Correlation study on Tibetan medicine Pterocephalus hookeri of bitter taste receptors based on molecular docking technology / 中国中药杂志

In order to study the interaction between Pterocephalus hookeri and bitter taste receptors,three-dimensional structural models of bitter taste receptors TAS2 R16,TAS2 R14 and TAS2 R13 were established by homology modeling in this paper. Maestro software was used for docking the chemical constituents of P. hookeri with bitter taste receptors. The results showed that 25 chemical components of P. hookeri can regulate three bitter taste receptors. And these components were mainly iridoid glycosides and phenolic acids.This research focused on the comprehensive application of homology modeling and molecular docking technology to explore the interaction between bitter chemical constituents of P. hookeri and bitter taste receptors. This study provided assistance in revealing pharmacodynamic basis of bitter Tibetan medicine at molecular level. It also provided new ideas and methods for the study of Tibetan medicine.

Investigation on intestinal absorption ingredients and their absorption characteristics in Pterocephali Herba by everted intestinal sac method / 中国中药杂志

The intestinal absorption characteristics of ten iridoid glycosides and phenolic acids in the Pterocephali Herba were evaluated via rat intestinal valgus model. The intestinal sac fluids at different time after administration of high,medium and low concentrations of Pterocephali Herba extract were collected and ten chemical components in fluid samples were detected by UPLC-PDA. Accumulative absorbed doses( Q) and absorption rate constants( Ka) of ten chemical constituents were calculated,while proportions between Pterocephali Herba extract and intestinal absorption liquid were compared. The results showed that the intestinal absorption of 10 chemical components was linear absorption( R2>0. 9) at different concentrations,which accorded with the zero-order absorption rate. The absorption rate constant was related to the concentration of the drug and the intestinal site,which indicated that intestinal adsorption mechanism of the components were passive diffusion and active transport. Proportions of chemical constituents in intestinal sac fluid were different from those in Pterocephali Herba extract. Therefore,those ten chemical components in Pterocephali Herba extract can be absorbed in whole intestine. Everted intestinal sac model can be used to evaluate intestinal absorption characteristics of ingredients in Pterocephali Herba extract effectively.

Triagem fitoquímica e avaliação da atividade antibacteriana de extratos das flores de Sambucus nigra L. (Caprifoliaceae) / Phytochemical screening and evaluation of the antibacterial activity of Sambucus nigra L. flower extracts (Caprifoliaceae)

RESUMO O presente trabalho teve como objetivo realizar a triagem fitoquímica e avaliar a atividade antibacteriana de extratos das flores de Sambucus nigraL. Os extratos; aquoso (10 %), etanólico (5 %) e Acetato de etila (5 %) foram submetidos a testes colorimétricos para triagem fitoquímica e a avaliação da atividade antibacteriana foi realizada pelo método de disco-difusão em ágar. Os resultados mostraram que nas concentrações de 6 e 12 mg o extrato aquoso apresentou halos significativos de inibição para Staphylococcus aureus, Pseudomonas aeruginosa e Streptococcus pyogenes, porém, quando comparado aos medicamentos usados como referência a atividade não foi satisfatória, e, ainda, evidenciou a ausência de inibição para todas as cepas testadas com o aumento da concentração para 18 e 24 mg. A análise da triagem fitoquímica evidenciou a presença de flavonoides com intensa reação de cor no extrato aquoso e etanólico, e de fraca intensidade no extrato acetato de etila. Nos mesmos extratos, pelos testes realizados, não foram detectados taninos, saponinas, antraquinonas e alcaloides. Concluiu-se que o extrato aquoso apresentou melhor efeito inibitório para Staphylococcus aureus, Pseudomonas aeruginosa e Streptococcus pyogenes, porém insuficiente para promover a inativação eficiente quando comparado aos controles.

