scholarly journals Assessment of Antidepressant Effect of the Aerial Parts of Micromeria myrtifolia Boiss. & Hohen on Mice

Molecules ◽  
2019 ◽  
Vol 24 (10) ◽  
pp. 1869 ◽  
Author(s):  
Esra Küpeli Akkol ◽  
Fatma Tuğçe Gürağaç Dereli ◽  
Mert Ilhan
Keyword(s):  
Rosmarinic Acid ◽  
Antidepressant Activity ◽  
Reversed Phase ◽  
Experimental Models ◽  
Antidepressant Effect ◽  
Significant Activity ◽  
Meoh Extract ◽  
Aerial Parts

The currently available antidepressant agents necessitate the development of newer alternatives because of their serious adverse effects and costs. Traditional medicinal knowledge is likely the key that opens the door to discover new medicines. In Turkish folk medicine, the infusion prepared from aerial parts of Micromeria myrtifolia Boiss. & Hohen is used as pleasure and medicinal tea for its relaxing action. The present research was conceived to confirm the antidepressant’s potential of this traditional medicinal plant. In this process, first of all, the collected and shade-dried aerial parts of M. myrtifolia were powdered and then, extracted using solvents with different polarity as follows; n-hexane, ethyl acetate (EtOAc), and methanol (MeOH). The antidepressant activity of the extracts was evaluated by using several in vivo and in vitro experimental models of depression. When the data obtained from the control and experimental groups were compared, it was determined that the MeOH extract was the most active. The active components of this extract were isolated and identified utilizing various chromatographic separation techniques. The MeOH extract was applied to reversed phase (RP-18) column chromatography to obtain five main fractions and they were tested on antidepressant activity models. The isolated compounds from the obtained fractions were elucidated as rosmarinic acid (1), myricetin (2), apigenin (3), and naringenin (4) which were assumed to be responsible for the antidepressant activity of the aerial parts. According to the results, rosmarinic acid, myricetin, apigenin, and naringenin showed statistically significant activity on forced swimming test and tetrabenazine-induced ptosis models, whereas only rosmarinic acid showed statistically significant activity on the tail suspension test. Apigenin displayed the highest inhibitory activity on MAO A and B enzymes. Studies in the future should be performed to investigate the antidepressant activity mechanism of these natural compounds. The current research could be an important step in the development of the new agents that can be used in the treatment of depression.

scholarly journals Antidepressant Potential of Lotus corniculatus L. subsp. corniculatus: An Ethnobotany Based Approach

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1299
Author(s):  
Fatma Tuğçe Gürağaç Dereli ◽  
Haroon Khan ◽  
Eduardo Sobarzo-Sánchez ◽  
Esra Küpeli Akkol
Keyword(s):  
Antidepressant Activity ◽  
Tail Suspension Test ◽  
Lotus Corniculatus ◽  
Antidepressant Effect ◽  
In Vivo Test ◽  
Aerial Parts ◽  
Test Models ◽  
Bioassay Guided Fractionation

As a Turkish traditional medicinal plant, aerial parts of Lotus corniculatus L. subsp. corniculatus (Fabaceae) are used as a painkiller, antihemoroidal, diuretic and sedative. In this study, the antidepressant potential of the plant has been attempted to clarify. Extracts with water, n-Hexane, ethyl acetate, and methanol were prepared respectively from the aerial parts. Antidepressant activity of the extracts were researched by using three different in vivo test models namely a tail suspension test, antagonism of tetrabenazine-induced hypothermia, ptosis, and suppression of locomotor activity and forced swimming test on male BALB/c mice and in vitro monoamine oxidase (MAO)-A and B inhibition assays. The results were evaluated through comparing with control and reference groups, and then active compounds of the active extract have been determined. Bioassay-guided fractionation of active fraction led to the isolation of three compounds and structures of the compounds were elucidated by spectroscopic methods. The data of this study demonstrate that the MeOH extract of the aerial parts of the plant showed remarkable in vivo antidepressant effect and the isolated compounds medicarpin-3-O-glucoside, gossypetin-3-O-glucoside and naringenin-7-O-glucoside (prunin) from the active sub-fractions could be responsible for the activity. Further mechanistic and toxicity studies are planned to develop new antidepressant-acting drugs.

