Polysaccharides of Saponin-Bearing Plants. XV. Structure of Glucoarabinogalactan from Acantophyllum Borszczowii Roots

The structure of the branched polysaccharide glucoarabinogalactan was investigated by periodate oxidation, methylation, and ¹³C NMR spectroscopy. The main chain consists of -16-bonded galactopyranoses. 12-Bonded D-glucopyranoses and 13-bonded D-galactopyranoses are located on the unreducing ends. There is a short side chain with -13-bonded L-arabinopyranoses.     

Water-Soluble Polysaccharides from Narcissus poeticus and Their Biological Activity

A homogeneous native acetylated glucomannan of molecular weight 32000 was isolated from bulbs of N. poeticus. A linear chain polymer consisting of -14-bound D-manno- and D-glucopyranoses was found using periodate and chromic oxidation and methylation. The glucomannan has low toxicity and exhibits distinct hypolipidemic activity.     

N－异丙基－O－芳基－O＇－半乳吡喃基硫代磷酰胺酯的合成、结构及生物活性

报道了新型Ｎ－异丙基－Ｏ－芳基Ｏ＇－半乳吡喃糖基硫代磷酰胺酯的合成，并对有关反应进行了讨论．通过重结晶分离得到了化合物Ｎ－异丙基－Ｏ－（对－氯苯基）－Ｏ＇－半乳吡喃糖基硫代磷酰胺酯的纯异构体，单晶Ｘ射线衍射分析结果表明，此纯异构体分子中手性磷原子的构型为Ｒ。初步测定了这类化合物的除草活性及抗病活性。     

N-异丙基-O-芳基-O'-半乳吡喃基硫代磷酰胺酯的合成、结构及生物活性

报道了新型N-异丙基-O-芳基O''-半乳吡喃糖基硫代磷酰胺酯的合成,并对有关反应进行了讨论。通过重结晶分离得到了化合物N-异丙基-O-(对-氯苯基)-O''-半乳吡喃糖基硫代磷酰胺酯的纯异构体,单晶X射线衍射分析结果表明,此纯异构体分子中手性磷原子的构型为R.初步测定了这类化合物的除草活性及抗病活性。     

Plant Polyprenols and Their Biological Activity

Research on the isolation, identification, and biological activity of plant polyprenols is reviewed.     

汉防己甲素衍生物的合成及其生物活性

为寻找更为有效的抗肿瘤药物,改善汉防己甲素的抗肿瘤活性,本文以汉防己甲素为原料,经过Suzuki反应设计并合成了6个新的双苄基异喹啉类衍生物。新化合物经过质谱(MS)、核磁共振氢谱(~1H NMR)、核磁共振碳谱(~(13)C NMR)等技术手段进行了结构确证。采用细胞计数试剂盒(CCK-8)法初步评价了6个新化合物对人肺癌细胞(A549)和小鼠白血病细胞(P388)的抗肿瘤活性。结果表明,化合物均有不同程度的抗肿瘤活性,其中化合物H1、H4、H6对A549细胞的抗肿瘤活性(IC5010μmol/L)明显优于阳性对照汉防己甲素。     

Synthesis of Lactosylated Piperazinyl Porphyrins and Their Biological Activity

The aim of this work is to synthesize of a new family of lactosylated piperazinly porphyrins, in which the galactoside piperazine moieties are linked to the tetra‐ and mono‐phenyl rings of tetraphenylporphyrin (TPP). 5,10,15,20‐Tetrakis[4‐(4‐lactobionylpiperazin‐1‐yl)phenyl]porphyrin (TLPP) and 5‐mono[4‐(4‐lactobionylpiperazin‐1‐yl)phenyl]‐10,15,20‐triphenylporphyrin (MLPP) have been synthesized. A detailed ¹H NMR study gave their complete structural elucidation. The UV‐Visible, mass spectra and elemental analysis are also presented. The biological activity on cancer cells and the pharmacokinetics have also been evaluated, showing a better biological activity, a very high liver to skin ratio and short retention time in tissues. It was suggested that such novel lactosylated piperazinly porphyrins, as potential hepatocyte‐selective targeting drugs, exhibit a promising activity in photodynamic therapy (PDT).     

Photochemical Reactivity of Naphthol-Naphthalimide Conjugates and Their Biological Activity

Quinone methide precursors 1a–e, with different alkyl linkers between the naphthol and the naphthalimide chromophore, were synthesized. Their photophysical properties and photochemical reactivity were investigated and connected with biological activity. Upon excitation of the naphthol, Förster resonance energy transfer (FRET) to the naphthalimide takes place and the quantum yields of fluorescence are low (Φ_F ≈ 10⁻²). Due to FRET, photodehydration of naphthols to QMs takes place inefficiently (Φ_R ≈ 10⁻⁵). However, the formation of QMs can also be initiated upon excitation of naphthalimide, the lower energy chromophore, in a process that involves photoinduced electron transfer (PET) from the naphthol to the naphthalimide. Fluorescence titrations revealed that 1a and 1e form complexes with ct-DNA with moderate association constants K_a ≈ 10⁵–10⁶ M⁻¹, as well as with bovine serum albumin (BSA) K_a ≈ 10⁵ M⁻¹ (1:1 complex). The irradiation of the complex 1e@BSA resulted in the alkylation of the protein, probably via QM. The antiproliferative activity of 1a–e against two human cancer cell lines (H460 and MCF 7) was investigated with the cells kept in the dark or irradiated at 350 nm, whereupon cytotoxicity increased, particularly for 1e (>100 times). Although the enhancement of this activity upon UV irradiation has no imminent therapeutic application, the results presented have importance in the rational design of new generations of anticancer phototherapeutics that absorb visible light.     

