Protective effect of α-asarone and β-asarone on Aβ -induced inflammatory response in PC12 cells and its / 浙江大学学报·医学版

To investigate effects of α-asarone and β-asarone on induced PC12 cell injury and related mechanisms. Aβ toxic injury cell model was induced by Aβ in PC12 cells. PC12 cells were divided into blank control group, model control group, α-asarone group (0.5, 1.0, β-asarone group (6.3, 12.5, vasoactive intestinal peptide (VIP) group, and VIP antagonist control group. Cell survival rate was detected by CCK-8 kit; cell apoptosis rate was detected by flow cytometry. The levels of inflammatory cytokines interleukin (IL)-1, , tumor necrosis factor (TNF)-α, oxidation-related inducible nitric oxide synthase (iNOS), nitric oxide (NO), apoptosis factors caspase-3 and p53 were detected by ELISA method. The expressions of C-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinase (p38MAPK) were detected by Western blotting. Compared with model control group, cell survival rates of group, β-asarone group and VIP group increased; the cell apoptosis rate decreased; levels of apoptosis-related factors caspase-3, p53, inflammatory factors IL-1, TNF-α decreased; IL-10 level increased; levels of oxidization-related factors iNOS and NO decreased; the expression of JNK and p38MAPK protein decreased (all 0.05). α-asarone and β-asarone have protective effects on PC12 cell injury induced by Aβ. β-asarone may inhibit inflammatory factors and oxidation-related factors through promoting VIP secretion, regulating JNK/MAPK pathway, and reducing PC12 cell apoptosis; however, the effect of α-asarone may be not related to VIP secretion.

Preparation and in vitro quality evaluation of self-microemulsion co-loaded with tenuifolin and β-asarone / 中国中药杂志

To prepare and optimize the self-microemulsion co-loaded with tenuifolin and β-asarone(TF/ASA-SMEDDS) and evaluate its quality. The prescription compositions of TF/ASA-SMEDDS were screened by solubility test, single factor test and pseudo-tern-ary phase diagram, and the prescriptions were further optimized by Box-Behnken response surface method, with the drug loading and particle size as the evaluation indexes. Then the optimized TF/ASA-SMEDDS was evaluated for emulsified appearance, particle size, morphology and drug release in vitro. The optimized prescription for TF/ASA-SMEDDS was as follows: caprylic citrate triglyceride polyoxyethylene castor oil-glycerol(10.8∶39.2∶50), drug loading of(5.563±0.065) mg·g~(-1) for tenuifolin and(5.526±0.022) mg·g~(-1) for β-asarone; uniform and transparent pan-blue nanoemulsion can be formed after emulsification, with particle size of(28.84±0.44) nm. TEM showed that TF/ASA-SMEDDS can form spherical droplets with a uniform particle size after emulsification; In vitro release test results showed that the drug release rate and cumulative release of tenuifolin and β-asarone were significantly improved. The preparation process of TF/ASA-SMEDDS was simple and can effectively improve in vitro release of tenuifolin and β-asarone.

Chemical characterization of the essential oil from leaves of basil genotypes cultivated in different seasons / Caracterización química del aceite esencial de hojas genotipos de albahaca cultivados en diferentes estaciones del año

The aim of this study was to evaluate the concentration and chemical composition of the essential oil the leaves of basil cultivars and hybrids cultivated in different cropping seasons: dry season and rainy season. The variables evaluated were the content and composition of essential oils in the two seasons. The essential oil content ranged from 0.66% to 3.21% in the dry season and from 0.80% to 4.20% in the rainy season. The major compounds found among the genotypes were linalool, methyl chavicol, neral, geranial, eugenol, and methyl (E)- cinnamate, defining the formation of five groups in each season, classified in the following chemotypes: methyl chavicol (Group 1), citral (neral+geranial) (Group 2), methyl cinnamate (Group 3), linalool (Group 4), and intermediate linalool (Group 5). All the traits evaluated had heritability (h ) greater than 95% and high CVg/CVe ratio values. The cropping season affected the content and chemical compositions of basil essential oil.

