Research progress of effective components of Astragalus on prevention and treatment of organ fibrosis / 药学学报

Astragalus, which was first documented in Shennong Bencao Jing, is the dried root of Astragalus membranaceus (Fisch.) Bge. or Astragalus membranaceus (Fisch.) Bge. var. mongholicus (Bge.) Hsiao. The active ingredients astragalus membranaceus saponins (AMS), astragalus polysaccharides (APS) and astragalus flavonoids (AFS) have pharmacological effects such as anti-tumor properties, lowering blood sugar, regulating lipid metabolism, cardiovascular protection, anti-oxidation, bone protection, anti-fibrosis, etc. Fibrosis affects almost all organs, particularly vital organs such as the lungs, liver, heart and kidneys. The primary pathological changes of fibrosis involve abnormal increase of myofibroblasts and excessive deposition of extracellular matrix (ECM) components, which lead to the formation of scar tissue, ultimately resulting in fibrosis and even functional loss or failure of organs, which seriously threatens human health and life. Recent, studies have shown that Astragalus membranaceus has a good therapetuic effect on organ fibrosis. This article reviews the current advances of Astragalus in the prevention and treatment of fibrosis of lungs, liver, heart, kidneys and other important organs.

Study on metabolism of Pulsatilla saponin in normal and ulcerative colitis model rats by UPLC-Q-TOF-MSE technology / 药学学报

In this study, ultra performance liquid chromatography-quadrupole-time of flight mass spectrometer-MSE (UPLC-Q-TOF-MSE) combined with UNIFI analysis platform was used to rapidly analyze and identify the metabolites of hederagenins 3-O-α-L-rhamnosyl-(1→2)-[β-D-glucopyranosyl-(1→4)]-α-L-arabopyranoside (Pulsatilla saponin D) and oleanolic acid 3-O-α-L-rhamnosyl-(1→2)-[β-D-glucopyranosyl-(1→4)]-α-L-arabopyranoside (Pulsatilla saponin B7) and hederagenins 3-O-α-L-rhamnosyl-(1→2)-α-L-arabopyranoside (Pulsatilla saponin BD) in plasma and colonic tissue of normal and ulcerative colitis (UC) rats. The database and analysis methods were established based on the precise molecular weight of compounds, retention time, neutral loss and reported data, and then the final data were obtained by comparing with the blank control group, combining with the deviation and the cracking rule of the compound. The results showed that the glucoses, hydroxylation and dehydroxylation, methylation and demethylation, dehydrogenation, decarboxylation and hydrolysis of saponin D, B7 and BD occurred in the plasma and colon tissues of normal and UC model rats. This study will clarify the metabolic transformation of Pulsatilla saponins D, B7 and BD in rats, determine the prototype components and their metabolites that enter the body, and whether colon injury will affect their metabolism in vivo, so as to explore the possible anti-colitis effective components in the prototype or metabolites of Pulsatilla saponins D, B7 and BD. This experiment was approved by Animal Ethics Committee of Jiangxi Science and Technology Normal University (approval number: Y202227).

Chemical constituents from Paris rugosa rhizomes and their antimicrobial activities / 中国中药杂志

Paris rugosa(Melanthiaceae) only grows in Yunnan province of China at present, and its chemical constituents have not been systematically studied. In this study, nine compounds, including one new compound pariposide G(1) and eight known compounds of cerin(2), stigmast-4-en-3-one(3), β-ecdysone(4), ophiopogonin C'(5), methyl protogracillin(6), gracillin(7), parissaponin H(8), and parisyunnanoside G(9), were isolated and identified from the ethanol extract of P. rugosa rhizomes by column chromatography methods and semi-preparative high-performance liquid chromatography(HPLC). Compounds 1-9 were isolated from this plant for the first time. The antibacterial and antifungal activities of all the compounds were evaluated. The results showed that ophiopogonin C' had strong inhibitory effects on Candida albicans [MIC_(90)=(4.68±0.01) μmol·L~(-1)] and the fluconazole-resistant strain of C. albicans [MIC_(90)=(4.66±0.02) μmol·L~(-1)].