scholarly journals Antinociceptive Activity and Redox Profile of the Monoterpenes (+)-Camphene, p-Cymene, and Geranyl Acetate in Experimental Models

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Lucindo Quintans-Júnior ◽  
José C. F. Moreira ◽  
Matheus A. B. Pasquali ◽  
Soheyla M. S. Rabie ◽  
André S. Pires ◽  
...  
Keyword(s):  
Free Radical ◽  
Antinociceptive Effect ◽  
Experimental Models ◽  
Geranyl Acetate ◽  
No Production ◽  
Significant Activity ◽  
High Doses ◽  
Antioxidant Effects

Objective. To evaluate antinocicpetive and redox properties of the monoterpenes (+)-camphene, p-cymene, and geranyl acetate in in vivo and in vitro experimental models. Methods. Evaluation of the in vitro antioxidant activity of (+)-camphene, p-cymene, and geranyl acetate using different free radical-generating systems and evaluation of antinociceptive actions by acetic acid-induced writhing and formalin-induced nociception tests in mice. Results. p-Cymene has the strongest antinociceptive effect, but (+)-camphene and geranyl acetate also present significant activity at high doses (200 mg/kg). (+)-Camphene had the strongest antioxidant effect in vitro at TBARS and TRAP/TAR assays and also had the highest scavenging activities against different free radicals, such as hydroxyl and superoxide radicals. Sodium nitroprussiate-derived NO production was enhanced by (+)-camphene. Geranyl acetate and p-cymene also presented some antioxidant effects, but with a varying profile according the free radical-generating system studied. Conclusion. (+)-Camphene, p-cymene, and geranyl acetate may present pharmacological properties related to inflammation and pain-related processes, being potentially useful for development of new therapeutic strategies, with limited possibilities for p-cymene and geranyl acetate.

Anti-inflammatory, Antinociceptive, and Antioxidant Potentials of Algerian Zizyphus jujuba Mill. Fruits and Leaves In Vivo and In Vitro in Different Experimental Models

2019 ◽  
Author(s):  
N. Gadiri ◽  
C. Tigrine ◽  
Z. Lakache ◽  
A. Kameli
Keyword(s):  
Antioxidant Properties ◽  
Experimental Models ◽  
Protective Capacity ◽  
Aerial Parts ◽  
Antioxidant Agents ◽  
Zizyphus Jujuba ◽  
Anti Inflammatory ◽  
Dpph Scavenging

The ethanolic extracts of the aerial parts, leaves, and fruits, of Zizyphus jujuba Mill. were studied in vivo and in vitro for their anti-inflammatory, analgesic, and antioxidant properties, respectively. A preliminary phytochemical screening was carried out. It revealed the presence of several phytoconstituents such as flavonoids, phenols, and alkaloids. The acute toxicity study was conducted using a limit dose of 2,000mg/kg. The extracts studied showed no signs of toxicity or mortality. Anti-inflammatory activity, assessed by carrageenan-induced paw edema, and antinociceptive activity, assessed by pain-induced acetic acid in mice, were significantly reduced (P < 0.001). Moreover, both extracts showed considerable DPPH scavenging activity and β-carotene protective capacity. The present study suggests that leaf and fruit extracts from Zizyphus jujuba have a pharmacological interest probably related to the presence of some bioactive compounds and could be a potential source of antiinflammatory, antinociceptive, and antioxidant agents that should be further investigated.

RP-HPLC-UV-ESI-MS phytochemical analysis of fruits of Conocarpus erectus L.

