Antiliver Fibrosis Screening of Active Ingredients from Apium graveolens L. Seeds via GC-TOF-MS and UHPLC-MS/MS

Although several studies have been performed on Apium graveolens L.(celery) seeds, their antiliver fibrosis effects remain to be unexplored. Firstly, we detected the effects of celery seeds extracted with different concentrations of aqueous ethanol on the proliferation of HSC-LX2 cells. Then, we detected the effects of fractions of the optimal effect extract on the proliferation and apoptosis of HSC-LX2 cells. Finally, the compounds of petroleum ether (PP), ethyl acetate (PE), n-butyl alcohol (PB), and water fractions (PW) of the optimal effect extract were determined by GC-TOF-MS and UHPLC-MS/MS, to confirm the potentially antifibrotic compounds combined with pharmacodynamic experiment of monomer compounds in vitro. The results revealed that 60% ethanol extract of celery seeds (60-extract) exhibited remarkable inhibition effect on the proliferation of HSC-LX2 cells compared with 95% ethanol and aqueous extract. Besides, it validated that the inhibition rates of PP, PE, PB, and PW on the proliferation of HSC-LX2 cells were 75.14%, 73.52%, 54.09%, and 43.36%, and their percentage of apoptotic cells were 37.5%, 4.3%, 0.7%, and 0.1% at high doses, respectively. Additionally, it was manifested that apigenin, aesculetin, and butylphthalide have major contribution to the overall compounds of celery seeds, and the inhibition effects on the cell proliferation clearly elevated with increase in their contents. In essence, apigenin, aesculetin, and butylphthalide may hopefully become the natural products of antiliver fibrosis, which laid a foundation for the subsequent development of celery seeds as antiliver fibrosis drugs.

Download Full-text

IN VITRO INHIBITION OF CELERY (Apium graveolens L.) EXTRACT ON THE ACTIVITY OF XANTHINE OXIDASE AND DETERMINATION OF ITS ACTIVE COMPOUND

Indonesian Journal of Chemistry ◽

10.22146/ijc.21338 ◽

2012 ◽

Vol 12 (3) ◽

pp. 247-254 ◽

Cited By ~ 3

Author(s):

Dyah Iswantini ◽

Tuti Hayati Ramdhani ◽

Latifah K Darusman

Keyword(s):

Xanthine Oxidase ◽

Ethanol Extract ◽

Ultraviolet Spectrum ◽

Apium Graveolens ◽

Active Compounds ◽

In Vitro Method ◽

Inhibition Effect ◽

The One

The objective of this study was to determine the inhibition effect of celery extracts toward xanthine oxidase by in vitro method, and its active compounds. Roots and herb of celery were extracted using water and ethanol solvents. Results indicated that the herbal ethanol extract had the highest inhibition effect (91.40%) at 1400 ppm. The components contained in the herbal ethanol extract were then separated by column chromatography using the best eluent (chloroform : ethyl acetate at 7:3). All of the fractions had inhibition effect greater than 50%. The fraction number 4 was the one with the highest inhibition effect followed by fraction 5 with inhibition percentage of both fractions at 200 ppm were 88.62 and 85.44%, respectively. The analysis of the ultraviolet spectrum of fraction 4 showed the presence of π-π* transition which was resulted by the aromatic C=C, -OH, and C-O chromophores, and also showing the n-σ* transition which was given by -C=O chromophore. The infrared spectrum analysis indicated the presence of aromatic -C=C, -OH, and C=O functional groups. Based on the phytochemical assay and both instrumental spectrums, it was thought that the active compounds of fraction 4 and 5 were in the flavonoid group.

Download Full-text

In Vivo Effect of Suloctidil as an Antiplatelet Agent

Thrombosis and Haemostasis ◽

10.1055/s-0038-1646799 ◽

1979 ◽

Vol 41 (03) ◽

pp. 465-474 ◽

Cited By ~ 7

Author(s):

Marcia R Stelzer ◽

Thomas S Burns ◽

Robert N Saunders

Keyword(s):

Ex Vivo ◽

Antiplatelet Agent ◽

Ratio Method ◽

Platelet Aggregate ◽

Permanent Effect ◽

Platelet Aggregates ◽

5 Ht Uptake ◽

High Doses

SummaryThe relationship between the effects of suloctidil in vivo as an antiplatelet agent and in vitro as a modifier of platelet serotonin (5-HT) parameters was investigated. Suloctidil was found to be effective in reducing platelet aggregates formation in the retired breeder rat as determined using the platelet aggregate ratio method (PAR) with an ED50 of 16.1 mg/kg 24 hours post administration. In contrast to the hypothesis that 5-HT depletion is involved in the anti-aggregatory mechanism of suloctidil, no correlation was found between platelet 5- HT content and this antiplatelet activity. Reduction of platelet 5-HT content required multiple injections of high doses (100 mg/kg/day) of suloctidil. Suloctidil administration for 8 days at 100 mg/kg/day, which lowered platelet 5-HT content by 50%, resulted in no permanent effect on ex vivo platelet 5-HT uptake or thrombin-induced release, nor alteration in the plasma 5-HT level. However, these platelets exhibited a short-lived, significant increase in percent leakage of 5-HT after 30 minutes of incubation. Therefore, suloctidil treatment at high doses may with time result in platelet 5-HT depletion, however this effect is probably not related to the primary anti-aggregatory activity of the drug.

