An unprecedented pair of Z/E isomeric pyridinium compound from the aqueous extract of Aspongopus chinensis Dallas / 药学学报

A novel pair of Z/E isomeric compounds with unprecedented carbon skeleton were isolated from an aqueous extract of Aspongopus chinensis Dallas by macroporous resin, silica gel, and semi-preparative high performance liquid chromatography (HPLC). Their structures were identified by nuclear magnetic resonance (NMR), Infrared spectroscopy (IR), Mass spectroscopy (MS) and other spectroscopic methods as (Z)-3-(but-1″-en-1″-yl)-1-(2ʹ-hydroxyethyl)-4-propylpyridin-1-ium, namely aspongopyridine A, and (E)-3-(but-1″-en-1″-yl)-1-(2ʹ-hydroxyethyl)-4-propylpyridin-1-ium, namely aspongopyridine B, respectively. Besides, the anti-inflammatory, anti-tumor, acetylcholinesterase inhibition and butyrylcholinesterase inhibition activities of the compounds 1 and 2 were evaluated. The results showed that compounds 1 and 2 have no anti-inflammatory, anti-tumor, and butyrylcholinesterase inhibition activities instead of weak acetylcholinesterase inhibition activity.

Phytochemical Investigation and in Vitro Antioxidant Activity of Panchavalkala Bark Extracts

Natural antioxidants have an important role in the prevention of many age-related diseases and promotion of health. Among natural antioxidants from plants, flavonoids and other phenolic compounds are potent antioxidants and chelating agents. Panchavalkala the barks of five trees i.e. Nyagrodha (Ficus benghalensis L.), Udumbara (Ficus racemosa L.), Ashwatha (Ficus religiosa L.), Plaksha (Ficus virens Aiton) and Parisha (Thespesia populnea (L.)Sol.ex Correa) are also known as Pancha Ksheeri Vrikshas in use since Vedic period. Barks of these trees are dried in shade and are used for different formulations (Pancha Kashaya Kalpanas), in different pathological conditions, especially as wound healing, gynecological disorders and etc. The plant samples were extracted using ethanol and water, and subjected for the phytochemical analysis. It was confirmed that samples contain many biologically active compounds like flavonoids, polyphenols, tannins, alkaloids, glycosides and terpinoids etc. The marker compound of each trial drug and the quantitative analysis has been carried out by high performance liquid chromatography. The antioxidant study was done by using in vitro method 1, 1­-diphenyl-2-picryl-hydrazyl (DPPH) radical scavenging assay. The marker compounds caffeic acid and gallic acid were quantified in each extract for their quality and efficacy. PVK barks showed high free radical scavenging activity as evidenced by the low IC50 values in DPPH (EE PVK- 20.46µg/ml, AE PVK-37.79µg/ml, EE T.poulenea-22µg/ml, AE T. poulenia- 23.31µg/ml AE F. benghalensis- 25.53µg/ml, EE F. benghalensis- 26.23µg/ml, EE F. religiosa - 34µg/ml). Quercetin- IC50 value 4.026µg/ml is used as standard. The results of the study demonstrated that PVK barks possess phyto-constituent’s viz. tannins, flavonoids, polyphenols etc. and has potential antioxidant activity. Thus these barks have good therapeutic potential as natural antioxidant and might be used in life style related conditions like hyperlipidemia, diabetes, obesity, cardiovascular disorders and etc.

Minor triterpenoid acids from an aqueous extract of Uncaria rhynchophylla / 药学学报

Seventeen minor triterpenoid acids (1-17) were isolated from an aqueous decoction of Uncaria rhynchophylla by a combinatory application of column chromatography using multiple stationary phases, including macroporous adsorbent resin, MCI resin, Sephadex LH-20, Toyopearl HW-40C, silica gel, and C18 reversed phase silica gel, combined with separation techniques of flash chromatography (FC) and high performance liquid chromatography (HPLC). Their structures were determined by analysis of HR-ESI-MS, UV, CD, and IR as well as 1D and 2D NMR spectroscopic data, of which eight new compounds (1-8) are named successively uncarinic acids Q-X, while the structures of 2 and 7 were confirmed by single crystal X-ray diffraction. In the in vitro assays, 27-hydroxyolean-12-en-28-oic acid (17) inhibited TGF-β-induced HSC-T6 cell activation at the concentration of 5 μmol·L-1.

Dimeric phthalides from an aqueous extract of the Angelica sinensis root head / 药学学报

Ten dimeric phthalide racemates (1-10) were isolated from an aqueous extract of the Angelica sinensis root head (Guitou) by separation techniques of column chromatography over macroporous adsorbent resin, MCI resin, silica gel, and Sephadex LH-20, together with preparative thin-layer chromatography and reversed phase HPLC. The racemates were further separated into (+)-/(-)-1-(+)-/(-)-10 with chiral HPLC. Their structures including absolute configurations were elucidated by comprehensive analysis of spectroscopic data, combined with electronic circular dichroism (ECD) and NMR calculations as well as single crystal X-ray diffractions. Compounds (+)-/(-)-1-(+)-/(-)-10 are either new structure or new natural product, named (+)-/(-)-angelidipthalidic acids A-H [(+)-/(-)-1-(+)-/(-)-8] and (+)-/(-)-angelidipthalidols A and B [(+)-/(-)-9 and (+)-/(-)-10], respectively. Meanwhile, dimeric phthalide mono- and bis-lactone derivatives with 3.3′a,8.6′- and 3.6′,8.3′a-coupling patterns as well as determination of their relative configurations are discussed.

