Mosquitocidal activities of Chenopodium botrys whole plant n-hexane extract against Culex quinquefasciatus / Atividades mosquitocidas do extrato de n-hexano de planta inteira de Chenopodium botrys contra Culex quinquefasciatus

This research aimed to investigate various mosquitocidal activities of Chenopodium botrys whole- plant n-hexane extract against Culex quinquefasciatus. The extract showed remarkable larvicidal, pupicidal, adulticidal, oviposition deterrent and adult emergence inhibitory activities against Cx. quinquefasciatus. During the larvicidal and pupicidal activities, the 24-hour lethal concentration (LC50) of extract against 2nd instar larvae, 4th instar larvae and pupae were 324.6, 495.6 and 950.8 ppm, respectively. During the CDC (Centers for Disease Control and Prevention) bottle bioassay for adulticidal activity, the median knockdown times (KDT50) at 1.25% concentration was 123.4 minutes. During the filter paper impregnation bioassay for adulticidal activity, the KDT50 value at 0.138 mg/cm2 concentration was 48.6 minutes. The extract was fractionated into 14 fractions through silica gel column chromatography which were then combined into six fractions on the basis of similar retention factor (Rf) value. These fractions were screened for adulticidal activity by applying CDC bottle bioassay. The fraction obtained through 60:40 to 50:50% n-hexanes-chloroform mobile phase with 0.5 Rf value showed 100% adulticidal activity at 0.2% concentration. During oviposition deterrent activity, the highest concentration (1000 ppm) showed 71.3 ± 4.4% effective repellence and 0.6 ± 0.1 oviposition activity index. During adult emergence inhibition activity, the median emergence inhibition (EI50) value was 312.3 ppm. From the outcome of the present investigation, it is concluded that the n-hexane extract of C. botrys whole- plant possesses strong larvicidal, pupicidal, adulticidal, oviposition deterrent and adult emergence inhibitory activities against Cx. quinquefasciatus.

Esta pesquisa teve como objetivo investigar várias atividades mosquitocidas do extrato n-hexano de planta inteira de Chenopodium botrys contra Culex quinquefasciatus. O extrato mostrou atividades larvicida, pupicida, adulticida, dissuasora de oviposição e inibidora da emergência de adultos contra a Cx. quinquefasciatus. Durante as atividades larvicida e pupicida, a concentração letal de 24 horas (CL50) do extrato contra larvas de 2º estádio, larvas de 4º estádio e pupa foi de 324,6, 495,6 e 950,8 ppm, respectivamente. Durante o bioensaio com frasco do CDC (Centros para Controle e Prevenção de Doenças) para adulticida, o tempo médio de desativação (KDT50) na concentração de 1,25% foi de 123,4 minutos. Durante o bioensaio de impregnação com papel de filtro para a atividade adulticida do extrato, o valor KDT50 na concentração de 0,138 mg / cm2 foi de 48,6 minutos. O extrato foi fracionado em 14 frações através de cromatografia em coluna de gel de sílica que foram então combinadas em seis frações com base em um valor de fator de retenção (Rf) semelhante. Essas frações foram selecionadas quanto à atividade adulticida por meio da aplicação do bioensaio com garrafa do CDC. A fração obtida através da fase móvel de n-hexanos-clorofórmio 60:40% a 50:50% com valor de 0,5 Rf apresentou atividade adulticida de 100% na concentração de 0,2%. Durante a atividade de dissuasão da oviposição, a maior concentração de extrato (1000 ppm) apresentou repelência efetiva de 71,3 ± 4,4% e índice de atividade de oviposição de 0,6 ± 0,1. Durante a atividade de inibição da emergência de adultos, o valor médio de inibição da emergência (EI50) foi de 312,3 ppm. A partir do resultado da presente investigação, conclui-se que o extrato de n-hexano da planta inteira de C. botrys possui fortes atividades larvicida, pupicida, adulticida, dissuasora da oviposição e inibidora da emergência de adultos contra a Cx. quinquefasciatus.