Download Full-text

Daunorubicin and Platelet Function

Thrombosis and Haemostasis ◽

10.1055/s-0038-1650125 ◽

1981 ◽

Vol 45 (01) ◽

pp. 038-042 ◽

Cited By ~ 9

Author(s):

M E Pogliani ◽

R Fantasia ◽

G Lambertenghi-Deliliers ◽

E Cofrancesco

Keyword(s):

Electron Microscope ◽

Cellular Membrane ◽

Hemorrhagic Diathesis ◽

Clot Retraction ◽

Freezing And Thawing ◽

Platelet Factor ◽

High Doses ◽

Very High ◽

Platelet Functions

SummaryThe influence of Daunorubicin on some platelet functions in vitro was investigated, using different concentrations of the drug (0.01-0.02-0.04 μg/ml). Daunorubicin was shown to inhibit Collagen and Thrombin induced platelet aggregation and the intensity of inhibition depended on both drug concentration and the time of preincubation.Daunorubicin was also shown to inhibit the release reaction, the platelet prostaglandin pathway and the availability platelet factor 3; the drug at concentrations for clinical use does not damage the platelet membrane, as is the case with the freezing and thawing test, in platelet uptake of 14C-serotonin and as confirmed by the electron microscope. When very high doses (0.16 mg) of Daunorubicin are used, lysis of the platelets can be observed and this is confirmed under the electron microscope by the presence of empty platelets with fractures at the level of the cytoplasmic membrane.Finally, Daunorubicin causes irreversible inhibition of reptilase clot-retraction, even if this is less severe than with Vincristine. Working with gel-filtered platelets, it would appear that the inhibition exercised by the drug on platelet reactions is not caused through modifications in Ca++ metabolism.The authors suggest that Daunorubicin, at the dosages used clinically, induces in vitro thrombocytopathy without damaging the cellular membrane as confirmed by the electron microscope.This impairment of platelet functions could play a part in hemorrhagic diathesis observed during Daunorubicin therapy.

Download Full-text

Effects of Two Different Doses of Hirudin on APTT, Determined with Eight Different Reagents

Thrombosis and Haemostasis ◽

10.1055/s-0038-1653754 ◽

1995 ◽

Vol 73 (02) ◽

pp. 219-222 ◽

Cited By ~ 4

Author(s):

Manuel Monreal ◽

Luis Monreal ◽

Rafael Ruiz de Gopegui ◽

Yvonne Espada ◽

Ana Maria Angles ◽

...

Keyword(s):

Ex Vivo ◽

Anticoagulant Activity ◽

Subcutaneous Administration ◽

In Vitro Study ◽

Ex Vivo Model ◽

Suitable Candidate ◽

Significant Prolongation ◽

High Doses ◽

Different Doses

SummaryThe APTT has been considered the most suitable candidate to monitor the anticoagulant activity of hirudin. However, its use is hampered by problems of standardization, which make the results heavily dependent on the responsiveness of the reagent used. Our aim was to investigate if this different responsiveness of different reagents when added in vitro is to be confirmed in an ex vivo study.Two different doses of r-hirudin (CGP 39393), 0.3 mg/kg and 1 mg/kg, were administered subcutaneously to 20 New Zealand male rabbits, and the differences in prolongation of APTT 2 and 12 h later were compared, using 8 widely used commercial reagents. All groups exhibited a significant prolongation of APTT 2 h after sc administration of hirudin, both at low and high doses. But this prolongation persisted 12 h later only when the PTTa reagent (Boehringer Mannheim) was used. In general, hirudin prolonged the APTT most with the silica- based reagents.In a further study, we compared the same APTT reagents in an in vitro study in which normal pooled plasma was mixed with increasing amount of hirudin. We failed to confirm a higher sensitivity for silica- containing reagents. Thus, we conclude that subcutaneous administration of hirudin prolongs the APTT most with the silica-based reagents, but this effect is exclusive for the ex vivo model.