Research progress in pharmacological effects of Aralia elata / 浙江大学学报·医学版

The traditional Chinese medicine Aralia elata (Miq.) Seem., also known as Aralia mandshurica, has the effect of "tonifying Qi and calming the mind, strengthening the essence and tonifying the kidneys, and dispelling wind and invigorating blood circulation". It is used in the treatment of neurasthenia, Yang deficiency and Qi deficiency, kidney Qi deficiency, spleen Yang deficiency, water-dampness stagnation, thirst, and bruises. Aralia elata saponins are the main components for the pharmacological effects. From the perspective of modern pharmacological science, Aralia elata has a wide range of effects, including anti-myocardial ischaemia and alleviation of secondary myocardium ischemic reperfusion injury by regulating ionic homeostasis, anti-tumor activity by inhibiting proliferation, promoting apoptosis and enhancing immunity, hypoglycemia and lipid lowering effects by regulating glucose and lipid metabolism, and hepato-protective, neuroprotective, anti-inflammatory/analgesic effects. The studies on pharmacological mechanisms of Aralia elata will be conducive to its development and application in the future. This article reviews the research progress of Aralia elata domestically and internationally in the last two decades and proposes new directions for further research.

Chemical constituents of Helleborus thibetanus / 中国中药杂志

The chemical constituents of Helleborus thibetanus were isolated and purified by silica gel column chromatography, Sephadex LH-20 gel column chromatography, and semi-preparative RP-HPLC, and the structures of all compounds were identified by modern spectrographic technology(MS, NMR). The MTT method was used to measure the cytotoxicity of compounds 1-8. Twelve compounds were isolated from the roots and rhizomes of H. thibetanus and were identified as(25R)-22β,25-expoxy-26-[(O-β-D-glucopyranosyl)oxy]-1β,3β-dihydroxyfurosta-5-en(1), β-sitosterol myristate(2), β-sitosterol lactate(3), β-sitosterol 3-O-β-D-glucopyrannoside(4), 4,6,8-trihydroxy-3,4-dihydronaphthalen-1(2H)-one(5), 1,3,5-trimethoxybenzene(6), 7,8-dimethylbenzo pteridine-2,4(1H,3H)-dione(7), 1H-indole-3-carboxylic acid(8), p-hydroxy cinnamic acid(9), lauric acid(10), n-butyl α-L-arabinofuranoside(11) and methyl-α-D-fructofuranoside(12), respectively. Among them, compound 1 is a new compound and named thibetanoside L; compounds 2, 5-8, 11 are first isolated from the family Ranunculaceae; compound 12 is isolated from the genus Helleborus for the first time. The results of MTT assay showed that the IC_(50) values of compounds 1-8 against HepG2 and HCT116 cells were greater than 100 μmol·L~(-1).

Study on the tissue distribution of eight effective components of Ziziphi Spinosae Semen aqueous extract by ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry / 药学学报

The aim is to study the tissue distribution characteristics of eight effective components in normal rats after oral administration of Ziziphi Spinosae Semen (ZSS) aqueous extract. An ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) analysis method was developed and validated for the determination of four flavonoids and four saponins in rat tissue using puerarin and ginsenoside Re as the internal standard (IS), respectively. Tissue samples including the heart, liver, spleen, lung, kidney, muscle, brain, small intestine, and serum, were collected from each rat at 0.5 h, 1.0 h, and 2.0 h after oral administration of ZSS aqueous extract (15 g·kg-1). All calibration curves exhibited good linearity (r > 0.994 6) over a wide concentration range for all components. The intra-day and inter-day precisions (RSD) at four different levels were both less than 19.77%, and the accuracies (RE) ranged from -19.68% to 19.46%; The extraction recoveries of the eight components ranged from 86.70% to 114.29%, and the matrix effects were from 82.14% to 114.57%. The validated method was successfully applied to the tissue distribution study of the eight components. The levels of swertisin, spinosin, 6‴-feruloylspinosin, and kaempferol-3-O-rutinoside in the small intestine were highest, then followed by the kidney, heart, and liver. Meanwhile, the levels of jujuboside A (JuA), jujuboside B (JuB), and jujuboside A1 (JuA1) in the small intestine were highest, then followed by the lung, spleen, and kidney. The concentrations of betulinic acid in the small intestine were higher than heart, lung, kidney, and liver. The flavonoids and saponins of ZSS with extremely low content could pass through the blood-brain barrier. The research results will provide an experimental basis for explaining the mechanism of nourishing the heart and tranquilizing the mind of ZSS. The animal experimental operations involved in this study followed the regulations of the Animal Ethics Committee of Shanxi University of Chinese Medicine and passed the animal experimental ethical review (No. 2021DW172).