El objetivo de este estudio fue evaluar la concentración y composición química del aceite esencial las hojas de cultivares de albahaca e híbridos cultivados en diferentes temporadas de cultivo: estación seca y estación lluviosa. Las variables evaluadas fueron la contenido y la composición de los aceites esenciales en las dos estaciones. La contenido de aceite esencial varió de 0.66% a 3.21% en la estación seca y de 0.80% a 4.20% en la estación lluviosa. Los principales compuestos encontrados entre los genotipos fueron linalool, metilchavicol, neral, geranial, eugenol y metil (E)-cinamato, definiendo la formación de cinco grupos en cada estación, clasificados en los siguientes quimiotipos: metil chavicol (Grupo 1), citral (neral + geranial) (Grupo 2), cinamato de metilo (Grupo 3), linalool (Grupo 4) y linalol intermedio (Grupo 5). Todos los rasgos evaluados mostraron una heredabilidad (h ) mayor que el 95% y altos valores de relación CVg/CVe. La temporada de cultivo afectó la contenido y las composiciones químicas del aceite esencial de albahaca.

Anethole reduces oxidative stress and improves in vitro survival and activation of primordial follicles

Primordial follicles, the main source of oocytes in the ovary, are essential for the maintenance of fertility throughout the reproductive lifespan. To the best of our knowledge, there are no reports describing the effect of anethole on this important ovarian follicle population. The aim of the study was to investigate the effect of different anethole concentrations on the in vitro culture of caprine preantral follicles enclosed in ovarian tissue. Randomized ovarian fragments were fixed immediately (non-cultured treatment) or distributed into five treatments: α-MEM+ (cultured control), α-MEM+ supplemented with ascorbic acid at 50 μg/mL (AA), and anethole at 30 (AN30), 300 (AN300), or 2000 µg/mL (AN2000), for 1 or 7 days. After 7 days of culture, a significantly higher percentage of morphologically normal follicles was observed when anethole at 2000 μg/mL was used. For both culture times, a greater percentage of growing follicles was observed with the AN30 treatment compared to AA and AN2000 treatments. Anethole at 30 and 2000 µg/mL concentrations at days 1 and 7 of culture resulted in significantly larger follicular diameter than in the cultured control treatment. Anethole at 30 µg/mL concentration at day 7 showed significantly greater oocyte diameter than the other treatments, except when compared to the AN2000 treatment. At day 7 of culture, levels of reactive oxygen species (ROS) were significantly lower in the AN30 treatment than the other treatments. In conclusion, supplementation of culture medium with anethole improves survival and early follicle development at different concentrations in the caprine species.

Study of embryo toxicity and the teratogenicity of 2, 4-dinitroanisole in rats / 中华劳动卫生职业病杂志

<p><b>OBJECTIVE</b>To detect the embryo toxicity and the teratogenicity of DNAN in rats and provide basic data to occupational protection.</p><p><b>METHODS</b>120 adult female SD rats and 60 male rats are mating for 1: 1, and the pregnant rats were randomly divided into five groups by the pregnant time. The negative control group are gavaged with 4% starch, and the three experiment groups are gavaged with DNAN suspension with the dose of 5 mg/kg, 15 mg/kg and 45 mg/kg respectively, while the positive control give aspirin of 280 mg/kg. All rats of the five groups are administrated gavage from gestation day 5 (GD5) to GD19 continuously. The rats are dislocated in GD20, and the toxicity of embryo and toetus are detected.</p><p><b>RESULTS</b>The net weight growth in all three dose group are less than that of negative group, while the dead foetus in high dose group is more than negative group. Moreover, the body weight, body lenghth, tail lenghth and the anal genital distance of foetus rats in high dose group are all less than that of negative group. The foetus external malformations of three dose groups appear no significant compared with negative group.However, the prevalences of skeleton malformation in high dose group and the internal organs malformation in the median and high dose group appear significant higher than that of negative group. There are significantly maternal reproductive toxicity, embryo toxicity and toetus toxicity in positive group.</p><p><b>CONCLUSION</b>DNAN can induced maternal reproductive toxicity, embryo toxicity and the teratogenicity to rats.</p>