Monoterpenes from an aqueous extract of the Angelica sinensis root head / 药学学报

Eleven monoterpenes including seven new chemical structures or new natural products covering two pairs of scalemic enantiomers, together with four known analogues, were isolated from an aqueous extract of the Angelica sinensis root head (Guitou) by separation techniques of column chromatography over macroporous adsorbent resin, MCI resin, silica gel, Sephadex LH-20, and Toyopearl HW-40C, together with preparative thin-layer chromatography as well as reversed phase and chiral HPLC. Their structures were determined by spectroscopic data analysis, combined with theoretic calculation of electronic circular dichroism (ECD) spectra and single crystal X-ray diffraction. The new structures or new natural products named (+)-/(-)-angelinones A and B [(+)-/(-)-1 and (+)-/(-)-2], angelinones C and D (3 and 4), and angelinol A (5), respectively, while the known analogues were 6β,9-dihydroxy-(+)-α-pinene (6), 1,1,5-trimethyl-2-hydroxymethyl-cyclohexa-2,5-dien-4-one (7), jasminol E (8), and (+)-trans-sobrerol (9). All the isolates were reported in this plant for the first time, except for the previously reported 6 from an ethanol extract of the aerial parts of A. sinensis, of which the structure was confirmed by X-ray crystallography in this study.

Qualitative Analysis of Metabolites of Aristolochiae Fructus Aqueous Extract in Rats / 中国实验方剂学杂志

ObjectiveBased on ultra performance liquid chromatography-quadrupole-time-of-flight mass spectrometry（UPLC-Q-TOF-MSE） technique， we identified qualitatively the metabolites of aristolochic acid（AAs） in rat in order to analyze the metabolic differences between water extract of Aristolochiae fructus（AFE） and Aristolochic acid Ⅰ（AAⅠ）. MethodSD rats were selected and administered AFE（110 g·kg-1·d-1） or AAⅠ（5 mg·kg-1·d-1） by oral for 5 days， respectively. Serum， urine and feces were collected after administration. Through sample pretreatment， ACQUITY UPLC BEH C18 column（2.1 mm×100 mm， 1.7 μm） was used with the mobile phase of 0.01% formic acid methanol（A）-0.01% formic acid water（B， containing 5 mmol·L-1 ammonium acetate） for gradient elution（0-1 min， 10%B； 1-7 min， 10%-75%B； 7-7.2 min， 75%-95%B； 7.2-10.2 min， 95%B； 10.2-10.3 min， 95%-10%B； 10.3-12 min， 10%B） at a flow rate of 0.3 mL·min-1. Positive ion mode of electrospray ionization（ESI+） was performed in the scanning range of m/z 100-1 200. In combination with UNIFI 1.9.4.053 system， the Pathway-MSE was used to qualitatively analyze and identify the AAs prototype and related metabolites in biological samples（serum， urine and feces）， and to compare the similarities and differences of metabolites in rats in the subacute toxicity test between AFE group and AAⅠ group. ResultCompared with AAⅠ group， 6， 10， 13 common metabolites and 14， 20， 30 unique metabolites were identified in biological samples（serum， urine and feces） of AFE group， respectively. Moreover， the main AAs components always followed the metabolic processes of demethylation， nitrate reduction and conjugation. Compared with common metabolites in AAⅠ group， prototype components of AAⅠ in serum and most metabolic derivatives of AAⅠ［AAⅠa， aristolochic lactam Ⅰ（ALⅠ）a， 7-OHALⅠ and its conjugated derivatives］ in biological samples were significantly increased in AFE group（P<0.05， P<0.01）， except that the metabolic amount of ALⅠ in feces of AFE group was remarkably lowed than that of AAⅠ group（P<0.01）. In addition， a variety of special ALⅠ efflux derivatives were also identified in the urine and feces of the AFE group. ConclusionAlthough major AAs components in AFE all show similar metabolic rules as AAⅠ components in vivo， the coexistence of multiple AAs components in Aristolochiae Fructus may affect the metabolism of AAⅠ， and achieve the attenuating effect by increasing the metabolic effection of AAⅠ and ALⅠ.