ABSTRACT This study aimed to perform a phytochemical screening and to evaluate the antibacterial activity of the extracts of Sambucusnigra L. flowers. The aqueous (10%), ethanolic (5%) and ethyl acetate (5%) extracts were subjected to colorimetric tests for phytochemical screening and the antibacterial activity evaluation was performed by the disk-diffusion method in agar. The results showed that in the 6 and 12 mg concentrations the aqueous extract presented significant inhibition halos for Staphylococcus aureus, Pseudomonas aeruginosa and Streptococcus pyogenes, but when compared with the medicines used as a reference, the activity was not satisfactory and, besides, it indicated the absence of inhibition for all the tested strains with the concentration increase of 18 and 24mg. The phytochemical screening analysis showed the presence of flavonoids with intense color reaction in the aqueous and ethanol extracts, and of low intensity in the ethyl acetate sample. In the same extracts, the tests did not detect tannins, saponins, alkaloids and anthraquinones. It was concluded that the aqueous extract showed better inhibitory effect on the Staphylococcus aureus, Pseudomonas aeruginosa and Streptococcus pyogenes, but not enough to promote an effective inactivation when compared with the medicine tests.

Effect of Sambucus sieboldiana Extract on the Cell Growth and Extracellular Matrix Formation in Osteoblast Cells

Sambucus sieboldiana (SS) is a member of the family Caprifoliaceae and has been recommended as a functional material because of its several bioactivities. Although numerous literatures are available on the pharmacological and biological activities, the biological activity of SS in bone regeneration process has not yet been well-defined. Therefore, in this study, the effect of SS was investigated in the proliferation and differentiation of MC3T3-E1 osteoblastic cell line. The treatment of SS did not significantly affect the cell proliferation in MC3T3-E1 cells. SS significantly accelerated the mineralization and significantly increased the expression of alkaline phosphatase (ALP) and osteocalcin (OC) mRNAs, compared to the control, in the differentiation of MC3T3-E1 cells. SS significantly accelerated the decrease of osteonectin (ON) mRNA expression as compared with the control in a time-dependent manner in the differentiation of MC3T3-E1 cells. These results suggest that the SS facilitate the osteoblast differentiation and mineralization in MC3T3-E1 osteoblastic cells. Therefore, there may be potential properties for development and clinical application of bone regeneration materials.

UFLC-PDA fingerprint of Tibetan medicine Pterocephalus hookeir / 中国中药杂志

This study was aimed to establish an UFLC fingerprint of Tibetan medicine Pterocephalus hookeir samples from different habitats. UFLC-PDA was adopted to analyse 21 batches of P. hookeir samples from different habitats. The chromatographic condition was as follow: Agilent proshell 120 SB-C18 column (4.6 mm x 100 mm, 2.7 microm) eluted with the mobile phases of acetonitrile and 0.2% phosphoric acid water in gradient mode. The flow rate was 1.0 mL x min(-1), and the detection wavelength was set at 238 nm. The fingerprints of 21 batches P. hookeir were carried out by similarity comparation, and 15 chromatographic peaks were extracted as the common peaks of fingerprint, of which 5 peaks were identified as chlorogenic acid, loganin, sweroside, sylvestroside III, triplostoside A. The similarity degrees of 18 batchs of samples were above 0.9, and the other 3 batchs of samples were below 0.9. This is the first established fingerprint of P. hookeir by using UFLC-PDA. This method has good precision, stability and repeatability that it could provide basis for quality control and evaluation of P. hookeir.

Spectrum-effect correlation analysis of traditional Tibetan medicine "Morina nepalensis" on nitric oxide production inhibition / 中国中药杂志

<p><b>OBJECTIVE</b>To establish an HPLC-ELSD fingerprint of the whole herbs of Morina nepalensis and perform the correlation analysis of chemical components of the herb and nitric oxide (NO) production inhibition.</p><p><b>METHOD</b>HPLC-ELSD assay was performed to evaluate 10 batches of M. nepalensis herbs. The chromatographic conditions were as following: Eclipse XDB C18 column (4.6 mm x 150 mm, 5 microm), water (A) and acetonitrile (B) as a gradient mobile phases, flow rate 1.0 mL x min(-1), and column temperature at 35 degress C. Evaporative light-detection conditions: atomization temperature at 104 degrees C, the flow rate of N2 2.8 L x min(-1) and 10 microL sample injection. Chromatographic fingerprint was developed, and the inhibition activity of production of NO in lipopolysaccharide-induced macrophages was also analyzed. The similarity and correlation analysis between the HPLC-ELSD fingerprints and NO production inhibition were carried out by PLS method.</p><p><b>RESULT</b>The common mode for M. nepalensis herb fingerprint was established, including 15 common characteristic peaks. Among them, 7 peaks were positively correlated with the NO production inhibition. According to the assessment on the similarity of 10 batches of samples, a similarity of over 0.90 were shown in HPLC-ELSD fingerprint and all samples were separated into two groups.</p><p><b>CONCLUSION</b>This method can be used to assess the quality of M. nepalensis, which provides a reliable method for scientific assessment and quality control.</p>