Five new spirosterol saponins from Allii Macrostemonis Bulbus / 中国天然药物

Five new spirostanol saponins (1-5) and seven known compounds (6-12) were isolated from the n-butanol fraction of 75% ethanol extract of Allii Macrostemonis Bulbus. The identification and structural elucidation of all the isolates were performed through extensive 1D and 2D NMR experiments, HR-ESI-MS data analysis and comparisons with literature values. Antioxidant evaluation showed that compounds 6-11 exhibited certain scavenging effects on ABTS radical, where compounds 6, 7 and 11 had IC50 values of 0.208, 0.057 and 0.014 mg·mL-1, respectively.

Comparative Repellency of Selected Plants to Adult Anopheles gambiea complex (Gilles) in the Laboratory

Aims: The study evaluated the repellency effects of some tropical plants and shrubs found in semi- rural communities of Badagry Area of Lagos state; which are acclaimed to have the potentials of repelling mosquitoes from human dwellings. The repellency effects of Moringa oleifera, Morinda lucida, Magnifera indica and Phyllanthus muellerianus to adult Anopheles gambiea was evaluated in the Laboratory. Study Design: The study was carried out at Central Research Laboratory of Lagos State University, Ojo, Lagos, Nigeria and Central Research Laboratory of University of Lagos, Akoka, Lagos, Nigeria. Powdered of dried test plants were prepared and admix with coconut husk as inert, different concentrations were rubbed on the forearm of volunteers and repellency to blood starved female Anopheles mosquitoes was observed. Methodology: Test plants were collected from Badagry area of Lagos State, they were identified at University of Lagos Herbarium and given numbers. They were dried between 10 and 14 days at temperature of 25-27oC and powdered. Different concentrations of the powder mixed with powdered coconut husk was used to treat volunteers forearms and they were exposed to 0-2 two day old adult unfed mosquitoes in an aluminum glass cage fitted with net as arm entrance and repellency was observed for a period of 180 minutes, with landing counts taken every 30 minutes. The test plants were also subjected to qualitative and quantitative phytochemical analysis at University of Lagos Central Research Laboratory. Results: Results showed that all test plants were able to repel Anopheles mosquitoes in the study, repellency was shown in descending order Moringa oleifera with 88%, Magnifera indica 83%, Phyllantus muellerianuss 80% and Morinda lucida 72%. There was no statistical significance in percentage repellency at 95% CL. The result of phytochemical screening of the test plants showed that only M .indica indicated presence of saponing (36.99%). While M.oleifera has highest phenol content (45.6%3), Alkaloid (38.68%), steroid (24.89%) and Tannin (33.19%). Flavonoid and reducing sugar quantity was highest in M. indica (39.39%) and (55.18%) respectively. Conclusion: The plants were able to show repellency to Anopheles gambiae a nuisance malaria vector of serious medical importance. These plants are available in all tropical areas of Africa, they can therefore be used to prevent nuisance and painful mosquito bites which could be a sustainable way to prevent mosquito vectored diseases

Construction of cell factories for high production of ginsenoside Rh_2 in Saccharomyces cerevisiae / 中国中药杂志

Ginsenoside Rh_2 is a rare active ingredient in precious Chinese medicinal materials such as Ginseng Radix et Rhizoma, Notoginseng Radix et Rhizoma, and Panacis Quinquefolii Radix. It has important pharmacological activities such as anti-cancer and improving human immunity. However, due to the extremely low content of ginsenoside Rh_2 in the source plants, the traditional way of obtaining it has limitations. This study intended to apply synthetic biological technology to develop a cell factory of Saccharomyces cerevisiae to produce Rh_2 by low-cost fermentation. First, we used the high protopanaxadiol(PPD)-yielding strain LPTA as the chassis strain, and inserted the Panax notoginseng enzyme gene Pn1-31, together with yeast UDP-glucose supply module genes[phosphoglucose mutase 1(PGM1), α-phosphoglucose mutase(PGM2), and uridine diphosphate glucose pyrophosphorylase(UGP1)], into the EGH1 locus of yeast chromosome. The engineered strain LPTA-RH2 produced 17.10 mg·g~(-1) ginsenoside Rh_2. This strain had low yield of Rh_2 while accumulated much precursor PPD, which severely restricted the application of this strain. In order to further improve the production of ginsenoside Rh_2, we strengthened the UDP glucose supply module and ginsenoside Rh_2 synthesis module by engineered strain LPTA-RH2-T. The shaking flask yield of ginsenoside Rh_2 was increased to 36.26 mg·g~(-1), which accounted for 3.63% of the dry weight of yeast cells. Compared with those of the original strain LPTA-RH2, the final production and the conversion efficiency of Rh_2 increased by 112.11% and 65.14%, respectively. This study provides an important basis for further obtaining the industrial-grade cell factory for the production of ginsenoside Rh_2.

