An unprecedented pair of Z/E isomeric pyridinium compound from the aqueous extract of Aspongopus chinensis Dallas / 药学学报

A novel pair of Z/E isomeric compounds with unprecedented carbon skeleton were isolated from an aqueous extract of Aspongopus chinensis Dallas by macroporous resin, silica gel, and semi-preparative high performance liquid chromatography (HPLC). Their structures were identified by nuclear magnetic resonance (NMR), Infrared spectroscopy (IR), Mass spectroscopy (MS) and other spectroscopic methods as (Z)-3-(but-1″-en-1″-yl)-1-(2ʹ-hydroxyethyl)-4-propylpyridin-1-ium, namely aspongopyridine A, and (E)-3-(but-1″-en-1″-yl)-1-(2ʹ-hydroxyethyl)-4-propylpyridin-1-ium, namely aspongopyridine B, respectively. Besides, the anti-inflammatory, anti-tumor, acetylcholinesterase inhibition and butyrylcholinesterase inhibition activities of the compounds 1 and 2 were evaluated. The results showed that compounds 1 and 2 have no anti-inflammatory, anti-tumor, and butyrylcholinesterase inhibition activities instead of weak acetylcholinesterase inhibition activity.

Green synthesis of gold nanaoparticles using Delphinium Chitralense tuber extracts, their characterization and enzyme inhibitory potential

Abstract Green synthesis has been introduced as an alternative to chemical synthesis due to the serious consequences. Metal nanoparticles synthesized through green approach have different pharmaceutical, medical and agricultural applications. The present study followed a green and simple route for the preparation of potentially bioactive gold nanoparticles (Au NPs). Au NPs were prepared via green synthesis approach using crude basic alkaloidal portion of the tuber of Delphinium chitralense. The green synthesized Au NPs were characterized by transmission electron microscopy (TEM), scanning electron microscopy (SEM), X-ray diffraction (XRD) fourier transform infrared (FTIR), and UV-Visible spectrophotometer. Morphological analysis shows that Au NPs have cubic geometry with different sizes. UV-Vis spectroscopic analysis confirmed the synthesis of Au NPs while XRD proved their pure crystalline phase. The Au NPs showed promising dose dependent inhibition of both AChE and BChE as compared to the crude as well as standard drug.

Resumo A síntese verde foi introduzida como uma alternativa à síntese química devido às graves consequências. As nanopartículas metálicas sintetizadas através da abordagem verde têm diferentes aplicações farmacêuticas, médicas e agrícolas. O presente estudo seguiu uma rota verde e simples para a preparação de nanopartículas de ouro potencialmente bioativas (Au NPs). As NPs de Au foram preparadas via abordagem de síntese verde usando a porção alcaloide básica bruta do tubérculo de Delphinium chitralense. As NPs de Au sintetizadas verdes foram caracterizadas por microscopia eletrônica de transmissão (TEM), microscopia eletrônica de varredura (MEV), difração de raios X (DRX), infravermelho com transformada de Fourier (FTIR) e espectrofotômetro UV-Visível. A análise morfológica mostra que as NPs de Au possuem geometria cúbica com tamanhos diferentes. A análise espectroscópica UV-Vis confirmou a síntese de Au NPs enquanto a XRD provou sua fase cristalina pura. O Au NPs mostrou inibição dependente da dose promissora de AChE e BChE em comparação com a droga bruta e padrão.