Change of the content of chemical constituents and anti-oxidative action of the decoction of radix ginseng combined with Flos Lonicerae, radix Polygoni Multiflori and Radix Astragali / 药学学报

Ginsenosides in the decoction of Radix Ginseng, Radix Ginseng with Flos Lonicerae, Radix Polygoni Multiflori or Radix Astragali have been investigated by high performance liquid chromatography (HPLC) and electrospray ionization mass spectrometric method (ESI-MS). Change of the content of ginsenosides was nonlinear in diverse combinative proportion of Radix Ginseng with Flos Lonicerae, while the stripping of ginsenosides was promoted by a small amount of Radix Polygoni Multiflori. In the combinative decoction of Radix Ginseng with Radix Astragali, ginsenosides contents were increased compared to single decoction of Radix Ginseng. Besides, ferric reducing antioxidant power (FRAP) method was developed for determination of the total antioxidative activity of n-butanol and water-soluble extracts from the decoction. The experimental results showed that antioxidative activity was better in the combinative decoction than that in single decoction, and the FRAP values of n-butanol extract were also greater compared with that of water extract.

DNA barcoding in medicinal plants Caprifoliaceae / 中国中药杂志

<p><b>OBJECTIVE</b>To determine the candidate sequences which can be used as DNA barcode to identify species in Caprifoliaceae family by screening out from four different DNA fragments sequences.</p><p><b>METHOD</b>PCR amplification, sequencing efficiency, differential intra- and interspecific divergences, the DNA barcoding gap and identification efficiency were used to evaluate these loci.</p><p><b>RESULT</b>The ITS2 was used as a candidate sequence of DNA barcode to identify the species in Caprifoliaceae family, whose rate of success in identification in genera level was 100% and in species 96.6%, and psbA-trnH as a complementary barcode to ITS2 for Caprifoliaceae.</p>

Caracterização farmacobotânica das espécies de Sambucus (Caprifoliaceae) utilizadas como medicinais no Brasil: Parte II. Sambucus australis Cham. & Schltdl. / Pharmacobotany of Sambucus species (Caprifoliaceae), used in traditional medicine in Brazil: Part II. Sambucus australis Cham. & Schltdl

Sambucus australis Cham. & Schltdl. (sabugueiro-do-rio-grande, Caprifoliaceae) é uma planta medicinal descrita apenas na primeira edição da Farmacopéia Brasileira. A espécie é nativa no Brasil, e suas flores são utilizadas na medicina popular, na forma de infusão ou decocção, como diuréticas, antipiréticas, antiinflamatórias, laxativo leve e no tratamento de doenças do aparelho respiratório. Visando elaborar uma monografia farmacopéica atualizada e comparativa com a de Sambucus nigra L., de origem européia, foram estabelecidos os caracteres botânicos macro e microscópicos, através da metodologia clássica utilizada em morfoanatomia vegetal. São características macroscópicas: flores morfologicamente monoclinas; corola de sete a dez milímetros de diâmetro; pétalas com cinco, raro quatro nervuras paralelas; estames curtos e longos; gineceu em regra com cinco lóculos. São características microscópicas: cutícula espessa e estriada; ausência de idioblastos de areia cristalina de oxalato de cálcio; estômatos anomocíticos; brácteas anfiestomáticas; sépalas hipoestomáticas; pétalas anfi-hipoestomáticas; células epidérmicas da face abaxial de sépalas e pétalas retilíneas a sinuosas; células epidérmicas do filete alongadas e de paredes retilíneas; tricomas tectores e glandulares de diferentes tipos; brácteas, sépalas e pétalas com mesofilo homogêneo; sistema vascular representado por feixes colaterais ou agrupamentos de elementos xilemáticos; presença de gotas lipídicas em todas as peças.