Zanthoxylum bungeanum Aqueous Extract Treated Rheumatoid Arthritis by Inhibiting Synovial Cell Proliferation and Inducing Cell Apoptosis / 中国实验方剂学杂志

ObjectiveTo investigate the therapeutic effect of the water extract of Zanthoxylum bungeanum aqueous extract（ZBAE）on rheumatoid arthritis. MethodThe sixty SD rats were divided into normal group， model group ［complete Freund's adjuvant （CFA）， 10 mg·kg-1］， methotrexate（MTX） group （0.25 mg·kg-1）， low -， medium -， and high-dose ZBAE groups （90， 180， 360 mg·kg-1）. The rats in MTX group were given intraperitoneal injection for two weeks， three times a week， and the rats in ZBAE group were administrated for 14 days. The swelling of the ankle joint and body weight were observed， and arthritis scores were also performed. Computed tomography （CT）， hematoxylin-eosin （HE） staining and safranine-O and fast green staining were used to observe the effect of ZBAE on synovial hyperplasia and bone protection. Cell counting kit-8（CCK-8）method was used to detect the proliferation of the RA-FLSs cells treated with ZBAE. According to the results of CCK-8 experiment， the optimal concentration and time of administration were determined， blank group， low -， medium -， and high-dose ZBAE groups （0.08，0.10，0.12 g·L-1） were set up. The cell cycle distribution and apoptosis rate were analyzed by flow cytometry，the migration ability of RA-FLSs cells was examined by scratch test. Western blot was used to detect the effect of ZBAE on phosphatidylinositol 3-kinase （PI3K）， protein kinase B （Akt）， cyclin-dependent kinase 2 （CDK2）， Cyclin A and phosphorylated PI3K， Akt （p-PI3K，p-Akt） protein expression in RA-FLSs cells. ResultCompared with the normal group，joint swelling index and arthritis score were increased in the model group （P<0.05），the bone of the ankle was seriously damaged， and there was obvious synovial hyperplasia. Compared with the model group， the ZBAE group could significantly reduce the joint swelling index （P<0.05）， inhibit synovial hyperplasia and cartilage destruction. In vitro study showed that compared with the blank group， ZBAE could inhibit the migration of RA-FLSs （P<0.05）， promoted cell apoptosis （P<0.05）， and acted on RA-FLSs cells in S phase to inhibit cell proliferation. Moreover， the result of Western blot showed that compared with the blank group， the expression of p-PI3K， p-Akt， CDK2 and Cyclin A proteins were significantly decreased in the high dose group of ZBAE （P<0.05）. ConclusionThese results suggest that ZBAE has a therapeutic effect on rheumatoid arthritis by inhibiting synovial hyperplasia， promoting synovial apoptosis and inhibiting its migration.

Effect of superfine powder and aqueous extract of Polygonati Rhizoma on rats with natural perimenopausal syndrome / 中国中药杂志

This study aims to examine the effect of superfine powder and aqueous extract of Polygonati Rhizomaon on natural perimenopausal syndrome in rats and explore the underlying mechanism. To be specific, a total of 60 female SD rats(14-15 months old) with estrous cycle disorder were screened by the vaginal smear and randomized into model control group, β-estradiol 3-benzoate group(0.1 mg·kg~(-1)), superfine powder of Polygonati Rhizoma group(0.25, 0.5 g·kg~(-1)) and aqueous extract of Polygonati Rhizoma group(0.25, 0.5 g·kg~(-1)), and another 10 female SD rats(14-15 months old) were selected as the youth control group. The administration lasted 6 weeks. Then the perimenopausal syndrome-related indexes such as body temperature, microcirculatory blood flow of face and ear, vertigo period, salivary secretion, grip force, and bone strength were determined and open field test was conducted. The immune system-related indexes such as the wet weight and index of thymus and spleen, percentage of T lymphocytes and subgroups in peripheral blood, and hematological indexes were measured. In addition, the ovary-related indexes such as estrous cycle, the wet weight and index of uterus and ovary, ovarian tissue morphology, and cell apoptosis were determined. Moreover, hypothalamus-pituitary-ovary axis(HPO)-related indexes such as serum sex hormone levels, cytochrome P450 family 11 subfamily A member 1(CYP11A1), cytochrome P450 family 19 subfamily A member 1(CYP19A1), and cytochrome P450 family 17 subfamily A member 1(P450 17A1) in ovarian tissue were measured. The results showed that the superfine powder and aqueous extract of Polygonati Rhizoma significantly decreased body temperature(anal, facial and dorsal temperature), microcirculatory blood flow in the ear, and vertigo period, increased salivary secretion, grip force, bone strength, total distance and total speed in the open field test, wet weight and index of thymus and spleen, lymphocyte ratio, CD3~+ level, and CD4~+/CD8~+ ratio, reduced neutrophil number and ratio, estrous cycle disorder ratio, and number of ovarian apoptotic cells, raised wet weight and index of uterus, wet weight of ovary, levels of inhibin B(INHB), estradiol(E_2), anti-müllerian hormone(AMH), and ovarian CYP11A1 and CYP19A1, decreased follicle-stimulating hormone(FSH) and luteinizing hormone(LH) content, and improved ovarian tissue morphology. It is suggested that the superfine powder and aqueous extract of Polygonati Rhizoma can improve the symptoms associated with natural perimenopausal syndrome in rats and enhance ovarian function and immune function. The mechanism is that they regulate HPO axis function by increasing estrogen synthesis.

