新异苯并二氢吡喃醌类抗生素G15—F和G15—G的提取与结构分析

从硫藤黄链轮丝菌Ｇ１５的发酵液中，通过溶媒提取，Ｓｅｐｈａｄｅｘ ＬＨ－２０凝胶柱层析和反相中压柱层析，分离出抗生素Ｇ１５－Ｆ和Ｇ１５－Ｇ。经ＵＶ、ＩＲ、ＭＳ、＾１Ｈ－ＮＭＲ、＾１３Ｃ－ＮＭＲ和ＤＥＰＴ等波谱数据的分析，确定Ｇ１５－Ｆ和Ｇ１５－Ｇ为新的异苯并二氢吡喃酯类抗生素。它们具有抗革兰氏阳性菌和人咽上皮癌ＫＢ细胞的活性。     

产生新的异苯并二氢吡喃醌类抗生素的G15菌株的分类鉴定

Ｇ１５菌株是从我国云南土壤分离的１株放线茵，它产生多种已知抗生素：ｔｈｉｏｌｕ－ｔｉｎ、ａｕｒｅｏｔｈｒｉｃｉｎ、ｍａｚｅｔｈｒａｍｙｃｉｎ、ｍｅｄｅｒｍｙｃｉｎ等和２个新的异苯并二氢吡喃醌类抗生素Ｇ１５－Ｆ和Ｇ１５－Ｇ。按照形态培养、生理生化特征、细胞壁化学组分以及抗生素的研究，Ｇ１５菌株非常近似硫藤黄链轮丝菌ＳｔｒｅｐｔｏｖｅｒｔｉｃｉｌｌｉｕｍｔｈｉｏｌｕｔｅｕｍＯｋａｍｉ１９５２，定名为硫藤黄链轮丝菌Ｇ１５（ＳｔｒｅｐｌｏｖｅｒｌｉｃｉｌｌｕｍｔｈｉｏｌｕｔｅｕｍＧ１５）。     

产生新的异苯并二氢吡喃酯类抗生素的G15菌株的分类鉴定

Ｇ１５菌株是从我国云南土壤分离的１株放线菌。它产生多种已知抗生素：ｔｈｉｏｌｕｔｉｎ、ａｕｒｅｏｔｈｒｉｃｉｎ、ｍａｚｅｔｈｒａｍｙｃｉｎ、ｍｅｄｅｒｍｙｃｉｎ等和２个新的异苯并二氢吡喃醌类抗生素Ｇ１５－Ｆ和Ｇ１５－Ｇ。按照形态培养、生理生化特征、细胞壁化学组分以及抗生素的研究，Ｇ１５菌株非常近似硫藤黄链轮丝菌Ｓｔｒｅｐｔｏｖｅｒｔｉｃｉｌｌｉｕｍ ｔｈｉｏｌｕｔｅｕｍ Ｏｋａｍｉ１９５２，定名为     

苯并二氢吡喃类非甾体雌激素衍生物的合成

在综合考察非甾体雌激素、异丙氧基异黄酮及雷洛昔芬的基础上,设计合成了一系列苯并二氢吡喃类非甾体雌激素衍生物。     

6—甲氨基苯并二氢—γ—吡喃酮的合成工艺改进

以对颈基苯甲醚和丙烯腈为起始原料经加成、水解、环合等３步反应制备６－甲氧基苯并二氢－γ－吡喃酮。工艺简单,产品质量好,成本低。     

7-甲氧基-苯并二氢-γ-吡喃酮的合成工艺研究

对７－甲氧基－苯并二氢－γ－吡喃酮的合成进行了工艺改进,采用间苯二酚为起始原料,经单甲基化、加成、水解、环合等步骤。得到较文献纯度高、收率高的产物,且成本较低。     

苯并二氢吡喃脘衍生物的合成及其初步药理活性

为进一步筛选活性更强、副作用更小的抗绝经后骨质疏松症药物，在综合考察雷洛昔芬和异丙氧基异黄酮的基础上，设计合成一系列苯并二氢吡喃脘化合物，化合物的结构均经波谱鉴定，并通过研究其对幼年小鼠子宫增5重血血碱性磷酸酶活性的影响。初步考察化合物的药理活性，结果表明，XY9902具有较弱的雌激素受体激动作用和一定的雌激素受体拮抗作用。并有助于成骨细胞增殖，对治疗骨质疏松症是有利的。     

