Investigation of myorelaxant activity of 9-aryl-3,4,6,7-tetrahydroacridine-1,8-(2H,5H,9H,10H)-diones in isolated rabbit gastric fundus

Fincan, Gökçe Sevim Öztürk; Gündüz, Miyase Gözde; Vural, Ismail Mert; Şimşek, Rahime; Sarıoğlu, Yusuf; Şafak, Cihat

doi:10.1007/s00044-011-9698-x

Cited by 8 publications

(4 citation statements)

References 39 publications

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“…Confirming unaltered transporter expression, challenges with glucose, glutamine and alanyl-glutamine substrates showed similar pEC 50 values between groups. Although the maximum response induced by glucose was different between undernourished and nourished groups, the pEC 50 is the best measure of receptor/agonist affinity and its potency ( 33 , 34 ). These data suggest a complete responsiveness of the intestinal absorption ability of the undernourished ileum.…”

Section: Discussionmentioning

confidence: 98%

Impact of acute undernutrition on growth, ileal morphology and nutrient transport in a murine model

Sampaio

Medeiros

Rodrigues

et al. 2016

Braz J Med Biol Res

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Undernutrition represents a major public health challenge for middle- and low-income countries. This study aimed to evaluate whether a multideficient Northeast Brazil regional basic diet (RBD) induces acute morphological and functional changes in the ileum of mice. Swiss mice (∼25 g) were allocated into two groups: i) control mice were fed a standard diet and II) undernourished mice were fed the RBD. After 7 days, mice were killed and the ileum collected for evaluation of electrophysiological parameters (Ussing chambers), transcription (RT-qPCR) and protein expression (western blotting) of intestinal transporters and tight junctions. Body weight gain was significantly decreased in the undernourished group, which also showed decreased crypt depth but no alterations in villus height. Electrophysiology measurements showed a reduced basal short circuit current (I sc) in the undernourished group, with no differences in transepithelial resistance. Specific substrate-evoked I sc related to affinity and efficacy (glutamine and alanyl-glutamine) were not different between groups, except for the maximum I sc (efficacy) induced by glucose. Transcription of Sglt1 and Pept1 was significantly higher in the undernourished group, while SN-2 transcription was decreased. No changes were found in transcription of CAT-1 and CFTR, while claudin-2 and occludin transcriptions were significantly increased in the undernourished group. Despite mRNA changes, SGLT-1, PEPT-1, claudin-2 and occludin protein expression showed no difference between groups. These results demonstrate early effects of the RBD on mice, which include reduced body weight and crypt depth in the absence of significant alterations to villus morphology, intestinal transporters and tight junction expression.

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Section: Discussionmentioning

confidence: 98%

Impact of acute undernutrition on growth, ileal morphology and nutrient transport in a murine model

Sampaio

Medeiros

Rodrigues

et al. 2016

Braz J Med Biol Res

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“…In vitro cell inhibition study for metastatic breast cancer (MDA‐MB231) and human chronic myeloid leukemia (K562) cells displayed good activity against control cell, HEK 293 [Scheme 35, Method 3]. Fincan and his coauthors [199] developed 9‐aryl‐3,4,6,7‐tetrahydroacridine‐1,8‐(2H,5H,9H,10H)‐diones through benzaldehyde, NH 4 OAc, dimedone in EtOH and demonstrated their myorelaxant activity. Among all the synthesized ones, most of the molecules displayed maximum relaxant effects (E max ) and good pD2 values against pinacidil and showed concentration‐dependent relaxation in rabbit gastric fundus smooth muscle strips [Scheme 35, Method 4].…”

Section: Biological Activity Of Acridinedione Derivativesmentioning

confidence: 99%

“…In vitro cell inhibition study for metastatic breast cancer (MDA-MB231) and human chronic myeloid leukemia (K562) cells displayed good activity against control cell, HEK 293 [Scheme 35, Method 3]. Fincan and his coauthors [199] Kaya and coauthors [200] reported p-dodesilbenzensulphonic acid (DBSA) catalyzed synthesis of dioxoacridine sulfonamide derivatives and screened for in vitro inhibition of human carbonic anhydrase isoenzymes (hCA I and hCA II). Compounds having methoxy and hydroxyl group displayed highest inhibition potency as compared to reference drug [Scheme 35, Method 5].…”

Section: Biological Activity Of Acridinedione Derivativesmentioning

confidence: 99%

Acridine‐1,8‐diones: Synthesis and Biological Applications

Sahiba¹,

Sethiya²,

Soni³

et al. 2021

ChemistrySelect

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The unpretentious features of acridine‐1,8‐diones viz. presence of N‐heteroatom, electronic behavior, acridine ring skeleton and wide possibilities of diversified substitution, bichromophoric structure and interaction ability with various proteins, make them an interesting scaffold of heterocyclic, medicinal and industrial chemistry. A tremendous development in the field of acridinediones in terms of synthetic strategies, bioactivity, industrial and other applicability has been explored in past four decades. In this perspective, an overview has been given on the state‐of‐art discoveries for the synthesis and biological applications of acridine‐1,8‐diones from 1980 to 2020. The study highlighted the history, chemistry and properties of these derivatives and provided deep insights into the synthetic protocols using various catalysts and techniques like nano‐catalyst, ionic‐liquids, microwave, ultrasound etc. under varied conditions along with biological activity against many lethal diseases. Finally, the respective prospects and limitations to these systems have been addressed. Furthermore, attempts have been done to bring many outstanding researches together and express the significance of acridine‐1,8‐diones through several aspects. We hope that the article shall deliver an impetus to explore further the synthetic values and mechanistic puzzles of acridinedione moiety and to design more promising hybrid multi‐targeted drugs and other industrial composites for the goodness of humanity

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“…Within the final few decades, investigation has been made for the advancement of modern techniques for their synthesis due to extraordinary organic significance of acridines . Acridine and fused acridine analogues have been associated with several biological activities such as anthelmintic, antiherpes, antidiabetic, antinociceptive, Myorelaxant activity etc., Drugs like Aminacrine, Amsacrine, Chlomacran, Dimetacrine, Nitracrine, Proflavine, Velnacrine, and Quinacrine contains acridine analog as core structure were used to treat various diseases (Figure. 1).…”

Section: Introductionmentioning

confidence: 99%

Microwave‐Assisted Synthesis of Positional Isomeric Dihydro‐triazolo‐pyrimido‐acridines and Biological studies

et al. 2020

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Microwave synthetic methodologies were proposed for the preparation of positional isomeric dihydro‐triazolo‐pyrimido‐acridines, 3 a‐j and 9 a‐h via friedlander synthesis using response surface methodology (RSM). The advantages of these methodologies over conventional methods are it provides good yields with short reaction times. Free radical scavenging and antifungal studies were performed for compounds 3 a‐j and 9 a‐h. The results of antioxidant assay revealed that compounds 3 c, 3 d and 9 b exhibited excellent property whereas compounds 3 a and 9 a showed significant antifungal property against Aspergillus flavus (A.flavus) and Aspergillus niger (A. niger).

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Investigation of myorelaxant activity of 9-aryl-3,4,6,7-tetrahydroacridine-1,8-(2H,5H,9H,10H)-diones in isolated rabbit gastric fundus

Cited by 8 publications

References 39 publications

Impact of acute undernutrition on growth, ileal morphology and nutrient transport in a murine model

Impact of acute undernutrition on growth, ileal morphology and nutrient transport in a murine model

Acridine‐1,8‐diones: Synthesis and Biological Applications

Microwave‐Assisted Synthesis of Positional Isomeric Dihydro‐triazolo‐pyrimido‐acridines and Biological studies

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