Green synthesis of gold nanaoparticles using Delphinium Chitralense tuber extracts, their characterization and enzyme inhibitory potential / Síntese verde de nanaopartículas de ouro utilizando extratos de tubérculos Delphinium chitralense, sua caracterização e potencial inibitório enzimático

Greeen synthesis has been introduced as an alternative to chemical synthesis due to the serious consequences. Metal nanoparticles synthesized through green approach have different pharmaceutical, medical and agricultural applications. The present study followed a green and simple route for the preparation of potentially bioactive gold nanoparticles (Au NPs). Au NPs were prepared via green synthesis approach using crude basic alkaloidal portion of the tuber of Delphinium chitralense. The green synthesized Au NPs were characterized by transmission electron microscopy (TEM), scanning electron microscopy (SEM), X-ray diffraction (XRD) fourier transform infrared (FTIR), and UV-Visible spectrophotometer. Morphological analysis shows that Au NPs have cubic geometry with different sizes. UV-Vis spectroscopic analysis confirmed the synthesis of Au NPs while XRD proved their pure crystalline phase. The Au NPs showed promising dose dependent inhibition of both AChE and BChE as compared to the crude as well as standard drug.

A síntese verde foi introduzida como uma alternativa à síntese química devido às graves consequências. As nanopartículas metálicas sintetizadas através da abordagem verde têm diferentes aplicações farmacêuticas, médicas e agrícolas. O presente estudo seguiu uma rota verde e simples para a preparação de nanopartículas de ouro potencialmente bioativas (Au NPs). As NPs de Au foram preparadas via abordagem de síntese verde usando a porção alcaloide básica bruta do tubérculo de Delphinium chitralense. As NPs de Au sintetizadas verdes foram caracterizadas por microscopia eletrônica de transmissão (TEM), microscopia eletrônica de varredura (MEV), difração de raios X (DRX), infravermelho com transformada de Fourier (FTIR) e espectrofotômetro UV-Visível. A análise morfológica mostra que as NPs de Au possuem geometria cúbica com tamanhos diferentes. A análise espectroscópica UV-Vis confirmou a síntese de Au NPs enquanto a XRD provou sua fase cristalina pura. O Au NPs mostrou inibição dependente da dose promissora de AChE e BChE em comparação com a droga bruta e padrão.

A new lignan glucoside from root of Paeonia lactiflora / 中国中药杂志

A new lignan glucoside,(+)-fragransin A_2-4-O-β-D-glucopyranoside(1), has been isolated from the dry root of Paeonia lactiflora by column chromatography on silica gel, Sephadex LH-20, and MCI-gel resin, as well as preparative RP-HPLC. The structure of the new compound was elucidated by spectroscopic data analysis(MS, UV, IR, CD, 1 D and 2 D NMR) and chemical method. Compound 1 showed moderate inhibition against lipopolysaccharide induced nitric oxide production in RAW264.7 macrophages, with an IC_(50) value of 21.3 μmol·L~(-1).

he potential therapeutic role of Fenugreek saponin against Alzheimer's disease: Evaluation of apoptotic and acetylcholinesterase inhibitory activities.

Alzheimer disease (AD) is known as lacking in the neuro-transmitters within the brain cells due to increase the Acetylcholinesterase (AchE) activity. So, use of AchE inhibitors (AchEI) is believed to be the best way in treatment of Alzheimer. Therefore, the aim of the present work was to evaluate the AchEI and apoptotic activities of fenugreek saponin against AD in vivo. Ninety male aged Sprague Dawley rats were allocated in several experimental groups including untreated animals, supplemented animals with 0.05%, 0.1% and 2% of fenugreek saponin (FS), animals treated with AlCl3 to induce AD, AD-induced animals treated with the previous doses of FS or with Rivastigmine. Brain tissues of different groups were used for determine the AchEI and apoptotic activities as well as generation of reactive oxygen species (ROS), DNA damage and expression of apoptotic related genes (Bax; Bcl2 and caspase-3). The results showed that FS increased the AChEI and apoptosis activities as well as elevated the gene expression levels of Bax; Bcl2 and caspase-3 genes in AD-induced rats. However, FS decreased the ROS generation and DNA damage in AD-induced rats compared with control rats. The results suggested that the ability of fenugreek saponin to inhibit AD due to increase AChE inhibition activity might be attributed to increase the antioxidants in this herb. Moreover, enhancement the apoptosis by fenugreek saponin could be attributed mainly to the regulation process of Bax, Bcl-2 and casapse-3 in the apoptotic pathway and not by generation of ROS in the brain cells of the AD-induced rats.

