苦木双碱甲和苦木双碱乙的结构

自苦木科(Simaroubaceae)植物苦木(Picrasma quassioides(D.Don.)Benn.)的木质部的乙醇提取物中经硅胶和氧化铝柱层析分离得到两个新β-咔巴啉二聚体生物碱,分别命名为苦木双碱甲(kumujansine)和苦木双碱乙(kumujantine),经光谱(UV,IR,¹H-NMR,^{13C-NMR,2D-NMR和MS)分析确定结构分别为式Ⅰ和Ⅱ。}     

苦木质量标准的探讨

苦木的细枝(直径:0.5～2 cm)中草酸钙结晶含量较多,但生物碱含量很少;粗枝(心材为深黄色)草酸钙结晶含量少或极少,而生物碱含量高.<中国药典>2000年版一部收载的苦木项下,性状与显微的描述为细枝的特征,而薄层鉴别为粗枝的生物碱反应,从而造成性状与显微特征符合规定的苦木,薄层鉴别却出现阴性结果.<中国药典>2000年版一部苦木项下,性状、显微鉴别与薄层鉴别相矛盾,建议修订完善其质量标准.     

麦角单菌核中麦角生物碱的薄层分离及荧光光密度法测定

本文介绍了麦角单菌核中麦角新碱、麦角酰胺、麦角胺及麦角克碱的薄层分离及荧光光密度法定量的分析方法。本法快速、灵敏,检出限度为1×10^-8g,四种生物碱的平均变异系数为6.10%,层离后的薄层斑点避光保存可稳定24小时。本法为探索麦角单个菌核问含麦角生物碱的质和量的变化以及为定向选育菌种提供了可能性。     

两个新的双去甲二萜生物碱高乌宁碱丁和高乌宁碱戊的结构研究

目的：研究高乌头Aconitum sinomontanum Nakai根的化学成分。方法：采用硅胶柱色谱及离心薄层色谱分离化学成分,IR, ¹HNMR, ¹³CNMR, ¹H-¹H COSY, HMBC, HMQC, MS等方法进行结构鉴定。结果：得到两个双去甲二萜生物碱高乌宁碱丁(sinomontanine D, 1)和高乌宁碱戊(sinomontanine E, 2)。结论：化合物1,2为新的双去甲二萜生物碱。     

十大功劳属部分植物茎中生物碱的高效毛细管电泳法测定

目的：对十大功劳属植物中3种生物碱的含量进行测定,为其内在质量的评价提供科学依据。方法：运用毛细管区带电泳(CZE)模式,以马钱子碱为内标化合物,测定了小檗碱、巴马亭和药根碱的含量。背景缓冲溶液为0.1 mol.L^-1磷酸缓冲液(pH 7.0)与甲醇(2∶1)的混合体系。线性范围：盐酸小檗碱为4.9～498.6 μg.mL^-1(γ=0.9990);盐酸巴马亭为5.0～504.9 μg.mL^-1(γ=0.9996);盐酸药根碱为5.1～505.8 μg.mL^-1(γ=0.9984)。回收率：盐酸小檗碱为96.00%～101.66%;盐酸巴马亭为100.15%～102.97%;盐酸药根碱为96.68%～102.44%。结果：不同品种、不同产地、不同采集时间的植物中的生物碱含量均有较大差别。结论：高效毛细管电泳法是中草药质量控制的一种简便、快速、有效的方法。十大功劳属多种植物生物碱含量较高,可作为新的药用资源。     

雷公藤倍半萜生物碱的研究

目的　研究雷公藤(Tripterygium wilfordii Hook.f.)的化学成分。方法　应用各种色谱技术进行分离纯化,用UV,IR,MS,HRMS,¹HNMR,¹³CNMR(COM和OFR),¹H-¹HCOSY,¹H-¹³CCOSY,2D-NOESY,¹H-¹³CCOLOC鉴定化合物。并进行初步的药理实验。结果　分离并鉴定了2个生物碱：euonine(I)和雷公藤康碱(IIwilfordconine)。结论　II为一种新的倍半萜生物碱,药理实验证明该生物碱有免疫抑制活性,并对白血病细胞有抑制作用。     

雷公藤榕碱的结构与分离

目的研究雷公藤(Tripterygium wilfordii Hook.f.)的化学成分。方法应用各种色谱技术进行分离纯化,用UV,IR,MS,HRMS,¹HNMR,¹³CNMR(COM和OFR),¹H-¹H COSY,¹H-¹³C COSY,2D-NOESY,¹H-¹³C COLOC鉴定化合物的结构。结果分离并鉴定了2个生物碱:I为wilforgine,II为雷公藤榕碱(wilfordlongine)。结论化合物II为一种新的倍半萜生物碱。     