Effect of Euphorbia helioscopia Aqueous Extract on Chronic Obstructive Pulmonary Disease and Precancerous Lesion-associated Proteins of Lung Tissues in Mice Induced by Cigarette Smoke / 中国实验方剂学杂志

ObjectiveTo investigate the protective effect and mechanism of Euphorbia helioscopia aqueous extract （EHE） on mice with chronic obstructive pulmonary disease （COPD） and its influence on precancerous lesion-associated proteins in lung tissues induced by cigarette smoke （CS）. MethodThe COPD model was induced by CS in 60 mice and the model mice were randomly divided into control group， model group， positive drug group （dexamethasone， 2 mg·kg-1）， and low-， medium-， and high-dose EHE groups （1.875， 3.75， 7.5 g·kg-1）. The high-performance liquid chromatography （HPLC） method was used to determine the related components in EHE. The changes in end-expiratory pause （EEP）， airway resistance （Penh）， expiratory flow at 50% vital capacity （EF50）， and other pulmonary function indexes were detected by the spirometer. The levels of inflammatory factors， such as interleukin （IL）-2， IL-5， IL-18， IL-17A， and IL-27 in bronchoalveolar lavage fluid （BALF） of mice were detected by high-throughput liquid protein chip technology. Hematoxylin-eosin （HE） staining was used to detect the pathological changes in lung tissues in mice. The content of malondialdehyde （MDA）， myeloperoxidase （MPO）， and glutathione peroxidase （GSH-Px） in lung tissues was determined by the colorimetric method. The mRNA relative expression of tumor necrosis factor-α （TNF-α）， transforming growth factor-β （TGF-β）， matrix metalloproteinase-2 （MMP-2）， matrix metalloproteinase-9 （MMP-9）， and matrix metalloproteinase-12 （MMP-12） was detected by Real-time fluorescence quantitative polymerase chain reaction （Real-time PCR）. Immunohistochemistry （IHC） was used to detect the expression of tumor protein （P53） and cell proliferation-associated antigen （Ki67） in lung tissues， and Western blot was used to detect the relative expression of tumor suppressor protein （P16）， DNA （cytosine-5）-methyltransferase 1 （DNMT1）， and fragile histidine triad （FHIT） in lung tissues. ResultThe results showed that the main compounds in EHE included phenols （gallic acid and protocatechuic acid） and flavonoids （such as hyperoside， rutin， myricetin， naringenin， quercetin， luteolin， kaempferol， and licorice chalcone A）， among which gallic acid and rutin were the highest in content. Compared with normal group， model group showed increased levels of EEP， EF50， and Penh （P<0.05）， and showed increased MDA and MPO levels （P<0.01） and decreased GSH-Px （P<0.01）， and the model group displayed increased levels of IL-2， IL-5， IL-18， IL-17A， IL-27， TNF-α， TGF-β， MMP-2， MMP-9， and MMP-12 （P<0.05）. And the model group exhibited up-regulated expression of P53， Ki67， and FHIT in lung tissues （P<0.01） and down-regulated expression of DNMT1 and P16 （P<0.01）. Compared with model group， the EHE groups showed decreased EEP and EF50 levels （P<0.05）. The pathological injury of lung tissues in mice of the model group was observed under HE staining， and the pathological injury of basal cell hyperplasia of lung tissues was gradually improved after treatment with EHE. The EHE groups showed reduced levels of MDA and MPO （P<0.01） and increased GSH-Px （P<0.01）. The EHE groups displayed decreased levels of IL-2， IL-5， IL-18， IL-17A， IL-27， TNF-α， TGF-β， MMP-2， MMP-9， and MMP-12 （P<0.05）. And the EHE groups showed down-regulated Ki67 and FHIT in lung tissues （P<0.05） and up-regulated expression of P53 and DNMT1 （P<0.05）. ConclusionEHE can protect mice from COPD and inhibit precancerous lesions， and the mechanism may be related to the inhibition of inflammation and oxidative stress response， regulation of protease and antiprotease imbalance， and regulation of epithelial cell growth.

Monoterpenes and hexenol glycosides from an aqueous extract of Monochasma savatieri / 药学学报

Twelve compounds, including 5 new monoterpenes and 7 known derivatives, were isolated from a water decoction of Monochasma savatieri by column chromatography over macroporous adsorbent resin, MCI resin, Sephadex LH-20, and HW-40C, combined with preparative TLC, reversed phase HPLC, and flash column chromatographic techniques. Their structures were elucidated by comprehensive analysis of spectroscopic data, along with enzymatic hydrolysis as well as electronic circular dichroism (ECD) and NMR calculations, the new structures named monochaside I (1) and monochairidols A-D (2-5), respectively. The known compounds 6-12 were obtained from the Monochasma plants for the first time.

