十个甾体皂甙元的~(13)C NMR谱

本文报道心不甘(Tupistra aurantiaca Wall et Backer)的十个甾体皂甙元:△~5一系列的3-epiruscogenin(1),3-epi-ruscogenin(2),tupisgenin(3)和aurantigenin(4),5-β-系列的ranmogenin A(5)、B(6)、C(7)、D(8)、△~(25(27))—pentrogenin(9)和1β、2β、3β、4β、5β、7α-hexahydroxy-spirost-25(27)-en-6-one(10)的~(13)C NMR的归属和解析的研究结果。     

滇产植物皂素成分的研究——Ⅸ.心不甘中甾体皂甙元的分离和结构鉴定(1)

心不甘系百合科植物橙花开口箭(Tupistra aurantiaca Wall et Backer),云南民间用其根治疗胃痛等。心不甘根的粗甙盐酸水解后、总甙元经硅胶柱层析先后得到六个甙元(A→F)。甙元A和B经红外、质谱及核磁共振氢谱鉴定分别为已知的3-epiruscogenin(1)和3-epi-neoruscogenin(2)。甙元C(tupisgenin)和甙元D(aurantigenin)为新化合物,它们的化学结构经红外、质谱、核磁共振氢谱和~(13)C核磁共振谱鉴定分别推定为(20s、22s、25s)-22,25-epoxy-5-furosten-1β、3α、26-triol(3)和(25s)-spirost-5-en-1β、3α、25-triol(4)。     

开口箭根茎中甾体化合物的研究

从开口箭根茎部位共分离得到9个甾体化合物,经波谱数据分析结合文献对照分别鉴定为3-epi-neoruscogenin-3-β-D-glucopyranoside(1),3-epi-ruscogenin-3-β-D-glucopyranoside(2),ranmogenin A(3),convallagenin B(4),3-epi-neoruscogenin(5),tupichigenin E(6),(20S,22R)-spirost-25(27)-ene-1β,2β,3β,4β,5β,7α-hexaol-6-one(7),β-谷甾醇(8)和胡萝卜苷(9)。其中化合物1、2和4为首次从该植物中分离得到。     

滇黄芩甙A和B的结构

从龙胆科滇黄芩属植物滇黄芩(Veratrilla baillonii Franch)中分离得到两个新的酮二糖甙,经~1H NMR,~(13)C NMR,FAB-MS,MS,2D NMR,UV,IR等物理方法和化学反应,推定为:2,3,4,7-四甲氧基酮-1-O-β-D-葡萄糖(6←1)-β-D-木糖甙(1)和7-羟基-2,3,4-三甲氧基酮-1-O-β-D-葡萄糖(6←1)-β-D-木糖甙(2),分别命名为:滇黄芩甙A和滇黄芩甙B。     

开口箭甾体皂甙元的分离鉴定及其抗荔枝霜疫霉菌活性

在以荔枝霜疫霉菌为指示菌的生物活性测定导向跟踪下,运用TLC、硅胶柱层析、反相硅胶柱层析和凝胶柱层析等分离纯化方法,从开口箭(Tupistra chinensis)甲醇提取物的乙酸乙酯分部萃取物中分离纯化得到2个抗菌化合物。经现代光谱(MS、IR、1D NMR和2D NMR)分析,确定化合物1为1β,2β,3β,4β,5β,7α-六羟基螺甾-25(27)-烯-6-酮,化合物2为螺甾-25(27)-烯-1β,2β,3β,4β,5β,6β,7α-七醇。离体抗菌活性测定化合物1和化合物2抑制荔枝霜疫霉菌(Peronophythora litchii)孢子囊萌发的EC50分别为100.28 mg.mL-1和124.37 mg.mL-1。用质量浓度为500 mg.mL-1的两个化合物分别处理后接种霜疫霉菌,供试荔枝果实的发病率分别为16.7%和18.9%。     

草珊瑚化学成分的研究

采用硅胶、SephadexLH-20、MCI等方法从草珊瑚(Sarcandra glabra)全草乙酸乙酯萃取部位分离得到10个化合物,经波谱学方法鉴定为Chlorajapolide C(1),Shizukanolide H(2),Chloranthalactone E(3),Istanbulin B(4),Istanbulin A(5),4-Hydroxy-4,7-dimethyl-1-tetralone(6),4α,7α-Epoxyguaiane-10α,11-diol(7),(+)-Hydroxydihydroneocurueol(8),3β-Hydroxystigmast-5-en-7-one(9),3β-Hydroxystigmast-5,22-dien-7-one(10)。其中6~10这5个化合物均为首次从该科植物中得到,1、2为首次从该植物中得到。     

心不甘中甾体皂甙元的分离和结构鉴定(3)

本文报告心不甘(Tupistra aurantiaca Wall et Backer)根的粗甙经盐酸水解后的总甙元中分离的甙元E和F的结构鉴定。甙元F经鉴定为△~(25(27))-pentrogenin(2)。甙元E(ranmo-genin D)为新化合物,其结构经IR、MS、~1H NMR和~(13)C NMR谱分析推定如(1)所示。     

茂汶淫羊藿化学成分的研究

从小檗科植物茂汶淫羊藿 (EpimediumplatyetalumK .Meyer)的地上部分首次分离得到 5种化合物 (1- 5 ) ,经化学和波谱法 (UV、IR、NMR和FAB_MS)鉴定 ,其中两种为新化合物 ,命名为茂藿甙A (3,5_dihydroxy_4′_methoxy_8_(3″_hydroxyisopentyl)_flavone_7_O_β_D_glucopyranoside ,1)和茂藿甙B (5_hydroxy_4′_methoxy_8_prenyl_flavone_3_O_β_D_glu copyranosyl(1→ 4 )_O_α_L_rhamnopyranosyl_7_O_β_D_glucopyranoside ,2 ) ,另三种为淫羊藿甙 (3)、宝藿甙_Ⅰ (4)和胡萝卜甙 (5 )。     

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。     

知母中甾体皂苷类成分的研究(英文)

从中药知母(Anemarrhena asphodeloides Bge.)的70%乙醇提取物中分离得到6个化合物,经波谱学方法和与已知样品对照鉴定为:3-O-β-D-glucopyranosyl-(1→2)-β-D-galactopyranosyl-(3β,5β)-pregn-16(17)-ene-20-one(1)、timosaponin AIII(2)、timosaponin BIII(3)、22-hydroxy-5β-furost-3β,15α-diol-3-O-β-D-glucopyranosyl(1→2)-β-D-galactopyranoside(4)、timosaponin G(5)、β-daucosterol(6)。其中化合物1为新天然产物,命名为知母孕甾A,是知母中首次发现的C21甾体类化合物,经HR ESI-MS、1D NMR、2D NMR确定其结构,并首次对其核磁数据进行归属。     

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).