2014 ◽  
Vol 68 (10) ◽  
Author(s):  
El-Sayed Abdel-Hameed ◽  
Salih Bazaid ◽  
Mohamed Shohayeb
Keyword(s):  
Antioxidant Properties ◽  
Reversed Phase ◽  
In Vivo Studies ◽  
Phytochemical Analysis ◽  
Meoh Extract ◽  
Esi Ms ◽  
Conocarpus Erectus ◽  
Rp Hplc

AbstractPrevious work revealed that the defatted methanol (MeOH) extract of fruits of Conocarpus erectus L. (Combretaceae family) exhibited antioxidant, antibacterial and anti-cancer activities. In further studies of this valuable plant, the defatted MeOH extract of C. erectus fruits was subjected to chromatographic fractionation in a silica gel glass column followed by reversed-phase high-performance liquid chromatography-ultraviolet-electrospray ionisation spectrometry analysis (RP-HPLC-UV-ESI-MS). The major and sharp peaks in each sample were identified or tentatively identified based on matching with some standard compounds and a review of the literature. Ellagic acid, vescalagin/castalagin isomer and di-(hexahydroxy diphenoyl) galloyl hexose isomer were tentatively identified as major components with many hydrolysable types of tannins on the basis of a comparison of its mass patterns with relevant items in the literature. Gallic acid, kaempferol 3-O-β-d-glucopyranoside and quercetin 3-O-β-d-glucopyranoside were identified on the basis of matching retention time (t R) and mass spectra with the standards. Polymethoxylated flavonoid isomers were also tentatively identified. The antioxidant properties of all samples were found to be associated with the total content of phenolic compounds. This may be considered as the first detailed phytochemical report in identifying the phytochemicals in C. erectus fruits. Due to the high antioxidant activity exhibited by both the crude MeOH extract and its fractions, it could be used as an effective natural antioxidant after further in vitro and in vivo studies.

scholarly journals Comparative Study of the in vitro Bioactivities of Bupleurum rigidum and B. fruticescens

2012 ◽  
Vol 7 (6) ◽  
pp. 1934578X1200700
Author(s):  
Jose M. Prieto ◽  
Makanjuola O. Ogunsina ◽  
Andrea Novak ◽  
Amit Joshi ◽  
Judit Kokai ◽  
...  
Keyword(s):  
Free Radical ◽  
Comparative Study ◽  
Radical Scavenging ◽  
Experimental Models ◽  
Free Radical Scavenging ◽  
Significant Activity ◽  
Aerial Parts ◽  
Melanoma B16f10 ◽  
Phytochemical Profile

Decoctions of the aerial parts of either Bupleurum rigidum or B. fruticescens are equally used in certain parts of Spain for the treatment of topical and musculoskeletal inflammations. In the present paper, their phytochemical profile and pharmacological value has been compared. After chromatographic and spectral analyses we could establish the presence of rutin and absence of chlorogenic acid in B. fruticescens, whilst the contrary applies to B. rigidum, providing a means to chemically differentiate extracts and dry materials from the two species. Their free radical scavenging and antiperoxidative activities were similar, with B. fruticescens being more active overall. The infusions of both Bupleurum species also showed similar anti-inflammatory activity when tested by NF-κB assay (40% and 42% at 60 μg·mL−1), as well as in a hexosaminidase exocytosis assay (30% at 50 μg·mL−1). Antimigratory effects on rat melanoma B16F10 showed significant activity for both infusions, with B. rigidum twice as potent as B. fruticescens, the activity of the latter not being fully explained by its content of rutin. Taking all these results together, we can conclude that, in the selected experimental models, there exist an in vitro bioequivalence of the infusions from both species, which is in agreement with the majority of ethnopharmacological reports.

Neutralization of a Low Molecular Weight Heparin (LHN-1) and Conventional Heparin by Protamine Sulfate in Rats

1986 ◽  
Vol 56 (03) ◽  
pp. 318-322 ◽  
Author(s):  
V Diness ◽  
P B Østergaard
Keyword(s):  
Molecular Weight ◽  
Low Molecular Weight Heparin ◽  
Thrombus Formation ◽  
Experimental Models ◽  
Protamine Sulfate ◽  
Low Molecular Weight ◽  
Antithrombotic Effect ◽  
Higher Doses