Acute toxicity study and phytochemical screening of Pterocarpus marsupium heartwood

Background: Conventionally, Ayurvedic herbs are being used to treat various diseases. These medicinal compounds have to be evaluated for their safety and presence of therapeutic compounds for the clinical application. Aims and Objectives: The present study was designed to obtain the scientific knowledge on the safety profile as well as to assess the presence of pharmacologically active principles in the Pterocarpus marsupium heartwood. Materials and methods: The aqueous extract of P. marsupium heartwood was subjected to an acute toxicity in albino rats. The animals were divided into four groups (n = 6) and fed with graded doses (1000, 2000, and 5000 mg/kg p.o.) of plant extract, respectively, whereas control group had received 2 ml distilled water orally. Animals were continuously observed for the toxicological symptoms for 2 h and intermittently for 48 h and latter once in a day for 14 days. The body weight of the animals was recorded. In addition, the qualitative phytochemical investigations were conducted to identify the presence of active principles. Results: The animals fed with aqueous extract of P. marsupium heartwood did not exhibit any toxic symptoms and the mortality. However, there was a significant (P < 0.05) dose-dependent change in the weight gain observed in comparison to the control group. The median lethal dose (LD50) of the plant extract was considered as >5000 mg/kg. Furthermore, the phytochemical investigations of the plant extract showed the presence of carbohydrates, flavonoids, triterpenoids, saponins, tannins and phenols. Conclusion: The aqueous extract of P. marsupium heartwood was found to be safe and well tolerated even at a large dose of 5000 mg/kg. Furthermore, the plant extract found to possess pharmacologically active principles having wide pharmacological spectrum. Hence, it can be preferred in various therapeutic conditions.

In vitroMeasurement of Anticoagulant Effect of Acacia Nilotica Aqueous Extract on Normal Human Plasma

Aims:To determine the anticoagulant effect of Acacia Nilotica aqueous extract on normal human plasma.Study Design:This is an experimental study.Place and Duration of the Study:Department of Haematology, Faculty of Medical Laboratory sciences, Alzaiem Alazhari, Khartoum –Sudan, during the period from July –August 2021. Methodology:A total of 20 human blood samples were collected for this study from apparently healthy subjects following ethical considerations. Samples were collected in tri-sodium citrate and platelets poor plasma (PPP) were immediately prepared by centrifugation. Aqueous solution of Acacia nilotica was prepared with distilled water (D.W), three concentrations of the solution (50%, 75% and 100%) were prepared. Prothrombin Time (PT) and Activated partial thromboplastin time (APTT) were tested by manual method before and after adding different concentrations of Acacia Nilotica solution. Statistical tests were performed by using SPSS version 16. Results:The results of study showed that Acacia Nilotica significantly prolonged the PT and APTT results of human plasma (Pvalues for 50%, 75% and 100% solutions were 0.000, 0.000 and 0.000 while for APTT 0.036, 0.000 and 0.000 for PT respectively). Also the study showed no significant correlation between control and A. nilotica concentrations among coagulation profile, except a significant positive correlation between control and 75% Acacia nilotica on APPT.Conclusion:Acacia Nilotica solutions had anticoagulant effect in human plasma, and could be nominated as a potential preventive agent for thromboembolic diseases

Rapid prediction of antioxidant activity in aqueous extract solutions of melastoma dodecandrum by ultraviolet spectroscopy / 药学实践杂志

Objective To establish a rapid prediction method of the antioxidant activity in aqueous extract solutions of Melastoma dodecandrum based on ultraviolet spectroscopy and partial least squares regression algorithm. Methods The DPPH free radical scavenging effect was used to characterize the antioxidant activity of aqueous extract solutions of Melastoma dodecandrum. The ultraviolet spectra of 190-600 nm were collected. The partial least squares regression model of antioxidant activity was established after optimizing the wavelength range and preprocessing method. The software was devised using Visual Basic as the integrated development environment to provide a convenient tool for the rapid determination of antioxidant activity. Results The optimal partial least squares regression model was established based on 200-290 nm as wavelength range and unit variance scaling as preprocessing method. The correlation coefficient of calibration, root mean square error of estimation, root mean square error of cross-validation was 0.887, 2.20% and 2.17%, respectively. The correlation coefficient of validation, root mean square error of prediction was 0.868, 2.08%. The average predicted recovery was 100.1±2.3%. With the predictive function in the software, the antioxidant activity of aqueous extract solution of Melastoma dodecandrum can be calculated automatically within 2 s after collecting the ultraviolet spectra. Conclusions This study provides a rapid method for the prediction of antioxidant activity in aqueous extract solutions of Melastoma dodecandrum.

Monoterpene glucosides from an aqueous extract of Monochasma savatieri / 药学学报

Eleven monoterpene glucosides were isolated from a water decoction of Monochasma savatieri by column chromatography over macroporous adsorbent resin, MCI resin, Sephadex LH-20, and HW-40C, combined with preparative TLC, reversed phase HPLC, and flash column chromatographic techniques. Their structures were elucidated by comprehensive analysis of spectroscopic data, along with acidic and enzymatic hydrolysis as well as electronic circular dichroism (ECD) and NMR calculations, including six new compounds (1-4, 7 and 8), named monochasides A-D, G and H, respectively. Comparing the reported data of 9-hydroxylinaloyl 3-O-β-D-glucoside (5), (6Z)-9-hydroxylinaloyl 3-O-β-D-glucoside (6), and kankanoside D1 (9) with those obtained in this study, the absolute configurations of 6 and 9 were proved for the first time. Other two compounds were identified as 8-hydroxygeraniol 1-O-β-D-glucopyranoside (10) and 8-hydroxygeraniol 8-O-β-D-glucopyranoside (11), respectively.