Download Full-text

Hypolipidemic and Hepatic Steatosis Preventing Activities of the Wood Ear Medicinal Mushroom Auricularia auricula-judae (Higher Basidiomycetes) Ethanol Extract In Vivo and In Vitro

International Journal of Medicinal Mushrooms ◽

10.1615/intjmedmushrooms.v17.i8.30 ◽

2015 ◽

Vol 17 (8) ◽

pp. 723-734 ◽

Cited By ~ 9

Author(s):

Md.Ahsanur Reza ◽

Md. Akil Hossain ◽

Dereje Damte ◽

Woo-Sik Jo ◽

Walter H. Hsu ◽

...

Keyword(s):

Hepatic Steatosis ◽

Ethanol Extract ◽

Medicinal Mushroom ◽

Auricularia Auricula

Download Full-text

Phytochemical composition and antioxidant activity of Malus baccata (L.) Borkh. fruits

Food Science and Applied Biotechnology ◽

10.30721/fsab2020.v3.i1.46 ◽

2020 ◽

Vol 3 (1) ◽

pp. 47

Author(s):

Nadezhda Petkova ◽

Manol Ognyanov ◽

Blaga Inyutin ◽

Petar Zhelev ◽

Panteley Denev

Keyword(s):

Phenolic Compounds ◽

Antioxidant Activities ◽

Ethanol Extract ◽

Titratable Acidity ◽

Total Phenolic ◽

Total Phenolic Compounds ◽

Frap Assay ◽

Phytochemical Composition ◽

Malus Baccata

Crab apple (Malus baccata (L.) Borkh.) was mainly distributed in Europe as an ornamental plant, but the nutritional properties of its edible fruits were not fully revealed. The aim of the current study was to characterize the phytochemical composition of ripen carb apple fruits and to evaluate their nutritional and antioxidant potentials. The fruits were assayed for moisture and ash content, proteins, lipids, carbohydrates, titratable acidity (TA), pH, total phenolic compounds and natural pigments. Among the analyzed carbohydrates cellulose was found in the highest content (6% dw), followed by sugars (sucrose, glucose and fructose) and 1.8 % dw uronic acids. The total chlorophylls and carotenoids contents in their fruits were 6.51 and 4.80 μg/g fw, respectively. Total monomeric anthocyanins were not detected. The highest content of total phenolic compounds (2.67 mg GAE/g fw) was found in 95 % ethanol extract from fruits, while the total flavonoids were relatively low – 0.1 mg QE/g fw. DPPH assay (17.27 mM TE/g fw) and FRAP assay (14.34 mM TE/g fw) demonstrated in vitro antioxidant activities of crabapple. Malus baccata fruits were evaluated as a rich source of dietary fibers and phenolic compounds with significant antioxidant potential that could be used in human nutrition.

Download Full-text

Polyphenols of leaves of Apium graveolens inhibit in vitro protein glycation and protect RINm5F cells against methylglyoxal-induced cytotoxicity

Functional Foods in Health and Disease ◽

10.31989/ffhd.v8i3.399 ◽

2018 ◽

Vol 8 (3) ◽

pp. 193 ◽

Cited By ~ 2

Author(s):

Rosa Martha Perez Gutierrez ◽

Alethia Muñiz-Ramirez ◽

Abraham Heriberto Garcia Campoy ◽

Jose Maria Mota Flores ◽

Sergio Odin Flores

Keyword(s):

Therapeutic Potential ◽

Health Benefits ◽

Protein Glycation ◽

Apium Graveolens ◽

Ionization Mass ◽

Intensity Level ◽

Edible Plants ◽

Rinm5f Cells ◽

Protein Carbonyl Content

Background: The health benefits of edible plants have been widely investigated and disseminated. However, only polyphenols have been found to have sufficient therapeutic potential to be considered in clinical trials. Fewer manuscripts have other applications such as prospective health benefits and disease treatment. Other components of edible plants are responsible for a range of other benefits including antimalarial, burns, flu, cancer, inflammation, diabetes, glycation, antimicrobial, prevention of neurodegeneration, analgesic, antimigraine activity, sedative activities, etc. Accordingly, the public needs to be informed of the potential edible plants have to act on different targets and maintain better control over diabetes compared to commercial drugs which can be toxic, have side effects, do not have the capacity to maintain blood glucose at normal levels, and do not protect the patient from the complications of diabetes over time. Consequently, edible plants, such as Apium graveolen, which have therapeutic targets on AGEs formation, are potentially a better alternative treatment for diabetes.Methods: The leaves of celery were extracted with methanol (CM). Polyphenols contents in CM were investigated by liquid chromatography-electrospray ionization mass. The ability of the compounds to inhibit formation of AGEs was evaluated in vitro models using formation of AGE fluorescence intensity, level of fructosamine, Nε-(carboxymethyl)lysine (CML), methylglyoxal (MG)-derived protein, and formation of amyloid cross β structure. Protein-oxidation was determined by thiol group and protein carbonyl content. Inhibition of MG-derived AGEs and MG-trapping ability were also measured. Additionally, insulin production was determined in methylglyoxal-treated pancreatic RINm5F cells assay. Results: Apigenin, kaempferol, apiin, rutin, caffeic acid, ferulic acid, chlorogenic acid, coumaroylquinic acid, and p-coumaric acid were the major polyphenols contained in CM. In all the model tests CM displayed potent AGE inhibitory activity, suggesting that CM delayed the three stages of glycation. Accordingly, the mechanisms of action of celery involving dicarbonyl trapping and breaking the crosslink structure in the AGEs formed may contribute to the protection of pancreatic RINm5F cells against MG conditions.Conclusion: These findings indicate that CM have an excellent anti-glycation effect which may be beneficial for future development of antiglycating agents for the treatment of diabetes.Keywords: Apium graveolens, anti-glycation, polyphenols methylglyoxal, insulin, pancreatic cells