The glycosyltransferases involved in triterpenoid saponin biosynthesis: a review / 生物工程学报

Triterpenoid saponins are widely used in medicine, health cares, cosmetics, food additives and agriculture because of their unique chemical properties and rich pharmacological activities. UDP-dependent glycosyltransferases (UGTs) are the key enzymes involved in triterpenoid saponin biosynthesis, and play important roles in the diversity of triterpenoid saponin structures and pharmacological activities. This review summarized the UGTs involved in plant triterpenoid saponin biosynthesis based on the sources of UGTs and the types of receptors. Moreover, the application of UGTs in heterologous biosynthesis of triterpenoid saponins based on synthetic biology was also discussed.

Effect of Pulsatilla Saponin A on Proliferation and Apoptosis of Burkitt Lymphoma Cells Based on JAK2/STAT3 Signaling Pathway / 中国实验方剂学杂志

ObjectiveTo investigate the effect of pulsatilla saponin A （PSA） on proliferation and apoptosis of human Burkitt lymphoma （BL） cell line Raji cells and expression of related pathway proteins. MethodWith Raji cells as the research object， the cell proliferation was detected by cell counting kit-8 （CCK-8） method， and the half-maximal inhibitory concentration （IC50） values of 24 h， 48 h and 72 h were calculated to be 19.77， 18.31， 16.70 μmol·L-1， respectively. In subsequent related experiments， 0， 8， 16， 32 μmol·L-1 PSA were selected according to the IC50 value of Raji cells treated with PAS for 72 h. After 0， 8， 16， 32 μmol·L-1 PSA acted on Raji cells for 24， 48， 72 h， the optical density values of cell growth curve were detected by CCK-8 method. The zymogen activities of cysteine aspartate-specific protease （Caspase）-3， Caspase-8 and Caspase-9 in Raji cells treated with 0， 8， 16 and 32 μmol·L-1 PSA for 24 h were measured by Caspase-3， Caspase-8 and Caspase-9 colorimetric assay kit. The apoptosis rate and cell cycle of Raji cells treated with different concentrations of PSA after 24 h were detected by flow cytometry. The expression of B-cell lymphoma 2 （Bcl-2）， Bcl-2-associated X protein （Bax）， cleaved poly（ADP-ribose） polymerase （cleaved PARP）， cleaved cysteinyl aspartate-specific protease-3 （cleaved Caspase-3） apoptosis related protein and Janus kinase 2 （JAK2）， signal transducer and activator of transcription 3 （STAT3）， phosphorylated-JAK2 （p-JAK2）， and phosphorylated- STAT3 （p-STAT3） pathway proteins in Raji cells after 24 h of treatment with 0， 8， 16 and 32 μmol·L-1 PSA were tested by Western blot. ResultCompared with control group， decreased cell survival rate， inhibited cell proliferation， activated zymogens of Caspase-3， Caspase-8 and Caspase-9 （P<0.01）， increased apoptosis （P<0.05， P<0.01）， and enhanced cell cycle arrest in Gap phase 2 （G2） were observed in 8， 16 and 32 μmol·L-1 PSA groups（P<0.05， P<0.01）. Compared with control group， cells treated with 8， 16 and 32 μmol·L-1 PSA had lower expression of Bcl-2， p-JAK2， p-STAT3 proteins （P<0.05， P<0.01）， and higher expression of Bax， cleaved PARP and cleaved Caspase-3 protein （P<0.01）， while no significant change was found in the expression of JAK2 and STAT3 proteins. ConclusionPSA could inhibit proliferation and induce apoptosis of Raji cells， and its potential mechanism might be related to the regulation of JAK2/STAT3 signaling pathway.