不对称1,3,2—二氧磷杂环己烷非对映选择性合成及其生物活性

不对称１，３，２－二氧磷杂环己烷非对映选择性合成及其生物活性邵瑞链＊杨敏华成俊然（南开大学元素有机化学研究所，元素有机化学国家重点实验室天津３０００７１）关键词二氧磷杂环，立体有择合成，顺反异构体，生物活性１９９７－０６－０４收稿，１９９７－１２－０...     

含嘧啶环的新拟除虫菊酯的合成及其生物活性的研究

拟除虫菊酯是一类高效、低毒、广谱性杀虫剂。嘧啶环是生物分子和医药中有较好活性的基团。本文拟在菊酯分子中引入嘧啶杂环,并测试其生物活性。我们以β-二酮为起始原料,分别与尿素、甲酰胺和脒缩合关环形成嘧啶,并进一步合成含嘧啶环的新拟除虫菊酯。所合成化合物的生物试验表明其中一些化合物对家蝇具有较好的击倒效应和杀虫效能。     

Biological Activity of Essential Oils of Four Juniper Species and Their Potential as Biopesticides

The objective of this study was to assess the biological activity of essential oils (EOs) of four Juniperus species obtained via two different distillation methods and their potential as biopesticides. The studied factors were juniper species (Juniperus communis L., J. oxycedrus L., J. pygmaea C. Koch., and J. sibirica Burgsd), plant sex (male (M) and female (F)), and distillation method (hydrodistillation via a standard Clevenger apparatus (ClevA) and semi-commercial (SCom) steam distillation). The hypothesis was that the EO will have differential antioxidant, antimicrobial, and insecticidal activities as a function of plant species, plant sex, and distillation method. The two distillation methods resulted in similar EO composition within a given species. However, there were differences in the EO content (yield) due to the sex of the plant, and also differences in the proportions of some EO components. The concentration of α-pinene, β-caryophyllene, δ-cadinene and δ-cadinol was dissimilar between the EO of M and F plants within all four species. Additionally, M and F plants of J. pygmaea, and J. sibirica had significantly different concentrations of sabinene within the respective species. The EOs obtained via ClevA extraction showed higher antioxidant capacity within a species compared with those from SCom extraction. All of the tested EOs had significant repellent and insecticidal activity against the two aphid species Rhopalosiphum padi (bird cherry-oat aphid) and Sitobion avenae (English grain aphid) at concentrations of the EO in the solution of 1%, 2.5%, and 5%. The tested EOs demonstrated moderate activity against selected pathogens Fusarium spp., Botrytis cinerea, Colletotrichum spp., Rhizoctonia solani and Cylindrocarpon pauciseptatum. The results demonstrate that the standard ClevA would provide comparable EO content and composition in comparison with SCom steam distillation; however, even slight differences in the EO composition may translate into differential bioactivity.     

新型含噻二唑环磺酰脲的合成及其生物活性的研究

新型含噻二唑环磺酰脲的合成及其生物活性的研究杨新玲,陈馥衡（北京农业大学应用化学系,北京,１０００９４）关键词噻二唑,磺酰脲,合成,生物活性磺酰脲是７０年代末出现的一类新型超高效除草剂［１］,它以极低的用量和良好的环境安全性而引起世人注目。２－氨基－...     

One Pot Synthesis of Some New Heteroylselenoglycolic Acids and Their Biological Activity

Abstract

A convenient one pot three-stage synthesis was used for obtaining new heteroylselenoglycolic and di-heteroylselenoglycolic acids by nucleophilic substitution reaction of the starting compounds pyridineselenol, pyridazineselenol, and quinolineselenol with α-chloro- or α,α-dichloroacetic acids for 1-h stirring. The newly synthesized compounds were screened biologically for anti-microbial and anti-oxidant activities. The structure of all new compounds was confirmed by ¹H NMR, ¹³C NMR, Mass, and IR spectroscopy and elemental analyses.     

Polysaccharides of saponin-bearing plants XI. An investigation of the polysaccharides ofAcanthophyllum knorringianum

Polysaccharides have been isolated from the epigeal organs and roots ofAcanthophyllum knorringianum and their quantitative levels and qualitative compositions have been established. A neutral polysaccharide of the epigeal organs belongs to the mannoarabinoglucogalactan type, and a neutral polysaccharide from the roots, to the arabinoglucogalactans.Institute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, Tashkent, fax (371) 120 64 75. Translated from Khimiya Prirodnykh Soedinenii, No. 2, pp. 169–170, March–April, 1999.     

含取代嘧啶环的苯磺酰脲的合成和生物活性测定

报道了１２种含不同取代嘧啶环的苯磺酰脲的合成及初步的生物活性测定结果，其中１０种为新化合物，结构经＾１ＨＮＭＲ，ＩＲ和元素分析等证实。     

Polysaccharides of Saponin-Bearing Plants. XIV. Structural Study of Glucoarabinogalactan from Acanthophyllum pungens Roots

The structure of the polysaccharide glucoarabinogalactan, which is a branched polysaccharide, was established by chemical and spectral methods. Its main chain consists of -16-bound galactopyranose units. Galactopyranose atoms C-2 and C-3 act as branching points. The side chains contain galactopyranose, glucopyranose, and chains of -(13)-bound arabinopyranose units. The linear structures of three galactooligosaccharides were identified and proved by partial acid hydrolysis.