Vernakalant en la reversión de la fibrilación auricular de reciente comienzo / Vernakalant for the conversion of atrial fibrillation of recent onset

La fibrilación auricular (FA) es la arritmia sostenida más frecuente. La cardioversión es uno de los tratamientos de primera elección para la finalización de la FA de reciente comienzo, especialmente la farmacológica, ya que tiene la ventaja de no utilizar sedación. El vernakalant es un antiarrítmico que actúa selectivamente sobre la aurícula, inhibiendo las corrientes de potasio, con mínimo bloqueo de la corriente ventricular IKr. Este antiarrítmico ha sido aprobado recientemente por la Unión Europea para la cardioversión farmacológica de la FA de reciente comienzo. El objetivo de esta revisión es analizar las características farmacocinéticas y farmacodinámicas del vernakalant, y demostrar la seguridad y eficacia del mismo para la conversión de la FA a ritmo sinusal.

Atrial fibrillation (AF) is the most common sustained arrhythmia. Cardioversion is considered one of the best treatments for recent onset AF, especially with drugs for avoiding sedation. Vernakalant is a novel antiarrhythmic that acts selectively in the atrium, and inhibits potassium currents, with minor blockade of IKr currents in the ventricle. It has been recently approved for pharmacological cardioversion of recent-onset AF in the European Union. The aim of this review is to analyze the pharmacokinetic and pharmacodynamic of vernakalant, and to show the efficacy and safety of this drug for the conversion of AF to sinus rhythm.

The effective parts of liangxue tongyu prescription on cooling-blood and activating-blood and analysis of chemical constituents by HPLC-MS and GC-MS / 药学学报

In order to clarify material basis of effective parts of liangxue tongyu prescription, blood-heat and blood-stasis rat model induced by dry yeast was established. The changes of rectal temperature, blood viscosity and plasma viscosity were used to evaluate the cooling-blood and activating-blood effects of liangxue tongyu prescription and its parts. Compared with the model group, the extract from liangxue tongyu prescription, its volatile oil and n-butanol part could significantly reduce rectal temperature (P<0.01), and also reduce blood viscosity and plasma viscosity to various degrees (P<0.01 or P<0.05). So volatile oil and n-butanol part were primarily identified as effective parts of liangxue tongyu prescription. By using GC-MS with normalization method of area to analyze volatile oil of liangxue tongyu prescription, 70 compounds were identified, accounting for about 92.54%, mainly as β-asarone, paeonol, α-asarone and shyobunone. 42 compounds such as peony glycosides, tannins, and iridoid glycosides were identified by HPLC-MS techniques and standard comparison. The study determined the effective parts of liangxue tongyu prescription and clarified the chemical composition providing the foundation for further studies on material basis of liangxue tongyu prescription.

Preparation and release behaviour of mPEG-PLA α-asarone nanoparticles designed for nasal administration / 中国中药杂志

Taking α-asarone as model drug, mono methoxy polyethylene glycol-polylactic acid copolymer (mPEG-PLA) as the drug carrier material to prepare drug-loading nanoparticles by premix membrane emulsification for nasal administration. The prepared nanoparticles were spherical with smooth surface and average particle size of 360 nm. Polydispersity index (PDI) was 0. 030, average drug loading of (11.5 ± 0.045) % (n = 3), and the encapsulation efficiency of (86.34 ± 0.11) % (n = 3). X-ray diffraction and differential scanning calorimetry results showed that, α-asarone existed in mPEG-PLA carrier in amorphous or molecular state, different from simple physical mixture. In the in vitro release test in simulated human nasal cavity, α-asarone apis can be released quickly at close to 94% at 102 h, in line with the first-order kinetics (R² = 0.981 9). mPEG-PLA drug-loading nanoparticles release only 54%, with slow release effect, in line with Riger-Peppas model (R² = 0.967 9, n = 0.630 2), for non-fick diffusion, released by the spread of drugs and skeleton dissolution dual control. This provided the foundation for nasal drug delivery in vivo pharmacokinetic study.