Identification of triterpenoid saponins from Anemone rivularis var. flore-minore and study on their antitumor activities / 中国药房

OBJECTIVE To study the triterpenoid saponins from Anemone rivularis var. flore-minore and their antitumor activities. METHODS The n-butanol extract of 70％ ethanol extract from rhizome of the plant was separated. The triterpenoid saponins were separated and purified by normal silica gel column chromatography ，reversed phase ODS column chromatography ， Sephadex LH- 20 gel column chromatography and semi-preparation high performance liquid chromatography. The structures of these saponins were identified by spectral analysis （NMR and MS ）and physical and chemical properties. MTT assay was used to test the proliferation inhibitory activity of the compounds against five kinds of human tumor cells （HL-60 cells，A549 cells，HepG2 cells，HeLa cells and U 87MG cells ）. The apoptosis inducing effect of compound 7 on U 87MG cells was evaluated by flow cytometric Annexin V-FITC/PI staining test. RESULTS：Sixteen triterpenoid saponins were obtained and identified as 3 β-O-β-D-xylopyranosyl-（1→2）-α-L-arabinopyranosyl-oleanolic acid-28-O-α-L-rhamnopyranosyl- （1→4） -β-D-glucopyranosyl-（1→6）-β-D-glucopyranoside（1），3β-O-L-arabinopyranosyl oleanolic acid- 28-O-β-D-glucopyranoside（2），saponin B （3）， 163.com oleanolic acid- 3β-O-β-D-glucopyranosyl-（1→2）-α-L-arabino- pyranoside（4），HN-saponin F （5），clematoside S （6），prosapogenin CP 4（7），cussonside B （8），pulsatilla saponin C （9）， clemastanoside D （10），3 β-O-β-D-glucopyranosyl-（1→2）-β-L-arabinopyranosyl-hederagenin-28-O-β-D-glucopyranoside（11）， ciwujianoside C 3（12），ciwujianoside A 1（13），huzhangoside D （14），kalopanaxsaponin B （15）and hederacolchiside E （16）. Compounds 3，4，6-9 displayed inhibitory activities on the proliferation of tumor cells to different extent ，and compound 7 had the strongest activity ；compound 7 induced the apoptosis of U 87MG cell so as to inhibit the proliferation of cancer cells in a time-dependent manner. CONCLUSIONS The obtained 16 saponins are all identified as oleanolane-type ，among which compound 1 is a new compound. The monodesmosidic saponins ，the sugar chain of which attached at C- 3 and a free carboxyl at C- 28， possess stronger antitumor activity than others.

The antitussive and expectorant mechanism of Platycodon total saponins based on metabonomics / 药学学报

UHPLC-Q-TOF/MS metabonomics technology was used to clarify the metabolic regulation pathways by which Platycodon total saponins (PTS) exert antitussive and expectorant effects in a mouse cough model, in which coughing is induced by concentrated ammonia, and in a phenol red excretion model. After approval by the Experimental Animal Ethics Committee of Jiangxi University of Chinese Medicine (Approval No. JZLLSC-20190235), the mice were randomly divided into a normal group, a model group, a positive drug group and a PTS group. Endogenous metabolites in mouse serum were identified by UHPLC-Q-TOF/MS. Principal component analysis (PCA) and orthogonal partial least squares discriminant analysis (OPLS-DA) were used for multivariate analysis. Metabolic pathways were analyzed by the Metaboanalyst platform. The results show that PTS can significantly prolong the cough latent period and cough frequency of mice, and significantly increase phenol red excretion. UHPLC-Q-TOF/MS identified 19 metabolites related to cough, and PTS significantly decreased 16 of them; 17 metabolites related to expectoration were identified, and PTS decreased the levels of all. Metabolic pathway analysis showed that linoleic acid metabolism, arachidonic acid metabolism and glycerophospholipid metabolism were the main pathways involved in serum metabolite changes in this mouse cough model. Linoleic acid metabolism, phenylalanine, tyrosine and tryptophan biosynthesis, arachidonic acid metabolism, phenylalanine metabolism and α-linolenic acid metabolism were the main pathways involved in serum metabolite changes in the phenol red excretion model. This study is the first to elucidate the regulation of antitussive and expectorant metabolic pathways and the effect of PTS on these pathways.