Mosquitocidal activities of Chenopodium botrys whole plant n-hexane extract against Culex quinquefasciatus

Abstract This research aimed to investigate various mosquitocidal activities of Chenopodium botrys whole- plant n-hexane extract against Culex quinquefasciatus. The extract showed remarkable larvicidal, pupicidal, adulticidal, oviposition deterrent and adult emergence inhibitory activities against Cx. quinquefasciatus. During the larvicidal and pupicidal activities, the 24-hour lethal concentration (LC50) of extract against 2nd instar larvae, 4th instar larvae and pupae were 324.6, 495.6 and 950.8 ppm, respectively. During the CDC (Centers for Disease Control and Prevention) bottle bioassay for adulticidal activity, the median knockdown times (KDT50) at 1.25% concentration was 123.4 minutes. During the filter paper impregnation bioassay for adulticidal activity, the KDT50 value at 0.138 mg/cm2 concentration was 48.6 minutes. The extract was fractionated into 14 fractions through silica gel column chromatography which were then combined into six fractions on the basis of similar retention factor (Rf) value. These fractions were screened for adulticidal activity by applying CDC bottle bioassay. The fraction obtained through 60:40 to 50:50% n-hexanes-chloroform mobile phase with 0.5 Rf value showed 100% adulticidal activity at 0.2% concentration. During oviposition deterrent activity, the highest concentration (1000 ppm) showed 71.3 ± 4.4% effective repellence and 0.6 ± 0.1 oviposition activity index. During adult emergence inhibition activity, the median emergence inhibition (EI50) value was 312.3 ppm. From the outcome of the present investigation, it is concluded that the n-hexane extract of C. botrys whole- plant possesses strong larvicidal, pupicidal, adulticidal, oviposition deterrent and adult emergence inhibitory activities against Cx. quinquefasciatus.

Resumo Esta pesquisa teve como objetivo investigar várias atividades mosquitocidas do extrato n-hexano de planta inteira de Chenopodium botrys contra Culex quinquefasciatus. O extrato mostrou atividades larvicida, pupicida, adulticida, dissuasora de oviposição e inibidora da emergência de adultos contra a Cx. quinquefasciatus. Durante as atividades larvicida e pupicida, a concentração letal de 24 horas (CL50) do extrato contra larvas de 2º estádio, larvas de 4º estádio e pupa foi de 324,6, 495,6 e 950,8 ppm, respectivamente. Durante o bioensaio com frasco do CDC (Centros para Controle e Prevenção de Doenças) para adulticida, o tempo médio de desativação (KDT50) na concentração de 1,25% foi de 123,4 minutos. Durante o bioensaio de impregnação com papel de filtro para a atividade adulticida do extrato, o valor KDT50 na concentração de 0,138 mg / cm2 foi de 48,6 minutos. O extrato foi fracionado em 14 frações através de cromatografia em coluna de gel de sílica que foram então combinadas em seis frações com base em um valor de fator de retenção (Rf) semelhante. Essas frações foram selecionadas quanto à atividade adulticida por meio da aplicação do bioensaio com garrafa do CDC. A fração obtida através da fase móvel de n-hexanos-clorofórmio 60:40% a 50:50% com valor de 0,5 Rf apresentou atividade adulticida de 100% na concentração de 0,2%. Durante a atividade de dissuasão da oviposição, a maior concentração de extrato (1000 ppm) apresentou repelência efetiva de 71,3 ± 4,4% e índice de atividade de oviposição de 0,6 ± 0,1. Durante a atividade de inibição da emergência de adultos, o valor médio de inibição da emergência (EI50) foi de 312,3 ppm. A partir do resultado da presente investigação, conclui-se que o extrato de n-hexano da planta inteira de C. botrys possui fortes atividades larvicida, pupicida, adulticida, dissuasora da oviposição e inibidora da emergência de adultos contra a Cx. quinquefasciatus.