Potential hepatoprotective effect of Cheatomorpha gracilis extract against High Fat Diet (HFD)-Induced Liver Damage, and its characterization by HPLC / Efeito hepatoprotetor potencial do extrato de Cheatomorpha gracilis contra dano hepático induzido por dieta alta em gordura (HFD), e sua caracterização por HPLC

The current investigation was carried out to estimate the protective effect of aqueous extract of Cheatomorpha gracilis (AEC) against High fat Diet (HFD) induced liver damage in mice. The results of the in vitro study showed that AEC have higher antioxidant capacities in the DPPH and hydroxyl radical-scavenging assays. Indeed, many phenolic compounds (gallic acid, quercetin, naringenin, apigenin, kaempferol and rutin) were identified in the AEC. In the animal studies, during 6 weeks, HFD promoted oxidative stress with a rise level of malonaldehyde (MDA), protein carbonyls (PCOs) levels and a significant decrease of the antioxidant enzyme activities such as superoxide dismutase, catalase and glutathione peroxidase. Interestingly, the treatment with AEC (250 mg/kg body weight) significantly reduced the effects of HFD disorders on some plasmatic liver biomarkers (AST, ALT and ALP) in addition to, plasmatic proteins inflammatory biomarkers (α2 and β1 decreases / β2 and γ globulins increases). It can be suggest that supplementation of MECG displays high potential to quench free radicals and attenuates high fat diet promoted liver oxidative stress and related disturbances.

A presente investigação foi realizada para estimar o efeito protetor do extrato aquoso de Cheatomorpha gracilis (AEC) contra o dano hepático induzido por dieta rica em gordura (HFD) em camundongos. Os resultados do estudo in vitro mostraram que os AEC têm maiores capacidades antioxidantes nos ensaios DPPH e de eliminação de radicais hidroxila. De fato, muitos compostos fenólicos (ácido gálico, quercetina, naringenina, apigenina, kaempferol e rutina) foram identificados no AEC. Nos estudos em animais, durante 6 semanas, HFD promoveu estresse oxidativo com aumento do nível de malonaldeído (MDA), níveis de proteína carbonil (PCOs) e diminuição significativa das atividades de enzimas antioxidantes como superóxido dismutase, catalase e glutationa peroxidase. Curiosamente, o tratamento com AEC (250 mg / kg de peso corporal) reduziu significativamente os efeitos dos distúrbios de HFD em alguns biomarcadores hepáticos plasmáticos (AST, ALT e ALP), além de biomarcadores inflamatórios de proteínas plasmáticas (reduções α2 e β1 / β2 e γ aumenta as globulinas). Pode-se sugerir que a suplementação de MECG apresenta alto potencial para extinguir os radicais livres e atenua o estresse oxidativo do fígado promovido pela dieta rica em gordura e distúrbios relacionados.

Potential Hepatoprotective Effect of Cheatomorpha gracilis extract against High Fat Diet (HFD)-Induced Liver Damage, and its characterization by HPLC

Abstract The current investigation was carried out to estimate the protective effect of aqueous extract of Cheatomorpha gracilis (AEC) against High fat Diet (HFD) induced liver damage in mice. The results of the in vitro study showed that AEC have higher antioxidant capacities in the DPPH and hydroxyl radical-scavenging assays. Indeed, many phenolic compounds (gallic acid, quercetin, naringenin, apigenin, kaempferol and rutin) were identified in the AEC. In the animal studies, during 6 weeks, HFD promoted oxidative stress with a rise level of malonaldehyde (MDA), protein carbonyls (PCOs) levels and a significant decrease of the antioxidant enzyme activities such as superoxide dismutase, catalase and glutathione peroxidase. Interestingly, the treatment with AEC (250 mg/kg body weight) significantly reduced the effects of HFD disorders on some plasmatic liver biomarkers (AST, ALT and ALP) in addition to, plasmatic proteins inflammatory biomarkers (2 and 1 decreases / 2 and globulins increases). It can be suggest that supplementation of MECG displays high potential to quench free radicals and attenuates high fat diet promoted liver oxidative stress and related disturbances.

Resumo A presente investigação foi realizada para estimar o efeito protetor do extrato aquoso de Cheatomorpha gracilis (AEC) contra o dano hepático induzido por dieta rica em gordura (HFD) em camundongos. Os resultados do estudo in vitro mostraram que os AEC têm maiores capacidades antioxidantes nos ensaios DPPH e de eliminação de radicais hidroxila. De fato, muitos compostos fenólicos (ácido gálico, quercetina, naringenina, apigenina, kaempferol e rutina) foram identificados no AEC. Nos estudos em animais, durante 6 semanas, HFD promoveu estresse oxidativo com aumento do nível de malonaldeído (MDA), níveis de proteína carbonil (PCOs) e diminuição significativa das atividades de enzimas antioxidantes como superóxido dismutase, catalase e glutationa peroxidase. Curiosamente, o tratamento com AEC (250 mg / kg de peso corporal) reduziu significativamente os efeitos dos distúrbios de HFD em alguns biomarcadores hepáticos plasmáticos (AST, ALT e ALP), além de biomarcadores inflamatórios de proteínas plasmáticas (reduções 2 e 1 / 2 e aumenta as globulinas). Pode-se sugerir que a suplementação de MECG apresenta alto potencial para extinguir os radicais livres e atenua o estresse oxidativo do fígado promovido pela dieta rica em gordura e distúrbios relacionados.