Synthesis, spectral analysis and pharmacological study of N'- substituted-2-(5-((2,4-dimethylphenoxy)methyl)-1,3,4-oxadiazol-2-ylthio)acetohydrazides

ABSTRACT A series of molecules bearing multiple functional groups were synthesized to study their antibiotic effect against Gram-positive and Gram-negative bacteria and lipoxygenase activity as well. 2,4-Dimethylcarbolic acid (1) was refluxed with ethyl 2-bromoacetate to synthesize ethyl 2-(2,4-dimethylphenoxy)acetate (2). Compound 2 was converted to the corresponding hydrazide 3, again on refluxing with hydrazine. The compound 5-((2,4-dimethylphenoxy)methyl)-1,3,4-oxadiazol-2-thiol (4) was synthesized by the reaction of 3 and CS2 in the presence of KOH. Compound 4 was further converted to the corresponding ester 5 and then 2-(5-((2,4-dimethylphenoxy)methyl)-1,3,4-oxadiazol-2-ylthio)acetohydrazide (6). The final molecules N'-substituted-2-(5-((2,4-dimethylphenoxy)methyl)-1,3,4-oxadiazol-2-ylthio)acetohydrazide, 8a-m, bearing ether, 1,3,4-oxadiazole, thioether, hydrazone and azomethine functional groups were synthesized by stirring the aryl carboxaldehydes 7a-m with 6 in methanol at room temperature. The depicted structures of all synthesized molecules were corroborated by IR, 1H-NMR and EIMS spectral data analysis. 8m and 8i showed substantial antibacterial activity and lipoxygenase inhibitory activity, respectively.

In vitro α-glucosidase inhibition and antioxidant activities of partially purified Antidesma bunius fruit and Gynura nepalensis leaf extracts.

Diabetes mellitus is a metabolic disorder characterized by increased blood glucose levels. Current treatments involve the use of sulfonylureas, α-glucosidase inhibitors, and other synthetic drugs. The study demonstrated the α-glucosidase inhibition and antioxidant properties of partially purified ethanolic extracts of Antidesma bunius fruits and Gynura nepalensis leaves, as possible herbal drug candidates. After ethanol extraction, the extracts were fractionated using normal phase liquid column chromatography, with elution solvents ethyl acetate, methanol and water. Fractionation resulted in five fractions for A. bunius (A1, A2, A3, A4 and A5) and seven fractions for G. nepalensis (G1, G2, G3, G4, G5, G6 and G7). Fraction G1 showed the highest α-glucosidase inhibition activity (90.61±8.05%) and possibly acted via a mixed mode of inhibition. For the antioxidant activities, Fraction A1 exhibited highest radical scavenging activity via DPPH assay (97.39±2.48%), Fraction G7 exhibited highest iron (II)-chelating activity (95.85±1.46%) and Fraction G6 exhibited highest ferric-ion reducing activity via FRAP assay (272.60 μg/mL FeSO4 equivalents). Phytochemical screening revealed that flavonoids and tannins were common among all fractions. The results demonstrated the potential of these plants as an antidiabetic herbal treatment. However, further studies needs to be done, specifically focusing on isolating the active component(s), structure and mechanism elucidation and toxicity assays.

