胶陀螺化学成分的研究

从胶陀螺中分离得到麦角甾醇、丙二酸和葡萄糖3种单体化合物：6-戊基-4羟基-2-一,四氢化-2氢-吡喃(2H—Pyran-2-one,tetrahydro-4-hydroxy-6-pentyl)和6-戊基-2-,5,6-二氢化-2氢-吡喃(2H—Pyran-2-one,5,6-dihydro-6-pentyl)2种主要香气成分;Bulgarhodin(I)和Bulgarein(Ⅱ)2种色素混合物。该菌中还含有碳原子数为13、14、15、16、17、20、21、36和44的一组饱和烃类化合物。     

GC-MS法分析曼陀罗挥发油的化学成分

用水蒸气蒸馏法从曼陀罗中提取挥发油,并用气相色谱/质谱联用技术(GC-MS)对挥发油的化学成分进行分离鉴定,用气相色谱峰面积归一化法确定各组分的相对含量.结果从曼陀罗挥发油中鉴定出58种化合物,占总挥发油量的92.37%.其中主要成分为5,6-二氢-6-戊基-2H-吡喃-2-酮(44.29%)、二苯胺(12.50%)、四十四烷(10.41%)、二十烷(4.19%)、(E)-3-己烯-1-醇(2.38%)、3,7,11,15-四甲基-2-十六碳烯-1-醇(2.28%)等.     

绿色木霉菌LTR-2孢子提取物的抑菌活性及化学成分分析

通过研究绿色木霉菌LTR-2分生孢子提取物的抑菌活性及化学成分,为进一步提取纯化新型抗生素提供依据。采用固体麸皮培养基培养绿色木霉菌LTR-2,以二氯甲烷浸提法提取分生孢子中的抗菌物质,采用菌丝生长法测定提取物的抑菌活性,并用气相色谱-质谱联用仪进行分析,峰面积归一法计算有关成分的相对含量。绿色木霉菌LTR-2分生孢子的提取物抑菌谱广,对供试11种植物病原真菌均有不同程度的抑制作用;抑制效果好,对禾谷丝核菌的抑制率为89.3%。从提取物中分离鉴定出60多种化学成分,其中烷烃类成分数量最多,为43种,其他成分有酮类、有机酸类、醇类、烯类等,主要成分是麦角固醇,含量为41.90%。结论:绿色木霉菌LTR-2分生孢子提取物具有抑菌作用。通过化学成分分析,提取物中含有化合物5,6-二氢-6-戊基-2H-吡喃-2-酮,含量为2.35%,结合文献报道,推测5,6-二氢-6-戊基-2H-吡喃-2-酮是提取物中起抑菌作用的物质。     

异叶三宝木叶的化学成分研究(英文)

从异叶三宝木(Trigonostemon flavidus)叶中分离得到9个化合物,经波谱数据分析鉴定为robustic acid(1),1-[6-hydroxy-2-methoxy-2″,2″-dimethylpyrano-(5″,6″:3,4)]-2-(4’-methoxyphenyl)-1,2-ethanedione(2),3β-ursolic acid(3),(6S,7E)-6-hydroxy-4,7-megastigmadien-3,9-dione(4),3(-hydroxy-5,6-epoxy-7-megastigmen-9-one(5),(3R,6R,7E)-3-hydroxy-4,7-megastigmadien-9-one(6),loliolide(7),methyl P-coumarate(8),和methyl si-napate(9)。化合物1～7和9为首次从三宝木属(Trigonostemon)植物中分离得到。     

博落回茎中抗玉米大斑病的生物碱类成分研究

为了解博落回茎中具有抗玉米大斑病的活性成分,采用天然产物分离和活性追踪的方法分离鉴定了8个生物碱类化合物。这8个化合物分别为6-(2-羟基乙基)-5,6-二氢血根碱(1)、6-(2-甲氧基-2-氧代乙基)-5,6-二氢血根碱(2)、6-丙酮基二氢血根碱(3)、6-丙酮基白屈菜红碱(4)、isointegriamide(5)、arnottianamide(6)、二氢血根碱(7)和白屈菜红碱(8)。其中化合物1、2、5、6首次从博落回茎中分离得到。以上生物碱类化合物(1～8)通过滤纸片琼脂糖扩散法对玉米大斑病进行抗菌测试,确定了化合物8具有显著的抗玉米大斑病的生物活性,然后用48孔板测定了化合物8对玉米大斑病孢子萌发实验,其IC_(50)值为12.0μg/mL,以上研究为防治玉米大斑病提供了一种潜在的新型生物农药原料。     

