A simple method of synthesis of triterpene glycosides similar to glycyrrhizic acid and their hepatoprotective activity in vitro

SummaryThe filter loop technique which measures platelet aggregation in vivo in the flowing-blood of the rat was compared to the optical density technique of Born which is carried out in vitro with platelet rich plasma. Using these two experimental models the effect on platelet aggregation of three known inhibitors sulfinpyrazone, dipyridamole and prostaglandin E1, and a novel compound 5-oxo-l-cyclopentene-l-heptanoic acid (AY-16, 804) was determined.The effects on platelet aggregation of the known inhibitors were consistent with information in the literature. Prostaglandin E1 was the most potent inhibitor in both techniques; sulfinpyrazone inhibited aggregation in both models but was less potent than prostaglandin E1. AY-16, 804 exhibited activity in vitro and in vivo similar to that of sulfinpyrazone. Dipyridamole did not inhibit platelet aggregation in vivo and did not inhibit aggregation in vitro in concentrations at which it remained soluble.The filter loop technique is a suitable model for measuring platelet aggregation in the flowing blood of the rat. It is a relatively simple method of determining aggregation and easily adapted to other species.

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Rhenium-188 labeled recombinant human plasminogen kringle5 (rhk5) and preliminary biodistribution

Nuklearmedizin ◽

10.3413/nukmed-0349-10-09 ◽

2011 ◽

Vol 50 (06) ◽

pp. 234-239 ◽

Cited By ~ 3

Author(s):

R. Guo ◽

Y. Ma ◽

R. Zhang ◽

S. Liang ◽

H. Shen ◽

...

Keyword(s):

Lung Adenocarcinoma ◽

Human Serum ◽

Critical Role ◽

Angiogenesis Inhibitor ◽

Simple Method ◽

Tumour Formation ◽

Human Plasminogen ◽

Specificity Of Binding ◽

A549 Lung

Summary Aim: Angiogenesis plays a critical role in tumour formation and metastasis. Suitable radiolabeled angiogenesis inhibitor can be used for noninvasive imaging of angiogenesis and radionuclide therapy. Here we prepare rhenium-188 labeled recombinant human plasminogen kringle5 (188Re-rhk5) in a convenient manner than evaluate its properties in A549 lung adenocarcinoma. Methods: 188Rerhk5 was obtained by conjugating His group at the C end of rhk5 with fac- [188Re(H2O)3(CO)3]+. Chelating efficiency of fac-[188Re(H2O)3(CO)3]+ and radiolabeling efficiency of 188Re-rhk5 were measured by radio thin-layer chromatography (RTLC). In vitro stability of 188Re-rhk5 was determined in human serum at 37°C and analyzed by RTLC. Competition test was also performed to verify the specificity of binding. A biodistribution study was carried out in nude mice bearing A549 lung adenocarcinoma. Results: 188Rerhk5 was obtained with a radiolabel efficiency of 66.1%, the radiochemical purity (RCP) can marreach 95.2% after purification. 188Re-rhk5 showed high stability in human serum, the RCP was more than 80% even 12 h after incubation. Competition test showed a high binding specificity. Furthermore, this radio-complex was excreted mainly through kidneys and showed specific tumour uptake in mice bearing A549 tumours. Conclusion: 188Re-rhk5 was prepared by a simple method. Preliminary biodistribution results showed its potential as an agent for possible tumour imaging, therapy and encouraged further investigation.

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Dipterocarpus tuberculatus Roxb. Ethanol Extract Has Anti-Inflammatory and Hepatoprotective Effects In Vitro and In Vivo by Targeting the IRAK1/AP-1 Pathway

Molecules ◽

10.3390/molecules26092529 ◽

2021 ◽

Vol 26 (9) ◽

pp. 2529

Author(s):

Haeyeop Kim ◽

Woo Seok Yang ◽

Khin Myo Htwe ◽

Mi-Nam Lee ◽

Young-Dong Kim ◽

...

Keyword(s):

Ethanol Extract ◽

Serum Levels ◽

Hepatoprotective Activity ◽

Tnf Α ◽

Anti Inflammatory ◽

Related Proteins ◽

Pro Inflammatory Cytokines ◽

Inflammatory Effect

Dipterocarpus tuberculatus Roxb. has been used traditionally as a remedy for many diseases, especially inflammation. Therefore, we analyzed and explored the mechanism of the anti-inflammatory effect of a Dipterocarpus tuberculatus Roxb. ethanol extract (Dt-EE). Dt-EE clearly and dose-dependently inhibited the expression of pro-inflammatory cytokines such as IL-6, TNF-α, and IL-1β in lipopolysaccharide (LPS)-treated RAW264.7 cells. Also, Dt-EE suppressed the activation of the MyD88/TRIF-mediated AP-1 pathway and the AP-1 pathway related proteins JNK2, MKK4/7, and TAK1, which occurred as a result of inhibiting the kinase activity of IRAK1 and IRAK4, the most upstream factors of the AP-1 pathway. Finally, Dt-EE displayed hepatoprotective activity in a mouse model of hepatitis induced with LPS/D-galactosamine (D-GalN) through decreasing the serum levels of alanine aminotransferase and suppressing the activation of JNK and IRAK1. Therefore, our results strongly suggest that Dt-EE could be a candidate anti-inflammatory herbal medicine with IRAK1/AP-1 inhibitory and hepatoprotective properties.

