STUDIES ON THE CONSTITUENTS OF ARTEMISIA ANNUA L / 药学学报

Six crystalline components were isolated from the lipophilic fraction of Artemisia annua L. They have been identified as four sesquiterpenes, one flavonol and one coumarin. Qinghaosu I and III are new sesquiterpenes. Five main constituents, camphene, iso-artemisia ketone, 1-camphor, β-carophyllene, and β-pinene were identified from the volatile oil of this herb.

Chemical Composition of the Leaf Essential Oils of Croton zambesicus Müll.-Arg. Grown in Lagos, South-West Nigeria.

The chemical composition of the leaf essential oil of Croton zambesicus Müll.-Arg., collected from Agbara-Lagos, Nigeria, was analysed by means of Gas chromatography flame ionization detector (GC-FID) and Gas chromatography coupled with Mass spectrometry (GC-MS). Sixty constituents accounting for 98.9% of the total oil contents were identified from the oil sample. The classes of compounds identified in the oil were monoterpene hydrocarbons (35.3%), oxygenated monoterpenes (22.9%), sesquiterpene hydrocarbons (32.4%) and oxygenated sesquiterpenes (5.6%). The oil was dominated by β-pinene (15.1%), β-caryophyllene (12.6%), germacrene D (10.9%), camphor (7.3%), linalool (7.0%), sabinene (6.4%) and α-pinene (5.2%). Aims: The aim of the research is to investigate the volatile constituents from C. zambesicus harvested in Lagos, Nigeria. Study Design: Extraction of essential oil from the air-dried leaf samples of C. zambesicus and investigation of its chemical constituents. Place and Duration of Study: Leaf samples of C. zambesicus were collected from Agbara, Lagos, on April 2011. Methodology: Air-dried and pulverized leaves were hydrodistilled in a Clevenger-type apparatus to obtained pale yellow volatile oil whose chemical constituents was analyzed by GC and GC/MS. Results: A total of sixty compounds were identified, amounting to 98.9%of the total oil contents. The major were compounds β-pinene (15.1%), β-caryophyllene (12.6%), germacrene D (10.9%) and camphor (7.3%). Variations in compositional pattern were observed between this result and the previous studies. Conclusion: The literature about the C. zambesicus indicates a high variability in the chemical composition of the essential oils.

Chemical composition, antimicrobial, insecticidal, phytotoxic and antioxidant activities of Mediterranean Pinus brutia and Pinus pinea resin essential oils / 中国天然药物

Essential oils of the resins of Pinus brutia and Pinus pinea were evaluated for their biological potential. Essential oils were characterized using GC-MS and GC/FID. in vitro antimicrobial, phytotoxic, antioxidant, and insecticidal activities were carried out using the direct contact and the fumigant assays, respectively. The chemical profile of the essential oils of the resins of P. pinea and P. brutia included mainly α-pinene (21.39% and 25.40%), β-pinene (9.68% and 9.69%), and caryophyllene (9.12% and 4.81%). The essential oils of P. pinea and P. brutia exerted notable antimicrobial activities on Micrococcus luteus and Bacillus subtilis, insecticidal activities on Ephestia kuehniella eggs, phytotoxic activities on Lactuca sativa, Lepidium sativum, and Portulaca oleracea, as well as antioxidant potential. Indications of the biological activities of the essential oils suggest their use in the formulation of ecofriendly and biocompatible pharmaceuticals.

Purification technology of procymidone residues in ginseng extracts by macroporous resins / 中国中药杂志

The macroporous resin separation technology has been mainly applied in the enrichment of saponins, flavonoids, alkaloids and other ingredients, and used in the removal of heavy metal impurities and pesticide residues in recent years. This paper focuses on the synthesis of the new-type macroporous adsorption resin LKS-11 according to the molecular structure characteristics of procymidone. Specifically, the selective absorptive property and other advantages of macroporous resin were utilized to analyze the procymidone removal efficiency in ginseng extracts from different sources. The type of macroporous resins, absorptive property and desorption conditions were observed respectively by static and dynamic adsorption methods to determined the optimum process conditions. According to the results, LKS-11 showed a good absorptive property to procymidone in ginseng extracts and provided a theoretical basis for studies on the removal of procymidone residues from ginseng extracts by using macroporous adsorption resin. Because of no secondary pollution on samples, low production and operation costs, high procymidone removal efficiency and high product recovery rate, this method is suitable to be applied in production.