清香木姜子的化学成分

从清香木姜子（Litsea euosma W．W．Smith）的枝叶中分离得到1个新化合物-α-吡喃酮衍生物（1）以及3个已知化合物：阿魏酸酯衍生物（2）,6-氧-棕榈酰-β-胡萝卜甙（3）和葡萄糖（4）,经波谱学鉴定新化合物α-吡喃酮衍生物的结构为：5-经基-6-甲基-3-（10-十一烯基）-5,6-二氢吡哺-2-酮。     

中国被毛孢液体发酵的化学成分

本文采用反相硅胶、正相硅胶和Sephadex LH-20凝胶等层析技术对中国被毛孢液体发酵的化学成分进行研究。经1D-NMR(1H NMR、13C NMR、DEPT)、2D-NMR(HSQC、HMBC、1H,1H-COSY)和ESI-MS、HR-EI-MS解析鉴定,从其菌丝体中分离到腺苷(1)、2'-脱氧腺苷(2)、2,3-二羟基丙基壬烷酸酯(3)和4-羟基-6-戊基-四氢吡喃-2-酮(4),从发酵液中分离到4-甲基-1H-咪唑-5-乙醇(5)。化合物3和5首次以天然产物形式分离得到。     

黄桐枝叶的化学成分研究

为研究黄桐(Endospermum chinense Benth.)的化学成分,运用柱层析等分离纯化方法从黄桐枝叶中分离得到13个化合物:pubinernoid A(1)、(E)-linalool-1-oic acid(2)、(+)-去氢催吐萝芙木醇(3)、3α-hydroxy-5,6-epoxy-7-megastigmen-9-one(4)、齐墩果酸(5)、3-羰基齐墩果酸(6)、3-oleana-9(11),12-dien-28-oic acid(7)、甘五酸(8)、altissimanin C(9)、7-羟基-β-谷甾醇(10)、丁香脂素(11)、ficusesquilignan A(12)、ficusesquilignan B(13)。其中化合物7为新天然产物,化合物1~4、8~13为首次从该属植物中分离得到。     

爆杖花的黄酮类成分研究

爆杖花(Rhododendron spinuliferum)茎叶75%丙酮水提取物采用硅胶柱色谱、Sephadex LH-20色谱、高效液相色谱等技术分离纯化,从其乙酸乙酯部分中共分离和鉴定了6个黄酮类化合物,槲皮素-3-O-[3″,4″-O-(异丙叉基)-β-D-木吡喃糖苷] (1),二氢槲皮素(2),二氢槲皮素-3-O-β-D-木吡喃糖苷(3),5,7,4′-三羟基-二氢黄酮醇-3-O-α-L-鼠李吡喃糖苷(4),二氢槲皮素-3-O-α-L-鼠李吡喃糖苷(5),花青素A-2(6).其中化合物1为新化合物,爆杖花的化学成分为首次报道.     

秃叶黄皮树叶子的化学成分研究(英文)

从秃叶黄皮树叶子(Phellodendron chinensevar.glabriusculumSchneid)分离到7个化合物,经波谱解析鉴定为6-O-乙酰基黄柏苷(1),6-O-乙酰基二氢黄柏苷(2),(2R)-4′,5-二羟基-7-O-β-D-吡喃葡萄糖基-8-异戊烯基-二氢黄酮(3),黄柏苷(4),2-O-β-D-吡喃葡萄糖基-6-羟基-苯甲酸苄酯(5),柑橘素C(6),3-羰基齐墩果烷(7),其中化合物1～3,5～7为首次从秃叶黄皮树叶子中分离得到。     