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Phytochemical Composition and Biological Activities of Scorzonera Species

International Journal of Molecular Sciences ◽

10.3390/ijms22105128 ◽

2021 ◽

Vol 22 (10) ◽

pp. 5128

Author(s):

Karolina Lendzion ◽

Agnieszka Gornowicz ◽

Krzysztof Bielawski ◽

Anna Bielawska

Keyword(s):

Biological Activities ◽

Folk Medicine ◽

Quinic Acid ◽

Hepatoprotective Activity ◽

Phytochemical Composition ◽

Starting Point ◽

Microbial Infections ◽

Bacteria And Fungi ◽

Bioactive Potential

The genus Scorzonera comprises nearly 200 species, naturally occurring in Europe, Asia, and northern parts of Africa. Plants belonging to the Scorzonera genus have been a significant part of folk medicine in Asia, especially China, Mongolia, and Turkey for centuries. Therefore, they have become the subject of research regarding their phytochemical composition and biological activity. The aim of this review is to present and assess the phytochemical composition, and bioactive potential of species within the genus Scorzonera. Studies have shown the presence of many bioactive compounds like triterpenoids, sesquiterpenoids, flavonoids, or caffeic acid and quinic acid derivatives in extracts obtained from aerial and subaerial parts of the plants. The antioxidant and cytotoxic properties have been evaluated, together with the mechanism of anti-inflammatory, analgesic, and hepatoprotective activity. Scorzonera species have also been investigated for their activity against several bacteria and fungi strains. Despite mild cytotoxicity against cancer cell lines in vitro, the bioactive properties in wound healing therapy and the treatment of microbial infections might, in perspective, be the starting point for the research on Scorzonera species as active agents in medical products designed for miscellaneous skin conditions.

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Hepatoprotective studies on methanolic extract fractions of Lindernia ciliata and development of qualitative analytical profile for the bioactive extract

Clinical Phytoscience ◽

10.1186/s40816-019-0123-1 ◽

2019 ◽

Vol 5 (1) ◽

Author(s):

Praneetha Pallerla ◽

Narsimha Reddy Yellu ◽

Ravi Kumar Bobbala

Keyword(s):

Methanolic Extract ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Liver Homogenate ◽

Reducing Power ◽

Hepatoprotective Activity ◽

Total Phenolic ◽

Effective Fraction

Abstract Background The objective of the study is to evaluate the hepatoprotective activity of methanolic extract fractions of Lindernia ciliata (LC) and development of qualitative analytical profile of the bioactive fraction using HPLC fingerprinting analysis. All the fractions of methanolic extract of Lindernia ciliata (LCME) are assessed for their total phenolic, flavonoid contents and in vitro antioxidant properties by using DPPH, superoxide, nitric oxide, hydroxyl radical scavenging activities and reducing power assay. Acute toxicity study was conducted for all the fractions and the two test doses 50 and 100 mg/kg were selected for the hepatoprotective study. Liver damage was induced in different groups of rats by administering 3 g/kg.b.w.p.o. paracetamol and the effect of fractions were tested for hepatoprotective potential by evaluating serum biochemical parameters and histology of liver of rats. The effective fraction was evaluated for its antihepatotoxic activity against D-Galactosamine (400 mg/kg b.w. i.p.) and in vivo antioxidant parameters viz., Glutathione (GSH), Melondialdehyde (MDA) and Catalase (CAT) levels are estimated using liver homogenate. Results Among all the fractions, butanone fraction of LCME, (BNF-LCME) has shown better hepatoprotective activity and hence it is selected to evaluate the antihepatotoxicity against D-GaIN. The activity of BNF-LCME is well supported in in vitro and in vivo antioxidant studies and may be attributed to flavonoidal, phenolic compounds present in the fraction. Hence, BNF-LCME was subjected to the development of qualitative analytical profile using HPLC finger printing analysis. Conclusions All the fractions of LCME exhibited significant hepatoprotective activity and BNF-LCME (50 mg/kg) was identified as the most effective fraction.

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Cemp1-p3 Peptide Promotes the Transformation of Octacalcium Phosphate into Hydroxyapatite Crystals

Crystals ◽

10.3390/cryst10121131 ◽

2020 ◽

Vol 10 (12) ◽

pp. 1131

Author(s):

Maricela Santana ◽

Gonzalo Montoya ◽

Raúl Herrera ◽

Lía Hoz ◽

Enrique Romo ◽

...