Mosquitocidal activities of Chenopodium botrys whole plant n-hexane extract against Culex quinquefasciatus / Atividades mosquitocidas do extrato de n-hexano de planta inteira de Chenopodium botrys contra Culex quinquefasciatus

Abstract This research aimed to investigate various mosquitocidal activities of Chenopodium botrys whole- plant n-hexane extract against Culex quinquefasciatus. The extract showed remarkable larvicidal, pupicidal, adulticidal, oviposition deterrent and adult emergence inhibitory activities against Cx. quinquefasciatus. During the larvicidal and pupicidal activities, the 24-hour lethal concentration (LC50) of extract against 2nd instar larvae, 4th instar larvae and pupae were 324.6, 495.6 and 950.8 ppm, respectively. During the CDC (Centers for Disease Control and Prevention) bottle bioassay for adulticidal activity, the median knockdown times (KDT50) at 1.25% concentration was 123.4 minutes. During the filter paper impregnation bioassay for adulticidal activity, the KDT50 value at 0.138 mg/cm2 concentration was 48.6 minutes. The extract was fractionated into 14 fractions through silica gel column chromatography which were then combined into six fractions on the basis of similar retention factor (Rf) value. These fractions were screened for adulticidal activity by applying CDC bottle bioassay. The fraction obtained through 60:40 to 50:50% n-hexanes-chloroform mobile phase with 0.5 Rf value showed 100% adulticidal activity at 0.2% concentration. During oviposition deterrent activity, the highest concentration (1000 ppm) showed 71.3 ± 4.4% effective repellence and 0.6 ± 0.1 oviposition activity index. During adult emergence inhibition activity, the median emergence inhibition (EI50) value was 312.3 ppm. From the outcome of the present investigation, it is concluded that the n-hexane extract of C. botrys whole- plant possesses strong larvicidal, pupicidal, adulticidal, oviposition deterrent and adult emergence inhibitory activities against Cx. quinquefasciatus.

Resumo Esta pesquisa teve como objetivo investigar várias atividades mosquitocidas do extrato n-hexano de planta inteira de Chenopodium botrys contra Culex quinquefasciatus. O extrato mostrou atividades larvicida, pupicida, adulticida, dissuasora de oviposição e inibidora da emergência de adultos contra a Cx. quinquefasciatus. Durante as atividades larvicida e pupicida, a concentração letal de 24 horas (CL50) do extrato contra larvas de 2º estádio, larvas de 4º estádio e pupa foi de 324,6, 495,6 e 950,8 ppm, respectivamente. Durante o bioensaio com frasco do CDC (Centros para Controle e Prevenção de Doenças) para adulticida, o tempo médio de desativação (KDT50) na concentração de 1,25% foi de 123,4 minutos. Durante o bioensaio de impregnação com papel de filtro para a atividade adulticida do extrato, o valor KDT50 na concentração de 0,138 mg / cm2 foi de 48,6 minutos. O extrato foi fracionado em 14 frações através de cromatografia em coluna de gel de sílica que foram então combinadas em seis frações com base em um valor de fator de retenção (Rf) semelhante. Essas frações foram selecionadas quanto à atividade adulticida por meio da aplicação do bioensaio com garrafa do CDC. A fração obtida através da fase móvel de n-hexanos-clorofórmio 60:40% a 50:50% com valor de 0,5 Rf apresentou atividade adulticida de 100% na concentração de 0,2%. Durante a atividade de dissuasão da oviposição, a maior concentração de extrato (1000 ppm) apresentou repelência efetiva de 71,3 ± 4,4% e índice de atividade de oviposição de 0,6 ± 0,1. Durante a atividade de inibição da emergência de adultos, o valor médio de inibição da emergência (EI50) foi de 312,3 ppm. A partir do resultado da presente investigação, conclui-se que o extrato de n-hexano da planta inteira de C. botrys possui fortes atividades larvicida, pupicida, adulticida, dissuasora da oviposição e inibidora da emergência de adultos contra a Cx. quinquefasciatus.

Analysis on Chemical Constituents and Dynamic Accumulation of Main Components in Arctium lappa Leaves / 中国实验方剂学杂志