Simultaneous determination of alpha-pinene, beta-pinene, eucalyptol and alpha-terpineolin in essential oil from Alpinia officinarum Hance by GC / 中国中药杂志

<p><b>OBJECTIVE</b>To establish a method for simultaneous determination of alpha-pinene, beta-pinene, eucalyptol and alpha-terpineolin in essential oil from Alpinia officinarum by GC.</p><p><b>METHOD</b>The essential oil was extracted by steam distillation. The determination was carried on with capillary column DB-1 (0.25 mm x 30 m, 0.25 microm). Temperature programs: 50 degrees C (hold 2 min) programmed to 130 degrees C (hold 3 min) at 8 degrees C x min(-1). The detector was FID. Inlet temperature was 230 degrees C. The detector temperature was 250 degrees C. Carrying gas was nitrogen (1.2 mL x min(-1)), split injection was conducted with split ratio of 10:1. Injection volumn was 1 microL.</p><p><b>RESULT</b>The linear ranges of alpha-pinene, beta-pinene, eucalyptol and alpha-terpineolin were 0.009-0.090 (r = 0.999 8), 0.009-0.091 (r = 0.999 8), 0.060 4-0.604 (r = 0.999 7) and 0.037 4-0.374 g x L(-1) (r = 0.999 5), respectively. The average recoveries (n = 9) of a-pinene, beta-pinene, eucalyptol and alpha-terpineolin were 96.2% (RSD 0.8%) and 96.7% (RSD 1.1%), 98.7% (RSD 1.1%) and 96.7% (RSD 2.2%), respectively.</p><p><b>CONCLUSION</b>The developed method is simple, quick and accurate, which is helpful to control the quality of A. officinarum.</p>

The antiandrogenic effect of dimethachlon and its mechanism / 中华劳动卫生职业病杂志

<p><b>OBJECTIVE</b>To evaluate the antiandrogenic effect of heterocyclic fungicide dimethachlon and its mechanism.</p><p><b>METHODS</b>A combination of in vivo and in vitro assays was selected. Hershberger assay was used to determine the antiandrogenic potential of dimethachlon in vivo. Six-week-old castrated male SD rats were administrated once daily for 7 days with testosterone propionate (TP, 100 micro g/d, sc) plus gavage doses of dimethachlon (50, 100 or 200 mg x kg(-1) x d(-1)), or procymidone (150 or 300 mg x kg(-1) x d(-1), positive control), or iprodione (100 mg x kg(-1) x d(-1), positive control), or flutamide (50 mg x kg(-1) x d(-1), positive control). Transcriptional activation assay in vitro was employed to determine the mechanism of antiandrogenic activity of dimethachlon. Human hepatoma liver cells HepG2 were transiently cotransfected with human androgen receptor (AR) expression plasmid and AR-dependent luciferase report plasmid. Transfected cells were exposed to various concentrations of dimethachlon or flutamide with or without dihydrotestosterone to induce the expression of luciferase gene.</p><p><b>RESULTS</b>In Hershberger assay, dimethachlon, as well as other known antiandrogens, caused decrease in weight of androgen dependent organs or tissues. In 200 mg/kg group, the weight of seminal vesicle, ventral prostate, dorsolateral prostate, Cowper's gland, and levator ani plus bulbocavernosus muscles decreased by 57.8%, 44.8%, 43.9%, 30.1%, and 34.1% respectively, but did not decrease in the vehicle control group. The order of their antiandrogenic potencies was: flutamide > procymidone > dimethachlon > iprodione. In transcriptional activation assay, dimethachlon could inhibit dihydrotestosterone-dependent AR activity in transfected HepG2 cells in dose-effect relationship. The inhibiting potency of dimethachlon was about 1/100 of that of flutamide.</p><p><b>CONCLUSION</b>Dimethachlon has antiandrogenic effect, and acts as an AR antagonist. Its antiandrogenic potency is lower than flutamide and procymidone, but higher than iprodione.</p>

Study on quality analysis of essential oil from twig and leaf of Baeckea frutescens / 中国中药杂志

<p><b>OBJECTIVE</b>To provide scientific methods for quality criterion by studying the chemical components of essential oil from Baeckea frutescens.</p><p><b>METHOD</b>The chemical components of essential oil from B. frutescens were identified by GC-MS-DS, TLC and capillary GC. The relative contents of main components were determined by area normalization.</p><p><b>RESULT</b>More than 50 peaks were separated, and 38 components were identified, which accounted for over 94% of the total GC peaks areas of the essential oil. The methods for quality evaluation of essential oil from B. frutescens by TLC and capillary GC were established.</p><p><b>CONCLUSION</b>The chemical components of essential oil from B. frutescens collected from different habitats and collecting periods have common characteristics as well as differences. Some components, such as linalool, can be used as a standard and chromatography fingerprint to analyze the quality of essential oil from B. frutescens.</p>

Antidepressant activity of hyperforin conjugates of the St. John's wort, Hypericum perforatum Linn.: an experimental study.