Keyword(s):

Electron Microscopy ◽

Octacalcium Phosphate ◽

Sequence Motifs ◽

Simple Method ◽

Transmission Electron ◽

Precursor Phase ◽

Mineralized Tissues ◽

Potent Growth

Dental cementum contains unique molecules that regulate the mineralization process in vitro and in vivo, such as cementum protein 1 (CEMP1). This protein possesses amino acid sequence motifs like the human recombinant CEMP1 with biological activity. This novel cementum protein 1-derived peptide (CEMP1-p3, from the CEMP1’s N-terminal domain: (QPLPKGCAAVKAEVGIPAPH), consists of 20 amino acids. Hydroxyapatite (HA) crystals could be obtained through the combination of the amorphous precursor phase and macromolecules such as proteins and peptides. We used a simple method to synthesize peptide/hydroxyapatite nanocomposites using OCP and CEMP1-p3. The characterization of the crystals through scanning electron microscopy (SEM), powder X-ray diffraction (XRD), high--resolution transmission electron microscopy (HRTEM), and Raman spectroscopy revealed that CEMP1-p3 transformed OCP into hydroxyapatite (HA) under constant ionic strength and in a buffered solution. CEMP1-p3 binds and highly adsorbs to OCP and is a potent growth stimulator of OCP crystals. CEMP1-p3 fosters the transformation of OCP into HA crystals with crystalline planes (300) and (004) that correspond to the cell of hexagonal HA. Octacalcium phosphate crystals treated with CEMP1-p3 grown in simulated physiological buffer acquired hexagonal arrangement corresponding to HA. These findings provide new insights into the potential application of CEMP1-p3 on possible biomimetic approaches to generate materials for the repair and regeneration of mineralized tissues, or restorative materials in the orthopedic field.

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Triterpene glycosides with in vitro anti-inflammatory activity from Cyclamen repandum tubers

Carbohydrate Research ◽

10.1016/j.carres.2009.12.028 ◽

2010 ◽

Vol 345 (5) ◽

pp. 709-714 ◽

Cited By ~ 11

Author(s):

Stefano Dall’Acqua ◽

Ignazio Castagliuolo ◽

Paola Brun ◽

Federica Ditadi ◽

Giorgio Palù ◽

...

Keyword(s):

Triterpene Glycosides ◽

Inflammatory Activity ◽

Anti Inflammatory

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A simple method to evaluate basophil tryptase after allergen challenge in vitro

Journal of Allergy and Clinical Immunology ◽

10.1016/s0091-6749(97)70087-3 ◽

1997 ◽

Vol 99 (4) ◽

pp. 575-576 ◽

Cited By ~ 4

Author(s):

G MONASTEROLO ◽

R ROSSI

Keyword(s):

Allergen Challenge ◽

Simple Method

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762 A combination of functional biomarkers improves identification of the tumor-specific reactive T cell repertoire

Journal for ImmunoTherapy of Cancer ◽

10.1136/jitc-2020-sitc2020.0762 ◽

2020 ◽

Vol 8 (Suppl 3) ◽

pp. A810-A810

Author(s):

Arianna Draghi ◽

Katja Harbst ◽

Inge Svane ◽

Marco Donia

Keyword(s):

T Cells ◽

T Cell ◽

De Novo ◽

Autologous Tumor ◽

T Cell Repertoire ◽

Cell Repertoire ◽

Simple Method ◽

Functional Biomarkers

BackgroundDetecting the entire repertoire of tumor-specific reactive T cells is essential for investigating the broad range of T cell functions in the tumor-microenvironment. At present, assays identifying tumor-specific functional activation measure either upregulation of specific surface molecules, de novo production of the most common antitumor cytokines or mobilization of cytotoxic granules.MethodsIn this study, we combined transcriptomic analyses of tumor-specific reactive tumorinfiltrating lymphocytes (TILs), TIL-autologous tumor cell co-cultures and commonly used established detection protocols to develop an intracellular flow cytometry staining method encompassing simultaneous detection of intracellular CD137, de novo production of TNF and IFNy and extracellular mobilization of CD107a.ResultsThis approach enabled the identification of a larger fraction of tumor-specific reactive T cells in vitro compared to standard methods, revealing the existence of multiple distinct functional clusters of tumor-specific reactive TILs. Publicly available datasets of fresh tumor single-cell RNA-sequencing from four cancer types were investigated to confirm that these functional biomarkers identified distinct functional clusters forming the entire repertoire of tumor-specific reactive T cells in situ.ConclusionsIn conclusion, we describe a simple method using a combination of functional biomarkers that improves identification of the tumor-specific reactive T cell repertoire in vitro and in situ.

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