ObjectiveTo determine the chemical constituents of burdock （Arctium lappa） leaves， and elucidate dynamic accumulation rule of four main components， in order to provide the basis for determining the suitable harvest time of burdock leaves. MethodSilica gel， macroporous resin， Sephadex LH-20， octadecylsilane chemically bonded silica （ODS）， microporous resin （MCI） column chromatography and reversed-phase preparative high performance liquid chromatography （HPLC） were used to isolate the main chemical constituents in burdock leaves. Their chemical structures were elucidated by spectroscopic techniques. HPLC-diode array detector （DAD） was used to analyze the dynamic accumulation of four components in burdock leaf. HPLC-DAD was performed on a Shim-pack GIST C18 column （4.6 mm×250 mm， 5 μm） with mobile phase of acetonitrile （A）-0.3% phosphoric acid aqueous solution （B） （0-9 min， 13%A； 9-10 min， 13%-24%A； 10-30 min， 24%A）， flow rate of 1.0 mL·min-1， column temperature of 40 ℃， and detection wavelength at 328 nm. ResultSeventeen compounds were isolated from burdock leaves， and identified as caffeic acid （1）， rutin （2）， kaempferol-3-O-rutinoside （3）， quercetin-3-O-β-D-glucopyranoside （4）， kaempferol-3-O-β-D-glucopyranoside （5）， chlorogenic acid （6）， isochlorogenic acid A （7）， daucosterol （8）， ursolic acid （9）， anemarrhenoside B （10）， （-）-secoisolariciresinol （11）， vladinol D （12）， melitensin （13）， esculetin （14）， 1-（-2-ethylphenyl）-1，2-ethanediol （15）， 1-（-4-ethylphenyl）-1，2-ethanediol （16）， 3-hydroxy-1-（4-hydroxy-3，5-dimethoxyphenyl）-1-propanone （17）. The contents of chlorogenic acid， rutin and kaempferol-3-O-rutinoside in burdock leaves showed an upward trend from April to August， and reached the highest in August. And the content of isochlorogenic acid A firstly increased and then decreased from April to August， and reached the highest in July. ConclusionCompounds 10， 12-17 were isolated from Arctium for the first time. Taking the contents of chlorogenic acid， rutin， kaempferol-3-O-rutinoside， and isochlorogenic acid A as indicators， considering the comprehensive development and utilization of burdock roots and leaves， it is recommended to harvest burdock leaves in mid-August.

Investigation of Adsorption and Desorption Properties of Total Ginsenosides on Anion-exchange Resins and Its LC-MS Analysis / 中国实验方剂学杂志

Objective:To compare the adsorption and desorption properties of different anion exchange resins for total ginsenosides， clarify their adsorption/desorption mechanism， and establish a simple protocol for the purification of total ginsenosides. Method:The adsorption and desorption properties of five different resins （D301， D315， D312， D330， D201） on total ginsenosides were evaluated with specific adsorption capacity， specific desorption capacity， desorption rate and recovery rate as indices. The adsorption kinetics and thermodynamics of the selected resin and D101 macroporous resin were investigated by pseudo-first-order and pseudo-second-order kinetic models， as well as Langmuir and Freundlich isothermal adsorption models， and the differences of adsorption mechanism between anion exchange resin and conventional macroporous resin were elucidated. The dynamic adsorption and desorption experiments were used to determine the optimum chromatographic parameters for anion exchange resin. After verifying the purification process of total ginsenosides， nine individual ginsenosides were qualitatively and quantitatively analyzed by liquid chromatography-mass spectrometry （LC-MS）. Result:D301 anion exchange resin was obviously superior to the other four kinds of anion exchange resin， the optimum parameters were set as follows：pH 8 of loading solution， loading volume of 2 BV， loading speed of 4 BV·h^-1， eluted with 3 BV of water and 20% ethanol for the impurities， eluted with 8 BV of 80% ethanol with elution speed of 4 BV·h^-1. After purified by D301 resin， the enrichment coefficients of 9 monomer ginsenosides were simultaneously increased to different degrees， the overall enrichment coefficient was up to 5.3， the recovery rate for the total amount of these ginsenosides was calculated to be 80.9%， and the purity of total ginsenosides in Ginseng Radix et Rhizoma extract increased from 17.07% to 91.19%. Conclusion:D301 anion exchange resin is suitable for rapid and practical purification of total ginsenosides， hence allowing for the enrichment of high-purity total ginsenosides from Ginseng Radix et Rhizoma via one-dimensional column chromatography.