Sambucus australis Cham. & Schltdl. (sabugueiro-do-rio-grande, Caprifoliaceae) is a medicinal plant described only in the first edition of Brazilian Pharmacopoeia. This species is native to Brazil, and its flowers are used in the folk medicine, with diuretic purpose, antipiretic, anti-inflammatory, mild laxative and to treat respiratory diseases, on infusions or decoctions forms. Aiming at elaborating an updated pharmacopoeical monograph and comparing it with the monograph of Sambucus nigra L., from Europe, it was established the macro and microscopic botanical characters, through the classic methodology used in plant morpho-anatomy. The macroscopic characters are: morphologic monoclin flowers; corolla with seven to ten millimeters of diameter; petals with five, rarely four parallel veins; shorter and longer stamens; ovary oftenly with five locules. The main microscopic characters are: thickned and striated cuticule; absense of idioblasts with calcium oxalate sandy cristals; anomocytic stomatas; amphystomatic bracts; hypostomatic sepals; amphi-hypostomatic petals; wavy and straight epidermal cells in the lower surface of sepals and petals; filaments epidermal cells with narrow and straight walls; glandular and non-glandular trichomes of different types; homogeneous mesophyll in bracts, sepals and petals; vascular system represented by both collateral bundles and xylematic elements; volatile and non volatile oil globules in all structures.

Caracterização farmacobotânica das espécies de Sambucus (Caprifoliaceae) utilizadas como medicinais no Brasil. Parte I. Sambucus nigra L. / Pharmacobotany characterization of Sambucus species (Caprifoliaceae), used in traditional medicine in Brazil. Part I. Sambucus nigra L

O sabugueiro (Sambucus nigra L., Caprifoliaceae) é uma planta medicinal descrita em farmacopéias estrangeiras, não constando da Farmacopéia Brasileira. A espécie é de origem européia e suas flores são comercializadas in natura sob o nome farmacopéico Sambuci flos, para uso na forma de infusão ou decocção, como diuréticas, antipiréticas, antiinflamatórias, laxativo leve e no tratamento de doenças do aparelho respiratório. Visando elaborar uma monografia farmacopéica atualizada, foram estabelecidos os caracteres botânicos macro e microscópicos, através da metodologia clássica utilizada em morfoanatomia vegetal. São características macroscópicas: flores monoclinas, iguais; corola de três a cinco milímetros de diâmetro; pétalas com três a quatro nervuras paralelas; estames iguais; gineceu em regra com três lóculos. São características microscópicas: cutícula espessa e estriada; presença de idioblastos de areia cristalina de oxalato de cálcio em brácteas, sépalas e pétalas; estômatos anomocíticos; brácteas hipoestomáticas; sépalas anfiestomáticas; pétalas anfi-hipoestomáticas; células epidérmicas da face abaxial de sépalas e pétalas muito sinuosas; células epidérmicas do filete alongadas e de paredes retilíneas; tricomas tectores e glandulares de diferentes tipos em todas as peças; brácteas, sépalas e pétalas com mesofilo homogêneo; sistema vascular representado por feixes colaterais ou agrupamentos de elementos xilemáticos; presença de gotas lipídicas em todas as peças.

The Elder tree (Sambucus nigra L., Caprifoliaceae) is a medicinal plant described in international pharmacopoeias, not yet mentioned in the Brazilian Pharmacopoeia. The flowers of this European species are commercialized in natura by the pharmacopeial name of Sambuci flos, with diuretic, antipyretic, anti-inflammatory and mild laxative purposes, and to treat respiratory diseases, through infusions or decoctions forms. Aiming at elaborating an updated pharmacopeial monograph, the macro and microscopic botanic characters were established, with the classic methodology used in plant morpho-anatomy. The macroscopic characters are: monoclin and equal flowers; corolla with three to five millimeters of diameter; petals with three to four parallel veins; equal stamens; ovary often with three locules. The main microscopic characters are: thickened and striated cuticle; anomocytic stomatas; bracts, sepals and petals with sandy crystals of calcium oxalate idioblasts; hypostomatic bracts; amphystomatic sepals; amphi-hypostomatic petals; strongly wavy epidermal cells in the lower surface of sepals and petals; filaments epidermal cells with narrow and straight walls; glandular and non-glandular trichomes of different types in all pieces; homogeneous mesophyll in bracts, sepals and petals; vascular system represented by both collateral bundles and xylematic elements; volatile and non-volatile oil globules in all structures.