Nine extracts of H. perforatum, containing hyperforin in conjugated forms, but devoid of free hyperforin and adhyperforin, were subjected to antidepressant screening using the forced swim test (FST). The observed activity was compared with that of SJW extracts containing hyperforin and adhyperforin (in free form). Results indicate that hyperforin conjugates exhibit significant antidepressant activity as evidenced by the reduced immobility period in the FST in rats.

Important amino acid residues of potato plant uncoupling protein (StUCP)

Chemical modifications were used to identify some of the functionally important amino acid residues of the potato plant uncoupling protein (StUCP). The proton-dependent swelling of potato mitochondria in K+-acetate in the presence of linoleic acid and valinomycin was inhibited by mersalyl (Ki = 5 æM) and other hydrophilic SH reagents such as Thiolyte MB, iodoacetate and 5,5'-dithio-bis-(2-nitrobenzoate), but not by hydrophobic N-ethylmaleimide. This pattern of inhibition by SH reagents was similar to that of brown adipose tissue uncoupling protein (UCP1). As with UCP1, the arginine reagent 2,3-butadione, but not N-ethylmaleimide or other hydrophobic SH reagents, prevented the inhibition of StUCP-mediated transport by ATP in isolated potato mitochondria or with reconstituted StUCP. The results indicate that the most reactive amino acid residues in UCP1 and StUCP are similar, with the exception of N-ethylmaleimide-reactive cysteines in the purine nucleotide-binding site

A synergistic aggregation pheromone component in the banana weevil cosmopolites sordidus germar 1824 (Coleoptera: Curculionidae)

Cosmopolites sordidus is an important pest on banana plantations worldwide. The chemistry of the aggregation pheromone of this insect has been recently resolved and here we present the first evidence from field trails that sordidin, a compound from the male releases aggregation pheromone, attracts significant number of weevils only if host plant odors are also present. Sordidin attracts few insects when it is presented without the host plant tissue. However, the attractiveness of host plant tissue increases more than tenfold when it is presented simultaneously with sordidin in field traps. We confirm experimentally that sordidin may be used as part of a system for mass trapping and monitoring this insect.

Synthesis of some diazabicyclic compounds of expected non narcotic analgetic activity

The biologically active 4H-pyrido [1, 2-a] pyrimidin-4-ones [1] including some hexahydro derivatives [2] are non acidic non-steroidal anti-inflammatory agents. Other pyrido [1, 2-a] pyrimidines were reported as analgetic anti-inflammatory agents [3-8]. In a search of analgetic pharmacophore in condensed pyrimidines, the chemistry and analgetic activity of the bioisoster pyrimido-[1, 2-a] azepine [9] 1 was reported. This work found that ester, carbamate, thiosemicarbazide, semicarbazide, urea and acyl urea groups are of special value in the analgetic activity of 1. On the other h and, it was assumed that any changes in the structure of 1, that might add to its analgetic effect, would be beneficial

Conformational Equilibria in 1, 3-Azabicyclic Systems

La comparación de los parámetros de RMN'H para la perhidro-oxazolo (3,4-a) piridina (Jgem-2.5 Hz, delta4.40,3.81 ) con los 6-etilderivados 7 y 8, muestra la existencia de un equilibrio conformacional entre los conformadores trans-fusionado y el O-interno del cis-fusionado. La espectroscopia de RMN a bajas temperaturas permitió observar señales para ambos conformadores; y la integración de estas señales indican un equilibrio existente a 18ºK entre el 73 por ciento de 3-t y el 27 por ciento de 3-c

Actividad hipoglucemiante en ratas machos de derivados del ácido biciclo (3,1,0) hexano-6-carboxílico / Hypoglycemic activity in male rats of bicyclo (3,1,0) hexane-6-carboxylic acid derivatives

Se determinó la glucemia después de la administración subcutánea de glucosa a ratas machos adultas en varios tiempos. Se evaluó el efecto hipoglucemiante conocido del clorhidrato de feniletilbiguanida (FEB) después de su administración oral, y este compuesto sirvió como referencia. Se probaron seis nuevos compuestos sintetizados por los autores, relacionados con el ácido biciclo (3, 1, 0) hexano-6-hexo-carboxílico (ABCH). Se comprobó la actividad hipoglicemiante conocida del ABCH). Los seis nuevos compuestos conservaron la configuración exo y todos mostraron actividad hipoglucemiante oral en tiempos variables