Optimization of Purification Technology of N-（E）-p-coumaroyltyrosine in Leaves of Abrus cantoniensis / 中国药房

OBJECTIVE： To establish a method for content determination of N-（E）-p-coumaroyltyrosine in leaves of Abrus cantoniensis， and to optimize its purification technology. METHODS： HPLC method was adopted for the content determination of N-（E）-p-coumaroyltyrosine in A. cantoniensis. The determination was performed on Hypersil BDS C18 column with mobile phase consisted of 0.1％ formic acid water （A）-methanol （B） （gradient elution） at a flow rate of 1.0 mL/min. The column temperature was set at 25 ℃. The detection wavelength was set at 300 nm， and sample size was 10 μL. Using polyamide resin as material， the yield of N-（E）-p-coumaroyltyrosine as indicators， single factor test was used to optimize the purification technology of N-（E）-p-coumaroyltyrosine， such as concentration， sample size， stationary adsorption time. RESULTS： The linear range was 2.575-51.50 μg （r＝0.999 9） for N-（E）-p-coumaroyl-tyrosine. The limit of quantification was 0.000 618 μg， and the detection limit was 0.000 129 μg. RSDs of precision， stability and reproducibility tests were all lower than 3％. The recoveries were 97.04％-102.43％ （RSD＝2.06％， n＝6）. The optimal purification technology was as follows： the concentration of the sample solution was 0.04 g /mL （by the leaves of A. cantoniensis）； sample capacity 50 mL； the sample flow rate was 1.0 mL/min； the stationary adsorption time was 20 min； the eluting solvents were ammonia containing water （containing 0.1％ acetic acid）， 20％ ethanol （containing 0.1％ acetic acid） and ammonia（pH 10）. Average yield was 98.94％，average dry paste content was 61.17 mg/g， and average dry paste purity was 19.73％ by optimal purification technology. CONCLUSIONS： Established method is simple， accurate and stable. The optimized technology is stable and feasible.

Prospects to the formation and control of potential dimer impurity E of pantoprazole sodium sesquihydrate / 药物分析学报

Pantoprazole sodium, a substituted benzimidazole derivative, is an irreversible proton pump inhibitor which is primarily used for the treatment of duodenal ulcers, gastric ulcers, and gastroesophageal reflux disease (GERD). The monographs of European Pharmacopoeia (Ph. Eur.) and United States Pharmaco-poeia (USP) specify six impurities, viz.; impurities A, B, C, D, E and F, respectively for its active phar-maceutical ingredient (API). The identification and synthesis of all impurities except impurity E are well described in the literature; however, there is no report related to impurity E. The prospects to the for-mation and controlling of impurity E up to ≤0.03％ in the synthesis of pantoprazole sodium sesquihydrate (PAN) were discussed in detail for the first time. The present work described the journey towards the successful development of an optimal preparation procedure of dimer impurity E. The most plausible mechanism involved in the formation of impurity E has been proposed.

Separation and preparation of epimers physanicantriol and 14-epi-physanicantriol from the leaves of Artemisia argyi / 国际药学研究杂志

Objective To establish a method for the preparative separation and isolation of the epimeric labdenetriols,phy?sanicantriol(1)and 14-epi-physanicantriol(2),from the leaves of Artemisia argyi.Methods The CH2Cl2fraction of 95% EtOH ex?tract from the leaves of A.argyi was separated by Diaion HP-20,silica gel and Sephadex LH-20 column chromatography and purified by semi-preparative HPLC to obtain an epimeric mixture of 1 and 2.Then,the epimeric mixture was separated by silica gel H column chromatography with eluting by n-hexane-CH2Cl2-isopropyl alcohol(1:1:0.15,V/V/V)to obtain compounds 1 and 2.The structures of 1 and 2 were identified by comparing MS and NMR data with those reported in the literature.Results and Conclusion Two diterpe?noids were isolated for the first time from the family Compositae.This method is effective,convenient and rapid,and is suitable for the separation and preparation of the epimers 1 and 2.