Pharmacokinetic study on dry powder inhalation administration of α-asarone in rats / 中国中药杂志

To study the pharmacokinetic characteristics and absolute bioavailability of α-asarone through dry powder inhalation in rats, and compare with that through oral administration and intravenous injection. A HPLC method was established for the determination of α-asarone in rat plasma to detect the changes in plasma concentrations of α-asarone through dry powder inhalation (20 mg · kg(-1)), oral administration (80 mg · kg(-1)) and intravenous injection (20 mg · kg(-1)) in rats. DAS 2.0 software was used to calculate the pharmacokinetic parameters. The absolute bioavailability of α-asarone was calculated according to AUC(0-t)) of administration routes and administration doses. According to the results, α-asarone showed good linear relations (r = 0. 999 4) at concentrations between 0.282-14.1 mg · L(-1), with the limit of detection (LOD) at 0.212 mg · L(-1). Through dry powder inhalation, oral administration and intravenous injection of α-asarone, the metabolic processes of α-asarone in rats conformed to one, two and three compartment models respectively, with the elimination half-life of (95.48 ± 48.28), (64.34 ± 27.59), (66.99 ± 29.76) min. According to the bioavailability formula, the absolute bioavailability of α-asarone through dry powder inhalation and oral administration were 78.32% and 33. 60%, respectively. This study showed that significant increase in elimination half-life and absolute bioavailability of α-asarone through dry powder inhalation, which lays a theoretical foundation for preparing α-asarone dry powder inhalers.

Actividad acaricida del aceite esencial de la corteza de Croton malambo H. Karst, metil-eugenol y metil-isoeugenol contra Dermatophagoides farinae Hughes, 1961 / Acaricide activity of essential oil of Croton malambo H. Karst, methyl-eugenol and methyl-isoeugenol against Dermatophagoides farinae Hughes, 1961

Dermotophagoides farinae lives in the indoor environment of houses, where it is source of allergens; therefore its control is a priority in preventing respiratory allergies. The aim of this study was to evaluate the acaricidal activity of essential oil of Croton malambo H. Karst bark and their components methyl-eugenol and methyl-isoeugenol against Dermatophagoides farinae. The essential oil was obtained through hydro-distillation assisted by microwave radiation and analyzed by GC-MS. Acaricidal activity was assessed by dose- response bioassay, at different times, using benzyl benzoate as a positive control. The relative amount of methyl-eugenol and methyl- isoeugenol in the essential oil was 68.4 percent and 4.9 percent, respectively. The acaricidal activity was: essential oil > methyl-eugenol > benzyl benzoate > methyl-isoeugenol. The acaricidal properties of essential oil of Croton malambo bark and methyl-eugenol against Dermatophagoides farinae were established...

Dermatophagoides farinae habita en el interior de las casas, donde es fuente importante de alérgenos, por tanto su control es una prioridad en la prevención de alergias respiratoria. El objetivo de este estudio fue evaluar la actividad acaricida del aceite esencial de la corteza de Croton malambo H. Karst y sus componentes metil-eugenol y metil-isoeugenol contra Dermatophagoides farinae. El aceite esencial se obtuvo por hidrodestilación asistida por radiación de microondas y se analizó por CG-EM. La actividad acaricida se evaluó mediante bioensayo de dosis-respuesta a diferentes tiempos, usando benzoato de bencilo como control. La cantidad relativa de metil-eugenol y metil-isoeugenol en el aceite fue 68.4 por ciento y 4.9 por ciento, respectivamente. La actividad acaricida fue: aceite esencial > metil-eugenol > benzoato de bencilo > metil-isoeugenol. Se establecieron las propiedades acaricidas del aceite esencial de la corteza de Croton malambo y metil-eugenol contra Dermatophagoides farinae...

