岩木瓜茎干化学成分及PTP1B抑制活性研究

综合运用天然产物化学分离、纯化技术从岩木瓜茎干中分离得到18个化合物,结合各化合物理化性质和光谱数据鉴定其结构,依次为对羟基苯乙酮(1)、对羟基苯甲酸(2)、对羟基苯甲酸乙酯(3)、3-hydroxy-1-(4-hydroxy-3-methoxyphenyl)propan-1-one(4)、咖啡酸(5)、咖啡酸乙酯(6)、对羟基苯甲醛(7)、咖啡酸甲酯(8)、对羟基桂皮酸(9)、水杨酸(10)、原儿茶酸(11)、3,5-二羟基-4-甲氧基苯甲酸(12)、对醛基苯基-1-O-葡萄糖苷(13)、色氨酸(14)、豆甾-3,6-二酮(15)、β-谷甾酮(16)、5α-9(11)-豆甾烯-3β-醇(17)和胡萝卜苷(18)。这些化合物均为首次从该植物分离得到,其中化合物4,6,16和17为首次从该属植物中分离得到。对从岩木瓜中分离得到的46个化合物进行PTP1B抑制活性筛选,11个化合物具有PTP1B抑制活性,IC50值在1.0~37.0μM之间。     

黄桐树皮的化学成分研究

从黄桐(Endospermum chinense Benth.)树皮中分离获得了10个化合物。通过光谱分析,分别鉴定为3-羰基齐墩果酸(1)、齐墩果酸(2)、7-羰基谷甾醇(3)、β-谷甾醇(4)、β-胡萝卜甙(5)、7-羰基-β-胡萝卜甙(6)、4-羟基-3-甲氧基苯甲醛(7)、7-羟基-6-甲氧基香豆素(8)、3-羟基-4-甲氧基苯甲酸(9)和壬二酸(10)。10个化合物均为首次从黄桐树皮中分离得到。     

红波罗花的化学成分研究(英文)

从红波罗花(Incarvillea delavayi)植物的干燥全草乙醇提取物中分离得到12个化合物,通过MS和NMR等方法鉴定为tecomine(1)、epidihydrotecomanine(2)、2,6-二甲基-6-羟基-2-庚烯-4-酮(3)、marine B(4)、(3R,5S)-3-methyl-cyclopentyl[1,2-c]pyridine-5-ol(5)、3,4,5-三甲氧基苯甲酸乙酯(6)、cleroindicin B(7)、3,4,5-三甲氧基苯甲酸甲酯(8)、2-(4’-乙氧基苯基)-乙醇(9)、6-羟基苯并二氢呋喃(10)、β-谷甾酮(11)、β-乙酰齐墩果酸(12)。其中化合物1～3、5～6、8～12为首次从角蒿属植物中分离得到,所有化合物均为首次从该植物中分离得到。     

马槟榔果实的化学成分研究（英文）

采用硅胶柱色谱和Sephadex LH-20等分离方法,对马槟榔Capparis masaikai果实的化学成分进行分离纯化,依据理化性质及波谱数据分析进行结构鉴定,从中分离鉴定了10个单体化合物,分别为:杜仲树脂酚(1)、erythro-guaiacylglycerol-β-O-4'-sinapyl ether(2)、hedyotol C(3)、hedyotisol A(4)、hedyotisol B(5)、ozoroalide(6)、5α,6α-epoxy-3β-hydroxyergosta-22-ene-7-one(7)、松柏醛(8)、3-羟基-5-(对羟基苯基)戊酸(9)、β-hydroxypropiovanillone(10)。分离得到的化合物结构类型包括木脂素、大环内酯、甾醇及酚类。化合物1~10为首次从该植物中分离,其中1~7为首次从该属植物中分离得到。     

米邦塔仙人掌化学成分研究

从米邦塔仙人掌正丁醇部分分离到10个化合物。应用色谱和光谱分析方法分别鉴定为对羟基苯甲酸(1)、β-羟基-3-甲氧基-4-羟基苯乙酮(2)、2,3,4-三羟基戊酸(3)、4-甲氧基桂皮酸(4)、3-羟基-4-甲氧基肉桂酸(5)、5-羟基阿魏酸(6)、4-羟基肉桂酸(7)、原儿茶酸(8)、n-butyl eucomate(9)和eucomic acid(10)。化合物2～10为首次从该植物分离得到。     