免疫抑制成分异雷公藤春碱的分离与结构

从雷公藤(Tripterygium wilfordii Hook.f.)根皮中分离到一种倍半萜生物碱，根据理化性质和光谱(UV，TR，Ms，HRMs，¹HNMR，¹³CNMR．¹H-¹H COSY，¹H-¹³C COSY．2D-NOESY，¹H-¹³C COLOC)数据解析，鉴定为一种新的生物碱，命名为异雷公藤春碱嘛(isowilfortrine)。药理实验证明该生物碱有免疫抑制活性．并发现对白血病细响有抑制作用。     

苦地丁中异喹啉生物碱的反相离子对高效液相色谱分析法

建立了苦地丁中4种主要生物碱(普洛托品、右旋紫堇灵、四氢黄连碱和乙酰紫堇灵)的反相离子对高效液相色谱分析法。用TSK-120A固定相,用含0.1%SDS(pH8.0)的0.025mol·L^-1磷酸二氢钠—甲醇(35:65)为流动相。方法简便、灵敏,并用此方法分析比较了4种不同产地和6种不同种类的苦地丁。     

雷公藤倍半萜生物碱的分离与结构

从雷公藤(Tripterygiu mwilfordii Hook.f.)根皮中分离到二个倍半萜生物碱,即碱Ⅰ和碱Ⅱ,根据理化性质和光谱(UV,IR,MS,HRMS,^lHNMR,¹³CNMR(COM和OFR),¹H-¹HCOSY,¹H-¹³CCOSY,NOESY和COLOC]解析,鉴定生物碱Ⅰ为euonymine,生物碱Ⅱ为一种新的生物碱,命名为雷公藤明碱(wilfordsine)。初步药理实验证明雷公藤明碱有免疫抑制活性。     

苦木生物碱的化学研究

苦木(Picrasma quassioides (D.Don)Benn.)总生物碱的各种制剂在临床上证明是有效的抗菌消炎药物。为了阐明其有效成分,对其生物碱进行了研究,自其茎心的乙醇提取物通过硅胶和氧化铝柱层析以及制备性薄层层析,分离得到七个生物碱,根据光谱分析,物理化学常数的测定和衍生物的制备,其中四种鉴别为已知的生物碱:1-甲氧甲酰-β-咔巴啉(Ⅱ),4.5-二甲氧基铁屎米酮(Ⅳ),铁屎米酮(Ⅴ),4-甲氧基-5-羟基铁屎米酮(Ⅵ)。另外三种为新的天然产物,证明其结构为1-乙氧甲酰-β-咔巴啉(Ⅰ),1-甲酰-β-咔巴啉(Ⅲ)和1-乙烯基-4.8-二甲氧基-β-咔巴啉(Ⅶ)。体外抗菌实验表明碱(Ⅱ),(Ⅳ),(Ⅵ)和(Ⅶ)为有效成分。其他生物碱因量少未进行抗菌实验。     

A microbial model of mammalian metabolism: biotransformation of 4,5-dimethoxyl-canthin-6-one using Cunninghamella blakesleeana CGMCC 3.970

1.?A filamentous fungus, Cunninghamella blakesleeana CGMCC 3.970, was applied as a microbial system to mimic mammalian metabolism of 4,5-dimethoxyl-canthin-6-one (1). Compound 1 belongs to canthin-6-one type alkaloids, which is a major bioactive constituent of a traditional Chinese medicine (the stems of Picrasma quassioides).

2.?After 72?h of incubation in potato dextrose broth, 1 was metabolized to seven metabolites as follows: 4-methoxyl-5-hydroxyl-canthin-6-one (M1), 4-hydroxyl-5-methoxyl-canthin-6-one (M2), canthin-6-one (M3), canthin-6-one N-oxide (M4), 10-hydroxyl-4,5-dimethoxyl-canthin-6-one (M5), 1-methoxycarbonl-β-carboline (M6), and 4-methoxyl-5-O-β-D-glucopyranosyl-canthin-6-one (M7).

3.?The structures of metabolites were determined using spectroscopic analyses, chemical methods, and comparison of NMR data with those of known compounds. Among them, M7 was a new compound.

4.?The metabolic pathways of 1 were proposed, and the metabolic processes involved phase I (O-demethylation, dehydroxylation, demethoxylation, N-oxidation, hydroxylation, and oxidative ring cleavage) and phase II (glycosylation) reactions.

5.?This was the first research on microbial transformation of canthin-6-one alkaloid, which could be a useful microbial model for producing the mammalian phase I and phase II metabolites of canthin-6-one alkaloids.

6.?1, M1?M5, and M7 are canthin-6-one alkaloids, whereas M6 belongs to β-carboline type alkaloids. The strain of Cunninghamella blakesleeana can supply an approach to transform canthin-6-one type alkaloids into β-carboline type alkaloids.     

