Abstract:The present study was carried out to evaluate anti-Helicobacter pylori and its associated urease activity of labdane diterpenoids isolated from Andrographis paniculata. A molecular docking analysis was performed by using ArgusLab 4.0.1 software. The results obtained indicate that compound A possesses strong inhibition to H. pylori, 28 ± 2.98 (minimum inhibitory concentration, 9 µg/mL), and its urease, 85.54 ± 2.62% (IC50 , 20.2 µg/mL). Compounds B, C, and D also showed moderate inhibition to H. pylori and its … Show more
“…However, luteolin, apigenin, diosmetin, O 4Ꞌ , O 7 ‐dihexyl apigenin, and chrysin exhibited significant inhibition toward urease compared with all other flavonoids. Several bioactive phenolic compounds were studied which were exhibiting a significant inhibitory effect and which have been identified from plant materials, among them are flavonoids, tannins, terpenes, aromatic aldehydes, alcohols, tannins, and catechins that are studied widely . Thus, the results are in accordance with reported studies.…”
Section: Resultssupporting
confidence: 84%
“…Several bioactive phenolic compounds were studied which were exhibiting a significant inhibitory effect and which have been identified from plant materials, among them are flavonoids, tannins, terpenes, aromatic aldehydes, alcohols, tannins, and catechins that are studied widely. [35] Thus, the results are in accordance with reported studies. The literature reported that flavonoids showed significant urease activity, and our results are in close agreement with the literature data.…”
The synthesized flavonoid derivatives were examined for their antioxidant, anti-inflammatory, xanthine oxidase (XO), urease inhibitory activity, and cytotoxicity. Except few, all the flavonoids under this study showed significant antioxidant activity (45.6%-85.5%, 32.6%-70.6%, and 24.9%-65.5% inhibition by DPPH, ferric reducing/antioxidant power, and oxygen radical absorption capacity assays) with promising TNF-inhibitory activity (42%-73% at 10 M) and IL-6 inhibitory activity (54%-81% at 10 M) compared with that of control dexamethasone. The flavonoidsO 7 -hexyl chrysin, showed an inhibition with IC 50 values (4.5-8.1 g/mL), more than allopurinol (8.5 g/mL) at 5 M against XO and showing more than 50% inhibition at a final concentration (5 mM) with an IC 50 value of ranging from 4.8 to 7.2 ( g/mL) in comparison with the positive control thiourea (5.8 g/mL) for urease inhibition. Thus, the flavonoid derivatives may be considered as potential antioxidant and antigout agents.
“…However, luteolin, apigenin, diosmetin, O 4Ꞌ , O 7 ‐dihexyl apigenin, and chrysin exhibited significant inhibition toward urease compared with all other flavonoids. Several bioactive phenolic compounds were studied which were exhibiting a significant inhibitory effect and which have been identified from plant materials, among them are flavonoids, tannins, terpenes, aromatic aldehydes, alcohols, tannins, and catechins that are studied widely . Thus, the results are in accordance with reported studies.…”
Section: Resultssupporting
confidence: 84%
“…Several bioactive phenolic compounds were studied which were exhibiting a significant inhibitory effect and which have been identified from plant materials, among them are flavonoids, tannins, terpenes, aromatic aldehydes, alcohols, tannins, and catechins that are studied widely. [35] Thus, the results are in accordance with reported studies. The literature reported that flavonoids showed significant urease activity, and our results are in close agreement with the literature data.…”
The synthesized flavonoid derivatives were examined for their antioxidant, anti-inflammatory, xanthine oxidase (XO), urease inhibitory activity, and cytotoxicity. Except few, all the flavonoids under this study showed significant antioxidant activity (45.6%-85.5%, 32.6%-70.6%, and 24.9%-65.5% inhibition by DPPH, ferric reducing/antioxidant power, and oxygen radical absorption capacity assays) with promising TNF-inhibitory activity (42%-73% at 10 M) and IL-6 inhibitory activity (54%-81% at 10 M) compared with that of control dexamethasone. The flavonoidsO 7 -hexyl chrysin, showed an inhibition with IC 50 values (4.5-8.1 g/mL), more than allopurinol (8.5 g/mL) at 5 M against XO and showing more than 50% inhibition at a final concentration (5 mM) with an IC 50 value of ranging from 4.8 to 7.2 ( g/mL) in comparison with the positive control thiourea (5.8 g/mL) for urease inhibition. Thus, the flavonoid derivatives may be considered as potential antioxidant and antigout agents.
“…In vitro studies found that several components from medicinal plants inhibited the activity of H. pylori urease, such as both methanol and acetone extracts from Acacia nilotica and Calotropis procera (Amin, Anwar, Naz, Mehmood, & Saari, 2013), betulinic acid and oleanolic acid from Forsythia suspense (Shin, Park, Baek, Chung, & Park, 2009), water extract from Terminalia chebula (inhibitory concentrations: 1 to 2.5 mg/mL; Malekzadeh, Ehsanifar, Shahamat, Levin, & Colwell, 2001). Labdane diterpenoids isolated from Andrographis paniculata inhibited urease activity in vitro with 50% inhibitory concentration (IC 50 ) of 20.2 μg/mL (Shaikh et al, 2016), and for dichloromethane extract from Parthenium hysterophorus roots, the IC 50 is 136.4 μg/mL (Espinosa-Rivero, Rendon-Huerta, & Romero, 2015). Pterocarpus santalinus could inhibit the activity of urease, and decrease the lipid peroxidation and lactate dehydrogenase when co-cultivated with gastric epithelial cells of rats (Narayan, Veeraraghavan, & Devi, 2007).…”
Helicobacter pylori is the main pathogen that induces chronic gastritis, peptic ulcers, atrophic gastritis, and other gastric disorders, and it is classified as a group I carcinogen. To eradicate H. pylori infection, triple therapy consisting of two antibiotics and a proton pump inhibitor is the most widely recommended first-line therapeutic strategy. Antimicrobial resistance to antibiotics contained in triple therapy could lead to therapeutic regimen failures. Recent studies showed that many natural products, including fruits, vegetables, spices, and medicinal plants, possess inhibitory effects on H. pylori, indicating their potential to be alternatives to prevent and manage H. pylori infection. This review summarizes the effects of natural products on H. pylori infection and highlights the mechanisms of action.
“…214 Andrographolide sodium bisulphite showed inhibitory potency on helicobacter pylori and helicobacter pylori urease. 215,216 Andrographolide was found to suppress the expression of E-selectin at the mRNA level, reducing the adherence of gastric cancer cells to human vascular endothelial cells. 200 Treatment with andrographolide decreased proliferation and increased apoptosis in three gastric cell lines: BGC-822, SGC7901, and C666-1 depending on time and concentration.…”
Andrographolide, a well-known natural lactone having a range of pharmacological actions in traditional Chinese medicine. It has long been used to cure a variety of ailments. In this review, we cover the pharmacokinetics and pharmacological activity of andrographolide which supports its further clinical application in cancers and inflammatory diseases. Growing evidence shows a good therapeutic effect in inflammatory diseases, including liver diseases, joint diseases, respiratory system diseases, nervous system diseases, heart diseases, inflammatory bowel diseases, and inflammatory skin diseases. As a result, the effects of andrographolide on immune cells and the processes that underpin them are discussed. The preclinical use of andrographolide to different organs in response to malignancies such as colorectal, liver, gastric,
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