Aldose Reductase Inhibitory Alkaloids from Corydalis ternata

A methanolic extract of Corydalis ternata having aldose reductase inhibitory activity was examined as a possible aldose reductase (ALR2) inhibitor, a key enzyme involved in diabetic complications. Seven alkaloids, tetrahydrocoptisine (1), corydaline (2), tetrahydropalmatine (3), isocorybulbine (4), corybulbine (5), dehydrocorydaline (6), and N-methyltetrahydroberbinium (7) were isolated from CHCl₃ fraction of C. ternata methanol extract. Among them, compounds 1, 5, and 7 exhibited 5.04 ± 1.97%, 5.00 ± 1.26%, and 1.80 ± 2.33% inhibitions, respectively at 40 µM. The activities of the single compounds were not comparable to that of the whole extract, suggesting that the whole combination of each single compound was responsible for the activity of the extract as shown in many cases of natural medicines. Even though this is the second report on aldose reductase inhibition activity of C. ternata, recombinant human aldose reductase was employed in this study unlike in the previous report. Furthermore, the aldose reductase inhibitory activities of isocorybulbine, corybulbine, and N-methyltetrahydroberbinium, to the best of our knowledge, were evaluated for the first time in this study. These results suggest a use of the extract of C. ternata for ameliorating diabetic complications.

NON-POLAR CONSTITUENTS FROM TARAXACUM OFFICINALE WEBER EX WIGG / Монголын эм зүй, эм судлал

The dichloromethane fraction from the ethanol extract of the aerial parts of Taraxacum offi cinale showed a good inhibitory effect on hepatocellular carcinoma cells (HCC). As a result of a series of column chromatographies and usage of nuclear magnetic resonances spectrometric methods and mass spectroscopy 9 known components as taraxasterol (1), taraxasterylacetate (2),pseudotaraxasterol (3), lupeolacetate (4), b-sitosterol (5), b-sitosterylglucopyranose (6), palmitic acid (7), monopalmitin (8) and chrysoerol (9) have been determined. Amongst them palmitic acid, monopalmitin and chrysoeriol have been determined for the fi rst time in the aerial parts of Taraxacum offi cinale. Six compounds as 1, 3, 4, 5, 6 and 7 were tested for their inhibitory activity on HCC and only palmitic acid exhibited more activity against HCC than others, suppressing cell proliferation, migration, adhesion and activated cell apoptosis.Keywords: Triterpenol and sterol derivatives; palmitic acid; hepatocellular carcinoma inhibition activity;IntroductionTaraxacum, commonly called dandelion, is a large genus of fl owering plants in the Asteraceae family. The latin name Taraxacum is from the Greek and means “disease remedy”, while the English name dandelion is originated from the French dent de leon, meaning “lion’s tooth”1. The Mongolian well-recognised name is “baaban beeben”, while in Japan it calls hokouei, respectively. Consequently, Taraxacum is widespread plant throughout the world, in particular, 19 species are found in the Mongolian fl ora2. Generally Taraxacum is considered weedy plant used as a medicinal herb and for food preparation. Traditionally, Taraxacum offi cinale Weber ex Wigg. in Mongolian and Tibetan medicine under the name “khurmong” the root has been used as the composition in a remedy for jaundice and other disorders of the liver and gallbladder, whilethe leaf is used as a diuretic and bitter digestive stimulant. Moreover, fresh dandelion stem latex is used for the warts treatment1,3-6. Taraxacum leaf is included as a medicinal drug in Herbal Pharmacopeia of several European countries. Numerous biological activity tests resulted that Taraxacum possessed an infl ammation modulating activity7-9, diuretic activity comparable to furosemide10, digestive stimulant, appetitive effect and activator for bile fl ow11-12, hypoglycemic activity13 and antitumor activity14. No side effects and carcinogenicity of T. offi cinale extracts and preparations have been noticed. Chemical constituents of T. offi cinale arewell studied. Scientists of different countries reported that whole plant T. offi cinale containedabundance of bitter principles as terpenoids and sterols, bile like terpenes and sterols, various fl avonoids and phenolic acids, large amount of polysaccharides as inulin and fructosans11,15-17.Also, dandelion is a rich in minerals such as iron, potassium and zinc18,19. In this work we are describing activity-guided isolation and the molecular structure elucidation of components from the dichloromethane fraction of the aerial parts of T. offi cinale, from the Mongolian fl ora.