Circadian variation of essential oil from Piper marginatum Jacq / Variaciones circadiana de aceite esencial de Piper marginatum Jacq

The composition of the essential oil from the leaves of Piper marginatum (Piperaceae) shows circadian variation and a higher yield during high solar incidence. The essential oils samples were investigated by GC-FID and GC-MS, which allowed identification of 29 compounds. Principal component analysis (PCA) and cluster analysis (CA) showed a significant quantitative variability in the chemical composition of the studied samples as well as a correlation between the oil profiles and the collection time. Two main groups were observed, with predominance of phenylpropanoids or sesquiterpenes. The predominant chemical compounds were phenylpropanoids, having as main representative (Z)-asarone and (E)-asarone.

La composición del aceite esencial de hojas de Piper marginatum (Piperaceae) muestra una variación circadiana y un mayor rendimiento durante la mayor incidencia solar. Las muestras de aceites esenciales se investigaron por GC-FID y GC-MS, lo que permitió la identificación de 29 compuestos. El análisis de componentes principales y el análisis de conglomerados mostraron una variación cuantitativa significativa en la composición química de las muestras estudiadas, así como una correlación entre los perfiles del aceite esencial y el tiempo de recolección. Se observaron dos grupos principales, con predominio de fenilpropanoides o sesquiterpenos. Los compuestos predominantes fueron los fenilpropanoides, (Z)-asarona y (E)-asarona.

Componentes volátiles de las hojas de Pimenta racemosa var racemosa(Mill. ) JW Moore (Myrtaceae) de Táchira – Venezuela / Volatile compounds of Pimenta racemosa var racemosa (Mill. ) JW Moore (Myrtaceae) leaves from Táchira-Venezuela

Pimenta racemosa var. racemosa (Mill.) J.W. Moore, is a Caribbean arboreal plant belonging to the family Myrtaceae with a special interest in their leaves for the production of essential oil, commonly known as "Bay-Rum". Steam distillation of fresh leaves collected in April 2012 produced two types of essential oil, one of these resulted lighter than water and was named (AL) and the other one heavier than water (AP). Gas chromatography/mass spectrometry analysis showed the presence of 17 components constituting 99.9 percent for AL, being the major compounds: eugenol (60.4 percent), myrcene (11.7 percent), chavicol (6.0 percent), limonene (5.4 percent) and linalool (4.4 percent); for the AP, 13components were identified (98.3 percent) from which eugenol (82.9 percent) and chavicol (9.3 percent) were in major proportions.

Pimenta racemosa var. racemosa (Mill.) J.W. Moore, es una planta caribeña, arbórea, perteneciente a la familia Myrtaceae y con un especial interés en sus hojas para la producción del aceite esencial comúnmente conocido como “Bay-Rum”. La destilación por arrastrecon vapor de las hojas frescas colectadas en abril 2012 produjo dos tipos de aceites esenciales, uno ligero (AL) y otro más pesado que elagua (AP). El análisis de sus componentes volátiles por cromatografía de gases/espectrometría de masas mostró 17 componentes lo que constituye el 99,9 por ciento del AL de los cuales los mayoritarios fueron eugenol (60,4 por ciento), mirceno (11,7 por ciento), chavicol (6,0 por ciento), limoneno (5,4 por ciento) ylinalool (4,4 por ciento); para el AP, 13 componentes fueron identificados (98,3 por ciento) de los cuales eugenol (82,9 por ciento) y chavicol (9,3 por ciento) fueron los mayoritarios.

Quality evaluation and stability investigation of asarone submicro emulsion injection / 中国中药杂志

The content of the asarone submicro emulsion injection was determind by HPLC method, and thereby a quality evaluation method was established based on indexes of pH value, particle size, peroxide value, methoxy aniline values, free fatty acid, lysophosphatidylcholine, visible foreign substances, insoluble particle, sterility, bacterial endotoxin and impurities, etc. The results showed that the injection exhibited uniform physical appearance and all the products were in milkwhite liquid. The content of the three batches products were respectively 102.9%, 100.8%, 97.70% of the labeled amount, with mean particle size of 210-250 nm, and other indexes all met with the standards. The reserved samples showed no obvious change in terms of detection indexes and indicated good stability after the accelerated stability test and long-term stability for 12 months. The quality evaluation method established in this study could be applied to quality control and stability investigation of asarone submicron emulsion injection, which laid a basis for further clinical research and application.