苯并二氢吡喃衍生物xy9902对乳腺癌细胞增殖的影响

目的:研究苯并二氢吡喃衍生物xy9902对乳腺癌细胞增殖的影响。方法:采用MTT比色法测定化合物对MCF-7细胞的增殖作用;用流式细胞术测定化合物对细胞周期的影响;用放射性配体结合法考察化合物与雌激素受体(estrogenicreceptor,ER)的亲和力。结果:低浓度的xy9902促进MCF-7细胞增殖并使细胞周期中S期细胞比例增多,高浓度对MCF-7细胞增殖有抑制作用并使S期细胞比例减少;他莫昔芬可阻断xy9902对MCF-7细胞的增殖作用;xy9902对ERα和ERβ的IC50分别为8.45×10-6和1.66×10-6mol·L-1。结论:化合物xy9902低浓度促进MCF-7细胞增殖,高浓度抑制MCF-7细胞增殖,其增殖作用机制与ERα激动有关。     

苯并二氢吡喃腙衍生物的合成及其初步药理活性

为进一步筛选活性更强、副作用更小的抗绝经后骨质疏松症药物 ,在综合考察雷洛昔芬和异丙氧基异黄酮的基础上 ,设计合成一系列苯并二氢吡喃腙化合物 .化合物的结构均经波谱鉴定 ,并通过研究其对幼年小鼠子宫增重和血碱性磷酸酶活性的影响 ,初步考察化合物的药理活性 .结果表明 ,XY990 2具有较弱的雌激素受体激动作用和一定的雌激素受体拮抗作用 ,并有助于成骨细胞增殖 ,对治疗骨质疏松症是有利的 .     

苯并二氢吡喃衍生物的合成及其对骨和血管的初步生物活性

绝经后骨质疏松症的主要治疗手段是雌激素替代疗法 (ＨＲＴ) ,但长期用雌激素可引起子宫内膜和乳腺增生 ,增加发生子宫内膜癌和乳腺癌的危险性[1,2 ] 。异丙氧基异黄酮 (ｉｐｒｉｆｌａｖｏｎｅ)和 1998年初美国上市的选择性雌激素受体调节剂 (ＳＥＲＭｓ)雷洛昔芬 (ｒａｌｏｘｉｆｅｎｅ)可降低雌性激素样活性和致癌危险性 ,实现了雌激素的药理作用分离[3] 。异丙氧基异黄酮有很强的心血管保护作用 ,但其对绝经后骨质疏松症的防治效力不及雷洛昔芬[4 ,5] 。分析对比两种药物结构 :异丙氧基异黄酮较雷洛昔芬的结构简单 ,两者均含有苯并杂环 …     

Isolation,purification, and structural elucidation of polysaccharides from Alhagi-honey

The polysaccharide extract (PE) of Uyghur medicinal preparation Alhagi-honey was prepared by water extraction and alcohol precipitation method. The purified polysaccharide AP1-1 was obtained from PE by macroporous adsorption resin chromatography, DEAE cellulose chromatography, and Sephadex gel chromatography; the homogeneity and the molecular weight of AP1-1 were determined by gel filtration; and the acid hydrolysis, periodate oxidation, Smith degradation, and NMR analysis were used to analyze the chemical structure of AP1-1. The result showed that AP1-1 was a homogeneous polysaccharide, whose relative molecular weight was 9.97 × 10⁴. Through high-performance capillary electrophoresis analysis, we found that its molecular structure was composed of mannose, glucose, galactose, and galacturonic acid with a molar ratio of about 1.1:1.9:3.9:2.1. The main chain of AP1-1 was mainly made up of → 4)β-d-GalpA-(1 → 4)β-d-GalpA-(1 → 4)-β-d-Galp-(1 → 4)-β-d-Galp-(1 → 6)α-d-Glcp-(1 → 4)α-d-Glcp(1 → , while the side chain is composed of → 6)-α-d-Glcp and 2-CH₃-α-d-Man.     

