scholarly journals Analgesic and antiinflammatory activities of the capilliposide derived from Lysimachia capillipes Hemsl., a traditional Chinese medicinal herb

2020 ◽  
Vol 72 (4) ◽  
pp. 515-523
Author(s):  
Zhipan Wu ◽  
Haote Han ◽  
Mengting Xu ◽  
Yuhang Shen ◽  
Chengcheng Gao ◽  
...  
Keyword(s):  
Latency Period ◽  
Medicinal Herb ◽  
Antiinflammatory Effect ◽  
Chinese Medicinal Herb ◽  
Cyclooxygenase 1 ◽  
Bioactive Component ◽  
Antiinflammatory Effects ◽  
Clinical Conditions ◽  
Necrosis Factor ◽  
Cox 1

Pain and inflammation are associated with the pathophysiology of different clinical conditions. The Lysimachia capillipes Hemsl. capilliposide (LCc) is the main bioactive component of this Chinese medicinal herb, which is widely used as a remedy for the treatment of colds and arthritis. This study investigated the analgesic and antiinflammatory activities of LCc in an animal model. LCc had no significant influence on the spleen, lung, liver and stomach coefficients in mice. Pharmacological studies showed that LCc at all doses (40, 60 and 90 mg/kg) increased the latency period of paw licking induced by thermal stimulation, and at the dose of 40 mg/kg it significantly suppressed abdominal writhing episodes of mice induced by intraperitoneal (i.p.) injection of acetic acid. LCc also had antiinflammatory effect on inflammation models. Doses of 60 and 90 mg/kg suppressed paw edema induced by subcutaneous (s.c.) injection of carrageenan. Mechanistic studies revealed that the antiinflammatory effect of LCc was associated with inhibition of the production of malondialdehyde (MDA), prostaglandin E2 (PGE2), tumor necrosis factor (TNF-?), cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) in paw tissue of carrageenan-injected mice. These results show that LCc has analgesic and antiinflammatory effects in mice.

scholarly journals Computational and pharmacological evaluation of stevioside derivatives for antinociceptive and antiinflammatory potential

2020 ◽  
Vol 19 (8) ◽  
pp. 1677-1684
Author(s):  
Sadaf Ahmad ◽  
Arif-ullah Khan ◽  
Muhammad Faheem ◽  
Muhammad Shahid Iqbal ◽  
Mohammad Akbar Hossain ◽  
...  
Keyword(s):  
Hydrogen Bonds ◽  
Latency Period ◽  
Binding Modes ◽  
Pharmacological Evaluation ◽  
Cyclooxygenase 1 ◽  
Prostaglandin Synthase ◽  
Anti Inflammatory ◽  
Pain Test ◽  
Further Development ◽  
Cox 1

Purpose: To carry out computational and pharmacological evaluation of two stevioside derivatives in order to develop more effective candidates for analgesia and inflammation.Methods: Primarily, compounds were docked against targets of nociception and inflammation such as cyclooxygenase-1, cyclooxygenase-2, 5-lypooxygenase 12-lypooxygenase, 15-lypooxygenase, prostaglandin synthase, leukotrienes C4 synthase, mu, kappa, and delta receptors to obtain their possible binding modes. Test compounds were then screened in animal model of nociception and inflammation.Results: The results of docking show that IO possesses good affinity when compared to ID. IO showed two hydrogen bonds against COX-1 and COX-2. IO also demonstrated good binding against 5-LOX, 12- LOX and 15-LOX, exhibited four, one and two hydrogen bonds respectively. Against PG synthase and LTC4, both IO and ID produced moderate binding. IO also showed significant binding against opoid receptors (p < 0.05). IO and ID significantly decrease the number of writhes to 21.20 ± 2.1 and 27.0 ± 2.12 at 10 mg/kg in acetic acid mediated pain test respectively. In hot plate method, IO and ID increase the latency period of mice to 14.14 ± 0.40 and 10.50 ± 0.34 s, respectively. IO and ID significantly reduced the paw edema to 1.69 ± 0.14 and 1.94 ± 0.14 mL, respectively, in acute inflammation (p < 0.05). In chronic inflammatory model, IO and ID decreased paw volume to 3.26 ± 0.38 and 4.20 ± 0.38 mL, respectively.Conclusion: The results show that IO is a promising candidate for further development as analgesic and anti-inflammatory agents. However, their pharmacokinetic and pharmacodynamic profiles need to be investigated. Keywords: Computational, Stevioside, Docking, Analgesic, Anti-inflammatory

Reducing effect of the Chinese medicinal herb, Salvia miltiorrhiza, on alcohol self-administration in Sardinian alcohol-preferring rats

Alcohol ◽  
2014 ◽  
Vol 48 (6) ◽  
pp. 587-593 ◽  
Author(s):  
Paola Maccioni ◽  
Daniela Vargiolu ◽  
Maura Falchi ◽  
Paolo Morazzoni ◽  
Antonella Riva ◽  
...  
Keyword(s):  
Salvia Miltiorrhiza ◽  
Medicinal Herb ◽  
Self Administration ◽  
Chinese Medicinal Herb