Comparative evaluation of polysaccharides isolated from Astragalus, oyster mushroom, and yacon as inhibitors of α-glucosidase / 中国天然药物

The incidence of diabetes has increased considerably, and become the third serious chronic disease following cancer and cardiovascular diseases. Though acarbose, metformin, and 1-deoxynojirimycin have good efficacy for clinical application as hypoglycemic drugs, their expensive costs and some degree of side effects have limited their clinical application. Recently, increasing attention has concentrated on the polysaccharides from natural plant and animal sources for diabetes. In order to illustrate the pharmaceutical activity of polysaccharides as natural hypoglycemic agents, polysaccharides isolated from Astragalus, oyster mushroom, and Yacon were evaluated for their inhibitory effects on α-glucosidase. Polysaccharides were extracted and purified from Astragalus, Oyster mushroom, and Yacon with hot water at 90 °C for 3 h, respectively. The total sugar content of the polysaccharide was determined by the phenol-sulfuric acid method. The α-glucosidase inhibitory activity was measured by the glucose oxidase method. The results exhibited that the inhibitory effects on α-glucosidase were in decreasing order, Astragalus > oyster mushroom > Yacon. The α-glucosidase inhibition percentage of Astragalus polysaccharide and oyster mushroom polysaccharide were over 40% at the polysaccharide concentration of 0.4 mg·mL(-1). The IC50 of Astragalus polysaccharide and oyster mushroom polysaccharide were 0.28 and 0.424 mg·mL(-1), respectively. The information obtained from this work is beneficial for the use polysaccharides as a dietary supplement for health foods and therapeutics for diabetes.

Isolation of Endophytic Fungus from Plantago Asiatica L. and Its Microbial Inhibition Activity / 世界科学技术-中医药现代化

This study was aimed to explore the resource diversity and microbial inhibition activity of endophytic fungi from medicinal plant Plantago asiatica L. The endophytic fungi were isolated from the root, stem and leaf of the host by tissue inoculation culture and five plant pathogenic fungi and four bacteria strains used as indicating microbes to test microbial inhibition activity by agar plate antagonistic action and modified agar gel diffusion methods. The results indicated that thirteen fungal endophytic strains were isolated from the host. Most of them came from stem, then leaf, and root as the least in number. The isolated strains attribute to five genera, two fam-ilies, and two orders based on morphological characteristics. For the isolated strains, eleven of them were found to have some microbial inhibition activities against one or more indicating fungi, making up 84.6% of the total iso-lates. Six isolated strains had some antimicrobial activities against one or more indicating bacteria, amounting to 46.2% of the total isolates. Three isolated active strains, which are PAEFS001, PAEFS007 and PAEFS008, ex-hibited evident inhibition activities against five kinds of pathogenic fungi used in the trials respectively. The strain of PAEFS001 ascribed to Ozonium sp. Both strains of PAEFS007 and PAEFS008 ascribed to Aspergillus sp. One active strain of PAEFS003 showed evident antibacterial activities to Bacillus subtilis and Staphyloccus aureus, which belonged to Fusidium sp. The endophytic fungi from medicinal plant Plantago asiatica L. have evident an-timicrobial activities. Their inhibition activities against pathogenic fungi have relatively broad spectrum. And their inhibition activities to both Bacillus subtilis and Staphyloccus aureus as G+ are evident and have certain selectivi-ty. It is feasible to find new bioactive compounds associated with endophytic fungi from Plantago asiatica L. Fur-ther research and development of the endophyic fungi will be important for the integrated utilization of the host.

Tyrosinase inhibition activity of Botrytis sp.metabolites a-pyrone / 中国海洋药物

Anti-tyrosinase assay guided isolation of marine-derived fungus Botrytis sp.led to separation of three ?-pyrone compounds.The structures of these compounds were elucidated by various physicochemical analytical methods.The bioactivities of these ?-pyrone derivatives were evaluated in terms of anti-tyrosinase activity.By correlating the bioactivities of these compounds with their structures,it concluded that the ?-pyrone with pentyl group gives highest anti-tyrosinase activity.