Apigenin glycoside: an antioxidant isolated from Alchornea coelophylla pax & k. Hoffm. (euphorbiaceae) leaf extract / Glicósido de apigenina: un antioxidante aislado del extracto de hoja de Alchornea coelophylla Pax & K. Hoflm. (Euphorbiaceae) / Glicosídeo de apigenina: um antioxidante do extrato das folhas de Alchornea coelophylla Pax & K. Hoflm. (Euphorbiaceae)

Abstract An antioxidant flavonoid has been isolated from methanolic leaf extract of Alchornea coelophylla Pax & K. Hoffm. by means of different column chromatography steps with DIAION HP-20 resin and silica gel in combination with analytical highperformance liquid chromatography (HPLC). It was identified as Apigenin-8-C- (α-L-rhamnopyranosyl-(1-›2)-β-D-glucopyranoside) on the basis of spectroscopic analysis and by comparison with related values reported in the literature. This compound exhibited high in vitro antioxidant activity through DPPH. and ABTS • + colorimetric assays with IC50 values of 7.528 and 379.7 µg. mL-1, respectively.

Resumen Se aisló un flavonoide antioxidante del extracto metanólico de hojas de Alchornea coelophylla Pax & K. Hoffm. El compuesto se obtuvo por medio de sucesivas cromatografías en columna (con la resina DIAION HP-20 y sílica gel), seguidas de cromatografía líquida de alta eficiencia (HPLC). Con base en el análisis espectroscópico y por comparación con valores relacionados reportados en la literatura, el flavonoide se identificó como Apigenin-8-C-(α-L-rhamnopiranosil-(1-›2)-β-D-glucopiranósido). Este compuesto presentó una alta actividad antioxidante in vitro: ensayos colorimétricos utilizando DPPH. y ABTS • + mostraron valores de IC50 de 7.528 y 379.7 µg mL-1, respectivamente.

Resumen Um flavonoide antioxidante foi isolado do extrato metanólico das folhas de Alchornea coelophylla Pax & K. Hoffm. por meio de diferentes etapas de cromatografia em coluna usando resina DIAION HP-20 e gel de sílica em combinação com Cromatografia Líquida de Alta Eficiencia (HPLC) analítica. O composto foi identificado como apigenina-8-C-(α-L-ramnopiranosil-(1-›2)-β-D-glicopiranosido) com base em análises espectroscópicas e por comparação com valores descritos na literatura. Este composto exibiu elevada atividade antioxidante in vitro por meio de ensaios colorimétricos por DPPH e ABTS • + com valores de IC50 de 7,528 e 379,7 µg. mL-1, respectivamente.

Monitoring method for macroporous resin column chromatography process of salvianolic acids based on near infrared spectroscopy / 中国中药杂志

To study and establish a monitoring method for macroporous resin column chromatography process of salvianolic acids by using near infrared spectroscopy (NIR) as a process analytical technology (PAT).The multivariate statistical process control (MSPC) model was developed based on 7 normal operation batches, and 2 test batches (including one normal operation batch and one abnormal operation batch) were used to verify the monitoring performance of this model. The results showed that MSPC model had a good monitoring ability for the column chromatography process. Meanwhile, NIR quantitative calibration model was established for three key quality indexes (rosmarinic acid, lithospermic acid and salvianolic acid B) by using partial least squares (PLS) algorithm. The verification results demonstrated that this model had satisfactory prediction performance. The combined application of the above two models could effectively achieve real-time monitoring for macroporous resin column chromatography process of salvianolic acids, and can be used to conduct on-line analysis of key quality indexes. This established process monitoring method could provide reference for the development of process analytical technology for traditional Chinese medicines manufacturing.

Research on antibacterial components of chloroform and ethyl acetate extracts of artemisia anomala / 第二军医大学学报

Objective To study the antibacterial components of chloroform and ethyl acetate extracts of the traditional Chinese medicine Artemísia anómala S. Moore. Methods The chloroform and ethyl acetate extracts of Artemísia anómala S. Moore was isolated by silica gel column chromatography. The antibiotic tests of the different isolated fractions in vilro were performed by using Kriby-Bauer method and broth dilution method. The compound structures of the significantly active components were identified by the method of chemical colored-reaction and spectrum analysis. Results Multiple components of chloroform and ethyl acetate extracts of Artemísia anómala had different degrees of antibacterial activities for common pathogenic strains in clinic. The structures of significantly active components were identified as: apigenin, eupatilin, and caffeic acid; eupatilin had the strongest antimicrobial activity for Standard Slaphylococcus aureus (ATCC25923) and Standard Staphylococcus aureua (ATCC29213), with the minimal bactericidal concentrations being both 0. 062 5 mg/mL. Conelusion The proposcd method in the present study is simple and quick; it can aceurately and cffectively obtain the antibacterial components of the chloroform and ethyl acetate extracts of Artemísia anómala. This study is the first to report the antibacterial activity of eupatilin.