Potential Hepatoprotective Effect of Cheatomorpha gracilis extract against High Fat Diet (HFD)-Induced Liver Damage, and its characterization by HPLC / Efeito Hepatoprotetor Potencial do Extrato de Cheatomorpha gracilis contra Dano Hepático Induzido por Dieta Alta em Gordura (HFD), e sua caracterização por HPLC

The current investigation was carried out to estimate the protective effect of aqueous extract of Cheatomorpha gracilis (AEC) against High fat Diet (HFD) induced liver damage in mice. The results of the in vitro study showed that AEC have higher antioxidant capacities in the DPPH and hydroxyl radical-scavenging assays. Indeed, many phenolic compounds (gallic acid, quercetin, naringenin, apigenin, kaempferol and rutin) were identified in the AEC. In the animal studies, during 6 weeks, HFD promoted oxidative stress with a rise level of malonaldehyde (MDA), protein carbonyls (PCOs) levels and a significant decrease of the antioxidant enzyme activities such as superoxide dismutase, catalase and glutathione peroxidase. Interestingly, the treatment with AEC (250 mg/kg body weight) significantly reduced the effects of HFD disorders on some plasmatic liver biomarkers (AST, ALT and ALP) in addition to, plasmatic proteins inflammatory biomarkers (α2 and ß1 decreases / ß2 and γ globulins increases). It can be suggest that supplementation of MECG displays high potential to quench free radicals and attenuates high fat diet promoted liver oxidative stress and related disturbances.

A presente investigação foi realizada para estimar o efeito protetor do extrato aquoso de Cheatomorpha gracilis (AEC) contra o dano hepático induzido por dieta rica em gordura (HFD) em camundongos. Os resultados do estudo in vitro mostraram que os AEC têm maiores capacidades antioxidantes nos ensaios DPPH e de eliminação de radicais hidroxila. De fato, muitos compostos fenólicos (ácido gálico, quercetina, naringenina, apigenina, kaempferol e rutina) foram identificados no AEC. Nos estudos em animais, durante 6 semanas, HFD promoveu estresse oxidativo com aumento do nível de malonaldeído (MDA), níveis de proteína carbonil (PCOs) e diminuição significativa das atividades de enzimas antioxidantes como superóxido dismutase, catalase e glutationa peroxidase. Curiosamente, o tratamento com AEC (250 mg / kg de peso corporal) reduziu significativamente os efeitos dos distúrbios de HFD em alguns biomarcadores hepáticos plasmáticos (AST, ALT e ALP), além de biomarcadores inflamatórios de proteínas plasmáticas (reduções α2 e ß1 / ß2 e γ aumenta as globulinas). Pode-se sugerir que a suplementação de MECG apresenta alto potencial para extinguir os radicais livres e atenua o estresse oxidativo do fígado promovido pela dieta rica em gordura e distúrbios relacionados.

Effect of Aqueous Extract of Trametes robiniophila on Proliferation of Human Prostate Cancer VCaP Cells / 中国实验方剂学杂志

ObjectiveTo investigate effect of aqueous extract of Trametes robiniophila （TRM，Huaier） on autophagy of human prostate cancer VCaP cells and Lamin B1 expression， so as to uncover its role in the proliferation of VCaP cells. MethodThe inhibitory effect of 0， 2， 4， 6， 8， 10 g·L-1 TRM aqueous extract on the proliferation of human prostate cancer VCaP cells at different time points were determined by cell counting kit-8 （CCK-8） assay. Acridine orange staining was conducted for analyzing the effect of TRM aqueous extract on the formation of autolysosomes in VCaP cells. After medication， the expression of microtubule-associated protein Ⅰ light chain 3 （LC3）， autophagy-related protein 3 （Atg3）， autophagy-related protein 5 （Atg5）， and autophagy-related protein 7 （Atg7） in VCaP cells were detected by Western blot. The effect of TRM aqueous extract alone and its combination with autophagy inhibitor bafilomycin A1 on the proliferation of VCaP cells were assayed by CCK-8 assay. RNA interference technology was used to explore the role of Lamin B1 in anti-proliferation of VCaP cells by TRM. ResultCompared with the blank group， TRM aqueous extract inhibited the proliferation of human prostate cancer VCaP cells in a time- and concentration-dependent manner （P<0.01）. Acridine orange staining showed that TRM aqueous extract promoted the formation of autolysosomes in VCaP cells. As revealed by Western blotting， TRM aqueous extract up-regulated the expression levels of LC3-Ⅱ， Atg3， Atg5， and Atg7 in contrast to those in the blank group （P<0.05）. All these indicated that TRM aqueous extract induced the autophagy of VCaP cells. In addition， autophagy inhibition impaired the sensitivity of VCaP cells to TRM aqueous extract （P<0.05）. The comparison with the blank group showed that TRM aqueous extract inhibited Lamin B1 protein expression in VCaP cells （P<0.01）， which in turns weakened the sensitivity of VCaP cells to TRM aqueous extract. ConclusionTRM aqueous extract inhibited the proliferation of human prostate cancer VCaP cells possibly by inducing autography and down-regulating Lamin B1 expression. This study has provided a theoretical basis for the clinical application of TRM.