胶陀螺的光敏活性组分

用石油醚、氯仿、乙酸乙酯和丙酮对胶陀螺子实体进行梯度提取,得到的粗提物做光敏活性药理试验,结果表明:胶陀螺的氯仿和乙酸乙酯粗提取物有明显的光敏活性。将氯仿和乙酸乙酯的粗提物分别用不同比例的氯仿—甲醇进行反复柱层析,同时配合光敏活性药理试验,得到6个有光敏活性的组分,分别为c2、c3、c4、c5、c6和c11。将6个组分合并后继续分离,最终得到1个有橙黄色荧光点的成分,对其进行光敏活性药理试验,结果证明其为胶陀螺的光敏活性成分。     

蛹虫草培养液成分研究

目的：研究蛹虫草培养液的化学成分。方法：采用硅胶柱色谱等技术分离纯化单体化合物,并根据理化性质及光谱数据鉴定结构。结果：分离并鉴定了8个化合物,分别是2-乙基-3-羟基4H吡喃酮（1）、1-甲酰基-苯并咪唑（2）、3-乙基-4-羟基-6-甲基．2H．吡喃-2-酮（3）、1-甲基-6-异丁基-2,5-哌嗪二酮（4）、1-异丙基-6-异丁基-2,5-哌嗪二酮（5）、3,6-二（对羟基苄基）-2,5-哌嗪二酮（6）、1-羟甲基-6-异丁基-2,5-哌嗪二酮（7）、麦角甾-7-22-二烯-3β,5α,6β-三醇（8）。结论：化合物1-5,7为首次从虫草属真菌中分离得到。     

Novel morpholin-3-one derivatives induced apoptosis and elevated the level of P53 and Fas in A549 lung cancer cells

Previously, we found that nine kinds of new morpholin-3-one derivatives could inhibit the growth of A549 lung cancer cells in a dose-dependent manner, but how they performed their function remained unknown. In this paper, we studied the effects of the three more effective morpholin-3-one derivatives {4-(4-chlorophenyl)-6-((4-nitrophenoxy) methyl) morpholin-3-one (1); 6-(4-chlorophenoxy)-4-(4-methoxyphenyl) morpholin-3-one (2); and 6-((4-nitrophenoxy) methyl)-4-phenylmorpholin-3-one (3)} on the cell cycle distribution, apoptosis, and the level of P53 and Fas that are two kinds of important proteins in the regulation of A549 cell growth and apoptosis. According to the results of cell viability, we selected 40 microg/ml of morpholin-3-one derivatives as the most appropriate concentration for the following study. The results showed that the morpholin-3-one derivatives partly blocked the cells at G1 phase, induced apoptosis, and elevated the level of P53 and Fas proteins significantly. The effect of the morpholin-3-one derivates was associated with translocation of P53 and clustering of Fas. Our data suggested that the morpholin-3-one derivates might be promising tools for elucidating the molecular mechanism of lung cancer cell apoptosis and they will be very potential candidates for developing anti-cancer drugs.     

胶陀螺(Bulgaria inquinans)的生药学研究

对胶陀螺药材性状、显微特点、理化特性和分子鉴定等方面研究结果表明,子实体初期呈黄褐色球形,并带有黄棕色麻点,顶端逐渐开裂,产生一至多个不等的裂口,裂口不断扩大,最后整个子实体表面呈黑色皱缩。子囊棒形。外囊盘被由圆形细胞组成,圆形细胞外侧生绒毛,细胞内含类似载色体的物质;中囊盘被由埋在胶质中的交错菌丝组成。采用子囊孢子弹射分离法所得菌丝有橘黄色菌丝和长有棒状等分生孢子的有隔菌丝无色;从子实体组织分离培养的菌丝状,无色,其中生有黑褐色或黄棕色的圆形细胞,呈念珠状。胶陀螺子实体DNA序列与菌丝DNA序列的同源性为99.65%,胶陀螺子实体的DNA序列与GenBank数据库中AY789345比对,其同源性为99.80%。     

中国歧裂灰包属Phellorinia Berk.的研究

根据对产于中国的材料的研究,作者认为歧裂灰包属Phellorinia应包括2个种,歧裂灰包P.inquinans和球果歧裂灰包P.strobilina,对这2个种进行了详细描述和显微绘图,并给出了该属种的检索表。     

