Potent Anti-Platelet Constituents from Centaurea iberica

Khan, Amna N.; Fatima, Itrat; Khaliq, Urooj Abdul; Malik, Abdul; Miana, Ghulam Abbas; Qureshi, Zia-ur-Rehman; Rasheed, Huma

doi:10.3390/molecules16032053

Cited by 16 publications

(14 citation statements)

References 18 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…It contains many phytochemical compounds. Previously, flavones, fatty acids, steroid, volatile constituents, and sesquiterpene lactones have been reported from this plant (Khan et al, 2011). It was known for its uses in folk medicine for the cure of peptic ulcer, malaria, stomach upset, common cold, abdominal pain, herpes infections, and suggested against inflammatory situations such as asthma and abscesses (Khammar and Djeddi., 2012).…”

Section: Introductionmentioning

confidence: 99%

Phytochemical Analysis, Total Phenolic Content, Hemolytic and Antihemolytic Activities of Centaurea iberica (Asteraceae)

Joujeh¹

2020

SJKFU

View full text Add to dashboard Cite

Several plants contain chemical substances that have various biological activities that might cause harmful effects to cellular membranes. This work deals with Centaurea iberica (Iberian starthistle) plant. The objective of this study is to identify the main chemical groups in the methanolic extract 80% of the plant, determine its total phenolic content, evaluate its toxic effect on human erythrocytes in addition to assessing its activity in protecting normal and glucose-6-phosphate dehydrogenase (G6PD) enzyme-deficient human erythrocytes membranes against oxidative hemolysis. Phytochemical analysis revealed that C. iberica extract contains several bioactive compounds. The results also showed that the plant extract contained good level of total phenolic compounds. The extract exhibited low hemolytic effect. It also showed excellent activity in the protection of normal and G6PDdeficient human erythrocytes against oxidative hemolysis.

show abstract

Section: Introductionmentioning

confidence: 99%

Phytochemical Analysis, Total Phenolic Content, Hemolytic and Antihemolytic Activities of Centaurea iberica (Asteraceae)

Joujeh¹

2020

SJKFU

View full text Add to dashboard Cite

show abstract

“…In this context, regular consumption of fruits and vegetables, apart of the called Mediterranean diet [14], might be related to the bioactive compounds found in them [15], which explains the increasing amount of attention in research on phytochemicals in the prevention of CVD [16]. Tomatoes ( Solanum lycopersicum ), fresh or processed (e.g., tomato paste), apart from their nutritional value, have been found to provide a cardioprotective effect, both at the endothelial and platelet levels [17].…”

Section: Introductionmentioning

confidence: 99%

Bioassay-Guided Isolation and HPLC Determination of Bioactive Compound That Relate to the Antiplatelet Activity (Adhesion, Secretion, and Aggregation) fromSolanum lycopersicum

Fuentes

Castro

Astudillo

et al. 2012

Evidence-Based Complementary and Alternative Medicine

View full text Add to dashboard Cite

In seeking the functionality of foodstuff applicable to medicine, ripe tomato fruits were found to show an antiplatelet activity. Therefore, the bioactive compound was isolated, structurally identified, and studied for an inhibitory effects on platelet adhesion, secretion, and aggregation. The concentration of adenosine in ripe tomato fruits (pulp and skin extracts) and its processing by-products (paste and pomace) was determined by reversed-phase high-performance liquid chromatography (HPLC). According to platelet aggregation inhibition induced by ADP, the total extract residual was fractionated by liquid-liquid separation, obtaining aqueous, ethyl acetate and petroleum ether extracts. The aqueous extract was subjected to repeated permeation over sephadex LH-20 and semipreparative TLC. The isolate finally obtained was identified as adenosine on the basis of ESI-MS, 1H NMR, HPLC, and UV spectra. Adenosine concentration dependently (2.3–457 μM) platelet aggregation inhibited induced by ADP. Also, adenosine present inhibition of platelet secretion and thrombus formation under flow conditions. The quantitative HPLC analysis revealed significant amounts of adenosine in ripe tomato fruits and its processing by-products. From these results, extracts/fractions of ripe tomato fruits and their processing by-products may be referred to as functional food and functional ingredients containing a compound that inhibits platelet function with a potent preventive effect on thrombus formation, as those that occur in stroke.

show abstract

“…Unfortunately, the presence of a nitroaromatic group in SJ000113972 makes it less desirable as a drug candidate, and a preliminary evaluation of structural analogs did not reveal a promising molecule without this functional group (see Table S2 in the supplemental material). Based on these observations, the dihydroquinazolinone (DHQZ) SJ000019548 (EC 50 ϭ 1.4 M) was chosen for moreextensive structure-activity relationship (SAR) analysis due to the potential of the core structure for drug development as evidenced by previous reports on the biological activities of DHQZs (23,24,25,26).…”

Section: Resultsmentioning

confidence: 99%

Dihydroquinazolinone Inhibitors of Proliferation of Blood and Liver Stage Malaria Parasites

Derbyshire

Min

Guiguemde

et al. 2014

Antimicrob Agents Chemother

View full text Add to dashboard Cite

bDrugs that target both the liver and blood stages of malaria will be needed to reduce the disease's substantial worldwide morbidity and mortality. Evaluation of a 259-member library of compounds that block proliferation of the blood stage of malaria revealed several scaffolds-dihydroquinazolinones, phenyldiazenylpyridines, piperazinyl methyl quinolones, and bis-benzimidazoles-with promising activity against the liver stage. Focused structure-activity studies on the dihydroquinazolinone scaffold revealed several molecules with excellent potency against both blood and liver stages. One promising early lead with dual activity is 2-(p-bromophenyl)-3-(2-(diethylamino)ethyl)-2,3-dihydroquinazolin-4(1H)-one with 50% effective concentrations (EC 50 s) of 0.46 M and 0.34 M against liver stage Plasmodium berghei ANKA and blood stage Plasmodium falciparum 3D7 parasites, respectively. Structure-activity relationships revealed that liver stage activity for this compound class requires a 3-dialkyl amino ethyl group and is abolished by substitution at the ortho-position of the phenyl moiety. These compounds have minimal toxicity to mammalian cells and are thus attractive compounds for further development.

show abstract

Potent Anti-Platelet Constituents from Centaurea iberica

Cited by 16 publications

References 18 publications

Phytochemical Analysis, Total Phenolic Content, Hemolytic and Antihemolytic Activities of Centaurea iberica (Asteraceae)

Phytochemical Analysis, Total Phenolic Content, Hemolytic and Antihemolytic Activities of Centaurea iberica (Asteraceae)

Bioassay-Guided Isolation and HPLC Determination of Bioactive Compound That Relate to the Antiplatelet Activity (Adhesion, Secretion, and Aggregation) fromSolanum lycopersicum

Dihydroquinazolinone Inhibitors of Proliferation of Blood and Liver Stage Malaria Parasites

Contact Info

Product

Resources

About