Anticoccidial effect of Origanum majoranum aqueous extract on Eimeria tenella-infected chicken

@#Avian coccidiosis, an important protozoal disease of chicken triggered by coccidian protozoa of genus Eimeria, causes considerable economic losses to broiler producers. The study was designed to assess the efficiency of Origanum majoranum aqueous extract (OMAE) on E. tenella-infected broiler chicken. Birds were divided into four groups including: positive control (PC, challenged with 5×104 sporulated oocysts of E. tenella at the 12th day of age), PC+OMAE (challenged with E. tenella oocysts at the 12th day of age and received OMAE (125 mg/kg BW) orally, started at the 7th day of age, and continued for 14 consecutive days), OMAE (received OMAE (125 mg/kg BW) orally, at the 7th day of age, for 14 consecutive days), and negative control (received basal diet only). Anticoccidial efficacy of OMAE was evaluated by complete blood picture, serum chemistry, serum protein electrophoresis, antioxidants markers, cecal oocysts count, and cecal lesions score. Briefly, collected data indicated that supplementation of OMAE could increase antioxidants concentrations and improve changes in hematobiochemical parameters and serum protein fractions, as well as decrease cecal oocysts count and reduce cecal lesion scores in E. tenella-infected birds. In conclusion, OMAE restores oxidant-antioxidant balance, and its supplementation in broiler chicken can alleviate E. tenella-infection and reduce its severity.

Extract from Modified Xiao Xianxiongtang Inhibits Epithelial-mesenchymal Transition and Invasion and Migration Mediated by TGF-β1 of Human Gastric Cancer MGC-803 Cells via Wnt5a/Ca2+/NFAT Signaling Pathway / 中国实验方剂学杂志

Objective:This studu aims to investigate the effect of aqueous extract of modified Xiao Xianxiongtang on the epithelial mesenchymal transition（EMT） and the change of its invasion and migration ability of human gastric cancer MGC-803 cells mediated by transforming growth factor-<italic>β</italic>₁（TGF-<italic>β</italic>₁），and to explore the mechanism of regulating Wnt5a/Ca²⁺/ activated T-cell nuclear factor（NFAT） signaling pathway to inhibit EMT and invasion and metastasis of MGC-803 cells. Method:TGF-<italic>β</italic>₁（10 μg·L^-1）was used to induce EMT and the invasion and metastasis model of human gastric cancer MGC-803 cells. Transwell chamber experiment， scratchhealing experiment， Western blot and immunofluorescence assay were used to detect cell invasion and migration ability， expression of EMT marker protein and key protein expression of Wnt5a/Ca²⁺/NFAT signaling pathway， and intracellular Ca²⁺ concentration. Result:Compared with the blank group， TGF-<italic>β</italic>₁ could significantly enhance the invasion and migration ability of MGC-803 cells（<italic>P</italic><0.01）， down-regulate the level of E-cadherin（<italic>P</italic><0.01）， up-regulate protein expressions of N-cadherin， Snail and Vimentin（<italic>P</italic><0.01）， and induce cell Wnt5a， calcineurin （CaN）， total protein of activated T-cell nuclear factor 1（NFAT1）， up-regulation of phosphorylated proteins p-NFAT1 and NFAT1 nucleoprotein and intracellular accumulation of Ca²⁺（<italic>P</italic><0.01）. Compared with the TGF-<italic>β</italic>₁ group， modified Xiao Xianxiongtang （10， 20， 40 mg·L^-1） could significantly inhibit this phenomenon，and 40 mg·L^-1 had the best effect（<italic>P</italic><0.05，<italic>P</italic><0.01）.The specific inhibitors of Wnt5a/Ca²⁺/NFAT signaling pathway （<italic>R</italic>）-（+）-Bay-K-8644 and modified Xiao Xianxiongtang （40 mg·L^-1） could significantly inhibit theinvasion and migration of MGC-803 cells mediated by TGF-<italic>β</italic>₁， up-regulate the level of E-cadherin， and down-regulate expressions of N-cadherin， Snail， Vimentin， Wnt5a， CaN and NFAT1 proteins and reduce the intracellular accumulation of Ca²⁺（<italic>P</italic><0.05，<italic>P</italic><0.01）.Moreover， （<italic>R</italic>）-（+）-Bay-K-8644 combined with modified Xiao Xianxiongtang （40 mg·L^-1） had stronger inhibitory effect（<italic>P</italic><0.05，<italic>P</italic><0.01）. Conclusion:These results suggest that modified Xiao Xianxiongtang can inhibit the EMT mediated by TGF-<italic>β</italic>₁ via Wnt5a/Ca²⁺/NFAT signaling pathway，thereby reducing the invasion and migration ability of MGC-803 cells.