藏药翁布的黄酮类化学成分研究

从藏药翁布(Myricaria germanica)的60%丙酮提取物中分离得到了11个黄酮类化合物,利用光谱、波谱分析法鉴定其结构分别为:35,,4’-三羟基-73,’-二甲氧基黄酮(1),3,5,4’-三羟基-7-甲氧基黄酮(2),3,5,3’,4’-四羟基-7-甲氧基黄酮(3),35,7,-三羟基-4’-甲氧基黄酮(4),柽柳素(5),山柰酚(6),槲皮素-3-O-β-D-葡萄糖苷(7)5,,7,4’-三羟基-3-O-β-D-葡萄糖醛酸(8),5,7,3’4,’-四羟基-3-O-β-D-葡萄糖醛酸(9),槲皮苷(10)和阿福豆苷(11)。上述化合物均为首次从该植物中分离得到,其中化合物4、5、7～11为首次从水柏枝属植物中分离得到。     

珍珠菜的化学成分研究(英文)

从珍珠菜(Lysimachia clethroidesDuby)的70%丙酮提取物中分离得到11个化合物,经理化性质及波谱数据分析分别鉴定为23-羟基乌苏酸(1)、Isotachioside(2)、对羟基苯甲酸(3)、3-甲氧基-4-羟基苯甲酸(4)、原儿茶酸(5)、3,5-二羟基苯甲酸(6)、甲基-α-D-呋喃果糖苷(7)、尿苷(8)、β-谷甾醇(9)、胡萝卜苷(10)和齐墩果酸(11)。化合物1、2、4、7和8为首次从该属植物中分离得到,化合物3、5、6、9~11为首次从该种植物中分离得到。     

小叶米仔兰枝条中的抗菌活性成分研究

为探讨小叶米仔兰(Aglaia odorata var.microphyllina)中的抗菌活性成分,从其枝条的乙醇提取物中分离得到6个化合物,通过波谱分析,分别鉴定为:4(15)-桉叶烯-1β,7,11-三醇(1)、4α,10β,11-三羟基-1,5-反-愈创木烷-6-烯(2)、6,15α-环氧-1β,4β-二羟基桉烷(3)、2-羟基-丁二酸-1-甲酯(4)、巴西红厚壳素(5)和胡萝卜苷(6)。以上化合物均为首次从该植物中分离得到,其中化合物1、2、4和5为首次从米仔兰属植物中分离得到。用滤纸片琼脂扩散法测定了化合物1~5的抗菌活性,结果显示化合物4和5对金黄色葡萄球菌有抑制作用。     

芒果叶化学成分研究Ⅲ

为了解芒果(Mangifera indica L.)的化学成分,从芒果叶70%乙醇提取物中分离鉴定了8个单体化合物,经波谱分析,分别鉴定为:5-(β-D-glucopyranosyloxy)-2-hydroxy benzoic acid methyl ester(1)、methyl salicylate glucoside(2)、对羟基苯甲酸(3)、nikoenoside(4)、(6R,9R)-3-oxo-α-ionol-β-D-glucopyranoside(5)、byzantionoside B(6)、icariside B2(7)和2-ethyl-3-methylmaleimide N-β-D-glucopyranoside(8)。化合物1、2、4~7均为首次从芒果属中分离得到,化合物8首次从该种中分离得到,化合物1的NMR数据是首次报道。     

蝴蝶花的化学成分研究

对鸢尾科鸢尾属植物蝴蝶花全草进行化学成分和生物活性研究。通过正相硅胶、Sephadex LH-20以及反相HPLC柱等等色谱方法对蝴蝶花的化学成分进行分离纯化,应用谱学技术鉴定化合物的结构。从蝴蝶花95%乙醇提取物中分离得到18个化合物,分别鉴定为:(+)-(7S,8R,7'E)-4-hydroxy-3,5'-dimethoxy-4',7-epoxy-8,3'-neolign-7'-ene-9,9'-diol 9'-ethyl ether(1)、丁香脂素(2)、erythro-guaiacylglycerol-β-O-4'-coniferylether(3)、threo-guaiacylglycerol-β-O-4'-coniferylether(4)、4-O-β-d-(6-O-vanilloylglucopyranosyl)vanillic acid(5)、4-[6-O-(4-hydroxy-3,5-dimethoxybenzoyl)-β-d-glucopyranosyloxy]-3-methoxybenzoic acid(6)、藏黄连新苷B(7)、belalloside B(8)、藏黄连新苷A(9)、茶叶花宁(10)、sakuranetin(11)、鼠李柠檬素(12)、鸢尾甲黄素B(13)、染料木素(14)、5,7,4'-三羟基-6,8-二甲氧基异黄酮(15)、野鸢尾苷元(16)、8-羟基鸢尾苷元(17)、3'-O-methylorobol(18)。其中,化合物1~18均为首次从该种植物中分离得到。化合物1、2、5、6、15为首次从该属植物中分离得到。对所分离得到的化合物进行了保肝、抗炎、抗氧化等体外药理活性筛选。     

Recent advances in the study of Kaposi's sarcoma-associated herpesvirus replication and pathogenesis

It has now been over twenty years since a novel herpesviral genome was identified in Kaposi's sarcoma biopsies. Since then, the cumulative research effort by molecular biologists, virologists, clinicians, and epidemiologists alike has led to the extensive characterization of this tumor virus, Kaposi's sarcoma-associated herpesvirus(KSHV; also known as human herpesvirus 8(HHV-8)), and its associated diseases. Here we review the current knowledge of KSHV biology and pathogenesis, with a particular emphasis on new and exciting advances in the field of epigenetics. We also discuss the development and practicality of various cell culture and animal model systems to study KSHV replication and pathogenesis.     