Chemical constituents of Dalbergia odorifera / 中国中药杂志

Fourteen compounds were isolated from Dalbergia odoriferae and purified by repeated column chromatography on silica and sephadex LH-20 gel and structurally identified by spectral analysis. These compounds were identified as 4, 9-dimethoxy-3-hydroxypterocarpan (1), medicarpin (2), 2', 4', 5-trihydroxy-7-methoxyisoflavone (3), 2', 3', 7-trihydroxy-4'-methoxyisoflavan (4), formononetin (5), 3, 8-dihydroxy-9-methoxypterocarpan (6), koparin (7), 3-hydroxy-9-methoxypterocarp-6a-ene (8), 2'-hydroxyformononetin (9), stevenin (10), 2', 7-dihydroxy-4', 5'-dimethoxyisoflavone (11), lyoniresinol (12), 2, 4-dihydroxy-5-methoxy-benzophenone (13) and neokhriol A (14). Compounds 1, 3, 4, 6, 8, 12 and 14 were isolated from this plant for the first time. Antibacterial activity assay showed that compound 4 had inhibitory effect on Ralstonia solanacearum.

Analytical method and comparison for static and dynamic headspace gas chromatography of anisole in water / 中华预防医学杂志

<p><b>OBJECTIVE</b>To establish and compare the method of static headspace gas chromatography hydrogen flame detector (static headspace method) and purge and trap gas chromatography-mass spectrometry (dynamic headspace method) of anisole in water.</p><p><b>METHODS</b>Nitrogen gas was used as carrier gas in the static headspace method, 5 g NaCl as matrix modifier was added into 10 ml water. The sample was balanced with high speed vibration at 75°C for 30 min, and anisole was detected by gas chromatography and quantified with external standard. Helium was used as carrier gas in dynamic headspace method, 5.0 ml water and 0.004 mg/L internal standard fluorobenzene was purged into the purge and trap apparatus. After purging, trapping and desorption, anisole was detected by the gas chromatography-mass spectrograph, confirmed by the retention time and comparison of mass-spectrogram in spectrum library and quantified with internal standard. The repeatability and sensitivity of assay were evaluated.</p><p><b>RESULTS</b>A good linear range for anisole was observed in static headspace gas chromatography and dynamic headspace gas chromatography-mass spectrometry, within the range of 10 - 500 µg/L and 0.5 - 60.0 µg/L respectively. The linear regression equation was Y = 782.150X + 1.3446 and Y = 0.0358X - 0.0209 respectively, both the correlation coefficient ≥ 0.999. The detection limit (LOD) were 0.002 µg/L and 0.110 µg/L, the lower limit of quantitation (LOQ) were 0.006 µg/L and 0.350 µg/L, the relative standard deviation (RSD) were 1.8% - 2.3% and 2.0% - 3.4%, and the spiking recovery were 93% - 101% and 96% - 101% respectively.</p><p><b>CONCLUSION</b>The methods of static headspace gas chromatography and dynamic headspace gas chromatography-mass spectrometry are simple and can measure anisole in water quickly, sensitively and accurately.</p>

Gene expression and activity of phenyl alanine amonia-lyase and essential oil composition of Ocimum basilicum L at different growth stages

Phenylalanine amonia-lyase [PAL] is one of the most important enzymes that plays a key role in regulation of phenylpropanoid production in plants. It catalyzes the first step of the phenylpropanoid pathway in which L-phenylalanine is deaminated to trans-cinnamic acid. This step is significant for metabolic engineering and hyper-expression of the major phenylpropanoid, methyl chavicol. We followed gene expression and activity of PAL in Ocimum basilicum L. at different stages of growth including seedling, beginning and middle of growth phase, budding stage and flowering, and their correlation with final concentration of phenylpropanoid compounds. The level of gene expression was monitored by semi quantitative RT-PCR and phenylpropanoid compounds were identified by gas chromatography/mass spectrometry [GC/MS]. PAL activity was assayed using spectrophotometer. The results indicated that the level of gene expression and activity of PAL enzyme are altered during the plant development, where the highest expression and activity [0.851 [micromol cinnamic acid/mg/min] was achieved at budding stage. In this experiment, changes of methylchavicol content were correlated to the transcription and activity of PAL enzyme