Identification and partial purification of antibacterial compounds against Streptococcus mutans from Galla Rhois / 대한구강보건학회지

OBJECTIVES: This study aims to identify and partially purify antibacterial compounds against Streptococcus mutans from Galla Rhois extract. METHODS: Galla Rhois was extracted with n-hexane or ethanol and concentrated in a rotary evaporator. The antibacterial effect of the Galla Rhois extract against S. mutans was determined by the paper discdiffusion method with n-hexane, ethanol, methanol, ethyl acetate, dimethyl sulfoxide (DMSO), acetone, and distilled water as the solvents. The active compounds were purified by partition chromatography, thin-layer chromatography (TLC), and high-performance liquid chromatography (HPLC). RESULTS: The antibacterial effect of the n-hexane extract was more effective against S. mutans than the ethanol extract (P<0.05). The antibacterial component of Galla Rhois was partially purified using partition chromatography and HPLC, and the antibacterial activity was confirmed. CONCLUSIONS: The partially purified component of Galla Rhois showed strong antibacterial effect against S. mutans. These results confirm that the antibacterial compounds of Galla Rhois can be used for the prevention of dental caries.

Preparation technology of new gel-purified prothrombin complexes concentrates / 中国生化药物杂志

Objective To study the process conditions for new gel Capto DEAE ion exchange chromatography to purify prothrombin complexes concentrates.Methods After removal of cryoprecipitate by centrifugation, healthy human plasma was mixed with DEAE-Sephadex A-50 gel.After that, the gel were washed and eluted to obtain eluate; then, the eluate, after being ultrafiltered, was loaded on a column packed with Capto DEAE-gel for chromatography to prepare PCC which was later determined for activities of coagulation factors Ⅱ,Ⅶ,Ⅸ,Ⅹ and anticoagulation protein C, with their yield calculated.Besides, the protein concentration of PCC was determined using the Bradford method, based on which the specific activity of the four coagulation factors and protein C were calculated. According to the results, purification effect of Capto DEAE-gel on the PCC was analyzed. Results Under different experimental conditions, the yield and purity of the coagulation factors FⅡ,FⅨ and FⅩ were high, and the equilibrum degree of the three factors was good;however, the yield and purity of coagulation factor FⅦwere very low.When the three variables ( sodium citrate, NaCl and pH) in balanced solution, washing solution and elution were 0.020-0.028 mol/L, 0.10-0.15 mol/L and 6.9-7.2;0.012-0.020 mol/L, 0.10-0.15 mol/L and 6.9-7.2;0.005-0.012 mol/L, 2.4 mol/L and 7.2-7.5 , respectively,the yield and purity of PCC prepared from Capto DEAE-gel were good. Under this condition, yield of factor Ⅸ was ( 74.40 ±10.89 )% and purity of factor Ⅸ was ( 3.31 ±0.31 ) IU/mL.Under different experimental conditions, yield and specific activity of anticoagulant protein C were higher.Conclusion The purity of four coagulation factors and anticoagulation protein C of PCC prepared by the new method that combined the batch adsorption with DEAE-sephadex A-50 was combined with column chromatography packed with Capto DEAE-gel are higher than those prepared by the routine procedure.Furthermore, the PCC are better than these products obtained by traditional process, whose purity are 2.17-3.31IU/mg.Therefore, these studies will lay the groundwork for exploring novel preparation process of producing PCC.

Isolation and Identification of Terpenoids from the Fruits of Acanthopanax chiisanensis

Phytochemical constituents were isolated from the fruits of Acanthopanax chiisanensis by repeated column chromatography. Their structures were identified as beta-sitosterol (1), daucosterol (2), sesamin (3), chiisanogenin (4), and 22alpha-hydroxy chiisanogenin (5) by spectroscopic analysis (MS, 1H-, and 13C-NMR). Compounds 1 - 5 were isolated for the first time from the fruits of A. chiisanensis.

