scholarly journals Mechanistic Studies of the Antiallergic Activity of Phyllanthus amarus Schum. & Thonn. and Its Compounds

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 695
Author(s):  
Nur Zahirah Abd Rani ◽  
Kok Wai Lam ◽  
Juriyati Jalil ◽  
Hazni Falina Mohamad ◽  
Mohd Shukri Mat Ali ◽  
...  
Keyword(s):  
High Performance ◽  
Binding Assay ◽  
Radioligand Binding ◽  
Positive Control ◽  
Phyllanthus Amarus ◽  
H1 Receptor ◽  
Antiallergic Activity ◽  
Ketotifen Fumarate ◽  
Antihistamine Activity ◽  
Basophilic Leukemia

Phyllanthus amarus Schum. & Thonn. (Phyllanthaceae) is a medicinal plant that is commonly used to treat diseases such as asthma, diabetes, and anemia. This study aimed to examine the antiallergic activity of P. amarus extract and its compounds. The antiallergic activity was determined by measuring the concentration of allergy markers release from rat basophilic leukemia (RBL-2H3) cells with ketotifen fumarate as the positive control. As a result, P. amarus did not stabilize mast cell degranulation but exhibited antihistamine activity. The antihistamine activity was evaluated by conducting a competition radioligand binding assay on the histamine 1 receptor (H1R). Four compounds were identified from the high performance liquid chromatography (HPLC) analysis which were phyllanthin (1), hypophyllanthin (2), niranthin (3), and corilagin (4). To gain insights into the binding interactions of the most active compound hypophyllanthin (2), molecular docking was conducted and found that hypophyllanthin (2) exhibited favorable binding in the H1R binding site. In conclusion, P. amarus and hypophyllanthin (2) could potentially exhibit antiallergic activity by preventing the activation of the H1 receptor.

Developing a High-performance Liquid Chromatography Method for Simultaneous Determination of Loratadine and its Metabolite Desloratadine in Human Plasma

2020 ◽  
Vol 20 (13) ◽  
pp. 1053-1059
Author(s):  
Mahmoud M. Sebaiy ◽  
Noha I. Ziedan
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
Human Plasma ◽  
High Performance ◽  
Allergic Diseases ◽  
Reversed Phase ◽  
Hplc Method ◽  
H1 Receptor ◽  
Chromatography Method

Background: Allergic diseases are considered as the major burden on public health with increased prevalence globally. Histamine H1-receptor antagonists are the foremost commonly used drugs in the treatment of allergic disorders. The target drug in this study, loratadine, belongs to this class of drugs and its biometabolite desloratadine which is also a non-sedating H1 receptor antagonist with anti-histaminic activity being 2.5 to 4 times greater than loratadine. This study aimed to develop and validate a novel isocratic Reversed-phase High-Performance Liquid Chromatography (RP-HPLC) method for rapid and simultaneous separation and determination of loratadine and its metabolite, desloratadine in human plasma. Methods: The drug extraction method from plasma was based on protein precipitation technique. The separation was carried out on a Thermo Scientific BDS Hypersil C18 column (5μm, 250 x 4.60 mm) in a mobile phase of MeOH: 0.025M KH2PO4 adjusted to pH 3.50 using orthophosphoric acid (85: 15, v/v) at an ambient temperature. The flow rate was maintained at 1 mL/min and maximum absorption was measured using the PDA detector at 248 nm. Results: The retention times of loratadine and desloratadine in plasma samples were recorded to be 4.10 and 5.08 minutes, respectively, indicating a short analysis time. Limits of detection were found to be 1.80 and 1.97 ng/mL for loratadine and desloratadine, respectively, showing a high degree of sensitivity of the method. The method was then validated according to FDA guidelines for the determination of the two analytes in human plasma. Conclusion: The results obtained indicate that the proposed method is rapid, sensitive in the nanogram range, accurate, selective, robust and reproducible compared to other reported methods.

scholarly journals Ingol and Ingenol-Type Diterpenes from Euphorbia trigona Miller with Keratinocyte Inhibitory Activity

Plants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1206
Author(s):  
Reham Hammadi ◽  
Norbert Kúsz ◽  
Csilla Zsuzsanna Dávid ◽  
Zoltán Behány ◽  
László Papp ◽  
...  
Keyword(s):  
Liquid Chromatography ◽  
Cytotoxic Activity ◽  
Inhibitory Activity ◽  
High Performance ◽  
Skin Condition ◽  
Positive Control ◽  
Active Species ◽  
The European Union ◽  
Ingenol Mebutate