Three new triterpenoid saponins from Aralia echinocaulis / 中草药·英文版

Objective: To study the active ingredients in the root bark of Aralia echinocaulis. Methods: Three triterpenoid saponins were separated from the 70% ethanol extracts and purified by column chromatography and their structures were determined by spectroscopic analysis. Compound 1 and 3 were evaluated for antioxidant activity by the in vitro DPPH free radical scavenging ability and the protective effect of OH

Antiglycation, antioxidant, antiacne, and photoprotective activities of crude extracts and triterpene saponin fraction of Sapindus saponaria L. fruits: An in vitro study

Objective: To evaluate the photoprotective, antioxidant, antiglycation, and antiacne activities of crude extract (CESs) and triterpene saponin fraction (TSSs) of Sapindus saponaria. Methods: HPLC-MS purification was performed on a Symmetry TM C18 column. The saponins were identified by a UV detector. Antioxidant activity was evaluated by DPPH and O 2 - radicals scavenging, and FRAP and TBARS assays. Glycation activity was assessed by relative electrophoretic mobility and inhibition of advanced glycation end products (AGEs) formation. Additionally, antiacne activity was determined by inhibition of Cutibacterium acnes, and photoprotective effect was evaluated by Mansur's method. Results: Most of the triterpene saponins detected in the fraction by HPLC-MS analysis were hederagenin as the aglycon. CESs and TSSs presented varying antioxidant activity in DPPH (CESs: 75.69% and TSSs: 83.65%), FRAP (CESs: 425.39 μM TE/g DW and TSSs: 649.36 μM TE/g DW), TBARS (CESs: 42.96% and TSSs: 52.16%) and O 2 - radicals scavenging (CESs: 61.33% and TSSs: 86.69%) tests. CESs and TSSs also exhibited antiglycation activity comparable to bovine serum albumin treated with aminoguanidine. In addition, CESs and TSSs showed inhibition of AGE formation (34.48% and 61.85%, respectively). Antiacne activity against Cutibacterium acnes was observed with a minimum inhibitory concentration equal to minimum bactericidal concentration (CESs: 36.11 μg/mL and TSSs: 18.34 μg/mL). In photoprotective assays, CESs and TSSs showed maximum absorbance of 1.42 to 0.20 and 2.80 to 1.30, respectively, in the wavelength range of 260 to 400 nm. Furthermore, CESs and TSSs showed sun protection factors of 8.89 and 14.89, respectively. Conclusions: Sapindus saponaria fruit extracts show strong antioxidant potential and antiglycation activity against bovine serum albumin glycation and AGE formation. Besides, they presented antibacterial activity against Cutibacterium acnes and photoprotective effect against UV-A and UV-B.

Evaluation of phytochemicals and antioxidant activity of gamma irradiated quinoa (Chenopodium quinoa) / Avaliação de fitoquímicos e atividade antioxidante de quinoa gama irradiada (Chenopodium quinoa)

Abstract Phytochemical and antioxidant activity of quinoa flour was evaluated after subjected to gamma irradiation processes at dose 3 and 6 kGy. Both non-irradiated and irradiated quinoa samples were subjected to successive extractions in ethanol solvent. The antioxidant activity after gamma irradiation treatment was investigated via Ferric reducing antioxidant power (FRAP) and radical-scavenging activity (RSA) using 2,2-diphenyl-1-picrylhydrazyl (DPPH).Total phenolic and flavonoid content were analyzed using Folin-Ciocalteu micro-method, aluminium chloride (AlCl3) method and High Performance Liquid Chromatography (HPLC). As well as, effect of irradiation treatment on saponin was also evaluated. Irradiation treatment showed slight differences in the saponin content after exposure to 3 and 6 kGy. Irradiation process enhanced both total phenolic content (TPC) and Total flavonoid content (TFC), TPC were 34.52 and 30.92 mg Gallic Acid Equivalent (GAE)/100g compared to 26.25 mg GAE/100g in non-irradiated quinoa. TFC were 67.44 and 62.89 mg Quercetin Equivalents (QE)/100g compared to 53.15 mg QE/100g. Irradiation dose 3 kGy significantly (p> 0.05) decreased the IC50 as DPPH-RSA and increased the FRAP.