A Unique Protease Cleavage Site Predicted in the Spike Protein of the Novel Pneumonia Coronavirus (2019-nCoV) Potentially Related to Viral Transmissibility

正Dear Editor,In December 2019, a novel human coronavirus caused an epidemic of severe pneumonia(Coronavirus Disease 2019,COVID-19) in Wuhan, Hubei, China(Wu et al. 2020; Zhu et al. 2020). So far, this virus has spread to all areas of China and even to other countries. The epidemic has caused 67,102 confirmed infections with 1526 fatal cases     

Curcuminoids as inhibitors of thioredoxin reductase: A receptor based pharmacophore study with distance mapping of the active site

Curcumin is the yellow pigment of turmeric that interacts irreversibly forming an adduct with thioredoxin reductase (TrxR), an enzyme responsible for redox control of cell and defence against oxidative stress. Docking at both the active sites of TrxR was performed to compare the potency of three naturally occurring curcuminoids, namely curcumin, demethoxy curcumin and bis-demethoxy curcumin. Results show that active sites of TrxR occur at the junction of E and F chains. Volume and area of both cavities is predicted. It has been concluded by distance mapping of the most active conformations that Se atom of catalytic residue SeCYS498, is at a distance of 3.56 from C13 of demethoxy curcumin at the E chain active site, whereas C13 carbon atom forms adduct with Se atom of SeCys 498. We report that at least one methoxy group in curcuminoids is necessary for interation with catalytic residues of thioredoxin. Pharmacophore of both active sites of the TrxR receptor for curcumin and demethoxy curcumin molecules has been drawn and proposed for design and synthesis of most probable potent antiproliferative synthetic drugs.     

Synthesis and antimicrobial studies of hydrazone derivatives of 4-[3-(2,4-difluorophenyl)-4-formyl-1H-pyrazol-1-yl]benzoic acid and 4-[3-(3,4-difluorophenyl)-4-formyl-1H-pyrazol-1-yl]benzoic acid

Microbial resistance to antibiotics is an unresolved global concern, which needs urgent and coordinated action. One of the guidelines of the Centers for Disease Control and Preventions (CDC) to combat antibiotic resistance is the development of new antibiotics to treat drug-resistant bacteria. In our effort to find new antibiotics, we report the synthesis and antimicrobial studies of 30 new pyrazole derivatives. These novel molecules have been synthesized by using readily available starting materials and benign reaction conditions. Some of these molecules have shown activity with MIC values as low as 0.78?µg/mL against four bacterial strains; Staphylococcus aureus, methicillin-resistant S. aureus, Bacillus subtilis, and Acinetobacter baumannii. Furthermore, active molecules are non-toxic to mammalian cell line.

     

Comparative morphology of the carpel in the Liliaceae: Hewardieae, Petrosavieae, and Tricyrteae

The young pistils in the melanthioid tribes, Hewardieae, Petrosavieae and Tricyrteae, are uniformly tricarpellate and syncarpous. They lack raphide idioblasts. All are multiovulate, with bitegmic ovules. The Petrosavieae are marked by the presence of septal glands and incomplete syncarpy. Tepals and stamens adhere to the ovary in the Hewardieae and the Petrosavieae but not in the Tricyrteae. Two vascular bundles occur in the stamens of the Hewartlieae and Tricyrtis latifolia. Ventral bundles in the upper part of the ovary of the Hewardieae are continuous with compound septal bundles and placental bundles in the lower part. Putative ventral bundles occur in the alternate position in the Tricyrteae and putative placental bundles in the opposite. position in the Petrosavieae. The dichtomously branched stigma in each carpel of the Tricyrteae is supplied by a bifurcated dorsal bundle.     

Novel compounds with potent CDK9 inhibitory activity for the treatment of myeloma

Cyclin-dependent kinases (CDKs) and Polo-like kinases (PLKs) play key role in the regulation of the cell cycle. The aim of our study was originally the further development of our recently discovered polo-like kinase 1 (PLK1) inhibitors. A series of new 2,4-disubstituted pyrimidine derivatives were synthesized around the original hit, but their PLK1 inhibitory activity was very poor. However the novel compounds showed nanomolar CDK9 inhibitory activity and very good antiproliferative effect on multiple myeloma cell lines (RPMI-8226).