-malarial potency was observed (IC₅₀ 0.62–6.5 μM), and no correlation was apparent between anti-malarial and anti-T. brucei activity. Phenethylamide 7e and Δ²⁽³⁾-glycine analogue 8k exhibited similar anti-Pf activity to 2 but with slightly enhanced selectivity (SI 72 and 93, respectively), while Δ²⁽³⁾-phenethylamide 8e (IC₅₀ 0.67 μM, SI 78) exhibited improved potency and selectivity towards T. brucei rhodesiense compared to the natural product hit. A second series of analogues were prepared that replaced the quinoline ring of 2 with benzofuran or benzothiophene moieties. While esters 10a/10b and 15 were once again found to exhibit cytotoxicity, carboxylic acid analogues exhibited potent anti-Pf activity (IC₅₀ 0.34–0.035 μM) combined with excellent selectivity (SI 560–4000). In vivo evaluation of a furan carboxylic acid analogue against P. berghei was undertaken, demonstrating 85.7% and 47% reductions in parasitaemia with ip or oral dosing respectively.     

Prednisone and Vinblastine Chemotherapy for Canine Mast Cell Tumor—41 Cases (1992–1997)

Forty-one dogs with mast cell tumors (MCTs) were treated with oral prednisone and injectable vinblastine (VBL), both in the adjuvant setting (23 dogs) and in dogs with gross disease (18 dogs). Adverse effects were noted in 20% (8/41) of the patients, usually after the 1st dose of VBL. Adverse effects were considered mild in 6, and severe, necessitating treatment discontinuation, in 2 (5%). Overall response rate in the evaluable dogs with gross disease was 47% (7/15), consisting of 5 complete responses and 2 partial responses. Median response duration was 154 days (24 to >645 days). As adjuvant therapy to incomplete surgical resection, prednisone and VBL conferred a 57% 1- and 2-year disease-free rate. Median survival time (MST) for the entire patient population was not reached with a median follow-up of 573 days; however, the MST for dogs with grade III MCT was 331 days, with 45% of dogs alive at 1 and 2 years. This is an apparent improvement over historical survival data employing surgery alone. Upon univariate analysis, significant prognostic factors (P < .05) for survival included presence of a locally recurrent tumor, presence of gross disease, argyrophilic nucleolar organizer region frequency, lymph node status, histologic grade, previous chemotherapy, and ulceration of the tumor. Similar criteria were significant when analyzed for time to treatment failure. Response to therapy was also predictive of survival in the gross disease group. Upon multivariate analysis, histologic grade (P = .012) and presence of a locally recurrent tumor (P < .001) were significant factors for survival.     

甘肃棘豆（Oxytropis kansuensis）毒性生物碱研究

采用生物碱系统撮法，从甘肃棘豆（Oxytropis kansuensis)中分离出A，B，C，D等4种生物碱组分，经体外血清－a甘露糖苷酶活性抑制试验和小鼠口服服毒性试验，证明C，D组分具有毒性，D组分经质谱和红外光谱分析鉴定为8－甲基－1－羟基吲哚兹定醇。     

冰川棘豆生物碱分析及苦马豆素的分离、鉴定

冰川棘豆干粉,经甲醇提取,盐酸酸化,酸水液用氯仿萃取数次,NaOH调pH至9～10,依次用氯仿、乙酸乙酯、正丁醇萃取.称重表明生物碱多集中在正丁醇组分,且以大极性生物碱为主.薄层层析检查结果显示,氯仿组分有10种生物碱,乙酸乙酯组分有7种生物碱,正丁醇组分有5种生物碱.将正丁醇组分经硅胶柱层析,乙酸乙酯一甲醇系统梯度洗脱,每30～50 mL收集1份,薄层层析监测,同类合并.Ehrlich＇s试剂显色明显段油浴升华,得到白色针状结晶,与苦马豆素标准样品进行薄层层析对照,其斑点形状、颜色相同,Rf值相近.通过熔点和IR、MS、^1HNMR、^13CNMR等鉴定其化学结构,为苦马豆素.     

复方苦豆子灌注液总生物碱含量测定方法的建立

为建立复方苦豆子灌注液总生物碱含量的测定方法,采用酸性染料比色法,以氧化苦参碱为对照品进行含量测定,检测波长420 nm 的吸光度。结果显示,氧化苦参碱在2．0μg／mL～10μg／mL 范围内与吸光度呈良好线性关系,回归方程为 A＝0．0058C＋0．1116,r＝0．9992,氧化苦参碱的平均回收率为99．6％,RSD＝2．20％（n＝5）。该方法简便灵敏、准确可靠,可作为复方苦豆子灌注液的质量控制方法。