Resumo Atividades fitoquímica e antioxidante da farinha de quinoa foram analisadas após submissão a processos de irradiação gama nas doses 3 e 6 kGy. As amostras de quinoa não irradiadas e irradiadas foram submetidas a extrações sucessivas em solvente etanol. A atividade antioxidante, após o tratamento com irradiação gama, foi investigada por meio do poder antioxidante redutor férrico (ARF) e da atividade de eliminação de radicais (AER) usando 2,2-difenil-1-picril-hidrazil (DPPH). O conteúdo fenólico total e o teor de flavonoide foram analisados usando o método de Folin-Ciocalteu, método de cloreto de alumínio (AlCl3) e cromatografia líquida de alta eficiência (CLAE). Além disso, o efeito do tratamento de irradiação na saponina também foi avaliado. O tratamento por irradiação não mostrou diferenças significativas no conteúdo de saponina após exposição a 3 e 6 kGy. O processo de irradiação aumentou o conteúdo fenólico total (CFT) e o teor total de flavonoides (TTF); o CFT foi de 34,52 e 30,92 mg de equivalente de ácido gálico (EAG) / 100 g em comparação com 26,25 mg de EAG / 100 g na quinoa não irradiada. Os TTF foram 67,44 e 62,89 mg de equivalentes de quercetina (EQ) / 100 g em comparação com 53,15 mg de EQ / 100 g. A dose de irradiação de 3 kGy diminuiu significativamente (p > 0,05) o IC50 como DPPH-AER e aumentou o ARF.

Simultaneous quantitative analysis of nine saponins in Gynostemma pentaphyllum before and after heat processing based on UPLC-Q-Trap-MS / 中国中药杂志

Heat-processed Gynostemma pentaphyllum has strong biological activity, and saponins are the main components. To investigate the changes of saponins in G. pentaphyllum before and after heat processing, the present study determined and analyzed the content of nine saponins in G. pentaphyllum from Zhangzhou of Fujian and Jinxiu of Guangxi by ultra-high performance liquid chromatography with quadrupole ion-trap mass spectrometry(UPLC-Q-Trap-MS). The separation of the analytes was performed on an ACQUITY UPLC BEH C_(18) column(2.1 mm×50 mm, 1.7 μm) at 30 ℃, with acetonitrile and 0.1% formic acid in water as the mobile phase by gradient elution, and the flow rate was 0.3 mL·min~(-1). Quantitative analysis was performed using electrospray ionization source(ESI) in the multiple reaction-monitoring(MRM) mode. The results showed that the content of saponins with biological activities increased after heat processing. Specifically, gypenoside L, gypenoside LI, damulin A, damulin B, ginsenoside Rg_3(S), and ginsenoside Rg_3(R) in G. pentaphyllum produced in Zhangzhou of Fujian increased by 7.369, 8.289, 12.155, 7.587, 0.929, and 1.068 μg·g~(-1), respectively, while the content of ginsenoside Rd, gypenoside LVI, and gypenoside XLVI, which were abundant in the raw materials, decreased by 0.779, 19.37, and 9.19 μg·g~(-1), respectively. The content of gypenoside L, gypenoside LI, damulin A, damulin B, ginsenoside Rg_3(S), and ginsenoside Rg_3(R) in G. pentaphyllum produced in Jinxiu of Guangxi increased by 0.100, 0.161, 0.317, 0.228, 3.280, and 3.395 μg·g~(-1), respectively, while the content of ginsenoside Rd, gypenoside LVI, and gypenoside XLVI in the raw materials was reduced by 1.661, 0.014, and 0.010 μg·g~(-1), respectively. The results suggest that heat processing is an effective way to transform rare gypenosides. Furthermore, it is found that there are great differences in the content of gypenosides in different regions.