Design, synthesis and evaluation of tacrine-methoxybenzene hybrids as cholinesterases inhibitors / 药学学报

A series of tacrine-methoxybenzene hybrids (5a-5i) were designed, synthesized and evaluated as inhibitors of cholinesterases (ChEs). All the compounds had better ChEs inhibitory activities than tacrine with IC50 values at the nanomolar range. Compound 5h exhibited the strongest inhibition on acetylcholinesterase (AChE) with an IC50 value of 6.74 nmol x L(-1) and compound 5f showed the most potent inhibition on butyrylcholinesterase with IC50 value of 3.83 nmol x L(-1). Kinetic and molecular modeling studies showed that these hybrids targeted both the catalytic active site and the peripheral anionic site of AChE.

Study on relationship of properties and drug release rate of hot melt pressure sensitive adhesive / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the relationship of properties and drug release rate of hot melt pressure sensitive adhesive (HMPSA), and to provide a recommendation of preparing and selecting of HMPSA for transdermal use.</p><p><b>METHOD</b>HMPSA with different properties were prepared using styrene-isoprene-styrene triblock copolymer as main material, and the tacks, adhesions and cohesions were determined. Drug-in-adhesive type patches were prepared using alpha-asarone as model drug, and the drug release rates were investigated on single chamber diffusion cells using 60% ethanol solution as release media.</p><p><b>RESULT</b>The prepared HMPSAs had different tacks, adhesions and cohesions. The drug release rates of HMPSA patches were related to the cohesions. The release rate decreased when the cohesion increased.</p><p><b>CONCLUSION</b>The HMPSA with appropriate cohesion should be selected when preparing patches to balance the drug release rate and patch property.</p>

Study on chemical constituents from leaves of Tripterygium wilfordii / 中国中药杂志

In order to study the chemical constituents of the leaves of Tripterygium wilfordii and provide references for the bio-active study, we isolated nine compounds from the dried leaves of Tripterygium wilfordii. Their structures were determined by application of spectroscopic (NMR, MS) and chemical methods. These compounds were isolated and identified as (+)-lyoniresinol (1), (+)-isolariciresinol (2), burselignan (3), dibutyl phthalate (4), cyclo-(S-Pro-R-Phe) (5), cyclo-(S-Pro-R-Leu) (6), cyclo-(S-Pro-S-Ile) (7), 3-hydroxy-1-(4-hydroxy-3,5-dimethoxyphenyl)-1-propanone (8) and daucosterol (9). Compounds 1-3, 5-8 were isolated from this plant for the first time.

Research on liposoluble ingredients of Quchiling / 中国中药杂志

<p><b>OBJECTIVE</b>To study the liposoluble ingredients of Quchiling (LQ), which enter the blood and the brain,and to confirm the active ingredients of LQ in vivo.</p><p><b>METHOD</b>Serum pharmacochemistry and gas chromatography mass spectroscopy were used to analyze ingredients of LQ entering the blood and the brain.</p><p><b>RESULT</b>There were eleven ingredients of LQ to enter the blood and six ingredients of LQ to enter the brain.</p><p><b>CONCLUSION</b>It is confirmed that eleven ingredients of LQ entered the blood, which are beta-asarone, schisandrol A, schisandrol B, deoxyschisandrin, schisandrin B, schisantherrin A, schisantherrin B, schisantherrin C, delta-cadinene, delta-cadinol and calamendiol in the blood, and that six ingredients are beta-asarone, schisandrol A, schisandrol B, deoxyschisandrin, schisandrin B and calamendiol in the brain.</p>