SummaryThe neutralization of a low molecular weight heparin (LHN-1) and conventional heparin (CH) by protamine sulfate has been studied in vitro and in vivo. In vitro, the APTT activity of CH was completely neutralized in parallel with the anti-Xa activity. The APTT activity of LHN-1 was almost completely neutralized in a way similar to the APTT activity of CH, whereas the anti-Xa activity of LHN-1 was only partially neutralized.In vivo, CH 3 mg/kg and LHN-1 7.2 mg/kg was given intravenously in rats. The APTT and anti-Xa activities, after neutralization by protamine sulfate in vivo, were similar to the results in vitro. In CH treated rats no haemorrhagic effect in the rat tail bleeding test and no antithrombotic effect in the rat stasis model was found at a protamine sulfate to heparin ratio of about 1, which neutralized APTT and anti-Xa activities. In LHN-1 treated rats the haemorrhagic effect was neutralized when APTT was close to normal whereas higher doses of protamine sulfate were required for neutralization of the antithrombotic effect. This probably reflects the fact that in most experimental models higher doses of heparin are needed to induce bleeding than to prevent thrombus formation. Our results demonstrate that even if complete neutralization of APTT and anti-Xa activities were not seen in LHN-1 treated rats, the in vivo effects of LHN-1 could be neutralized as efficiently as those of conventional heparin. The large fall in blood pressure caused by high doses of protamine sulfate alone was prevented by the prior injection of LHN-1.

Antimicrobial peptides for the treatment of pulmonary tuberculosis, allies or foes?

2018 ◽  
Vol 24 (10) ◽  
pp. 1138-1147
Author(s):  
Bruno Rivas-Santiago ◽  
Flor Torres-Juarez
Keyword(s):  
Pulmonary Tuberculosis ◽  
Antimicrobial Peptides ◽  
Experimental Models ◽  
New Drugs ◽  
World Health ◽  
Public Health Issue ◽  
Health Organization ◽  
Drug Resistant Strains

Tuberculosis is an ancient disease that has become a serious public health issue in recent years, although increasing incidence has been controlled, deaths caused by Mycobacterium tuberculosis have been accentuated due to the emerging of multi-drug resistant strains and the comorbidity with diabetes mellitus and HIV. This situation is threatening the goals of World Health Organization (WHO) to eradicate tuberculosis in 2035. WHO has called for the creation of new drugs as an alternative for the treatment of pulmonary tuberculosis, among the plausible molecules that can be used are the Antimicrobial Peptides (AMPs). These peptides have demonstrated remarkable efficacy to kill mycobacteria in vitro and in vivo in experimental models, nevertheless, these peptides not only have antimicrobial activity but also have a wide variety of functions such as angiogenesis, wound healing, immunomodulation and other well-described roles into the human physiology. Therapeutic strategies for tuberculosis using AMPs must be well thought prior to their clinical use; evaluating comorbidities, family history and risk factors to other diseases, since the wide function of AMPs, they could lead to collateral undesirable effects.

Epithelial Organotypic Cultures: A Viable Model to Address Mechanisms of Carcinogenesis by Epitheliotropic Viruses

2018 ◽  
Vol 18 (4) ◽  
pp. 246-255 ◽  
Author(s):  
Lara Termini ◽  
Enrique Boccardo
Keyword(s):  
Three Dimensional ◽  
Cell Types ◽  
Experimental Models ◽  
Biological Research ◽  
Specific Gene ◽  
Specific Cell ◽  
Organotypic Cultures ◽  
Skin Physiology

In vitro culture of primary or established cell lines is one of the leading techniques in many areas of basic biological research. The use of pure or highly enriched cultures of specific cell types obtained from different tissues and genetics backgrounds has greatly contributed to our current understanding of normal and pathological cellular processes. Cells in culture are easily propagated generating an almost endless source of material for experimentation. Besides, they can be manipulated to achieve gene silencing, gene overexpression and genome editing turning possible the dissection of specific gene functions and signaling pathways. However, monolayer and suspension cultures of cells do not reproduce the cell type diversity, cell-cell contacts, cell-matrix interactions and differentiation pathways typical of the three-dimensional environment of tissues and organs from where they were originated. Therefore, different experimental animal models have been developed and applied to address these and other complex issues in vivo. However, these systems are costly and time consuming. Most importantly the use of animals in scientific research poses moral and ethical concerns facing a steadily increasing opposition from different sectors of the society. Therefore, there is an urgent need for the development of alternative in vitro experimental models that accurately reproduce the events observed in vivo to reduce the use of animals. Organotypic cultures combine the flexibility of traditional culture systems with the possibility of culturing different cell types in a 3D environment that reproduces both the structure and the physiology of the parental organ. Here we present a summarized description of the use of epithelial organotypic for the study of skin physiology, human papillomavirus biology and associated tumorigenesis.