Syntheses and biological activities of pyranyl-substituted cinnamates

Twenty-two kinds of pyranyl-substituted cinnamates were synthesized by the reaction of 4-hydroxy-6-(2-phenylethyl)-2H-pyran-2-one or 4-hydroxy-6-methyl-2H-pyran-2-one (HMP) with a variety of substituted cinnamic acids, and their antifungal and plant growth inhibitory activities were investigated. Among the compounds prepared, 6-methyl-2-oxo-2H-pyran-4-yl 3-(4-isopropylphenyl)propenoate (H5) showed the strongest antifungal activity against Rhizoctonia solani and Sclerotium dellfinii, and 6-methyl-2-oxo-2H-pyran-4-yl 3-(2-methylphenyl)propenoate (H2) had the highest plant growth inhibitory activity toward Brassica rapa.     

Isolation and characterization of several unique lipids from Azotobacter vinelandii cysts.

Unique cyclic compounds were found in the lipid fraction of Azotobacter vinelandii cysts. In addition to two major molecular species which had already been identified, 5-n-alkylresorcinol and its galactoside derivative, five other molecular species (two alkyl side chain homologs of each) were isolated, and their structures were established by infrared, ultraviolet, nuclear magnetic resonance, and mass spectroscopy. These 10 compounds were 6-n-heneicosylresorcylic acid methyl ester and 6-n-tricosylresorcylic acid methyl ester, 5-n-(2-hydroxy)heneicosylresorcinol and 5-n-(2-hydroxy-tricosylresorcinol, 5-n-heneicosyl-4-acetylresorcinol and 5-n-tricosyl-4-acetylresorcinol, 6-n-heneicosyl-4-hydroxypyran-2-one and 6-n-tricosyl-4-hydroxypyran-2-one, and 6-(2-oxotricosyl)-4-hydroxy-pyran-2-one and 6-(2-oxopentacosyl)-4-hydroxypyran-2-one.     

Diazepinone Nucleosides as Inhibitors of Cytidine Deaminase.

Abstract

The synthesis of 2′-deoxy and 2′,3′-dideoxy derivatives of 1-ß-D-ribofuranosyl-1,3,4,7-tetrahydro-2H-1,3-diazepin-2-one (2) was undertaken in order to find new cytidine deaminase (CDA) inhibitors and potential adjuvants in anticancer chemotherapy. Replacement of ribose by a 2-deoxyribose moiety led to compound 9 that appeared slightly more potent than 2 (Ki = 2.5 × 10^?8 M). Remarkably, the corresponding α-2′-deoxynucleoside 10 acted as a very potent inhibitor of human placenta CDA, with a Ki = 7.5 × 10^?8 M. Attempt to synthesize the 2′,3′-dideoxy derivative of 2 led to N-[4,5-dihydroxy-1-(2-oxo-2,3,4,7-tetrahydro[1,3] diazepin-1-yl)-pentyl]-2,2,2-trifluoroacetamide (13), which is devoid of CDA inhibitory activity.     

3-Alkyl- and 3-amido-isothiazoloquinolin-4-ones as ligands for the benzodiazepine site of GABA(A) receptors

Based on a pharmacophore model of the benzodiazepine binding site of the GABA(A) receptors, developed with synthetic flavones and potent 3-carbonylquinolin-4-ones, 3-alkyl- and 3-amido-6-methylisothiazoloquinolin-4-ones were designed, prepared and assayed. The suggestion that the interaction between the hydrogen bond donor site H1 with the 3-carbonyl oxygen in 3-carbonylquinolin-4-ones can be replaced by an interaction between H1 and N-2 in the isothiazoloquinolin-4-ones, was confirmed. As with the 3-carbonylquinolin-4-ones, the length of the chain in position 3 is critical for an efficient interaction with the lipophilic pockets of the pharmacophore model. The most potent 3-alkyl derivative, 3-pentyl-6-methylisothiazoloquinolin-4-one, has an affinity (K(i) value) for the benzodiazepine binding site of the GABA(A) receptors of 13 nM. However, by replacing the 3-pentyl with a 3-butyramido group an even more potent compound was obtained, with a K(i) value of 2.8 nM, indicating that the amide function facilitates additional interactions with the binding site.