Study on activity of VEGF-binding factors in Paris polyphylla / 中草药

Objective: To screen and isolate vascular endothelial growth factor (VEGF)-binding factors from Paris polyphylla var. yunnanensis, and explore their property for stimulating VEGF activity. Methods: The VEGF-binding factors from water extract of P. polyphylla var. yunnanensis were screened by VEGF-affinity chromatography and further purified by HPLC method. Their activity on proliferation of VEGF-dependent cells was determined by MTT analysis with sensitive cell line HepG2 as model. We also predicted the possible components according to RRLC-QTOF and UV results. Results: The VEGF-binding factors screened from the water extract of P. polyphylla var. yunnanensis were named as factor B3 which included three compounds and could induce the proliferation of VEGF-dependent cell line HepG2 but not the VEGF-independent cell line HEK293. Further studies indicated that factor B3 had an additive effect with VEGF to induce the proliferation of HepG2, and the additive effect could be attenuated by VEGF antibody. In addition, the proliferation of HepG2 cells induced by factor B3 alone could also be attenuated by VEGF antibody. Furthermore, based on the results of RRLC-QTOF and UV analysis, we predicted that factor B3 are probably members of saponin family. Conclusion: The factor B3 isolated from P. polyphylla var. yunnanensis has the property to stimulate VEGF activity.

Research on Adsorption Properties Changes of Mannotriose by Modified Activated Carbon / 世界科学技术-中医药现代化

This study was aimed to explore the impact of activated carbon adsorption modified by different concentrations of nitric acid and ammonia,in order to examine the impact on adsorption of mannotriose by modified activated carbon.The activated carbon was processed by different concentrations of nitric acid and ammonia.And then,the adsorption capacity of benzene,iodine,methylene blue and the purification effects on mannotriose were measured.The results showed that the active carbon modified by nitric acid and ammonia had some changes of adsorptions for methylene blue,iodine and benzene.The purification effect of mannotriose with nitric acid-modified activated carbon was declined.The purification effect of mannotriose with ammonia-modified activated carbon was increased.It was concluded that the pore structure of activated carbon had been changed by nitric acid and ammonia.The adsorption capacity of nitric acid modified active carbon to mannotriose was declined.However,the adsorption capacity of ammonia modified active carbon to mannotriose was increased.It showed that ammonia modified active carbon was suitable for the purification of mannotriose.And the adsorption capacity of iodine reflected the adsorption capacity of mannotriose by active carbon.

Study on Chemical Constituents in Rubus Pinfaensis / 中国药师

Objective:To study the chemical constituents in the dry roots of Rubus pinfaensis. Methods:The compounds were sep-arated from the alcohol extract of the roots of Rubus pinfaensis by silica gel column chromatography, and identified by IR, 1 H-NMR and EI-MS methods. Results:Five compounds were isolated and identified as oleanolic acid (Ⅰ) , 3-keto, 16α-hydroxy, 24-noroleanolic acid (Ⅱ) , 3′-methoxy myricetin (Ⅲ) , 2′-deoxyuridine (Ⅳ) and p-hydroxy phenylacetic acid (Ⅴ) . Conclusion: Compound Ⅰ,Ⅱ,Ⅲ,Ⅳ and Ⅴ are isolated from Rubus pinfaensis for the first time.

Chemical Constituents in Groups of Effective Components Extracted fromXiaoxuming Decoction / 世界科学技术-中医药现代化

This article was aimed to study the chemical constituents in groups of effective components extracted from Xiaoxuming Decoction. Twelve compounds were isolated and purified by dynamic axial compression column chromatography. Their chemical structures were identified by spectral analysis. The results showed that twelve compounds were isolated and identified as octacosanoic acid(1), cetanol(2), oroxylin A(3), wogonin(4), baicalein(5), tetrandrine(6), fangchinoline(7), wogonoside(8), baicalin(9), paeoniflorin(10), amygdalin(11), manntol(12). It was concluded that all compounds were isolated from this compound prescription for the first time.