Ingenol mebutate, isolated from Euphorbia peplus, is an ingenane-type diterpenoid, primarily used for the topical treatment of actinic keratosis, a premalignant skin condition. The aim of our work was to investigate other Euphorbia species to find structurally similar diterpenes that can be used as alternatives to ingenol mebutate. Pharmacological investigation of Euphorbia candelabrum, Euphorbia cotinifolia, Euphorbia ramipressa, and Euphorbia trigona revealed the potent keratinocyte (HPV-Ker cell line) inhibitory activity of these spurge species. From the methanolic extract of the aerial parts of Euphorbia trigona Miller, the most active species, five ingol (1–5) and four ingenane-type diterpenoids (6–9) were isolated by various chromatographic separation techniques, including open column chromatography, vacuum liquid chromatography, thin-layer chromatography, and high-performance liquid chromatography. The structures of the compounds were determined by NMR spectroscopic analysis and by comparison of the assignations with the literature data. The cytotoxic activity of the compounds against keratinocytes was tested in vitro by using ingenol mebutate as a positive control. Among the isolated compounds, two ingenane derivatives (6 and 7) exhibited remarkably stronger cytotoxic activity (IC50 values 0.39 μM and 0.32 μM, respectively) on keratinocytes than ingenol mebutate (IC50 value 0.84 μM). These compounds could serve as starting materials for further investigations to find alternatives to Picato® (with active substance ingenol mebutate), which was withdrawn from marketing authorization in the European Union.

Ranitidine as an alcohol dehydrogenase inhibitor in acute methanol toxicity in rats

2009 ◽  
Vol 29 (2) ◽  
pp. 93-101 ◽  
Author(s):  
Amal A El-Bakary ◽  
Sahar A El-Dakrory ◽  
Sohayla M Attalla ◽  
Nawal A Hasanein ◽  
Hala A Malek
Keyword(s):  
Alcohol Dehydrogenase ◽  
High Performance ◽  
Negative Control Group ◽  
Positive Control ◽  
Negative Control ◽  
Control Group ◽  
Sprague Dawley ◽  
Blood Samples ◽  
Methanol Poisoning ◽  
Sprague Dawley Rats

Methanol poisoning is a hazardous intoxication characterized by visual impairment and formic acidemia. The therapy for methanol poisoning is alcohol dehydrogenase (ADH) inhibitors to prevent formate accumulation. Ranitidine has been considered to be an inhibitor of both gastric alcohol and hepatic aldehyde dehydrogenase enzymes. This study aimed at testing ranitidine as an antidote for methanol acute toxicity and comparing it with ethanol and 4-methyl pyrazole (4-MP). This study was conducted on 48 Sprague-Dawley rats, divided into 6 groups, with 8 rats in each group (one negative control group [C1], two positive control groups [C2, C3] and three test groups [1, 2 and 3]). C2, C3 and all test groups were exposed to nitrous oxide by inhalation, then, C3 group was given methanol (3 g/kg orally). The three test groups 1, 2 and 3 were given ethanol (0.5 g/kg orally), 4-MP (15 mg/kg intraperitoneally) and ranitidine (30 mg/kg intraperitoneally), respectively, 4 hours after giving methanol. Rats were sacrificed and heparinized, cardiac blood samples were collected for blood pH and bicarbonate. Non-heparinized blood samples were collected for formate levels by high performance liquid chromatography. Eye balls were enucleated for histological examination of the retina. Ranitidine corrected metabolic acidosis (p = .025), decreased formate levels (p = .014) and improved the histological findings in the retina induced by acute methanol toxicity.

A radioligand-binding assay for detecting antibodies specific for proinsulin and insulin using 35S-proinsulin

2003 ◽  
Vol 279 (1-2) ◽  
pp. 173-181 ◽  
Author(s):  
Silvina N. Valdez ◽  
Rubén F. Iacono ◽  
Anabel Villalba ◽  
Alejandro Cardoso Landaburu ◽  
Mario R. Ermácora ◽  
...  
Keyword(s):  
Binding Assay ◽  
Radioligand Binding ◽  
Radioligand Binding Assay

scholarly journals Inhibitory Activity of 8 Alkaloids on P-gp and Their Distribution in Chinese Uncaria Species

2020 ◽  
Vol 15 (11) ◽  
pp. 1934578X2097350
Author(s):  
Yanan Gai ◽  
Nannan Yang ◽  
Jian Chen
Keyword(s):  
High Performance ◽  
Positive Control ◽  
Inhibitory Effects ◽  
Glycoprotein P ◽  
Chromatography Analysis ◽  
Chemical Content ◽  
Polymerase Chain ◽  
Chemical Distribution ◽  
And Function ◽  
Mcf 7