Interactions of gallic acid, resveratrol, quercetin and aspirin at the platelet cyclooxygenase-1 level Functional and modelling studies

2009 ◽  
Vol 102 (08) ◽  
pp. 336-346 ◽  
Author(s):  
Marilena Crescente ◽  
Gisela Jessen ◽  
Stefania Momi ◽  
Hans-Dieter Höltje ◽  
Paolo Gresele ◽  
...  
Keyword(s):  
Salicylic Acid ◽  
Platelet Aggregation ◽  
Gallic Acid ◽  
Molecular Modelling ◽  
In Silico Docking ◽  
Cyclooxygenase 1 ◽  
Modelling Studies ◽  
Cox 1

SummaryWhile resveratrol and quercetin possess antiplatelet activity, little is known on the effect of gallic acid on platelets.We studied the interactions of these three different polyphenols among themselves and with aspirin, at the level of platelet cyclooxygenase-1 (COX-1). Both functional (in vitro and in vivo) and molecular modelling approaches were used. All three polyphenols showed comparable antioxidant activity (arachidonic acid [AA]-induced intraplatelet ROS production); however, resveratrol and quercetin, but not gallic acid, inhibited AA-induced platelet aggregation. Gallic acid, similarly to salicylic acid, the major aspirin metabolite, prevented inhibition of AA-induced platelet function by aspirin but, at variance with salicylic acid, also prevented inhibition by the other two polyphenols. Molecular modelling studies, performed by in silico docking the polyphenols into the crystal structure of COX-1, suggested that all compounds form stable complexes into the COX-1 channel, with slightly different but functionally relevant interaction geometries. Experiments in mice showed that gallic acid administered before aspirin, resveratrol or quercetin fully prevented their inhibitory effect on serum TxB2. Finally, a mixture of resveratrol, quercetin and gallic acid, at relative concentrations similar to those contained in most red wines, did not inhibit platelet aggregation, but potentiated sub-inhibitory concentrations of aspirin. Gallic acid interactions with other polyphenols or aspirin at the level of platelet COX-1 might partly explain the complex,and possibly contrasting, effects of wine and other components of the Mediterranean diet on platelets and on the pharmacologic effect of lowdose aspirin.

scholarly journals Differential expression of cyclooxygenase 1 and cyclooxygenase 2 in the bovine oviduct

2006 ◽  
Vol 191 (1) ◽  
pp. 263-274 ◽  
Author(s):  
Simone Odau ◽  
Christoph Gabler ◽  
Christoph Holder ◽  
Ralf Einspanier
Keyword(s):  
Mrna Expression ◽  
Estrous Cycle ◽  
Luteal Phase ◽  
Cellular Level ◽  
Differential Distribution ◽  
Cyclooxygenase 1 ◽  
Epithelial Cell Layer ◽  
Cox 2 ◽  
Cycle Dependent ◽  
Cox 1

The aim of the present study was to investigate the enzymes for the local prostaglandin (PG) biosynthesis present in the bovine oviduct during the estrous cycle to influence early reproductive events. Bovine oviducts were classified into four phases: pre-ovulatory, post-ovulatory, early-to-mid luteal, and late luteal phase, subdivided further into ipsi- or contralateral site and separated into ampulla or isthmus. Oviductal cells were gained by flushing the oviductal regions. Quantitative real-time reverse transcriptase-PCR was performed for the secretory and cytosolic phospholipases A2 (sPLA2IB, cPLA2α, and cPLA2β) and cyclooxygenases (COX-1 and COX-2) as the first step enzymes of PG synthesis. COX-1 and cPLA2β showed significant highest mRNA expression around and before ovulation compared with the luteal phase respectively. sPLA2IB and cPLA2α mRNA expression was unregulated during the estrous cycle. Regional differences in mRNA content were found for sPLA2IB with higher mRNA expression in the ampulla than in the isthmus. Western blot analysis revealed the highest COX-1 protein content in the early-to-mid luteal phase. Immunohistochemistry demonstrated that COX-1 was localized in epithelial and smooth muscle cells, whereas COX-2 was only localized in epithelial cells. COX-2 showed a differential distribution within the epithelial cell layer suggesting a regulation on a cellular level, although the COX-2 mRNA and protein amounts did not vary throughout the estrous cycle. A COX activity assay of oviductal cells revealed that COX activity originated predominantly from COX-1 than from COX-2. Treatment of primary oviductal cells with 10 pg/ml 17β-estradiol or 10 ng/ml progesterone resulted in a higher expression of COX-2 and cPLA2α, but not of the other enzymes. The expression pattern of these enzymes suggests that an estrous-cycle dependent and region-specific PG synthesis in the bovine oviduct may be required for a successful reproduction.