scholarly journals In Silico Predicted Antifungal Peptides: In Vitro and In Vivo Anti-Candida Activity

2021 ◽  
Vol 7 (6) ◽  
pp. 439
Author(s):  
Tecla Ciociola ◽  
Walter Magliani ◽  
Tiziano De Simone ◽  
Thelma A. Pertinhez ◽  
Stefania Conti ◽  
...  
Keyword(s):  
In Silico ◽  
Mammalian Cells ◽  
Galleria Mellonella ◽  
Ex Vivo ◽  
Consensus Sequence ◽  
In Silico Analysis ◽  
Significant Activity ◽  
Synthetic Antibody

It has been previously demonstrated that synthetic antibody-derived peptides could exert a significant activity in vitro, ex vivo, and/or in vivo against microorganisms and viruses, as well as immunomodulatory effects through the activation of immune cells. Based on the sequence of previously described antibody-derived peptides with recognized antifungal activity, an in silico analysis was conducted to identify novel antifungal candidates. The present study analyzed the candidacidal and structural properties of in silico designed peptides (ISDPs) derived by amino acid substitutions of the parent peptide KKVTMTCSAS. ISDPs proved to be more active in vitro than the parent peptide and all proved to be therapeutic in Galleria mellonella candidal infection, without showing toxic effects on mammalian cells. ISDPs were studied by circular dichroism spectroscopy, demonstrating different structural organization. These results allowed to validate a consensus sequence for the parent peptide KKVTMTCSAS that may be useful in the development of novel antimicrobial molecules.

scholarly journals In-vitro and in-vivo metabolism of different aspirin formulations studied by a validated liquid chromatography tandem mass spectrometry method

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Michele Dei Cas ◽  
Jessica Rizzo ◽  
Mariangela Scavone ◽  
Eti Femia ◽  
Gian Marco Podda ◽  
...  
Keyword(s):  
Oral Administration ◽  
Whole Blood ◽  
Serum Levels ◽  
Reversed Phase ◽  
Weekly Treatment ◽  
Low Dose Aspirin ◽  
Liquid Chromatography Tandem Mass ◽  
Enteric Coated

AbstractLow-dose aspirin (ASA) is used to prevent cardiovascular events. The most commonly used formulation is enteric-coated ASA (EC-ASA) that may be absorbed more slowly and less efficiently in some patients. To uncover these “non-responders” patients, the availability of proper analytical methods is pivotal in order to study the pharmacodynamics, the pharmacokinetics and the metabolic fate of ASA. We validated a high-throughput, isocratic reversed-phase, negative MRM, LC–MS/MS method useful for measuring circulating ASA and salicylic acid (SA) in blood and plasma. ASA-d4 and SA-d4 were used as internal standards. The method was applied to evaluate: (a) the "in vitro" ASA degradation by esterases in whole blood and plasma, as a function of time and concentration; (b) the "in vivo" kinetics of ASA and SA after 7 days of oral administration of EC-ASA or plain-ASA (100 mg) in healthy volunteers (three men and three women, 37–63 years). Parameters of esterases activity were Vmax 6.5 ± 1.9 and Km 147.5 ± 64.4 in plasma, and Vmax 108.1 ± 20.8 and Km 803.2 ± 170.7 in whole blood. After oral administration of the two formulations, tmax varied between 3 and 6 h for EC-ASA and between 0.5 and 1.0 h for plain-ASA. Higher between-subjects variability was seen after EC-ASA, and one subject had a delayed absorption over eight hours. Plasma AUC was 725.5 (89.8–1222) for EC-ASA, and 823.1(624–1196) ng h/mL (median, 25–75% CI) for plain ASA. After the weekly treatment, serum levels of TxB2 were very low (< 10 ng/mL at 24 h from the drug intake) in all the studied subjects, regardless of the formulation or the tmax. This method proved to be suitable for studies on aspirin responsiveness.

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