P-glycoprotein (P-gp) inhibition conduces to improving the ability of chemicals to cross through blood-brain barrier (BBB). The hook-bearing branch of Uncaria is used as a traditional herbal medicine for the treatment of hypertension, headache, stroke, and Alzheimer’s disease in recent years. In this study, the inhibitory effects of 8 alkaloids sourced from Uncaria plants on P-gp were evaluated. Meanwhile, the content of 8 alkaloids in 8 Chinese Uncaria species was quantified simultaneously by high-performance liquid chromatography analysis. Western blotting, real-time quantitative reverse transcription-polymerase chain reaction, and flow cytometry were used to evaluate the P-gp levels in MCF-7/adriamycin-resistant (ADR) cells. It was shown that hirsuteine and hirsutine, selected from 8 candidate alkaloids, could remarkably suppressed P-gp level and function in MCF-7/ADR cells when using Verapamil as positive control. By tracking their chemical distribution in 8 Chinese Uncaria species, we found that hirsuteine and hirsutine were much more abundant in Uncaria rhynchophylla and Uncaria hirsuta than in any other 6 species. And a chemical content profile of these alkaloids was plotted within 8 Chinese species.

scholarly journals Synthesis, Characterization, and Antioxidant Activity of 8-Hydroxygenistein

2020 ◽  
Vol 15 (1) ◽  
pp. 1934578X2090139 ◽  
Author(s):  
Jin Shao ◽  
Tong Zhao ◽  
Hui-Ping Ma ◽  
Zheng-Ping Jia ◽  
Lin-Lin Jing
Keyword(s):  
Antioxidant Activity ◽  
High Performance ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Positive Control ◽  
Raw Material ◽  
Biochanin A ◽  
Total Antioxidant Activity ◽  
Nitric Oxide Radical ◽  
Total Antioxidant

It was reported that 8-hydroxygenistein (8-OHG) was synthesized by methylation, bromination, methoxylation, and demethylation using cheap and readily available biochanin A as raw material. All synthesized products were structurally confirmed by ultra-high-performance liquid chromatography (UHPLC), infrared spectroscopy, mass spectrometry, 1H-nuclear magnetic resonance (NMR), and 13C-NMR. In addition, we examined the antioxidant capacity of 8-OHG using 6 different methods such as 1,1-diphenyl-2-picrylhydrazyl radical scavenging, 2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonate) radical (ABTS) scavenging, nitric oxide radical (NO) scavenging, superoxide radical (O2 −•) scavenging, reducing power assay, and total antioxidant activity using ascorbic acid (VC) as a positive control. Compared with VC, 8-OHG exhibited higher total antioxidant activity and stronger scavenging activity on ABTS, NO, and O2 −•. These results indicate that 8-OHG is an excellent antioxidant agent and may be effective in preventing damage induced by free radical.

scholarly journals Synthesis of Glycosides of α-Tocopherol, Daidzein, Resveratrol, Hesperetin, Naringenin, and Chrysin as Antiallergic Functional Foods and Cosmetics

2020 ◽  
Vol 15 (9) ◽  
pp. 1934578X2094466
Author(s):  
Yuya Fujitaka ◽  
Hiroki Hamada ◽  
Hatsuyuki Hamada ◽  
Takafumi Iwaki ◽  
Kei Shimoda ◽  
...  
Keyword(s):  
Antibody Formation ◽  
Immunoglobulin E ◽  
Positive Control ◽  
Phytolacca Americana ◽  
Antiallergic Activity ◽  
Ige Antibody ◽  
Peritoneal Mast Cells ◽  
7S Globulin ◽  
Antityrosinase Activity

Glucosyltransferase from Phytolacca americana (Phytolaccaceae), glucosylated α-tocopherol, daidzein, resveratrol, hesperetin, naringenin, and chrysin to α-tocopherol 6-β-d-glucoside, daidzein 7-β-d-glucoside, resveratrol 3-β-d-glucoside, hesperetin 7-β-d-glucoside, naringenin 7-β-d-glucoside, and chrysin 7-β-d-glucoside, respectively. The antiallergic activity of the glycosides and their aglycons was examined by an in vivo immunoglobulin E (IgE) antibody formation-suppression bioassay using rat. It was found that α-tocopherol 6-β-d-glucoside showed much higher antiallergic activity against glutenin than the positive control, hydrocortisone. On the other hand, daidzein 7-β-d-glucoside had much higher antiallergic activity toward 7S-globulin than hydrocortisone. These glycosides inhibited O2 − generation from rat neutrophils, which leads to the suppression of histamine release from rat peritoneal mast cells, resulting in the decrease of IgE antibody formation in rat. Chrysin 7-β-d-glucoside had stronger antityrosinase activity than chrysin. Cultured P. americana cells regioselectively introduced methoxyl and glucosyl residues on exogenously administrated chrysin to give 8-methoxychrysin and chrysin 7-β-d-glucoside. This is the first report on methoxylation of flavone compound at its eighth position by cultured plant cells.

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