Chikusetsu saponin Ⅳa ameliorates myocardial hypertrophy of rats through regulating expression of miR199a-5p/Atg5 / 中国中药杂志

The present study investigated the effects of chikusetsu saponin Ⅳa(CHS Ⅳa) on isoproterenol(ISO)-induced myocardial hypertrophy in rats and explored the underlying molecular mechanism. ISO was applied to establish a rat model of myocardial hypertrophy, and CHS Ⅳa(5 and 15 mg·kg~(-1)·d~(-1)) was used for intervention. The tail artery blood pressure was measured. Cardiac ultrasound examination was performed. The ratio of heart weight to body weight(HW/BW) was calculated. Morphological changes in the myocardial tissue were observed by HE staining. Collagen deposition in the myocardial tissue was observed by Masson staining. The mRNA expression of myocardial hypertrophy indicators(ANP and BNP), autophagy-related genes(Atg5, P62 and beclin1), and miR199 a-5 p was detected by qRT-PCR. Atg5 protein expression was detected by Western blot. The results showed that the model group exhibited increased tail artery blood pressure and HW/BW ratio, thickened left ventricular myocardium, enlarged myocardial cells, disordered myocardial fibers with widened interstitium, and a large amount of collagen aggregating around the extracellular matrix and blood vessels. ANP and BNP were largely expressed. Moreover, P62 expression was up-regulated, while beclin1 expression was down-regulated. After intervention by CHS Ⅳa at different doses, myocardial hypertrophy was ameliorated and autophagy activity in the myocardial tissue was enhanced. Meanwhile, miR199 a-5 p expression declined and Atg5 expression increased. As predicted by bioinformatics, Atg5 was a target gene of miR199 a-5 p. CHS Ⅳa was capable of preventing myocardial hypertrophy by regulating autophagy of myocardial cells through the miR-199 a-5 p/Atg5 signaling pathway.

A novel dammarane-type saponin from Gynostemma pentaphyllum and its neuroprotective effect / 中国中药杂志

One new and two known dammarane-type saponins were isolated from the leaves of Gynostemma pentaphyllum using various chromatographic methods. Their structures were identified by HR-ESI-MS,~( 1)H-NMR, ~(13)C-NMR, 2 D-NMR spectra as 2α,3β,12β,20,24(S)-tetrahdroxydammar-25-en-3-O-[β-D-glucopyranosyl(1→2)-β-D-glucopyranosyl]-20-O-β-D-xylopyranosyl(1→6)-β-D-glucopyranoside(1, a new compound, namely gypenoside J5) and 2α,3β,12β,20,24(R)-tetrahdroxydammar-25-en-3-O-[β-D-glucopyranosyl(1→2)-β-D-glucopyranosyl]-20-O-β-D-xylopyranosyl(1→6)-β-D-glucopyranoside(2) and 2α,3β,12β,20-tetrahydroxy-25-hydroperoxy-dammar-23-en-3-O-[β-D-glucopyranosyl(1→2)][β-D-glucopyranosyl]-20-O-[β-D-xylopyranosyl(1→6)]-β-D-glucopy-ranoside(3), respectively. Compounds 1 and 2 were a pair of C-24 epimers. All compounds showed weak cytotoxicity agxinst H1299, HepG2, PC-3, SH-SY5 Y cancer cell lines. However, they exerted protective effect against SH-SY5 Y cellular damage induced by H_2O_2 dose-dependently, of which compound 1 displayed the strongest antioxidant effect. The present study suggested that G. pentaphyllum has antioxidative potential and the saponins from G. pentaphyllum are considered as the active compounds with neuroprotecitve effect.

Qualitative analysis of Gynostemma longipes for medicinal usage / 中国中药杂志

The Qinling-Daba Mountains area is the main producing areas of Gynostemma longipes for medicinal usage, and samples of wild whole plants in Pingli, Shaanxi Province and Qingchuan, Sichuan Province were collected. The ultra-high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry(UHPLC-Q-TOF-MS~E) was used to profile the chemical compositions and analyze the similarities and differences of G. longipes samples in these areas. Based on the accurate molecular weight and fragment information obtained from Q-TOF-MS~E, the structures of the main components were identified by combining with the mass spectra, chromatographic behaviors of reference standards and related literatures. The results showed that the components of wild G. longipes from different places among Qinling-Daba Mountains area were similar. Forty-five chemical components were identified in the whole plant of G. longipes from Pingli, Shaanxi Province, including 43 triterpenoid saponins and 2 flavonoids which contain all main peaks in its fingerprint. The main components are dammarane-type triterpenoid saponins, such asgypenoside ⅩLⅨ, gypenoside A and its malonylated product of glycosyl.