The C50T polymorphism of the cyclooxygenase-1 gene and the risk of thrombotic events during low-dose therapy with acetyl salicylic acid

2008 ◽  
Vol 100 (07) ◽  
pp. 70-75 ◽  
Author(s):  
Martijn G. H. van Oijen ◽  
Santosh Sundaresan ◽  
Marc A. Brouwer ◽  
Rene H. M. te Morsche ◽  
Wessel Keuper ◽  
...  
Keyword(s):  
Myocardial Infarction ◽  
Platelet Aggregation ◽  
Primary Endpoint ◽  
Low Dose ◽  
Cardiovascular Death ◽  
Hazard Ratio ◽  
Cyclooxygenase 1 ◽  
Thromboxane Production ◽  
The Common ◽  
Cox 1

SummaryAspirin prevents thrombotic events by inhibiting platelet cyclooxygenase-1 (COX-1), thus reducing thromboxane A2 formation and platelet aggregation. The C50T polymorphism of COX-1 is associated with an impaired inhibition of both thromboxane production and in-vitro platelet aggregation by aspirin. We studied whether this polymorphism is also associated with the risk of clinical thrombotic events in patients using aspirin. We included 496 patients admitted to our Coronary Care Unit for various indications treated with aspirin 80 mg daily. Genotyping for the C50T polymorphism demonstrated that 86.7% of the patients had the common genotype, and 13.3% had the variant (12.5% heterozygous, 0.8% homozygous). Baseline variables were well balanced, except that patients with the common genotype more frequently used aspirin prior to admission compared to those patients with the variant genotype. The composite primary endpoint of myocardial infarction, stroke, and/or cardiovascular death occurred in 98 patients (19.8%). Myocardial infarction occurred in 9.6% of patients, stroke in 1.6%, and cardiovascular death in 12.1%.The unadjusted hazard ratio (95% CI) for the primary endpoint for patients with the variant versus the common genotype was 1.07 (0.62–1.85), p=0.8.The adjusted hazard ratio was 0.86 (0.49–1.50), p=0.6. In prior laboratory studies the COX-1 C50T polymorphism was associated with an impaired inhibitory effect of aspirin on thromboxane production and platelet function. However, in this cohort of patients using low-dose aspirin for secondary prevention the polymorphism was not associated with a higher risk of atherothrombotic events.

scholarly journals Synthesis of Novel Curcumin Analogues and Their Evaluation as Selective Cyclooxygenase-1 (COX-1) Inhibitors

2007 ◽  
Vol 55 (1) ◽  
pp. 64-71 ◽  
Author(s):  
Norbert Handler ◽  
Walter Jaeger ◽  
Helmut Puschacher ◽  
Klaus Leisser ◽  
Thomas Erker
Keyword(s):  
Curcumin Analogues ◽  
Cyclooxygenase 1 ◽  
Cox 1

scholarly journals Meloxicam in pain syndrome treatment of comorbid diseases patients

2021 ◽  
pp. 209-215
Author(s):  
O. A. Shavlovskaya ◽  
I. A. Bokova ◽  
N. I. Shavlovskiy
Keyword(s):  
Gastrointestinal Tract ◽  
Pain Syndrome ◽  
Cardiovascular Risks ◽  
Lower Back ◽  
Cyclooxygenase 1 ◽  
Inflammatory Drugs ◽  
Cox 2 ◽  
Comorbid Diseases ◽  
Per Oral ◽  
Cox 1

The issue nonsteroidal anti-inflammatory drugs (NSAIDs) use safety is associated with a high frequency of adverse events (AEs) from the gastrointestinal tract and cardiovascular risks. Patients with lower back pain (LBP) and osteoarthritis (OA), as a rule, have comorbid diseases, such as arterial hypertension (AH), coronary heart disease (CHD), gastrointestinal tract (GIT) diseases, which significantly complicates the appointment of NSAIDs. The main guideline in NSAIDs appointment is the selective ability to inhibit cyclooxygenase-1 and -2 (COX). The ratio of the activity of NSAIDs when blocking COX-1/COX-2 allows us to judge their potential toxicity. And, then higher the selectivity of NSAIDs, then lower its toxicity. For example, the ratio of COX-1/COX-2 in meloxicam is 0.33, diclofenac – 2.2, tenoxicam – 15, piroxicam – 33, indomethacin – 107. To the predominantly selective COX-2 NSAIDs include meloxicam, which has little effect on the GIT, the lowest relative risk (RR) of complications from the cardiovascular system (CVS). The therapeutic efficacy of meloxicam is comparable to piroxicam and diclofenac. A number of studies have shown the high efficacy of meloxicam, both with per oral (p/o) administration (7.5–15 mg/d), and with intramuscular (i/m) administration (1.5 ml), and when injected into trigger zones. Both with p/o and the injectable form of meloxicam has minimal GIT AEs and absence local reaction in the injection area. The drug can be recommended both as a combination therapy and prescribed in monotherapy.

Sign in / Sign up

Export Citation Format

Share Document