Download Full-text

EKSTRAK KULIT BUAH MANGGIS (Garcinia Mangostana L.) SEBAGAI OBAT ANTI DIARE

Jurnal Penelitian Farmasi & Herbal ◽

10.36656/jpfh.v2i1.195 ◽

2019 ◽

Vol 2 (1) ◽

pp. 9-13

Author(s):

Zaim Anshari ◽

Chrismis Novalinda Ginting ◽

Linda Chiuman ◽

Yuliani Mardiati Lubis

Keyword(s):

Blood Vessels ◽

Smooth Muscles ◽

Latin Square ◽

Ethanol Extract ◽

Garcinia Mangostana ◽

Pharmacology And Toxicology ◽

The Difference ◽

North Sumatra ◽

Papaverine Hydrochloride

This study aims to determine whether mangosteen rind extract (in the form of ethanol extract/EE) can be used as an anti-diarrhea drug after compared with other anti-diarrhea substances in three experimental groups. This research is an in vitro experimental study using adult male guinea pigs weighing 400-600 gr through the standard method of Magnus with the Latin square controlled experiment design. The study was conducted at the Pharmacology and Toxicology Laboratory of the Faculty of Pharmacy, University of North Sumatra. The results showed that the contraction of ileum in Ach with Atp + Ach compared the difference in contraction of ileum Ach with EE + Ach showed the difference in difference between the two contractions of the ileum was significant, the contraction of ileum in His with Dip + His compared indifference in contraction of ileum His with EE + His showed a difference indifference. the two ileal contractions are significant, the ileal contraction in the bar with Papa + Bar compared to the difference between the ileum bar contraction with EE + Bar shows no difference in the difference between the two ileum contractions. The conclusion is that the Mangosteen Skin Ethanol Extract works similarly to Papaverine Hydrochloride which is an antidiarrheal drug used to relax smooth muscles so that it can also make blood vessels dilate by relaxing smooth muscles in the walls of blood vessels.

Download Full-text

Anti-Mycobacterial Peroxides: A New Class of Agents for Development Against Tuberculosis

Medicinal Chemistry ◽

10.2174/1573406415666190430143535 ◽

2020 ◽

Vol 16 (3) ◽

pp. 392-402

Author(s):

Christiaan W. van der Westhuyzen ◽

Richard K. Haynes ◽

Jenny-Lee Panayides ◽

Ian Wiid ◽

Christopher J. Parkinson

Keyword(s):

Subsequent Development ◽

Antitubercular Activity ◽

Organic Peroxide ◽

New Drugs ◽

Skeletal Myoblast ◽

Artemisinin Derivatives ◽

Malaria Therapy ◽

New Class ◽

Alternative Approach

Background: With few exceptions, existing tuberculosis drugs were developed many years ago and resistance profiles have emerged. This has created a need for new drugs with discrete modes of action. There is evidence that tuberculosis (like other bacteria) is susceptible to oxidative pressure and this has yet to be properly utilised as a therapeutic approach in a manner similar to that which has proven highly successful in malaria therapy. Objective: To develop an alternative approach to the incorporation of bacterial siderophores that results in the creation of antitubercular peroxidic leads for subsequent development as novel agents against tuberculosis. Methods: Eight novel peroxides were prepared and the antitubercular activity (H37Rv) was compared to existing artemisinin derivatives in vitro. The potential for toxicity was evaluated against the L6 rat skeletal myoblast and HeLa cervical cancer lines in vitro. Results: The addition of a pyrimidinyl residue to an artemisinin or, preferably, a tetraoxane peroxidic structure results in antitubercular activity in vitro. The same effect is not observed in the absence of the pyrimidine or with other heteroaromatic substituents. Conclusion: The incorporation of a pyrimidinyl residue adjacent to the peroxidic function in an organic peroxide results in anti-tubercular activity in an otherwise inactive peroxidic compound. This will be a useful approach for creating oxidative drugs to target tuberculosis.

Download Full-text