新蒽环类抗生素G0041-3c的理化性质及结构分析

从链霉索G0041-3菌株的发酵液中提取、分离得到5个具有抗肿瘤活性成分．对G0041-3c进行了理化性质测定和各种光谱分析,将其确定为具有蒽环类紫红霉素型结构的新成员。     

Isolation and structural elucidation of new 18-membered macrolide antibiotics, viranamycins A and B.

Two cytotoxic antibiotics, designated viranamycins A and B, were isolated from the culture broth of Streptomyces sp. CH41. Their structures were elucidated as new 18-membered macrolides related to virustomycin A and concanamycin A from NMR spectral analysis. Viranamycins A and B inhibited the growth of P388 mouse leukemia and KB human squamous-cell-carcinoma cells.     

Coumamidines, new broad spectrum antibiotics of the cinodine type. II. Isolation and structural elucidation

Two novel, isomeric compounds, coumamidines gamma 1 and gamma 2, were isolated from fermentations of an actinomycete. The structures were elucidated spectroscopically using 2D NMR correlation experiments and mass spectral data. The coumamidines were found to be close structural relatives of the cinodines (LL-BM123 gamma 1 and gamma 2).     

尼拉霉素新组分98-23的研究——分离、结构鉴别及抗菌活性

从黑暗链霉菌(S．tenebrarius)菌种诱变中得到一变株．其发酵产物系单一组分．经大孔离子交换剂、葡聚糖Sephadex离子交换剂提取精制，制得纯品，经IR、MS、^1H-NMR、^13C-NMR、^1H-^1H COSY、HOHA-HA、HMQC等光谱解析，确定为氨基糖苷类中的新抗生索．化学名为0-3-amino-6-O-(anlinocarbonyl)-3-deoxy-Q-D-glucopyranosyl-(1→6)-0-[2-amino-2．3-dideoxy-n-D-glucopyranosyl-(1→4)]-2-deoxy-D-strep-tamine．并测定了部分菌株的MIC数据以及LD50的范围。     

A new class of potent liver injury protective compounds: Structural elucidation,total synthesis and bioactivity study

A new class of potent liver injury protective compounds,phychetins A-D(1-4) featuring an unique 6/6/5/6/5 pentacyclic framework,were isolated and structurally characterized from a Chinese medicinal plant Phyllanthus franchetianus.Compounds 2-4 are three pairs of enantiomers that were initially obtained in a racemic manner,and were further separated by chiral HPLC preparation.Compounds 1-4 were proposed to be originated biosynthetically from a coexisting lignan via an intramolecular Friedel-Craft...     

Isolation and structure elucidation of new antibiotics related to angolamycin.

Angolamycin (1) and two novel analogues (2 and 3) were isolated from the culture broth of a Streptomyces strain. NMR and MS analysis proved that 2 is the 18-dihydro-, while 3 is the 18-deoxo-18-dihydro derivative of angolamycin. Full experimental assignment of the 1H and the 13C NMR spectra of these compounds was obtained from 1D and 2D chemical shift correlation measurements. Compounds 2 and 3 are less potent antibiotics than angolamycin.     

孕烯醇酮中微量杂质的分离和结构确证

目的:分离和确证孕烯醇酮中所含杂质的结构.方法:采用柱色谱和制备高效液相色谱法进行分离纯化,MS和NMR等光谱方法确证结构,并合成杂质A后进一步确证其结构.结果:从孕烯醇酮中分离出4个杂质,其中杂质A得到结构确证,其它3个有待确证.合成产物的HPLC、NMR等分析结果与该杂质一致.结论:所得杂质A的结构为:3β,20(R)-二羟基-孕甾-5-烯.