甙中结合糖测定方法的研究

甙是一类重要的中草药有效成分。在鉴定甙时,必须先将甙水解,然后分别鉴定水解后生成的甙元和糖。本文目的是研究甙中结合糖的分离、鉴定和定量的方法。甙可用酸回流法、封管法或在薄层上用酸蒸气水解;水解后的糖可用纸层析法。气相层析法、高效液相层析法及薄层层析法分离;分离后的糖常用比色法或薄层扫描法测定。     

Two new <Emphasis Type="Italic">β</Emphasis>-carboline alkaloids from the stems of <Emphasis Type="Italic">Picrasma quassioides</Emphasis>

Two new β-carboline alkaloids, 1-acetyl-4-methoxy-8-hydroxy-β-carboline (1) and 1-acetyl-4,8-dimethoxy-β-carboline (2), together with 10 known compounds; seven β-carboline alkaloids (3–9), two canthin-6-one alkaloids (10 and 11), and one quassinoid (12) were isolated from the stems of Picrasma quassioides. The structure of the new compounds 1 and 2 were determined by spectroscopic analyses including 1D- and 2D-NMR and HRMS interpretation. All the isolates (1–12) were evaluated for their cytotoxicity against human ovarian carcinoma A2780 and SKOV3 cell lines using MTT assays. Of the isolates, compounds 5–7 exhibited the most potent cytotoxicity on both A2780 and SKOV3 cell lines in vitro.     

长春胺中间体——1—乙基六氢吲(口朶)喹嗪的合成

本文提出了一条不以色胺为原料合成长春胺的关键中间体——高氯酸Wenkert氏烯胺的新途径。由于1-邻苯二甲酰亚胺基-4,5-辛二酮-4-苯腙(Ⅴ)的吲哚合成这一步收率很高,使这一途径成为合成1-正丙基-3,4-二氢-β-卡波林(Ⅶ)及Wenkert氏烯胺(Ⅹ)的较好方法。本文还利用红外光谱、质谱和核磁共振确定了1-邻羧基苯甲酰胺基-4,5-辛二酮-4-苯腙(Ⅳa)和1-正丙基-3,4-二氢-β-卡波林(Ⅶ)存在互变异构现象.     

秦艽生物碱的薄层色谱扫描测定

用CS-930型双波长薄层扫描仪探讨适合秦艽生物碱定量测定条件。以乙醚—丙酮为展开剂,在硅胶GF₂₅₄板上分离了秦艽甲素和丙素,分别用荧光熄灭和荧光法检出斑点后扫描测定。扫描参数:秦艽甲素λ_s255nm,λ_R280nm;秦艽丙素λ_s300nm,λ_R330nm;反射法锯齿扫描;SX=7;外标一点法;△y=0.2。得到两条通过原点直线。秦艽甲素及丙素的回收率分别为102.75%及100.42%,变异系数分別为2.48%及0.22%。用此法测定了中药秦艽中甲素和丙素的含量;对比了不同产地、同一产地野生和种植、地上和地下部分药材的生物碱含量,为开发秦艽资源提供信息。     

Chemical studies on the ether-soluble alkaloidal fraction ofPanax ginseng. Isolation of 1-carbobutoxy-β-carboline and 1-carbomethoxy-β-carboline

Two alkaloids were isolated from an ether-soluble alkaloidal fraction ofPanax ginseng. They were identified as 1-carbobutoxy-β-carboline and 1-carbomethoxy-β-carboline.     

吴茱萸化学成分的研究

吴茱萸化学成分的研究唐元清，冯孝章，黄量（中国医学科学院、中国协和医科大学药物研究所，北京１０００５０）中药吴茱萸（Ｅｖｏｄｉａｒｕｔａｅｃａｒｐａ［Ｊｕｓｓ］Ｂｅｎｔｈ）为芸香科植物吴茱萸干燥将近成熟的果实，有温中散寒、疏肝止痛之功效￣［１］，常用...     

Phytochemical study of the bark of some plants of the Elaeagnaceae family as a natural source of β-carboline indole alkaloids

We have studied the qualitative and quantitative composition of β-carboline indole alkaloids that have been isolated for the first time from bark of Hippopha? rhamnoides L., Elaeagnus angustifolia L., E. orientalis L., E. umbellata Thunb., E. multiflora Thunb., and E. argentea Pursh. occurring in Russia. Results of a phytochemical study showed that the bark of all these plants contains β-carboline alkaloids and that the first four of them can be promising sources of β-carboline alkaloids for the creation of drugs. Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 42, No. 11, pp. 27–29, November, 2008.     

Anticariogenic β-carboline alkaloids fromCommelina communis

The methanolic extract ofCommelina communis (aerial part) showed antibacterial activity aganist a cariogenic bacterium,Streptococcus mutans OMZ 176. The active principles were identified to be β-carboline alkaloids, 1-carbomethoxy-β-carboline, norharman and harman, which were bactericidal in the minimal inhibitory concentration (MIC) of 100 μg/ml against the strain.